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Identification
NameDiazepam
Accession NumberDB00829  (APRD00642, DB07699)
TypeSmall Molecule
GroupsApproved, Illicit, Vet Approved
DescriptionA benzodiazepine with anticonvulsant, anxiolytic, sedative, muscle relaxant, and amnesic properties and a long duration of action. Its actions are mediated by enhancement of gamma-aminobutyric acid activity. It is used in the treatment of severe anxiety disorders, as a hypnotic in the short-term management of insomnia, as a sedative and premedicant, as an anticonvulsant, and in the management of alcohol withdrawal syndrome. (From Martindale, The Extra Pharmacopoeia, 30th ed, p589)
Structure
Thumb
Synonyms
7-chloro-1,3-dihydro-1-methyl-5-phenyl-2H-1,4-benzodiazepin-2-one
Diazepam
Methyl diazepinone
Valium
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Bio-diazepamTablet2 mgOralBiomed Pharma2003-04-23Not applicableCanada
Bio-diazepamTablet5 mgOralBiomed Pharma2003-04-23Not applicableCanada
Bio-diazepamTablet10 mgOralBiomed Pharma2003-04-23Not applicableCanada
DiastatGel20 mg/4mLRectalValeant Pharmaceuticals North America LLC1997-07-29Not applicableUs
DiastatGel2.5 mg/.5mLRectalValeant Pharmaceuticals North America LLC1997-07-29Not applicableUs
DiastatGel10 mg/2mLRectalValeant Pharmaceuticals North America LLC1997-07-29Not applicableUs
DiastatGel5 mgRectalValeant Pharmaceuticals North America LLC2000-01-28Not applicableCanada
DiazemulsEmulsion5 mgIntramuscular; IntravenousActavis Group Ptc Ehf1995-12-312016-01-05Canada
DiazepamGel2.5 mg/.5mLRectalTeva Pharmaceuticals USA Inc2010-10-01Not applicableUs
DiazepamGel10 mg/2mLRectalTeva Pharmaceuticals USA Inc2010-09-03Not applicableUs
DiazepamGel20 mg/4mLRectalTeva Pharmaceuticals USA Inc2010-09-03Not applicableUs
Diazepam 10mg TabletsTablet10 mgOralLaboratoires Confab IncNot applicableNot applicableCanada
Diazepam 10tab 10mgTablet10 mgOralPro Doc Limitee1978-12-31Not applicableCanada
Diazepam 2mg TabletsTablet2 mgOralLaboratoires Confab IncNot applicableNot applicableCanada
Diazepam 2tab 2mgTablet2 mgOralPro Doc Limitee1978-12-312012-07-23Canada
Diazepam 5 TabTablet5 mgOralPro Doc Limitee1974-12-31Not applicableCanada
Diazepam 5mg TabletsTablet5 mgOralLaboratoires Confab IncNot applicableNot applicableCanada
Diazepam AutoinjectorLiquid5 mgIntramuscularMeridian Medical Technologies Inc.2007-01-24Not applicableCanada
Diazepam Injection SdzSolution5 mgIntramuscular; IntravenousSandoz Canada Incorporated2013-03-27Not applicableCanada
Diazepam Injection USPSolution5 mgIntramuscular; IntravenousAlveda Pharmaceuticals IncNot applicableNot applicableCanada
Diazepam Injection USPSolution5 mgIntramuscular; IntravenousSandoz Canada Incorporated1980-12-31Not applicableCanada
E Pam Tab 10mgTablet10 mgOralIcn Canada Ltd.1973-12-312005-04-26Canada
E Pam Tab 2mgTablet2 mgOralIcn Canada Ltd.1973-12-312005-04-26Canada
E Pam Tab 5mgTablet5 mgOralIcn Canada Ltd.1973-12-312005-04-26Canada
Meval 2Tablet2 mgOralMedic Laboratory LtÉe1973-12-311996-09-09Canada
Meval 5Tablet5 mgOralMedic Laboratory LtÉe1973-12-311996-09-09Canada
Novo-dipam Tab 10mgTablet10 mgOralNovopharm Limited1973-12-312015-10-26Canada
Novo-dipam Tab 2mgTablet2 mgOralNovopharm Limited1973-12-312015-10-26Canada
Novo-dipam Tab 5mgTablet5 mgOralNovopharm Limited1973-12-312015-10-26Canada
PMS-diazepamTablet2 mgOralPharmascience Inc2003-12-10Not applicableCanada
PMS-diazepamTablet5 mgOralPharmascience Inc2003-12-10Not applicableCanada
PMS-diazepamTablet10 mgOralPharmascience Inc2003-12-10Not applicableCanada
PMS-diazepam Solution 1mg/mlSolution1 mgOralPharmascience Inc1992-12-31Not applicableCanada
ValiumTablet10 mg/1OralCardinal Health1963-11-152016-10-13Us
ValiumTablet5 mg/1OralGenentech, Inc.1963-11-15Not applicableUs
ValiumTablet5 mg/1OralPd Rx Pharmaceuticals, Inc.1963-11-15Not applicableUs
ValiumTablet10 mg/1OralGenentech, Inc.1963-11-15Not applicableUs
ValiumTablet5 mg/1OralREMEDYREPACK INC.2012-11-282017-11-04Us
ValiumTablet5 mg/1OralCardinal Health1963-11-152016-10-13Us
ValiumTablet2 mg/1OralGenentech, Inc.1963-11-15Not applicableUs
Valium 10 TabTablet10 mgOralHoffmann La Roche Limited1978-12-312001-07-19Canada
Valium 5 TabTablet5 mgOralHoffmann La Roche Limited1978-12-31Not applicableCanada
Valium Inj Roche 5mg/mlLiquid10 mgIntramuscular; IntravenousHoffmann La Roche Limited1968-12-312000-07-27Canada
VivolTablet10 mgOralAxxess Pharma Inc.1970-12-312011-07-22Canada
VivolTablet2 mgOralCarter Horner Corp.1970-12-312004-07-09Canada
VivolTablet5 mgOralAxxess Pharma Inc.1970-12-312011-07-22Canada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo Diazepam Tab 10mgTablet10 mgOralApotex Inc1979-12-31Not applicableCanada
Apo Diazepam Tab 2mgTablet2 mgOralApotex Inc1979-12-31Not applicableCanada
Apo Diazepam Tab 5mgTablet5 mgOralApotex Inc1977-12-31Not applicableCanada
DiazepamTablet10 mg/1OralA S Medication Solutions Llc2006-03-31Not applicableUs
DiazepamSolution5 mg/5mLOralWest Ward Pharmaceuticals Corp.1987-04-03Not applicableUs
DiazepamTablet10 mg/1OralPhysicians Total Care, Inc.2004-06-03Not applicableUs
DiazepamTablet2 mg/1OralMayne Pharma Inc.2016-08-03Not applicableUs
DiazepamTablet5 mg/1OralMylan Pharmaceuticals Inc.1985-09-04Not applicableUs
DiazepamTablet10 mg/1OralRebel Distributors Corp.2009-11-09Not applicableUs
DiazepamTablet5 mg/1OralA S Medication Solutions1985-09-04Not applicableUs
DiazepamInjection, solution5 mg/mLIntramuscular; IntravenousA S Medication Solutions2005-08-23Not applicableUs
DiazepamTablet5 mg/1OralProficient Rx LP1986-12-10Not applicableUs
DiazepamTablet5 mg/1OralRed Pharm Drug Inc.2006-05-01Not applicableUs
DiazepamTablet10 mg/1OralSTAT Rx USA LLC2009-11-20Not applicableUs
DiazepamTablet10 mg/1OralA S Medication Solutions Llc2006-03-31Not applicableUs
DiazepamTablet10 mg/1OralPreferred Pharmaceuticals, Inc.2011-11-09Not applicableUs
DiazepamSolution5 mg/5mLOralRoxane Laboratories, Inc1990-06-142016-10-13Us
DiazepamTablet10 mg/1OralApotheca, Inc.2009-01-15Not applicableUs
DiazepamTablet5 mg/1OralPreferred Pharmaceuticals Inc.2016-06-10Not applicableUs
DiazepamTablet10 mg/1OralLake Erie Medical DBA Quality Care Products LLC2016-08-03Not applicableUs
DiazepamInjection, solution5 mg/mLIntramuscular; IntravenousCardinal Health1987-10-13Not applicableUs
DiazepamTablet5 mg/1OralTYA Pharmaceuticals1986-12-10Not applicableUs
DiazepamTablet2 mg/1Oralbryant ranch prepack1986-12-10Not applicableUs
DiazepamTablet5 mg/1OralPreferred Pharmaceuticals, Inc.2012-01-17Not applicableUs
DiazepamTablet5 mg/1OralA S Medication Solutions Llc2006-03-31Not applicableUs
DiazepamTablet10 mg/1OralCardinal Health2009-11-20Not applicableUs
DiazepamTablet5 mg/1OralCardinal Health2009-10-13Not applicableUs
DiazepamTablet2 mg/1OralLake Erie Medical DBA Quality Care Products LLC1987-02-03Not applicableUs
DiazepamTablet2 mg/1OralActavis Pharma, Inc.1987-02-03Not applicableUs
DiazepamTablet2 mg/1OralAidarex Pharmaceuticals LLC2006-03-31Not applicableUs
DiazepamTablet10 mg/1OralQualitest Pharmaceuticals2006-03-312019-08-31Us
DiazepamInjection, solution5 mg/mLIntramuscular; IntravenousA S Medication Solutions2005-08-23Not applicableUs
DiazepamTablet10 mg/1OralMylan Institutional Inc.1997-10-31Not applicableUs
DiazepamTablet2 mg/1OralLake Erie Medical DBA Quality Care Products LLC1986-12-10Not applicableUs
DiazepamTablet2 mg/1OralDispensing Solutions, Inc.1987-02-03Not applicableUs
DiazepamTablet2 mg/1OralAphena Pharma Solutions Tennessee, Llc2006-03-31Not applicableUs
DiazepamInjection, solution5 mg/mLIntramuscular; IntravenousGENERAL INJECTABLES AND VACCINES, INC.2010-05-01Not applicableUs
DiazepamInjection, solution5 mg/mLIntramuscular; IntravenousA S Medication Solutions Llc1987-10-13Not applicableUs
DiazepamTablet10 mg/1OralNcs Health Care Of Ky, Inc Dba Vangard Labs1986-12-10Not applicableUs
DiazepamTablet5 mg/1OralKAISER FOUNDATION HOSPITALS2002-01-29Not applicableUs
DiazepamSolution5 mg/5mLOralAtlantic Biologicals Corps1987-04-03Not applicableUs
DiazepamTablet2 mg/1OralA S Medication Solutions Llc1986-12-10Not applicableUs
DiazepamInjection, solution5 mg/mLIntramuscular; IntravenousHospira, Inc.1988-12-20Not applicableUs
DiazepamTablet2 mg/1OralPhysicians Total Care, Inc.2008-07-23Not applicableUs
DiazepamTablet5 mg/1OralMayne Pharma Inc.2016-08-03Not applicableUs
DiazepamTablet10 mg/1OralMylan Pharmaceuticals Inc.1985-09-04Not applicableUs
DiazepamInjection, solution5 mg/mLIntramuscular; IntravenousRebel Distributors Corp1987-10-13Not applicableUs
DiazepamTablet10 mg/1OralRedPharm Drug, Inc.2015-01-01Not applicableUs
DiazepamTablet10 mg/1OralProficient Rx LP1986-12-10Not applicableUs
DiazepamTablet10 mg/1OralAphena Pharma Solutions Tennessee, Llc2006-03-31Not applicableUs
DiazepamTablet10 mg/1OralTYA Pharmaceuticals1987-02-03Not applicableUs
DiazepamTablet5 mg/1OralSTAT Rx USA LLC2009-11-20Not applicableUs
DiazepamTablet2 mg/1OralA S Medication Solutions Llc1986-12-10Not applicableUs
DiazepamTablet5 mg/1OralPreferred Pharmaceuticals, Inc.2011-11-09Not applicableUs
DiazepamTablet2 mg/1OralIVAX Pharmaceuticals, Inc.1986-12-10Not applicableUs
DiazepamTablet2 mg/1OralSTAT Rx USA LLC2006-03-31Not applicableUs
DiazepamTablet5 mg/1OralDIRECT RX2014-01-01Not applicableUs
DiazepamTablet5 mg/1OralREMEDYREPACK INC.2016-11-10Not applicableUs
DiazepamTablet5 mg/1OralPd Rx Pharmaceuticals, Inc.1987-02-03Not applicableUs
DiazepamTablet5 mg/1OralCardinal Health2009-11-09Not applicableUs
DiazepamTablet10 mg/1OralProficient Rx LP2006-03-31Not applicableUs
DiazepamTablet5 mg/1OralMajor Pharmaceuticals2008-06-05Not applicableUs
DiazepamTablet5 mg/1OralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC1987-02-03Not applicableUs
DiazepamTablet5 mg/1OralA S Medication Solutions1986-12-10Not applicableUs
DiazepamTablet10 mg/1Oralbryant ranch prepack2006-03-31Not applicableUs
DiazepamTablet5 mg/1OralMc Kesson Contract Packaging2011-10-13Not applicableUs
DiazepamTablet5 mg/1OralUnit Dose Services1986-12-10Not applicableUs
DiazepamTablet5 mg/1OralCardinal Health2009-11-20Not applicableUs
DiazepamInjection5 mg/mLIntramuscular; IntravenousGENERAL INJECTABLES AND VACCINES, INC.2010-06-01Not applicableUs
DiazepamTablet5 mg/1OralPhysicians Total Care, Inc.2008-08-19Not applicableUs
DiazepamTablet5 mg/1OralNcs Health Care Of Ky, Inc Dba Vangard Labs1985-09-04Not applicableUs
