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IdentificationPharmacologyInteractionsReferencesTrialsEconomicsPropertiesSpectraTaxonomyIdentification
- 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
Structure for DB00683 (Midazolam)
- Synonyms
- Buccolam
- Dormicum
- Midazolam
- Midazolamum
- External IDs
- Dea No. 2884 / Ro 21-3981/001 / Ro 21-3981/003
- Product Ingredients
Ingredient UNII CAS InChI Key Midazolam Hydrochloride W7TTW573JJ 59467-96-8 PLYSCVSCYOQVRP-UHFFFAOYSA-N Midazolam maleate 77520S18SE 59467-94-6 XYGVIBXOJOOCFR-BTJKTKAUSA-N - Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Buccolam Solution 5 mg Buccal Shire Services Bvba 2011-09-05 Not applicable EU 
Buccolam Solution 10 mg Buccal Shire Services Bvba 2011-09-05 Not applicable EU Buccolam Solution 2.5 mg Buccal Shire Services Bvba 2011-09-05 Not applicable EU Buccolam Solution 7.5 mg Buccal Shire Services Bvba 2011-09-05 Not applicable EU Midazolam Injection Solution 1 mg Intramuscular; Intravenous Sandoz Canada Incorporated 1999-07-21 Not applicable Canada 
Midazolam Injection Solution 1 mg Intramuscular; Intravenous Novopharm Limited 2001-12-17 Not applicable Canada Midazolam Injection Solution 5 mg Intramuscular; Intravenous Pfizer 2015-03-31 Not applicable Canada Midazolam Injection Liquid 5 mg Intramuscular; Intravenous Fresenius Kabi 2001-03-26 Not applicable Canada Midazolam Injection Solution 5 mg Intramuscular; Intravenous Mylan Pharmaceuticals Not applicable Not applicable Canada Midazolam Injection Solution 1 mg Intramuscular; Intravenous Pfizer 2015-03-31 Not applicable Canada - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Apo-midazolam Injectable 1 mg/ml Liquid 1 mg Intramuscular; Intravenous Apotex Corporation 2001-04-10 2013-08-02 Canada Apo-midazolam Injectable 5 mg/ml Liquid 5 mg Intramuscular; Intravenous Apotex Corporation 2001-04-10 2013-08-02 Canada Midazolam Injection, solution 10 mg/2mL Intramuscular; Intravenous Fresenius Kabi 2014-10-03 Not applicable US 
Midazolam Injection, solution 5 mg/mL Intramuscular; Intravenous Athenex Pharmaceutical Division, Llc. 2016-12-14 Not applicable US Midazolam Injection 1 mg/mL Intramuscular; Intravenous Akorn 2005-05-06 Not applicable US Midazolam Injection 1 mg/mL Intramuscular; Intravenous General Injectables & Vaccines 2018-03-05 Not applicable US Midazolam Injection 1 mg/mL Intramuscular; Intravenous West Ward Pharmaceutical 2000-06-20 Not applicable US Midazolam Injection 5 mg/mL Intramuscular; Intravenous West Ward Pharmaceutical 2000-06-20 Not applicable US Midazolam Injection, solution 1 mg/mL Intramuscular; Intravenous The Medicines Company 2000-07-14 Not applicable US Midazolam Injection, solution 1 mg/mL Intramuscular; Intravenous The Medicines Company 2000-07-14 Not applicable US - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Midazolam HCl Midazolam Hydrochloride (.5 mg/mL) Injection, solution Intravenous Cantrell Drug Company 2013-01-30 Not applicable US Midazolam HCl Midazolam Hydrochloride (1 mg/mL) Injection, solution Intravenous Cantrell Drug Company 2010-08-02 Not applicable US - 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
- Adjuvants, Anesthesia
- Anesthetics
- Anesthetics, General
- Anesthetics, Intravenous
- Anti-Anxiety Agents
- Benzazepines
- Benzodiazepine Derivatives
- Benzodiazepines
- Central Nervous System Agents
- Central Nervous System Depressants
- Combined Inhibitors of CYP3A4 and P-glycoprotein
- CYP3A Substrates (Sensitive)
- Cytochrome P-450 CYP2B6 Substrates
- Cytochrome P-450 CYP2E1 Inhibitors
- Cytochrome P-450 CYP3A Inhibitors
- Cytochrome P-450 CYP3A4 Inhibitors
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 CYP3A5 Substrates
- Cytochrome P-450 CYP3A7 Substrates
- Cytochrome P-450 Enzyme Inhibitors
- GABA Agents
- GABA Modulators
- Hypnotics and Sedatives
- Nervous System
- Neurotransmitter Agents
- P-glycoprotein/ABCB1 Inducers
- P-glycoprotein/ABCB1 Inhibitors
- P-glycoprotein/ABCB1 Substrates
- Psycholeptics
- Psychotropic Drugs
- Tranquilizing Agents
- 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.
- Structured Indications
- 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.
- 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
Drug Interaction Drug group 1,10-Phenanthroline The serum concentration of Midazolam can be increased when it is combined with 1,10-Phenanthroline. Experimental 3,4-Dichloroisocoumarin The serum concentration of Midazolam can be increased when it is combined with 3,4-Dichloroisocoumarin. Experimental 4-(2-Aminoethyl)Benzenesulfonyl Fluoride The serum concentration of Midazolam can be increased when it is combined with 4-(2-Aminoethyl)Benzenesulfonyl Fluoride. Experimental 7-Nitroindazole The risk or severity of adverse effects can be increased when Midazolam is combined with 7-Nitroindazole. Experimental Acepromazine The risk or severity of adverse effects can be increased when Midazolam is combined with Acepromazine. Approved, Vet Approved Aceprometazine The risk or severity of adverse effects can be increased when Midazolam is combined with Aceprometazine. Approved Adipiplon The risk or severity of adverse effects can be increased when Midazolam is combined with Adipiplon. Investigational Afatinib The serum concentration of Afatinib can be decreased when it is combined with Midazolam. Approved Agomelatine The risk or severity of adverse effects can be increased when Midazolam is combined with Agomelatine. Approved, Investigational Alaproclate The risk or severity of adverse effects can be increased when Midazolam is combined with Alaproclate. Experimental Alfaxalone The risk or severity of adverse effects can be increased when Midazolam is combined with Alfaxalone. Vet Approved Alfentanil The risk or severity of adverse effects can be increased when Midazolam is combined with Alfentanil. Approved, Illicit Allopregnanolone The risk or severity of adverse effects can be increased when Midazolam is combined with Allopregnanolone. Investigational Alogliptin The serum concentration of Midazolam can be increased when it is combined with Alogliptin. Approved Alpha-1-proteinase inhibitor The serum concentration of Midazolam can be increased when it is combined with Alpha-1-proteinase inhibitor. Approved Alphacetylmethadol The risk or severity of adverse effects can be increased when Midazolam is combined with Alphacetylmethadol. Experimental, Illicit Alphaprodine The risk or severity of adverse effects can be increased when Midazolam is combined with Alphaprodine. Illicit Alprazolam The risk or severity of adverse effects can be increased when Alprazolam is combined with Midazolam. Approved, Illicit, Investigational Ambroxol acefyllinate The therapeutic efficacy of Midazolam can be decreased when used in combination with Ambroxol acefyllinate. Experimental, Investigational Aminophylline The therapeutic efficacy of Midazolam can be decreased when used in combination with Aminophylline. Approved Amiodarone The metabolism of Midazolam can be decreased when combined with Amiodarone. Approved, Investigational Amisulpride The risk or severity of adverse effects can be increased when Midazolam is combined with Amisulpride. Approved, Investigational Amitriptyline The risk or severity of adverse effects can be increased when Midazolam is combined with Amitriptyline. Approved Amobarbital The risk or severity of adverse effects can be increased when Midazolam is combined with Amobarbital. Approved, Illicit Amoxapine The risk or severity of adverse effects can be increased when Midazolam is combined with Amoxapine. Approved Amperozide The risk or severity of adverse effects can be increased when Midazolam is combined with Amperozide. Experimental Amprenavir The serum concentration of Midazolam can be increased when it is combined with Amprenavir. Approved, Investigational Antithrombin III human The serum concentration of Midazolam can be increased when it is combined with Antithrombin III human. Approved Apalutamide The serum concentration of Midazolam can be decreased when it is combined with Apalutamide. Approved, Investigational Apixaban The serum concentration of Midazolam can be increased when it is combined with Apixaban. Approved Aprepitant The serum concentration of Midazolam can be increased when it is combined with Aprepitant. Approved, Investigational Aprotinin The serum concentration of Midazolam can be increased when it is combined with Aprotinin. Approved, Investigational, Withdrawn Argatroban The serum concentration of Midazolam can be increased when it is combined with Argatroban. Approved, Investigational Aripiprazole The risk or severity of adverse effects can be increased when Midazolam is combined with Aripiprazole. Approved, Investigational Articaine The risk or severity of adverse effects can be increased when Midazolam is combined with Articaine. Approved Asenapine The risk or severity of adverse effects can be increased when Midazolam is combined with Asenapine. Approved Asunaprevir The serum concentration of Midazolam can be decreased when it is combined with Asunaprevir. Approved, Investigational, Withdrawn Atazanavir The serum concentration of Midazolam can be increased when it is combined with Atazanavir. Approved, Investigational Atomoxetine The metabolism of Midazolam can be decreased when combined with Atomoxetine. Approved Atorvastatin The serum concentration of Midazolam can be increased when it is combined with Atorvastatin. Approved Azaperone The risk or severity of adverse effects can be increased when Midazolam is combined with Azaperone. Investigational, Vet Approved Azelastine Midazolam may increase the central nervous system depressant (CNS depressant) activities of Azelastine. Approved Baclofen The risk or severity of adverse effects can be increased when Midazolam is combined with Baclofen. Approved Barbital The risk or severity of adverse effects can be increased when Midazolam is combined with Barbital. Illicit Batimastat The serum concentration of Midazolam can be increased when it is combined with Batimastat. Experimental Benazepril The serum concentration of Midazolam can be increased when it is combined with Benazepril. Approved, Investigational Benperidol The risk or severity of adverse effects can be increased when Midazolam is combined with Benperidol. Approved, Investigational Benzamidine The serum concentration of Midazolam can be increased when it is combined with Benzamidine. Experimental Benzocaine The risk or severity of adverse effects can be increased when Midazolam is combined with Benzocaine. Approved, Investigational Benzyl alcohol The risk or severity