Identification

Name
Diazepam
Accession Number
DB00829  (APRD00642, DB07699)
Type
Small Molecule
Groups
Approved, Illicit, Vet Approved
Description

A 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
External IDs
NSC-169897 / NSC-77518 / RO 5-2807 / RO-5-2807 / WY-3467
Product Ingredients
IngredientUNIICASInChI Key
Diazepam hydrochloride6JD21U639H52468-36-7BPYZIOINRAWEQL-UHFFFAOYSA-N
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Bio-diazepamTablet5 mgOralBiomed Pharma2003-04-23Not applicableCanada
Bio-diazepamTablet10 mgOralBiomed Pharma2003-04-23Not applicableCanada
Bio-diazepamTablet2 mgOralBiomed Pharma2003-04-23Not applicableCanada
DiastatGel10 mg/2mLRectalValeant Pharmaceuticals North America1997-07-29Not applicableUs
DiastatGel5 mgRectalValeant Pharmaceuticals North America2000-01-28Not applicableCanada
DiastatGel20 mg/4mLRectalValeant Pharmaceuticals North America1997-07-29Not applicableUs
DiastatGel2.5 mg/.5mLRectalValeant Pharmaceuticals North America1997-07-29Not applicableUs
DiazemulsEmulsion5 mgIntramuscular; IntravenousActavis Group Ptc Ehf.1995-12-312016-01-05Canada
DiazepamGel10 mg/2mLRectalOceanside Pharmaceuticals1997-07-29Not applicableUs
DiazepamGel20 mg/4mLRectalTeva2010-09-03Not applicableUs
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo Diazepam Tab 10mgTablet10 mgOralApotex Corporation1979-12-31Not applicableCanada
Apo Diazepam Tab 2mgTablet2 mgOralApotex Corporation1979-12-31Not applicableCanada
Apo Diazepam Tab 5mgTablet5 mgOralApotex Corporation1977-12-31Not applicableCanada
DiazepamTablet5 mg/1OralLake Erie Medical &Surgical Supply Dba Quality Care Products Llc2011-11-292017-02-02Us
DiazepamTablet2 mg/1OralRemedy Repack2015-07-21Not applicableUs
DiazepamTablet5 mg/1OralRemedy Repack2016-11-10Not applicableUs
DiazepamTablet5 mg/1OralKaiser Foundations Hospitals2002-01-29Not applicableUs
DiazepamTablet10 mg/1OralPhysicians Total Care, Inc.2004-06-03Not applicableUs
DiazepamTablet5 mg/1OralMc Kesson Contract Packaging2011-10-13Not applicableUs
DiazepamTablet5 mg/1OralQualitest2006-03-312017-10-31Us
Unapproved/Other Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
DiazepamTablet10 mg/1OralDirectrx2017-11-01Not applicableUs
DiazepamTablet10 mg/1OralDirectrx2016-11-01Not applicableUs
International/Other Brands
Diapam (Orion) / Nervium (Saba) / Relanium (GlaxoSmithKline) / Valium
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
Gabavale-5Diazepam + CholineKitPhysician Therapeutics Llc2011-05-072016-10-13Us
Topical Nerve PainDiazepam (.1 g/100mL) + Diclofenac sodium (.1 g/100mL) + Gabapentin (.1 g/100mL) + Ketamine (.1 g/100mL)CreamTopicalDr Marc's Manufacturing And Sales2016-02-23Not applicableUs
Topical PainDiazepam (.1 g/100mL) + Hydrocodone (.1 g/100mL) + Ibuprofen (.1 g/100mL) + Tramadol (.1 g/100mL)CreamTopicalDr Marc's Manufacturing And Sales2016-02-23Not applicableUs
Categories
UNII
Q3JTX2Q7TU
CAS number
439-14-5
Weight
Average: 284.74
Monoisotopic: 284.071640755
Chemical Formula
C16H13ClN2O
InChI Key
AAOVKJBEBIDNHE-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

Indication

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.

Structured Indications
Pharmacodynamics

Diazepam, 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 action

Benzodiazepines 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.

TargetActionsOrganism
AGamma-aminobutyric acid receptor subunit alpha-1
potentiator
Human
AGamma-aminobutyric acid receptor subunit alpha-2
potentiator
Human
AGamma-aminobutyric acid receptor subunit alpha-3
potentiator
Human
AGamma-aminobutyric acid receptor subunit alpha-5
potentiator
Human
AGamma-aminobutyric acid receptor subunit beta-1
potentiator
Human
AGamma-aminobutyric acid receptor subunit beta-2
potentiator
Human
AGamma-aminobutyric acid receptor subunit beta-3
potentiator
Human
AGamma-aminobutyric acid receptor subunit gamma-1
potentiator
Human
AGamma-aminobutyric acid receptor subunit gamma-2
potentiator
Human
AGamma-aminobutyric acid receptor subunit gamma-3
potentiator
Human
AGamma-aminobutyric acid receptor subunit delta
potentiator
Human
AGamma-aminobutyric acid receptor subunit epsilon
potentiator
Human
AGamma-aminobutyric acid receptor subunit pi
potentiator
Human
AGamma-aminobutyric acid receptor subunit rho-1
potentiator
Human
AGamma-aminobutyric acid receptor subunit rho-2
potentiator
Human
AGamma-aminobutyric acid receptor subunit rho-3
potentiator
Human
AGamma-aminobutyric acid receptor subunit theta
potentiator
Human
UTranslocator protein
potentiator
Human
AGABA-A receptor (anion channel)
positive allosteric modulator
Human
Absorption

Essentially complete, with a bioavailability of 93%.

Volume of distribution
  • 0.8 to 1.0 L/kg [young healthy males]
Protein binding

98.5%

Metabolism

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

Route of elimination

Diazepam and its metabolites are excreted mainly in the urine, predominantly as their glucuronide conjugates.

Half life

Biphasic 1-2 days and 2-5 days, active metabolites with long half lives.

Clearance
  • 20-30 mL/min
Toxicity

Symptoms of overdose include somnolence, confusion, coma, and diminished reflexes. Respiration, pulse and blood pressure should be monitored.