DiazepamTablet10 mg/1OralKAISER FOUNDATION HOSPITALS2002-01-29Not applicableUs
DiazepamTablet2 mg/1OralRebel Distributors Corp.2009-11-09Not applicableUs
DiazepamTablet5 mg/1OralA S Medication Solutions1986-12-10Not applicableUs
DiazepamTablet5 mg/1OralRed Pharm Drug, Inc.2013-01-01Not applicableUs
DiazepamTablet10 mg/1OralDIRECT RX2014-01-01Not applicableUs
DiazepamTablet5 mg/1OralContract Pharmacy Services Pa2011-08-01Not applicableUs
DiazepamTablet5 mg/1OralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2011-11-29Not applicableUs
DiazepamTablet5 mg/1Oralbryant ranch prepack1986-12-10Not applicableUs
DiazepamSolution5 mg/5mLOralPrecision Dose Inc.2012-02-22Not applicableUs
DiazepamTablet2 mg/1OralA S Medication Solutions Llc2006-03-31Not applicableUs
DiazepamInjection, solution5 mg/mLIntramuscular; IntravenousHospira, Inc.1987-10-13Not applicableUs
DiazepamTablet5 mg/1OralCardinal Health2006-11-15Not applicableUs
DiazepamTablet10 mg/1OralMayne Pharma Inc.2016-08-03Not applicableUs
DiazepamTablet5 mg/1OralActavis Pharma, Inc.1987-02-03Not applicableUs
DiazepamTablet5 mg/1OralAidarex Pharmaceuticals LLC2006-03-31Not applicableUs
DiazepamTablet2 mg/1OralQualitest Pharmaceuticals2006-03-312018-03-31Us
DiazepamTablet10 mg/1OralPd Rx Pharmaceuticals, Inc.2009-11-20Not applicableUs
DiazepamTablet10 mg/1OralDispensing Solutions, Inc.2006-03-31Not applicableUs
DiazepamTablet5 mg/1OralPd Rx Pharmaceuticals, Inc.1987-02-03Not applicableUs
DiazepamTablet5 mg/1OralA S Medication Solutions Llc2006-03-31Not applicableUs
DiazepamInjection, solution5 mg/mLIntramuscular; IntravenousREMEDYREPACK INC.2016-03-07Not applicableUs
DiazepamTablet5 mg/1OralIVAX Pharmaceuticals, Inc.1986-12-10Not applicableUs
DiazepamTablet5 mg/1OralSTAT Rx USA LLC2006-03-31Not applicableUs
DiazepamTablet5 mg/1OralPd Rx Pharmaceuticals, Inc.1985-09-04Not applicableUs
DiazepamTablet2 mg/1OralMylan Institutional Inc.1997-10-31Not applicableUs
DiazepamTablet2 mg/1OralCardinal Health2009-11-20Not applicableUs
DiazepamTablet10 mg/1OralCardinal Health2009-11-09Not applicableUs
DiazepamTablet10 mg/1OralNu Care Pharmaceuticals, Inc.2006-03-31Not applicableUs
DiazepamTablet10 mg/1OralBlenheim Pharmacal, Inc.2010-04-13Not applicableUs
DiazepamTablet10 mg/1OralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC1987-02-03Not applicableUs
DiazepamTablet10 mg/1OralUnit Dose Services1987-02-03Not applicableUs
DiazepamTablet5 mg/1OralMc Kesson Packaging Services Business Unit Of Mc Kesson Corporation2006-11-15Not applicableUs
DiazepamTablet10 mg/1OralMc Kesson Contract Packaging2009-11-09Not applicableUs
DiazepamTablet10 mg/1OralUnit Dose Services2006-03-31Not applicableUs
DiazepamInjection, solution5 mg/mLIntramuscular; IntravenousPhysicians Total Care, Inc.2002-02-13Not applicableUs
DiazepamTablet10 mg/1OralREMEDYREPACK INC.2007-09-06Not applicableUs
DiazepamTablet2 mg/1OralMylan Pharmaceuticals Inc.1985-09-04Not applicableUs
DiazepamTablet5 mg/1OralRebel Distributors Corp.2009-11-09Not applicableUs
DiazepamTablet5 mg/1OralA S Medication Solutions1985-09-04Not applicableUs
DiazepamTablet10 mg/1OralREMEDYREPACK INC.2016-11-23Not applicableUs
DiazepamTablet5 mg/1OralDIRECT RX2015-01-01Not applicableUs
DiazepamTablet10 mg/1OralContract Pharmacy Services Pa2011-03-29Not applicableUs
DiazepamTablet10 mg/1OralA S Medication Solutions Llc2006-03-31Not applicableUs
DiazepamTablet10 mg/1Oralbryant ranch prepack2006-03-31Not applicableUs
DiazepamTablet10 mg/1OralPreferred Pharmaceuticals, Inc.2012-01-17Not applicableUs
DiazepamTablet5 mg/1OralA S Medication Solutions Llc2006-03-31Not applicableUs
DiazepamSolution, concentrate5 mg/mLOralLannett Company, Inc.2014-04-14Not applicableUs
DiazepamSolution5 mg/5mLOralCardinal Health2012-02-22Not applicableUs
DiazepamTablet5 mg/1OralA S Medication Solutions1985-09-04Not applicableUs
DiazepamTablet10 mg/1OralActavis Pharma, Inc.1987-02-03Not applicableUs
DiazepamTablet10 mg/1OralAidarex Pharmaceuticals LLC2006-03-31Not applicableUs
DiazepamTablet5 mg/1OralQualitest Pharmaceuticals2006-03-312017-10-31Us
DiazepamTablet2 mg/1OralPd Rx Pharmaceuticals, Inc.1987-02-03Not applicableUs
DiazepamTablet5 mg/1OralDispensing Solutions, Inc.2006-03-31Not applicableUs
DiazepamTablet5 mg/1OralAphena Pharma Solutions Tennessee, Llc2006-03-31Not applicableUs
DiazepamTablet2 mg/1OralAvera Mc Kennan Hospital2015-05-05Not applicableUs
DiazepamTablet10 mg/1OralA S Medication Solutions Llc2006-03-31Not applicableUs
DiazepamSolution5 mg/5mLOralLannett Company, Inc.2016-06-24Not applicableUs
DiazepamTablet10 mg/1OralIVAX Pharmaceuticals, Inc.1986-12-10Not applicableUs
DiazepamTablet10 mg/1OralSTAT Rx USA LLC2006-03-31Not applicableUs
DiazepamTablet10 mg/1OralA S Medication Solutions1986-12-10Not applicableUs
DiazepamTablet5 mg/1OralMylan Institutional Inc.1997-11-04Not applicableUs
DiazepamTablet2 mg/1OralREMEDYREPACK INC.2015-07-22Not applicableUs
DiazepamInjection, solution5 mg/mLIntramuscular; IntravenousCardinal Health1988-12-20Not applicableUs
DiazepamTablet5 mg/1OralNu Care Pharmaceuticals, Inc.1987-02-03Not applicableUs
DiazepamTablet5 mg/1OralApotheca, Inc.2009-12-09Not applicableUs
DiazepamTablet10 mg/1OralLake Erie Medical DBA Quality Care Products LLC1986-12-10Not applicableUs
DiazepamTablet5 mg/1OralLake Erie Medical DBA Quality Care Products LLC2016-08-03Not applicableUs
DiazepamTablet2 mg/1OralTYA Pharmaceuticals1986-12-10Not applicableUs
DiazepamTablet5 mg/1OralAmerican Health Packaging2009-10-132015-12-29Us
DiazepamTablet5 mg/1OralREMEDYREPACK INC.2013-07-032016-10-13Us
Diazepam IntensolSolution, concentrate5 mg/mLOralWest Ward Pharmaceuticals Corp.1987-04-03Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
DiapamOrion
NerviumSaba
RelaniumGlaxoSmithKline
Brand mixtures
NameLabellerIngredients
Gabavale-5Physician Therapeutics Llc
SaltsNot Available
Categories
UNIIQ3JTX2Q7TU
CAS number439-14-5
WeightAverage: 284.74
Monoisotopic: 284.071640755
Chemical FormulaC16H13ClN2O
InChI KeyAAOVKJBEBIDNHE-UHFFFAOYSA-N
InChI
InChI=1S/C16H13ClN2O/c1-19-14-8-7-12(17)9-13(14)16(18-10-15(19)20)11-5-3-2-4-6-11/h2-9H,10H2,1H3
IUPAC Name
7-chloro-1-methyl-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one
SMILES
CN1C2=C(C=C(Cl)C=C2)C(=NCC1=O)C1=CC=CC=C1
Pharmacology
IndicationUsed in the treatment of severe anxiety disorders, as a hypnotic in the short-term management of insomnia, as a sedative and premedicant, as an anticonvulsant, and in the management of alcohol withdrawal syndrome.
Structured Indications
PharmacodynamicsDiazepam, a benzodiazepine, generates the same active metabolite as chlordiazepoxide and clorazepate. In animals, diazepam appears to act on parts of the limbic system, the thalamus and hypothalamus, and induces calming effects. Diazepam, unlike chlorpromazine and reserpine, has no demonstrable peripheral autonomic blocking action, nor does it produce extrapyramidal side effects; however, animals treated with diazepam do have a transient ataxia at higher doses. Diazepam was found to have transient cardiovascular depressor effects in dogs. Long-term experiments in rats revealed no disturbances of endocrine function. Injections into animals have produced localized irritation of tissue surrounding injection sites and some thickening of veins after intravenous use.
Mechanism of actionBenzodiazepines bind nonspecifically to benzodiazepine receptors which mediate sleep, affects muscle relaxation, anticonvulsant activity, motor coordination, and memory. As benzodiazepine receptors are thought to be coupled to gamma-aminobutyric acid-A (GABAA) receptors, this enhances the effects of GABA by increasing GABA affinity for the GABA receptor. Binding of GABA to the site opens the chloride channel, resulting in a hyperpolarized cell membrane that prevents further excitation of the cell.
TargetKindPharmacological actionActionsOrganismUniProt ID
Gamma-aminobutyric acid receptor subunit alpha-1Proteinyes
potentiator
HumanP14867 details
Gamma-aminobutyric acid receptor subunit alpha-2Proteinyes
potentiator
HumanP47869 details
Gamma-aminobutyric acid receptor subunit alpha-3Proteinyes
potentiator
HumanP34903 details
Gamma-aminobutyric acid receptor subunit alpha-5Proteinyes
potentiator
HumanP31644 details
Gamma-aminobutyric acid receptor subunit beta-1Proteinyes
potentiator
HumanP18505 details
Gamma-aminobutyric acid receptor subunit beta-2Proteinyes
potentiator
HumanP47870 details
Gamma-aminobutyric acid receptor subunit beta-3Proteinyes
potentiator
HumanP28472 details
Gamma-aminobutyric acid receptor subunit gamma-1Proteinyes
potentiator
HumanQ8N1C3 details
Gamma-aminobutyric acid receptor subunit gamma-2Proteinyes
potentiator
HumanP18507 details
Gamma-aminobutyric acid receptor subunit gamma-3Proteinyes
potentiator
HumanQ99928 details
Gamma-aminobutyric acid receptor subunit deltaProteinyes
potentiator
HumanO14764 details
Gamma-aminobutyric acid receptor subunit epsilonProteinyes
potentiator
HumanP78334 details
Gamma-aminobutyric acid receptor subunit piProteinyes
potentiator
HumanO00591 details
Gamma-aminobutyric acid receptor subunit rho-1Proteinyes
potentiator
HumanP24046 details
Gamma-aminobutyric acid receptor subunit rho-2Proteinyes
potentiator
HumanP28476 details
Gamma-aminobutyric acid receptor subunit rho-3Proteinyes
potentiator
HumanA8MPY1 details
Gamma-aminobutyric acid receptor subunit thetaProteinyes
potentiator
HumanQ9UN88 details
Translocator proteinProteinunknown
potentiator
HumanP30536 details
GABA-A receptor (anion channel)Protein groupyes
positive allosteric modulator
Humannot applicabledetails
Related Articles
AbsorptionEssentially complete, with a bioavailability of 93%.
Volume of distribution
  • 0.8 to 1.0 L/kg [young healthy males]
Protein binding98.5%
Metabolism

Hepatic via the Cytochrome P450 enzyme system. The main active metabolite is desmethyldiazepam, in addition to minor active metabolites including temazepam and oxazepam.

SubstrateEnzymesProduct
Diazepam
NordiazepamDetails
Diazepam
TemazepamDetails
Diazepam
OxazepamDetails
Diazepam
Not Available
desmethyldiazepamDetails
Nordiazepam
OxazepamDetails
Temazepam
OxazepamDetails
Nordiazepam
Not Available
Nordiazepam O-glucuronideDetails
Route of eliminationDiazepam and its metabolites are excreted mainly in the urine, predominantly as their glucuronide conjugates.
