Identification

Name
Midazolam
Accession Number
DB00683  (APRD00680)
Type
Small Molecule
Groups
Approved, Illicit
Description

A short-acting hypnotic-sedative drug with anxiolytic and amnestic properties. It is used in dentistry, cardiac surgery, endoscopic procedures, as preanesthetic medication, and as an adjunct to local anesthesia. The short duration and cardiorespiratory stability makes it useful in poor-risk, elderly, and cardiac patients. It is water-soluble at pH less than 4 and lipid-soluble at physiological pH. [PubChem] Midazolam is a schedule IV drug in the United States.

Structure
Thumb
Synonyms
  • Buccolam
  • Dormicum
  • Midazolam
  • Midazolamum
External IDs
Dea No. 2884 / Ro 21-3981/001 / Ro 21-3981/003
Product Ingredients
IngredientUNIICASInChI Key
Midazolam HydrochlorideW7TTW573JJ59467-96-8PLYSCVSCYOQVRP-UHFFFAOYSA-N
Midazolam maleate77520S18SE59467-94-6XYGVIBXOJOOCFR-BTJKTKAUSA-N
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
BuccolamSolution5 mgBuccalShire Services Bvba2011-09-05Not applicableEu
BuccolamSolution10 mgBuccalShire Services Bvba2011-09-05Not applicableEu
BuccolamSolution2.5 mgBuccalShire Services Bvba2011-09-05Not applicableEu
BuccolamSolution7.5 mgBuccalShire Services Bvba2011-09-05Not applicableEu
Midazolam InjectionSolution1 mgIntramuscular; IntravenousSandoz Canada Incorporated1999-07-21Not applicableCanada
Midazolam InjectionSolution5 mgIntramuscular; IntravenousPfizer2015-03-31Not applicableCanada
Midazolam InjectionSolution1 mgIntramuscular; IntravenousNovopharm Limited2001-12-17Not applicableCanada
Midazolam InjectionLiquid5 mgIntramuscular; IntravenousFresenius Kabi2001-03-26Not applicableCanada
Midazolam InjectionSolution1 mgIntramuscular; IntravenousPfizer2015-03-31Not applicableCanada
Midazolam InjectionSolution5 mgIntramuscular; IntravenousMylan PharmaceuticalsNot applicableNot applicableCanada
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-midazolam Injectable 1 mg/mlLiquid1 mgIntramuscular; IntravenousApotex Corporation2001-04-102013-08-02Canada
Apo-midazolam Injectable 5 mg/mlLiquid5 mgIntramuscular; IntravenousApotex Corporation2001-04-102013-08-02Canada
MidazolamInjection1 mg/mLIntramuscular; IntravenousWest Ward Pharmaceutical2000-06-20Not applicableUs
MidazolamInjection, solution5 mg/mLIntramuscular; IntravenousAthenex Pharmaceutical Division, Llc.2016-12-14Not applicableUs
MidazolamInjection1 mg/mLIntramuscular; IntravenousAkorn2005-05-06Not applicableUs
MidazolamInjection1 mg/mLIntramuscular; IntravenousGeneral Injectables & Vaccines2018-03-05Not applicableUs
MidazolamInjection5 mg/mLIntramuscular; IntravenousWest Ward Pharmaceutical2000-06-20Not applicableUs
MidazolamInjection, solution10 mg/2mLIntramuscular; IntravenousFresenius Kabi2014-10-03Not applicableUs
MidazolamInjection, solution1 mg/mLIntramuscular; IntravenousThe Medicines Company2000-07-14Not applicableUs
MidazolamInjection, solution1 mg/mLIntramuscular; IntravenousThe Medicines Company2000-07-14Not applicableUs
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
Midazolam HClMidazolam Hydrochloride (1 mg/mL)Injection, solutionIntravenousCantrell Drug Company2010-08-02Not applicableUs
Midazolam HClMidazolam Hydrochloride (.5 mg/mL)Injection, solutionIntravenousCantrell Drug Company2013-01-30Not applicableUs
International/Other Brands
Anquil (General Pharma) / Benzosed (Pharmaceutical) / Dalam (Richmond) / Damizol (Specifar) / Demizolam (Dem Ilaç) / Doricum (Roche) / Dormicum (Roche) / Dormid (Scott) / Dormipron (Chalver) / Dormire (Cristália) / Dormitol (Square) / Dormixal (Demo) / Dormonid (Roche) / Drimnorth (Northia) / Epistatus (IFET) / Flormidal (Galenika) / Fulsed (Ranbaxy) / Fulsed Injection (Terapia) / Garen (Bio-Pharma) / Gobbizolam (Gobbi) / Hipnazolam (EMS) / Hipnoz (Pharos) / Hypnofast (Incepta) / Hypnovel (Roche) / Ipnovel (Roche) / Nocturna (Lafi) / Setam (Rimsa) / Talentum (Fisiopharma) / Terap (Sanitas) / Versed (Roche)
Categories
UNII
R60L0SM5BC
CAS number
59467-70-8
Weight
Average: 325.767
Monoisotopic: 325.078203343
Chemical Formula
C18H13ClFN3
InChI Key
DDLIGBOFAVUZHB-UHFFFAOYSA-N
InChI
InChI=1S/C18H13ClFN3/c1-11-21-9-13-10-22-18(14-4-2-3-5-16(14)20)15-8-12(19)6-7-17(15)23(11)13/h2-9H,10H2,1H3
IUPAC Name
12-chloro-9-(2-fluorophenyl)-3-methyl-2,4,8-triazatricyclo[8.4.0.0²,⁶]tetradeca-1(10),3,5,8,11,13-hexaene
SMILES
CC1=NC=C2CN=C(C3=CC=CC=C3F)C3=C(C=CC(Cl)=C3)N12

Pharmacology

Indication

The midazolam injection is indicated for preoperative sedation/anziolysis/amnesia. It is also an agent for sedation/anziolysis/amnesia prior to or during diagnostic, therapeutic, or endoscopic procedures. Midazolam can also be given intravenously for induction of general anaesthesia.

Associated Conditions
Associated Therapies
Pharmacodynamics

Midazolam is a short-acting benzodiazepine central nervous system (CNS) depressant. Pharmacodynamic properties of midazolam and its metabolites, which are similar to those of other benzodiazepines, include sedative, anxiolytic, amnesic and hypnotic activities. Benzodiazepine pharmacologic effects appear to result from reversible interactions with the (gamma)-amino butyric acid (GABA) benzodiazepine receptor in the CNS, the major inhibitory neurotransmitter in the central nervous system. The action of midazolam is readily reversed by the benzodiazepine receptor antagonist, flumazenil.

Mechanism of action

It is thought that the actions of benzodiazepines such as midazolam are mediated through the inhibitory neurotransmitter gamma-aminobutyric acid (GABA), which is one of the major inhibitory neurotransmitters in the brain. Benzodiazepines increase the activity of GABA, thereby producing a calming effect, relaxing skeletal muscles, and inducing sleep. Benzodiazepines bind to the benzodiazepine site on GABA-A receptors, which potentiates the effects of GABA by increasing the frequency of chloride channel opening.

TargetActionsOrganism
AGamma-aminobutyric acid receptor subunit alpha-1
potentiator
Human
AGamma-aminobutyric acid receptor subunit alpha-2
potentiator
Human
AGamma-aminobutyric acid receptor subunit alpha-3
potentiator
Human
AGamma-aminobutyric acid receptor subunit alpha-4
potentiator
Human
AGamma-aminobutyric acid receptor subunit alpha-5
potentiator
Human
AGamma-aminobutyric acid receptor subunit beta-1
potentiator
Human
AGamma-aminobutyric acid receptor subunit beta-3
potentiator
Human
AGamma-aminobutyric acid receptor subunit beta-2
potentiator
Human
AGamma-aminobutyric acid receptor subunit alpha-6
potentiator
Human
AGamma-aminobutyric acid receptor subunit gamma-1
potentiator
Human
AGamma-aminobutyric acid receptor subunit gamma-2
potentiator
Human
AGamma-aminobutyric acid receptor subunit gamma-3
potentiator
Human
AGamma-aminobutyric acid receptor subunit delta
potentiator
Human
AGamma-aminobutyric acid receptor subunit epsilon
potentiator
Human
AGamma-aminobutyric acid receptor subunit pi
potentiator
Human
AGamma-aminobutyric acid receptor subunit rho-1
potentiator
Human
AGamma-aminobutyric acid receptor subunit rho-2
potentiator
Human
AGamma-aminobutyric acid receptor subunit rho-3
potentiator
Human
AGamma-aminobutyric acid receptor subunit theta
potentiator
Human
Absorption

Rapidly absorbed after oral administration. The absolute bioavailability of the midazolam syrup in pediatric patients is about 36%. The absolute bioavailability, if given intramuscularly (IM), is greater than 90%. Cmax, IM = 90 ng/mL; Tmax, IM = 0.5 hours. Following IM administered, Cmax for midazolam and its 1-hydroxy metabolite were approxiately one-half of those achieved after intravenous injection.

Volume of distribution
  • 1.24 to 2.02 L/kg [pediatric patients (6 months to <16 years) receiving 0.15 mg/kg IV midazolam,]
  • 1 to 3.1 L/kg [intravenously administered, healthy adults] Female gender, old age, and obesity may increase the volume of distribution. Midazolam may also cross the placenta and has been detected in human milk and cerebrospinal fluid.
Protein binding

97% protein bound.

Metabolism

Midazolam is primarily metabolized in the liver and gut by human cytochrome P450 IIIA4 (CYP3A4) to its pharmacologic active metabolite, (alpha)-hydroxymidazolam (also known as 1-hydroxy-midazolam), and 4-hydroxymidazolam (makes up 5% or less of the biotransformation products). 1-hydroxy-midazolam is at least as potent as the parent compound and may contributed to the overall activity of midazolam. In vitro studies have demonstrated that the affinities of 1- and 4-hydroxy-midazolam for the benzodiazepine receptor are approximately 20% and 7%, respectively, relative to midazolam. It also undergoes N-glucuronidation via UGT1A4.

Route of elimination

Midazolam is primarily metabolized in the liver and gut by human cytochrome P450 IIIA4 (CYP3A4) to its pharmacologic active metabolite, α-hydroxymidazolam, followed by glucuronidation of the α–hydroxyl metabolite which is present in unconjugated and conjugated forms in human plasma. The α- hydroxymidazolam glucuronide is then excreted in urine. No significant amount of parent drug or metabolites is extractable from urine before beta-glucuronidase and sulfatase deconjugation, indicating that the urinary metabolites are excreted mainly as conjugates. The amount of midazolam excreted unchanged in the urine when given intravenously is less than 0.5%. 45% to 57% of the dose was excreted in the urine as 1-hydroxymethyl midazolam conjugate.

Half life

Intravenous, healthy adults = 1.8 to 6.4 hours (mean of 3 hours)

Clearance
  • 9.3 to 11 mL/min/kg [pediatric patients (6 months to <16 years old)]
  • 0.25 to 0.54 L/hr/kg [intravenous, healthy adults]
Toxicity

LD50=825 mg/kg (Orally in rats). Signs of overdose include sedation, somnolence, confusion, impaired coordination, diminished reflexes, coma, and deleterious effects on vital signs.