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Interacting Gene/EnzymeAllele nameGenotype(s)Defining Change(s)Type(s)DescriptionDetails
Cytochrome P450 2C19CYP2C19*2ANot Available681G>AEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2C19CYP2C19*2BNot Available681G>AEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2C19CYP2C19*3Not Available636G>AEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2C19CYP2C19*4Not Available1A>GEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2C19CYP2C19*5Not Available1297C>TEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2C19CYP2C19*6Not Available395G>AEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2C19CYP2C19*7Not Available19294T>AEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2C19CYP2C19*22Not Available557G>C / 991A>GEffect InferredPoor drug metabolizer.Details
Cytochrome P450 2C19CYP2C19*24Not Available99C>T / 991A>G  … show all Effect InferredPoor drug metabolizer.Details
Cytochrome P450 2C19CYP2C19*35Not Available12662A>GEffect InferredPoor drug metabolizer.Details
Cytochrome P450 3A4CYP3A4*20Not Available1461_1462insAEffect InferredPoor drug metabolizer.Details
Cytochrome P450 3A4CYP3A4*26Not Available802C>TEffect InferredPoor drug metabolizer.Details

Interactions

Drug Interactions
DrugInteractionDrug group
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
AdipiplonThe risk or severity of adverse effects can be increased when Diazepam is combined with Adipiplon.Investigational
AgomelatineThe risk or severity of adverse effects can be increased when Diazepam is combined with Agomelatine.Approved, Investigational
AlaproclateThe risk or severity of adverse effects can be increased when Diazepam is combined with Alaproclate.Experimental
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
AllopregnanoloneThe risk or severity of adverse effects can be increased when Diazepam is combined with Allopregnanolone.Investigational
AlphacetylmethadolThe risk or severity of adverse effects can be increased when Diazepam is combined with Alphacetylmethadol.Experimental, Illicit
AlphaprodineThe risk or severity of adverse effects can be increased when Diazepam is combined with Alphaprodine.Illicit
AlprazolamThe risk or severity of adverse effects can be increased when Alprazolam is combined with Diazepam.Approved, Illicit, Investigational
Ambroxol acefyllinateThe therapeutic efficacy of Diazepam can be decreased when used in combination with Ambroxol acefyllinate.Experimental, Investigational
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 risk or severity of adverse effects can be increased when Diazepam is combined with Amitriptyline.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
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
AtazanavirThe metabolism of Diazepam can be decreased when combined with Atazanavir.Approved, Investigational
AtomoxetineThe metabolism of Diazepam can be decreased when combined with Atomoxetine.Approved
AtorvastatinThe risk or severity of adverse effects can be increased when Diazepam is combined with Atorvastatin.Approved
AzaperoneThe risk or severity of adverse effects can be increased when Diazepam is combined with Azaperone.Investigational, Vet Approved
AzelastineDiazepam may increase the central nervous system depressant (CNS depressant) activities of Azelastine.Approved
AzithromycinThe metabolism of Diazepam can be decreased when 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 risk or severity of adverse effects can be increased when Diazepam is combined with Benzocaine.Approved
Benzyl alcoholThe risk or severity of adverse effects can be increased when Diazepam is combined with Benzyl alcohol.Approved
BoceprevirThe metabolism of Diazepam can be decreased when combined with Boceprevir.Approved, Withdrawn
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
BrexpiprazoleThe risk or severity of adverse effects can be increased when Diazepam is combined with Brexpiprazole.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
BromisovalThe risk or severity of adverse effects can be increased when Diazepam is combined with Bromisoval.Experimental
BromocriptineThe risk or severity of adverse effects can be increased when Bromocriptine is combined with Diazepam.Approved, Investigational
BromperidolThe risk or severity of adverse effects can be increased when Diazepam is combined with Bromperidol.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, Investigational, Withdrawn
BupivacaineThe risk or severity of adverse effects can be increased when Diazepam is combined with Bupivacaine.Approved, Investigational
BuprenorphineDiazepam may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.Approved, Illicit, Investigational, Vet Approved
BuspironeThe risk or severity of adverse effects can be increased when Buspirone is combined with Diazepam.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
CabergolineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Diazepam.Approved
CaffeineThe metabolism of Diazepam can be decreased when combined with Caffeine.Approved
CanertinibThe risk or severity of adverse effects can be increased when Diazepam is combined with Canertinib.Investigational
CapecitabineThe metabolism of Diazepam can be decreased when combined with Capecitabine.Approved, Investigational
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, Investigational, Vet Approved
CarisoprodolThe risk or severity of adverse effects can be increased when Diazepam is combined with Carisoprodol.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
CerivastatinThe serum concentration of Cerivastatin can be increased when it is combined with Diazepam.Withdrawn
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, Investigational, Withdrawn
ChloroprocaineThe risk or severity of adverse effects can be increased when Diazepam is combined with Chloroprocaine.Approved
ChlorphenamineThe risk or severity of adverse effects can be increased when Diazepam is combined with Chlorphenamine.Approved
ChlorpromazineThe risk or severity of adverse effects can be increased when Chlorpromazine is combined with Diazepam.Approved, Vet Approved
ChlorprothixeneThe risk or severity of adverse effects can be increased when Diazepam is combined with Chlorprothixene.Approved, Investigational, 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
CilostazolThe serum concentration of Cilostazol can be increased when it is combined with Diazepam.Approved
CimetidineThe metabolism of Diazepam can be decreased when combined with Cimetidine.Approved
CinchocaineThe risk or severity of adverse effects can be increased when Diazepam is combined with Cinchocaine.Approved, Vet Approved
CitalopramThe metabolism of Diazepam can be decreased when 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
clomethiazoleThe risk or severity of adverse effects can be increased when Diazepam is combined with clomethiazole.Investigational
ClomipramineThe risk or severity of adverse effects can be increased when Diazepam 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
ClopenthixolThe risk or severity of adverse effects can be increased when Diazepam is combined with Clopenthixol.Experimental
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
ClothiapineThe risk or severity of adverse effects can be increased when Diazepam is combined with Clothiapine.Experimental