Half lifeBiphasic 1-2 days and 2-5 days, active metabolites with long half lives.
Clearance
  • 20-30 mL/min
ToxicitySymptoms of overdose include somnolence, confusion, coma, and diminished reflexes. Respiration, pulse and blood pressure should be monitored.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
1,1,1,2 TetrafluoroethaneThe risk or severity of adverse effects can be increased when Diazepam is combined with 1,1,1,2 Tetrafluoroethane.Investigational
7-NitroindazoleThe risk or severity of adverse effects can be increased when Diazepam is combined with 7-Nitroindazole.Experimental
AbirateroneThe serum concentration of Diazepam can be increased when it is combined with Abiraterone.Approved
AcepromazineThe risk or severity of adverse effects can be increased when Diazepam is combined with Acepromazine.Approved, Vet Approved
AceprometazineThe risk or severity of adverse effects can be increased when Diazepam is combined with Aceprometazine.Approved
AcetaminophenThe serum concentration of Diazepam can be increased when it is combined with Acetaminophen.Approved
adipiplonThe risk or severity of adverse effects can be increased when Diazepam is combined with adipiplon.Investigational
AfatinibThe serum concentration of Diazepam can be increased when it is combined with Afatinib.Approved
AgomelatineThe risk or severity of adverse effects can be increased when Diazepam is combined with Agomelatine.Approved, Investigational
AlbendazoleThe serum concentration of Diazepam can be increased when it is combined with Albendazole.Approved, Vet Approved
AldosteroneThe serum concentration of Diazepam can be decreased when it is combined with Aldosterone.Experimental
AlectinibThe serum concentration of Diazepam can be increased when it is combined with Alectinib.Approved
AlfaxaloneThe risk or severity of adverse effects can be increased when Diazepam is combined with Alfaxalone.Vet Approved
AlfentanilDiazepam may increase the central nervous system depressant (CNS depressant) activities of Alfentanil.Approved, Illicit
AlphacetylmethadolThe risk or severity of adverse effects can be increased when Diazepam is combined with Alphacetylmethadol.Experimental, Illicit
AlprazolamThe risk or severity of adverse effects can be increased when Alprazolam is combined with Diazepam.Approved, Illicit, Investigational
AmantadineThe serum concentration of Diazepam can be increased when it is combined with Amantadine.Approved
Ambroxol acefyllinateThe therapeutic efficacy of Diazepam can be decreased when used in combination with Ambroxol acefyllinate.Experimental
Aminohippuric acidThe serum concentration of Diazepam can be increased when it is combined with Aminohippuric acid.Approved
AminophyllineThe therapeutic efficacy of Diazepam can be decreased when used in combination with Aminophylline.Approved
AmiodaroneThe metabolism of Diazepam can be decreased when combined with Amiodarone.Approved, Investigational
AmisulprideThe risk or severity of adverse effects can be increased when Diazepam is combined with Amisulpride.Approved, Investigational
AmitriptylineThe serum concentration of Diazepam can be increased when it is combined with Amitriptyline.Approved
AmlodipineThe serum concentration of Diazepam can be increased when it is combined with Amlodipine.Approved
AmobarbitalThe risk or severity of adverse effects can be increased when Diazepam is combined with Amobarbital.Approved, Illicit
AmoxapineThe risk or severity of adverse effects can be increased when Diazepam is combined with Amoxapine.Approved
AmperozideThe risk or severity of adverse effects can be increased when Diazepam is combined with Amperozide.Experimental
AmprenavirThe serum concentration of Diazepam can be decreased when it is combined with Amprenavir.Approved
AmsacrineThe serum concentration of Diazepam can be increased when it is combined with Amsacrine.Approved
AprepitantThe serum concentration of Diazepam can be increased when it is combined with Aprepitant.Approved, Investigational
AripiprazoleThe risk or severity of adverse effects can be increased when Diazepam is combined with Aripiprazole.Approved, Investigational
ArmodafinilThe metabolism of Diazepam can be decreased when combined with Armodafinil.Approved, Investigational
ArticaineThe risk or severity of adverse effects can be increased when Diazepam is combined with Articaine.Approved
AsenapineThe risk or severity of adverse effects can be increased when Diazepam is combined with Asenapine.Approved
AstemizoleThe serum concentration of Diazepam can be increased when it is combined with Astemizole.Approved, Withdrawn
AtazanavirThe metabolism of Diazepam can be decreased when combined with Atazanavir.Approved, Investigational
AtenololThe serum concentration of Diazepam can be increased when it is combined with Atenolol.Approved
AtomoxetineThe metabolism of Diazepam can be decreased when combined with Atomoxetine.Approved
AtorvastatinThe serum concentration of Diazepam can be increased when it is combined with Atorvastatin.Approved
AzaperoneThe risk or severity of adverse effects can be increased when Diazepam is combined with Azaperone.Vet Approved
AzelastineDiazepam may increase the central nervous system depressant (CNS depressant) activities of Azelastine.Approved
AzelastineThe serum concentration of Diazepam can be increased when it is combined with Azelastine.Approved
AzithromycinThe serum concentration of Diazepam can be increased when it is combined with Azithromycin.Approved
BaclofenThe risk or severity of adverse effects can be increased when Diazepam is combined with Baclofen.Approved
BarbitalThe risk or severity of adverse effects can be increased when Diazepam is combined with Barbital.Illicit
BenperidolThe risk or severity of adverse effects can be increased when Diazepam is combined with Benperidol.Investigational
BenzocaineThe serum concentration of Diazepam can be increased when it is combined with Benzocaine.Approved
Benzyl alcoholThe risk or severity of adverse effects can be increased when Diazepam is combined with Benzyl alcohol.Approved
BepridilThe serum concentration of Diazepam can be increased when it is combined with Bepridil.Approved, Withdrawn
BexaroteneThe serum concentration of Diazepam can be decreased when it is combined with Bexarotene.Approved, Investigational
BiperidenThe serum concentration of Diazepam can be increased when it is combined with Biperiden.Approved
BoceprevirThe metabolism of Diazepam can be decreased when combined with Boceprevir.Approved
BortezomibThe metabolism of Diazepam can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Diazepam can be decreased when it is combined with Bosentan.Approved, Investigational
BosutinibThe serum concentration of Diazepam can be increased when it is combined with Bosutinib.Approved
BrexpiprazoleThe risk or severity of adverse effects can be increased when Diazepam is combined with Brexpiprazole.Approved
BrimonidineThe risk or severity of adverse effects can be increased when Diazepam is combined with Brimonidine.Approved
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Diazepam.Approved
BromazepamThe risk or severity of adverse effects can be increased when Diazepam is combined with Bromazepam.Approved, Illicit
BromocriptineThe serum concentration of Diazepam can be increased when it is combined with Bromocriptine.Approved, Investigational
BrompheniramineThe risk or severity of adverse effects can be increased when Diazepam is combined with Brompheniramine.Approved
BrotizolamThe risk or severity of adverse effects can be increased when Diazepam is combined with Brotizolam.Approved, Withdrawn
BupivacaineThe risk or severity of adverse effects can be increased when Bupivacaine is combined with Diazepam.Approved, Investigational
BuprenorphineDiazepam may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.Approved, Illicit, Investigational, Vet Approved
BuspironeThe serum concentration of Diazepam can be increased when it is combined with Buspirone.Approved, Investigational
ButabarbitalThe risk or severity of adverse effects can be increased when Butabarbital is combined with Diazepam.Approved, Illicit
ButacaineThe risk or severity of adverse effects can be increased when Diazepam is combined with Butacaine.Vet Approved
ButalbitalThe risk or severity of adverse effects can be increased when Diazepam is combined with Butalbital.Approved, Illicit
ButambenThe risk or severity of adverse effects can be increased when Diazepam is combined with Butamben.Approved
ButethalThe risk or severity of adverse effects can be increased when Diazepam is combined with Butethal.Approved, Illicit
ButorphanolThe risk or severity of adverse effects can be increased when Butorphanol is combined with Diazepam.Approved, Illicit, Vet Approved
CabazitaxelThe serum concentration of Diazepam can be increased when it is combined with Cabazitaxel.Approved
CaffeineThe serum concentration of Diazepam can be increased when it is combined with Caffeine.Approved
CanagliflozinThe serum concentration of Diazepam can be increased when it is combined with Canagliflozin.Approved
CandesartanThe serum concentration of Diazepam can be increased when it is combined with Candesartan.Approved
CapecitabineThe metabolism of Diazepam can be decreased when combined with Capecitabine.Approved, Investigational
CaptoprilThe serum concentration of Diazepam can be increased when it is combined with Captopril.Approved
CarbamazepineThe metabolism of Diazepam can be increased when combined with Carbamazepine.Approved, Investigational
CarbinoxamineThe risk or severity of adverse effects can be increased when Diazepam is combined with Carbinoxamine.Approved
CarfentanilThe risk or severity of adverse effects can be increased when Diazepam is combined with Carfentanil.Illicit, Vet Approved
CarisoprodolThe risk or severity of adverse effects can be increased when Diazepam is combined with Carisoprodol.Approved
CarvedilolThe serum concentration of Diazepam can be increased when it is combined with Carvedilol.Approved, Investigational
CaspofunginThe serum concentration of Diazepam can be increased when it is combined with Caspofungin.Approved
CelecoxibThe metabolism of Diazepam can be decreased when combined with Celecoxib.Approved, Investigational
CeritinibThe serum concentration of Diazepam can be increased when it is combined with Ceritinib.Approved
CetirizineThe risk or severity of adverse effects can be increased when Diazepam is combined with Cetirizine.Approved
Chloral hydrateThe risk or severity of adverse effects can be increased when Diazepam is combined with Chloral hydrate.Approved, Illicit, Vet Approved
ChloramphenicolThe metabolism of Diazepam can be decreased when combined with Chloramphenicol.Approved, Vet Approved
ChlordiazepoxideThe risk or severity of adverse effects can be increased when Chlordiazepoxide is combined with Diazepam.Approved, Illicit
ChlormezanoneThe risk or severity of adverse effects can be increased when Diazepam is combined with Chlormezanone.Approved, Withdrawn
ChloroprocaineThe risk or severity of adverse effects can be increased when Diazepam is combined with Chloroprocaine.Approved
ChloroquineThe serum concentration of Diazepam can be increased when it is combined with Chloroquine.Approved, Vet Approved
ChlorphenamineThe risk or severity of adverse effects can be increased when Diazepam is combined with Chlorphenamine.Approved
ChlorpromazineThe serum concentration of Diazepam can be increased when it is combined with Chlorpromazine.Approved, Vet Approved
ChlorpropamideThe serum concentration of Diazepam can be increased when it is combined with Chlorpropamide.Approved
ChlorprothixeneThe serum concentration of Diazepam can be increased when it is combined with Chlorprothixene.Approved, Withdrawn
ChlorzoxazoneThe risk or severity of adverse effects can be increased when Diazepam is combined with Chlorzoxazone.Approved
CholecalciferolThe metabolism of Diazepam can be decreased when combined with Cholecalciferol.Approved, Nutraceutical
CholesterolThe serum concentration of Diazepam can be increased when it is combined with Cholesterol.Experimental
Cholic AcidThe serum concentration of Diazepam can be decreased when it is combined with Cholic Acid.Approved
CilazaprilThe serum concentration of Diazepam can be increased when it is combined with Cilazapril.Approved
CilostazolThe serum concentration of Cilostazol can be increased when it is combined with Diazepam.Approved
CimetidineThe serum concentration of Diazepam can be decreased when it is combined with Cimetidine.Approved
CinchocaineThe risk or severity of adverse effects can be increased when Cinchocaine is combined with Diazepam.Approved, Vet Approved
CiprofloxacinThe serum concentration of Diazepam can be increased when it is combined with Ciprofloxacin.Approved, Investigational
CitalopramThe serum concentration of Diazepam can be increased when it is combined with Citalopram.Approved
ClarithromycinThe metabolism of Diazepam can be decreased when combined with Clarithromycin.Approved
ClemastineThe metabolism of Diazepam can be decreased when combined with Clemastine.Approved
ClidiniumThe risk or severity of adverse effects can be increased when Diazepam is combined with Clidinium.Approved
ClobazamThe risk or severity of adverse effects can be increased when Diazepam is combined with Clobazam.Approved, Illicit
ClofazimineThe serum concentration of Diazepam can be increased when it is combined with Clofazimine.Approved, Investigational
clomethiazoleThe risk or severity of adverse effects can be increased when Diazepam is combined with clomethiazole.Investigational
ClomipramineThe serum concentration of Diazepam can be increased when it is combined with Clomipramine.Approved, Vet Approved
ClonazepamThe risk or severity of adverse effects can be increased when Diazepam is combined with Clonazepam.Approved, Illicit
ClonidineThe risk or severity of adverse effects can be increased when Diazepam is combined with Clonidine.Approved
ClopidogrelThe metabolism of Diazepam can be decreased when combined with Clopidogrel.Approved, Nutraceutical
ClorazepateThe risk or severity of adverse effects can be increased when Clorazepate is combined with Diazepam.Approved, Illicit
ClotrimazoleThe metabolism of Diazepam can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineThe risk or severity of adverse effects can be increased when Diazepam is combined with Clozapine.Approved
CobicistatThe metabolism of Diazepam can be decreased when combined with Cobicistat.Approved
CocaineThe risk or severity of adverse effects can be increased when Diazepam is combined with Cocaine.Approved, Illicit
CodeineThe risk or severity of adverse effects can be increased when Codeine is combined with Diazepam.Approved, Illicit
ColchicineThe serum concentration of Diazepam can be increased when it is combined with Colchicine.Approved