of adverse effects can be increased when Midazolam is combined with Benzyl alcohol. Approved Bivalirudin The serum concentration of Midazolam can be increased when it is combined with Bivalirudin. Approved, Investigational Boceprevir The serum concentration of Midazolam can be increased when it is combined with Boceprevir. Approved, Withdrawn Bortezomib The metabolism of Midazolam can be decreased when combined with Bortezomib. Approved, Investigational Bosentan The serum concentration of Midazolam can be decreased when it is combined with Bosentan. Approved, Investigational Bosutinib The serum concentration of Bosutinib can be increased when it is combined with Midazolam. Approved Brentuximab vedotin The serum concentration of Brentuximab vedotin can be decreased when it is combined with Midazolam. Approved, Investigational Brexpiprazole The risk or severity of adverse effects can be increased when Midazolam is combined with Brexpiprazole. Approved, Investigational Brigatinib The serum concentration of Midazolam can be decreased when it is combined with Brigatinib. Approved, Investigational Brimonidine Brimonidine may increase the central nervous system depressant (CNS depressant) activities of Midazolam. Approved Bromazepam The risk or severity of adverse effects can be increased when Midazolam is combined with Bromazepam. Approved, Illicit, Investigational Bromisoval The risk or severity of adverse effects can be increased when Midazolam is combined with Bromisoval. Experimental Bromocriptine The risk or severity of adverse effects can be increased when Bromocriptine is combined with Midazolam. Approved, Investigational Bromperidol The risk or severity of adverse effects can be increased when Midazolam is combined with Bromperidol. Approved, Investigational Brompheniramine The risk or severity of adverse effects can be increased when Midazolam is combined with Brompheniramine. Approved Brotizolam The risk or severity of adverse effects can be increased when Midazolam is combined with Brotizolam. Approved, Investigational, Withdrawn Bupivacaine The risk or severity of adverse effects can be increased when Midazolam is combined with Bupivacaine. Approved, Investigational Buprenorphine Midazolam may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine. Approved, Illicit, Investigational, Vet Approved Buspirone The risk or severity of adverse effects can be increased when Buspirone is combined with Midazolam. Approved, Investigational Butabarbital The risk or severity of adverse effects can be increased when Butabarbital is combined with Midazolam. Approved, Illicit Butacaine The risk or severity of adverse effects can be increased when Midazolam is combined with Butacaine. Vet Approved Butalbital The risk or severity of adverse effects can be increased when Midazolam is combined with Butalbital. Approved, Illicit Butamben The risk or severity of adverse effects can be increased when Midazolam is combined with Butamben. Approved, Withdrawn Butethal The risk or severity of adverse effects can be increased when Midazolam is combined with Butethal. Approved, Illicit Butorphanol The risk or severity of adverse effects can be increased when Butorphanol is combined with Midazolam. Approved, Illicit, Vet Approved Cabergoline The risk or severity of adverse effects can be increased when Cabergoline is combined with Midazolam. Approved Camostat The serum concentration of Midazolam can be increased when it is combined with Camostat. Experimental Candoxatril The serum concentration of Midazolam can be increased when it is combined with Candoxatril. Experimental Candoxatrilat The serum concentration of Midazolam can be increased when it is combined with Candoxatrilat. Experimental Canertinib The risk or severity of adverse effects can be increased when Midazolam is combined with Canertinib. Investigational Captopril The serum concentration of Midazolam can be increased when it is combined with Captopril. Approved Carbamazepine The metabolism of Midazolam can be increased when combined with Carbamazepine. Approved, Investigational Carbinoxamine The risk or severity of adverse effects can be increased when Midazolam is combined with Carbinoxamine. Approved Carbomycin The serum concentration of Midazolam can be increased when it is combined with Carbomycin. Vet Approved Carfentanil The risk or severity of adverse effects can be increased when Midazolam is combined with Carfentanil. Illicit, Investigational, Vet Approved Carisoprodol The risk or severity of adverse effects can be increased when Midazolam is combined with Carisoprodol. Approved Ceritinib The serum concentration of Midazolam can be increased when it is combined with Ceritinib. Approved Cerivastatin The serum concentration of Cerivastatin can be increased when it is combined with Midazolam. Approved, Withdrawn Cetirizine The risk or severity of adverse effects can be increased when Midazolam is combined with Cetirizine. Approved Chloral hydrate The risk or severity of adverse effects can be increased when Midazolam is combined with Chloral hydrate. Approved, Illicit, Investigational, Vet Approved Chlordiazepoxide The risk or severity of adverse effects can be increased when Chlordiazepoxide is combined with Midazolam. Approved, Illicit, Investigational Chlormezanone The risk or severity of adverse effects can be increased when Midazolam is combined with Chlormezanone. Approved, Investigational, Withdrawn Chloroprocaine The risk or severity of adverse effects can be increased when Midazolam is combined with Chloroprocaine. Approved Chlorphenamine The risk or severity of adverse effects can be increased when Midazolam is combined with Chlorphenamine. Approved Chlorpromazine The risk or severity of adverse effects can be increased when Chlorpromazine is combined with Midazolam. Approved, Investigational, Vet Approved Chlorprothixene The risk or severity of adverse effects can be increased when Midazolam is combined with Chlorprothixene. Approved, Investigational, Withdrawn Chlorzoxazone The risk or severity of adverse effects can be increased when Midazolam is combined with Chlorzoxazone. Approved Cholesterol The serum concentration of Midazolam can be increased when it is combined with Cholesterol. Approved, Experimental, Investigational Chymostatin The serum concentration of Midazolam can be increased when it is combined with Chymostatin. Experimental Cilastatin The serum concentration of Midazolam can be increased when it is combined with Cilastatin. Approved, Investigational Cilazapril The serum concentration of Midazolam can be increased when it is combined with Cilazapril. Approved Cinchocaine The risk or severity of adverse effects can be increased when Midazolam is combined with Cinchocaine. Approved, Vet Approved Citalopram The metabolism of Midazolam can be decreased when combined with Citalopram. Approved Clarithromycin The serum concentration of Midazolam can be increased when it is combined with Clarithromycin. Approved Clemastine The metabolism of Midazolam can be decreased when combined with Clemastine. Approved, Investigational Clidinium The risk or severity of adverse effects can be increased when Midazolam is combined with Clidinium. Approved Clobazam The risk or severity of adverse effects can be increased when Midazolam is combined with Clobazam. Approved, Illicit clomethiazole The risk or severity of adverse effects can be increased when Midazolam is combined with clomethiazole. Investigational Clomipramine The risk or severity of adverse effects can be increased when Midazolam is combined with Clomipramine. Approved, Investigational, Vet Approved Clonazepam The risk or severity of adverse effects can be increased when Midazolam is combined with Clonazepam. Approved, Illicit Clonidine The risk or severity of adverse effects can be increased when Midazolam is combined with Clonidine. Approved Clopenthixol The risk or severity of adverse effects can be increased when Midazolam is combined with Clopenthixol. Experimental Clopidogrel The metabolism of Midazolam can be decreased when combined with Clopidogrel. Approved Clorazepate The risk or severity of adverse effects can be increased when Clorazepate is combined with Midazolam. Approved, Illicit Clothiapine The risk or severity of adverse effects can be increased when Midazolam is combined with Clothiapine. Experimental Clotrimazole The metabolism of Midazolam can be decreased when combined with Clotrimazole. Approved, Vet Approved Clozapine The risk or severity of adverse effects can be increased when Midazolam is combined with Clozapine. Approved Cobicistat The serum concentration of Midazolam can be increased when it is combined with Cobicistat. Approved Cocaine The risk or severity of adverse effects can be increased when Midazolam is combined with Cocaine. Approved, Illicit Codeine The risk or severity of adverse effects can be increased when Codeine is combined with Midazolam. Approved, Illicit Colchicine The serum concentration of Colchicine can be increased when it is combined with Midazolam. Approved Conivaptan The serum concentration of Conivaptan can be increased when it is combined with Midazolam. Approved, Investigational Crizotinib The metabolism of Midazolam can be decreased when combined with Crizotinib. Approved Cyclizine The risk or severity of adverse effects can be increased when Midazolam is combined with Cyclizine. Approved Cyclobenzaprine The risk or severity of adverse effects can be increased when Midazolam is combined with Cyclobenzaprine. Approved Cyclopropane The risk or severity of adverse effects can be increased when Midazolam is combined with Cyclopropane. Experimental Cyclosporine The metabolism of Midazolam can be decreased when combined with Cyclosporine. Approved, Investigational, Vet Approved Cyproheptadine The risk or severity of adverse effects can be increased when Midazolam is combined with Cyproheptadine. Approved Dabigatran etexilate The serum concentration of Dabigatran etexilate can be decreased when it is combined with Midazolam. Approved Dabrafenib The serum concentration of Midazolam can be decreased when it is combined with Dabrafenib. Approved, Investigational Dantrolene The risk or severity of adverse effects can be increased when Midazolam is combined with Dantrolene. Approved, Investigational Dapiprazole The risk or severity of adverse effects can be increased when Midazolam is combined with Dapiprazole. Approved Dapoxetine The risk or severity of adverse effects can be increased when Midazolam is combined with Dapoxetine. Investigational Darexaban The serum concentration of Midazolam