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
ConivaptanThe serum concentration of Diazepam can be increased when it is combined with Conivaptan.Approved, Investigational
CrisaboroleThe metabolism of Diazepam can be decreased when combined with Crisaborole.Approved
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
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
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 Diazepam is combined with Dapiprazole.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
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 risk or severity of adverse effects can be increased when Diazepam is combined with Desipramine.Approved
DesloratadineThe risk or severity of adverse effects can be increased when Diazepam 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
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 Diazepam is combined with Dexmedetomidine.Approved, Vet 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 Diazepam is combined with Dextropropoxyphene.Approved, Illicit, Investigational, Withdrawn
DezocineThe risk or severity of adverse effects can be increased when Diazepam is combined with Dezocine.Approved, Investigational
Diethyl etherThe risk or severity of adverse effects can be increased when Diazepam is combined with Diethyl ether.Experimental
DifenoxinThe risk or severity of adverse effects can be increased when Diazepam is combined with Difenoxin.Approved, Illicit
DihydrocodeineThe risk or severity of adverse effects can be increased when Diazepam is combined with Dihydrocodeine.Approved, Illicit
DihydroergocornineThe risk or severity of adverse effects can be increased when Dihydroergocornine is combined with Diazepam.Approved
DihydroergocristineThe risk or severity of adverse effects can be increased when Dihydroergocristine is combined with Diazepam.Experimental
DihydroergocryptineThe risk or severity of adverse effects can be increased when Dihydroergocryptine is combined with Diazepam.Experimental
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
DisulfiramThe serum concentration of Diazepam can be increased when it is combined with Disulfiram.Approved
DixyrazineThe risk or severity of adverse effects can be increased when Diazepam is combined with Dixyrazine.Experimental
DoramectinThe risk or severity of adverse effects can be increased when Diazepam is combined with Doramectin.Vet Approved
DosulepinThe metabolism of Diazepam can be decreased when combined with Dosulepin.Approved
DoxepinThe risk or severity of adverse effects can be increased when Diazepam is combined with Doxepin.Approved
DoxorubicinThe metabolism of Diazepam can be decreased when 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 Diazepam is combined with Dyclonine.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
EcopipamThe risk or severity of adverse effects can be increased when Diazepam is combined with Ecopipam.Investigational
EfavirenzThe risk or severity of adverse effects can be increased when Diazepam is combined with Efavirenz.Approved, Investigational
EltanoloneThe risk or severity of adverse effects can be increased when Diazepam is combined with Eltanolone.Investigational
EnfluraneThe risk or severity of adverse effects can be increased when Diazepam is combined with Enflurane.Approved, Investigational, 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 risk or severity of adverse effects can be increased when Ergonovine is combined with Diazepam.Approved
ErgotamineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Diazepam.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 metabolism of Diazepam can be decreased when 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
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 Diazepam is combined with Ethchlorvynol.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 chlorideThe risk or severity of adverse effects can be increased when Diazepam is combined with Ethyl chloride.Experimental, Investigational
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.Investigational, 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 Diazepam is combined with Etomidate.Approved
EtoperidoneThe risk or severity of adverse effects can be increased when Diazepam is combined with Etoperidone.Withdrawn
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 metabolism of Diazepam can be decreased when 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 risk or severity of adverse effects can be increased when Fentanyl is combined with Diazepam.Approved, Illicit, Investigational, Vet Approved
FexofenadineThe risk or severity of adverse effects can be increased when Diazepam is combined with Fexofenadine.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
FluanisoneThe risk or severity of adverse effects can be increased when Diazepam is combined with Fluanisone.Experimental
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 metabolism of Diazepam can be decreased when combined with Fluoxetine.Approved, Vet Approved
FlupentixolThe risk or severity of adverse effects can be increased when Diazepam is combined with Flupentixol.Approved, Withdrawn
FluphenazineThe risk or severity of adverse effects can be increased when Fluphenazine is combined with Diazepam.Approved
FlurazepamThe risk or severity of adverse effects can be increased when Flurazepam is combined with Diazepam.Approved, Illicit
FluspirileneThe risk or severity of adverse effects can be increased when Diazepam is combined with Fluspirilene.Approved, Investigational
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, Investigational
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, Investigational
GemfibrozilThe metabolism of Diazepam can be decreased when combined with Gemfibrozil.Approved
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
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 Diazepam is combined with Halazepam.Approved, Illicit, Withdrawn
HaloperidolThe risk or severity of adverse effects can be increased when Haloperidol is combined with Diazepam.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, Investigational
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
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 risk or severity of adverse effects can be increased when Diazepam 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
IndiplonThe risk or severity of adverse effects can be increased when Diazepam is combined with Indiplon.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
KetamineThe risk or severity of adverse effects can be increased when Diazepam 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, Investigational
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
LapatinibThe metabolism of Diazepam can be decreased when 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, Investigational
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
Levomethadyl AcetateThe risk or severity of adverse effects can be increased when Diazepam is combined with Levomethadyl Acetate.Approved, Investigational
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
LidocaineThe metabolism of Diazepam can be decreased when combined with Lidocaine.Approved, Vet Approved
