Identification

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

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

Structure
Thumb
Synonyms
  • Buccolam
  • Dormicum
  • Midazolam
  • Midazolamum
External IDs
Dea No. 2884 / Ro 21-3981/001 / Ro 21-3981/003
Product Ingredients
IngredientUNIICASInChI Key
Midazolam HydrochlorideW7TTW573JJ59467-96-8PLYSCVSCYOQVRP-UHFFFAOYSA-N
Midazolam maleate77520S18SE59467-94-6XYGVIBXOJOOCFR-BTJKTKAUSA-N
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
BuccolamSolution5 mgBuccalShire Services Bvba2011-09-05Not applicableEu
BuccolamSolution10 mgBuccalShire Services Bvba2011-09-05Not applicableEu
BuccolamSolution7.5 mgBuccalShire Services Bvba2011-09-05Not applicableEu
BuccolamSolution2.5 mgBuccalShire Services Bvba2011-09-05Not applicableEu
Midazolam InjectionSolution1 mgIntramuscular; IntravenousMylan PharmaceuticalsNot applicableNot applicableCanada
Midazolam InjectionSolution1 mgIntramuscular; IntravenousSandoz Canada Incorporated1999-07-21Not applicableCanada
Midazolam InjectionSolution1 mgIntramuscular; IntravenousFresenius Kabi2001-03-26Not applicableCanada
Midazolam InjectionSolution1 mgIntramuscular; IntravenousNovopharm Limited2001-12-17Not applicableCanada
Midazolam InjectionSolution5 mgIntramuscular; IntravenousPfizer2015-03-31Not applicableCanada
Midazolam InjectionLiquid5 mgIntramuscular; IntravenousFresenius Kabi2001-03-26Not applicableCanada
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-midazolam Injectable 1 mg/mlLiquid1 mgIntramuscular; IntravenousApotex Corporation2001-04-102013-08-02Canada
Apo-midazolam Injectable 5 mg/mlLiquid5 mgIntramuscular; IntravenousApotex Corporation2001-04-102013-08-02Canada
MidazolamInjection, solution2 mg/2mLIntramuscular; IntravenousFresenius Kabi2014-10-03Not applicableUs
MidazolamInjection1 mg/1mLIntramuscular; IntravenousBedford Pharmaceuticals2000-06-212013-06-30Us
MidazolamInjection, solution5 mg/1mLIntramuscular; IntravenousHF Acquisition Co LLC, DBA HealthFirst2018-09-16Not applicableUs
MidazolamInjection, solution5 mg/1mLIntramuscular; IntravenousAlvogen, Inc.2017-08-11Not applicableUs
MidazolamInjection5 mg/1mLIntramuscular; IntravenousA-S Medication Solutions2000-06-20Not applicableUs
MidazolamInjection5 mg/1mLIntramuscular; IntravenousGeneral Injectables & Vaccines2017-11-28Not applicableUs
MidazolamInjection, solution5 mg/1mLIntramuscular; IntravenousSagent Pharmaceuticals2012-03-19Not applicableUs
MidazolamInjection, solution5 mg/1mLIntramuscular; IntravenousSagent Pharmaceuticals2012-03-19Not applicableUs
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
Midazolam HClMidazolam Hydrochloride (0.5 mg/1mL)Injection, solutionIntravenousCantrell Drug Company2014-09-03Not applicableUs
Midazolam HClMidazolam Hydrochloride (1 mg/1mL)Injection, solutionIntravenousCantrell Drug Company2013-06-28Not applicableUs
International/Other Brands
Anquil (General Pharma) / Benzosed (Pharmaceutical) / Dalam (Richmond) / Damizol (Specifar) / Demizolam (Dem Ilaç) / Doricum (Roche) / Dormicum (Roche) / Dormid (Scott) / Dormipron (Chalver) / Dormire (Cristália) / Dormitol (Square) / Dormixal (Demo) / Dormonid (Roche) / Drimnorth (Northia) / Epistatus (IFET) / Flormidal (Galenika) / Fulsed (Ranbaxy) / Fulsed Injection (Terapia) / Garen (Bio-Pharma) / Gobbizolam (Gobbi) / Hipnazolam (EMS) / Hipnoz (Pharos) / Hypnofast (Incepta) / Hypnovel (Roche) / Ipnovel (Roche) / Nocturna (Lafi) / Setam (Rimsa) / Talentum (Fisiopharma) / Terap (Sanitas) / Versed (Roche)
Categories
UNII
R60L0SM5BC
CAS number
59467-70-8
Weight
Average: 325.767
Monoisotopic: 325.078203343
Chemical Formula
C18H13ClFN3
InChI Key
DDLIGBOFAVUZHB-UHFFFAOYSA-N
InChI
InChI=1S/C18H13ClFN3/c1-11-21-9-13-10-22-18(14-4-2-3-5-16(14)20)15-8-12(19)6-7-17(15)23(11)13/h2-9H,10H2,1H3
IUPAC Name
12-chloro-9-(2-fluorophenyl)-3-methyl-2,4,8-triazatricyclo[8.4.0.0²,⁶]tetradeca-1(10),3,5,8,11,13-hexaene
SMILES
CC1=NC=C2CN=C(C3=CC=CC=C3F)C3=C(C=CC(Cl)=C3)N12

Pharmacology

Indication

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

Associated Conditions
Associated Therapies
Pharmacodynamics

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

Mechanism of action

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

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

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

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

97% protein bound.

Metabolism

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

Route of elimination

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

Half life

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

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

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

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

Interactions

Drug Interactions
DrugInteraction
(R)-warfarinThe metabolism of Midazolam can be decreased when combined with (R)-warfarin.
(S)-WarfarinThe metabolism of Midazolam can be decreased when combined with (S)-Warfarin.
16-BromoepiandrosteroneThe metabolism of Midazolam can be decreased when combined with 16-Bromoepiandrosterone.
2,5-Dimethoxy-4-ethylthioamphetamineThe risk or severity of adverse effects can be increased when Midazolam is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
3-isobutyl-1-methyl-7H-xanthineThe therapeutic efficacy of Midazolam can be decreased when used in combination with 3-isobutyl-1-methyl-7H-xanthine.
3,4-MethylenedioxyamphetamineThe risk or severity of adverse effects can be increased when Midazolam is combined with 3,4-Methylenedioxyamphetamine.
3,5-diiodothyropropionic acidThe metabolism of Midazolam can be decreased when combined with 3,5-diiodothyropropionic acid.
4-Bromo-2,5-dimethoxyamphetamineThe risk or severity of adverse effects can be increased when Midazolam is combined with 4-Bromo-2,5-dimethoxyamphetamine.
4-hydroxycoumarinThe metabolism of 4-hydroxycoumarin can be decreased when combined with Midazolam.
4-MethoxyamphetamineThe risk or severity of adverse effects can be increased when Midazolam is combined with 4-Methoxyamphetamine.
Food Interactions
  • Grapefruit juice slows the product's absorption and significantly increases its bioavailability.