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
(1S,6R)-3-{[3-(TRIFLUOROMETHYL)-5,6-DIHYDRO[1,2,4]TRIAZOLO[4,3-A]PYRAZIN-7(8H)-YL]CARBONYL}-6-(2,4,5-TRIFLUOROPHENYL)CYCLOHEX-3-EN-1-AMINEThe serum concentration of Midazolam can be increased when it is combined with (1S,6R)-3-{[3-(TRIFLUOROMETHYL)-5,6-DIHYDRO[1,2,4]TRIAZOLO[4,3-A]PYRAZIN-7(8H)-YL]CARBONYL}-6-(2,4,5-TRIFLUOROPHENYL)CYCLOHEX-3-EN-1-AMINE.Experimental
1,10-PhenanthrolineThe serum concentration of Midazolam can be increased when it is combined with 1,10-Phenanthroline.Experimental
3,4-DichloroisocoumarinThe serum concentration of Midazolam can be increased when it is combined with 3,4-Dichloroisocoumarin.Experimental
4-(2-Aminoethyl)Benzenesulfonyl FluorideThe serum concentration of Midazolam can be increased when it is combined with 4-(2-Aminoethyl)Benzenesulfonyl Fluoride.Experimental
7-NitroindazoleThe risk or severity of adverse effects can be increased when Midazolam is combined with 7-Nitroindazole.Experimental
AcepromazineThe risk or severity of adverse effects can be increased when Midazolam is combined with Acepromazine.Approved, Vet Approved
AceprometazineThe risk or severity of adverse effects can be increased when Midazolam is combined with Aceprometazine.Approved
Acetyl sulfisoxazoleThe metabolism of Midazolam can be decreased when combined with Acetyl sulfisoxazole.Approved, Vet Approved
AdipiplonThe risk or severity of adverse effects can be increased when Midazolam is combined with Adipiplon.Investigational
AfatinibThe serum concentration of Afatinib can be decreased when it is combined with Midazolam.Approved
AgomelatineThe risk or severity of adverse effects can be increased when Midazolam is combined with Agomelatine.Approved, Investigational
AlaproclateThe risk or severity of adverse effects can be increased when Midazolam is combined with Alaproclate.Experimental
AlfaxaloneThe risk or severity of adverse effects can be increased when Midazolam is combined with Alfaxalone.Vet Approved
AlfentanilThe risk or severity of adverse effects can be increased when Midazolam is combined with Alfentanil.Approved, Illicit
AllopregnanoloneThe risk or severity of adverse effects can be increased when Midazolam is combined with Allopregnanolone.Investigational
AlogliptinThe serum concentration of Midazolam can be increased when it is combined with Alogliptin.Approved
Alpha-1-proteinase inhibitorThe serum concentration of Midazolam can be increased when it is combined with Alpha-1-proteinase inhibitor.Approved
AlphacetylmethadolThe risk or severity of adverse effects can be increased when Midazolam is combined with Alphacetylmethadol.Experimental, Illicit
AlphaprodineThe risk or severity of adverse effects can be increased when Midazolam is combined with Alphaprodine.Illicit
AlprazolamThe risk or severity of adverse effects can be increased when Alprazolam is combined with Midazolam.Approved, Illicit, Investigational
Ambroxol acefyllinateThe therapeutic efficacy of Midazolam can be decreased when used in combination with Ambroxol acefyllinate.Experimental, Investigational
AminophyllineThe therapeutic efficacy of Midazolam can be decreased when used in combination with Aminophylline.Approved
AmiodaroneThe metabolism of Midazolam can be decreased when combined with Amiodarone.Approved, Investigational
AmisulprideThe risk or severity of adverse effects can be increased when Midazolam is combined with Amisulpride.Approved, Investigational
AmitriptylineThe risk or severity of adverse effects can be increased when Midazolam is combined with Amitriptyline.Approved
AmobarbitalThe risk or severity of adverse effects can be increased when Midazolam is combined with Amobarbital.Approved, Illicit
AmoxapineThe risk or severity of adverse effects can be increased when Midazolam is combined with Amoxapine.Approved
AmperozideThe risk or severity of adverse effects can be increased when Midazolam is combined with Amperozide.Experimental
AmprenavirThe serum concentration of Midazolam can be increased when it is combined with Amprenavir.Approved, Investigational
Antithrombin III humanThe serum concentration of Midazolam can be increased when it is combined with Antithrombin III human.Approved
ApalutamideThe serum concentration of Midazolam can be decreased when it is combined with Apalutamide.Approved, Investigational
ApixabanThe serum concentration of Midazolam can be increased when it is combined with Apixaban.Approved
AprepitantThe serum concentration of Midazolam can be increased when it is combined with Aprepitant.Approved, Investigational
AprotininThe serum concentration of Midazolam can be increased when it is combined with Aprotinin.Approved, Investigational, Withdrawn
ArgatrobanThe serum concentration of Midazolam can be increased when it is combined with Argatroban.Approved, Investigational
AripiprazoleThe risk or severity of adverse effects can be increased when Midazolam is combined with Aripiprazole.Approved, Investigational
ArticaineThe risk or severity of adverse effects can be increased when Midazolam is combined with Articaine.Approved
AsenapineThe risk or severity of adverse effects can be increased when Midazolam is combined with Asenapine.Approved
AsunaprevirThe serum concentration of Midazolam can be decreased when it is combined with Asunaprevir.Approved, Investigational, Withdrawn
AtazanavirThe serum concentration of Midazolam can be increased when it is combined with Atazanavir.Approved, Investigational
AtomoxetineThe metabolism of Midazolam can be decreased when combined with Atomoxetine.Approved
AtorvastatinThe serum concentration of Midazolam can be increased when it is combined with Atorvastatin.Approved
AzaperoneThe risk or severity of adverse effects can be increased when Midazolam is combined with Azaperone.Investigational, Vet Approved
AzelastineMidazolam may increase the central nervous system depressant (CNS depressant) activities of Azelastine.Approved
BaclofenThe risk or severity of adverse effects can be increased when Midazolam is combined with Baclofen.Approved
BarbitalThe risk or severity of adverse effects can be increased when Midazolam is combined with Barbital.Illicit
BatimastatThe serum concentration of Midazolam can be increased when it is combined with Batimastat.Experimental
BenazeprilThe serum concentration of Midazolam can be increased when it is combined with Benazepril.Approved, Investigational
BenperidolThe risk or severity of adverse effects can be increased when Midazolam is combined with Benperidol.Approved, Investigational
BenzamidineThe serum concentration of Midazolam can be increased when it is combined with Benzamidine.Experimental
BenzocaineThe risk or severity of adverse effects can be increased when Midazolam is combined with Benzocaine.Approved, Investigational
Benzyl alcoholThe risk or severity of adverse effects can be increased when Midazolam is combined with Benzyl alcohol.Approved
BivalirudinThe serum concentration of Midazolam can be increased when it is combined with Bivalirudin.Approved, Investigational
BoceprevirThe serum concentration of Midazolam can be increased when it is combined with Boceprevir.Approved, Withdrawn
BortezomibThe metabolism of Midazolam can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Midazolam can be decreased when it is combined with Bosentan.Approved, Investigational
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Midazolam.Approved
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be decreased when it is combined with Midazolam.Approved, Investigational
BrexpiprazoleThe risk or severity of adverse effects can be increased when Midazolam is combined with Brexpiprazole.Approved, Investigational
BrigatinibThe serum concentration of Midazolam can be decreased when it is combined with Brigatinib.Approved, Investigational
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Midazolam.Approved
BromazepamThe risk or severity of adverse effects can be increased when Midazolam is combined with Bromazepam.Approved, Illicit, Investigational
BromisovalThe risk or severity of adverse effects can be increased when Midazolam is combined with Bromisoval.Experimental
BromocriptineThe risk or severity of adverse effects can be increased when Bromocriptine is combined with Midazolam.Approved, Investigational
BromperidolThe risk or severity of adverse effects can be increased when Midazolam is combined with Bromperidol.Approved, Investigational
BrompheniramineThe risk or severity of adverse effects can be increased when Midazolam is combined with Brompheniramine.Approved
BrotizolamThe risk or severity of adverse effects can be increased when Midazolam is combined with Brotizolam.Approved, Investigational, Withdrawn
BupivacaineThe risk or severity of adverse effects can be increased when Midazolam is combined with Bupivacaine.Approved, Investigational
BuprenorphineMidazolam may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.Approved, Illicit, Investigational, Vet Approved
BuspironeThe risk or severity of adverse effects can be increased when Buspirone is combined with Midazolam.Approved, Investigational
ButabarbitalThe risk or severity of adverse effects can be increased when Butabarbital is combined with Midazolam.Approved, Illicit
ButacaineThe risk or severity of adverse effects can be increased when Midazolam is combined with Butacaine.Vet Approved
ButalbitalThe risk or severity of adverse effects can be increased when Midazolam is combined with Butalbital.Approved, Illicit
ButambenThe risk or severity of adverse effects can be increased when Midazolam is combined with Butamben.Approved, Withdrawn
ButethalThe risk or severity of adverse effects can be increased when Midazolam is combined with Butethal.Approved, Illicit
ButorphanolThe risk or severity of adverse effects can be increased when Butorphanol is combined with Midazolam.Approved, Illicit, Vet Approved
CabergolineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Midazolam.Approved
CamostatThe serum concentration of Midazolam can be increased when it is combined with Camostat.Experimental
CandoxatrilThe serum concentration of Midazolam can be increased when it is combined with Candoxatril.Experimental
CandoxatrilatThe serum concentration of Midazolam can be increased when it is combined with Candoxatrilat.Experimental
CanertinibThe risk or severity of adverse effects can be increased when Midazolam is combined with Canertinib.Investigational
CaptoprilThe serum concentration of Midazolam can be increased when it is combined with Captopril.Approved
CarbamazepineThe metabolism of Midazolam can be increased when combined with Carbamazepine.Approved, Investigational
CarbinoxamineThe risk or severity of adverse effects can be increased when Midazolam is combined with Carbinoxamine.Approved
CarbomycinThe serum concentration of Midazolam can be increased when it is combined with Carbomycin.Vet Approved
CarfentanilThe risk or severity of adverse effects can be increased when Midazolam is combined with Carfentanil.Illicit, Investigational, Vet Approved
CarisoprodolThe risk or severity of adverse effects can be increased when Midazolam is combined with Carisoprodol.Approved
CeritinibThe serum concentration of Midazolam can be increased when it is combined with Ceritinib.Approved
CerivastatinThe serum concentration of Cerivastatin can be increased when it is combined with Midazolam.Approved, Withdrawn
CetirizineThe risk or severity of adverse effects can be increased when Midazolam is combined with Cetirizine.Approved
Chloral hydrateThe risk or severity of adverse effects can be increased when Midazolam is combined with Chloral hydrate.Approved, Illicit, Investigational, Vet Approved
ChlordiazepoxideThe risk or severity of adverse effects can be increased when Chlordiazepoxide is combined with Midazolam.Approved, Illicit, Investigational
ChlormezanoneThe risk or severity of adverse effects can be increased when Midazolam is combined with Chlormezanone.Approved, Investigational, Withdrawn
ChloroprocaineThe risk or severity of adverse effects can be increased when Midazolam is combined with Chloroprocaine.Approved
ChlorphenamineThe risk or severity of adverse effects can be increased when Midazolam is combined with Chlorphenamine.Approved
ChlorpromazineThe risk or severity of adverse effects can be increased when Chlorpromazine is combined with Midazolam.Approved, Investigational, Vet Approved
ChlorprothixeneThe risk or severity of adverse effects can be increased when Midazolam is combined with Chlorprothixene.Approved, Investigational, Withdrawn
ChlorzoxazoneThe risk or severity of adverse effects can be increased when Midazolam is combined with Chlorzoxazone.Approved
ChymostatinThe serum concentration of Midazolam can be increased when it is combined with Chymostatin.Experimental
CilastatinThe serum concentration of Midazolam can be increased when it is combined with Cilastatin.Approved, Investigational
CilazaprilThe serum concentration of Midazolam can be increased when it is combined with Cilazapril.Approved
CinchocaineThe risk or severity of adverse effects can be increased when Midazolam is combined with Cinchocaine.Approved, Vet Approved
CitalopramThe metabolism of Midazolam can be decreased when combined with Citalopram.Approved
ClarithromycinThe serum concentration of Midazolam can be increased when it is combined with Clarithromycin.Approved
ClemastineThe metabolism of Midazolam can be decreased when combined with Clemastine.Approved, Investigational
ClidiniumThe risk or severity of adverse effects can be increased when Midazolam is combined with Clidinium.Approved
ClobazamThe risk or severity of adverse effects can be increased when Midazolam is combined with Clobazam.Approved, Illicit
clomethiazoleThe risk or severity of adverse effects can be increased when Midazolam is combined with clomethiazole.Investigational
ClomipramineThe risk or severity of adverse effects can be increased when Midazolam is combined with Clomipramine.Approved, Investigational, Vet Approved
ClonazepamThe risk or severity of adverse effects can be increased when Midazolam is combined with Clonazepam.Approved, Illicit
ClonidineThe risk or severity of adverse effects can be increased when Midazolam is combined with Clonidine.Approved
ClopenthixolThe risk or severity of adverse effects can be increased when Midazolam is combined with Clopenthixol.Experimental
ClopidogrelThe metabolism of Midazolam can be decreased when combined with Clopidogrel.Approved
ClorazepateThe risk or severity of adverse effects can be increased when Clorazepate is combined with Midazolam.Approved, Illicit
ClothiapineThe risk or severity of adverse effects can be increased when Midazolam is combined with Clothiapine.Experimental
ClotrimazoleThe metabolism of Midazolam can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineThe risk or severity of adverse effects can be increased when Midazolam is combined with Clozapine.Approved
CobicistatThe serum concentration of Midazolam can be increased when it is combined with Cobicistat.Approved
CocaineThe risk or severity of adverse effects can be increased when Midazolam is combined with Cocaine.Approved, Illicit
CodeineThe risk or severity of adverse effects can be increased when Codeine is combined with Midazolam.Approved, Illicit
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Midazolam.Approved
ConivaptanThe serum concentration of Conivaptan can be increased when it is combined with Midazolam.Approved, Investigational
CrizotinibThe metabolism of Midazolam can be decreased when combined with Crizotinib.Approved
CurcuminThe metabolism of Midazolam can be decreased when combined with Curcumin.Approved, Investigational
CyclizineThe risk or severity of adverse effects can be increased when Midazolam is combined with Cyclizine.Approved
CyclobenzaprineThe risk or severity of adverse effects can be increased when Midazolam is combined with Cyclobenzaprine.Approved
CyclopropaneThe risk or severity of adverse effects can be increased when Midazolam is combined with Cyclopropane.Experimental
CyclosporineThe metabolism of Midazolam can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
CyproheptadineThe risk or severity of adverse effects can be increased when Midazolam is combined with Cyproheptadine.Approved
Dabigatran etexilateThe serum concentration of Dabigatran etexilate can be decreased when it is combined with Midazolam.Approved
DabrafenibThe serum concentration of Midazolam can be decreased when it is combined with Dabrafenib.Approved, Investigational
DantroleneThe risk or severity of adverse effects can be increased when Midazolam is combined with Dantrolene.Approved, Investigational
DapiprazoleThe risk or severity of adverse effects can be increased when Midazolam is combined with Dapiprazole.Approved
DapoxetineThe risk or severity of adverse effects can be increased when Midazolam is combined with Dapoxetine.Investigational
DarexabanThe serum concentration of Midazolam can be increased when it is combined with Darexaban.Investigational
DarunavirThe serum concentration of Midazolam can be increased when it is combined with Darunavir.Approved
DasatinibThe serum concentration of Midazolam can be increased when it is combined with Dasatinib.Approved, Investigational
DeferasiroxThe serum concentration of Midazolam can be decreased when it is combined with Deferasirox.Approved, Investigational
DelanzomibThe serum concentration of Midazolam can be increased when it is combined with Delanzomib.Investigational
DelaprilThe serum concentration of Midazolam can be increased when it is combined with Delapril.Investigational
DelavirdineThe metabolism of Midazolam can be decreased when combined with Delavirdine.Approved
DeramciclaneThe risk or severity of adverse effects can be increased when Midazolam is combined with Deramciclane.Investigational
DesfluraneThe risk or severity of adverse effects can be increased when Midazolam is combined with Desflurane.Approved
DesipramineThe metabolism of Midazolam can be decreased when combined with Desipramine.Approved, Investigational
DesloratadineThe risk or severity of adverse effects can be increased when Midazolam is combined with Desloratadine.Approved, Investigational
DesvenlafaxineThe risk or severity of adverse effects can be increased when Midazolam is combined with Desvenlafaxine.Approved, Investigational
DetomidineThe risk or severity of adverse effects can be increased when Midazolam is combined with Detomidine.Vet Approved
DeutetrabenazineThe risk or severity of sedation and somnolence can be increased when Midazolam is combined with Deutetrabenazine.Approved, Investigational
DexbrompheniramineThe risk or severity of adverse effects can be increased when Midazolam is combined with Dexbrompheniramine.Approved
DexmedetomidineThe risk or severity of adverse effects can be increased when Midazolam is combined with Dexmedetomidine.Approved, Vet Approved
DextromoramideThe risk or severity of adverse effects can be increased when Midazolam is combined with Dextromoramide.Experimental, Illicit
DextropropoxypheneThe risk or severity of adverse effects can be increased when Midazolam is combined with Dextropropoxyphene.Approved, Illicit, Investigational, Withdrawn
DezocineThe risk or severity of adverse effects can be increased when Midazolam is combined with Dezocine.Approved, Investigational
DiazepamThe risk or severity of adverse effects can be increased when Midazolam is combined with Diazepam.Approved, Illicit, Investigational, Vet Approved
Diethyl etherThe risk or severity of adverse effects can be increased when Midazolam is combined with Diethyl ether.Experimental
DifenoxinThe risk or severity of adverse effects can be increased when Midazolam is combined with Difenoxin.Approved, Illicit
DihydrocodeineThe risk or severity of adverse effects can be increased when Midazolam is combined with Dihydrocodeine.Approved, Illicit
DihydroergocornineThe risk or severity of adverse effects can be increased when Dihydroergocornine is combined with Midazolam.Approved
DihydroergocristineThe risk or severity of adverse effects can be increased when Dihydroergocristine is combined with Midazolam.Approved, Experimental
DihydroergocryptineThe risk or severity of adverse effects can be increased when Dihydroergocryptine is combined with Midazolam.Experimental
DihydroergotamineThe risk or severity of adverse effects can be increased when Dihydroergotamine is combined with Midazolam.Approved, Investigational
DihydroetorphineThe risk or severity of adverse effects can be increased when Midazolam is combined with Dihydroetorphine.Experimental, Illicit
DihydromorphineThe risk or severity of adverse effects can be increased when Midazolam is combined with Dihydromorphine.Experimental, Illicit
DiltiazemThe metabolism of Midazolam can be decreased when combined with Diltiazem.Approved, Investigational
DimenhydrinateThe risk or severity of adverse effects can be increased when Midazolam is combined with Dimenhydrinate.Approved
DiphenhydramineThe risk or severity of adverse effects can be increased when Midazolam is combined with Diphenhydramine.Approved, Investigational
DiphenoxylateThe risk or severity of adverse effects can be increased when Midazolam is combined with Diphenoxylate.Approved, Illicit
DixyrazineThe risk or severity of adverse effects can be increased when Midazolam is combined with Dixyrazine.Experimental
DoramectinThe risk or severity of adverse effects can be increased when Midazolam is combined with Doramectin.Vet Approved
DoxepinThe risk or severity of adverse effects can be increased when Midazolam is combined with Doxepin.Approved, Investigational
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Midazolam.Approved, Investigational
DoxorubicinThe metabolism of Midazolam can be decreased when combined with Doxorubicin.Approved, Investigational
DoxycyclineThe metabolism of Midazolam can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Midazolam.Approved, Vet Approved
DPDPEThe risk or severity of adverse effects can be increased when Midazolam is combined with DPDPE.Experimental
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Midazolam.Approved, Illicit
DronedaroneThe metabolism of Midazolam can be decreased when combined with Dronedarone.Approved
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Midazolam.Approved, Vet Approved
DrotebanolThe risk or severity of adverse effects can be increased when Midazolam is combined with Drotebanol.Experimental, Illicit
DuloxetineThe risk or severity of adverse effects can be increased when Midazolam is combined with Duloxetine.Approved
DyclonineThe risk or severity of adverse effects can be increased when Midazolam is combined with Dyclonine.Approved
DyphyllineThe therapeutic efficacy of Midazolam can be decreased when used in combination with Dyphylline.Approved
EcabetThe serum concentration of Midazolam can be increased when it is combined with Ecabet.Approved, Investigational
EcgonineThe risk or severity of adverse effects can be increased when Midazolam is combined with Ecgonine.Experimental, Illicit
EcopipamThe risk or severity of adverse effects can be increased when Midazolam is combined with Ecopipam.Investigational
EdoxabanThe serum concentration of Midazolam can be increased when it is combined with Edoxaban.Approved
EfavirenzThe risk or severity of adverse effects can be increased when Midazolam is combined with Efavirenz.Approved, Investigational
ElafinThe serum concentration of Midazolam can be increased when it is combined with Elafin.Investigational