LisurideThe risk or severity of adverse effects can be increased when Lisuride is combined with Diazepam.Approved, Investigational
LithiumThe risk or severity of adverse effects can be increased when Diazepam is combined with Lithium.Approved
LobeglitazoneThe metabolism of Diazepam can be decreased when combined with Lobeglitazone.Approved, Investigational
LofentanilThe risk or severity of adverse effects can be increased when Diazepam is combined with Lofentanil.Illicit
LopinavirThe metabolism of Diazepam can be decreased when combined with Lopinavir.Approved
LoprazolamThe risk or severity of adverse effects can be increased when Diazepam is combined with Loprazolam.Experimental
LoratadineThe risk or severity of adverse effects can be increased when Diazepam is combined with Loratadine.Approved
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Diazepam.Approved
LormetazepamThe risk or severity of adverse effects can be increased when Diazepam is combined with Lormetazepam.Approved
LosartanThe metabolism of Diazepam can be decreased when 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
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
Lysergic Acid DiethylamideThe risk or severity of adverse effects can be increased when Lysergic Acid Diethylamide is combined with Diazepam.Illicit, Investigational, Withdrawn
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Diazepam.Approved, Vet Approved
ManidipineThe metabolism of Diazepam can be decreased when combined with Manidipine.Approved, Investigational
MaprotilineThe risk or severity of adverse effects can be increased when Diazepam is combined with Maprotiline.Approved
MebicarThe risk or severity of adverse effects can be increased when Diazepam is combined with Mebicar.Experimental
MeclizineThe risk or severity of adverse effects can be increased when Diazepam is combined with Meclizine.Approved
MedazepamThe risk or severity of adverse effects can be increased when Diazepam is combined with Medazepam.Experimental
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
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, Investigational
MepivacaineThe risk or severity of adverse effects can be increased when Diazepam is combined with Mepivacaine.Approved, Vet Approved
MeprobamateThe risk or severity of adverse effects can be increased when Meprobamate is combined with Diazepam.Approved, Illicit
MeptazinolThe risk or severity of adverse effects can be increased when Diazepam is combined with Meptazinol.Experimental
MesoridazineThe risk or severity of adverse effects can be increased when Diazepam is combined with Mesoridazine.Approved, Investigational
MetaxaloneThe risk or severity of adverse effects can be increased when Diazepam is combined with Metaxalone.Approved
MetergolineThe risk or severity of adverse effects can be increased when Metergoline is combined with Diazepam.Experimental
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, Investigational, Vet Approved
MethsuximideThe risk or severity of adverse effects can be increased when Diazepam is combined with Methsuximide.Approved
MethylecgonineThe risk or severity of adverse effects can be increased when Diazepam is combined with Methylecgonine.Experimental
MethylergometrineThe risk or severity of adverse effects can be increased when Methylergometrine is combined with Diazepam.Approved
MethylphenobarbitalThe risk or severity of adverse effects can be increased when Diazepam is combined with Methylphenobarbital.Approved
MethysergideThe risk or severity of adverse effects can be increased when Methysergide is combined with Diazepam.Approved
MetyrosineDiazepam may increase the sedative activities of Metyrosine.Approved
MevastatinThe serum concentration of Mevastatin can be increased when it is combined with Diazepam.Experimental
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, Investigational
MidazolamThe risk or severity of adverse effects can be increased when Midazolam is combined with Diazepam.Approved, Illicit
MidostaurinThe metabolism of Diazepam can be decreased when combined with Midostaurin.Approved
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
MitotaneThe serum concentration of Diazepam can be decreased when it is combined with Mitotane.Approved
MoclobemideThe metabolism of Diazepam can be decreased when combined with Moclobemide.Approved
ModafinilThe metabolism of Diazepam can be decreased when combined with Modafinil.Approved, Investigational
MolindoneThe risk or severity of adverse effects can be increased when Diazepam is combined with Molindone.Approved
MorphineThe risk or severity of adverse effects can be increased when Morphine is combined with Diazepam.Approved, Investigational
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Diazepam.Approved, Investigational
NalbuphineThe risk or severity of adverse effects can be increased when Diazepam is combined with Nalbuphine.Approved
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
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
NicergolineThe risk or severity of adverse effects can be increased when Nicergoline is combined with Diazepam.Approved, Investigational
NilotinibThe metabolism of Diazepam can be decreased when combined with Nilotinib.Approved, Investigational
NitrazepamThe risk or severity of adverse effects can be increased when Diazepam is combined with Nitrazepam.Approved
Nitrous oxideThe risk or severity of adverse effects can be increased when Diazepam is combined with Nitrous oxide.Approved, Vet Approved
NorfluraneThe risk or severity of adverse effects can be increased when Diazepam is combined with Norflurane.Investigational
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 metabolism of Diazepam can be decreased when 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
OxethazaineThe risk or severity of adverse effects can be increased when Diazepam is combined with Oxethazaine.Approved, 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
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
PantoprazoleThe metabolism of Diazepam can be decreased when combined with Pantoprazole.Approved
ParaldehydeDiazepam may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.Approved, Investigational
ParoxetineThe metabolism of Diazepam can be decreased when combined with Paroxetine.Approved, Investigational
Peginterferon alfa-2bThe serum concentration of Diazepam can be increased when it is combined with Peginterferon alfa-2b.Approved
PenfluridolThe risk or severity of adverse effects can be increased when Diazepam is combined with Penfluridol.Experimental
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
PergolideThe risk or severity of adverse effects can be increased when Pergolide is combined with Diazepam.Approved, Investigational, Vet Approved, Withdrawn
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
PhenazocineThe risk or severity of adverse effects can be increased when Diazepam is combined with Phenazocine.Experimental
PhenibutThe risk or severity of adverse effects can be increased when Diazepam is combined with Phenibut.Experimental
PhenobarbitalThe metabolism of Diazepam can be increased when combined with Phenobarbital.Approved
PhenoperidineThe risk or severity of adverse effects can be increased when Diazepam is combined with Phenoperidine.Experimental