References

Synthesis Reference

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

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

Clinical Trials
PhaseStatusPurposeConditionsCount
0CompletedPreventionDepression1
0CompletedTreatmentAnxiety Disease1
0CompletedTreatmentBipolar I Disorder / Bipolar II Disorder / Depression, Bipolar / Major Depressive Disorder (MDD) / Suicidal Ideation1
0RecruitingTreatmentCancers / Ketamine / Tiredness1
0RecruitingTreatmentMidazolam Overdose1
0RecruitingTreatmentSedation, Conscious1
1Active Not RecruitingBasic ScienceHealthy Volunteers1
1Active Not RecruitingBasic ScienceNash1
1Active Not RecruitingBasic ScienceNeoplasms Metastasis1
1Active Not RecruitingOtherBiological Availability1
1Active Not RecruitingOtherLeukemia, Lymphocytic, Chronic, B-Cell1
1Active Not RecruitingOtherNeoplasms1
1Active Not RecruitingTreatmentAdvanced Non-Central Nervous System (CNS) Malignancies1
1Active Not RecruitingTreatmentCancer of the Ovary / Carcinoid tumour of the gastrointestinal tract / Colorectal Cancers / Head and Neck Carcinoma / Islet Cell Tumor / Lung Cancers / Metastatic Cancers / Neuroendocrine Carcinoma of the Skin / Pheochromocytomas / Sarcomas / Unspecified Adult Solid Tumor, Protocol Specific1
1Active Not RecruitingTreatmentDrug Interaction Potential1
1Active Not RecruitingTreatmentEpidermal Growth Factor Receptor Mutations / Lung Cancer Non-Small Cell Cancer (NSCLC)1
1Active Not RecruitingTreatmentMultiple Myeloma (MM)1
1Active Not RecruitingTreatmentNon-Hodgkin's Lymphoma (NHL) / Non-Hodgkin's Lymphoma, Solid Cancers / Solid Cancers1
1Active Not RecruitingTreatmentTumors1
1CompletedNot AvailableHealthy Volunteers10
1CompletedNot AvailableHealthy Volunteers / Pharmacokinetics of ASP015K and Midazolam1
1CompletedNot AvailableHealthy Volunteers / Pharmacokinetics of Isavuconazole / Pharmacokinetics of Midazolam1
1CompletedNot AvailableHepatitis C Viral Infection1
1CompletedNot AvailableHuman Immunodeficiency Virus Infection(HIV)/Acquired Immunodeficiency Syndrome (AIDS)1
1CompletedNot AvailablePain, Chronic1
1CompletedNot AvailablePharmacokinetic Interactions1
1CompletedNot AvailableSchizophrenia Patients1
1CompletedBasic ScienceAlzheimer's Disease (AD) / Metabolism1
1CompletedBasic ScienceAtopic Dermatitis (AD)1
1CompletedBasic ScienceDiabetes Mellitus (DM) / Glucose Metabolism Disorders / Type 2 Diabetes Mellitus1
1CompletedBasic ScienceDrug Biotransformation / Membrane Transport1
1CompletedBasic ScienceDrug Interactions1
1CompletedBasic ScienceEndometriosis1
1CompletedBasic ScienceGenotype-related Drug Metabolism1
1CompletedBasic ScienceHealthy Adult Subjects and Healthy Elderly Subjects1
1CompletedBasic ScienceHealthy Adult Volunteers1
1CompletedBasic ScienceHealthy Male Volunteers1
1CompletedBasic ScienceHealthy Participants1
1CompletedBasic ScienceHealthy Volunteers16
1CompletedBasic ScienceHealthy Volunteers / Human Immunodeficiency Virus (HIV) Infections1
1CompletedBasic ScienceHealthy Volunteers / Pharmacologic Actions1
1CompletedBasic ScienceModerate to Severe Plaque Psoriasis1
1CompletedBasic SciencePharmacokinetic Assessments in Healthy Volunteers1
1CompletedBasic ScienceRheumatoid Arthritis3
1CompletedBasic ScienceType 2 Diabetes Mellitus1
1CompletedBasic ScienceVA Drug Interactions / VA Drug Interactions [VA Drug Interaction]1
1CompletedDiagnosticCytochrome / Pharmacokinetics1
1CompletedDiagnosticDigestive System Disorders1
1CompletedDiagnosticDrug Interactions1
1CompletedDiagnosticHealthy Volunteers2
1CompletedHealth Services ResearchHealthy Volunteers1
1CompletedOtherALK-positive Advanced Tumors1
1CompletedOtherAdvanced Solid Tumors1
1CompletedOtherDrug Interactions / Healthy Volunteers1
1CompletedOtherHealthy Volunteers4
1CompletedOtherHealthy Volunteers / Rheumatoid Arthritis1
1CompletedOtherProstatic Neoplasms1
1CompletedOtherTumors, Solid1
1CompletedTreatmentAcute Myocardial Infarction (AMI) / Pain1
1CompletedTreatmentAdult Solid Neoplasm1
1CompletedTreatmentAdvanced Solid Tumors, Excluding Breast Cancer1
1CompletedTreatmentAmnesia-Memory Loss / Memory Losses1
1CompletedTreatmentAnemias / Healthy Volunteers1
1CompletedTreatmentAtherosclerosis1
1CompletedTreatmentBacterial Infections / Pneumonia / Skin Diseases, Infectious1
1CompletedTreatmentCancers1
1CompletedTreatmentCancers / Neoplasms, Breast1
1CompletedTreatmentCarcinoma NOS / Hodgkins Disease (HD) / Lymphoma, Large-Cell, Anaplastic / Neoplasms / Non-Hodgkin's Lymphoma (NHL)1
1CompletedTreatmentCastration Resistant Prostate Cancer (CRPC) / Pharmacokinetics of MDV31001
1CompletedTreatmentChemotherapy-Induced Nausea and Vomiting (CINV) / Post-Operative Nausea and Vomiting (PONV)1
1CompletedTreatmentChronic Hepatitis C Virus (HCV) Infection1
1CompletedTreatmentCrohn's Disease (CD)1
1CompletedTreatmentDepressive Disorders / Healthy Volunteers1
1CompletedTreatmentDrug Interaction Potentiation3
1CompletedTreatmentDrug Interactions2
1CompletedTreatmentDrug reactions1
1CompletedTreatmentHealthy Male Volunteers1
1CompletedTreatmentHealthy Volunteers25
1CompletedTreatmentHealthy Volunteers / Psoriasis1
1CompletedTreatmentHeart Failure, Unspecified1
1CompletedTreatmentImpaired Renal Function1