EltanoloneThe risk or severity of adverse effects can be increased when Midazolam is combined with Eltanolone.Investigational
EnalaprilThe serum concentration of Midazolam can be increased when it is combined with Enalapril.Approved, Vet Approved
EnalaprilatThe serum concentration of Midazolam can be increased when it is combined with Enalaprilat.Approved
EnalkirenThe serum concentration of Midazolam can be increased when it is combined with Enalkiren.Experimental
EnfluraneThe risk or severity of adverse effects can be increased when Midazolam is combined with Enflurane.Approved, Investigational, Vet Approved
EntacaponeThe risk or severity of adverse effects can be increased when Midazolam is combined with Entacapone.Approved, Investigational
EnzalutamideThe serum concentration of Midazolam can be decreased when it is combined with Enzalutamide.Approved
ErgonovineThe risk or severity of adverse effects can be increased when Ergonovine is combined with Midazolam.Approved
ErgotamineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Midazolam.Approved
ErythromycinThe serum concentration of Midazolam can be increased when it is combined with Erythromycin.Approved, Investigational, Vet Approved
EscitalopramThe risk or severity of adverse effects can be increased when Midazolam is combined with Escitalopram.Approved, Investigational
EstazolamThe risk or severity of adverse effects can be increased when Midazolam is combined with Estazolam.Approved, Illicit
EszopicloneThe risk or severity of adverse effects can be increased when Eszopiclone is combined with Midazolam.Approved, Investigational
EthanolMidazolam may increase the central nervous system depressant (CNS depressant) activities of Ethanol.Approved
EthchlorvynolThe risk or severity of adverse effects can be increased when Midazolam is combined with Ethchlorvynol.Approved, Illicit, Withdrawn
EthosuximideThe risk or severity of adverse effects can be increased when Midazolam is combined with Ethosuximide.Approved
EthotoinThe risk or severity of adverse effects can be increased when Midazolam is combined with Ethotoin.Approved
Ethyl carbamateThe risk or severity of adverse effects can be increased when Midazolam is combined with Ethyl carbamate.Withdrawn
Ethyl chlorideThe risk or severity of adverse effects can be increased when Midazolam is combined with Ethyl chloride.Approved, Experimental, Investigational
Ethyl loflazepateThe risk or severity of adverse effects can be increased when Midazolam is combined with Ethyl loflazepate.Approved, Illicit
EthylmorphineThe risk or severity of adverse effects can be increased when Midazolam is combined with Ethylmorphine.Approved, Illicit
EtidocaineThe risk or severity of adverse effects can be increased when Midazolam is combined with Etidocaine.Approved
EtifoxineThe risk or severity of adverse effects can be increased when Midazolam is combined with Etifoxine.Investigational, Withdrawn
EtizolamThe risk or severity of adverse effects can be increased when Midazolam is combined with Etizolam.Approved
EtomidateThe risk or severity of adverse effects can be increased when Midazolam is combined with Etomidate.Approved
EtoperidoneThe risk or severity of adverse effects can be increased when Midazolam is combined with Etoperidone.Withdrawn
EtorphineThe risk or severity of adverse effects can be increased when Midazolam is combined with Etorphine.Illicit, Vet Approved
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Midazolam.Approved
EzogabineThe risk or severity of adverse effects can be increased when Midazolam is combined with Ezogabine.Approved, Investigational
FaldaprevirThe serum concentration of Midazolam can be increased when it is combined with Faldaprevir.Investigational
FelbamateThe risk or severity of adverse effects can be increased when Midazolam is combined with Felbamate.Approved
FencamfamineThe risk or severity of adverse effects can be increased when Midazolam is combined with Fencamfamine.Approved, Illicit, Withdrawn
FentanylThe risk or severity of adverse effects can be increased when Midazolam is combined with Fentanyl.Approved, Illicit, Investigational, Vet Approved
FexofenadineThe risk or severity of adverse effects can be increased when Midazolam is combined with Fexofenadine.Approved, Investigational
FlibanserinThe risk or severity of adverse effects can be increased when Midazolam is combined with Flibanserin.Approved, Investigational
FluanisoneThe risk or severity of adverse effects can be increased when Midazolam is combined with Fluanisone.Experimental
FluconazoleThe metabolism of Midazolam can be decreased when combined with Fluconazole.Approved, Investigational
FludiazepamThe risk or severity of adverse effects can be increased when Midazolam is combined with Fludiazepam.Approved, Illicit
FlunarizineThe risk or severity of adverse effects can be increased when Midazolam is combined with Flunarizine.Approved
FlunitrazepamThe risk or severity of adverse effects can be increased when Midazolam is combined with Flunitrazepam.Approved, Illicit
FluoxetineThe risk or severity of adverse effects can be increased when Midazolam is combined with Fluoxetine.Approved, Vet Approved
FlupentixolThe risk or severity of adverse effects can be increased when Midazolam is combined with Flupentixol.Approved, Investigational, Withdrawn
FluphenazineThe risk or severity of adverse effects can be increased when Fluphenazine is combined with Midazolam.Approved
FlurazepamThe risk or severity of adverse effects can be increased when Midazolam is combined with Flurazepam.Approved, Illicit, Investigational
FluspirileneThe risk or severity of adverse effects can be increased when Midazolam is combined with Fluspirilene.Approved, Investigational
Fluticasone propionateThe risk or severity of adverse effects can be increased when Midazolam is combined with Fluticasone propionate.Approved
FluvastatinThe serum concentration of Fluvastatin can be increased when it is combined with Midazolam.Approved
FluvoxamineThe metabolism of Midazolam can be decreased when combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe serum concentration of Midazolam can be increased when it is combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Midazolam can be increased when it is combined with Fosaprepitant.Approved
FosinoprilThe serum concentration of Midazolam can be increased when it is combined with Fosinopril.Approved
FosphenytoinThe serum concentration of Fosphenytoin can be increased when it is combined with Midazolam.Approved, Investigational
FospropofolThe risk or severity of adverse effects can be increased when Midazolam is combined with Fospropofol.Approved, Illicit, Investigational
Fusidic AcidThe serum concentration of Midazolam can be increased when it is combined with Fusidic Acid.Approved, Investigational
GabapentinThe risk or severity of adverse effects can be increased when Midazolam is combined with Gabapentin.Approved, Investigational
Gabapentin EnacarbilThe risk or severity of adverse effects can be increased when Midazolam is combined with Gabapentin Enacarbil.Approved, Investigational
GabexateThe serum concentration of Midazolam can be increased when it is combined with Gabexate.Investigational
Gamma Hydroxybutyric AcidThe risk or severity of adverse effects can be increased when Midazolam is combined with Gamma Hydroxybutyric Acid.Approved, Illicit, Investigational
GeldanamycinThe serum concentration of Midazolam can be increased when it is combined with Geldanamycin.Experimental, Investigational
GepironeThe risk or severity of adverse effects can be increased when Midazolam is combined with Gepirone.Investigational
Ginkgo bilobaThe serum concentration of Midazolam can be decreased when it is combined with Ginkgo biloba.Approved, Investigational, Nutraceutical
GlutethimideThe risk or severity of adverse effects can be increased when Midazolam is combined with Glutethimide.Approved, Illicit
GM6001The serum concentration of Midazolam can be increased when it is combined with GM6001.Experimental
GuanfacineThe risk or severity of adverse effects can be increased when Midazolam is combined with Guanfacine.Approved, Investigational
HalazepamThe risk or severity of adverse effects can be increased when Midazolam is combined with Halazepam.Approved, Illicit, Withdrawn
HaloperidolThe risk or severity of adverse effects can be increased when Haloperidol is combined with Midazolam.Approved
HalothaneThe risk or severity of adverse effects can be increased when Midazolam is combined with Halothane.Approved, Vet Approved
HeroinThe risk or severity of adverse effects can be increased when Midazolam is combined with Heroin.Approved, Illicit, Investigational
HexobarbitalThe risk or severity of adverse effects can be increased when Midazolam is combined with Hexobarbital.Approved
HyaluronidaseThe therapeutic efficacy of Midazolam can be decreased when used in combination with Hyaluronidase.Approved, Investigational
HydrocodoneMidazolam may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.Approved, Illicit
HydromorphoneThe risk or severity of adverse effects can be increased when Hydromorphone is combined with Midazolam.Approved, Illicit
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Midazolam.Approved
IbrutinibThe serum concentration of Ibrutinib can be increased when it is combined with Midazolam.Approved
IdelalisibThe serum concentration of Midazolam can be increased when it is combined with Idelalisib.Approved
IdraparinuxThe serum concentration of Midazolam can be increased when it is combined with Idraparinux.Investigational
IloperidoneThe risk or severity of adverse effects can be increased when Midazolam is combined with Iloperidone.Approved
ImatinibThe metabolism of Midazolam can be decreased when combined with Imatinib.Approved
ImidaprilThe serum concentration of Midazolam can be increased when it is combined with Imidapril.Investigational
ImipramineThe risk or severity of adverse effects can be increased when Midazolam is combined with Imipramine.Approved
IndalpineThe risk or severity of adverse effects can be increased when Midazolam is combined with Indalpine.Investigational, Withdrawn
IndinavirThe serum concentration of Midazolam can be increased when it is combined with Indinavir.Approved
IndiplonThe risk or severity of adverse effects can be increased when Midazolam is combined with Indiplon.Investigational
IsavuconazoleThe serum concentration of Midazolam can be increased when it is combined with Isavuconazole.Approved, Investigational
IsavuconazoniumThe metabolism of Midazolam can be decreased when combined with Isavuconazonium.Approved, Investigational
IsocarboxazidThe therapeutic efficacy of Midazolam can be increased when used in combination with Isocarboxazid.Approved
IsofluraneThe risk or severity of adverse effects can be increased when Midazolam is combined with Isoflurane.Approved, Vet Approved
IsoflurophateThe serum concentration of Midazolam can be increased when it is combined with Isoflurophate.Approved, Investigational, Withdrawn
IsradipineThe metabolism of Midazolam can be decreased when combined with Isradipine.Approved, Investigational
ItraconazoleThe serum concentration of Midazolam can be increased when it is combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Midazolam can be increased when it is combined with Ivacaftor.Approved
IxazomibThe serum concentration of Midazolam can be increased when it is combined with Ixazomib.Approved, Investigational
JosamycinThe serum concentration of Midazolam can be increased when it is combined with Josamycin.Approved, Investigational
KetamineThe risk or severity of adverse effects can be increased when Midazolam is combined with Ketamine.Approved, Vet Approved
KetazolamThe risk or severity of adverse effects can be increased when Midazolam is combined with Ketazolam.Approved
KetobemidoneThe risk or severity of adverse effects can be increased when Midazolam is combined with Ketobemidone.Approved, Investigational
KetoconazoleThe serum concentration of Midazolam can be increased when it is combined with Ketoconazole.Approved, Investigational
KitasamycinThe serum concentration of Midazolam can be increased when it is combined with Kitasamycin.Experimental
LamotrigineThe risk or severity of adverse effects can be increased when Midazolam is combined with Lamotrigine.Approved, Investigational
LedipasvirThe serum concentration of Ledipasvir can be decreased when it is combined with Midazolam.Approved
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Midazolam.Approved
LepirudinThe serum concentration of Midazolam can be increased when it is combined with Lepirudin.Approved
LetaxabanThe serum concentration of Midazolam can be increased when it is combined with Letaxaban.Investigational
LevetiracetamThe risk or severity of adverse effects can be increased when Midazolam is combined with Levetiracetam.Approved, Investigational
LevobupivacaineThe risk or severity of adverse effects can be increased when Midazolam is combined with Levobupivacaine.Approved, Investigational
LevocabastineThe risk or severity of adverse effects can be increased when Midazolam is combined with Levocabastine.Approved, Investigational
LevocetirizineThe risk or severity of adverse effects can be increased when Midazolam is combined with Levocetirizine.Approved
LevodopaThe risk or severity of adverse effects can be increased when Midazolam is combined with Levodopa.Approved
Levomethadyl AcetateThe risk or severity of adverse effects can be increased when Midazolam is combined with Levomethadyl Acetate.Approved, Investigational
LevomilnacipranThe risk or severity of adverse effects can be increased when Midazolam is combined with Levomilnacipran.Approved, Investigational
LevorphanolThe risk or severity of adverse effects can be increased when Midazolam is combined with Levorphanol.Approved
LidocaineThe risk or severity of adverse effects can be increased when Midazolam is combined with Lidocaine.Approved, Vet Approved
LinagliptinThe serum concentration of Midazolam can be increased when it is combined with Linagliptin.Approved
LisinoprilThe serum concentration of Midazolam can be increased when it is combined with Lisinopril.Approved, Investigational
LisurideThe risk or severity of adverse effects can be increased when Lisuride is combined with Midazolam.Approved, Investigational
Lithium cationThe risk or severity of adverse effects can be increased when Midazolam is combined with Lithium.Experimental
LofentanilThe risk or severity of adverse effects can be increased when Midazolam is combined with Lofentanil.Illicit
LofexidineThe therapeutic efficacy of Midazolam can be increased when used in combination with Lofexidine.Approved, Investigational
LopinavirThe serum concentration of Midazolam can be increased when it is combined with Lopinavir.Approved
LoprazolamThe risk or severity of adverse effects can be increased when Midazolam is combined with Loprazolam.Experimental
LoratadineThe risk or severity of adverse effects can be increased when Midazolam is combined with Loratadine.Approved, Investigational
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Midazolam.Approved
LormetazepamThe risk or severity of adverse effects can be increased when Midazolam is combined with Lormetazepam.Approved
LorpiprazoleThe serum concentration of Midazolam can be increased when it is combined with Lorpiprazole.Approved
LovastatinThe serum concentration of Lovastatin can be increased when it is combined with Midazolam.Approved, Investigational
LoxapineThe risk or severity of adverse effects can be increased when Loxapine is combined with Midazolam.Approved
LuliconazoleThe serum concentration of Midazolam can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of Midazolam can be decreased when it is combined with Lumacaftor.Approved
LurasidoneThe risk or severity of adverse effects can be increased when Midazolam is combined with Lurasidone.Approved, Investigational
Lysergic Acid DiethylamideThe risk or severity of adverse effects can be increased when Lysergic Acid Diethylamide is combined with Midazolam.Illicit, Investigational, Withdrawn
Magnesium sulfateThe therapeutic efficacy of Midazolam can be increased when used in combination with Magnesium sulfate.Approved, Investigational, Vet Approved
MaprotilineThe risk or severity of adverse effects can be increased when Midazolam is combined with Maprotiline.Approved, Investigational
MebicarThe risk or severity of adverse effects can be increased when Midazolam is combined with Mebicar.Experimental
MeclizineThe risk or severity of adverse effects can be increased when Midazolam is combined with Meclizine.Approved
MedazepamThe risk or severity of adverse effects can be increased when Midazolam is combined with Medazepam.Experimental
MedetomidineThe risk or severity of adverse effects can be increased when Midazolam is combined with Medetomidine.Vet Approved
MelagatranThe serum concentration of Midazolam can be increased when it is combined with Melagatran.Experimental
MelatoninThe risk or severity of adverse effects can be increased when Midazolam is combined with Melatonin.Approved, Nutraceutical, Vet Approved
MelperoneThe risk or severity of adverse effects can be increased when Midazolam is combined with Melperone.Approved, Investigational
MepivacaineThe risk or severity of adverse effects can be increased when Midazolam is combined with Mepivacaine.Approved, Vet Approved
MeprobamateThe risk or severity of adverse effects can be increased when Meprobamate is combined with Midazolam.Approved, Illicit
MeptazinolThe risk or severity of adverse effects can be increased when Midazolam is combined with Meptazinol.Experimental
MesoridazineThe risk or severity of adverse effects can be increased when Midazolam is combined with Mesoridazine.Approved, Investigational
MetaxaloneThe risk or severity of adverse effects can be increased when Midazolam is combined with Metaxalone.Approved
MetergolineThe risk or severity of adverse effects can be increased when Metergoline is combined with Midazolam.Experimental
MethadoneMidazolam may increase the central nervous system depressant (CNS depressant) activities of Methadone.Approved
Methadyl AcetateThe risk or severity of adverse effects can be increased when Midazolam is combined with Methadyl Acetate.Approved, Illicit
MethapyrileneThe risk or severity of adverse effects can be increased when Midazolam is combined with Methapyrilene.Withdrawn
MethaqualoneThe risk or severity of adverse effects can be increased when Midazolam is combined with Methaqualone.Illicit, Withdrawn
MethocarbamolThe risk or severity of adverse effects can be increased when Midazolam is combined with Methocarbamol.Approved, Vet Approved
MethohexitalThe risk or severity of adverse effects can be increased when Methohexital is combined with Midazolam.Approved
MethotrimeprazineMidazolam may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.Approved, Investigational
MethoxyfluraneThe risk or severity of adverse effects can be increased when Midazolam is combined with Methoxyflurane.Approved, Investigational, Vet Approved
MethsuximideThe risk or severity of adverse effects can be increased when Midazolam is combined with Methsuximide.Approved
MethylecgonineThe risk or severity of adverse effects can be increased when Midazolam is combined with Methylecgonine.Experimental
MethylergometrineThe risk or severity of adverse effects can be increased when Methylergometrine is combined with Midazolam.Approved
MethylphenobarbitalThe risk or severity of adverse effects can be increased when Midazolam is combined with Methylphenobarbital.Approved
MethysergideThe risk or severity of adverse effects can be increased when Methysergide is combined with Midazolam.Approved
MetyrosineMidazolam may increase the sedative activities of Metyrosine.Approved
MevastatinThe serum concentration of Mevastatin can be increased when it is combined with Midazolam.Experimental
MifepristoneThe serum concentration of Midazolam can be increased when it is combined with Mifepristone.Approved, Investigational
MilnacipranThe risk or severity of adverse effects can be increased when Midazolam is combined with Milnacipran.Approved, Investigational
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Midazolam.Approved, Investigational
MirtazapineMidazolam may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.Approved
MitotaneThe serum concentration of Midazolam can be decreased when it is combined with Mitotane.Approved
MoexiprilThe serum concentration of Midazolam can be increased when it is combined with Moexipril.Approved
MolindoneThe risk or severity of adverse effects can be increased when Midazolam is combined with Molindone.Approved
MorphineThe risk or severity of adverse effects can be increased when Morphine is combined with Midazolam.Approved, Investigational
N-(3-Propylcarbamoyloxirane-2-Carbonyl)-Isoleucyl-ProlineThe serum concentration of Midazolam can be increased when it is combined with N-(3-Propylcarbamoyloxirane-2-Carbonyl)-Isoleucyl-Proline.Experimental
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Midazolam.Approved, Investigational
NafamostatThe serum concentration of Midazolam can be increased when it is combined with Nafamostat.Approved, Investigational
NalbuphineThe risk or severity of adverse effects can be increased when Midazolam is combined with Nalbuphine.Approved
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Midazolam.Approved
NefazodoneThe metabolism of Midazolam can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe serum concentration of Midazolam can be increased when it is combined with Nelfinavir.Approved
NetupitantThe serum concentration of Midazolam can be increased when it is combined with Netupitant.Approved, Investigational
NevirapineThe metabolism of Midazolam can be increased when combined with Nevirapine.Approved
NicergolineThe risk or severity of adverse effects can be increased when Nicergoline is combined with Midazolam.Approved, Investigational
NilotinibThe metabolism of Midazolam can be decreased when combined with Nilotinib.Approved, Investigational
NintedanibThe serum concentration of Nintedanib can be increased when it is combined with Midazolam.Approved
NitrazepamThe risk or severity of adverse effects can be increased when Midazolam is combined with Nitrazepam.Approved
Nitrous oxideThe risk or severity of adverse effects can be increased when Midazolam is combined with Nitrous oxide.Approved, Vet Approved
NordazepamThe risk or severity of adverse effects can be increased when Midazolam is combined with Nordazepam.Approved
NorfluraneThe risk or severity of adverse effects can be increased when Midazolam is combined with Norflurane.Approved, Investigational
NormethadoneThe risk or severity of adverse effects can be increased when Midazolam is combined with Normethadone.Approved, Illicit
NortriptylineThe risk or severity of adverse effects can be increased when Midazolam is combined with Nortriptyline.Approved
OlanzapineThe risk or severity of adverse effects can be increased when Midazolam is combined with Olanzapine.Approved, Investigational
OlaparibThe metabolism of Midazolam can be decreased when combined with Olaparib.Approved
OleandomycinThe serum concentration of Midazolam can be increased when it is combined with Oleandomycin.Vet Approved
OlopatadineThe risk or severity of adverse effects can be increased when Midazolam is combined with Olopatadine.Approved
OmapatrilatThe serum concentration of Midazolam can be increased when it is combined with Omapatrilat.Investigational