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 risk or severity of adverse effects can be increased when Diazepam 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, Investigational
PipotiazineThe risk or severity of adverse effects can be increased when Diazepam is combined with Pipotiazine.Approved, Investigational
PiritramideThe risk or severity of adverse effects can be increased when Diazepam is combined with Piritramide.Investigational
PitavastatinThe serum concentration of Pitavastatin can be increased when it is combined with Diazepam.Approved
PizotifenThe risk or severity of adverse effects can be increased when Diazepam is combined with Pizotifen.Approved
PomalidomideThe risk or severity of adverse effects can be increased when Diazepam is combined with Pomalidomide.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 Pravastatin can be increased when it is combined with Diazepam.Approved
PrazepamThe risk or severity of adverse effects can be increased when Diazepam is combined with Prazepam.Approved, Illicit
PregabalinThe risk or severity of adverse effects can be increased when Pregabalin is combined with Diazepam.Approved, Illicit, Investigational
PrilocaineThe risk or severity of adverse effects can be increased when Diazepam is combined with Prilocaine.Approved
PrimidoneThe metabolism of Diazepam can be increased when combined with Primidone.Approved, Vet Approved
ProcaineThe risk or severity of adverse effects can be increased when Diazepam is combined with Procaine.Approved, Investigational, Vet Approved
ProchlorperazineThe risk or severity of adverse effects can be increased when Prochlorperazine is combined with Diazepam.Approved, Vet Approved
PromazineThe risk or severity of adverse effects can be increased when Promazine is combined with Diazepam.Approved, Vet Approved
PromethazineThe risk or severity of adverse effects can be increased when Diazepam is combined with Promethazine.Approved
PropanididThe risk or severity of adverse effects can be increased when Diazepam is combined with Propanidid.Experimental
ProparacaineThe risk or severity of adverse effects can be increased when Diazepam is combined with Proparacaine.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
ProtriptylineThe risk or severity of adverse effects can be increased when Diazepam is combined with Protriptyline.Approved
ProxibarbalThe risk or severity of adverse effects can be increased when Diazepam is combined with Proxibarbal.Experimental
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
QuetiapineThe risk or severity of adverse effects can be increased when Diazepam is combined with Quetiapine.Approved
QuinineThe metabolism of Diazepam can be decreased when combined with Quinine.Approved
QuinisocaineThe risk or severity of adverse effects can be increased when Diazepam is combined with Quinisocaine.Experimental
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
RanolazineThe serum concentration of Diazepam can be increased when it is combined with Ranolazine.Approved, Investigational
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 Diazepam is combined with Remoxipride.Approved, Withdrawn
ReserpineThe risk or severity of adverse effects can be increased when Reserpine is combined with Diazepam.Approved, Investigational
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
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
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 Diazepam is combined with Ropivacaine.Approved
RosiglitazoneThe metabolism of Diazepam can be decreased when combined with Rosiglitazone.Approved, Investigational
RosuvastatinThe serum concentration of Rosuvastatin can be increased when it is combined with Diazepam.Approved
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
SaquinavirThe serum concentration of Diazepam can be increased when it is combined with Saquinavir.Approved, Investigational
ScopolamineThe risk or severity of adverse effects can be increased when Diazepam is combined with Scopolamine.Approved
SecobarbitalThe metabolism of Diazepam can be increased when combined with Secobarbital.Approved, Vet Approved
SepranoloneThe risk or severity of adverse effects can be increased when Diazepam is combined with Sepranolone.Investigational
SertindoleThe risk or severity of adverse effects can be increased when Diazepam is combined with Sertindole.Approved, Investigational, Withdrawn
SertralineThe metabolism of Diazepam can be decreased when 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 Simvastatin can be increased when it is combined with Diazepam.Approved
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Diazepam.Approved
SorafenibThe metabolism of Diazepam can be decreased when combined with Sorafenib.Approved, Investigational
St. John's WortThe serum concentration of Diazepam can be decreased when it is combined with St. John's Wort.Investigational, Nutraceutical
StiripentolThe serum concentration of Diazepam can be increased when it is combined with Stiripentol.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
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 Diazepam is combined with Sulpiride.Approved, Investigational
SultoprideThe risk or severity of adverse effects can be increased when Diazepam is combined with Sultopride.Experimental
SuvorexantDiazepam may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.Approved
TamoxifenThe metabolism of Diazepam can be decreased when 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
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, Withdrawn
TelithromycinThe metabolism of Diazepam can be decreased when combined with Telithromycin.Approved
TemazepamThe risk or severity of adverse effects can be increased when Temazepam is combined with Diazepam.Approved
Tenofovir disoproxilThe metabolism of Diazepam can be decreased when combined with Tenofovir disoproxil.Approved, Investigational
TergurideThe risk or severity of adverse effects can be increased when Terguride is combined with Diazepam.Experimental
TeriflunomideThe serum concentration of Diazepam can be decreased when it is combined with Teriflunomide.Approved
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
TetrahydropalmatineThe risk or severity of adverse effects can be increased when Diazepam is combined with Tetrahydropalmatine.Investigational
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 Diazepam is combined with Thiopental.Approved, Vet Approved
ThioridazineThe risk or severity of adverse effects can be increased when Thioridazine is combined with Diazepam.Approved, Withdrawn
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.Approved, Investigational
TicagrelorThe metabolism of Diazepam can be decreased when 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
TilidineThe risk or severity of adverse effects can be increased when Diazepam is combined with Tilidine.Experimental
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
TopiramateThe risk or severity of adverse effects can be increased when Diazepam is combined with Topiramate.Approved
TopiroxostatThe metabolism of Diazepam can be decreased when combined with Topiroxostat.Approved, Investigational
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 Diazepam is combined with Tranylcypromine.Approved
TrazodoneThe risk or severity of adverse effects can be increased when Diazepam is combined with Trazodone.Approved, Investigational