1CompletedTreatmentInfectious Diseases1
1CompletedTreatmentInfluenza in Humans1
1CompletedTreatmentJapanese Healthy Adult Males1
1CompletedTreatmentLow Back Pain (LBP)1
1CompletedTreatmentNeoplasms1
1CompletedTreatmentPostmenopausal Osteoporosis (PMO)1
1CompletedTreatmentPsoriasis2
1CompletedTreatmentRelapsed or Refractory Advanced Cancer1
1CompletedTreatmentSchizophrenia or Schizoaffective Disorder1
1CompletedTreatmentSeizures1
1CompletedTreatmentSkin Diseases, Bacterial1
1CompletedTreatmentTuberculosis1
1CompletedTreatmentTuberculosis / Tuberculosis, Pulmonary2
1CompletedTreatmentTumors, Solid2
1CompletedTreatmentType 2 Diabetes Mellitus2
1CompletedTreatmentCMET-dysregulated Advanced Solid Tumors1
1Not Yet RecruitingOtherCarcinoma, Advanced ALK+ or ROS1+Non-Small-Cell Lung, Neoplasm, Advanced ALK+ or ROS1+Solid Tumors1
1Not Yet RecruitingOtherHealthy Volunteers1
1Not Yet RecruitingTreatmentAtopic Dermatitis (AD)1
1Not Yet RecruitingTreatmentHeathy Volunteer1
1RecruitingBasic ScienceHealthy Volunteers1
1RecruitingOtherCrohn's Disease (CD)1
1RecruitingOtherDepression, Bipolar / Major Depressive Episode / Unipolar Depression1
1RecruitingOtherHealthy Volunteers1
1RecruitingOtherPhase 11
1RecruitingTreatmentAmyotrophic Lateral Sclerosis (ALS)1
1RecruitingTreatmentCancer, Advanced / Colorectal Cancers / Metastatic Melanoma / Metastatic Non-Small Cell Lung Cancer / Metastatic Pancreatic Ductal Adenocarcinoma1
1RecruitingTreatmentCancer, Advanced / Lung Cancer Non-Small Cell Cancer (NSCLC) / Mesothelioma, Malignant / Metastatic Breast Cancer (MBC) / Metastatic Cancers / Non-Hodgkin's Lymphoma (NHL)1
1RecruitingTreatmentHealthy Volunteers1
1RecruitingTreatmentHepatitis B Chronic Infection1
1RecruitingTreatmentTumors, Solid1
1TerminatedBasic ScienceCancer, Advanced1
1TerminatedOtherDepression / Depressive Disorder, Recurrent / Major Depressive Disorder (MDD) / Relapses1
1TerminatedOtherHealthy Volunteers3
1TerminatedOtherPsoriasis Vulgaris (Plaque Psoriasis)1
1TerminatedTreatmentCervical Pain1
1TerminatedTreatmentEpilepsies1
1TerminatedTreatmentHealthy Volunteers1
1WithdrawnTreatmentHealthy Volunteers2
1, 2Active Not RecruitingTreatmentBipolar Disorder (BD) / Major Depressive Episode / Suicidal Ideation1
1, 2CompletedPreventionPost Operative Pain1
1, 2CompletedTreatmentShock, Septic1
1, 2RecruitingTreatmentCoughing1
1, 2RecruitingTreatmentDisseminated Sclerosis / Tiredness1
1, 2TerminatedPreventionSepsis1
1, 2TerminatedTreatmentDependence, Cocaine1
1, 2TerminatedTreatmentObsessive Compulsive Disorder (OCD)1
2Active Not RecruitingTreatmentObsessive-Compulsive Disorder (OCD)1
2CompletedPreventionForearm Surgeries1
2CompletedSupportive CareChildren1
2CompletedSupportive CareDental Anxiety1
2CompletedTreatmentAnxiety Disorders / Depression / PTSD / Stress Disorders, Post-Traumatic1
2CompletedTreatmentChildren Requiring Sedation to Facilitate Laceration Repair1
2CompletedTreatmentEndoscopy / Procedural Sedation1
2CompletedTreatmentMajor Depressive Disorder (MDD) / Treatment Resistant Depression (TRD)1
2CompletedTreatmentPain1
2CompletedTreatmentSeizures1
2CompletedTreatmentTreatment Resistant Depression (TRD)1
2Not Yet RecruitingTreatmentMajor Depressive Episode1
2RecruitingDiagnosticDelayed Recovery From Anaesthesia1
2RecruitingPreventionSedation During Spinal Anesthesia1
2RecruitingSupportive CareCancer of the Breast / Cancer, Breast / Malignant Neoplasm of Female Breast1
2RecruitingTreatmentAdministration and Dosage of Ketamine / Endoscopic Sedation1
2RecruitingTreatmentBipolar Disorder (BD)1
2RecruitingTreatmentBorderline Personality Disorder (BPD)1
2RecruitingTreatmentKetamine / Violent Aggressive Behavior1
2RecruitingTreatmentMajor Depressive Disorder (MDD)1
2RecruitingTreatmentMajor depressive disorder, recurrent episode1
2RecruitingTreatmentObsessive-Compulsive Disorder (OCD)1
2RecruitingTreatmentPosttraumatic Stress Disorders1
2RecruitingTreatmentSubarachnoid Haemorrhage (SAH)1
2TerminatedTreatmentFeeling Anxious / Pain1
2Unknown StatusPreventionAdenoidectomy / Otorhinolaryngologic Surgical Procedures / Postoperative Care / Postoperative pain / Surgical Procedures, Operative / Tonsillectomy1
2Unknown StatusSupportive CareIntracranial Hemorrhages / Ischemia, Brain / Strokes / Vasospasm, Intracranial1
2Unknown StatusTreatmentPost Dural Puncture Headache1
2WithdrawnDiagnosticComputerized tomography / Procedural Sedation / Traumatic Brain Injury (TBI)1
2WithdrawnSupportive CareDelirium / Dyspnea / Nausea / Pain Intractable1
2, 3CompletedPreventionDiagnostic Esophagogastroduodenoscopy1
2, 3CompletedTreatmentAnaesthesia therapy1
2, 3CompletedTreatmentAnalgesia, Patient-Controlled / Spinal Stenosis1
2, 3CompletedTreatmentChronic Otitis Media1
2, 3CompletedTreatmentColonoscopy / Colorectal Polyps1
2, 3CompletedTreatmentCritical Illness1
2, 3CompletedTreatmentDental Anxiety / Impacted Third Molar Tooth1
2, 3CompletedTreatmentMajor depressive disorder, recurrent episode1
2, 3CompletedTreatmentPostoperative pain1
2, 3CompletedTreatmentSedation therapy1
2, 3Not Yet RecruitingTreatmentAcute Ischemic Stroke (AIS)1
2, 3Not Yet RecruitingTreatmentDepression / Pain, Acute1
2, 3Not Yet RecruitingTreatmentTreatment Resistant Depression (TRD)1