ColforsinThe serum concentration of Diazepam can be increased when it is combined with Colforsin.Experimental
ConivaptanThe serum concentration of Diazepam can be increased when it is combined with Conivaptan.Approved, Investigational
CrizotinibThe metabolism of Diazepam can be decreased when combined with Crizotinib.Approved
CyclizineThe risk or severity of adverse effects can be increased when Diazepam is combined with Cyclizine.Approved
CyclobenzaprineThe risk or severity of adverse effects can be increased when Diazepam is combined with Cyclobenzaprine.Approved
CyclophosphamideThe serum concentration of Diazepam can be increased when it is combined with Cyclophosphamide.Approved, Investigational
CyclosporineThe metabolism of Diazepam can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
CyproheptadineThe risk or severity of adverse effects can be increased when Diazepam is combined with Cyproheptadine.Approved
Cyproterone acetateThe serum concentration of Diazepam can be decreased when it is combined with Cyproterone acetate.Approved, Investigational
DabrafenibThe serum concentration of Diazepam can be decreased when it is combined with Dabrafenib.Approved
DaclatasvirThe serum concentration of Diazepam can be increased when it is combined with Daclatasvir.Approved
DactinomycinThe serum concentration of Diazepam can be increased when it is combined with Dactinomycin.Approved
DantroleneThe risk or severity of adverse effects can be increased when Diazepam is combined with Dantrolene.Approved
DapiprazoleThe risk or severity of adverse effects can be increased when Dapiprazole is combined with Diazepam.Approved
DapoxetineThe risk or severity of adverse effects can be increased when Diazepam is combined with Dapoxetine.Investigational
DarunavirThe metabolism of Diazepam can be decreased when combined with Darunavir.Approved
DasatinibThe serum concentration of Diazepam can be increased when it is combined with Dasatinib.Approved, Investigational
DaunorubicinThe serum concentration of Diazepam can be decreased when it is combined with Daunorubicin.Approved
DeferasiroxThe serum concentration of Diazepam can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe metabolism of Diazepam can be decreased when combined with Delavirdine.Approved
deramciclaneThe risk or severity of adverse effects can be increased when Diazepam is combined with deramciclane.Investigational
DesfluraneThe risk or severity of adverse effects can be increased when Diazepam is combined with Desflurane.Approved
DesipramineThe serum concentration of Diazepam can be increased when it is combined with Desipramine.Approved
DesloratadineThe serum concentration of Diazepam can be increased when it is combined with Desloratadine.Approved, Investigational
DesvenlafaxineThe risk or severity of adverse effects can be increased when Diazepam is combined with Desvenlafaxine.Approved
DetomidineThe risk or severity of adverse effects can be increased when Diazepam is combined with Detomidine.Vet Approved
DexamethasoneThe serum concentration of Diazepam can be decreased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
DexbrompheniramineThe risk or severity of adverse effects can be increased when Diazepam is combined with Dexbrompheniramine.Approved
DexmedetomidineThe risk or severity of adverse effects can be increased when Dexmedetomidine is combined with Diazepam.Approved, Vet Approved
DextromethorphanThe serum concentration of Diazepam can be increased when it is combined with Dextromethorphan.Approved
DextromoramideThe risk or severity of adverse effects can be increased when Diazepam is combined with Dextromoramide.Experimental, Illicit
DextropropoxypheneThe risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Diazepam.Approved, Illicit, Withdrawn
DezocineThe risk or severity of adverse effects can be increased when Diazepam is combined with Dezocine.Approved
DiclofenacThe serum concentration of Diazepam can be increased when it is combined with Diclofenac.Approved, Vet Approved
DifenoxinThe risk or severity of adverse effects can be increased when Diazepam is combined with Difenoxin.Approved, Illicit
DigoxinThe serum concentration of Diazepam can be decreased when it is combined with Digoxin.Approved
DihydrocodeineThe risk or severity of adverse effects can be increased when Diazepam is combined with Dihydrocodeine.Approved, Illicit
DihydroergotamineThe metabolism of Diazepam can be decreased when combined with Dihydroergotamine.Approved
DihydroetorphineThe risk or severity of adverse effects can be increased when Diazepam is combined with Dihydroetorphine.Experimental, Illicit
DihydromorphineThe risk or severity of adverse effects can be increased when Diazepam is combined with Dihydromorphine.Experimental, Illicit
DiltiazemThe metabolism of Diazepam can be decreased when combined with Diltiazem.Approved
DimenhydrinateThe risk or severity of adverse effects can be increased when Diazepam is combined with Dimenhydrinate.Approved
DiphenhydramineThe risk or severity of adverse effects can be increased when Diazepam is combined with Diphenhydramine.Approved
DiphenoxylateThe risk or severity of adverse effects can be increased when Diazepam is combined with Diphenoxylate.Approved, Illicit
DipyridamoleThe serum concentration of Diazepam can be increased when it is combined with Dipyridamole.Approved
DisulfiramThe serum concentration of Diazepam can be increased when it is combined with Disulfiram.Approved
DoramectinThe risk or severity of adverse effects can be increased when Diazepam is combined with Doramectin.Vet Approved
DoxazosinThe serum concentration of Diazepam can be increased when it is combined with Doxazosin.Approved
DoxepinThe serum concentration of Diazepam can be increased when it is combined with Doxepin.Approved
DoxorubicinThe serum concentration of Diazepam can be decreased when it is combined with Doxorubicin.Approved, Investigational
DoxycyclineThe metabolism of Diazepam can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Diazepam.Approved, Vet Approved
DPDPEThe risk or severity of adverse effects can be increased when Diazepam is combined with DPDPE.Investigational
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Diazepam.Approved, Illicit
DronedaroneThe metabolism of Diazepam can be decreased when combined with Dronedarone.Approved
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Diazepam.Approved, Vet Approved
DrotebanolThe risk or severity of adverse effects can be increased when Diazepam is combined with Drotebanol.Experimental, Illicit
DuloxetineThe risk or severity of adverse effects can be increased when Diazepam is combined with Duloxetine.Approved
DyclonineThe risk or severity of adverse effects can be increased when Dyclonine is combined with Diazepam.Approved
DyphyllineThe therapeutic efficacy of Diazepam can be decreased when used in combination with Dyphylline.Approved
EcgonineThe risk or severity of adverse effects can be increased when Diazepam is combined with Ecgonine.Experimental, Illicit
ECGONINE METHYL ESTERThe risk or severity of adverse effects can be increased when Diazepam is combined with ECGONINE METHYL ESTER.Experimental
EcopipamThe risk or severity of adverse effects can be increased when Diazepam is combined with Ecopipam.Investigational
EfavirenzThe serum concentration of Diazepam can be decreased when it is combined with Efavirenz.Approved, Investigational
ElbasvirThe serum concentration of Diazepam can be increased when it is combined with Elbasvir.Approved
EnalaprilThe serum concentration of Diazepam can be increased when it is combined with Enalapril.Approved, Vet Approved
EnfluraneThe risk or severity of adverse effects can be increased when Enflurane is combined with Diazepam.Approved, Vet Approved
EntacaponeThe risk or severity of adverse effects can be increased when Diazepam is combined with Entacapone.Approved, Investigational
EnzalutamideThe serum concentration of Diazepam can be decreased when it is combined with Enzalutamide.Approved
ErgonovineThe serum concentration of Diazepam can be increased when it is combined with Ergonovine.Approved
ErgotamineThe serum concentration of Diazepam can be increased when it is combined with Ergotamine.Approved
ErythromycinThe metabolism of Diazepam can be decreased when combined with Erythromycin.Approved, Vet Approved
EscitalopramThe risk or severity of adverse effects can be increased when Diazepam is combined with Escitalopram.Approved, Investigational
Eslicarbazepine acetateThe serum concentration of Diazepam can be decreased when it is combined with Eslicarbazepine acetate.Approved
EsomeprazoleThe metabolism of Diazepam can be decreased when combined with Esomeprazole.Approved, Investigational
EstazolamThe risk or severity of adverse effects can be increased when Diazepam is combined with Estazolam.Approved, Illicit
EstramustineThe serum concentration of Diazepam can be increased when it is combined with Estramustine.Approved
EstriolThe serum concentration of Diazepam can be decreased when it is combined with Estriol.Approved, Vet Approved
EstroneThe serum concentration of Diazepam can be decreased when it is combined with Estrone.Approved
EszopicloneThe risk or severity of adverse effects can be increased when Eszopiclone is combined with Diazepam.Approved
EthanolDiazepam may increase the central nervous system depressant (CNS depressant) activities of Ethanol.Approved
EthchlorvynolThe risk or severity of adverse effects can be increased when Ethchlorvynol is combined with Diazepam.Approved, Illicit, Withdrawn
EthosuximideThe risk or severity of adverse effects can be increased when Diazepam is combined with Ethosuximide.Approved
EthotoinThe risk or severity of adverse effects can be increased when Diazepam is combined with Ethotoin.Approved
Ethyl carbamateThe risk or severity of adverse effects can be increased when Diazepam is combined with Ethyl carbamate.Withdrawn
Ethyl loflazepateThe risk or severity of adverse effects can be increased when Diazepam is combined with Ethyl loflazepate.Approved, Illicit
EthylmorphineThe risk or severity of adverse effects can be increased when Diazepam is combined with Ethylmorphine.Approved, Illicit
EtidocaineThe risk or severity of adverse effects can be increased when Diazepam is combined with Etidocaine.Approved
EtifoxineThe risk or severity of adverse effects can be increased when Diazepam is combined with Etifoxine.Withdrawn
EtizolamThe risk or severity of adverse effects can be increased when Diazepam is combined with Etizolam.Approved
EtomidateThe risk or severity of adverse effects can be increased when Etomidate is combined with Diazepam.Approved
EtoperidoneThe risk or severity of adverse effects can be increased when Diazepam is combined with Etoperidone.Approved
EtoposideThe serum concentration of Diazepam can be increased when it is combined with Etoposide.Approved
EtorphineThe risk or severity of adverse effects can be increased when Diazepam is combined with Etorphine.Illicit, Vet Approved
EtravirineThe serum concentration of Diazepam can be decreased when it is combined with Etravirine.Approved
EzogabineThe risk or severity of adverse effects can be increased when Diazepam is combined with Ezogabine.Approved
FelbamateThe risk or severity of adverse effects can be increased when Diazepam is combined with Felbamate.Approved
FelodipineThe serum concentration of Diazepam can be increased when it is combined with Felodipine.Approved, Investigational
FencamfamineThe risk or severity of adverse effects can be increased when Diazepam is combined with Fencamfamine.Approved, Illicit, Withdrawn
FentanylThe serum concentration of Diazepam can be increased when it is combined with Fentanyl.Approved, Illicit, Investigational, Vet Approved
FexofenadineThe serum concentration of Diazepam can be increased when it is combined with Fexofenadine.Approved
FidaxomicinThe serum concentration of Diazepam can be increased when it is combined with Fidaxomicin.Approved
FlibanserinThe risk or severity of adverse effects can be increased when Diazepam is combined with Flibanserin.Approved
FloxuridineThe metabolism of Diazepam can be decreased when combined with Floxuridine.Approved
FluconazoleThe metabolism of Diazepam can be decreased when combined with Fluconazole.Approved
FludiazepamThe risk or severity of adverse effects can be increased when Diazepam is combined with Fludiazepam.Approved, Illicit
FlunarizineThe risk or severity of adverse effects can be increased when Diazepam is combined with Flunarizine.Approved
FlunitrazepamThe risk or severity of adverse effects can be increased when Diazepam is combined with Flunitrazepam.Approved, Illicit
FluorouracilThe metabolism of Diazepam can be decreased when combined with Fluorouracil.Approved
FluoxetineThe serum concentration of Diazepam can be increased when it is combined with Fluoxetine.Approved, Vet Approved
FlupentixolThe serum concentration of Diazepam can be increased when it is combined with Flupentixol.Approved, Withdrawn
FluphenazineThe serum concentration of Diazepam can be increased when it is combined with Fluphenazine.Approved
FlurazepamThe serum concentration of Diazepam can be increased when it is combined with Flurazepam.Approved, Illicit
FluspirileneThe risk or severity of adverse effects can be increased when Diazepam is combined with Fluspirilene.Approved
Fluticasone PropionateThe risk or severity of adverse effects can be increased when Diazepam is combined with Fluticasone Propionate.Approved
FluvastatinThe metabolism of Diazepam can be decreased when combined with Fluvastatin.Approved
FluvoxamineThe metabolism of Diazepam can be decreased when combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe serum concentration of Diazepam can be increased when it is combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Diazepam can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe serum concentration of Fosphenytoin can be increased when it is combined with Diazepam.Approved
FospropofolThe risk or severity of adverse effects can be increased when Diazepam is combined with Fospropofol.Approved, Illicit
Fusidic AcidThe serum concentration of Diazepam can be increased when it is combined with Fusidic Acid.Approved
GabapentinThe risk or severity of adverse effects can be increased when Diazepam is combined with Gabapentin.Approved, Investigational
gabapentin enacarbilThe risk or severity of adverse effects can be increased when Diazepam is combined with gabapentin enacarbil.Approved
Gamma Hydroxybutyric AcidThe risk or severity of adverse effects can be increased when Diazepam is combined with Gamma Hydroxybutyric Acid.Approved, Illicit
GefitinibThe serum concentration of Diazepam can be increased when it is combined with Gefitinib.Approved, Investigational
