Identification

Name
Nitrazepam
Accession Number
DB01595
Type
Small Molecule
Groups
Approved
Description

A benzodiazepine derivative used as an anticonvulsant and hypnotic.

Structure
Thumb
Synonyms
  • 1,3-dihydro-7-Nitro-5-phenyl-2H-1,4-benzodiazepin-2-one
  • 2,3-dihydro-7-Nitro-5-phenyl-1H-1,4-benzodiazepin-2-one
  • 7-Nitro-1,3-dihydro-5-phenyl-2H-1,4-benzodiazepin-2-one
  • 7-Nitro-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one
  • Apodorm
  • Atempol
  • Benzalin
  • Calsmin
  • Eatan
  • Eunoctin
  • Gerson
  • Hipnax
  • Hipsal
  • Ibrovek
  • Imeson
  • Imesont
  • N-Desmethylnimetazepam
  • Nelbon
  • Nelmat
  • Neozepam
  • Neuchlonic
  • Nitrazepamum
  • Paxisyn
  • Pelson
  • Persopit
  • Radedorm
  • Relact
  • Somitran
  • Sonebon
  • Sonnolin
  • Trazenin
External IDs
N05CD02 / NSC-58775 / RO 4-5360 / RO 5-3059
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
MogadonTablet10 mgOralAa Pharma Inc1980-12-31Not applicableCanada
MogadonTablet5 mgOralAa Pharma Inc1980-12-31Not applicableCanada
NitrazadonTablet5 mgOralAa Pharma Inc1996-11-082014-06-25Canada
NitrazadonTablet10 mgOralAa Pharma Inc1996-11-082014-06-25Canada
Nitrazepam-10Tablet10 mgOralPro Doc Limitee2004-07-292010-07-13Canada
Nitrazepam-5Tablet5 mgOralPro Doc Limitee2004-07-292010-07-13Canada
Sandoz NitrazepamTablet10 mgOralSandoz Canada Incorporated1997-12-02Not applicableCanada
Sandoz NitrazepamTablet5 mgOralSandoz Canada Incorporated1997-12-02Not applicableCanada
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-nitrazepam Tablets BPTablet5 mgOralApotex Corporation2002-09-17Not applicableCanada
Apo-nitrazepam Tablets BPTablet10 mgOralApotex Corporation2002-09-17Not applicableCanada
International/Other Brands
Alodorm / Arem / Benzalin / Insoma / Mogadon / Nitrados / Nitrosun / Ormodon / Pacisyn / Paxadorm / Remnos / Somnite / Surem / Unisomnia
Categories
UNII
9CLV70W7HS
CAS number
146-22-5
Weight
Average: 281.2661
Monoisotopic: 281.080041233
Chemical Formula
C15H11N3O3
InChI Key
KJONHKAYOJNZEC-UHFFFAOYSA-N
InChI
InChI=1S/C15H11N3O3/c19-14-9-16-15(10-4-2-1-3-5-10)12-8-11(18(20)21)6-7-13(12)17-14/h1-8H,9H2,(H,17,19)
IUPAC Name
7-nitro-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one
SMILES
[O-][N+](=O)C1=CC2=C(NC(=O)CN=C2C2=CC=CC=C2)C=C1

Pharmacology

Indication

Used to treat short-term sleeping problems (insomnia), such as difficulty falling asleep, frequent awakenings during the night, and early-morning awakening.

Structured Indications
Pharmacodynamics

Nitrazepam is a type of benzodiazepine drug. It is a powerful hypnotic drug which possesses strong sedative, anxiolytic, amnestic, anticonvulsant, and skeletal muscle relaxant properties. Nitrazepam shortens the time required to fall asleep and lengthens the duration of sleep. It is also useful for the management of myoclonic seizures.

Mechanism of action

Nitrazepam belongs to a group of medicines called benzodiazepines. It acts on benzodiazepine receptors in the brain which are associated with the GABA receptors causing an enhanced binding of GABA (gamma amino butyric acid) to GABAA receptors. GABA is a major inhibitory neurotransmitter in the brain, involved in inducing sleepiness, muscular relaxation and control of anxiety and fits, and slows down the central nervous system. The anticonvulsant properties of nitrazepam and other benzodiazepines may be in part or entirely due to binding to voltage-dependent sodium channels rather than benzodiazepine receptors. Sustained repetitive firing seems to be limited by benzodiazepines effect of slowing recovery of sodium channels from inactivation.