OndansetronThe risk or severity of adverse effects can be increased when Midazolam is combined with Ondansetron.Approved
OpiumThe risk or severity of adverse effects can be increased when Midazolam is combined with Opium.Approved, Illicit
OrphenadrineMidazolam may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
OsanetantThe risk or severity of adverse effects can be increased when Midazolam is combined with Osanetant.Investigational
OsimertinibThe serum concentration of Midazolam can be increased when it is combined with Osimertinib.Approved
OtamixabanThe serum concentration of Midazolam can be increased when it is combined with Otamixaban.Investigational
OxazepamThe risk or severity of adverse effects can be increased when Midazolam is combined with Oxazepam.Approved
OxprenololThe risk or severity of adverse effects can be increased when Midazolam is combined with Oxprenolol.Approved
OxybuprocaineThe risk or severity of adverse effects can be increased when Midazolam is combined with Oxybuprocaine.Approved, Investigational
OxycodoneThe risk or severity of adverse effects can be increased when Oxycodone is combined with Midazolam.Approved, Illicit, Investigational
OxymorphoneThe risk or severity of adverse effects can be increased when Midazolam is combined with Oxymorphone.Approved, Investigational, Vet Approved
PalbociclibThe serum concentration of Midazolam can be increased when it is combined with Palbociclib.Approved, Investigational
PaliperidoneThe risk or severity of adverse effects can be increased when Midazolam is combined with Paliperidone.Approved
ParaldehydeMidazolam may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.Approved, Investigational
ParoxetineThe metabolism of Midazolam can be decreased when combined with Paroxetine.Approved, Investigational
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Midazolam.Approved
PenfluridolThe risk or severity of adverse effects can be increased when Midazolam is combined with Penfluridol.Experimental
PentazocineThe risk or severity of adverse effects can be increased when Pentazocine is combined with Midazolam.Approved, Vet Approved
PentobarbitalThe metabolism of Midazolam can be increased when combined with Pentobarbital.Approved, Investigational, Vet Approved
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Midazolam.Approved
PerazineThe risk or severity of adverse effects can be increased when Midazolam is combined with Perazine.Approved, Investigational
PergolideThe risk or severity of adverse effects can be increased when Pergolide is combined with Midazolam.Approved, Investigational, Vet Approved, Withdrawn
PerindoprilThe serum concentration of Midazolam can be increased when it is combined with Perindopril.Approved
PerospironeThe risk or severity of adverse effects can be increased when Midazolam is combined with Perospirone.Approved
PerphenazineThe risk or severity of adverse effects can be increased when Midazolam is combined with Perphenazine.Approved
PethidineThe risk or severity of adverse effects can be increased when Pethidine is combined with Midazolam.Approved
PhenazocineThe risk or severity of adverse effects can be increased when Midazolam is combined with Phenazocine.Experimental
PhenibutThe risk or severity of adverse effects can be increased when Midazolam is combined with Phenibut.Experimental
PhenobarbitalThe metabolism of Midazolam can be increased when combined with Phenobarbital.Approved, Investigational
PhenoperidineThe risk or severity of adverse effects can be increased when Midazolam is combined with Phenoperidine.Experimental
PhenoxyethanolThe risk or severity of adverse effects can be increased when Midazolam is combined with Phenoxyethanol.Approved
PhenytoinThe serum concentration of Phenytoin can be increased when it is combined with Midazolam.Approved, Vet Approved
PhosphoramidonThe serum concentration of Midazolam can be increased when it is combined with Phosphoramidon.Experimental
PimozideThe risk or severity of adverse effects can be increased when Midazolam is combined with Pimozide.Approved
PipamperoneThe risk or severity of adverse effects can be increased when Midazolam is combined with Pipamperone.Approved, Investigational
PipotiazineThe risk or severity of adverse effects can be increased when Midazolam is combined with Pipotiazine.Approved, Investigational
PiritramideThe risk or severity of adverse effects can be increased when Midazolam is combined with Piritramide.Approved, Investigational
PitavastatinThe serum concentration of Pitavastatin can be increased when it is combined with Midazolam.Approved
PitolisantThe serum concentration of Midazolam can be decreased when it is combined with Pitolisant.Approved, Investigational
PizotifenThe risk or severity of adverse effects can be increased when Midazolam is combined with Pizotifen.Approved
PomalidomideThe risk or severity of adverse effects can be increased when Midazolam is combined with Pomalidomide.Approved
PosaconazoleThe metabolism of Midazolam can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
PramipexoleMidazolam may increase the sedative activities of Pramipexole.Approved, Investigational
PramocaineThe risk or severity of adverse effects can be increased when Midazolam is combined with Pramocaine.Approved
PravastatinThe serum concentration of Pravastatin can be increased when it is combined with Midazolam.Approved
PrazepamThe risk or severity of adverse effects can be increased when Midazolam is combined with Prazepam.Approved, Illicit
PregabalinThe therapeutic efficacy of Midazolam can be increased when used in combination with Pregabalin.Approved, Illicit, Investigational
PrilocaineThe risk or severity of adverse effects can be increased when Midazolam is combined with Prilocaine.Approved
PrimidoneThe metabolism of Midazolam can be increased when combined with Primidone.Approved, Vet Approved
PrinomastatThe serum concentration of Midazolam can be increased when it is combined with Prinomastat.Investigational
ProcaineThe risk or severity of adverse effects can be increased when Midazolam is combined with Procaine.Approved, Investigational, Vet Approved
ProchlorperazineThe risk or severity of adverse effects can be increased when Prochlorperazine is combined with Midazolam.Approved, Vet Approved
PromazineThe risk or severity of adverse effects can be increased when Promazine is combined with Midazolam.Approved, Vet Approved
PromethazineThe risk or severity of adverse effects can be increased when Midazolam is combined with Promethazine.Approved, Investigational
PropanididThe risk or severity of adverse effects can be increased when Midazolam is combined with Propanidid.Experimental
ProparacaineThe risk or severity of adverse effects can be increased when Midazolam is combined with Proparacaine.Approved, Vet Approved
PropofolThe serum concentration of Propofol can be increased when it is combined with Midazolam.Approved, Investigational, Vet Approved
PropoxycaineThe risk or severity of adverse effects can be increased when Midazolam is combined with Propoxycaine.Approved
ProtriptylineThe risk or severity of adverse effects can be increased when Midazolam is combined with Protriptyline.Approved
ProxibarbalThe risk or severity of adverse effects can be increased when Midazolam is combined with Proxibarbal.Experimental
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Midazolam.Approved
PSD502The risk or severity of adverse effects can be increased when Midazolam is combined with PSD502.Investigational
QuazepamThe serum concentration of Midazolam can be increased when it is combined with Quazepam.Approved, Illicit
QuetiapineThe risk or severity of adverse effects can be increased when Midazolam is combined with Quetiapine.Approved
QuinaprilThe serum concentration of Midazolam can be increased when it is combined with Quinapril.Approved, Investigational
QuinisocaineThe risk or severity of adverse effects can be increased when Midazolam is combined with Quinisocaine.Experimental
RacecadotrilThe serum concentration of Midazolam can be increased when it is combined with Racecadotril.Investigational
RacloprideThe risk or severity of adverse effects can be increased when Midazolam is combined with Raclopride.Investigational
RamelteonThe risk or severity of adverse effects can be increased when Midazolam is combined with Ramelteon.Approved, Investigational
RamiprilThe serum concentration of Midazolam can be increased when it is combined with Ramipril.Approved
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Midazolam.Approved, Investigational
RemifentanilThe risk or severity of adverse effects can be increased when Midazolam is combined with Remifentanil.Approved
RemikirenThe serum concentration of Midazolam can be increased when it is combined with Remikiren.Approved
RemoxiprideThe risk or severity of adverse effects can be increased when Midazolam is combined with Remoxipride.Approved, Withdrawn
ReserpineThe risk or severity of adverse effects can be increased when Reserpine is combined with Midazolam.Approved, Investigational
RibociclibThe serum concentration of Midazolam can be increased when it is combined with Ribociclib.Approved, Investigational
RifabutinThe metabolism of Midazolam can be increased when combined with Rifabutin.Approved, Investigational
RifampicinThe metabolism of Midazolam can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Midazolam can be increased when combined with Rifapentine.Approved, Investigational
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Midazolam.Approved, Investigational
RilpivirineThe serum concentration of Rilpivirine can be increased when it is combined with Midazolam.Approved
RisperidoneThe risk or severity of adverse effects can be increased when Midazolam is combined with Risperidone.Approved, Investigational
RitanserinThe risk or severity of adverse effects can be increased when Midazolam is combined with Ritanserin.Investigational
RitonavirThe serum concentration of Midazolam can be increased when it is combined with Ritonavir.Approved, Investigational
RivaroxabanThe serum concentration of Midazolam can be increased when it is combined with Rivaroxaban.Approved
RomifidineThe risk or severity of adverse effects can be increased when Midazolam is combined with Romifidine.Vet Approved
RopiniroleMidazolam may increase the sedative activities of Ropinirole.Approved, Investigational
RopivacaineThe risk or severity of adverse effects can be increased when Midazolam is combined with Ropivacaine.Approved
RosuvastatinThe serum concentration of Rosuvastatin can be increased when it is combined with Midazolam.Approved
RotigotineMidazolam may increase the sedative activities of Rotigotine.Approved
RucaparibThe metabolism of Midazolam can be decreased when combined with Rucaparib.Approved, Investigational
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Midazolam.Approved
S-3304The serum concentration of Midazolam can be increased when it is combined with S-3304.Investigational
SaquinavirThe serum concentration of Midazolam can be increased when it is combined with Saquinavir.Approved, Investigational
SarilumabThe therapeutic efficacy of Midazolam can be decreased when used in combination with Sarilumab.Approved, Investigational
SaxagliptinThe serum concentration of Midazolam can be increased when it is combined with Saxagliptin.Approved
ScopolamineThe risk or severity of adverse effects can be increased when Midazolam is combined with Scopolamine.Approved, Investigational
SecobarbitalThe risk or severity of adverse effects can be increased when Secobarbital is combined with Midazolam.Approved, Vet Approved
SepranoloneThe risk or severity of adverse effects can be increased when Midazolam is combined with Sepranolone.Investigational
SertindoleThe risk or severity of adverse effects can be increased when Midazolam is combined with Sertindole.Approved, Investigational, Withdrawn
SertralineThe metabolism of Midazolam can be decreased when combined with Sertraline.Approved
SevofluraneThe risk or severity of adverse effects can be increased when Midazolam is combined with Sevoflurane.Approved, Vet Approved
SildenafilThe metabolism of Midazolam can be decreased when combined with Sildenafil.Approved, Investigational
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Midazolam.Approved
SiltuximabThe serum concentration of Midazolam can be decreased when it is combined with Siltuximab.Approved, Investigational
SimeprevirThe serum concentration of Midazolam can be increased when it is combined with Simeprevir.Approved
SimvastatinThe serum concentration of Simvastatin can be increased when it is combined with Midazolam.Approved
SitagliptinThe serum concentration of Midazolam can be increased when it is combined with Sitagliptin.Approved, Investigational
SivelestatThe serum concentration of Midazolam can be increased when it is combined with Sivelestat.Investigational
Sodium oxybateMidazolam may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.Approved
SofosbuvirThe serum concentration of Sofosbuvir can be decreased when it is combined with Midazolam.Approved
SolithromycinThe serum concentration of Midazolam can be increased when it is combined with Solithromycin.Investigational
SorafenibThe metabolism of Midazolam can be decreased when combined with Sorafenib.Approved, Investigational
SpiraprilThe serum concentration of Midazolam can be increased when it is combined with Spirapril.Approved
St. John's WortThe serum concentration of Midazolam can be decreased when it is combined with St. John's Wort.Approved, Investigational, Nutraceutical
StiripentolThe serum concentration of Midazolam can be increased when it is combined with Stiripentol.Approved
SufentanilThe risk or severity of adverse effects can be increased when Midazolam is combined with Sufentanil.Approved, Investigational
SulfisoxazoleThe metabolism of Midazolam can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
SulpirideThe risk or severity of adverse effects can be increased when Midazolam is combined with Sulpiride.Approved, Investigational
SultoprideThe risk or severity of adverse effects can be increased when Midazolam is combined with Sultopride.Experimental
SuvorexantMidazolam may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.Approved, Investigational
TandospironeThe risk or severity of adverse effects can be increased when Midazolam is combined with Tandospirone.Investigational
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Midazolam.Approved
TasimelteonThe risk or severity of adverse effects can be increased when Midazolam is combined with Tasimelteon.Approved, Investigational
TeduglutideThe serum concentration of Midazolam can be increased when it is combined with Teduglutide.Approved
TelaprevirThe serum concentration of Midazolam can be increased when it is combined with Telaprevir.Approved, Withdrawn
TelithromycinThe serum concentration of Midazolam can be increased when it is combined with Telithromycin.Approved
TemazepamThe risk or severity of adverse effects can be increased when Temazepam is combined with Midazolam.Approved, Investigational
TemocaprilThe serum concentration of Midazolam can be increased when it is combined with Temocapril.Experimental, Investigational
TergurideThe risk or severity of adverse effects can be increased when Terguride is combined with Midazolam.Experimental
TetrabenazineThe risk or severity of adverse effects can be increased when Midazolam is combined with Tetrabenazine.Approved, Investigational
TetracaineThe risk or severity of adverse effects can be increased when Midazolam is combined with Tetracaine.Approved, Vet Approved
TetrahydropalmatineThe risk or severity of adverse effects can be increased when Midazolam is combined with Tetrahydropalmatine.Investigational
TetrodotoxinThe risk or severity of adverse effects can be increased when Midazolam is combined with Tetrodotoxin.Investigational
ThalidomideMidazolam may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.Approved, Investigational, Withdrawn
TheophyllineThe therapeutic efficacy of Midazolam can be decreased when used in combination with Theophylline.Approved
ThiamylalThe risk or severity of adverse effects can be increased when Midazolam is combined with Thiamylal.Approved, Vet Approved
ThiopentalThe risk or severity of adverse effects can be increased when Midazolam is combined with Thiopental.Approved, Vet Approved
ThioridazineThe risk or severity of adverse effects can be increased when Thioridazine is combined with Midazolam.Approved, Withdrawn
ThiorphanThe serum concentration of Midazolam can be increased when it is combined with Thiorphan.Experimental
ThiotepaThe metabolism of Midazolam can be decreased when combined with Thiotepa.Approved, Investigational
ThiothixeneThe risk or severity of adverse effects can be increased when Midazolam is combined with Thiothixene.Approved
TiagabineThe risk or severity of adverse effects can be increased when Midazolam is combined with Tiagabine.Approved, Investigational
TiaprideThe risk or severity of adverse effects can be increased when Midazolam is combined with Tiapride.Approved, Investigational
TiclopidineThe metabolism of Midazolam can be decreased when combined with Ticlopidine.Approved
TiletamineThe risk or severity of adverse effects can be increased when Midazolam is combined with Tiletamine.Vet Approved
TilidineThe risk or severity of adverse effects can be increased when Midazolam is combined with Tilidine.Experimental
TipranavirThe serum concentration of Midazolam can be increased when it is combined with Tipranavir.Approved, Investigational
TizanidineThe risk or severity of adverse effects can be increased when Midazolam is combined with Tizanidine.Approved, Investigational
TocilizumabThe serum concentration of Midazolam can be decreased when it is combined with Tocilizumab.Approved
TolcaponeThe risk or severity of adverse effects can be increased when Midazolam is combined with Tolcapone.Approved, Withdrawn
TolvaptanThe serum concentration of Tolvaptan can be increased when it is combined with Midazolam.Approved
TopiramateThe risk or severity of adverse effects can be increased when Midazolam is combined with Topiramate.Approved
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Midazolam.Approved, Investigational
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with Midazolam.Approved, Investigational
TrandolaprilThe serum concentration of Midazolam can be increased when it is combined with Trandolapril.Approved
TranylcypromineThe risk or severity of adverse effects can be increased when Midazolam is combined with Tranylcypromine.Approved, Investigational
TrazodoneThe risk or severity of adverse effects can be increased when Midazolam is combined with Trazodone.Approved, Investigational
TriazolamThe risk or severity of adverse effects can be increased when Midazolam is combined with Triazolam.Approved, Investigational
Tricaine methanesulfonateThe risk or severity of adverse effects can be increased when Midazolam is combined with Tricaine methanesulfonate.Vet Approved
TrichloroethyleneThe risk or severity of adverse effects can be increased when Midazolam is combined with Trichloroethylene.Approved
TrifluoperazineThe risk or severity of adverse effects can be increased when Midazolam is combined with Trifluoperazine.Approved, Investigational
TrifluperidolThe risk or severity of adverse effects can be increased when Midazolam is combined with Trifluperidol.Experimental
TriflupromazineThe risk or severity of adverse effects can be increased when Midazolam is combined with Triflupromazine.Approved, Vet Approved
TrimipramineThe risk or severity of adverse effects can be increased when Midazolam is combined with Trimipramine.Approved
TriprolidineThe risk or severity of adverse effects can be increased when Midazolam is combined with Triprolidine.Approved
TylosinThe serum concentration of Midazolam can be increased when it is combined with Tylosin.Vet Approved
UbenimexThe serum concentration of Midazolam can be increased when it is combined with Ubenimex.Experimental, Investigational
UlinastatinThe serum concentration of Midazolam can be increased when it is combined with Ulinastatin.Investigational
Valproic AcidThe risk or severity of adverse effects can be increased when Midazolam is combined with Valproic Acid.Approved, Investigational
VemurafenibThe serum concentration of Midazolam can be increased when it is combined with Vemurafenib.Approved
VenlafaxineThe metabolism of Midazolam can be decreased when combined with Venlafaxine.Approved
VeraliprideThe risk or severity of adverse effects can be increased when Midazolam is combined with Veralipride.Experimental
VerapamilThe metabolism of Midazolam can be decreased when combined with Verapamil.Approved
VigabatrinThe risk or severity of adverse effects can be increased when Midazolam is combined with Vigabatrin.Approved
VildagliptinThe serum concentration of Midazolam can be increased when it is combined with Vildagliptin.Approved, Investigational
VincristineThe serum concentration of Vincristine can be decreased when it is combined with Midazolam.Approved, Investigational
Vinyl etherThe risk or severity of adverse effects can be increased when Midazolam is combined with Vinyl ether.Experimental
VoriconazoleThe metabolism of Midazolam can be decreased when combined with Voriconazole.Approved, Investigational
VortioxetineThe risk or severity of adverse effects can be increased when Midazolam is combined with Vortioxetine.Approved, Investigational
XenonThe risk or severity of adverse effects can be increased when Midazolam is combined with Xenon.Experimental
XimelagatranThe serum concentration of Midazolam can be increased when it is combined with Ximelagatran.Approved, Investigational, Withdrawn
XylazineThe risk or severity of adverse effects can be increased when Midazolam is combined with Xylazine.Vet Approved
YohimbineThe therapeutic efficacy of Midazolam can be decreased when used in combination with Yohimbine.Approved, Investigational, Vet Approved
Z-Val-Ala-Asp fluoromethyl ketoneThe serum concentration of Midazolam can be increased when it is combined with Z-Val-Ala-Asp fluoromethyl ketone.Experimental
ZaleplonThe risk or severity of adverse effects can be increased when Midazolam is combined with Zaleplon.Approved, Illicit, Investigational
ZiconotideThe risk or severity of adverse effects can be increased when Midazolam is combined with Ziconotide.Approved
ZimelidineThe risk or severity of adverse effects can be increased when Midazolam is combined with Zimelidine.Withdrawn
ZiprasidoneThe metabolism of Midazolam can be decreased when combined with Ziprasidone.Approved
ZofenoprilThe serum concentration of Midazolam can be increased when it is combined with Zofenopril.Experimental
ZolazepamThe risk or severity of adverse effects can be increased when Midazolam is combined with Zolazepam.Vet Approved
ZolpidemMidazolam may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.Approved
ZonisamideThe risk or severity of adverse effects can be increased when Midazolam is combined with Zonisamide.Approved, Investigational
ZopicloneThe risk or severity of adverse effects can be increased when Midazolam is combined with Zopiclone.Approved
ZotepineThe risk or severity of adverse effects can be increased when Midazolam is combined with Zotepine.Approved, Investigational, Withdrawn
ZuclopenthixolThe risk or severity of adverse effects can be increased when Midazolam is combined with Zuclopenthixol.Approved, Investigational
Food Interactions
  • Grapefruit juice slows the product's absorption and significantly increases its bioavailability.