GemfibrozilThe metabolism of Diazepam can be decreased when combined with Gemfibrozil.Approved
GenisteinThe serum concentration of Diazepam can be increased when it is combined with Genistein.Investigational
GepironeThe risk or severity of adverse effects can be increased when Diazepam is combined with Gepirone.Investigational
GlutethimideThe risk or severity of adverse effects can be increased when Diazepam is combined with Glutethimide.Approved, Illicit
GlyburideThe serum concentration of Diazepam can be increased when it is combined with Glyburide.Approved
GlycerolThe serum concentration of Diazepam can be increased when it is combined with Glycerol.Experimental
Gramicidin DThe serum concentration of Diazepam can be increased when it is combined with Gramicidin D.Approved
GrepafloxacinThe serum concentration of Diazepam can be increased when it is combined with Grepafloxacin.Withdrawn
GuanfacineThe risk or severity of adverse effects can be increased when Diazepam is combined with Guanfacine.Approved, Investigational
HalazepamThe risk or severity of adverse effects can be increased when Halazepam is combined with Diazepam.Approved, Illicit, Withdrawn
HaloperidolThe serum concentration of Diazepam can be increased when it is combined with Haloperidol.Approved
HalothaneThe risk or severity of adverse effects can be increased when Diazepam is combined with Halothane.Approved, Vet Approved
HeroinThe risk or severity of adverse effects can be increased when Diazepam is combined with Heroin.Approved, Illicit
HexobarbitalThe risk or severity of adverse effects can be increased when Diazepam is combined with Hexobarbital.Approved
HyaluronidaseThe therapeutic efficacy of Diazepam can be decreased when used in combination with Hyaluronidase.Approved, Investigational
HydrocodoneDiazepam may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.Approved, Illicit
HydrocortisoneThe serum concentration of Diazepam can be increased when it is combined with Hydrocortisone.Approved, Vet Approved
HydromorphoneThe risk or severity of adverse effects can be increased when Hydromorphone is combined with Diazepam.Approved, Illicit
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Diazepam.Approved
IdelalisibThe serum concentration of Diazepam can be increased when it is combined with Idelalisib.Approved
IloperidoneThe risk or severity of adverse effects can be increased when Diazepam is combined with Iloperidone.Approved
ImatinibThe metabolism of Diazepam can be decreased when combined with Imatinib.Approved
ImipramineThe serum concentration of Diazepam can be increased when it is combined with Imipramine.Approved
IndalpineThe risk or severity of adverse effects can be increased when Diazepam is combined with Indalpine.Investigational, Withdrawn
IndinavirThe metabolism of Diazepam can be decreased when combined with Indinavir.Approved
IndomethacinThe serum concentration of Diazepam can be increased when it is combined with Indomethacin.Approved, Investigational
IrbesartanThe metabolism of Diazepam can be decreased when combined with Irbesartan.Approved, Investigational
IsavuconazoniumThe metabolism of Diazepam can be decreased when combined with Isavuconazonium.Approved, Investigational
IsofluraneThe risk or severity of adverse effects can be increased when Isoflurane is combined with Diazepam.Approved, Vet Approved
IsoniazidThe metabolism of Diazepam can be decreased when combined with Isoniazid.Approved
IsradipineThe metabolism of Diazepam can be decreased when combined with Isradipine.Approved
ItraconazoleThe metabolism of Diazepam can be decreased when combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Diazepam can be increased when it is combined with Ivacaftor.Approved
IvermectinThe serum concentration of Diazepam can be increased when it is combined with Ivermectin.Approved, Vet Approved
KetamineThe serum concentration of Diazepam can be increased when it is combined with Ketamine.Approved, Vet Approved
KetazolamThe risk or severity of adverse effects can be increased when Diazepam is combined with Ketazolam.Approved
KetobemidoneThe risk or severity of adverse effects can be increased when Diazepam is combined with Ketobemidone.Approved
KetoconazoleThe metabolism of Diazepam can be decreased when combined with Ketoconazole.Approved, Investigational
LamotrigineThe risk or severity of adverse effects can be increased when Diazepam is combined with Lamotrigine.Approved, Investigational
LansoprazoleThe serum concentration of Diazepam can be increased when it is combined with Lansoprazole.Approved, Investigational
LapatinibThe serum concentration of Diazepam can be increased when it is combined with Lapatinib.Approved, Investigational
LeflunomideThe metabolism of Diazepam can be decreased when combined with Leflunomide.Approved, Investigational
LevetiracetamThe risk or severity of adverse effects can be increased when Diazepam is combined with Levetiracetam.Approved, Investigational
LevobupivacaineThe risk or severity of adverse effects can be increased when Diazepam is combined with Levobupivacaine.Approved
LevocabastineThe risk or severity of adverse effects can be increased when Diazepam is combined with Levocabastine.Approved
LevocetirizineThe risk or severity of adverse effects can be increased when Diazepam is combined with Levocetirizine.Approved
LevodopaThe risk or severity of adverse effects can be increased when Diazepam is combined with Levodopa.Approved
LevofloxacinThe serum concentration of Diazepam can be increased when it is combined with Levofloxacin.Approved, Investigational
Levomethadyl AcetateThe risk or severity of adverse effects can be increased when Diazepam is combined with Levomethadyl Acetate.Approved
LevomilnacipranThe risk or severity of adverse effects can be increased when Diazepam is combined with Levomilnacipran.Approved
LevorphanolThe risk or severity of adverse effects can be increased when Diazepam is combined with Levorphanol.Approved
LevothyroxineThe serum concentration of Diazepam can be decreased when it is combined with Levothyroxine.Approved
LidocaineThe serum concentration of Diazepam can be increased when it is combined with Lidocaine.Approved, Vet Approved
LiothyronineThe serum concentration of Diazepam can be decreased when it is combined with Liothyronine.Approved, Vet Approved
LiotrixThe serum concentration of Diazepam can be decreased when it is combined with Liotrix.Approved
LisinoprilThe serum concentration of Diazepam can be increased when it is combined with Lisinopril.Approved, Investigational
LithiumThe risk or severity of adverse effects can be increased when Diazepam is combined with Lithium.Approved
LofentanilThe risk or severity of adverse effects can be increased when Diazepam is combined with Lofentanil.Illicit
LomitapideThe serum concentration of Diazepam can be increased when it is combined with Lomitapide.Approved
LoperamideThe serum concentration of Diazepam can be increased when it is combined with Loperamide.Approved
LopinavirThe metabolism of Diazepam can be decreased when combined with Lopinavir.Approved
LoratadineThe serum concentration of Diazepam can be increased when it is combined with Loratadine.Approved
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Diazepam.Approved
LosartanThe serum concentration of Diazepam can be increased when it is combined with Losartan.Approved
LovastatinThe metabolism of Diazepam can be decreased when combined with Lovastatin.Approved, Investigational
LoxapineThe risk or severity of adverse effects can be increased when Loxapine is combined with Diazepam.Approved
Lu AA21004The risk or severity of adverse effects can be increased when Diazepam is combined with Lu AA21004.Investigational
LuliconazoleThe serum concentration of Diazepam can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of Diazepam can be increased when it is combined with Lumacaftor.Approved
LurasidoneThe risk or severity of adverse effects can be increased when Diazepam is combined with Lurasidone.Approved
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Diazepam.Approved, Vet Approved
MaprotilineThe serum concentration of Diazepam can be increased when it is combined with Maprotiline.Approved
MebendazoleThe serum concentration of Diazepam can be increased when it is combined with Mebendazole.Approved, Vet Approved
MeclizineThe risk or severity of adverse effects can be increased when Diazepam is combined with Meclizine.Approved
MedetomidineThe risk or severity of adverse effects can be increased when Diazepam is combined with Medetomidine.Vet Approved
MefloquineThe therapeutic efficacy of Diazepam can be decreased when used in combination with Mefloquine.Approved
Megestrol acetateThe serum concentration of Diazepam can be increased when it is combined with Megestrol acetate.Approved, Vet Approved
MelatoninThe risk or severity of adverse effects can be increased when Diazepam is combined with Melatonin.Approved, Nutraceutical, Vet Approved
MelperoneThe risk or severity of adverse effects can be increased when Diazepam is combined with Melperone.Approved
MepivacaineThe risk or severity of adverse effects can be increased when Diazepam is combined with Mepivacaine.Approved, Vet Approved
MeprobamateThe serum concentration of Diazepam can be increased when it is combined with Meprobamate.Approved, Illicit
MesoridazineThe risk or severity of adverse effects can be increased when Diazepam is combined with Mesoridazine.Approved
MetaxaloneThe risk or severity of adverse effects can be increased when Diazepam is combined with Metaxalone.Approved
MethadoneDiazepam may increase the central nervous system depressant (CNS depressant) activities of Methadone.Approved
Methadyl AcetateThe risk or severity of adverse effects can be increased when Diazepam is combined with Methadyl Acetate.Approved, Illicit
MethapyrileneThe risk or severity of adverse effects can be increased when Diazepam is combined with Methapyrilene.Withdrawn
MethaqualoneThe risk or severity of adverse effects can be increased when Diazepam is combined with Methaqualone.Illicit, Withdrawn
MethocarbamolThe risk or severity of adverse effects can be increased when Diazepam is combined with Methocarbamol.Approved, Vet Approved
MethohexitalThe risk or severity of adverse effects can be increased when Methohexital is combined with Diazepam.Approved
MethotrimeprazineDiazepam may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.Approved
MethoxyfluraneThe risk or severity of adverse effects can be increased when Diazepam is combined with Methoxyflurane.Approved, Vet Approved
MethsuximideThe risk or severity of adverse effects can be increased when Diazepam is combined with Methsuximide.Approved
MethylphenobarbitalThe risk or severity of adverse effects can be increased when Diazepam is combined with Methylphenobarbital.Approved
MetoprololThe serum concentration of Diazepam can be increased when it is combined with Metoprolol.Approved, Investigational
MetyrosineDiazepam may increase the sedative activities of Metyrosine.Approved
MexiletineThe metabolism of Diazepam can be decreased when combined with Mexiletine.Approved
MianserinThe therapeutic efficacy of Diazepam can be decreased when used in combination with Mianserin.Approved
MibefradilThe serum concentration of Diazepam can be increased when it is combined with Mibefradil.Withdrawn
MiconazoleThe serum concentration of Diazepam can be increased when it is combined with Miconazole.Approved, Investigational, Vet Approved
MidazolamThe serum concentration of Diazepam can be decreased when it is combined with Midazolam.Approved, Illicit
MifepristoneThe serum concentration of Diazepam can be increased when it is combined with Mifepristone.Approved, Investigational
MilnacipranThe risk or severity of adverse effects can be increased when Diazepam is combined with Milnacipran.Approved
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Diazepam.Approved, Investigational
MirtazapineDiazepam may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.Approved
MitomycinThe serum concentration of Diazepam can be increased when it is combined with Mitomycin.Approved
MitotaneThe serum concentration of Diazepam can be decreased when it is combined with Mitotane.Approved
MitoxantroneThe serum concentration of Diazepam can be decreased when it is combined with Mitoxantrone.Approved, Investigational
MoclobemideThe metabolism of Diazepam can be decreased when combined with Moclobemide.Approved
ModafinilThe serum concentration of Diazepam can be decreased when it is combined with Modafinil.Approved, Investigational
MolindoneThe risk or severity of adverse effects can be increased when Diazepam is combined with Molindone.Approved
MorphineThe serum concentration of Diazepam can be increased when it is combined with Morphine.Approved, Investigational
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Diazepam.Approved, Investigational
NafcillinThe serum concentration of Diazepam can be decreased when it is combined with Nafcillin.Approved
NalbuphineThe risk or severity of adverse effects can be increased when Diazepam is combined with Nalbuphine.Approved
NaltrexoneThe serum concentration of Diazepam can be increased when it is combined with Naltrexone.Approved, Investigational, Vet Approved
NaringeninThe serum concentration of Diazepam can be increased when it is combined with Naringenin.Experimental
NefazodoneThe metabolism of Diazepam can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe metabolism of Diazepam can be decreased when combined with Nelfinavir.Approved
NeostigmineThe serum concentration of Diazepam can be increased when it is combined with Neostigmine.Approved, Vet Approved
NetupitantThe serum concentration of Diazepam can be increased when it is combined with Netupitant.Approved
NevirapineThe metabolism of Diazepam can be increased when combined with Nevirapine.Approved
NicardipineThe metabolism of Diazepam can be decreased when combined with Nicardipine.Approved
NifedipineThe serum concentration of Diazepam can be decreased when it is combined with Nifedipine.Approved
NilotinibThe metabolism of Diazepam can be decreased when combined with Nilotinib.Approved, Investigational
NisoldipineThe serum concentration of Diazepam can be increased when it is combined with Nisoldipine.Approved
NitrazepamThe serum concentration of Diazepam can be increased when it is combined with Nitrazepam.Approved
NitrendipineThe serum concentration of Diazepam can be increased when it is combined with Nitrendipine.Approved
Nitrous oxideThe risk or severity of adverse effects can be increased when Diazepam is combined with Nitrous oxide.Approved, Vet Approved
NorethisteroneThe serum concentration of Diazepam can be decreased when it is combined with Norethisterone.Approved