2, 3RecruitingTreatmentAnalgesia, Postoperative1
2, 3RecruitingTreatmentFeeling Anxious / Post-Operative Nausea and Vomiting (PONV) / Postoperative pain1
2, 3RecruitingTreatmentPosttraumatic Stress Disorder (PTSD)1
2, 3WithdrawnTreatmentPTSD1
3CompletedNot AvailableChronic Renal Failure (CRF) / Hip Fractures1
3CompletedDiagnosticCancer, Breast1
3CompletedPreventionEmergence Delirium1
3CompletedPreventionHigh Blood Pressure (Hypertension)1
3CompletedPreventionPost-operative Pain for Total Knee Arthroplasty1
3CompletedSupportive CareColonoscopy1
3CompletedSupportive CareEpilepsies / Hydrocephaly1
3CompletedTreatmentAcute Traumatic Pain1
3CompletedTreatmentAnaesthesia therapy1
3CompletedTreatmentBronchoscopy1
3CompletedTreatmentChild's Anxiety / Parental/Caregiver Anxiety1
3CompletedTreatmentColonoscopy1
3CompletedTreatmentContinuous Sedation in Initially Sedated Adults in ICU1
3CompletedTreatmentDental Anxiety1
3CompletedTreatmentFracture Bone1
3CompletedTreatmentPaediatric Outpatient Surgery1
3CompletedTreatmentPediatric Status Epilepticus1
3CompletedTreatmentSedation therapy1
3Not Yet RecruitingTreatmentAnaesthesia therapy / Shock, Septic1
3RecruitingSupportive CareFluoride Poisoning / Hepatic Function / Poisoning by Inhaled Anaesthetic / Recovery From Sedation / Renal Function1
3RecruitingTreatmentBreech Presentation1
3RecruitingTreatmentFeeling Anxious / Peripheral Nerve Blocks1
3RecruitingTreatmentInflammatory Reaction / Neurocostal neuralgia / Pain, Chronic1
3RecruitingTreatmentInguinal Hernias / Local Anesthesia / Sedation, Conscious1
3RecruitingTreatmentLiver Cirrhosis1
3RecruitingTreatmentSedation in Intensive Care1
3RecruitingTreatmentTreatment Resistant Depressive Disorder1
3TerminatedTreatmentAcute Agitated Patients1
3TerminatedTreatmentAnxiety Disorders / Dementias / Depression / Psychosomatic Disorders / Schizophrenic Disorders1
3TerminatedTreatmentEpilepsies1
3TerminatedTreatmentTraumatic Brain Injury (TBI)1
3Unknown StatusSupportive CareSedation therapy1
3Unknown StatusTreatmentIntubation Complications1
4Active Not RecruitingSupportive CareEpilepsies / Metabolic Diseases / Traumas1
4Active Not RecruitingSupportive CareFeeling Anxious / Laceration1
4Active Not RecruitingTreatmentAcute Lung Injury (ALI) / Acute Respiratory Distress Syndrome (ARDS) / Critical Illness / Sleep1
4Active Not RecruitingTreatmentDriving Performance After Minor Ambulatory Surgery / Minor Surgical Procedures With Monitored Anesthesia Care1
4Active Not RecruitingTreatmentEffect of Sedation on Heart Rate Variability1
4CompletedNot AvailableDisorders of Gallbladder, Biliary Tract and Pancrease1
4CompletedNot AvailableFailed Moderate Sedation During Procedure1
4CompletedBasic ScienceAnalgesic Drugs / Antinociceptive Agents1
4CompletedBasic SciencePharmacokinetics1
4CompletedBasic ScienceRejection, Transplant1
4CompletedDiagnosticAlteration of Cognitive Function / Gastrointestinal Dysfunction1
4CompletedPreventionAdenotonsillectomy1
4CompletedPreventionAdrenocortical Deficiency / Hemodynamics Instability1
4CompletedPreventionCognitive Impairments1
4CompletedPreventionDelirium1
4CompletedPreventionDelirium on Emergence / Inhalational Anesthetics Adverse Reaction / Strabismus Following Ocular Surgery1
4CompletedPreventionDisease, Chronic1
4CompletedPreventionElective Orthopedic Surgery1
4CompletedPreventionEmergence Agitation1
4CompletedPreventionPatients Undergoing Puncture of the Bone Marrow1
4CompletedPreventionPremedication1
4CompletedSupportive CareAnesthesia; Reaction1
4CompletedSupportive CareEndoscopy1
4CompletedSupportive CareHypothermia1
4CompletedSupportive CareIBS / Malignant Neoplasm of Colon / Polyps1
4CompletedSupportive CareInfertilities1
4CompletedSupportive CareIntubation; Difficult1
4CompletedTreatmentAbscesses / Pain1
4CompletedTreatmentAcute Respiratory Distress Syndrome (ARDS)1
4CompletedTreatmentAggressive Behavior / Depression / Feeling Anxious / Postoperative Period / Tiredness1
4CompletedTreatmentAnaesthesia / Premedication1
4CompletedTreatmentBrain Diseases1
4CompletedTreatmentBronchoscopy1
4CompletedTreatmentCataracts / Phacoemulsification1
4CompletedTreatmentChild Behavior / Conscious Sedation Failure During Procedure / Dental Decay1
4CompletedTreatmentChild Behavior / Dental Decay1
4CompletedTreatmentCholangiocarcinomas / Choledocholithiasis / Malignant Neoplasm of Pancreas / Pancreatitis1
4CompletedTreatmentColonoscopy / Sedation, Conscious1
4CompletedTreatmentComplications1
4CompletedTreatmentConscious Sedation Failure During Procedure1
4CompletedTreatmentCoronary Artery Disease1
4CompletedTreatmentDiagnostic Colonoscopy Screening1
4CompletedTreatmentDrug Safety / Procedural Sedation1
4CompletedTreatmentEarly Childhood Caries1
4CompletedTreatmentEfficacy and Safety of Mivacurium Chloride for Pediatric Patients1
4CompletedTreatmentEndoscopy1
4CompletedTreatmentEndoscopy, Gastrointestinal / Moderate Sedation / Propofol / Target Controlled Infusion (TCI)1
4CompletedTreatmentEndoscopy / Inflammatory Bowel Diseases (IBD) / Sedation therapy1
4CompletedTreatmentEndoscopy / Sedation therapy1
4CompletedTreatmentFailed Moderate Sedation During Procedure1