can be increased when it is combined with Darexaban. Investigational Darunavir The serum concentration of Midazolam can be increased when it is combined with Darunavir. Approved Dasatinib The serum concentration of Midazolam can be increased when it is combined with Dasatinib. Approved, Investigational Deferasirox The serum concentration of Midazolam can be decreased when it is combined with Deferasirox. Approved, Investigational Delanzomib The serum concentration of Midazolam can be increased when it is combined with Delanzomib. Investigational Delapril The serum concentration of Midazolam can be increased when it is combined with Delapril. Experimental Delavirdine The metabolism of Midazolam can be decreased when combined with Delavirdine. Approved Deramciclane The risk or severity of adverse effects can be increased when Midazolam is combined with Deramciclane. Investigational Desflurane The risk or severity of adverse effects can be increased when Midazolam is combined with Desflurane. Approved Desipramine The metabolism of Midazolam can be decreased when combined with Desipramine. Approved, Investigational Desloratadine The risk or severity of adverse effects can be increased when Midazolam is combined with Desloratadine. Approved, Investigational Desvenlafaxine The risk or severity of adverse effects can be increased when Midazolam is combined with Desvenlafaxine. Approved, Investigational Detomidine The risk or severity of adverse effects can be increased when Midazolam is combined with Detomidine. Vet Approved Deutetrabenazine The risk or severity of sedation and somnolence can be increased when Midazolam is combined with Deutetrabenazine. Approved, Investigational Dexbrompheniramine The risk or severity of adverse effects can be increased when Midazolam is combined with Dexbrompheniramine. Approved Dexmedetomidine The risk or severity of adverse effects can be increased when Midazolam is combined with Dexmedetomidine. Approved, Vet Approved Dextromoramide The risk or severity of adverse effects can be increased when Midazolam is combined with Dextromoramide. Experimental, Illicit Dextropropoxyphene The risk or severity of adverse effects can be increased when Midazolam is combined with Dextropropoxyphene. Approved, Illicit, Investigational, Withdrawn Dezocine The risk or severity of adverse effects can be increased when Midazolam is combined with Dezocine. Approved, Investigational Diazepam The risk or severity of adverse effects can be increased when Midazolam is combined with Diazepam. Approved, Illicit, Investigational, Vet Approved Diethyl ether The risk or severity of adverse effects can be increased when Midazolam is combined with Diethyl ether. Experimental Difenoxin The risk or severity of adverse effects can be increased when Midazolam is combined with Difenoxin. Approved, Illicit Dihydrocodeine The risk or severity of adverse effects can be increased when Midazolam is combined with Dihydrocodeine. Approved, Illicit Dihydroergocornine The risk or severity of adverse effects can be increased when Dihydroergocornine is combined with Midazolam. Approved Dihydroergocristine The risk or severity of adverse effects can be increased when Dihydroergocristine is combined with Midazolam. Approved, Experimental Dihydroergocryptine The risk or severity of adverse effects can be increased when Dihydroergocryptine is combined with Midazolam. Experimental Dihydroergotamine The risk or severity of adverse effects can be increased when Dihydroergotamine is combined with Midazolam. Approved, Investigational Dihydroetorphine The risk or severity of adverse effects can be increased when Midazolam is combined with Dihydroetorphine. Experimental, Illicit Dihydromorphine The risk or severity of adverse effects can be increased when Midazolam is combined with Dihydromorphine. Experimental, Illicit Diltiazem The metabolism of Midazolam can be decreased when combined with Diltiazem. Approved, Investigational Dimenhydrinate The risk or severity of adverse effects can be increased when Midazolam is combined with Dimenhydrinate. Approved Diphenhydramine The risk or severity of adverse effects can be increased when Midazolam is combined with Diphenhydramine. Approved, Investigational Diphenoxylate The risk or severity of adverse effects can be increased when Midazolam is combined with Diphenoxylate. Approved, Illicit Dixyrazine The risk or severity of adverse effects can be increased when Midazolam is combined with Dixyrazine. Experimental Doramectin The risk or severity of adverse effects can be increased when Midazolam is combined with Doramectin. Vet Approved Doxepin The risk or severity of adverse effects can be increased when Midazolam is combined with Doxepin. Approved, Investigational Doxorubicin The serum concentration of Doxorubicin can be increased when it is combined with Midazolam. Approved, Investigational Doxorubicin The metabolism of Midazolam can be decreased when combined with Doxorubicin. Approved, Investigational Doxycycline The metabolism of Midazolam can be decreased when combined with Doxycycline. Approved, Investigational, Vet Approved Doxylamine Doxylamine may increase the central nervous system depressant (CNS depressant) activities of Midazolam. Approved, Vet Approved DPDPE The risk or severity of adverse effects can be increased when Midazolam is combined with DPDPE. Experimental Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Midazolam. Approved, Illicit Dronedarone The metabolism of Midazolam can be decreased when combined with Dronedarone. Approved Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Midazolam. Approved, Vet Approved Drotebanol The risk or severity of adverse effects can be increased when Midazolam is combined with Drotebanol. Experimental, Illicit Duloxetine The risk or severity of adverse effects can be increased when Midazolam is combined with Duloxetine. Approved Dyclonine The risk or severity of adverse effects can be increased when Midazolam is combined with Dyclonine. Approved Dyphylline The therapeutic efficacy of Midazolam can be decreased when used in combination with Dyphylline. Approved Ecabet The serum concentration of Midazolam can be increased when it is combined with Ecabet. Approved, Investigational Ecgonine The risk or severity of adverse effects can be increased when Midazolam is combined with Ecgonine. Experimental, Illicit Ecopipam The risk or severity of adverse effects can be increased when Midazolam is combined with Ecopipam. Investigational Edoxaban The serum concentration of Midazolam can be increased when it is combined with Edoxaban. Approved Efavirenz The risk or severity of adverse effects can be increased when Midazolam is combined with Efavirenz. Approved, Investigational Elafin The serum concentration of Midazolam can be increased when it is combined with Elafin. Investigational Eltanolone The risk or severity of adverse effects can be increased when Midazolam is combined with Eltanolone. Investigational Enalapril The serum concentration of Midazolam can be increased when it is combined with Enalapril. Approved, Vet Approved Enalaprilat The serum concentration of Midazolam can be increased when it is combined with Enalaprilat. Approved Enalkiren The serum concentration of Midazolam can be increased when it is combined with Enalkiren. Experimental Enflurane The risk or severity of adverse effects can be increased when Midazolam is combined with Enflurane. Approved, Investigational, Vet Approved Entacapone The risk or severity of adverse effects can be increased when Midazolam is combined with Entacapone. Approved, Investigational Enzalutamide The serum concentration of Midazolam can be decreased when it is combined with Enzalutamide. Approved Epigallocatechin Gallate The serum concentration of Midazolam can be increased when it is combined with Epigallocatechin Gallate. Investigational Ergonovine The risk or severity of adverse effects can be increased when Ergonovine is combined with Midazolam. Approved Ergotamine The risk or severity of adverse effects can be increased when Ergotamine is combined with Midazolam. Approved Erythromycin The serum concentration of Midazolam can be increased when it is combined with Erythromycin. Approved, Investigational, Vet Approved Escitalopram The risk or severity of adverse effects can be increased when Midazolam is combined with Escitalopram. Approved, Investigational Estazolam The risk or severity of adverse effects can be increased when Midazolam is combined with Estazolam. Approved, Illicit Eszopiclone The risk or severity of adverse effects can be increased when Eszopiclone is combined with Midazolam. Approved, Investigational Ethanol Midazolam may increase the central nervous system depressant (CNS depressant) activities of Ethanol. Approved Ethchlorvynol The risk or severity of adverse effects can be increased when Midazolam is combined with Ethchlorvynol. Approved, Illicit, Withdrawn Ethosuximide The risk or severity of adverse effects can be increased when Midazolam is combined with Ethosuximide. Approved Ethotoin The risk or severity of adverse effects can be increased when Midazolam is combined with Ethotoin. Approved Ethyl carbamate The risk or severity of adverse effects can be increased when Midazolam is combined with Ethyl carbamate. Withdrawn Ethyl chloride The risk or severity of adverse effects can be increased when Midazolam is combined with Ethyl chloride. Approved, Experimental, Investigational Ethyl loflazepate The risk or severity of adverse effects can be increased when Midazolam is combined with Ethyl loflazepate. Approved, Illicit Ethylmorphine The risk or severity of adverse effects can be increased when Midazolam is combined with Ethylmorphine. Approved, Illicit Etidocaine The risk or severity of adverse effects can be increased when Midazolam is combined with Etidocaine. Approved Etifoxine The risk or severity of adverse effects can be increased when Midazolam is combined with Etifoxine. Investigational, Withdrawn Etizolam The risk or severity of adverse effects can be increased when Midazolam is combined with Etizolam. Approved Etomidate The risk or severity of adverse effects can be increased when Midazolam is combined with Etomidate. Approved Etoperidone The risk or severity of adverse effects can be increased when Midazolam is combined with Etoperidone. Withdrawn Etorphine The risk or severity of adverse effects can be increased when Midazolam is combined with Etorphine. Illicit, Vet Approved Everolimus The serum concentration of Everolimus can be increased when it is combined with Midazolam. Approved Ezogabine