TriazolamThe risk or severity of adverse effects can be increased when Diazepam is combined with Triazolam.Approved
Tricaine methanesulfonateThe risk or severity of adverse effects can be increased when Diazepam is combined with Tricaine methanesulfonate.Vet Approved
TrichloroethyleneThe risk or severity of adverse effects can be increased when Diazepam is combined with Trichloroethylene.Experimental
TrifluoperazineThe risk or severity of adverse effects can be increased when Diazepam is combined with Trifluoperazine.Approved
TrifluperidolThe risk or severity of adverse effects can be increased when Diazepam is combined with Trifluperidol.Experimental
TriflupromazineThe risk or severity of adverse effects can be increased when Diazepam is combined with Triflupromazine.Approved, Vet Approved
TrimethoprimThe metabolism of Diazepam can be decreased when combined with Trimethoprim.Approved, Vet Approved
TrimipramineThe risk or severity of adverse effects can be increased when Diazepam is combined with Trimipramine.Approved
TriprolidineThe risk or severity of adverse effects can be increased when Diazepam is combined with Triprolidine.Approved
UbidecarenoneThe serum concentration of Ubidecarenone can be increased when it is combined with Diazepam.Approved, Experimental
Valproic AcidThe risk or severity of adverse effects can be increased when Diazepam is combined with Valproic Acid.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
VeraliprideThe risk or severity of adverse effects can be increased when Diazepam is combined with Veralipride.Experimental
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
Vinyl etherThe risk or severity of adverse effects can be increased when Diazepam is combined with Vinyl ether.Experimental
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
XenonThe risk or severity of adverse effects can be increased when Diazepam is combined with Xenon.Experimental
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 risk or severity of adverse effects can be increased when Diazepam 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, Investigational
ZucapsaicinThe metabolism of Diazepam can be decreased when combined with Zucapsaicin.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
Human Metabolome Database
HMDB14967
KEGG Drug
D00293
KEGG Compound
C06948
PubChem Compound
3016
PubChem Substance
46505210
ChemSpider
2908
BindingDB
50000766
ChEBI
49575
ChEMBL
CHEMBL12
Therapeutic Targets Database
DNC000549
PharmGKB
PA449283
IUPHAR
3364
Guide to Pharmacology
GtP Drug Page
HET
DZP
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
PDRhealth
PDRhealth Drug Page
Wikipedia
Diazepam
ATC Codes
N05BA01 — Diazepam
AHFS Codes
  • 28:24.08 — Benzodiazepines
PDB Entries
2bxf
FDA label
Download (260 KB)
MSDS
Download (53.1 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0CompletedTreatmentAnxiety Disease1
0RecruitingTreatmentLumbar Spinal Instability / Lumbar Spine Degeneration / Spinal Stenosis of Lumbar Region1
1CompletedNot AvailableEpilepsies1
1CompletedNot AvailableHealthy Volunteers1
1Not Yet RecruitingPreventionPost-Operative Delirium1
1RecruitingTreatmentAcute Repetitive Seizures1
1TerminatedTreatmentMetabolism, Drug1
1Unknown StatusNot AvailableRheumatoid Arthritis1
2CompletedTreatmentAbdominal Pain (AP) / Cannabinoid / Pancreatitis, Chronic / Tetrahydrocannabinol1
2CompletedTreatmentEpilepsies1
2CompletedTreatmentPelvic Floor Disorders / Pelvic Pain1
2CompletedTreatmentSeizures1
2RecruitingTreatmentPost-Operative Pain1
2TerminatedTreatmentRefractory Epilepsy1
2Unknown StatusTreatmentPain1
2, 3CompletedPreventionPain Relief During Prostate Biopsy1
2, 3CompletedTreatmentRefractory seizure disorders1
2, 3Enrolling by InvitationTreatmentLandau-Kleffner Syndrome / Status Epilepticus, Electrographic1
3CompletedTreatmentEpilepsies / Epilepsy, Complex Partial / Epilepsy, Generalized / Epilepsy, Localization Related / Seizures1
3CompletedTreatmentRefractory seizure disorders1
3RecruitingTreatmentAcute Repetitive Seizures / Breakthrough Seizures1
3TerminatedTreatmentAnxiety Disorders / Dementias / Depression / Psychosomatic Disorders / Schizophrenic Disorders1
4CompletedTreatmentFeeling Anxious1
4CompletedTreatmentLow Back Pain (LBP)1
4CompletedTreatmentMethamphetamine-induced Psychosis1
4CompletedTreatmentOpiate Dependent Patients Who Are Undergoing Inpatient Detoxification in Singapore1
4Not Yet RecruitingSupportive CareInfertilities1
4RecruitingTreatmentAcute Agitation / Behavioural Emergency1
4RecruitingTreatmentAlcohol Use Disorder (AUD) / Alcohol Withdrawal Syndrome(AWS)1
4Unknown StatusPreventionPosttraumatic Stress Disorders1
Not AvailableCompletedNot AvailableAlcohol Withdrawal Syndrome(AWS)1
Not AvailableCompletedNot AvailableHealthy Volunteers1
Not AvailableCompletedTreatmentAlcohol Withdrawal Syndrome(AWS)1
Not AvailableCompletedTreatmentAlcoholism1
Not AvailableCompletedTreatmentBenign Paroxysmal Positional Vertigo (BPPV)1
Not AvailableCompletedTreatmentCancer, Breast / Postoperative pain1
Not AvailableCompletedTreatmentColonoscopy1
Not AvailableCompletedTreatmentNeoplasms, Pancreatic1
Not AvailableCompletedTreatmentOccasional Constipation1
Not AvailableRecruitingNot AvailableAcute Bacterial Exacerbation of Chronic Bronchitis (ABECB) / Acute Bacterial Sinusitis (ABS) / Acute Decompensated Heart Failure (ADHF) / Acute Pyelonephritis / Adenovirus / Adjunct to general anesthesia therapy / Adrenal Insufficiency / Airway Swelling / Anaesthesia therapy / Anxiolysis / Arterial Hypotension / Autism, Early Infantile / Autistic Disorder / Bartonellosis / Benzodiazepine Withdrawal / Benzodiazepines / Bipolar Disorder (BD) / Bloodstream Infections / Bone and Joint Infections / Brain Swelling / Bronchospasm / Brucellosis / Cardiac Arrest / Central Nervous System Infections / Cholera / Chronic Bacterial Prostatitis / Community Acquired Pneumonia (CAP) / Complicated Urinary Tract Infections / Convulsions / Cyanide Poisoning / Cytomegalovirus Retinitis / Drug hypersensitivity reaction / Early-onset Schizophrenia Spectrum Disorders / Edema / Epilepsies / Feeling Anxious / Flu caused by Influenza / Gastroparesis / GYNAECOLOGICAL INFECTION / Headaches / Herpes Simplex Virus / Hospital-acquired bacterial pneumonia / Hypercholesterolaemia / Hyperlipidemias / Hypertensive / Infantile Hemangiomas / Infection NOS / Inflammatory Conditions / Inflammatory Reaction / Influenza Treatment or Prophylaxis / Inhalational Anthrax (Post-Exposure) / Intra-Abdominal Infections / Life-threatening Fungal Infections / Lower Respiratory Tract Infection (LRTI) / Meningitis, Bacterial / Migraines / Muscle Spasms / Nausea / Opioid Addiction / Pain / Plague / Pneumonia / Prophylaxis / Psittacosis / Q Fever / Reflux / Relapsing Fever / Rocky Mountain Spotted Fever / Schizophrenic Disorders / Sedation therapy / Seizures / Sepsis / Skeletal Muscle Spasms / Skin and Subcutaneous Tissue Bacterial Infections / Skin Structures and Soft Tissue Infections / Stable Angina (SA) / Thromboprophylaxis / Thrombosis / Trachoma / Treatment-resistant Schizophrenia / Tularemia / Typhus Fever / Uncomplicated Skin and Skin Structure Infections / Uncomplicated Urinary Tract Infections / Urinary Tract Infections (UTIs) / Vomiting / Withdrawal1
Not AvailableRecruitingPreventionContraception1