TargetActionsOrganism
AGamma-aminobutyric acid receptor subunit alpha-1
potentiator
Human
AGamma-aminobutyric acid receptor subunit alpha-2
potentiator
Human
AGamma-aminobutyric acid receptor subunit alpha-3
potentiator
Human
AGamma-aminobutyric acid receptor subunit alpha-4
potentiator
Human
AGamma-aminobutyric acid receptor subunit alpha-5
potentiator
Human
AGamma-aminobutyric acid receptor subunit alpha-6
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
USodium channel protein type 1 subunit alpha
other/unknown
Human
Absorption

Bioavailability is 53-94% following oral administration.

Volume of distribution
Not Available
Protein binding
Not Available
Metabolism
Not Available
Route of elimination
Not Available
Half life

15-38 hours (mean elimination half life 26 hours).

Clearance
Not Available
Toxicity

Nitrazepam is a drug which is very frequently involved in drug intoxication, including overdose. Nitrazepam overdose may result in stereotypical symptoms of benzodiazepine overdose including intoxication, impaired balance, slurred speech. In cases of severe overdose this may progress to a comatose state with the possibility of death.

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

Interactions

Drug Interactions
DrugInteractionDrug group
7-NitroindazoleThe risk or severity of adverse effects can be increased when Nitrazepam is combined with 7-Nitroindazole.Experimental
AcepromazineThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Acepromazine.Approved, Vet Approved
AceprometazineThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Aceprometazine.Approved
AdipiplonThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Adipiplon.Investigational
AfatinibThe serum concentration of Afatinib can be increased when it is combined with Nitrazepam.Approved
AgomelatineThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Agomelatine.Approved, Investigational
AlaproclateThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Alaproclate.Experimental
AlfaxaloneThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Alfaxalone.Vet Approved
AlfentanilThe risk or severity of adverse effects can be increased when Alfentanil is combined with Nitrazepam.Approved, Illicit
AllopregnanoloneThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Allopregnanolone.Investigational
AlphacetylmethadolThe risk or severity of adverse effects can be increased when Alphacetylmethadol is combined with Nitrazepam.Experimental, Illicit
AlphaprodineThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Alphaprodine.Illicit
AlprazolamThe risk or severity of adverse effects can be increased when Alprazolam is combined with Nitrazepam.Approved, Illicit, Investigational
Ambroxol acefyllinateThe therapeutic efficacy of Nitrazepam can be decreased when used in combination with Ambroxol acefyllinate.Experimental, Investigational
AmiodaroneThe metabolism of Nitrazepam can be decreased when combined with Amiodarone.Approved, Investigational
AmisulprideThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Amisulpride.Approved, Investigational
AmobarbitalThe risk or severity of adverse effects can be increased when Amobarbital is combined with Nitrazepam.Approved, Illicit
AmperozideThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Amperozide.Experimental
AprepitantThe serum concentration of Nitrazepam can be increased when it is combined with Aprepitant.Approved, Investigational
AripiprazoleThe risk or severity of adverse effects can be increased when Aripiprazole is combined with Nitrazepam.Approved, Investigational
ArticaineThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Articaine.Approved
AsenapineThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Asenapine.Approved
AtazanavirThe metabolism of Nitrazepam can be decreased when combined with Atazanavir.Approved, Investigational
AtomoxetineThe metabolism of Nitrazepam can be decreased when combined with Atomoxetine.Approved
AzaperoneThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Azaperone.Investigational, Vet Approved
AzelastineNitrazepam may increase the central nervous system depressant (CNS depressant) activities of Azelastine.Approved
BarbitalThe risk or severity of adverse effects can be increased when Barbital is combined with Nitrazepam.Illicit
BenperidolThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Benperidol.Investigational
BenzocaineThe risk or severity of adverse effects can be increased when Benzocaine is combined with Nitrazepam.Approved
Benzyl alcoholThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Benzyl alcohol.Approved
BoceprevirThe metabolism of Nitrazepam can be decreased when combined with Boceprevir.Approved, Withdrawn
BortezomibThe metabolism of Nitrazepam can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Nitrazepam can be decreased when it is combined with Bosentan.Approved, Investigational
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Nitrazepam.Approved
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Nitrazepam.Approved
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Nitrazepam.Approved
BromazepamThe risk or severity of adverse effects can be increased when Bromazepam is combined with Nitrazepam.Approved, Illicit
BromisovalThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Bromisoval.Experimental
BromperidolThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Bromperidol.Investigational
BrotizolamThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Brotizolam.Approved, Investigational, Withdrawn
BupivacaineThe risk or severity of adverse effects can be increased when Bupivacaine is combined with Nitrazepam.Approved, Investigational
BuprenorphineNitrazepam 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 Nitrazepam.Approved, Investigational
ButabarbitalThe risk or severity of adverse effects can be increased when Butabarbital is combined with Nitrazepam.Approved, Illicit
ButacaineThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Butacaine.Vet Approved
ButambenThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Butamben.Approved
ButethalThe risk or severity of adverse effects can be increased when Butethal is combined with Nitrazepam.Approved, Illicit
ButorphanolThe risk or severity of adverse effects can be increased when Butorphanol is combined with Nitrazepam.Approved, Illicit, Vet Approved
CanertinibThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Canertinib.Investigational
CarbamazepineThe metabolism of Nitrazepam can be increased when combined with Carbamazepine.Approved, Investigational
CarfentanilThe risk or severity of adverse effects can be increased when Carfentanil is combined with Nitrazepam.Illicit, Investigational, Vet Approved
CeritinibThe serum concentration of Nitrazepam can be increased when it is combined with Ceritinib.Approved
Chloral hydrateThe risk or severity of adverse effects can be increased when Chloral hydrate is combined with Nitrazepam.Approved, Illicit, Vet Approved
ChlordiazepoxideThe risk or severity of adverse effects can be increased when Chlordiazepoxide is combined with Nitrazepam.Approved, Illicit
ChlormezanoneThe risk or severity of adverse effects can be increased when Chlormezanone is combined with Nitrazepam.Approved, Investigational, Withdrawn
ChloroprocaineThe risk or severity of adverse effects can be increased when Chloroprocaine is combined with Nitrazepam.Approved
ChlorpromazineThe risk or severity of adverse effects can be increased when Chlorpromazine is combined with Nitrazepam.Approved, Vet Approved
ChlorprothixeneThe risk or severity of adverse effects can be increased when Chlorprothixene is combined with Nitrazepam.Approved, Investigational, Withdrawn
CinchocaineThe risk or severity of adverse effects can be increased when Cinchocaine is combined with Nitrazepam.Approved, Vet Approved
CitalopramThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Citalopram.Approved
ClarithromycinThe metabolism of Nitrazepam can be decreased when combined with Clarithromycin.Approved
ClemastineThe metabolism of Nitrazepam can be decreased when combined with Clemastine.Approved
clomethiazoleThe risk or severity of adverse effects can be increased when Nitrazepam is combined with clomethiazole.Investigational
ClopenthixolThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Clopenthixol.Experimental
ClorazepateThe risk or severity of adverse effects can be increased when Clorazepate is combined with Nitrazepam.Approved, Illicit
ClothiapineThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Clothiapine.Experimental
ClotrimazoleThe metabolism of Nitrazepam can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Clozapine.Approved
CobicistatThe metabolism of Nitrazepam can be decreased when combined with Cobicistat.Approved
CocaineThe risk or severity of adverse effects can be increased when Cocaine is combined with Nitrazepam.Approved, Illicit
CodeineThe risk or severity of adverse effects can be increased when Codeine is combined with Nitrazepam.Approved, Illicit
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Nitrazepam.Approved
ConivaptanThe serum concentration of Conivaptan can be increased when it is combined with Nitrazepam.Approved, Investigational
CrizotinibThe metabolism of Nitrazepam can be decreased when combined with Crizotinib.Approved
CyclobenzaprineThe risk or severity of adverse effects can be increased when Cyclobenzaprine is combined with Nitrazepam.Approved
CyclosporineThe metabolism of Nitrazepam can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
Dabigatran etexilateThe serum concentration of the active metabolites of Dabigatran etexilate can be increased when Dabigatran etexilate is used in combination with Nitrazepam.Approved
DabrafenibThe serum concentration of Nitrazepam can be decreased when it is combined with Dabrafenib.Approved
DapiprazoleThe risk or severity of adverse effects can be increased when Dapiprazole is combined with Nitrazepam.Approved
DapoxetineThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Dapoxetine.Investigational
DarunavirThe metabolism of Nitrazepam can be decreased when combined with Darunavir.Approved
DasatinibThe serum concentration of Nitrazepam can be increased when it is combined with Dasatinib.Approved, Investigational
DeferasiroxThe serum concentration of Nitrazepam can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe metabolism of Nitrazepam can be decreased when combined with Delavirdine.Approved
DeramciclaneThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Deramciclane.Investigational
DesfluraneThe risk or severity of adverse effects can be increased when Desflurane is combined with Nitrazepam.Approved
DesvenlafaxineThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Desvenlafaxine.Approved
DetomidineThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Detomidine.Vet Approved
DexmedetomidineThe risk or severity of adverse effects can be increased when Dexmedetomidine is combined with Nitrazepam.Approved, Vet Approved
DextromoramideThe risk or severity of adverse effects can be increased when Dextromoramide is combined with Nitrazepam.Experimental, Illicit
DextropropoxypheneThe risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Nitrazepam.Approved, Illicit, Investigational, Withdrawn
DezocineThe risk or severity of adverse effects can be increased when Dezocine is combined with Nitrazepam.Approved, Investigational
DiazepamThe risk or severity of adverse effects can be increased when Diazepam is combined with Nitrazepam.Approved, Illicit, Vet Approved
Diethyl etherThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Diethyl ether.Experimental
DihydrocodeineThe risk or severity of adverse effects can be increased when Dihydrocodeine is combined with Nitrazepam.Approved, Illicit
DihydroergotamineThe metabolism of Nitrazepam can be decreased when combined with Dihydroergotamine.Approved
DihydroetorphineThe risk or severity of adverse effects can be increased when Dihydroetorphine is combined with Nitrazepam.Experimental, Illicit
DihydromorphineThe risk or severity of adverse effects can be increased when Dihydromorphine is combined with Nitrazepam.Experimental, Illicit
DiltiazemThe metabolism of Nitrazepam can be decreased when combined with Diltiazem.Approved
DiphenhydramineThe risk or severity of adverse effects can be increased when Diphenhydramine is combined with Nitrazepam.Approved
DiphenoxylateThe risk or severity of adverse effects can be increased when Diphenoxylate is combined with Nitrazepam.Approved, Illicit
DixyrazineThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Dixyrazine.Experimental
DoramectinThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Doramectin.Vet Approved
DoxofyllineThe serum concentration of Doxofylline can be decreased when it is combined with Nitrazepam.Approved, Investigational
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Nitrazepam.Approved, Investigational
DoxycyclineThe metabolism of Nitrazepam can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Nitrazepam.Approved, Vet Approved
DPDPEThe risk or severity of adverse effects can be increased when Nitrazepam is combined with DPDPE.Experimental
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Nitrazepam.Approved, Illicit
DronedaroneThe metabolism of Nitrazepam can be decreased when combined with Dronedarone.Approved
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Nitrazepam.Approved, Vet Approved
DrotebanolThe risk or severity of adverse effects can be increased when Drotebanol is combined with Nitrazepam.Experimental, Illicit
DuloxetineThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Duloxetine.Approved
DyclonineThe risk or severity of adverse effects can be increased when Dyclonine is combined with Nitrazepam.Approved
EcgonineThe risk or severity of adverse effects can be increased when Ecgonine is combined with Nitrazepam.Experimental, Illicit
EcopipamThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Ecopipam.Investigational
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Nitrazepam.Approved
EltanoloneThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Eltanolone.Investigational
EnfluraneThe risk or severity of adverse effects can be increased when Enflurane is combined with Nitrazepam.Approved, Investigational, Vet Approved
EnzalutamideThe serum concentration of Nitrazepam can be decreased when it is combined with Enzalutamide.Approved
ErythromycinThe metabolism of Nitrazepam can be decreased when combined with Erythromycin.Approved, Vet Approved
EscitalopramThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Escitalopram.Approved, Investigational
EstazolamThe risk or severity of adverse effects can be increased when Estazolam is combined with Nitrazepam.Approved, Illicit
EszopicloneThe risk or severity of adverse effects can be increased when Eszopiclone is combined with Nitrazepam.Approved
EthanolNitrazepam may increase the central nervous system depressant (CNS depressant) activities of Ethanol.Approved
EthchlorvynolThe risk or severity of adverse effects can be increased when Ethchlorvynol is combined with Nitrazepam.Approved, Illicit, Withdrawn
Ethyl carbamateThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Ethyl carbamate.Withdrawn
Ethyl chlorideThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Ethyl chloride.Experimental, Investigational
Ethyl loflazepateThe risk or severity of adverse effects can be increased when Ethyl loflazepate is combined with Nitrazepam.Approved, Illicit
EthylmorphineThe risk or severity of adverse effects can be increased when Ethylmorphine is combined with Nitrazepam.Approved, Illicit
EtidocaineThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Etidocaine.Approved
EtifoxineThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Etifoxine.Investigational, Withdrawn
EtizolamThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Etizolam.Approved
EtomidateThe risk or severity of adverse effects can be increased when Etomidate is combined with Nitrazepam.Approved
EtoperidoneThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Etoperidone.Withdrawn