The risk or severity of adverse effects can be increased when Midazolam is combined with Ezogabine. Approved, Investigational Faldaprevir The serum concentration of Midazolam can be increased when it is combined with Faldaprevir. Investigational Felbamate The risk or severity of adverse effects can be increased when Midazolam is combined with Felbamate. Approved Fencamfamine The risk or severity of adverse effects can be increased when Midazolam is combined with Fencamfamine. Approved, Illicit, Withdrawn Fentanyl The risk or severity of adverse effects can be increased when Midazolam is combined with Fentanyl. Approved, Illicit, Investigational, Vet Approved Fexofenadine The risk or severity of adverse effects can be increased when Midazolam is combined with Fexofenadine. Approved, Investigational Flibanserin The risk or severity of adverse effects can be increased when Midazolam is combined with Flibanserin. Approved, Investigational Fluanisone The risk or severity of adverse effects can be increased when Midazolam is combined with Fluanisone. Experimental Fluconazole The metabolism of Midazolam can be decreased when combined with Fluconazole. Approved, Investigational Fludiazepam The risk or severity of adverse effects can be increased when Midazolam is combined with Fludiazepam. Approved, Illicit Flunarizine The risk or severity of adverse effects can be increased when Midazolam is combined with Flunarizine. Approved Flunitrazepam The risk or severity of adverse effects can be increased when Midazolam is combined with Flunitrazepam. Approved, Illicit Fluoxetine The risk or severity of adverse effects can be increased when Midazolam is combined with Fluoxetine. Approved, Vet Approved Flupentixol The risk or severity of adverse effects can be increased when Midazolam is combined with Flupentixol. Approved, Investigational, Withdrawn Fluphenazine The risk or severity of adverse effects can be increased when Fluphenazine is combined with Midazolam. Approved Flurazepam The risk or severity of adverse effects can be increased when Midazolam is combined with Flurazepam. Approved, Illicit, Investigational Fluspirilene The risk or severity of adverse effects can be increased when Midazolam is combined with Fluspirilene. Approved, Investigational Fluticasone propionate The risk or severity of adverse effects can be increased when Midazolam is combined with Fluticasone propionate. Approved Fluvastatin The serum concentration of Fluvastatin can be increased when it is combined with Midazolam. Approved Fluvoxamine The metabolism of Midazolam can be decreased when combined with Fluvoxamine. Approved, Investigational Fosamprenavir The serum concentration of Midazolam can be increased when it is combined with Fosamprenavir. Approved Fosaprepitant The serum concentration of Midazolam can be increased when it is combined with Fosaprepitant. Approved Fosinopril The serum concentration of Midazolam can be increased when it is combined with Fosinopril. Approved Fosphenytoin The serum concentration of Fosphenytoin can be increased when it is combined with Midazolam. Approved, Investigational Fospropofol The risk or severity of adverse effects can be increased when Midazolam is combined with Fospropofol. Approved, Illicit, Investigational Fusidic Acid The serum concentration of Midazolam can be increased when it is combined with Fusidic Acid. Approved, Investigational Gabapentin The risk or severity of adverse effects can be increased when Midazolam is combined with Gabapentin. Approved, Investigational Gabapentin Enacarbil The risk or severity of adverse effects can be increased when Midazolam is combined with Gabapentin Enacarbil. Approved, Investigational Gabexate The serum concentration of Midazolam can be increased when it is combined with Gabexate. Investigational Gamma Hydroxybutyric Acid The risk or severity of adverse effects can be increased when Midazolam is combined with Gamma Hydroxybutyric Acid. Approved, Illicit, Investigational Geldanamycin The serum concentration of Midazolam can be increased when it is combined with Geldanamycin. Experimental, Investigational Gepirone The risk or severity of adverse effects can be increased when Midazolam is combined with Gepirone. Investigational Ginkgo biloba The serum concentration of Midazolam can be decreased when it is combined with Ginkgo biloba. Approved, Investigational, Nutraceutical Glutethimide The risk or severity of adverse effects can be increased when Midazolam is combined with Glutethimide. Approved, Illicit GM6001 The serum concentration of Midazolam can be increased when it is combined with GM6001. Experimental Guanfacine The risk or severity of adverse effects can be increased when Midazolam is combined with Guanfacine. Approved, Investigational Halazepam The risk or severity of adverse effects can be increased when Midazolam is combined with Halazepam. Approved, Illicit, Withdrawn Haloperidol The risk or severity of adverse effects can be increased when Haloperidol is combined with Midazolam. Approved Halothane The risk or severity of adverse effects can be increased when Midazolam is combined with Halothane. Approved, Vet Approved Heroin The risk or severity of adverse effects can be increased when Midazolam is combined with Heroin. Approved, Illicit, Investigational Hexobarbital The risk or severity of adverse effects can be increased when Midazolam is combined with Hexobarbital. Approved Hyaluronidase The therapeutic efficacy of Midazolam can be decreased when used in combination with Hyaluronidase. Approved, Investigational Hydrocodone Midazolam may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone. Approved, Illicit Hydromorphone The risk or severity of adverse effects can be increased when Hydromorphone is combined with Midazolam. Approved, Illicit Hydroxyzine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Midazolam. Approved Ibrutinib The serum concentration of Ibrutinib can be increased when it is combined with Midazolam. Approved Idelalisib The serum concentration of Midazolam can be increased when it is combined with Idelalisib. Approved Idraparinux The serum concentration of Midazolam can be increased when it is combined with Idraparinux. Investigational Iloperidone The risk or severity of adverse effects can be increased when Midazolam is combined with Iloperidone. Approved Imatinib The metabolism of Midazolam can be decreased when combined with Imatinib. Approved Imidapril The serum concentration of Midazolam can be increased when it is combined with Imidapril. Investigational Imipramine The risk or severity of adverse effects can be increased when Midazolam is combined with Imipramine. Approved Indalpine The risk or severity of adverse effects can be increased when Midazolam is combined with Indalpine. Investigational, Withdrawn Indinavir The serum concentration of Midazolam can be increased when it is combined with Indinavir. Approved Indiplon The risk or severity of adverse effects can be increased when Midazolam is combined with Indiplon. Investigational Isavuconazole The serum concentration of Midazolam can be increased when it is combined with Isavuconazole. Approved, Investigational Isavuconazonium The metabolism of Midazolam can be decreased when combined with Isavuconazonium. Approved, Investigational Isocarboxazid The therapeutic efficacy of Midazolam can be increased when used in combination with Isocarboxazid. Approved Isoflurane The risk or severity of adverse effects can be increased when Midazolam is combined with Isoflurane. Approved, Vet Approved Isoflurophate The serum concentration of Midazolam can be increased when it is combined with Isoflurophate. Approved, Investigational, Withdrawn Isradipine The metabolism of Midazolam can be decreased when combined with Isradipine. Approved, Investigational Itraconazole The serum concentration of Midazolam can be increased when it is combined with Itraconazole. Approved, Investigational Ivacaftor The serum concentration of Midazolam can be increased when it is combined with Ivacaftor. Approved Ixazomib The serum concentration of Midazolam can be increased when it is combined with Ixazomib. Approved, Investigational Josamycin The serum concentration of Midazolam can be increased when it is combined with Josamycin. Approved, Investigational Ketamine The risk or severity of adverse effects can be increased when Midazolam is combined with Ketamine. Approved, Vet Approved Ketazolam The risk or severity of adverse effects can be increased when Midazolam is combined with Ketazolam. Approved Ketobemidone The risk or severity of adverse effects can be increased when Midazolam is combined with Ketobemidone. Approved, Investigational Ketoconazole The serum concentration of Midazolam can be increased when it is combined with Ketoconazole. Approved, Investigational Kitasamycin The serum concentration of Midazolam can be increased when it is combined with Kitasamycin. Experimental Lamotrigine The risk or severity of adverse effects can be increased when Midazolam is combined with Lamotrigine. Approved, Investigational Ledipasvir The serum concentration of Ledipasvir can be decreased when it is combined with Midazolam. Approved Ledipasvir The serum concentration of Ledipasvir can be increased when it is combined with Midazolam. Approved Lepirudin The serum concentration of Midazolam can be increased when it is combined with Lepirudin. Approved Letaxaban The serum concentration of Midazolam can be increased when it is combined with Letaxaban. Investigational Levetiracetam The risk or severity of adverse effects can be increased when Midazolam is combined with Levetiracetam. Approved, Investigational Levobupivacaine The risk or severity of adverse effects can be increased when Midazolam is combined with Levobupivacaine. Approved, Investigational Levocabastine The risk or severity of adverse effects can be increased when Midazolam is combined with Levocabastine. Approved, Investigational Levocetirizine The risk or severity of adverse effects can be increased when Midazolam is combined with Levocetirizine. Approved Levodopa The risk or severity of adverse effects can be increased when Midazolam is combined with Levodopa. Approved Levomethadyl Acetate The risk or severity of adverse effects can be increased when Midazolam is combined with Levomethadyl Acetate. Approved, Investigational Levomilnacipran The risk or severity of adverse effects can be increased when Midazolam is combined with Levomilnacipran. Approved, Investigational Levorphanol The risk or severity of adverse effects can be increased when Midazolam is combined with