4CompletedTreatmentFailed Moderate Sedation During Procedure / Minimally Conscious State1
4CompletedTreatmentFeeling Anxious3
4CompletedTreatmentFeeling Anxious / Hepatitis, Chronic / Liver Cirrhosis1
4CompletedTreatmentFeeling Anxious / Laceration1
4CompletedTreatmentFeeling Anxious / Nausea / Pain1
4CompletedTreatmentCaudal epidural block therapy / Forearm Injuries / Orthopedic Procedures / Traumas / Upper Extremity1
4CompletedTreatmentGastrointestinal Stroma Tumors / Lung Cancer Non-Small Cell Cancer (NSCLC) / Renal-cell Cancer1
4CompletedTreatmentHealthy Volunteers / Human Immunodeficiency Virus (HIV) Infections1
4CompletedTreatmentHernia1
4CompletedTreatmentInadequate or Impaired Respiratory Function / Pain1
4CompletedTreatmentIntraoperative Analgesic Use / Postcraniotomy Headache / Postoperative Analgesic Use / Postoperative Complications1
4CompletedTreatmentKetamine Induced Agitation1
4CompletedTreatmentLung Cancers1
4CompletedTreatmentComputerized tomography / MRI of liver / Ultrasound1
4CompletedTreatmentMajor Depressive Disorder (MDD)1
4CompletedTreatmentMajor Depressive Disorder (MDD) / Suicidal Ideation1
4CompletedTreatmentMechanically Ventilated and Intubated Subjects1
4CompletedTreatmentOsteoarthritis (OA)1
4CompletedTreatmentOther Surgical Procedures1
4CompletedTreatmentOxidative Stress / Sedation therapy1
4CompletedTreatmentProcedural Sedation1
4CompletedTreatmentProstate Cancer1
4CompletedTreatmentSedation therapy2
4CompletedTreatmentSedation, Conscious1
4CompletedTreatmentSepsis / Shock, Septic / Systemic Inflammatory Response Syndrome (SIRS)1
4CompletedTreatmentSleep Quality of Patients Undergoing TURP1
4CompletedTreatmentSuicidal Ideation1
4CompletedTreatmentTerminal Cancer1
4Enrolling by InvitationTreatmentAnesthesia Complication / Hemodynamics Instability / Ileus paralytic / Nausea / Postoperative pain / Vomiting1
4Enrolling by InvitationTreatmentComplications / Delirium / Ventilations, Mechanical1
4Not Yet RecruitingNot AvailableChildren / Dormicum / Sedation, Conscious1
4Not Yet RecruitingPreventionCritical Illness1
4Not Yet RecruitingPreventionInhalation Anesthesia1
4Not Yet RecruitingSupportive CareBronchoscopy1
4Not Yet RecruitingTreatmentAcute Pulmonary Edema1
4Not Yet RecruitingTreatmentEmergency / Procedural anxiety1
4Not Yet RecruitingTreatmentPostoperative pain1
4Not Yet RecruitingTreatmentPreanesthetic Medication1
4Not Yet RecruitingTreatmentSafety and Efficacy of Intranasal Dexmedetomidine1
4RecruitingBasic ScienceSevere Sepsis1
4RecruitingBasic ScienceType 2 Diabetes Mellitus1
4RecruitingDiagnosticCopeptin / Preanesthetic Medication1
4RecruitingDiagnosticLiver Diseases1
4RecruitingHealth Services ResearchGeneral Surgery / Sedation therapy1
4RecruitingOtherAnaesthesia therapy1
4RecruitingOtherLumbar Punctures / Minor Incision Drainage of Abscesses Not Requiring Extensive Debridement / Sedation, Conscious / Simple Lacerations Less Than 4 cm1
4RecruitingTreatmentAcute Agitation, Behavioural Emergency1
4RecruitingTreatmentAnxiety Disorders / Major Depressive Disorder (MDD)1
4RecruitingTreatmentBladder Tumors / Postoperative Cognitive Dysfunction1
4RecruitingTreatmentCritical Illness / Deep Sedation / Ventilators, Mechanical1
4RecruitingTreatmentCrohn's Disease (CD) / Ulcerative Colitis (UC)1
4RecruitingTreatmentDexmedetomidine / Mechanically Ventilated Sedated Patients / Midazolam / Sedation therapy / Ventilations, Mechanical1
4RecruitingTreatmentFeeling Anxious / Pediatric ALL / Procedural anxiety1
4RecruitingTreatmentFlexible Bronchoscopy / Safety / Satisfaction / Sedation therapy1
4RecruitingTreatmentKnee Injuries1
4RecruitingTreatmentLaceration of Skin1
4RecruitingTreatmentPatients Requiring Diagnostic Gastroscopy Suitable for Sedation / Patients Requiring Diagnostic Gastroscopy With Sedation1
4RecruitingTreatmentSedation in Intensive Care Unit Patients1
4RecruitingTreatmentSedation therapy1
4RecruitingTreatmentSeizures1
4RecruitingTreatmentShock, Septic1
4TerminatedTreatmentAnaesthesia therapy1
4TerminatedTreatmentCritical Illness / Ventilations, Mechanical1
4TerminatedTreatmentFeeling Anxious1
4TerminatedTreatmentOrthopedic Procedures / Procedural Sedation / Regional Anesthesia Block1
4TerminatedTreatmentTraumatic Brain Injury (TBI)1
4Unknown StatusNot AvailableObesity, Morbid1
4Unknown StatusBasic ScienceHyperalgesia4
4Unknown StatusPreventionAnaesthetic Preconditioning / Myocardial Injury1
4Unknown StatusPreventionDelirium1
4Unknown StatusPreventionSedative Withdrawal Delirium1
4Unknown StatusTreatmentAnaesthesia therapy / Hemodynamics / Oxidative Stress1
4Unknown StatusTreatmentAnalgesia, Patient-Controlled / Arthroplasty / Gastric Resection1
4Unknown StatusTreatmentCongenital Choledochal Cyst / Congenital Hydronephrosis / Fracture Bone1
4Unknown StatusTreatmentConscious Sedation Failure During Procedure1
4Unknown StatusTreatmentDelirium1
4Unknown StatusTreatmentDexmedetomidine / Mechanically Ventilated Patients / Midazolam / Sedation therapy1
4Unknown StatusTreatmentEmergency1
4Unknown StatusTreatmentFailed Conscious Sedation During Procedure1
4Unknown StatusTreatmentHepatic Encephalopathy1
4Unknown StatusTreatmentInflammatory Disorder of Immune System / Sepsis1