NormethadoneThe risk or severity of adverse effects can be increased when Diazepam is combined with Normethadone.Approved, Illicit
NortriptylineThe risk or severity of adverse effects can be increased when Diazepam is combined with Nortriptyline.Approved
OlanzapineThe risk or severity of adverse effects can be increased when Olanzapine is combined with Diazepam.Approved, Investigational
OlaparibThe metabolism of Diazepam can be decreased when combined with Olaparib.Approved
OlopatadineThe risk or severity of adverse effects can be increased when Diazepam is combined with Olopatadine.Approved
OmeprazoleThe serum concentration of Diazepam can be increased when it is combined with Omeprazole.Approved, Investigational, Vet Approved
OndansetronThe risk or severity of adverse effects can be increased when Diazepam is combined with Ondansetron.Approved
OpiumThe risk or severity of adverse effects can be increased when Diazepam is combined with Opium.Approved, Illicit
OrlistatThe serum concentration of Diazepam can be decreased when it is combined with Orlistat.Approved, Investigational
OrphenadrineDiazepam may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
OsanetantThe risk or severity of adverse effects can be increased when Diazepam is combined with Osanetant.Investigational
OsimertinibThe serum concentration of Diazepam can be increased when it is combined with Osimertinib.Approved
OxazepamThe risk or severity of adverse effects can be increased when Diazepam is combined with Oxazepam.Approved
OxetacaineThe risk or severity of adverse effects can be increased when Diazepam is combined with Oxetacaine.Investigational
OxprenololThe risk or severity of adverse effects can be increased when Diazepam is combined with Oxprenolol.Approved
OxybuprocaineThe risk or severity of adverse effects can be increased when Diazepam is combined with Oxybuprocaine.Approved
OxycodoneThe risk or severity of adverse effects can be increased when Oxycodone is combined with Diazepam.Approved, Illicit, Investigational
OxymorphoneThe risk or severity of adverse effects can be increased when Diazepam is combined with Oxymorphone.Approved, Investigational, Vet Approved
P-NitrophenolThe serum concentration of Diazepam can be increased when it is combined with P-Nitrophenol.Experimental
PaclitaxelThe serum concentration of Diazepam can be increased when it is combined with Paclitaxel.Approved, Vet Approved
PalbociclibThe serum concentration of Diazepam can be increased when it is combined with Palbociclib.Approved
PaliperidoneThe risk or severity of adverse effects can be increased when Diazepam is combined with Paliperidone.Approved
Palmitic AcidThe serum concentration of Diazepam can be increased when it is combined with Palmitic Acid.Experimental
PantoprazoleThe serum concentration of Diazepam can be increased when it is combined with Pantoprazole.Approved
ParaldehydeDiazepam may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.Approved
ParoxetineThe serum concentration of Diazepam can be increased when it is combined with Paroxetine.Approved, Investigational
Peginterferon alfa-2bThe serum concentration of Diazepam can be increased when it is combined with Peginterferon alfa-2b.Approved
PentazocineThe risk or severity of adverse effects can be increased when Pentazocine is combined with Diazepam.Approved, Vet Approved
PentobarbitalThe metabolism of Diazepam can be increased when combined with Pentobarbital.Approved, Vet Approved
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Diazepam.Approved
PerazineThe risk or severity of adverse effects can be increased when Diazepam is combined with Perazine.Investigational
PerindoprilThe serum concentration of Diazepam can be increased when it is combined with Perindopril.Approved
PerospironeThe risk or severity of adverse effects can be increased when Diazepam is combined with Perospirone.Approved
PerphenazineThe risk or severity of adverse effects can be increased when Diazepam is combined with Perphenazine.Approved
PethidineThe risk or severity of adverse effects can be increased when Pethidine is combined with Diazepam.Approved
PhenobarbitalThe metabolism of Diazepam can be increased when combined with Phenobarbital.Approved
PhenoxyethanolThe risk or severity of adverse effects can be increased when Diazepam is combined with Phenoxyethanol.Approved
PhenytoinThe serum concentration of Phenytoin can be increased when it is combined with Diazepam.Approved, Vet Approved
PimozideThe serum concentration of Diazepam can be increased when it is combined with Pimozide.Approved
PioglitazoneThe metabolism of Diazepam can be decreased when combined with Pioglitazone.Approved, Investigational
PipamperoneThe risk or severity of adverse effects can be increased when Diazepam is combined with Pipamperone.Approved
PipotiazineThe risk or severity of adverse effects can be increased when Diazepam is combined with Pipotiazine.Approved
PiritramideThe risk or severity of adverse effects can be increased when Diazepam is combined with Piritramide.Investigational
PizotifenThe risk or severity of adverse effects can be increased when Diazepam is combined with Pizotifen.Approved
Platelet Activating FactorThe serum concentration of Diazepam can be decreased when it is combined with Platelet Activating Factor.Experimental
PomalidomideThe risk or severity of adverse effects can be increased when Diazepam is combined with Pomalidomide.Approved
PonatinibThe serum concentration of Diazepam can be increased when it is combined with Ponatinib.Approved
PosaconazoleThe metabolism of Diazepam can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
PramipexoleDiazepam may increase the sedative activities of Pramipexole.Approved, Investigational
PramocaineThe risk or severity of adverse effects can be increased when Diazepam is combined with Pramocaine.Approved
PravastatinThe serum concentration of Diazepam can be increased when it is combined with Pravastatin.Approved
PrazepamThe risk or severity of adverse effects can be increased when Diazepam is combined with Prazepam.Approved, Illicit
PrazosinThe serum concentration of Diazepam can be increased when it is combined with Prazosin.Approved
PrednisoneThe serum concentration of Diazepam can be increased when it is combined with Prednisone.Approved, Vet Approved
PregabalinThe risk or severity of adverse effects can be increased when Pregabalin is combined with Diazepam.Approved, Illicit, Investigational
PregnanoloneThe risk or severity of adverse effects can be increased when Diazepam is combined with Pregnanolone.Investigational
PrilocaineThe risk or severity of adverse effects can be increased when Prilocaine is combined with Diazepam.Approved
PrimidoneThe metabolism of Diazepam can be increased when combined with Primidone.Approved, Vet Approved
ProbenecidThe serum concentration of Diazepam can be increased when it is combined with Probenecid.Approved
ProcaineThe risk or severity of adverse effects can be increased when Procaine is combined with Diazepam.Approved, Investigational, Vet Approved
ProchlorperazineThe risk or severity of adverse effects can be increased when Prochlorperazine is combined with Diazepam.Approved, Vet Approved
ProgesteroneThe serum concentration of Diazepam can be decreased when it is combined with Progesterone.Approved, Vet Approved
PromazineThe risk or severity of adverse effects can be increased when Promazine is combined with Diazepam.Approved, Vet Approved
PromethazineThe serum concentration of Diazepam can be increased when it is combined with Promethazine.Approved
PropafenoneThe serum concentration of Diazepam can be increased when it is combined with Propafenone.Approved
ProparacaineThe risk or severity of adverse effects can be increased when Proparacaine is combined with Diazepam.Approved, Vet Approved
PropofolThe risk or severity of adverse effects can be increased when Propofol is combined with Diazepam.Approved, Investigational, Vet Approved
PropoxycaineThe risk or severity of adverse effects can be increased when Diazepam is combined with Propoxycaine.Approved
PropranololThe serum concentration of Diazepam can be increased when it is combined with Propranolol.Approved, Investigational
ProtriptylineThe serum concentration of Diazepam can be increased when it is combined with Protriptyline.Approved
PSD502The risk or severity of adverse effects can be increased when Diazepam is combined with PSD502.Investigational
PyrimethamineThe metabolism of Diazepam can be decreased when combined with Pyrimethamine.Approved, Vet Approved
QuazepamThe serum concentration of Diazepam can be increased when it is combined with Quazepam.Approved, Illicit
QuercetinThe serum concentration of Diazepam can be increased when it is combined with Quercetin.Experimental
QuetiapineThe risk or severity of adverse effects can be increased when Diazepam is combined with Quetiapine.Approved
QuinacrineThe serum concentration of Diazepam can be increased when it is combined with Quinacrine.Approved
QuinidineThe serum concentration of Diazepam can be increased when it is combined with Quinidine.Approved
QuinineThe serum concentration of Diazepam can be increased when it is combined with Quinine.Approved
RabeprazoleThe metabolism of Diazepam can be decreased when combined with Rabeprazole.Approved, Investigational
RacloprideThe risk or severity of adverse effects can be increased when Diazepam is combined with Raclopride.Investigational
RamelteonThe risk or severity of adverse effects can be increased when Diazepam is combined with Ramelteon.Approved, Investigational
RanitidineThe serum concentration of Diazepam can be increased when it is combined with Ranitidine.Approved
RanolazineThe serum concentration of Diazepam can be increased when it is combined with Ranolazine.Approved, Investigational
ReboxetineThe serum concentration of Diazepam can be increased when it is combined with Reboxetine.Approved, Investigational
RegorafenibThe serum concentration of Diazepam can be increased when it is combined with Regorafenib.Approved
RemifentanilThe risk or severity of adverse effects can be increased when Diazepam is combined with Remifentanil.Approved
RemoxiprideThe risk or severity of adverse effects can be increased when Remoxipride is combined with Diazepam.Approved, Withdrawn
ReserpineThe serum concentration of Diazepam can be decreased when it is combined with Reserpine.Approved
RifabutinThe metabolism of Diazepam can be increased when combined with Rifabutin.Approved
RifampicinThe metabolism of Diazepam can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Diazepam can be increased when combined with Rifapentine.Approved
RilpivirineThe serum concentration of Diazepam can be increased when it is combined with Rilpivirine.Approved
RisperidoneThe risk or severity of adverse effects can be increased when Risperidone is combined with Diazepam.Approved, Investigational
RitanserinThe risk or severity of adverse effects can be increased when Diazepam is combined with Ritanserin.Investigational
RitonavirThe serum concentration of Diazepam can be increased when it is combined with Ritonavir.Approved, Investigational
RolapitantThe serum concentration of Diazepam can be increased when it is combined with Rolapitant.Approved
RomifidineThe risk or severity of adverse effects can be increased when Diazepam is combined with Romifidine.Vet Approved
RopiniroleDiazepam may increase the sedative activities of Ropinirole.Approved, Investigational
RopivacaineThe risk or severity of adverse effects can be increased when Ropivacaine is combined with Diazepam.Approved
RosiglitazoneThe metabolism of Diazepam can be decreased when combined with Rosiglitazone.Approved, Investigational
RotigotineDiazepam may increase the sedative activities of Rotigotine.Approved
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Diazepam.Approved
S-EthylisothioureaThe risk or severity of adverse effects can be increased when Diazepam is combined with S-Ethylisothiourea.Experimental
Sage 547The risk or severity of adverse effects can be increased when Diazepam is combined with Sage 547.Investigational
SaquinavirThe serum concentration of Diazepam can be increased when it is combined with Saquinavir.Approved, Investigational
ScopolamineThe serum concentration of Diazepam can be increased when it is combined with Scopolamine.Approved
SecobarbitalThe metabolism of Diazepam can be increased when combined with Secobarbital.Approved, Vet Approved
SelegilineThe serum concentration of Diazepam can be increased when it is combined with Selegiline.Approved, Investigational, Vet Approved
SertindoleThe risk or severity of adverse effects can be increased when Diazepam is combined with Sertindole.Approved, Withdrawn
SertralineThe serum concentration of Diazepam can be increased when it is combined with Sertraline.Approved
SevofluraneThe risk or severity of adverse effects can be increased when Diazepam is combined with Sevoflurane.Approved, Vet Approved
SildenafilThe metabolism of Diazepam can be decreased when combined with Sildenafil.Approved, Investigational
SiltuximabThe serum concentration of Diazepam can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Diazepam can be increased when it is combined with Simeprevir.Approved
SimvastatinThe serum concentration of Diazepam can be increased when it is combined with Simvastatin.Approved
SirolimusThe serum concentration of Diazepam can be decreased when it is combined with Sirolimus.Approved, Investigational
Sodium oxybateDiazepam may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.Approved
SorafenibThe serum concentration of Diazepam can be increased when it is combined with Sorafenib.Approved, Investigational
SpironolactoneThe serum concentration of Diazepam can be increased when it is combined with Spironolactone.Approved
St. John's WortThe serum concentration of Diazepam can be decreased when it is combined with St. John's Wort.Nutraceutical
StaurosporineThe serum concentration of Diazepam can be increased when it is combined with Staurosporine.Experimental
StiripentolThe serum concentration of Diazepam can be increased when it is combined with Stiripentol.Approved
StreptozocinThe serum concentration of Diazepam can be decreased when it is combined with Streptozocin.Approved
SufentanilThe risk or severity of adverse effects can be increased when Sufentanil is combined with Diazepam.Approved, Investigational
SulfadiazineThe metabolism of Diazepam can be decreased when combined with Sulfadiazine.Approved, Vet Approved
SulfamethoxazoleThe metabolism of Diazepam can be decreased when combined with Sulfamethoxazole.Approved
SulfinpyrazoneThe serum concentration of Diazepam can be increased when it is combined with Sulfinpyrazone.Approved
SulfisoxazoleThe metabolism of Diazepam can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