Levorphanol. Approved Lidocaine The risk or severity of adverse effects can be increased when Midazolam is combined with Lidocaine. Approved, Vet Approved Linagliptin The serum concentration of Midazolam can be increased when it is combined with Linagliptin. Approved Lisinopril The serum concentration of Midazolam can be increased when it is combined with Lisinopril. Approved, Investigational Lisuride The risk or severity of adverse effects can be increased when Lisuride is combined with Midazolam. Approved, Investigational Lithium The risk or severity of adverse effects can be increased when Midazolam is combined with Lithium. Approved Lofentanil The risk or severity of adverse effects can be increased when Midazolam is combined with Lofentanil. Illicit Lopinavir The serum concentration of Midazolam can be increased when it is combined with Lopinavir. Approved Loprazolam The risk or severity of adverse effects can be increased when Midazolam is combined with Loprazolam. Experimental Loratadine The risk or severity of adverse effects can be increased when Midazolam is combined with Loratadine. Approved, Investigational Lorazepam The risk or severity of adverse effects can be increased when Lorazepam is combined with Midazolam. Approved Lormetazepam The risk or severity of adverse effects can be increased when Midazolam is combined with Lormetazepam. Approved Lorpiprazole The serum concentration of Midazolam can be increased when it is combined with Lorpiprazole. Approved Lovastatin The serum concentration of Lovastatin can be increased when it is combined with Midazolam. Approved, Investigational Loxapine The risk or severity of adverse effects can be increased when Loxapine is combined with Midazolam. Approved Luliconazole The serum concentration of Midazolam can be increased when it is combined with Luliconazole. Approved Lumacaftor The serum concentration of Midazolam can be decreased when it is combined with Lumacaftor. Approved Lurasidone The risk or severity of adverse effects can be increased when Midazolam is combined with Lurasidone. Approved, Investigational Lysergic Acid Diethylamide The risk or severity of adverse effects can be increased when Lysergic Acid Diethylamide is combined with Midazolam. Illicit, Investigational, Withdrawn Magnesium sulfate The therapeutic efficacy of Midazolam can be increased when used in combination with Magnesium sulfate. Approved, Investigational, Vet Approved Maprotiline The risk or severity of adverse effects can be increased when Midazolam is combined with Maprotiline. Approved, Investigational Mebicar The risk or severity of adverse effects can be increased when Midazolam is combined with Mebicar. Experimental Meclizine The risk or severity of adverse effects can be increased when Midazolam is combined with Meclizine. Approved Medazepam The risk or severity of adverse effects can be increased when Midazolam is combined with Medazepam. Experimental Medetomidine The risk or severity of adverse effects can be increased when Midazolam is combined with Medetomidine. Vet Approved Melagatran The serum concentration of Midazolam can be increased when it is combined with Melagatran. Experimental Melatonin The risk or severity of adverse effects can be increased when Midazolam is combined with Melatonin. Approved, Nutraceutical, Vet Approved Melperone The risk or severity of adverse effects can be increased when Midazolam is combined with Melperone. Approved, Investigational Mepivacaine The risk or severity of adverse effects can be increased when Midazolam is combined with Mepivacaine. Approved, Vet Approved Meprobamate The risk or severity of adverse effects can be increased when Meprobamate is combined with Midazolam. Approved, Illicit Meptazinol The risk or severity of adverse effects can be increased when Midazolam is combined with Meptazinol. Experimental Mesoridazine The risk or severity of adverse effects can be increased when Midazolam is combined with Mesoridazine. Approved, Investigational Metaxalone The risk or severity of adverse effects can be increased when Midazolam is combined with Metaxalone. Approved Metergoline The risk or severity of adverse effects can be increased when Metergoline is combined with Midazolam. Experimental Methadone Midazolam may increase the central nervous system depressant (CNS depressant) activities of Methadone. Approved Methadyl Acetate The risk or severity of adverse effects can be increased when Midazolam is combined with Methadyl Acetate. Approved, Illicit Methapyrilene The risk or severity of adverse effects can be increased when Midazolam is combined with Methapyrilene. Withdrawn Methaqualone The risk or severity of adverse effects can be increased when Midazolam is combined with Methaqualone. Illicit, Withdrawn Methocarbamol The risk or severity of adverse effects can be increased when Midazolam is combined with Methocarbamol. Approved, Vet Approved Methohexital The risk or severity of adverse effects can be increased when Methohexital is combined with Midazolam. Approved Methotrimeprazine Midazolam may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine. Approved, Investigational Methoxyflurane The risk or severity of adverse effects can be increased when Midazolam is combined with Methoxyflurane. Approved, Investigational, Vet Approved Methsuximide The risk or severity of adverse effects can be increased when Midazolam is combined with Methsuximide. Approved Methylecgonine The risk or severity of adverse effects can be increased when Midazolam is combined with Methylecgonine. Experimental Methylergometrine The risk or severity of adverse effects can be increased when Methylergometrine is combined with Midazolam. Approved Methylphenobarbital The risk or severity of adverse effects can be increased when Midazolam is combined with Methylphenobarbital. Approved Methysergide The risk or severity of adverse effects can be increased when Methysergide is combined with Midazolam. Approved Metyrosine Midazolam may increase the sedative activities of Metyrosine. Approved Mevastatin The serum concentration of Mevastatin can be increased when it is combined with Midazolam. Experimental Mifepristone The serum concentration of Midazolam can be increased when it is combined with Mifepristone. Approved, Investigational Milnacipran The risk or severity of adverse effects can be increased when Midazolam is combined with Milnacipran. Approved, Investigational Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Midazolam. Approved, Investigational Mirtazapine Midazolam may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine. Approved Mitotane The serum concentration of Midazolam can be decreased when it is combined with Mitotane. Approved Moexipril The serum concentration of Midazolam can be increased when it is combined with Moexipril. Approved Molindone The risk or severity of adverse effects can be increased when Midazolam is combined with Molindone. Approved Morphine The risk or severity of adverse effects can be increased when Morphine is combined with Midazolam. Approved, Investigational N-(3-Propylcarbamoyloxirane-2-Carbonyl)-Isoleucyl-Proline The serum concentration of Midazolam can be increased when it is combined with N-(3-Propylcarbamoyloxirane-2-Carbonyl)-Isoleucyl-Proline. Experimental Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Midazolam. Approved, Investigational Nafamostat The serum concentration of Midazolam can be increased when it is combined with Nafamostat. Approved, Investigational Nalbuphine The risk or severity of adverse effects can be increased when Midazolam is combined with Nalbuphine. Approved Naloxegol The serum concentration of Naloxegol can be increased when it is combined with Midazolam. Approved Nefazodone The metabolism of Midazolam can be decreased when combined with Nefazodone. Approved, Withdrawn Nelfinavir The serum concentration of Midazolam can be increased when it is combined with Nelfinavir. Approved Netupitant The serum concentration of Midazolam can be increased when it is combined with Netupitant. Approved, Investigational Nevirapine The metabolism of Midazolam can be increased when combined with Nevirapine. Approved Nicergoline The risk or severity of adverse effects can be increased when Nicergoline is combined with Midazolam. Approved, Investigational Nilotinib The metabolism of Midazolam can be decreased when combined with Nilotinib. Approved, Investigational Nintedanib The serum concentration of Nintedanib can be increased when it is combined with Midazolam. Approved Nitrazepam The risk or severity of adverse effects can be increased when Midazolam is combined with Nitrazepam. Approved Nitroaspirin The serum concentration of Midazolam can be increased when it is combined with Nitroaspirin. Investigational Nitrous oxide The risk or severity of adverse effects can be increased when Midazolam is combined with Nitrous oxide. Approved, Vet Approved Norflurane The risk or severity of adverse effects can be increased when Midazolam is combined with Norflurane. Approved, Investigational Normethadone The risk or severity of adverse effects can be increased when Midazolam is combined with Normethadone. Approved, Illicit Nortriptyline The risk or severity of adverse effects can be increased when Midazolam is combined with Nortriptyline. Approved Olanzapine The risk or severity of adverse effects can be increased when Midazolam is combined with Olanzapine. Approved, Investigational Olaparib The metabolism of Midazolam can be decreased when combined with Olaparib. Approved Oleandomycin The serum concentration of Midazolam can be increased when it is combined with Oleandomycin. Vet Approved Olopatadine The risk or severity of adverse effects can be increased when Midazolam is combined with Olopatadine. Approved Omapatrilat The serum concentration of Midazolam can be increased when it is combined with Omapatrilat. Investigational Ondansetron The risk or severity of adverse effects can be increased when Midazolam is combined with Ondansetron. Approved Opium The risk or severity of adverse effects can be increased when Midazolam is combined with Opium. Approved, Illicit Orphenadrine Midazolam may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine. Approved Osanetant The risk or severity of adverse effects can be increased when Midazolam is combined with Osanetant. Investigational Osimertinib The serum concentration of Midazolam can be increased when it is combined with Osimertinib. Approved Otamixaban The serum concentration of Midazolam can be increased when it is combined with Otamixaban. Investigational Oxazepam The risk or