References

Synthesis Reference

Madhup K. Dhaon, "Process for the preparation of midazolam." U.S. Patent US6262260, issued August, 1979.

US6262260
General References
  1. Skerritt JH, Johnston GA: Enhancement of GABA binding by benzodiazepines and related anxiolytics. Eur J Pharmacol. 1983 May 6;89(3-4):193-8. [PubMed:6135616]
  2. Isojarvi JI, Tokola RA: Benzodiazepines in the treatment of epilepsy in people with intellectual disability. J Intellect Disabil Res. 1998 Dec;42 Suppl 1:80-92. [PubMed:10030438]
  3. Garratt JC, Gent JP, Feely M, Haigh JR: Can benzodiazepines be classified by characterising their anticonvulsant tolerance-inducing potential? Eur J Pharmacol. 1988 Jan 5;145(1):75-80. [PubMed:2894998]
  4. Tokunaga S, Takeda Y, Shinomiya K, Hirase M, Kamei C: Effects of some H1-antagonists on the sleep-wake cycle in sleep-disturbed rats. J Pharmacol Sci. 2007 Feb;103(2):201-6. Epub 2007 Feb 8. [PubMed:17287588]
  5. Vermeeren A: Residual effects of hypnotics: epidemiology and clinical implications. CNS Drugs. 2004;18(5):297-328. [PubMed:15089115]
External Links
Human Metabolome Database
HMDB0014821
KEGG Drug
D00550
KEGG Compound
C07524
PubChem Compound
4192
PubChem Substance
46507611
ChemSpider
4047
BindingDB
21363
ChEBI
6931
ChEMBL
CHEMBL655
Therapeutic Targets Database
DAP000241
PharmGKB
PA450496
IUPHAR
3342
Guide to Pharmacology
GtP Drug Page
HET
08J
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Midazolam
ATC Codes
N05CD08 — Midazolam
AHFS Codes
  • 28:24.08 — Benzodiazepines
PDB Entries
3u5k / 5te8
MSDS
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Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0CompletedPreventionDepression1
0CompletedTreatmentAnxiety Disease1
0CompletedTreatmentBipolar I Disorder / Bipolar II Disorder / Depression, Bipolar / Major Depressive Disorder (MDD) / Suicidal Ideation1
0RecruitingTreatmentCancers / Ketamine / Tiredness1
0RecruitingTreatmentMidazolam Overdose1
0RecruitingTreatmentSedation, Conscious1
1Active Not RecruitingBasic ScienceNash1
1Active Not RecruitingBasic ScienceNeoplasms Metastasis1
1Active Not RecruitingOtherBiological Availability1
1Active Not RecruitingOtherLeukemia, Lymphocytic, Chronic, B-Cell1
1Active Not RecruitingOtherNeoplasms1
1Active Not RecruitingTreatmentAdvanced Non-Central Nervous System (CNS) Malignancies1
1Active Not RecruitingTreatmentCancer of the Ovary / Carcinoid tumour of the gastrointestinal tract / Colorectal Cancers / Head and Neck Carcinoma / Islet Cell Tumor / Lung Cancers / Metastatic Cancers / Neuroendocrine Carcinoma of the Skin / Pheochromocytomas / Sarcomas / Unspecified Adult Solid Tumor, Protocol Specific1
1Active Not RecruitingTreatmentEpidermal Growth Factor Receptor Mutations / Lung Cancer Non-Small Cell Cancer (NSCLC)1
1Active Not RecruitingTreatmentImpaired Renal Function1
1Active Not RecruitingTreatmentMultiple Myeloma (MM)1
1Active Not RecruitingTreatmentNeoplasms1
1Active Not RecruitingTreatmentTumors1
1CompletedNot AvailableHealthy Volunteers10
1CompletedNot AvailableHealthy Volunteers / Pharmacokinetics of ASP015K and Midazolam1
1CompletedNot AvailableHealthy Volunteers / Pharmacokinetics of Isavuconazole / Pharmacokinetics of Midazolam1
1CompletedNot AvailableHepatitis C Viral Infection1
1CompletedNot AvailableHuman Immunodeficiency Virus Infection(HIV)/Acquired Immunodeficiency Syndrome (AIDS)1
1CompletedNot AvailablePain, Chronic1
1CompletedNot AvailablePharmacokinetic Interactions1
1CompletedNot AvailableSchizophrenia Patients1
1CompletedBasic ScienceAlzheimer's Disease (AD) / Metabolism1
1CompletedBasic ScienceAtopic Dermatitis (AD)1
1CompletedBasic ScienceDiabetes Mellitus (DM) / Glucose Metabolism Disorders / Type 2 Diabetes Mellitus1
1CompletedBasic ScienceDrug Biotransformation / Membrane Transport1
1CompletedBasic ScienceDrug Interactions1
1CompletedBasic ScienceEndometriosis1
1CompletedBasic ScienceGenotype-related Drug Metabolism1
1CompletedBasic ScienceHealthy Adult Subjects and Healthy Elderly Subjects1
1CompletedBasic ScienceHealthy Adult Volunteers1
1CompletedBasic ScienceHealthy Male Volunteers1
1CompletedBasic ScienceHealthy Participants1
1CompletedBasic ScienceHealthy Volunteers15
1CompletedBasic ScienceHealthy Volunteers / Human Immunodeficiency Virus (HIV) Infections1
1CompletedBasic ScienceHealthy Volunteers / Pharmacologic Actions1
1CompletedBasic ScienceModerate to Severe Plaque Psoriasis1
1CompletedBasic SciencePharmacokinetic Assessments in Healthy Volunteers1
1CompletedBasic ScienceRheumatoid Arthritis3
1CompletedBasic ScienceType 2 Diabetes Mellitus1
1CompletedBasic ScienceVA Drug Interactions / VA Drug Interactions [VA Drug Interaction]1
1CompletedDiagnosticCytochrome / Pharmacokinetics1
1CompletedDiagnosticDigestive System Disorders1
1CompletedDiagnosticDrug Interactions1
1CompletedDiagnosticHealthy Volunteers2
1CompletedHealth Services ResearchHealthy Volunteers1
1CompletedOtherALK-positive Advanced Tumors1
1CompletedOtherDrug Interactions / Healthy Volunteers1
1CompletedOtherHealthy Volunteers4
1CompletedOtherHealthy Volunteers / Rheumatoid Arthritis1
1CompletedOtherProstatic Neoplasms1
1CompletedOtherTumors, Solid1
1CompletedTreatmentAcute Myocardial Infarction (AMI) / Pain1
1CompletedTreatmentAdult Solid Neoplasm1
1CompletedTreatmentAdvanced Solid Tumors, Excluding Breast Cancer1
1CompletedTreatmentAmnesia-Memory Loss / Memory Losses1
1CompletedTreatmentAnemias / Healthy Volunteers1
1CompletedTreatmentAtherosclerosis1
1CompletedTreatmentBacterial Infections / Pneumonia / Skin Diseases, Infectious1
1CompletedTreatmentCancers1
1CompletedTreatmentCancers / Neoplasms, Breast1
1CompletedTreatmentCarcinoma NOS / Hodgkins Disease (HD) / Lymphoma, Large-Cell, Anaplastic / Neoplasms / Non-Hodgkin's Lymphoma (NHL)1
1CompletedTreatmentCastration Resistant Prostate Cancer (CRPC) / Pharmacokinetics of MDV31001
1CompletedTreatmentChronic Hepatitis C Virus (HCV) Infection1
1CompletedTreatmentCrohn's Disease (CD)1
1CompletedTreatmentDRUG REACTIONS1
1CompletedTreatmentDepressive Disorders / Healthy Volunteers1
1CompletedTreatmentDrug Interaction Potentiation2
1CompletedTreatmentDrug Interactions2
1CompletedTreatmentHealthy Male Volunteers1
1CompletedTreatmentHealthy Volunteers24
1CompletedTreatmentHeart Failure, Unspecified1
1CompletedTreatmentInfectious Diseases1
1CompletedTreatmentInfluenza in Humans1
1CompletedTreatmentJapanese Healthy Adult Males1
1CompletedTreatmentLow Back Pain (LBP)1
1CompletedTreatmentPostmenopausal Osteoporosis (PMO)1
1CompletedTreatmentProphylaxis against postoperative nausea and vomiting / Prophylaxis of acute chemotherapy induced nausea and vomiting1
1CompletedTreatmentPsoriasis2
1CompletedTreatmentRelapsed or Refractory Advanced Cancer1
1CompletedTreatmentSchizophrenia or Schizoaffective Disorder1
1CompletedTreatmentSeizures1
1CompletedTreatmentSkin Diseases, Bacterial1
1CompletedTreatmentTuberculosis1
1CompletedTreatmentTuberculosis / Tuberculosis, Pulmonary1
1CompletedTreatmentTumors, Solid2
1CompletedTreatmentType 2 Diabetes Mellitus2
1CompletedTreatmentCMET-dysregulated Advanced Solid Tumors1
1Not Yet RecruitingOtherCarcinoma, Advanced ALK+ or ROS1+Non-Small-Cell Lung, Neoplasm, Advanced ALK+ or ROS1+Solid Tumors1
1Not Yet RecruitingTreatmentAtopic Dermatitis (AD)1
1Not Yet RecruitingTreatmentDrug Interaction Potentiation1
1Not Yet RecruitingTreatmentHeathy Volunteer1
1RecruitingBasic ScienceHealthy Volunteers1
1RecruitingOtherAdvanced Solid Tumors1
1RecruitingOtherCrohn's Disease (CD)1
1RecruitingOtherDepression, Bipolar / Major Depressive Episode / Unipolar Depression1
1RecruitingOtherDepression / Major Depressive Disorder (MDD) / Recurrent Depressive Disorder / Relapses1
1RecruitingOtherHealthy Volunteers1
1RecruitingOtherInvasive Aspergillosis1
1RecruitingTreatmentAmyotrophic Lateral Sclerosis (ALS)1
1RecruitingTreatmentCancer, Advanced / Colorectal Cancers / Metastatic Melanoma / Metastatic Non-Small Cell Lung Cancer / Metastatic Pancreatic Ductal Adenocarcinoma1
1RecruitingTreatmentCancer, Advanced / Lung Cancer Non-Small Cell Cancer (NSCLC) / Mesothelioma, Malignant / Metastatic Breast Cancer (MBC) / Metastatic Cancers / Non-Hodgkin's Lymphoma (NHL)1
1RecruitingTreatmentDrug Interaction Potential1
1RecruitingTreatmentHealthy Volunteers2
1RecruitingTreatmentHealthy Volunteers / Psoriasis1
1RecruitingTreatmentHepatitis B,Chronic1
1RecruitingTreatmentNon-Hodgkin's Lymphoma (NHL) / Non-Hodgkin's Lymphoma, Solid Cancers / Solid Cancers1
1RecruitingTreatmentTuberculosis / Tuberculosis, Pulmonary1
1RecruitingTreatmentTumors, Solid1
1SuspendedOtherHealthy Volunteers1
1TerminatedBasic ScienceCancer, Advanced1
1TerminatedOtherHealthy Volunteers2
1TerminatedOtherPsoriasis Vulgaris (Plaque Psoriasis)1
1TerminatedTreatmentCervical Pain1
1TerminatedTreatmentEpilepsies1
1TerminatedTreatmentHealthy Volunteers1
1Unknown StatusBasic ScienceHealthy Volunteers1
1WithdrawnTreatmentHealthy Volunteers2
1, 2Active Not RecruitingTreatmentBipolar Disorder (BD) / Major Depressive Episode / Suicidal Ideation1
1, 2CompletedPreventionPost Operative Pain1
1, 2CompletedTreatmentShock, Septic1
1, 2Not Yet RecruitingTreatmentDisseminated Sclerosis / Tiredness1
1, 2RecruitingTreatmentCoughing1
1, 2TerminatedPreventionSepsis1
1, 2TerminatedTreatmentDependence, Cocaine1
1, 2TerminatedTreatmentObsessive Compulsive Disorder (OCD)1
2Active Not RecruitingTreatmentObsessive-Compulsive Disorder (OCD)1
2CompletedSupportive CareChildren1
2CompletedSupportive CareDental Anxiety1
2CompletedTreatmentAnxiety Disorders / Depression / PTSD / Stress Disorders, Post-Traumatic1
2CompletedTreatmentChildren Requiring Sedation to Facilitate Laceration Repair1
2CompletedTreatmentEndoscopy / Procedural Sedation1
2CompletedTreatmentMajor Depressive Disorder (MDD) / Treatment Resistant Depression (TRD)1
2CompletedTreatmentPain1
2CompletedTreatmentSeizures1
2CompletedTreatmentTreatment Resistant Depression (TRD)1
2Not Yet RecruitingPreventionSedation During Spinal Anesthesia1
2Not Yet RecruitingTreatmentKetamine / Violent Aggressive Behavior1
2Not Yet RecruitingTreatmentMajor Depressive Episode1
2RecruitingDiagnosticDelayed Recovery From Anaesthesia1
2RecruitingPreventionForearm Surgeries1
2RecruitingSupportive CareCancer of the Breast / Cancer, Breast / Malignant Neoplasm of Female Breast1
2RecruitingTreatmentAdministration and Dosage of Ketamine / Endoscopic Sedation1
2RecruitingTreatmentBipolar Disorder (BD)1
2RecruitingTreatmentBorderline Personality Disorder (BPD)1
2RecruitingTreatmentMajor Depressive Disorder (MDD)1
2RecruitingTreatmentMajor depressive disorder, recurrent episode1
2RecruitingTreatmentObsessive-Compulsive Disorder (OCD)1
2RecruitingTreatmentPosttraumatic Stress Disorders1
2RecruitingTreatmentSubarachnoid Haemorrhage (SAH)1
2TerminatedTreatmentFeeling Anxious / Pain1
2Unknown StatusPreventionAdenoidectomy / Otorhinolaryngologic Surgical Procedures / Postoperative Care / Postoperative pain / Surgical Procedures, Operative / Tonsillectomy1
2Unknown StatusSupportive CareIntracranial Hemorrhages / Ischemia, Brain / Strokes / Vasospasm, Intracranial1
2Unknown StatusTreatmentPost Dural Puncture Headache1
2WithdrawnDiagnosticComputerized tomography / Procedural Sedation / Traumatic Brain Injury (TBI)1
2WithdrawnSupportive CareDelirium / Dyspnea / Nausea / Pain Intractable1
2, 3CompletedPreventionDiagnostic Esophagogastroduodenoscopy1
2, 3CompletedTreatmentAnaesthesia therapy1
2, 3CompletedTreatmentAnalgesia, Patient-Controlled / Spinal Stenosis1
2, 3CompletedTreatmentChronic Otitis Media1
2, 3CompletedTreatmentColonoscopy / Colorectal Polyps1
2, 3CompletedTreatmentCritical Illness1
2, 3CompletedTreatmentDental Anxiety / Impacted Third Molar Tooth1
2, 3CompletedTreatmentMajor depressive disorder, recurrent episode1
2, 3CompletedTreatmentPostoperative pain1
2, 3CompletedTreatmentSedation therapy1
2, 3Not Yet RecruitingTreatmentAcute Ischemic Stroke (AIS)1
2, 3Not Yet RecruitingTreatmentDepression / Pain, Acute1
2, 3RecruitingTreatmentFeeling Anxious / Postoperative pain / Prophylaxis against postoperative nausea and vomiting1
2, 3RecruitingTreatmentPosttraumatic Stress Disorder (PTSD)1
2, 3WithdrawnTreatmentPTSD1
3CompletedNot AvailableChronic Renal Failure (CRF) / Hip Fractures1
3CompletedDiagnosticCancer, Breast1
3CompletedPreventionHigh Blood Pressure (Hypertension)1
3CompletedPreventionPost-operative Pain for Total Knee Arthroplasty1
3CompletedSupportive CareColonoscopy1
3CompletedSupportive CareEpilepsies / Hydrocephaly1
3CompletedTreatmentAcute Traumatic Pain1
3CompletedTreatmentAnaesthesia therapy1
3CompletedTreatmentBronchoscopy1
3CompletedTreatmentChild's Anxiety / Parental/Caregiver Anxiety1
3CompletedTreatmentColonoscopy1
3CompletedTreatmentContinuous Sedation in Initially Sedated Adults in ICU1
3CompletedTreatmentDental Anxiety1
3CompletedTreatmentFracture Bone1
3CompletedTreatmentPaediatric Outpatient Surgery1
3CompletedTreatmentSedation therapy1
3Not Yet RecruitingTreatmentBreech Presentation1
3RecruitingPreventionEmergence Delirium1
3RecruitingSupportive CareFluoride Poisoning / Hepatic Function / Poisoning by Inhaled Anaesthetic / Recovery From Sedation / Renal Function1
3RecruitingTreatmentFeeling Anxious / Peripheral Nerve Blocks1
3RecruitingTreatmentInflammatory Reaction / Neurocostal neuralgia / Pain, Chronic1
3RecruitingTreatmentInguinal Hernias / Local Anesthesia / Sedation, Conscious1
3RecruitingTreatmentLiver Cirrhosis1
3RecruitingTreatmentSedation in Intensive Care1
3RecruitingTreatmentTreatment Resistant Depressive Disorder1
3TerminatedTreatmentAcute Agitated Patients1
3TerminatedTreatmentAnxiety Disorders / Dementias / Depression / Psychosomatic Disorders / Schizophrenic Disorders1
3TerminatedTreatmentEpilepsies1
3TerminatedTreatmentTraumatic Brain Injury (TBI)1
3Unknown StatusSupportive CareSedation therapy1
3Unknown StatusTreatmentIntubation Complications1
4Active Not RecruitingSupportive CareEpilepsies / Metabolic Diseases / Traumas1
4Active Not RecruitingSupportive CareFeeling Anxious / Laceration1
4Active Not RecruitingTreatmentAcute Lung Injury (ALI) / Acute Respiratory Distress Syndrome (ARDS) / Critical Illness / Sleep1
4Active Not RecruitingTreatmentDriving Performance After Minor Ambulatory Surgery / Minor Surgical Procedures With Monitored Anesthesia Care1
4CompletedNot AvailableDisorders of Gallbladder, Biliary Tract and Pancrease1
4CompletedNot AvailableFailed Moderate Sedation During Procedure1
4CompletedBasic ScienceAnalgesic Drugs / Antinociceptive Agents1
4CompletedBasic SciencePharmacokinetics1
4CompletedBasic ScienceRejection, Transplant1
4CompletedDiagnosticAlteration of Cognitive Function / Gastrointestinal Dysfunction1
4CompletedPreventionAdenotonsillectomy1
4CompletedPreventionAdrenocortical Deficiency / Hemodynamics Instability1
4CompletedPreventionChronic Diseases1
4CompletedPreventionCognitive Impairments1
4CompletedPreventionDelirium1
4CompletedPreventionDelirium on Emergence / Inhalational Anesthetics Adverse Reaction / Strabismus Following Ocular Surgery1
4CompletedPreventionElective Orthopedic Surgery1
4CompletedPreventionEmergence Agitation1
4CompletedPreventionPatients Undergoing Puncture of the Bone Marrow1
4CompletedPreventionPremedication1
4CompletedSupportive CareAnesthesia; Reaction1
4CompletedSupportive CareEndoscopy1
4CompletedSupportive CareHypothermia1
4CompletedSupportive CareIBS / Malignant Neoplasm of Colon / Polyps1
4CompletedSupportive CareInfertilities1
4CompletedSupportive CareIntubation; Difficult1
4CompletedTreatmentAbscesses / Pain1
4CompletedTreatmentAcute Respiratory Distress Syndrome (ARDS)1
4CompletedTreatmentAggressive Behavior / Depression / Feeling Anxious / Postoperative Period / Tiredness1
4CompletedTreatmentAnaesthesia / Premedication1
4CompletedTreatmentBrain Diseases1
4CompletedTreatmentBronchoscopy1
4CompletedTreatmentCataracts / Phacoemulsification1
4CompletedTreatmentChild Behavior / Conscious Sedation Failure During Procedure / Dental Decay1