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
GelRectal2.5 mg/.5mL
GelRectal5 mg
EmulsionIntramuscular; Intravenous5 mg
GelRectal10 mg/2mL
GelRectal20 mg/4mL
InjectionIntramuscular5 mg/mL
Injection, solutionIntramuscular; Intravenous10 mg/2mL
Injection, solutionIntramuscular; Intravenous5 mg/mL
SolutionOral5 mg/5mL
TabletOral10 mg/1
TabletOral2 mg/1
TabletOral5 mg/1
TabletOral10 mg
TabletOral5 mg
LiquidIntramuscular10 mg
SolutionIntramuscular; Intravenous10 mg
SolutionIntramuscular; Intravenous5 mg
Solution, concentrateOral5 mg/mL
Kit
SolutionOral1 mg
CreamTopical
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)
US5462740No1993-09-172013-09-17Us
CA2171627No2006-01-312014-09-12Canada

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)125-126Chase, 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 RuleNoChemAxon
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)

Spectra

Mass Spec (NIST)
Download (10.4 KB)
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
GC-MS Spectrum - CI-BGC-MSsplash10-000i-0090000000-413ec5151b3a9fd41c47
GC-MS Spectrum - EI-BGC-MSsplash10-0a4i-3690000000-3c601fed832ff090653a
GC-MS Spectrum - EI-BGC-MSsplash10-0a59-1290000000-da27f63bddb3263e0063
Mass Spectrum (Electron Ionization)MSsplash10-0a59-2490000000-41352db33c43d0b96876
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-000i-0090000000-bece36773a183e23bfff
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-000i-0490000000-fbdfb84836374f27ffc7
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-0006-0950000000-75d9ab376c968b83f255
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-0006-0940000000-c585bcb21e1b3008adc1
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0a4i-0590000000-2c33d4fd40c36c20a4a6
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-000i-0090000000-695f91d3d5f2e1902be3
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-000i-0090000000-15d8ced2d42d3e292bb1
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-000i-0290000000-dfdaecb8b27bc1ad2c9e
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0fdx-0890000000-b77eb07ad61e288eeb19
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0006-0940000000-fb79dac6c46f730fb465
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0006-1930000000-a6412a87698303834034
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-000i-0090000000-31830c983339c0e0d918
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-000i-0090000000-1028986b8e3b82b4bf96
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-000i-0290000000-0c2338f41998da54e8c5
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0fdx-0890000000-48e88a1c67f0fc25384f
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0f6x-0940000000-ce56b132903858bd3b6b
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0006-1930000000-b61e92cac5094920cf32
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0a4i-0590000000-e26e1398541d17b6632e
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0f7c-0590000000-541488ae806b0dbd97cb
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0006-0940000000-4d1f9651cdfcc7b3eda7
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-052r-0290000000-d6f262c29a34d822e0bb
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0a4i-0590000000-2b62dea3c793e2686145
MS/MS Spectrum - , positiveLC-MS/MSsplash10-000i-0290000000-a55f8538b17bcc2d6bc7
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-000i-0290000000-b867d84dd13d808b9cc2

Taxonomy

Description
This 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.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Benzodiazepines
Sub Class
1,4-benzodiazepines
Direct Parent
1,4-benzodiazepines
Alternative Parents
Alpha amino acids and derivatives / Benzene and substituted derivatives / Aryl chlorides / Tertiary carboxylic acid amides / Lactams / Ketimines / Propargyl-type 1,3-dipolar organic compounds / Azacyclic compounds / Organopnictogen compounds / Organochlorides
show 3 more
Substituents
1,4-benzodiazepine / Alpha-amino acid or derivatives / Aryl chloride / Aryl halide / Monocyclic benzene moiety / Benzenoid / Tertiary carboxylic acid amide / Carboxamide group / Ketimine / Lactam
show 16 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
organochlorine compound, 1,4-benzodiazepinone (CHEBI:49575)