SulpirideThe risk or severity of adverse effects can be increased when Sulpiride is combined with Diazepam.Approved
SumatriptanThe serum concentration of Diazepam can be increased when it is combined with Sumatriptan.Approved, Investigational
SunitinibThe serum concentration of Diazepam can be increased when it is combined with Sunitinib.Approved, Investigational
SuvorexantDiazepam may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.Approved
TacrineThe serum concentration of Diazepam can be increased when it is combined with Tacrine.Withdrawn
TacrolimusThe serum concentration of Diazepam can be decreased when it is combined with Tacrolimus.Approved, Investigational
TamoxifenThe serum concentration of Diazepam can be decreased when it is combined with Tamoxifen.Approved
TandospironeThe risk or severity of adverse effects can be increased when Diazepam is combined with Tandospirone.Investigational
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Diazepam.Approved
TasimelteonThe risk or severity of adverse effects can be increased when Diazepam is combined with Tasimelteon.Approved
Taurocholic AcidThe serum concentration of Diazepam can be increased when it is combined with Taurocholic Acid.Experimental
TeduglutideThe serum concentration of Diazepam can be increased when it is combined with Teduglutide.Approved
TelaprevirThe metabolism of Diazepam can be decreased when combined with Telaprevir.Approved
TelithromycinThe metabolism of Diazepam can be decreased when combined with Telithromycin.Approved
TelmisartanThe serum concentration of Diazepam can be increased when it is combined with Telmisartan.Approved, Investigational
TemazepamThe risk or severity of adverse effects can be increased when Temazepam is combined with Diazepam.Approved
TemsirolimusThe serum concentration of Diazepam can be increased when it is combined with Temsirolimus.Approved
TenofovirThe metabolism of Diazepam can be decreased when combined with Tenofovir.Approved, Investigational
TerazosinThe serum concentration of Diazepam can be increased when it is combined with Terazosin.Approved
TerfenadineThe serum concentration of Diazepam can be increased when it is combined with Terfenadine.Withdrawn
TeriflunomideThe serum concentration of Diazepam can be decreased when it is combined with Teriflunomide.Approved
TesmilifeneThe serum concentration of Diazepam can be decreased when it is combined with Tesmilifene.Investigational
TestosteroneThe serum concentration of Diazepam can be increased when it is combined with Testosterone.Approved, Investigational
TetrabenazineThe risk or severity of adverse effects can be increased when Diazepam is combined with Tetrabenazine.Approved
TetracaineThe risk or severity of adverse effects can be increased when Diazepam is combined with Tetracaine.Approved, Vet Approved
TetracosactideTetracosactide may increase the hepatotoxic activities of Diazepam.Approved
TetrodotoxinThe risk or severity of adverse effects can be increased when Diazepam is combined with Tetrodotoxin.Investigational
ThalidomideDiazepam may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.Approved, Investigational, Withdrawn
TheophyllineThe therapeutic efficacy of Diazepam can be decreased when used in combination with Theophylline.Approved
ThiamylalThe risk or severity of adverse effects can be increased when Diazepam is combined with Thiamylal.Approved, Vet Approved
ThiopentalThe risk or severity of adverse effects can be increased when Thiopental is combined with Diazepam.Approved, Vet Approved
ThioridazineThe risk or severity of adverse effects can be increased when Thioridazine is combined with Diazepam.Approved
ThiotepaThe metabolism of Diazepam can be decreased when combined with Thiotepa.Approved
ThiothixeneThe risk or severity of adverse effects can be increased when Diazepam is combined with Thiothixene.Approved
TiagabineThe risk or severity of adverse effects can be increased when Diazepam is combined with Tiagabine.Approved
TiaprideThe risk or severity of adverse effects can be increased when Diazepam is combined with Tiapride.Investigational
TicagrelorThe serum concentration of Diazepam can be increased when it is combined with Ticagrelor.Approved
TiclopidineThe metabolism of Diazepam can be decreased when combined with Ticlopidine.Approved
TiletamineThe risk or severity of adverse effects can be increased when Diazepam is combined with Tiletamine.Vet Approved
TizanidineThe risk or severity of adverse effects can be increased when Diazepam is combined with Tizanidine.Approved
TocilizumabThe serum concentration of Diazepam can be decreased when it is combined with Tocilizumab.Approved
TolbutamideThe metabolism of Diazepam can be decreased when combined with Tolbutamide.Approved
TolcaponeThe risk or severity of adverse effects can be increased when Diazepam is combined with Tolcapone.Approved, Withdrawn
TolvaptanThe serum concentration of Diazepam can be increased when it is combined with Tolvaptan.Approved
TopiramateThe risk or severity of adverse effects can be increased when Diazepam is combined with Topiramate.Approved
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with Diazepam.Approved, Investigational
Trans-2-PhenylcyclopropylamineThe risk or severity of adverse effects can be increased when Diazepam is combined with Trans-2-Phenylcyclopropylamine.Experimental
TranylcypromineThe risk or severity of adverse effects can be increased when Tranylcypromine is combined with Diazepam.Approved
TrazodoneThe serum concentration of Diazepam can be decreased when it is combined with Trazodone.Approved, Investigational
TriazolamThe risk or severity of adverse effects can be increased when Diazepam is combined with Triazolam.Approved
TrifluoperazineThe serum concentration of Diazepam can be increased when it is combined with Trifluoperazine.Approved
TriflupromazineThe serum concentration of Diazepam can be increased when it is combined with Triflupromazine.Approved, Vet Approved
TrimethoprimThe serum concentration of Diazepam can be decreased when it is combined with Trimethoprim.Approved, Vet Approved
TrimipramineThe serum concentration of Diazepam can be increased when it is combined with Trimipramine.Approved
TriprolidineThe risk or severity of adverse effects can be increased when Diazepam is combined with Triprolidine.Approved
TroleandomycinThe serum concentration of Diazepam can be increased when it is combined with Troleandomycin.Approved
Uc1010The risk or severity of adverse effects can be increased when Diazepam is combined with Uc1010.Investigational
Valproic AcidThe risk or severity of adverse effects can be increased when Valproic Acid is combined with Diazepam.Approved, Investigational
ValsartanThe metabolism of Diazepam can be decreased when combined with Valsartan.Approved, Investigational
VemurafenibThe serum concentration of Diazepam can be increased when it is combined with Vemurafenib.Approved
VenlafaxineThe metabolism of Diazepam can be decreased when combined with Venlafaxine.Approved
VerapamilThe metabolism of Diazepam can be decreased when combined with Verapamil.Approved
VigabatrinThe risk or severity of adverse effects can be increased when Diazepam is combined with Vigabatrin.Approved
VinblastineThe serum concentration of Diazepam can be decreased when it is combined with Vinblastine.Approved
VincristineThe serum concentration of Diazepam can be decreased when it is combined with Vincristine.Approved, Investigational
VinorelbineThe serum concentration of Diazepam can be increased when it is combined with Vinorelbine.Approved, Investigational
VoriconazoleThe metabolism of Diazepam can be decreased when combined with Voriconazole.Approved, Investigational
VortioxetineThe risk or severity of adverse effects can be increased when Diazepam is combined with Vortioxetine.Approved
XylazineThe risk or severity of adverse effects can be increased when Diazepam is combined with Xylazine.Vet Approved
YohimbineThe therapeutic efficacy of Diazepam can be decreased when used in combination with Yohimbine.Approved, Vet Approved
ZafirlukastThe metabolism of Diazepam can be decreased when combined with Zafirlukast.Approved, Investigational
ZaleplonThe risk or severity of adverse effects can be increased when Diazepam is combined with Zaleplon.Approved, Illicit, Investigational
ZiconotideThe risk or severity of adverse effects can be increased when Diazepam is combined with Ziconotide.Approved
ZimelidineThe serum concentration of Diazepam can be increased when it is combined with Zimelidine.Withdrawn
ZiprasidoneThe metabolism of Diazepam can be decreased when combined with Ziprasidone.Approved
ZolazepamThe risk or severity of adverse effects can be increased when Diazepam is combined with Zolazepam.Vet Approved
ZolpidemDiazepam may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.Approved
ZonisamideThe risk or severity of adverse effects can be increased when Diazepam is combined with Zonisamide.Approved, Investigational
ZopicloneThe risk or severity of adverse effects can be increased when Diazepam is combined with Zopiclone.Approved
ZotepineThe risk or severity of adverse effects can be increased when Diazepam is combined with Zotepine.Approved
ZuclopenthixolThe risk or severity of adverse effects can be increased when Diazepam is combined with Zuclopenthixol.Approved, Investigational
Food Interactions
  • Avoid alcohol.
  • Avoid excessive quantities of coffee or tea (caffeine).
  • Avoid taking with grapefruit or grapefruit juice as grapefruit can significantly increase serum levels of this product.
  • Take with food.
References
Synthesis Reference

Chase, G.; U.S. Patent 3,102,116; August 27, 1963; assigned to Hoffmann-La Roche Inc. Reeder, E. and Sternbach, L.H.; U.S. Patent 3,109,843; November 5, 1963; assigned to
Hoffmann-La Roche lnc.
Reeder, E. and Sternbach, L.H.; U.S. Patent 3,136,815; June 9, 1964; assigned to Hoffmann-
La Roche Inc.
Reeder, E. and Sternbach, L.H.; US. Patent 3,371,085; February 27, 1968; assigned to
Hoffmann-La Roche Inc.

General References
  1. Mant A, Whicker SD, McManus P, Birkett DJ, Edmonds D, Dumbrell D: Benzodiazepine utilisation in Australia: report from a new pharmacoepidemiological database. Aust J Public Health. 1993 Dec;17(4):345-9. [PubMed:7911332 ]
  2. Earley JV, Fryer RI, Ning RY: Quinazolines and 1,4-benzodiazepines. LXXXIX: Haptens useful in benzodiazepine immunoassay development. J Pharm Sci. 1979 Jul;68(7):845-50. [PubMed:458601 ]
  3. Usami N, Yamamoto T, Shintani S, Ishikura S, Higaki Y, Katagiri Y, Hara A: Substrate specificity of human 3(20)alpha-hydroxysteroid dehydrogenase for neurosteroids and its inhibition by benzodiazepines. Biol Pharm Bull. 2002 Apr;25(4):441-5. [PubMed:11995921 ]
  4. Oishi R, Nishibori M, Itoh Y, Saeki K: Diazepam-induced decrease in histamine turnover in mouse brain. Eur J Pharmacol. 1986 May 27;124(3):337-42. [PubMed:3089825 ]
  5. McLean MJ, Macdonald RL: Benzodiazepines, but not beta carbolines, limit high frequency repetitive firing of action potentials of spinal cord neurons in cell culture. J Pharmacol Exp Ther. 1988 Feb;244(2):789-95. [PubMed:2450203 ]
External Links
ATC CodesN05BA01
AHFS Codes
  • 28:24.08
PDB EntriesNot Available
FDA labelDownload (260 KB)
MSDSDownload (53.1 KB)
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9948
Blood Brain Barrier+0.9934
Caco-2 permeable+0.8867
P-glycoprotein substrateSubstrate0.661
P-glycoprotein inhibitor INon-inhibitor0.5557
P-glycoprotein inhibitor IINon-inhibitor0.8383
Renal organic cation transporterInhibitor0.6152
CYP450 2C9 substrateNon-substrate0.6699
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateSubstrate0.8177
CYP450 1A2 substrateInhibitor0.8175
CYP450 2C9 inhibitorNon-inhibitor0.5562
CYP450 2D6 inhibitorNon-inhibitor0.858
CYP450 2C19 inhibitorInhibitor0.5221
CYP450 3A4 inhibitorInhibitor0.6423
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.5693
Ames testNon AMES toxic0.9133
CarcinogenicityNon-carcinogens0.8312
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.5946 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9948
hERG inhibition (predictor II)Non-inhibitor0.8734
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Hoffmann la roche inc
  • Roxane laboratories inc
  • Valeant pharmaceuticals international
  • Abraxis pharmaceutical products
  • Baxter healthcare corp anesthesia and critical care
  • Hospira inc
  • Marsam pharmaceuticals llc
  • Parenta pharmaceuticals inc
  • Us army medical research materiel command
  • Warner chilcott div warner lambert co
  • Watson laboratories inc
  • Pharmacia and upjohn co
  • Actavis elizabeth llc
  • Barr laboratories inc
  • Dava pharmaceuticals inc
  • Duramed pharmaceuticals inc sub barr laboratories inc
  • Ferndale laboratories inc
  • Halsey drug co inc
  • Ivax pharmaceuticals inc sub teva pharmaceuticals usa
  • Martec usa llc
  • Mylan pharmaceuticals inc
  • Par pharmaceutical inc
  • Pioneer pharmaceuticals inc
  • Sandoz inc
  • Vintage pharmaceuticals inc
  • Quantum pharmics ltd
Packagers
Dosage forms
FormRouteStrength
TabletOral2 mg
GelRectal5 mg
EmulsionIntramuscular; Intravenous5 mg
GelRectal10 mg/2mL
GelRectal2.5 mg/.5mL
GelRectal20 mg/4mL
InjectionIntramuscular; Intravenous5 mg/mL
Injection, solutionIntramuscular; Intravenous5 mg/mL
SolutionOral5 mg/5mL
TabletOral10 mg
TabletOral5 mg
LiquidIntramuscular5 mg
SolutionIntramuscular; Intravenous5 mg
Solution, concentrateOral5 mg/mL
Kit
SolutionOral1 mg
TabletOral10 mg/1
TabletOral2 mg/1
TabletOral5 mg/1
LiquidIntramuscular; Intravenous10 mg
Prices
Unit descriptionCostUnit
Diastat acudial 12.5-15-20 mg429.58USD each
Diastat acudial 5-7.5-10 mg kit429.58USD kit
Diastat AcuDial 10 mg Gel 1 Box Contains Two 10 mg Syringes423.95USD box
Diastat AcuDial 20 mg Gel 1 Box Contains Two 20 mg Syringes413.6USD box
Diastat 2.5 mg pedi system362.12USD each
Valium 10 mg tablet6.06USD tablet
Diazepam powder3.99USD g
Valium 5 mg tablet2.55USD tablet
Valium 2 mg tablet2.43USD tablet
Diazemuls 5 mg/ml Emulsion1.23USD ml
Diazepam 5 mg/ml0.69USD ml
Diazepam 10 mg tablet0.38USD tablet
Diazepam 5 mg tablet0.3USD tablet
Diazepam 2 mg tablet0.26USD tablet
Diazepam 5 mg/ml vial0.17USD ml
Apo-Diazepam 10 mg Tablet0.09USD tablet
Apo-Diazepam 5 mg Tablet0.07USD tablet
Apo-Diazepam 2 mg Tablet0.05USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2171627 No2006-01-312014-09-12Canada
US5462740 No1993-09-172013-09-17Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point125-126Chase, G.; U.S. Patent 3,102,116; August 27, 1963; assigned to Hoffmann-La Roche Inc. Reeder, E. and Sternbach, L.H.; U.S. Patent 3,109,843; November 5, 1963; assigned to Hoffmann-La Roche lnc. Reeder, E. and Sternbach, L.H.; U.S. Patent 3,136,815; June 9, 1964; assigned to Hoffmann- La Roche Inc. Reeder, E. and Sternbach, L.H.; US. Patent 3,371,085; February 27, 1968; assigned to Hoffmann-La Roche Inc.