4CompletedTreatmentChild Behavior / Dental Decay1
4CompletedTreatmentCholangiocarcinomas / Choledocholithiasis / Malignant Neoplasm of Pancreas / Pancreatitis1
4CompletedTreatmentColonoscopy / Sedation, Conscious1
4CompletedTreatmentComplications1
4CompletedTreatmentConscious Sedation Failure During Procedure1
4CompletedTreatmentCoronary Artery Disease1
4CompletedTreatmentDiagnostic Colonoscopy Screening1
4CompletedTreatmentDrug Safety / Procedural Sedation1
4CompletedTreatmentEarly Childhood Caries1
4CompletedTreatmentEfficacy and Safety of Mivacurium Chloride for Pediatric Patients1
4CompletedTreatmentEndoscopy1
4CompletedTreatmentEndoscopy, Gastrointestinal / Moderate Sedation / Propofol / Target Controlled Infusion (TCI)1
4CompletedTreatmentEndoscopy / Inflammatory Bowel Diseases (IBD) / Sedation therapy1
4CompletedTreatmentEndoscopy / Sedation therapy1
4CompletedTreatmentFailed Moderate Sedation During Procedure1
4CompletedTreatmentFailed Moderate Sedation During Procedure / Minimally Conscious State1
4CompletedTreatmentFeeling Anxious3
4CompletedTreatmentFeeling Anxious / Hepatitis, Chronic / Liver Cirrhosis1
4CompletedTreatmentFeeling Anxious / Laceration1
4CompletedTreatmentFeeling Anxious / Nausea / Pain1
4CompletedTreatmentCaudal epidural block therapy / Forearm Injuries / Orthopedic Procedures / Traumas / Upper Extremity1
4CompletedTreatmentGastrointestinal Stroma Tumors / Lung Cancer Non-Small Cell Cancer (NSCLC) / Renal-cell Cancer1
4CompletedTreatmentHealthy Volunteers / Human Immunodeficiency Virus (HIV) Infections1
4CompletedTreatmentHernia1
4CompletedTreatmentInadequate or Impaired Respiratory Function / Pain1
4CompletedTreatmentIntraoperative Analgesic Use / Postcraniotomy Headache / Postoperative Analgesic Use / Postoperative Complications1
4CompletedTreatmentKetamine Induced Agitation1
4CompletedTreatmentLung Cancers1
4CompletedTreatmentComputerized tomography / MRI of liver / Ultrasound1
4CompletedTreatmentMajor Depressive Disorder (MDD)1
4CompletedTreatmentMajor Depressive Disorder (MDD) / Suicidal Ideation1
4CompletedTreatmentMechanically Ventilated and Intubated Subjects1
4CompletedTreatmentOsteoarthritis (OA)1
4CompletedTreatmentOther Surgical Procedures1
4CompletedTreatmentOxidative Stress / Sedation therapy1
4CompletedTreatmentProcedural Sedation1
4CompletedTreatmentProstate Cancer1
4CompletedTreatmentSedation therapy2
4CompletedTreatmentSedation, Conscious1
4CompletedTreatmentSepsis / Shock, Septic / Systemic Inflammatory Response Syndrome (SIRS)1
4CompletedTreatmentSleep Quality of Patients Undergoing TURP1
4CompletedTreatmentSuicidal Ideation1
4CompletedTreatmentTerminal Cancer1
4Enrolling by InvitationTreatmentAnesthesia Complication / Hemodynamics Instability / Ileus paralytic / Nausea / Postoperative pain / Vomiting1
4Enrolling by InvitationTreatmentComplications / Delirium / Ventilations, Mechanical1
4Not Yet RecruitingNot AvailableChildren / Dormicum / Sedation, Conscious1
4Not Yet RecruitingOtherAnaesthesia therapy1
4Not Yet RecruitingOtherLumbar Punctures / Minor Incision Drainage of Abscesses Not Requiring Extensive Debridement / Sedation, Conscious / Simple Lacerations Less Than 4 cm1
4Not Yet RecruitingPreventionCritical Illness1
4Not Yet RecruitingPreventionInhalation Anesthesia1
4Not Yet RecruitingTreatmentAcute Pulmonary Edema1
4Not Yet RecruitingTreatmentEmergency / Procedural anxiety1
4Not Yet RecruitingTreatmentLaceration of Skin1
4Not Yet RecruitingTreatmentPostoperative pain1
4Not Yet RecruitingTreatmentPreanesthetic Medication1
4Not Yet RecruitingTreatmentSafety and Efficacy of Intranasal Dexmedetomidine1
4RecruitingBasic ScienceSevere Sepsis1
4RecruitingBasic ScienceType 2 Diabetes Mellitus1
4RecruitingDiagnosticCopeptin / Preanesthetic Medication1
4RecruitingDiagnosticLiver Diseases1
4RecruitingHealth Services ResearchGeneral Surgery / Sedation therapy1
4RecruitingTreatmentAcute Agitation, Behavioural Emergency1
4RecruitingTreatmentAnxiety Disorders / Major Depressive Disorder (MDD)1
4RecruitingTreatmentBladder Tumors / Postoperative Cognitive Dysfunction1
4RecruitingTreatmentCritical Illness / Deep Sedation / Ventilators, Mechanical1
4RecruitingTreatmentCrohn's Disease (CD) / Ulcerative Colitis (UC)1
4RecruitingTreatmentDexmedetomidine / Mechanically Ventilated Sedated Patients / Midazolam / Sedation therapy / Ventilations, Mechanical1
4RecruitingTreatmentFeeling Anxious / Pediatric ALL / Procedural anxiety1
4RecruitingTreatmentFlexible Bronchoscopy / Safety / Satisfaction / Sedation therapy1
4RecruitingTreatmentKnee Injuries1
4RecruitingTreatmentSedation in Intensive Care Unit Patients1
4RecruitingTreatmentSedation therapy1
4RecruitingTreatmentSeizures1
4RecruitingTreatmentShock, Septic1
4SuspendedTreatmentPatients Requiring Diagnostic Gastroscopy Suitable for Sedation / Patients Requiring Diagnostic Gastroscopy With Sedation1
4TerminatedTreatmentAnaesthesia therapy1
4TerminatedTreatmentCritical Illness / Ventilations, Mechanical1
4TerminatedTreatmentFeeling Anxious1
4TerminatedTreatmentOrthopedic Procedures / Procedural Sedation / Regional Anesthesia Block1
4TerminatedTreatmentTraumatic Brain Injury (TBI)1
4Unknown StatusNot AvailableObesity, Morbid1
4Unknown StatusBasic ScienceHyperalgesia4
4Unknown StatusPreventionAnaesthetic Preconditioning / Myocardial Injury1
4Unknown StatusPreventionDelirium1
4Unknown StatusPreventionSedative Withdrawal Delirium1
4Unknown StatusTreatmentAnaesthesia therapy / Hemodynamics / Oxidative Stress1
4Unknown StatusTreatmentAnalgesia, Patient-Controlled / Arthroplasty / Gastric Resection1
4Unknown StatusTreatmentCongenital Choledochal Cyst / Congenital Hydronephrosis / Fracture Bone1
4Unknown StatusTreatmentConscious Sedation Failure During Procedure1
4Unknown StatusTreatmentDelirium1
4Unknown StatusTreatmentDexmedetomidine / Mechanically Ventilated Patients / Midazolam / Sedation therapy1
4Unknown StatusTreatmentEmergency1
4Unknown StatusTreatmentFailed Conscious Sedation During Procedure1
4Unknown StatusTreatmentHepatic Encephalopathy1
4Unknown StatusTreatmentInflammatory Disorder of Immune System / Sepsis1
4Unknown StatusTreatmentLaceration1
4Unknown StatusTreatmentLaryngoscopy / Preanesthetic Medication1
4Unknown StatusTreatmentLiver Cirrhosis1
4Unknown StatusTreatmentMechanical Ventilation Complication1
4Unknown StatusTreatmentSafety of Dexmedetomidine Sedation1
4Unknown StatusTreatmentTraumatic Brain Injury (TBI)1
4Unknown StatusTreatmentAdjunct to general anesthesia therapy1
4WithdrawnPreventionC.Surgical Procedure; Cardiac / Delirium1
4WithdrawnSupportive CareAlcoholism / Respiration, Artificial1
4WithdrawnTreatmentPostoperative pain1
4WithdrawnTreatmentSleep1
Not AvailableActive Not RecruitingNot AvailableAAT Deficiency / AATD / Alpha-1 Antitrypsin Deficiency / Fibrosis, Liver1
Not AvailableActive Not RecruitingNot AvailableAortic Valve Stenosis1
Not AvailableActive Not RecruitingNot AvailablePostoperative Cognitive Dysfunction1
Not AvailableActive Not RecruitingTreatmentIntubated Requiring Sedation for Greater Than 48 Hours1
Not AvailableActive Not RecruitingTreatmentPulmonary Diseases1
Not AvailableCompletedNot AvailableAnaesthesia therapy1
Not AvailableCompletedNot AvailableClinical Indications for Transesophageal Echocardiography1
Not AvailableCompletedNot AvailableEarly Gastric Cancer / Gastric Adenoma1
Not AvailableCompletedNot AvailableFeeling Anxious / Satisfaction / Sedation therapy / Tolerance1
Not AvailableCompletedNot AvailablePain1
Not AvailableCompletedNot AvailablePharmacokinetics / Voriconazole1
Not AvailableCompletedNot AvailablePsychomotor Agitation1
Not AvailableCompletedNot AvailableRhytidoplasty1
Not AvailableCompletedBasic ScienceCritical Care / Deep Sedation / Sedation, Conscious1
Not AvailableCompletedBasic ScienceDrug-Drug Interaction (DDI) / Healthy Volunteers1
Not AvailableCompletedBasic ScienceHealthy Volunteers1
Not AvailableCompletedBasic SciencePharmacokinetics1
Not AvailableCompletedBasic ScienceSaccadic Eye Movements1
Not AvailableCompletedDiagnosticConscious Sedation Failure During Procedure1
Not AvailableCompletedDiagnosticEGD Procedure1
Not AvailableCompletedDiagnosticPain1
Not AvailableCompletedDiagnosticSacroiliac Joint Pain / Sympathetically Maintained Pain1
Not AvailableCompletedOtherEndobronchial Ultrasound Guided Transbronchial Needle Aspiration1
Not AvailableCompletedPreventionAkathisia1
Not AvailableCompletedPreventionAnesthesia Morbidity / Children / Delirium on Emergence1
Not AvailableCompletedPreventionGeneral Surgery1
Not AvailableCompletedPreventionGeneral Surgery / Prostate Cancer1
Not AvailableCompletedPreventionPediatric Emergence Agitation and Pain1
Not AvailableCompletedPreventionProphylaxis against postoperative nausea and vomiting1
Not AvailableCompletedPreventionPsychomotor Agitation1
Not AvailableCompletedSupportive CareAnaesthesia therapy / Body Temperature Changes1
Not AvailableCompletedSupportive CareCancers1
Not AvailableCompletedSupportive CareFeeling Anxious1
Not AvailableCompletedSupportive CareFeeling Anxious / Pain1
Not AvailableCompletedSupportive CareLiver Cirrhosis1
Not AvailableCompletedSupportive CarePre Operative Anxiety1
Not AvailableCompletedSupportive CareTransient Hypertension1
Not AvailableCompletedTreatmentAnaesthesia therapy1
Not AvailableCompletedTreatmentAnxiety Preoperative / Midazolam Premedication / Premedication1
Not AvailableCompletedTreatmentBasal Cell Carcinoma (BCC) / Feeling Anxious / Skin Cancers / Squamous Cell Carcinoma (SCC)1
Not AvailableCompletedTreatmentChronic Lung Diseases1
Not AvailableCompletedTreatmentCritical Illness1
Not AvailableCompletedTreatmentEchocardiography, Transesophageal1
Not AvailableCompletedTreatmentEndoscopy / Sedation therapy1
Not AvailableCompletedTreatmentFeeling Anxious1
Not AvailableCompletedTreatmentFeeling Anxious / Pain, Acute1
Not AvailableCompletedTreatmentFractures, Compression1
Not AvailableCompletedTreatmentHemodynamics After Spinal Anesthesia1
Not AvailableCompletedTreatmentIntubations1
Not AvailableCompletedTreatmentOther Surgical Procedures1
Not AvailableCompletedTreatmentPostoperative Cognitive Functions1
Not AvailableCompletedTreatmentPsychomotor Agitation1
Not AvailableCompletedTreatmentRespiration Disorders1
Not AvailableCompletedTreatmentSedation, Bronchoscopy1
Not AvailableCompletedTreatmentSepsis / Shock1
Not AvailableCompletedTreatmentSepsis / Traumas1
Not AvailableCompletedTreatmentStress, Psychological1
Not AvailableEnrolling by InvitationOtherIntestinal Microbiota / Ventilations, Mechanical1
Not AvailableEnrolling by InvitationTreatmentVirtual Reality1
Not AvailableNot Yet RecruitingNot AvailablePostoperative pain1
Not AvailableNot Yet RecruitingBasic ScienceSedation therapy1
Not AvailableNot Yet RecruitingDevice FeasibilitySedation therapy / Spinal Anaesthesia1
Not AvailableNot Yet RecruitingPreventionPeripheral Obliterative Arteriopathy1
Not AvailableNot Yet RecruitingPreventionTonsillitis1
Not AvailableNot Yet RecruitingTreatmentAtherosclerosis / Coronary Artery Disease / Feeling Anxious / Pain, Acute / Vasospasm;Peripheral / Virtual Reality1
Not AvailableNot Yet RecruitingTreatmentBrachial Plexus Block / Shoulder Dislocation1
Not AvailableNot Yet RecruitingTreatmentChildren Under General Anaesthesia1
Not AvailableNot Yet RecruitingTreatmentHypercatabolism / Sedative, Hypnotic, or Anxiolytic Use Disorders1
Not AvailableNot Yet RecruitingTreatmentObesity, Morbid1
Not AvailableRecruitingNot AvailableAcute Bacterial Exacerbation of Chronic Bronchitis (ABECB) / Acute Bacterial Sinusitis (ABS) / Acute Decompensated Heart Failure (ADHF) / Acute Pyelonephritis / Adenovirus / Adjunct to general anesthesia therapy / Adrenal Insufficiency / Airway Swelling / Anaesthesia therapy / Anxiolysis / Arterial Hypotension / Autism, Early Infantile / Autistic Disorder / Bartonellosis / Benzodiazepine Withdrawal / Benzodiazepines / Bipolar Disorder (BD) / Bloodstream Infections / Bone and Joint Infections / Brain Swelling / Bronchospasm / Brucellosis / Cardiac Arrest / Central Nervous System Infections / Cholera / Chronic Bacterial Prostatitis / Community Acquired Pneumonia (CAP) / Complicated Urinary Tract Infections / Convulsions / Cyanide Poisoning / Cytomegalovirus Retinitis / Drug hypersensitivity reaction / Early-onset Schizophrenia Spectrum Disorders / Edema / Epilepsies / Feeling Anxious / Flu caused by Influenza / Gastroparesis / GYNAECOLOGICAL INFECTION / Headaches / Herpes Simplex Virus / High Blood Cholesterol Level / High Blood Pressure (Hypertension) / Hospital-acquired bacterial pneumonia / Hyperlipidemias / Infantile Hemangiomas / Infection NOS / Inflammatory Conditions / Inflammatory Reaction / Influenza Treatment or Prophylaxis / Inhalational Anthrax (Post-Exposure) / Intra-Abdominal Infections / Life-threatening Fungal Infections / Lower Respiratory Tract Infection (LRTI) / Meningitis, Bacterial / Migraines / Muscle Spasms / Nausea / Opioid Addiction / Pain / Plague / Pneumonia / Prophylaxis / Psittacosis / Q Fever / Reflux / Relapsing Fever / Rocky Mountain Spotted Fever / Schizophrenic Disorders / Sedation therapy / Seizures / Sepsis / Skeletal Muscle Spasms / Skin and Subcutaneous Tissue Bacterial Infections / Skin Structures and Soft Tissue Infections / Stable Angina (SA) / Thromboprophylaxis / Thrombosis / Trachoma / Treatment-resistant Schizophrenia / Tularemia / Typhus Fever / Uncomplicated Skin and Skin Structure Infections / Uncomplicated Urinary Tract Infections / Urinary Tract Infections (UTIs) / Vomiting / Withdrawal1
Not AvailableRecruitingNot AvailableAnaesthesia therapy1
Not AvailableRecruitingNot AvailableCerebral Ischemia-Hypoxia1
Not AvailableRecruitingNot AvailableDepression1
Not AvailableRecruitingNot AvailableGliomas1
Not AvailableRecruitingBasic ScienceAmnesia / Anaesthesia therapy / Anesthetics / Pain / Sedation, Conscious1
Not AvailableRecruitingDiagnosticVentricular Tachycardia (VT)1
Not AvailableRecruitingHealth Services ResearchSedation therapy1
Not AvailableRecruitingOtherSedation therapy / Spinal Anaesthesia1
Not AvailableRecruitingPreventionIntubation; Difficult or Failed1
Not AvailableRecruitingTreatmentAcute Respiratory Failure1
Not AvailableRecruitingTreatmentAnoxic Encephalopathy / Cardiac Arrest / Refractory seizure disorders1
Not AvailableRecruitingTreatmentBronchoscopy / Sedation therapy1
Not AvailableRecruitingTreatmentColonoscopy1
Not AvailableRecruitingTreatmentExtrusion of Tooth1
Not AvailableRecruitingTreatmentMajor Depressive Disorder (MDD) / Severe Depression / Treatment Resistant Depression (TRD)1
Not AvailableRecruitingTreatmentPostoperative Pain Control / Wrist Injury1
Not AvailableRecruitingTreatmentTonsillectomy1
Not AvailableSuspendedTreatmentPaediatric Flexible Bronchoscopy1
Not AvailableTerminatedNot AvailableVesicoureteral Reflux1
Not AvailableTerminatedOtherChronic Alcoholism1
Not AvailableTerminatedTreatmentBMI >30 kg/m2 / Sleep Apnea, Obstructive1
Not AvailableTerminatedTreatmentBipolar Disorder (BD)1
Not AvailableTerminatedTreatmentRespiratory Failure1
Not AvailableUnknown StatusNot AvailableFunctional disorders of the biliary tract / Pancreatic Diseases1
Not AvailableUnknown StatusBasic SciencePhobic Disorders1
Not AvailableUnknown StatusPreventionCystoscopy1
Not AvailableUnknown StatusScreeningAnesthesia Recovery Period / Delirium, Dementia, Cognitive Disorders / Mental Competency / Neurobehavioural Manifestation1
Not AvailableUnknown StatusSupportive CareDiverticulosis, Colonic / Malignant Neoplasm of Colon / Rectal Carcinoma1
Not AvailableUnknown StatusSupportive CarePacemaker Implantation / Pain1
Not AvailableUnknown StatusSupportive CareSleeplessness1
Not AvailableUnknown StatusTreatmentAcute Agitation1
Not AvailableUnknown StatusTreatmentAnaesthesia therapy1
Not AvailableUnknown StatusTreatmentBronchoscopy; / Central Airway Stenosis / Interventional; / Noninvasive Positive Pressure Ventilation / Sedation therapy1
Not AvailableUnknown StatusTreatmentLiver Diseases1
Not AvailableWithdrawnNot AvailableTraumas1