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Potentiator
General Function
Inhibitory extracellular ligand-gated ion channel activity
Specific Function
Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine...
Gene Name
GABRA1
Uniprot ID
P14867
Uniprot Name
Gamma-aminobutyric acid receptor subunit alpha-1
Molecular Weight
51801.395 Da
References
  1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090]
  2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [PubMed:18384456]
  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
Uniprot Name
Gamma-aminobutyric acid receptor subunit alpha-2
Molecular Weight
51325.85 Da
References
  1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090]
  2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [PubMed:18384456]
  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
Uniprot Name
Gamma-aminobutyric acid receptor subunit alpha-3
Molecular Weight
55164.055 Da
References
  1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090]
  2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [PubMed:18384456]
  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
Uniprot Name
Gamma-aminobutyric acid receptor subunit alpha-5
Molecular Weight
52145.645 Da
References
  1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090]
  2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [PubMed:18384456]
  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...
Gene Name
GABRB1
Uniprot ID
P18505
Uniprot Name
Gamma-aminobutyric acid receptor subunit beta-1
Molecular Weight
54234.085 Da
References
  1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090]
  2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [PubMed:18384456]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Potentiator
General Function
Inhibitory extracellular ligand-gated ion channel activity
Specific Function
Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine...
Gene Name
GABRB2
Uniprot ID
P47870
Uniprot Name
Gamma-aminobutyric acid receptor subunit beta-2
Molecular Weight
59149.895 Da
References
  1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090]
  2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [PubMed:18384456]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Potentiator
General Function
Gaba-gated chloride ion channel activity
Specific Function
Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine...
Gene Name
GABRB3
Uniprot ID
P28472
Uniprot Name
Gamma-aminobutyric acid receptor subunit beta-3
Molecular Weight
54115.04 Da
References
  1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090]
  2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [PubMed:18384456]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Potentiator
General Function
Inhibitory extracellular ligand-gated ion channel activity
Specific Function
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
Gene Name
GABRG1
Uniprot ID
Q8N1C3
Uniprot Name
Gamma-aminobutyric acid receptor subunit gamma-1
Molecular Weight
53594.49 Da
References
  1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090]
  2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [PubMed:18384456]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Potentiator
General Function
Inhibitory extracellular ligand-gated ion channel activity
Specific Function
Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine...
Gene Name
GABRG2
Uniprot ID
P18507
Uniprot Name
Gamma-aminobutyric acid receptor subunit gamma-2
Molecular Weight
54161.78 Da
References
  1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090]
  2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [PubMed:18384456]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Potentiator
General Function
Inhibitory extracellular ligand-gated ion channel activity
Specific Function
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
Gene Name
GABRG3
Uniprot ID
Q99928
Uniprot Name
Gamma-aminobutyric acid receptor subunit gamma-3
Molecular Weight
54288.16 Da
References
  1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090]
  2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [PubMed:18384456]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Potentiator
General Function
Gaba-a receptor activity
Specific Function
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
Gene Name
GABRD
Uniprot ID
O14764
Uniprot Name
Gamma-aminobutyric acid receptor subunit delta
Molecular Weight
50707.835 Da
References
  1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090]
  2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [PubMed:18384456]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Potentiator
General Function
Inhibitory extracellular ligand-gated ion channel activity
Specific Function
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
Gene Name
GABRE
Uniprot ID
P78334
Uniprot Name
Gamma-aminobutyric acid receptor subunit epsilon
Molecular Weight
57971.175 Da
References
  1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090]
  2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [PubMed:18384456]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Potentiator
General Function
Gaba-a receptor activity
Specific Function
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel. In the ute...
Gene Name
GABRP
Uniprot ID
O00591
Uniprot Name
Gamma-aminobutyric acid receptor subunit pi
Molecular Weight
50639.735 Da
References
  1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090]
  2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [PubMed:18384456]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Potentiator
General Function
Gaba-a receptor activity
Specific Function
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel. Rho-1 GABA...
Gene Name
GABRR1
Uniprot ID
P24046
Uniprot Name
Gamma-aminobutyric acid receptor subunit rho-1
Molecular Weight
55882.91 Da
References
  1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090]
  2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [PubMed:18384456]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Potentiator
General Function
Gaba-a receptor activity
Specific Function
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel. Rho-2 GABA...
Gene Name
GABRR2
Uniprot ID
P28476
Uniprot Name
Gamma-aminobutyric acid receptor subunit rho-2
Molecular Weight
54150.41 Da
References
  1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090]
  2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [PubMed:18384456]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Potentiator
General Function
Gaba-a receptor activity
Specific Function
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
Gene Name
GABRR3
Uniprot ID
A8MPY1
Uniprot Name
Gamma-aminobutyric acid receptor subunit rho-3
Molecular Weight
54271.1 Da
References
  1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090]
  2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [PubMed:18384456]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Potentiator
General Function
Transmembrane signaling receptor activity
Specific Function
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
Gene Name
GABRQ
Uniprot ID
Q9UN88
Uniprot Name
Gamma-aminobutyric acid receptor subunit theta
Molecular Weight
72020.875 Da
References
  1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090]
  2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [PubMed:18384456]
Details
18. Translocator protein
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 l...
Gene Name
TSPO
Uniprot ID
P30536
Uniprot Name
Translocator protein
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]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. 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 un...
Gene Name
CYP3A5
Uniprot ID
P20815
Uniprot Name
Cytochrome P450 3A5
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 un...
Gene Name
CYP3A7
Uniprot ID
P24462
Uniprot Name
Cytochrome P450 3A7
Molecular Weight
57525.03 Da
References
  1. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
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 im...
Gene Name
CYP2C19
Uniprot ID
P33261
Uniprot Name
Cytochrome P450 2C19
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
Substrate
Inhibitor
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2C9
Uniprot ID
P11712
Uniprot Name
Cytochrome P450 2C9
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 un...
Gene Name
CYP2B6
Uniprot ID
P20813
Uniprot Name
Cytochrome P450 2B6
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
Substrate
Inhibitor
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 un...
Gene Name
CYP1A2
Uniprot ID
P05177
Uniprot Name
Cytochrome P450 1A2
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 un...
Gene Name
CYP2C18
Uniprot ID
P33260
Uniprot Name
Cytochrome P450 2C18
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 un...
Gene Name
CYP2C8
Uniprot ID
P10632
Uniprot Name
Cytochrome P450 2C8
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 gas...
Gene Name
PTGS1
Uniprot ID
P23219
Uniprot Name
Prostaglandin G/H synthase 1
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 ...
Gene Name
CYP2E1
Uniprot ID
P05181
Uniprot Name
Cytochrome P450 2E1
Molecular Weight
56848.42 Da
References
  1. Tassaneeyakul W, Birkett DJ, Miners JO: Inhibition of human hepatic cytochrome P4502E1 by azole antifungals, CNS-active drugs and non-steroidal anti-inflammatory agents. Xenobiotica. 1998 Mar;28(3):293-301. [PubMed:9574817]

Carriers

Details
1. Serum albumin
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 colloid...
Gene Name
ALB
Uniprot ID
P02768
Uniprot Name
Serum albumin
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
Uniprot Name
Multidrug resistance protein 1
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]

Drug created on June 13, 2005 07:24 / Updated on November 19, 2017 20:34