severity of adverse effects can be increased when Midazolam is combined with Oxazepam. Approved Oxethazaine The risk or severity of adverse effects can be increased when Midazolam is combined with Oxethazaine. Approved, Investigational Oxprenolol The risk or severity of adverse effects can be increased when Midazolam is combined with Oxprenolol. Approved Oxybuprocaine The risk or severity of adverse effects can be increased when Midazolam is combined with Oxybuprocaine. Approved, Investigational Oxycodone The risk or severity of adverse effects can be increased when Oxycodone is combined with Midazolam. Approved, Illicit, Investigational Oxymorphone The risk or severity of adverse effects can be increased when Midazolam is combined with Oxymorphone. Approved, Investigational, Vet Approved Palbociclib The serum concentration of Midazolam can be increased when it is combined with Palbociclib. Approved, Investigational Paliperidone The risk or severity of adverse effects can be increased when Midazolam is combined with Paliperidone. Approved Paraldehyde Midazolam may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde. Approved, Investigational Paroxetine The metabolism of Midazolam can be decreased when combined with Paroxetine. Approved, Investigational Pazopanib The serum concentration of Pazopanib can be increased when it is combined with Midazolam. Approved Penfluridol The risk or severity of adverse effects can be increased when Midazolam is combined with Penfluridol. Experimental Pentazocine The risk or severity of adverse effects can be increased when Pentazocine is combined with Midazolam. Approved, Vet Approved Pentobarbital The metabolism of Midazolam can be increased when combined with Pentobarbital. Approved, Investigational, Vet Approved Perampanel Perampanel may increase the central nervous system depressant (CNS depressant) activities of Midazolam. Approved Perazine The risk or severity of adverse effects can be increased when Midazolam is combined with Perazine. Approved, Investigational Pergolide The risk or severity of adverse effects can be increased when Pergolide is combined with Midazolam. Approved, Investigational, Vet Approved, Withdrawn Perindopril The serum concentration of Midazolam can be increased when it is combined with Perindopril. Approved Perospirone The risk or severity of adverse effects can be increased when Midazolam is combined with Perospirone. Approved Perphenazine The risk or severity of adverse effects can be increased when Midazolam is combined with Perphenazine. Approved Pethidine The risk or severity of adverse effects can be increased when Pethidine is combined with Midazolam. Approved Phenazocine The risk or severity of adverse effects can be increased when Midazolam is combined with Phenazocine. Experimental Phenibut The risk or severity of adverse effects can be increased when Midazolam is combined with Phenibut. Experimental Phenobarbital The metabolism of Midazolam can be increased when combined with Phenobarbital. Approved, Investigational Phenoperidine The risk or severity of adverse effects can be increased when Midazolam is combined with Phenoperidine. Experimental Phenoxyethanol The risk or severity of adverse effects can be increased when Midazolam is combined with Phenoxyethanol. Approved Phenytoin The serum concentration of Phenytoin can be increased when it is combined with Midazolam. Approved, Vet Approved Phosphoramidon The serum concentration of Midazolam can be increased when it is combined with Phosphoramidon. Experimental Pimozide The risk or severity of adverse effects can be increased when Midazolam is combined with Pimozide. Approved Pipamperone The risk or severity of adverse effects can be increased when Midazolam is combined with Pipamperone. Approved, Investigational Pipotiazine The risk or severity of adverse effects can be increased when Midazolam is combined with Pipotiazine. Approved, Investigational Piritramide The risk or severity of adverse effects can be increased when Midazolam is combined with Piritramide. Approved, Investigational Pitavastatin The serum concentration of Pitavastatin can be increased when it is combined with Midazolam. Approved Pitolisant The serum concentration of Midazolam can be decreased when it is combined with Pitolisant. Approved, Investigational Pizotifen The risk or severity of adverse effects can be increased when Midazolam is combined with Pizotifen. Approved Pomalidomide The risk or severity of adverse effects can be increased when Midazolam is combined with Pomalidomide. Approved Posaconazole The metabolism of Midazolam can be decreased when combined with Posaconazole. Approved, Investigational, Vet Approved Pramipexole Midazolam may increase the sedative activities of Pramipexole. Approved, Investigational Pramocaine The risk or severity of adverse effects can be increased when Midazolam is combined with Pramocaine. Approved Pravastatin The serum concentration of Pravastatin can be increased when it is combined with Midazolam. Approved Prazepam The risk or severity of adverse effects can be increased when Midazolam is combined with Prazepam. Approved, Illicit Pregabalin The therapeutic efficacy of Midazolam can be increased when used in combination with Pregabalin. Approved, Illicit, Investigational Prilocaine The risk or severity of adverse effects can be increased when Midazolam is combined with Prilocaine. Approved Primidone The metabolism of Midazolam can be increased when combined with Primidone. Approved, Vet Approved Prinomastat The serum concentration of Midazolam can be increased when it is combined with Prinomastat. Investigational Procaine The risk or severity of adverse effects can be increased when Midazolam is combined with Procaine. Approved, Investigational, Vet Approved Prochlorperazine The risk or severity of adverse effects can be increased when Prochlorperazine is combined with Midazolam. Approved, Vet Approved Promazine The risk or severity of adverse effects can be increased when Promazine is combined with Midazolam. Approved, Vet Approved Promethazine The risk or severity of adverse effects can be increased when Midazolam is combined with Promethazine. Approved, Investigational Propanidid The risk or severity of adverse effects can be increased when Midazolam is combined with Propanidid. Experimental Proparacaine The risk or severity of adverse effects can be increased when Midazolam is combined with Proparacaine. Approved, Vet Approved Propofol The serum concentration of Propofol can be increased when it is combined with Midazolam. Approved, Investigational, Vet Approved Propoxycaine The risk or severity of adverse effects can be increased when Midazolam is combined with Propoxycaine. Approved Protriptyline The risk or severity of adverse effects can be increased when Midazolam is combined with Protriptyline. Approved Proxibarbal The risk or severity of adverse effects can be increased when Midazolam is combined with Proxibarbal. Experimental Prucalopride The serum concentration of Prucalopride can be increased when it is combined with Midazolam. Approved PSD502 The risk or severity of adverse effects can be increased when Midazolam is combined with PSD502. Investigational Quazepam The serum concentration of Midazolam can be increased when it is combined with Quazepam. Approved, Illicit Quetiapine The risk or severity of adverse effects can be increased when Midazolam is combined with Quetiapine. Approved Quinapril The serum concentration of Midazolam can be increased when it is combined with Quinapril. Approved, Investigational Quinisocaine The risk or severity of adverse effects can be increased when Midazolam is combined with Quinisocaine. Experimental Racecadotril The serum concentration of Midazolam can be increased when it is combined with Racecadotril. Investigational Raclopride The risk or severity of adverse effects can be increased when Midazolam is combined with Raclopride. Investigational Ramelteon The risk or severity of adverse effects can be increased when Midazolam is combined with Ramelteon. Approved, Investigational Ramipril The serum concentration of Midazolam can be increased when it is combined with Ramipril. Approved Ranolazine The serum concentration of Ranolazine can be increased when it is combined with Midazolam. Approved, Investigational Remifentanil The risk or severity of adverse effects can be increased when Midazolam is combined with Remifentanil. Approved Remikiren The serum concentration of Midazolam can be increased when it is combined with Remikiren. Approved Remoxipride The risk or severity of adverse effects can be increased when Midazolam is combined with Remoxipride. Approved, Withdrawn Reserpine The risk or severity of adverse effects can be increased when Reserpine is combined with Midazolam. Approved, Investigational Ribociclib The serum concentration of Midazolam can be increased when it is combined with Ribociclib. Approved, Investigational Rifabutin The metabolism of Midazolam can be increased when combined with Rifabutin. Approved, Investigational Rifampicin The metabolism of Midazolam can be increased when combined with Rifampicin. Approved Rifapentine The metabolism of Midazolam can be increased when combined with Rifapentine. Approved, Investigational Rifaximin The serum concentration of Rifaximin can be increased when it is combined with Midazolam. Approved, Investigational Rilpivirine The serum concentration of Rilpivirine can be increased when it is combined with Midazolam. Approved Risperidone The risk or severity of adverse effects can be increased when Midazolam is combined with Risperidone. Approved, Investigational Ritanserin The risk or severity of adverse effects can be increased when Midazolam is combined with Ritanserin. Investigational Ritonavir The serum concentration of Midazolam can be increased when it is combined with Ritonavir. Approved, Investigational Rivaroxaban The serum concentration of Midazolam can be increased when it is combined with Rivaroxaban. Approved Romifidine The risk or severity of adverse effects can be increased when Midazolam is combined with Romifidine. Vet Approved Ropinirole Midazolam may increase the sedative activities of Ropinirole. Approved, Investigational Ropivacaine The risk or severity of adverse effects can be increased when Midazolam is combined with Ropivacaine. Approved Rosuvastatin The serum concentration of Rosuvastatin can be increased when it is combined with Midazolam. Approved Rotigotine Midazolam may increase the sedative activities of Rotigotine. Approved Rucaparib The metabolism of Midazolam can be decreased