Pharmacoeconomics

Manufacturers
  • Apothecon inc div bristol myers squibb
  • App pharmaceuticals llc
  • Astrazeneca pharmaceuticals lp
  • Baxter healthcare corp anesthesia and critical care
  • Baxter healthcare corp anesthesia critical care
  • Bedford laboratories div ben venue laboratories inc
  • Ben venue laboratories inc
  • Claris lifesciences ltd
  • Hospira inc
  • International medicated systems ltd
  • International medication systems ltd
  • Taylor pharmaceuticals
  • Wockhardt ltd
  • Hlr technology
  • Apotex inc richmond hill
  • Hi tech pharmacal co inc
  • Paddock laboratories inc
  • Ranbaxy laboratories ltd
  • Roxane laboratories inc
  • Hoffmann la roche inc
Packagers
  • Akorn Inc.
  • APP Pharmaceuticals
  • A-S Medication Solutions LLC
  • B&B Pharmaceuticals
  • Baxter International Inc.
  • Bedford Labs
  • Ben Venue Laboratories Inc.
  • Cardinal Health
  • Cura Pharmaceutical Co. Inc.
  • Dispensing Solutions
  • Ebewe Pharma
  • Hi Tech Pharmacal Co. Inc.
  • Hospira Inc.
  • Mikart Inc.
  • Novex Pharma
  • Paddock Labs
  • Patheon Inc.
  • Pharmedium
  • Physicians Total Care Inc.
  • Ranbaxy Laboratories
  • Roxane Labs
  • Wockhardt Ltd.
Dosage forms
FormRouteStrength
LiquidIntramuscular; Intravenous1 mg
LiquidIntramuscular; Intravenous5 mg
SolutionBuccal10 mg
SolutionBuccal2.5 mg
SolutionBuccal5 mg
SolutionBuccal7.5 mg
Injection, solutionIntramuscular; Intravenous10 mg/2mL
Injection, solutionIntramuscular; Intravenous2 mg/2mL
Injection, solutionIntravenous.5 mg/mL
Injection, solutionIntravenous1 mg/mL
InjectionIntramuscular; Intravenous1 mg/mL
InjectionIntramuscular; Intravenous10 mg/2mL
InjectionIntramuscular; Intravenous2 mg/2mL
InjectionIntramuscular; Intravenous5 mg/mL
Injection, solutionIntramuscular; Intravenous1 mg/mL
Injection, solutionIntramuscular; Intravenous5 mg/mL
SyrupOral10 mg/5mL
SyrupOral2 mg/mL
SolutionIntramuscular; Intravenous1 mg
SolutionIntramuscular; Intravenous5 mg
Prices
Unit descriptionCostUnit
Midazolam 5 mg/ml3.9USD ml
Midazolam-nacl 2 mg/ml inj2.31USD ml
Midazolam hcl 5 mg/ml vial1.18USD ml
Midazolam-nacl 1 mg/ml inj1.13USD ml
Midazolam hcl 2 mg/ml syrup1.08USD ml
Midazolam 1 mg/ml isecure syr0.73USD ml
Midazolam hcl 1 mg/ml vial0.26USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)159 °CPhysProp
water solubility0.024 mg/mLThorsteinn Loftsson and Dagný Hreinsdóttir, 2006
Predicted Properties
PropertyValueSource
Water Solubility0.00987 mg/mLALOGPS
logP3.89ALOGPS
logP3.33ChemAxon
logS-4.5ALOGPS
pKa (Strongest Basic)6.57ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area30.18 Å2ChemAxon
Rotatable Bond Count1ChemAxon
Refractivity99.43 m3·mol-1ChemAxon
Polarizability32.7 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.9724
Caco-2 permeable+0.8866
P-glycoprotein substrateNon-substrate0.5074
P-glycoprotein inhibitor IInhibitor0.5587
P-glycoprotein inhibitor IIInhibitor0.8388
Renal organic cation transporterInhibitor0.7476
CYP450 2C9 substrateNon-substrate0.7366
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateSubstrate0.7194
CYP450 1A2 substrateInhibitor0.8586
CYP450 2C9 inhibitorInhibitor0.7132
CYP450 2D6 inhibitorNon-inhibitor0.6887
CYP450 2C19 inhibitorInhibitor0.6554
CYP450 3A4 inhibitorNon-inhibitor0.5214
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.9001
Ames testNon AMES toxic0.8024
CarcinogenicityNon-carcinogens0.7703
BiodegradationNot ready biodegradable1.0
Rat acute toxicity3.1488 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9827
hERG inhibition (predictor II)Non-inhibitor0.7379
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Mass Spectrum (Electron Ionization)MSsplash10-03di-3839000000-42781254e15bcd5b31b6
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-004i-0009000000-2411220f611ba30ef225
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-004i-0009000000-c724b297ae99edb399d3
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-004l-0098000000-b57c162c4eeaad9ef111
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-0006-0090000000-a3133528f5491f4c9a6b
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-05fs-0290000000-ee126555f849ecfff795
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-004i-0009000000-4ae622c7b53369b0cfb1
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-004i-0019000000-00c3c9e2813a454acda1
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-002f-0093000000-a8ca99ef6c84536bff07
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0006-0091000000-3edc4aa6f67d99b789a8
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0abd-0290000000-aa5e16437618ad2adb86
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-05fs-0490000000-a323090224c5b01e3990
MS/MS Spectrum - , positiveLC-MS/MSsplash10-004i-0189000000-6e704a4a2a65211394ab
MS/MS Spectrum - , positiveLC-MS/MSsplash10-03di-0910000000-98021a5812f1663e9397