4Unknown StatusTreatmentLaceration1
4Unknown StatusTreatmentLaryngoscopy / Preanesthetic Medication1
4Unknown StatusTreatmentLiver Cirrhosis1
4Unknown StatusTreatmentMechanical Ventilation Complication1
4Unknown StatusTreatmentSafety of Dexmedetomidine Sedation1
4Unknown StatusTreatmentTraumatic Brain Injury (TBI)1
4Unknown StatusTreatmentAdjunct to general anesthesia therapy1
4WithdrawnPreventionC.Surgical Procedure; Cardiac / Delirium1
4WithdrawnSupportive CareAlcoholism / Respiration, Artificial1
4WithdrawnTreatmentPostoperative pain1
4WithdrawnTreatmentSleep1
Not AvailableActive Not RecruitingNot AvailableAAT Deficiency / AATD / Alpha-1 Antitrypsin Deficiency / Fibrosis, Liver1
Not AvailableActive Not RecruitingNot AvailableAortic Valve Stenosis1
Not AvailableActive Not RecruitingNot AvailablePostoperative Cognitive Dysfunction1
Not AvailableActive Not RecruitingTreatmentIntubated Requiring Sedation for Greater Than 48 Hours1
Not AvailableActive Not RecruitingTreatmentPulmonary Diseases1
Not AvailableCompletedNot AvailableAnaesthesia therapy1
Not AvailableCompletedNot AvailableClinical Indications for Transesophageal Echocardiography1
Not AvailableCompletedNot AvailableDexmedetomidine / Endoscopy, Gastrointestinal / Sedation therapy1
Not AvailableCompletedNot AvailableEarly Gastric Cancer / Gastric Adenoma1
Not AvailableCompletedNot AvailableFeeling Anxious / Satisfaction / Sedation therapy / Tolerance1
Not AvailableCompletedNot AvailableMidazolam1
Not AvailableCompletedNot AvailablePain1
Not AvailableCompletedNot AvailablePharmacokinetics / Voriconazole1
Not AvailableCompletedNot AvailablePsychomotor Agitation1
Not AvailableCompletedNot AvailableRhytidoplasty1
Not AvailableCompletedBasic ScienceCritical Care / Deep Sedation / Sedation, Conscious1
Not AvailableCompletedBasic ScienceDrug-Drug Interaction (DDI) / Healthy Volunteers1
Not AvailableCompletedBasic ScienceHealthy Volunteers1
Not AvailableCompletedBasic SciencePharmacokinetics1
Not AvailableCompletedBasic ScienceSaccadic Eye Movements1
Not AvailableCompletedDiagnosticConscious Sedation Failure During Procedure1
Not AvailableCompletedDiagnosticEGD Procedure1
Not AvailableCompletedDiagnosticPain1
Not AvailableCompletedDiagnosticSacroiliac Joint Pain / Sympathetically Maintained Pain1
Not AvailableCompletedOtherEndobronchial Ultrasound Guided Transbronchial Needle Aspiration1
Not AvailableCompletedPreventionAkathisia1
Not AvailableCompletedPreventionAnesthesia Morbidity / Children / Delirium on Emergence1
Not AvailableCompletedPreventionGeneral Surgery1
Not AvailableCompletedPreventionGeneral Surgery / Prostate Cancer1
Not AvailableCompletedPreventionPediatric Emergence Agitation and Pain1
Not AvailableCompletedPreventionPost-Operative Nausea and Vomiting (PONV)1
Not AvailableCompletedPreventionPsychomotor Agitation1
Not AvailableCompletedSupportive CareAnaesthesia therapy / Body Temperature Changes1
Not AvailableCompletedSupportive CareCancers1
Not AvailableCompletedSupportive CareFeeling Anxious1
Not AvailableCompletedSupportive CareFeeling Anxious / Pain1
Not AvailableCompletedSupportive CareLiver Cirrhosis1
Not AvailableCompletedSupportive CarePre Operative Anxiety1
Not AvailableCompletedSupportive CareTransient Hypertension1
Not AvailableCompletedTreatmentAnaesthesia therapy1
Not AvailableCompletedTreatmentAnxiety Preoperative / Midazolam Premedication / Premedication1
Not AvailableCompletedTreatmentBasal Cell Carcinoma (BCC) / Feeling Anxious / Skin Cancers / Squamous Cell Carcinoma (SCC)1
Not AvailableCompletedTreatmentChronic Lung Diseases1
Not AvailableCompletedTreatmentCritical Illness1
Not AvailableCompletedTreatmentEchocardiography, Transesophageal1
Not AvailableCompletedTreatmentEndoscopy / Sedation therapy1
Not AvailableCompletedTreatmentFeeling Anxious1
Not AvailableCompletedTreatmentFeeling Anxious / Pain, Acute1
Not AvailableCompletedTreatmentFractures, Compression1
Not AvailableCompletedTreatmentHemodynamics After Spinal Anesthesia1
Not AvailableCompletedTreatmentIntubations1
Not AvailableCompletedTreatmentOther Surgical Procedures1
Not AvailableCompletedTreatmentPostoperative Cognitive Functions1
Not AvailableCompletedTreatmentPsychomotor Agitation1
Not AvailableCompletedTreatmentRespiration Disorders1
Not AvailableCompletedTreatmentSedation in Critically Ill COPD Patients1
Not AvailableCompletedTreatmentSedation, Bronchoscopy1
Not AvailableCompletedTreatmentSepsis / Shock1
Not AvailableCompletedTreatmentSepsis / Traumas1
Not AvailableCompletedTreatmentStress, Psychological1
Not AvailableEnrolling by InvitationOtherIntestinal Microbiota / Ventilations, Mechanical1
Not AvailableEnrolling by InvitationTreatmentVirtual Reality1
Not AvailableNot Yet RecruitingNot AvailableDrug Effect1
Not AvailableNot Yet RecruitingNot AvailablePostoperative pain1
Not AvailableNot Yet RecruitingBasic ScienceSedation therapy1
Not AvailableNot Yet RecruitingDevice FeasibilitySedation therapy / Spinal Anaesthesia1
Not AvailableNot Yet RecruitingPreventionTonsillitis1
Not AvailableNot Yet RecruitingTreatmentAtherosclerosis / Coronary Artery Disease / Feeling Anxious / Pain, Acute / Vasospasm;Peripheral / Virtual Reality1