when combined with Rucaparib. Approved, Investigational Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Midazolam. Approved S-3304 The serum concentration of Midazolam can be increased when it is combined with S-3304. Investigational Saquinavir The serum concentration of Midazolam can be increased when it is combined with Saquinavir. Approved, Investigational Sarilumab The therapeutic efficacy of Midazolam can be decreased when used in combination with Sarilumab. Approved, Investigational Saxagliptin The serum concentration of Midazolam can be increased when it is combined with Saxagliptin. Approved Scopolamine The risk or severity of adverse effects can be increased when Midazolam is combined with Scopolamine. Approved, Investigational Secobarbital The risk or severity of adverse effects can be increased when Secobarbital is combined with Midazolam. Approved, Vet Approved Sepranolone The risk or severity of adverse effects can be increased when Midazolam is combined with Sepranolone. Investigational Sertindole The risk or severity of adverse effects can be increased when Midazolam is combined with Sertindole. Approved, Investigational, Withdrawn Sertraline The metabolism of Midazolam can be decreased when combined with Sertraline. Approved Sevoflurane The risk or severity of adverse effects can be increased when Midazolam is combined with Sevoflurane. Approved, Vet Approved Sildenafil The metabolism of Midazolam can be decreased when combined with Sildenafil. Approved, Investigational Silodosin The serum concentration of Silodosin can be increased when it is combined with Midazolam. Approved Siltuximab The serum concentration of Midazolam can be decreased when it is combined with Siltuximab. Approved, Investigational Simeprevir The serum concentration of Midazolam can be increased when it is combined with Simeprevir. Approved Simvastatin The serum concentration of Simvastatin can be increased when it is combined with Midazolam. Approved Sitagliptin The serum concentration of Midazolam can be increased when it is combined with Sitagliptin. Approved, Investigational Sivelestat The serum concentration of Midazolam can be increased when it is combined with Sivelestat. Investigational Sodium oxybate Midazolam may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate. Approved Sofosbuvir The serum concentration of Sofosbuvir can be decreased when it is combined with Midazolam. Approved Solithromycin The serum concentration of Midazolam can be increased when it is combined with Solithromycin. Investigational Sorafenib The metabolism of Midazolam can be decreased when combined with Sorafenib. Approved, Investigational Spirapril The serum concentration of Midazolam can be increased when it is combined with Spirapril. Approved St. John's Wort The serum concentration of Midazolam can be decreased when it is combined with St. John's Wort. Approved, Investigational, Nutraceutical Stiripentol The serum concentration of Midazolam can be increased when it is combined with Stiripentol. Approved Sufentanil The risk or severity of adverse effects can be increased when Midazolam is combined with Sufentanil. Approved, Investigational Sulfisoxazole The metabolism of Midazolam can be decreased when combined with Sulfisoxazole. Approved, Vet Approved Sulpiride The risk or severity of adverse effects can be increased when Midazolam is combined with Sulpiride. Approved, Investigational Sultopride The risk or severity of adverse effects can be increased when Midazolam is combined with Sultopride. Experimental Suvorexant Midazolam may increase the central nervous system depressant (CNS depressant) activities of Suvorexant. Approved, Investigational Tandospirone The risk or severity of adverse effects can be increased when Midazolam is combined with Tandospirone. Investigational Tapentadol Tapentadol may increase the central nervous system depressant (CNS depressant) activities of Midazolam. Approved Tasimelteon The risk or severity of adverse effects can be increased when Midazolam is combined with Tasimelteon. Approved, Investigational Teduglutide The serum concentration of Midazolam can be increased when it is combined with Teduglutide. Approved Telaprevir The serum concentration of Midazolam can be increased when it is combined with Telaprevir. Approved, Withdrawn Telithromycin The serum concentration of Midazolam can be increased when it is combined with Telithromycin. Approved Temazepam The risk or severity of adverse effects can be increased when Temazepam is combined with Midazolam. Approved, Investigational Temocapril The serum concentration of Midazolam can be increased when it is combined with Temocapril. Experimental, Investigational Terguride The risk or severity of adverse effects can be increased when Terguride is combined with Midazolam. Experimental Tetrabenazine The risk or severity of adverse effects can be increased when Midazolam is combined with Tetrabenazine. Approved, Investigational Tetracaine The risk or severity of adverse effects can be increased when Midazolam is combined with Tetracaine. Approved, Vet Approved Tetrahydropalmatine The risk or severity of adverse effects can be increased when Midazolam is combined with Tetrahydropalmatine. Investigational Tetrodotoxin The risk or severity of adverse effects can be increased when Midazolam is combined with Tetrodotoxin. Investigational Thalidomide Midazolam may increase the central nervous system depressant (CNS depressant) activities of Thalidomide. Approved, Investigational, Withdrawn Theophylline The therapeutic efficacy of Midazolam can be decreased when used in combination with Theophylline. Approved Thiamylal The risk or severity of adverse effects can be increased when Midazolam is combined with Thiamylal. Approved, Vet Approved Thiopental The risk or severity of adverse effects can be increased when Midazolam is combined with Thiopental. Approved, Vet Approved Thioridazine The risk or severity of adverse effects can be increased when Thioridazine is combined with Midazolam. Approved, Withdrawn Thiorphan The serum concentration of Midazolam can be increased when it is combined with Thiorphan. Experimental Thiotepa The metabolism of Midazolam can be decreased when combined with Thiotepa. Approved, Investigational Thiothixene The risk or severity of adverse effects can be increased when Midazolam is combined with Thiothixene. Approved Tiagabine The risk or severity of adverse effects can be increased when Midazolam is combined with Tiagabine. Approved, Investigational Tiapride The risk or severity of adverse effects can be increased when Midazolam is combined with Tiapride. Approved, Investigational Ticlopidine The metabolism of Midazolam can be decreased when combined with Ticlopidine. Approved Tiletamine The risk or severity of adverse effects can be increased when Midazolam is combined with Tiletamine. Vet Approved Tilidine The risk or severity of adverse effects can be increased when Midazolam is combined with Tilidine. Experimental Tipranavir The serum concentration of Midazolam can be increased when it is combined with Tipranavir. Approved, Investigational Tizanidine The risk or severity of adverse effects can be increased when Midazolam is combined with Tizanidine. Approved, Investigational Tocilizumab The serum concentration of Midazolam can be decreased when it is combined with Tocilizumab. Approved Tolcapone The risk or severity of adverse effects can be increased when Midazolam is combined with Tolcapone. Approved, Withdrawn Tolvaptan The serum concentration of Tolvaptan can be increased when it is combined with Midazolam. Approved Topiramate The risk or severity of adverse effects can be increased when Midazolam is combined with Topiramate. Approved Topotecan The serum concentration of Topotecan can be increased when it is combined with Midazolam. Approved, Investigational Tramadol The risk or severity of adverse effects can be increased when Tramadol is combined with Midazolam. Approved, Investigational Trandolapril The serum concentration of Midazolam can be increased when it is combined with Trandolapril. Approved Tranylcypromine The risk or severity of adverse effects can be increased when Midazolam is combined with Tranylcypromine. Approved, Investigational Trazodone The risk or severity of adverse effects can be increased when Midazolam is combined with Trazodone. Approved, Investigational Triazolam The risk or severity of adverse effects can be increased when Midazolam is combined with Triazolam. Approved, Investigational Tricaine methanesulfonate The risk or severity of adverse effects can be increased when Midazolam is combined with Tricaine methanesulfonate. Vet Approved Trichloroethylene The risk or severity of adverse effects can be increased when Midazolam is combined with Trichloroethylene. Approved Trifluoperazine The risk or severity of adverse effects can be increased when Midazolam is combined with Trifluoperazine. Approved, Investigational Trifluperidol The risk or severity of adverse effects can be increased when Midazolam is combined with Trifluperidol. Experimental Triflupromazine The risk or severity of adverse effects can be increased when Midazolam is combined with Triflupromazine. Approved, Vet Approved Trimipramine The risk or severity of adverse effects can be increased when Midazolam is combined with Trimipramine. Approved Triprolidine The risk or severity of adverse effects can be increased when Midazolam is combined with Triprolidine. Approved Tylosin The serum concentration of Midazolam can be increased when it is combined with Tylosin. Vet Approved Ubenimex The serum concentration of Midazolam can be increased when it is combined with Ubenimex. Experimental, Investigational Ulinastatin The serum concentration of Midazolam can be increased when it is combined with Ulinastatin. Investigational Valproic Acid The risk or severity of adverse effects can be increased when Midazolam is combined with Valproic Acid. Approved, Investigational Vemurafenib The serum concentration of Midazolam can be increased when it is combined with Vemurafenib. Approved Venlafaxine The metabolism of Midazolam can be decreased when combined with Venlafaxine. Approved Veralipride The risk or severity of adverse effects can be increased when Midazolam is combined with Veralipride. Experimental Verapamil The metabolism of Midazolam can be decreased when combined with Verapamil. Approved Vigabatrin The risk or severity of adverse effects can be increased when Midazolam is combined with Vigabatrin. Approved Vildagliptin The serum concentration of Midazolam can be increased when