Taxonomy

Description
This compound belongs to the class of organic compounds known as imidazo[1,5-a][1,4]benzodiazepines. These are compounds containing an imidazole ring and a 1,4-benzodiazepine ring system, both sharing one nitrogen atom.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Benzodiazepines
Sub Class
1,4-benzodiazepines
Direct Parent
Imidazo[1,5-a][1,4]benzodiazepines
Alternative Parents
Fluorobenzenes / 1,4-diazepines / N-substituted imidazoles / Aryl fluorides / Aryl chlorides / Heteroaromatic compounds / Ketimines / Propargyl-type 1,3-dipolar organic compounds / Azacyclic compounds / Organopnictogen compounds
show 3 more
Substituents
Imidazo[1,5-a][1,4]benzodiazepine / Para-diazepine / Fluorobenzene / Halobenzene / Aryl chloride / Aryl fluoride / Aryl halide / Monocyclic benzene moiety / Benzenoid / N-substituted imidazole
show 16 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
diazepine (CHEBI:6931)

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Potentiator
General Function
Inhibitory extracellular ligand-gated ion channel activity
Specific Function
Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine...
Gene Name
GABRA1
Uniprot ID
P14867
Uniprot Name
Gamma-aminobutyric acid receptor subunit alpha-1
Molecular Weight
51801.395 Da
References
  1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090]
  2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [PubMed:18384456]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Potentiator
General Function
Inhibitory extracellular ligand-gated ion channel activity
Specific Function
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
Gene Name
GABRA2
Uniprot ID
P47869
Uniprot Name
Gamma-aminobutyric acid receptor subunit alpha-2
Molecular Weight
51325.85 Da
References
  1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090]
  2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [PubMed:18384456]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Potentiator
General Function
Inhibitory extracellular ligand-gated ion channel activity
Specific Function
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
Gene Name
GABRA3
Uniprot ID
P34903
Uniprot Name
Gamma-aminobutyric acid receptor subunit alpha-3
Molecular Weight
55164.055 Da
References
  1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090]
  2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [PubMed:18384456]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Potentiator
General Function
Inhibitory extracellular ligand-gated ion channel activity
Specific Function
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
Gene Name
GABRA4
Uniprot ID
P48169
Uniprot Name
Gamma-aminobutyric acid receptor subunit alpha-4
Molecular Weight
61622.645 Da
References
  1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090]
  2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [PubMed:18384456]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Potentiator
General Function
Transporter activity
Specific Function
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
Gene Name
GABRA5
Uniprot ID
P31644
Uniprot Name
Gamma-aminobutyric acid receptor subunit alpha-5
Molecular Weight
52145.645 Da
References
  1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090]
  2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [PubMed:18384456]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Potentiator
General Function
Ligand-gated ion channel activity
Specific Function
Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine...
Gene Name
GABRB1
Uniprot ID
P18505
Uniprot Name
Gamma-aminobutyric acid receptor subunit beta-1
Molecular Weight
54234.085 Da
References
  1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090]
  2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [PubMed:18384456]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Potentiator
General Function
Gaba-gated chloride ion channel activity
Specific Function
Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine...
Gene Name
GABRB3
Uniprot ID
P28472
Uniprot Name
Gamma-aminobutyric acid receptor subunit beta-3
Molecular Weight
54115.04 Da
References
  1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090]
  2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [PubMed:18384456]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Potentiator
General Function
Inhibitory extracellular ligand-gated ion channel activity
Specific Function
Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine...
Gene Name
GABRB2
Uniprot ID
P47870
Uniprot Name
Gamma-aminobutyric acid receptor subunit beta-2
Molecular Weight
59149.895 Da
References
  1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090]
  2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [PubMed:18384456]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Potentiator
General Function
Inhibitory extracellular ligand-gated ion channel activity
Specific Function
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
Gene Name
GABRA6
Uniprot ID
Q16445
Uniprot Name
Gamma-aminobutyric acid receptor subunit alpha-6
Molecular Weight
51023.69 Da
References
  1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090]
  2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [PubMed:18384456]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Potentiator
General Function
Inhibitory extracellular ligand-gated ion channel activity
Specific Function
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
Gene Name
GABRG1
Uniprot ID
Q8N1C3
Uniprot Name
Gamma-aminobutyric acid receptor subunit gamma-1
Molecular Weight
53594.49 Da
References
  1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090]
  2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [PubMed:18384456]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Potentiator
General Function
Inhibitory extracellular ligand-gated ion channel activity
Specific Function
Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine...
Gene Name
GABRG2
Uniprot ID
P18507
Uniprot Name
Gamma-aminobutyric acid receptor subunit gamma-2
Molecular Weight
54161.78 Da
References
  1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090]
  2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [PubMed:18384456]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Potentiator
General Function
Inhibitory extracellular ligand-gated ion channel activity
Specific Function
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
Gene Name
GABRG3
Uniprot ID
Q99928
Uniprot Name
Gamma-aminobutyric acid receptor subunit gamma-3
Molecular Weight
54288.16 Da
References
  1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090]
  2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [PubMed:18384456]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Potentiator
General Function
Gaba-a receptor activity
Specific Function
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
Gene Name
GABRD
Uniprot ID
O14764
Uniprot Name
Gamma-aminobutyric acid receptor subunit delta
Molecular Weight
50707.835 Da
References
  1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090]
  2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [PubMed:18384456]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Potentiator
General Function
Inhibitory extracellular ligand-gated ion channel activity
Specific Function
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
Gene Name
GABRE
Uniprot ID
P78334
Uniprot Name
Gamma-aminobutyric acid receptor subunit epsilon
Molecular Weight
57971.175 Da
References
  1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090]
  2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [PubMed:18384456]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Potentiator
General Function
Gaba-a receptor activity
Specific Function
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel. In the ute...
Gene Name
GABRP
Uniprot ID
O00591
Uniprot Name
Gamma-aminobutyric acid receptor subunit pi
Molecular Weight
50639.735 Da
References
  1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090]
  2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [PubMed:18384456]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Potentiator
General Function
Gaba-a receptor activity
Specific Function
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel. Rho-1 GABA...
Gene Name
GABRR1
Uniprot ID
P24046
Uniprot Name
Gamma-aminobutyric acid receptor subunit rho-1
Molecular Weight
55882.91 Da
References
  1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090]
  2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [PubMed:18384456]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Potentiator
General Function
Gaba-a receptor activity
Specific Function
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel. Rho-2 GABA...
Gene Name
GABRR2
Uniprot ID
P28476
Uniprot Name
Gamma-aminobutyric acid receptor subunit rho-2
Molecular Weight
54150.41 Da
References
  1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090]
  2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [PubMed:18384456]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Potentiator
General Function
Gaba-a receptor activity
Specific Function
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
Gene Name
GABRR3
Uniprot ID
A8MPY1
Uniprot Name
Gamma-aminobutyric acid receptor subunit rho-3
Molecular Weight
54271.1 Da
References
  1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090]
  2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [PubMed:18384456]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Potentiator
General Function
Transmembrane signaling receptor activity
Specific Function
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
Gene Name
GABRQ
Uniprot ID
Q9UN88
Uniprot Name
Gamma-aminobutyric acid receptor subunit theta
Molecular Weight
72020.875 Da
References
  1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090]
  2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [PubMed:18384456]

Enzymes

Details
1. Cytochrome P450 3A4
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Foti RS, Rock DA, Wienkers LC, Wahlstrom JL: Selection of alternative CYP3A4 probe substrates for clinical drug interaction studies using in vitro data and in vivo simulation. Drug Metab Dispos. 2010 Jun;38(6):981-7. doi: 10.1124/dmd.110.032094. Epub 2010 Mar 4. [PubMed:20203109]
  2. Pelkonen O, Maenpaa J, Taavitsainen P, Rautio A, Raunio H: Inhibition and induction of human cytochrome P450 (CYP) enzymes. Xenobiotica. 1998 Dec;28(12):1203-53. [PubMed:9890159]
  3. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
  4. Zhou S, Chan E, Lim LY, Boelsterli UA, Li SC, Wang J, Zhang Q, Huang M, Xu A: Therapeutic drugs that behave as mechanism-based inhibitors of cytochrome P450 3A4. Curr Drug Metab. 2004 Oct;5(5):415-42. [PubMed:15544435]
  5. Williams JA, Ring BJ, Cantrell VE, Jones DR, Eckstein J, Ruterbories K, Hamman MA, Hall SD, Wrighton SA: Comparative metabolic capabilities of CYP3A4, CYP3A5, and CYP3A7. Drug Metab Dispos. 2002 Aug;30(8):883-91. [PubMed:12124305]
  6. Galetin A, Clarke SE, Houston JB: Quinidine and haloperidol as modifiers of CYP3A4 activity: multisite kinetic model approach. Drug Metab Dispos. 2002 Dec;30(12):1512-22. [PubMed:12433827]
  7. Obach RS, Reed-Hagen AE: Measurement of Michaelis constants for cytochrome P450-mediated biotransformation reactions using a substrate depletion approach. Drug Metab Dispos. 2002 Jul;30(7):831-7. [PubMed:12065442]
  8. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Oxygen binding
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP3A5
Uniprot ID
P20815
Uniprot Name
Cytochrome P450 3A5
Molecular Weight
57108.065 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
  2. Patki KC, Von Moltke LL, Greenblatt DJ: In vitro metabolism of midazolam, triazolam, nifedipine, and testosterone by human liver microsomes and recombinant cytochromes p450: role of cyp3a4 and cyp3a5. Drug Metab Dispos. 2003 Jul;31(7):938-44. [PubMed:12814972]
  3. Wandel C, Bocker R, Bohrer H, Browne A, Rugheimer E, Martin E: Midazolam is metabolized by at least three different cytochrome P450 enzymes. Br J Anaesth. 1994 Nov;73(5):658-61. [PubMed:7826796]
  4. Rendic S: Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448. [PubMed:11996015]
  5. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Oxygen binding
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP3A7
Uniprot ID
P24462
Uniprot Name
Cytochrome P450 3A7
Molecular Weight
57525.03 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
  2. Gorski JC, Hall SD, Jones DR, VandenBranden M, Wrighton SA: Regioselective biotransformation of midazolam by members of the human cytochrome P450 3A (CYP3A) subfamily. Biochem Pharmacol. 1994 Apr 29;47(9):1643-53. [PubMed:8185679]
  3. Ghosal A, Satoh H, Thomas PE, Bush E, Moore D: Inhibition and kinetics of cytochrome P4503A activity in microsomes from rat, human, and cdna-expressed human cytochrome P450. Drug Metab Dispos. 1996 Sep;24(9):940-7. [PubMed:8886602]
  4. Rendic S: Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448. [PubMed:11996015]
  5. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2B6
Uniprot ID
P20813
Uniprot Name
Cytochrome P450 2B6
Molecular Weight
56277.81 Da
References
  1. Ekins S, Vandenbranden M, Ring BJ, Gillespie JS, Yang TJ, Gelboin HV, Wrighton SA: Further characterization of the expression in liver and catalytic activity of CYP2B6. J Pharmacol Exp Ther. 1998 Sep;286(3):1253-9. [PubMed:9732386]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
  3. Rendic S: Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448. [PubMed:11996015]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Oxygen binding
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP4B1
Uniprot ID
P13584
Uniprot Name
Cytochrome P450 4B1
Molecular Weight
58990.64 Da
References
  1. Rendic S: Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448. [PubMed:11996015]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Protein homodimerization activity
Specific Function
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform glucuronidates bilirubin IX-alpha to form both the...
Gene Name
UGT1A4
Uniprot ID
P22310
Uniprot Name
UDP-glucuronosyltransferase 1-4
Molecular Weight
60024.535 Da
References
  1. Klieber S, Hugla S, Ngo R, Arabeyre-Fabre C, Meunier V, Sadoun F, Fedeli O, Rival M, Bourrie M, Guillou F, Maurel P, Fabre G: Contribution of the N-glucuronidation pathway to the overall in vitro metabolic clearance of midazolam in humans. Drug Metab Dispos. 2008 May;36(5):851-62. doi: 10.1124/dmd.107.019539. Epub 2008 Feb 6. [PubMed:18256203]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Steroid hydroxylase activity
Specific Function
Metabolizes several precarcinogens, drugs, and solvents to reactive metabolites. Inactivates a number of drugs and xenobiotics and also bioactivates many xenobiotic substrates to their hepatotoxic ...
Gene Name
CYP2E1
Uniprot ID
P05181
Uniprot Name
Cytochrome P450 2E1
Molecular Weight
56848.42 Da
References
  1. Tassaneeyakul W, Birkett DJ, Miners JO: Inhibition of human hepatic cytochrome P4502E1 by azole antifungals, CNS-active drugs and non-steroidal anti-inflammatory agents. Xenobiotica. 1998 Mar;28(3):293-301. [PubMed:9574817]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
Inducer
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. Schuetz EG, Beck WT, Schuetz JD: Modulators and substrates of P-glycoprotein and cytochrome P4503A coordinately up-regulate these proteins in human colon carcinoma cells. Mol Pharmacol. 1996 Feb;49(2):311-8. [PubMed:8632764]
  2. Katoh M, Nakajima M, Yamazaki H, Yokoi T: Inhibitory effects of CYP3A4 substrates and their metabolites on P-glycoprotein-mediated transport. Eur J Pharm Sci. 2001 Feb;12(4):505-13. [PubMed:11231118]
  3. Schwab D, Fischer H, Tabatabaei A, Poli S, Huwyler J: Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery. J Med Chem. 2003 Apr 24;46(9):1716-25. [PubMed:12699389]
  4. Takano M, Hasegawa R, Fukuda T, Yumoto R, Nagai J, Murakami T: Interaction with P-glycoprotein and transport of erythromycin, midazolam and ketoconazole in Caco-2 cells. Eur J Pharmacol. 1998 Oct 9;358(3):289-94. [PubMed:9822896]
  5. Kim RB, Wandel C, Leake B, Cvetkovic M, Fromm MF, Dempsey PJ, Roden MM, Belas F, Chaudhary AK, Roden DM, Wood AJ, Wilkinson GR: Interrelationship between substrates and inhibitors of human CYP3A and P-glycoprotein. Pharm Res. 1999 Mar;16(3):408-14. [PubMed:10213372]
  6. Polli JW, Wring SA, Humphreys JE, Huang L, Morgan JB, Webster LO, Serabjit-Singh CS: Rational use of in vitro P-glycoprotein assays in drug discovery. J Pharmacol Exp Ther. 2001 Nov;299(2):620-8. [PubMed:11602674]
  7. Mahar Doan KM, Humphreys JE, Webster LO, Wring SA, Shampine LJ, Serabjit-Singh CJ, Adkison KK, Polli JW: Passive permeability and P-glycoprotein-mediated efflux differentiate central nervous system (CNS) and non-CNS marketed drugs. J Pharmacol Exp Ther. 2002 Dec;303(3):1029-37. [PubMed:12438524]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Secondary active organic cation transmembrane transporter activity
Specific Function
Translocates a broad array of organic cations with various structures and molecular weights including the model compounds 1-methyl-4-phenylpyridinium (MPP), tetraethylammonium (TEA), N-1-methylnico...
Gene Name
SLC22A1
Uniprot ID
O15245
Uniprot Name
Solute carrier family 22 member 1
Molecular Weight
61153.345 Da
References
  1. Zhang L, Schaner ME, Giacomini KM: Functional characterization of an organic cation transporter (hOCT1) in a transiently transfected human cell line (HeLa). J Pharmacol Exp Ther. 1998 Jul;286(1):354-61. [PubMed:9655880]

Drug created on June 13, 2005 07:24 / Updated on July 13, 2018 01:01