Not AvailableNot Yet RecruitingTreatmentBrachial Plexus Block / Shoulder Dislocation1
Not AvailableNot Yet RecruitingTreatmentHypercatabolism / Sedative, Hypnotic, or Anxiolytic Use Disorders1
Not AvailableNot Yet RecruitingTreatmentIntra-nasal Delevery Device / Procedural Sedation1
Not AvailableNot Yet RecruitingTreatmentObesity, Morbid1
Not AvailableRecruitingNot AvailableAcute Bacterial Exacerbation of Chronic Bronchitis (ABECB) / Acute Bacterial Sinusitis (ABS) / Acute Decompensated Heart Failure (ADHF) / Acute Pyelonephritis / Adenovirus / Adjunct to general anesthesia therapy / Adrenal Insufficiency / Airway Swelling / Anaesthesia therapy / Anxiolysis / Arterial Hypotension / Autism, Early Infantile / Autistic Disorder / Bartonellosis / Benzodiazepine Withdrawal / Benzodiazepines / Bipolar Disorder (BD) / Bloodstream Infections / Bone and Joint Infections / Brain Swelling / Bronchospasm / Brucellosis / Cardiac Arrest / Central Nervous System Infections / Cholera / Chronic Bacterial Prostatitis / Community Acquired Pneumonia (CAP) / Complicated Urinary Tract Infections / Convulsions / Cyanide Poisoning / Cytomegalovirus Retinitis / Drug hypersensitivity reaction / Early-onset Schizophrenia Spectrum Disorders / Edema / Epilepsies / Feeling Anxious / Flu caused by Influenza / Gastroparesis / Gynaecological infection / Headaches / Herpes Simplex Virus / High Blood Pressure (Hypertension) / High Cholesterol / Hospital-acquired bacterial pneumonia / Hyperlipidemias / Infantile Hemangiomas / Infection NOS / Inflammatory Conditions / Inflammatory Reaction / Influenza Treatment or Prophylaxis / Inhalational Anthrax (Post-Exposure) / Intra-Abdominal Infections / Life-threatening Fungal Infections / Lower Respiratory Tract Infection (LRTI) / Meningitis, Bacterial / Migraines / Muscle Spasms / Nausea / Opioid Addiction / Pain / Plague / Pneumonia / Prophylaxis / Psittacosis / Q Fever / Reflux / Relapsing Fever / Rocky Mountain Spotted Fever / Schizophrenic Disorders / Sedation therapy / Seizures / Sepsis / Skeletal Muscle Spasms / Skin and Subcutaneous Tissue Bacterial Infections / Skin Structures and Soft Tissue Infections / Stable Angina (SA) / Thromboprophylaxis / Thrombosis / Trachoma / Treatment-resistant Schizophrenia / Tularemia / Typhus Fever / Uncomplicated Skin and Skin Structure Infections / Uncomplicated Urinary Tract Infections / Urinary Tract Infections (UTIs) / Vomiting / Withdrawal1
Not AvailableRecruitingNot AvailableAnaesthesia therapy1
Not AvailableRecruitingNot AvailableCerebral Ischemia-Hypoxia1
Not AvailableRecruitingNot AvailableDepression1
Not AvailableRecruitingNot AvailableGliomas1
Not AvailableRecruitingBasic ScienceAmnesia / Anaesthesia therapy / Anesthetics / Pain / Sedation, Conscious1
Not AvailableRecruitingDiagnosticVentricular Tachycardia (VT)1
Not AvailableRecruitingHealth Services ResearchSedation therapy1
Not AvailableRecruitingOtherSedation therapy / Spinal Anaesthesia1
Not AvailableRecruitingPreventionIntubation; Difficult or Failed1
Not AvailableRecruitingPreventionPeripheral Obliterative Arteriopathy1
Not AvailableRecruitingPreventionPost-Operative Nausea and Vomiting (PONV)1
Not AvailableRecruitingTreatmentAcute Respiratory Failure1
Not AvailableRecruitingTreatmentAnoxic Encephalopathy / Cardiac Arrest / Refractory seizure disorders1
Not AvailableRecruitingTreatmentBronchoscopy / Sedation therapy1
Not AvailableRecruitingTreatmentChildren Under General Anaesthesia1
Not AvailableRecruitingTreatmentColonoscopy1
Not AvailableRecruitingTreatmentExtrusion of Tooth1
Not AvailableRecruitingTreatmentMajor Depressive Disorder (MDD)1
Not AvailableRecruitingTreatmentMajor Depressive Disorder (MDD) / Severe Depression / Treatment Resistant Depression (TRD)1
Not AvailableRecruitingTreatmentPostoperative Pain Control / Wrist Injury1
Not AvailableRecruitingTreatmentTonsillectomy1
Not AvailableSuspendedTreatmentPaediatric Flexible Bronchoscopy1
Not AvailableTerminatedNot AvailableVesicoureteral Reflux1
Not AvailableTerminatedOtherChronic Alcoholism1
Not AvailableTerminatedTreatmentBMI >30 kg/m2 / Sleep Apnea, Obstructive1
Not AvailableTerminatedTreatmentBipolar Disorder (BD)1
Not AvailableTerminatedTreatmentRespiratory Failure1
Not AvailableUnknown StatusNot AvailableFunctional disorders of the biliary tract / Pancreatic Diseases1
Not AvailableUnknown StatusBasic SciencePhobic Disorders1
Not AvailableUnknown StatusPreventionCystoscopy1
Not AvailableUnknown StatusScreeningAnesthesia Recovery Period / Delirium, Dementia, Cognitive Disorders / Mental Competency / Neurobehavioural Manifestation1
Not AvailableUnknown StatusSupportive CareDiverticulosis, Colonic / Malignant Neoplasm of Colon / Rectal Carcinoma1
Not AvailableUnknown StatusSupportive CarePacemaker Implantation / Pain1
Not AvailableUnknown StatusSupportive CareSleeplessness1
Not AvailableUnknown StatusTreatmentAcute Agitation1
Not AvailableUnknown StatusTreatmentAnaesthesia therapy1
Not AvailableUnknown StatusTreatmentBronchoscopy; / Central Airway Stenosis / Interventional; / Noninvasive Positive Pressure Ventilation / Sedation therapy1
Not AvailableUnknown StatusTreatmentLiver Diseases1
Not AvailableWithdrawnNot AvailableTraumas1