it is combined with Vildagliptin. Approved, Investigational Vincristine The serum concentration of Vincristine can be decreased when it is combined with Midazolam. Approved, Investigational Vinyl ether The risk or severity of adverse effects can be increased when Midazolam is combined with Vinyl ether. Experimental Voriconazole The metabolism of Midazolam can be decreased when combined with Voriconazole. Approved, Investigational Vortioxetine The risk or severity of adverse effects can be increased when Midazolam is combined with Vortioxetine. Approved, Investigational Xenon The risk or severity of adverse effects can be increased when Midazolam is combined with Xenon. Experimental Ximelagatran The serum concentration of Midazolam can be increased when it is combined with Ximelagatran. Approved, Investigational, Withdrawn Xylazine The risk or severity of adverse effects can be increased when Midazolam is combined with Xylazine. Vet Approved Yohimbine The therapeutic efficacy of Midazolam can be decreased when used in combination with Yohimbine. Approved, Investigational, Vet Approved Z-Val-Ala-Asp fluoromethyl ketone The serum concentration of Midazolam can be increased when it is combined with Z-Val-Ala-Asp fluoromethyl ketone. Experimental Zaleplon The risk or severity of adverse effects can be increased when Midazolam is combined with Zaleplon. Approved, Illicit, Investigational Ziconotide The risk or severity of adverse effects can be increased when Midazolam is combined with Ziconotide. Approved Zimelidine The risk or severity of adverse effects can be increased when Midazolam is combined with Zimelidine. Withdrawn Ziprasidone The metabolism of Midazolam can be decreased when combined with Ziprasidone. Approved Zofenopril The serum concentration of Midazolam can be increased when it is combined with Zofenopril. Experimental Zolazepam The risk or severity of adverse effects can be increased when Midazolam is combined with Zolazepam. Vet Approved Zolpidem Midazolam may increase the central nervous system depressant (CNS depressant) activities of Zolpidem. Approved Zonisamide The risk or severity of adverse effects can be increased when Midazolam is combined with Zonisamide. Approved, Investigational Zopiclone The risk or severity of adverse effects can be increased when Midazolam is combined with Zopiclone. Approved Zotepine The risk or severity of adverse effects can be increased when Midazolam is combined with Zotepine. Approved, Investigational, Withdrawn Zuclopenthixol The 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
- 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]
- 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]
- 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]
- 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]
- 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
- Download (73.7 KB)
Clinical Trials
- Clinical Trials
Pharmacoeconomics
- Manufacturers
- Apothecon inc div bristol myers squibb
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- Baxter healthcare corp anesthesia and critical care
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- Packagers
- Akorn Inc.
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- A-S Medication Solutions LLC
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- Baxter International Inc.
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- Dispensing Solutions
- Ebewe Pharma
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- Dosage forms
Form Route Strength Liquid Intramuscular; Intravenous 1 mg Liquid Intramuscular; Intravenous 5 mg Solution Buccal 10 mg Solution Buccal 2.5 mg Solution Buccal 5 mg Solution Buccal 7.5 mg Injection, solution Intramuscular; Intravenous 10 mg/2mL Injection, solution Intramuscular; Intravenous 2 mg/2mL Injection, solution Intravenous .5 mg/mL Injection, solution Intravenous 1 mg/mL Injection Intramuscular; Intravenous 1 mg/mL Injection Intramuscular; Intravenous 10 mg/2mL Injection Intramuscular; Intravenous 2 mg/2mL Injection Intramuscular; Intravenous 5 mg/mL Injection, solution Intramuscular; Intravenous 1 mg/mL Injection, solution Intramuscular; Intravenous 5 mg/mL Syrup Oral 10 mg/5mL Syrup Oral 2 mg/mL Solution Intramuscular; Intravenous 1 mg Solution Intramuscular; Intravenous 5 mg - Prices
Unit description Cost Unit Midazolam 5 mg/ml 3.9USD ml Midazolam-nacl 2 mg/ml inj 2.31USD ml Midazolam hcl 5 mg/ml vial 1.18USD ml Midazolam-nacl 1 mg/ml inj 1.13USD ml Midazolam hcl 2 mg/ml syrup 1.08USD ml Midazolam 1 mg/ml isecure syr 0.73USD ml Midazolam hcl 1 mg/ml vial 0.26USD ml DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 159 °C PhysProp water solubility 0.024 mg/mL Thorsteinn Loftsson and Dagný Hreinsdóttir, 2006 - Predicted Properties
Property Value Source Water Solubility 0.00987 mg/mL ALOGPS logP 3.89 ALOGPS logP 3.33 ChemAxon logS -4.5 ALOGPS pKa (Strongest Basic) 6.57 ChemAxon Physiological Charge 0 ChemAxon Hydrogen Acceptor Count 2 ChemAxon Hydrogen Donor Count 0 ChemAxon Polar Surface Area 30.18 Å2 ChemAxon Rotatable Bond Count 1 ChemAxon Refractivity 99.43 m3·mol-1 ChemAxon Polarizability 32.7 Å3 ChemAxon Number of Rings 4 ChemAxon Bioavailability 1 ChemAxon Rule of Five Yes ChemAxon Ghose Filter Yes ChemAxon Veber's Rule Yes ChemAxon MDDR-like Rule No ChemAxon - Predicted ADMET features
Property Value Probability Human Intestinal Absorption + 1.0 Blood Brain Barrier + 0.9724 Caco-2 permeable + 0.8866 P-glycoprotein substrate Non-substrate 0.5074 P-glycoprotein inhibitor I Inhibitor 0.5587 P-glycoprotein inhibitor II Inhibitor 0.8388 Renal organic cation transporter Inhibitor 0.7476 CYP450 2C9 substrate Non-substrate 0.7366 CYP450 2D6 substrate Non-substrate 0.9116 CYP450 3A4 substrate Substrate 0.7194 CYP450 1A2 substrate Inhibitor 0.8586 CYP450 2C9 inhibitor Inhibitor 0.7132 CYP450 2D6 inhibitor Non-inhibitor 0.6887 CYP450 2C19 inhibitor Inhibitor 0.6554 CYP450 3A4 inhibitor Non-inhibitor 0.5214 CYP450 inhibitory promiscuity High CYP Inhibitory Promiscuity 0.9001 Ames test Non AMES toxic 0.8024 Carcinogenicity Non-carcinogens 0.7703 Biodegradation Not ready biodegradable 1.0 Rat acute toxicity 3.1488 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9827 hERG inhibition (predictor II) Non-inhibitor 0.7379
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
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
- Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090]
- 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
- Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090]
- 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
- Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090]
- 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
- Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090]
- 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
- Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090]
- 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
- Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090]
- 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
- Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090]
- 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
- Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090]
- 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
- Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090]
- 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
- Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090]
- 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
- Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090]
- 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
- Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090]
- 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
- Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090]
- 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
- Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090]
- 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
- Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090]
- 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
- Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090]
- 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
- Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090]
- 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
- Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090]
- 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
- Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090]
- 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
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- 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
- 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]
- 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]
- 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]
- 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]
- 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]
- 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]
- 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]
- 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
- 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]
- 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]
- 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]
- 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]
- Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- 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
- 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]
- 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]
- 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]
- 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]
- 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
- 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]
- 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]
- 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
- 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
- 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
- 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
- SubstrateInhibitorInducer
- 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
- 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]
- 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]
- 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]
- 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]
- 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]
- 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]
- 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
- 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 April 23, 2018 23:02