water solubility50 mg/L (at 25 °C)YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP2.82SANGSTER (1994)
Caco2 permeability-4.32ADME Research, USCD
pKa3.4MERCK INDEX (1996)
Predicted Properties
PropertyValueSource
Water Solubility0.0122 mg/mLALOGPS
logP2.63ALOGPS
logP3.08ChemAxon
logS-4.4ALOGPS
pKa (Strongest Basic)2.92ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area32.67 Å2ChemAxon
Rotatable Bond Count1ChemAxon
Refractivity79.81 m3·mol-1ChemAxon
Polarizability29.39 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Download (10.4 KB)
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
MSMass Spectrum (Electron Ionization)splash10-0a59-2490000000-41352db33c43d0b96876View in MoNA
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as 1,4-benzodiazepines. These are organic compounds containing a benzene ring fused to a 1,4-azepine.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassBenzodiazepines
Sub Class1,4-benzodiazepines
Direct Parent1,4-benzodiazepines
Alternative Parents
Substituents
  • 1,4-benzodiazepine
  • Chlorobenzene
  • Benzenoid
  • Monocyclic benzene moiety
  • Aryl halide
  • Aryl chloride
  • Tertiary carboxylic acid amide
  • Tertiary amine
  • Lactam
  • Ketimine
  • Carboxamide group
  • Azacycle
  • Organic 1,3-dipolar compound
  • Propargyl-type 1,3-dipolar organic compound
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Organochloride
  • Organohalogen compound
  • Imine
  • Carbonyl group
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors

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. Functions as receptor for diazepines and various anesthetics, such as pentobarbital; these are bound at a separate allosteric effector binding site. Functions as ligand-gated chloride channel (By si...
Gene Name:
GABRA1
Uniprot ID:
P14867
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 ]
  3. Derry JM, Dunn SM, Davies M: Identification of a residue in the gamma-aminobutyric acid type A receptor alpha subunit that differentially affects diazepam-sensitive and -insensitive benzodiazepine site binding. J Neurochem. 2004 Mar;88(6):1431-8. [PubMed:15009644 ]
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
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 ]
  3. Derry JM, Dunn SM, Davies M: Identification of a residue in the gamma-aminobutyric acid type A receptor alpha subunit that differentially affects diazepam-sensitive and -insensitive benzodiazepine site binding. J Neurochem. 2004 Mar;88(6):1431-8. [PubMed:15009644 ]
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
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 ]
  3. Derry JM, Dunn SM, Davies M: Identification of a residue in the gamma-aminobutyric acid type A receptor alpha subunit that differentially affects diazepam-sensitive and -insensitive benzodiazepine site binding. J Neurochem. 2004 Mar;88(6):1431-8. [PubMed:15009644 ]
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
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 ]
  3. Derry JM, Dunn SM, Davies M: Identification of a residue in the gamma-aminobutyric acid type A receptor alpha subunit that differentially affects diazepam-sensitive and -insensitive benzodiazepine site binding. J Neurochem. 2004 Mar;88(6):1431-8. [PubMed:15009644 ]
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. Functions as receptor for diazepines and various anesthetics, such as pentobarbital; these are bound at a separate allosteric effector binding site. Functions as ligand-gated chloride channel (By si...
Gene Name:
GABRB1
Uniprot ID:
P18505
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:
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. Functions as receptor for diazepines and various anesthetics, such as pentobarbital; these are bound at a separate allosteric effector binding site. Functions as ligand-gated chloride channel.
Gene Name:
GABRB2
Uniprot ID:
P47870
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:
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. Functions as receptor for diazepines and various anesthetics, such as pentobarbital; these are bound at a separate allosteric effector binding site. Functions as ligand-gated chloride channel.
Gene Name:
GABRB3
Uniprot ID:
P28472
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:
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
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. Functions as receptor for diazepines and various anesthetics, such as pentobarbital; these are bound at a separate allosteric effector binding site. Functions as ligand-gated chloride channel.
Gene Name:
GABRG2
Uniprot ID:
P18507
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
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
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
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 uterus, the function of the receptor appears to be related to tissue contractility. The binding of this pI subunit with other GABA(A) receptor subunits alters the sensitivity of recombinant receptors to ...
Gene Name:
GABRP
Uniprot ID:
O00591
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 receptor could play a role in retinal neurotransmission.
Gene Name:
GABRR1
Uniprot ID:
P24046
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 receptor could play a role in retinal neurotransmission.
Gene Name:
GABRR2
Uniprot ID:
P28476
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
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
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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
potentiator
General Function:
Cholesterol binding
Specific Function:
Can bind protoporphyrin IX and may play a role in the transport of porphyrins and heme (By similarity). Promotes the transport of cholesterol across mitochondrial membranes and may play a role in lipid metabolism (PubMed:24814875), but its precise physiological role is controversial. It is apparently not required for steroid hormone biosynthesis. Was initially identified as peripheral-type benz...
Gene Name:
TSPO
Uniprot ID:
P30536
Molecular Weight:
18827.81 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  2. Falchi AM, Battetta B, Sanna F, Piludu M, Sogos V, Serra M, Melis M, Putzolu M, Diaz G: Intracellular cholesterol changes induced by translocator protein (18 kDa) TSPO/PBR ligands. Neuropharmacology. 2007 Aug;53(2):318-29. Epub 2007 Jun 2. [PubMed:17631921 ]
Kind
Protein group
Organism
Human
Pharmacological action
yes
Actions
positive allosteric modulator
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. Functions as receptor for diazepines and various anesthetics, such as pentobarbital; these are bound at a separate allosteric effector binding site. Functions as ligand-gated chloride channel (By similarity).
Components:
NameUniProt IDDetails
Gamma-aminobutyric acid receptor subunit alpha-1P14867 Details
Gamma-aminobutyric acid receptor subunit alpha-2P47869 Details
Gamma-aminobutyric acid receptor subunit alpha-3P34903 Details
Gamma-aminobutyric acid receptor subunit alpha-4P48169 Details
Gamma-aminobutyric acid receptor subunit alpha-5P31644 Details
Gamma-aminobutyric acid receptor subunit alpha-6Q16445 Details
Gamma-aminobutyric acid receptor subunit beta-1P18505 Details
Gamma-aminobutyric acid receptor subunit beta-2P47870 Details
Gamma-aminobutyric acid receptor subunit beta-3P28472 Details
Gamma-aminobutyric acid receptor subunit deltaO14764 Details
Gamma-aminobutyric acid receptor subunit epsilonP78334 Details
Gamma-aminobutyric acid receptor subunit gamma-1Q8N1C3 Details
Gamma-aminobutyric acid receptor subunit gamma-2P18507 Details
Gamma-aminobutyric acid receptor subunit gamma-3Q99928 Details
Gamma-aminobutyric acid receptor subunit piO00591 Details
Gamma-aminobutyric acid receptor subunit thetaQ9UN88 Details
References
  1. ChEMBL Compound Report Card [Link]

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 reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  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. 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 unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A5
Uniprot ID:
P20815
Molecular Weight:
57108.065 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  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. 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 unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A7
Uniprot ID:
P24462
Molecular Weight:
57525.03 Da
References
  1. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and imipramine.
Gene Name:
CYP2C19
Uniprot ID:
P33261
Molecular Weight:
55930.545 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  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. Jung F, Richardson TH, Raucy JL, Johnson EF: Diazepam metabolism by cDNA-expressed human 2C P450s: identification of P4502C18 and P4502C19 as low K(M) diazepam N-demethylases. Drug Metab Dispos. 1997 Feb;25(2):133-9. [PubMed:9029042 ]
  4. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
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 unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenyto...
Gene Name:
CYP2C9
Uniprot ID:
P11712
Molecular Weight:
55627.365 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  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. Jung F, Richardson TH, Raucy JL, Johnson EF: Diazepam metabolism by cDNA-expressed human 2C P450s: identification of P4502C18 and P4502C19 as low K(M) diazepam N-demethylases. Drug Metab Dispos. 1997 Feb;25(2):133-9. [PubMed:9029042 ]
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 unrelated compounds, including steroids, fatty acids, and xenobiotics. Acts as a 1,4-cineole 2-exo-monooxygenase.
Gene Name:
CYP2B6
Uniprot ID:
P20813
Molecular Weight:
56277.81 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  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. Lin Y, Lu P, Tang C, Mei Q, Sandig G, Rodrigues AD, Rushmore TH, Shou M: Substrate inhibition kinetics for cytochrome P450-catalyzed reactions. Drug Metab Dispos. 2001 Apr;29(4 Pt 1):368-74. [PubMed:11259318 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
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 unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
Molecular Weight:
58293.76 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. Source [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 unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP2C18
Uniprot ID:
P33260
Molecular Weight:
55710.075 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 ]
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 unrelated compounds, including steroids, fatty acids, and xenobiotics. In the epoxidation of arachidonic acid it generates only 14,15- and 11,12-cis-epoxyeicosatrienoic acids. It is the principal enzyme...
Gene Name:
CYP2C8
Uniprot ID:
P10632
Molecular Weight:
55824.275 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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Prostaglandin-endoperoxide synthase activity
Specific Function:
Converts arachidonate to prostaglandin H2 (PGH2), a committed step in prostanoid synthesis. Involved in the constitutive production of prostanoids in particular in the stomach and platelets. In gastric epithelial cells, it is a key step in the generation of prostaglandins, such as prostaglandin E2 (PGE2), which plays an important role in cytoprotection. In platelets, it is involved in the gener...
Gene Name:
PTGS1
Uniprot ID:
P23219
Molecular Weight:
68685.82 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
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 or carcinogenic forms.
Gene Name:
CYP2E1
Uniprot ID:
P05181
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 ]

Carriers

Kind
Protein
Organism
Human
Pharmacological action
no
General Function:
Toxic substance binding
Specific Function:
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloidal osmotic pressure of blood. Major zinc transporter in plasma, typically binds about 80% of all plasma zinc.
Gene Name:
ALB
Uniprot ID:
P02768
Molecular Weight:
69365.94 Da
References
  1. Bertucci C, Wainer IW: Improved chromatographic performance of a modified human albumin based stationary phase. Chirality. 1997;9(4):335-40. [PubMed:9275312 ]
  2. Brodersen R, Honore B: Drug binding properties of neonatal albumin. Acta Paediatr Scand. 1989 May;78(3):342-6. [PubMed:2545072 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
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
Molecular Weight:
141477.255 Da
References
  1. Yamazaki M, Neway WE, Ohe T, Chen I, Rowe JF, Hochman JH, Chiba M, Lin JH: In vitro substrate identification studies for p-glycoprotein-mediated transport: species difference and predictability of in vivo results. J Pharmacol Exp Ther. 2001 Mar;296(3):723-35. [PubMed:11181899 ]
  2. Adachi Y, Suzuki H, Sugiyama Y: Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8. [PubMed:11785684 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23