Pharmacoeconomics

Manufacturers
  • Apothecon inc div bristol myers squibb
  • App pharmaceuticals llc
  • Astrazeneca pharmaceuticals lp
  • Baxter healthcare corp anesthesia and critical care
  • Baxter healthcare corp anesthesia critical care
  • Bedford laboratories div ben venue laboratories inc
  • Ben venue laboratories inc
  • Claris lifesciences ltd
  • Hospira inc
  • International medicated systems ltd
  • International medication systems ltd
  • Taylor pharmaceuticals
  • Wockhardt ltd
  • Hlr technology
  • Apotex inc richmond hill
  • Hi tech pharmacal co inc
  • Paddock laboratories inc
  • Ranbaxy laboratories ltd
  • Roxane laboratories inc
  • Hoffmann la roche inc
Packagers
  • Akorn Inc.
  • APP Pharmaceuticals
  • A-S Medication Solutions LLC
  • B&B Pharmaceuticals
  • Baxter International Inc.
  • Bedford Labs
  • Ben Venue Laboratories Inc.
  • Cardinal Health
  • Cura Pharmaceutical Co. Inc.
  • Dispensing Solutions
  • Ebewe Pharma
  • Hi Tech Pharmacal Co. Inc.
  • Hospira Inc.
  • Mikart Inc.
  • Novex Pharma
  • Paddock Labs
  • Patheon Inc.
  • Pharmedium
  • Physicians Total Care Inc.
  • Ranbaxy Laboratories
  • Roxane Labs
  • Wockhardt Ltd.
Dosage forms
FormRouteStrength
LiquidIntramuscular; Intravenous1 mg
LiquidIntramuscular; Intravenous5 mg
SolutionBuccal10 mg
SolutionBuccal2.5 mg
SolutionBuccal5 mg
SolutionBuccal7.5 mg
Injection, solutionIntramuscular; Intravenous10 mg/2mL
Injection, solutionIntramuscular; Intravenous2 mg/2mL
Injection, solutionIntravenous0.5 mg/1mL
Injection, solutionIntravenous1 mg/1mL
InjectionIntramuscular; Intravenous1 mg/1mL
InjectionIntramuscular; Intravenous10 mg/2mL
InjectionIntramuscular; Intravenous2 mg/2mL
InjectionIntramuscular; Intravenous5 mg/1mL
Injection, solutionIntramuscular; Intravenous1 mg/1mL
Injection, solutionIntramuscular; Intravenous5 mg/1mL
SyrupOral10 mg/5mL
SyrupOral2 mg/1mL
SolutionIntramuscular; Intravenous1 mg
SolutionIntramuscular; Intravenous5 mg
Injection, solutionIntramuscular5 mg/1mL
Prices
Unit descriptionCostUnit
Midazolam 5 mg/ml3.9USD ml
Midazolam-nacl 2 mg/ml inj2.31USD ml
Midazolam hcl 5 mg/ml vial1.18USD ml
Midazolam-nacl 1 mg/ml inj1.13USD ml
Midazolam hcl 2 mg/ml syrup1.08USD ml
Midazolam 1 mg/ml isecure syr0.73USD ml
Midazolam hcl 1 mg/ml vial0.26USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

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

Spectra

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

Taxonomy

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

Targets

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

Enzymes

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

Transporters

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
Inducer
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. Schuetz EG, Beck WT, Schuetz JD: Modulators and substrates of P-glycoprotein and cytochrome P4503A coordinately up-regulate these proteins in human colon carcinoma cells. Mol Pharmacol. 1996 Feb;49(2):311-8. [PubMed:8632764]
  2. Katoh M, Nakajima M, Yamazaki H, Yokoi T: Inhibitory effects of CYP3A4 substrates and their metabolites on P-glycoprotein-mediated transport. Eur J Pharm Sci. 2001 Feb;12(4):505-13. [PubMed:11231118]
  3. Schwab D, Fischer H, Tabatabaei A, Poli S, Huwyler J: Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery. J Med Chem. 2003 Apr 24;46(9):1716-25. [PubMed:12699389]
  4. Takano M, Hasegawa R, Fukuda T, Yumoto R, Nagai J, Murakami T: Interaction with P-glycoprotein and transport of erythromycin, midazolam and ketoconazole in Caco-2 cells. Eur J Pharmacol. 1998 Oct 9;358(3):289-94. [PubMed:9822896]
  5. Kim RB, Wandel C, Leake B, Cvetkovic M, Fromm MF, Dempsey PJ, Roden MM, Belas F, Chaudhary AK, Roden DM, Wood AJ, Wilkinson GR: Interrelationship between substrates and inhibitors of human CYP3A and P-glycoprotein. Pharm Res. 1999 Mar;16(3):408-14. [PubMed:10213372]
  6. Polli JW, Wring SA, Humphreys JE, Huang L, Morgan JB, Webster LO, Serabjit-Singh CS: Rational use of in vitro P-glycoprotein assays in drug discovery. J Pharmacol Exp Ther. 2001 Nov;299(2):620-8. [PubMed:11602674]
  7. Mahar Doan KM, Humphreys JE, Webster LO, Wring SA, Shampine LJ, Serabjit-Singh CJ, Adkison KK, Polli JW: Passive permeability and P-glycoprotein-mediated efflux differentiate central nervous system (CNS) and non-CNS marketed drugs. J Pharmacol Exp Ther. 2002 Dec;303(3):1029-37. [PubMed:12438524]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Secondary active organic cation transmembrane transporter activity
Specific Function
Translocates a broad array of organic cations with various structures and molecular weights including the model compounds 1-methyl-4-phenylpyridinium (MPP), tetraethylammonium (TEA), N-1-methylnico...
Gene Name
SLC22A1
Uniprot ID
O15245
Uniprot Name
Solute carrier family 22 member 1
Molecular Weight
61153.345 Da
References
  1. Zhang L, Schaner ME, Giacomini KM: Functional characterization of an organic cation transporter (hOCT1) in a transiently transfected human cell line (HeLa). J Pharmacol Exp Ther. 1998 Jul;286(1):354-61. [PubMed:9655880]
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Substrate
General Function
Transporter activity
Specific Function
Involved in the ATP-dependent secretion of bile salts into the canaliculus of hepatocytes.
Gene Name
ABCB11
Uniprot ID
O95342
Uniprot Name
Bile salt export pump
Molecular Weight
146405.83 Da
References
  1. Pedersen JM, Matsson P, Bergstrom CA, Hoogstraate J, Noren A, LeCluyse EL, Artursson P: Early identification of clinically relevant drug interactions with the human bile salt export pump (BSEP/ABCB11). Toxicol Sci. 2013 Dec;136(2):328-43. doi: 10.1093/toxsci/kft197. Epub 2013 Sep 6. [PubMed:24014644]

Drug created on June 13, 2005 07:24 / Updated on October 16, 2018 08:29