EtorphineThe risk or severity of adverse effects can be increased when Etorphine is combined with Nitrazepam.Illicit, Vet Approved
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Nitrazepam.Approved
FencamfamineThe risk or severity of adverse effects can be increased when Fencamfamine is combined with Nitrazepam.Approved, Illicit, Withdrawn
FentanylThe risk or severity of adverse effects can be increased when Fentanyl is combined with Nitrazepam.Approved, Illicit, Investigational, Vet Approved
FluanisoneThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Fluanisone.Experimental
FluconazoleThe metabolism of Nitrazepam can be decreased when combined with Fluconazole.Approved
FludiazepamThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Nitrazepam.Approved, Illicit
FlunitrazepamThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Nitrazepam.Approved, Illicit
FluoxetineThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Fluoxetine.Approved, Vet Approved
FlupentixolThe risk or severity of adverse effects can be increased when Flupentixol is combined with Nitrazepam.Approved, Withdrawn
FluphenazineThe risk or severity of adverse effects can be increased when Fluphenazine is combined with Nitrazepam.Approved
FlurazepamThe risk or severity of adverse effects can be increased when Flurazepam is combined with Nitrazepam.Approved, Illicit
FluspirileneThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Fluspirilene.Approved, Investigational
FluvoxamineThe metabolism of Nitrazepam can be decreased when combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe metabolism of Nitrazepam can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Nitrazepam can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe serum concentration of Fosphenytoin can be increased when it is combined with Nitrazepam.Approved
FospropofolThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Fospropofol.Approved, Illicit, Investigational
Fusidic AcidThe serum concentration of Nitrazepam can be increased when it is combined with Fusidic Acid.Approved
GabapentinThe risk or severity of adverse effects can be increased when Gabapentin is combined with Nitrazepam.Approved, Investigational
Gamma Hydroxybutyric AcidThe risk or severity of adverse effects can be increased when Gamma Hydroxybutyric Acid is combined with Nitrazepam.Approved, Illicit, Investigational
GepironeThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Gepirone.Investigational
GlutethimideThe risk or severity of adverse effects can be increased when Glutethimide is combined with Nitrazepam.Approved, Illicit
HalazepamThe risk or severity of adverse effects can be increased when Halazepam is combined with Nitrazepam.Approved, Illicit, Withdrawn
HaloperidolThe risk or severity of adverse effects can be increased when Haloperidol is combined with Nitrazepam.Approved
HalothaneThe risk or severity of adverse effects can be increased when Halothane is combined with Nitrazepam.Approved, Vet Approved
HeroinThe risk or severity of adverse effects can be increased when Heroin is combined with Nitrazepam.Approved, Illicit, Investigational
HexobarbitalThe risk or severity of adverse effects can be increased when Hexobarbital is combined with Nitrazepam.Approved
HyaluronidaseThe therapeutic efficacy of Nitrazepam can be decreased when used in combination with Hyaluronidase.Approved, Investigational
HydrocodoneNitrazepam 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 Nitrazepam.Approved, Illicit
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Nitrazepam.Approved
IdelalisibThe metabolism of Nitrazepam can be decreased when combined with Idelalisib.Approved
ImatinibThe metabolism of Nitrazepam can be decreased when combined with Imatinib.Approved
IndalpineThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Indalpine.Investigational, Withdrawn
IndinavirThe metabolism of Nitrazepam can be decreased when combined with Indinavir.Approved
IndiplonThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Indiplon.Investigational
IsavuconazoniumThe metabolism of Nitrazepam can be decreased when combined with Isavuconazonium.Approved, Investigational
IsofluraneThe risk or severity of adverse effects can be increased when Isoflurane is combined with Nitrazepam.Approved, Vet Approved
IsradipineThe metabolism of Nitrazepam can be decreased when combined with Isradipine.Approved
ItraconazoleThe metabolism of Nitrazepam can be decreased when combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Nitrazepam can be increased when it is combined with Ivacaftor.Approved
KetamineThe risk or severity of adverse effects can be increased when Ketamine is combined with Nitrazepam.Approved, Vet Approved
KetazolamThe risk or severity of adverse effects can be increased when Ketazolam is combined with Nitrazepam.Approved
KetobemidoneThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Ketobemidone.Approved, Investigational
KetoconazoleThe metabolism of Nitrazepam can be decreased when combined with Ketoconazole.Approved, Investigational
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Nitrazepam.Approved
LevobupivacaineThe risk or severity of adverse effects can be increased when Levobupivacaine is combined with Nitrazepam.Approved, Investigational
Levomethadyl AcetateThe risk or severity of adverse effects can be increased when Levomethadyl Acetate is combined with Nitrazepam.Approved, Investigational
LevomilnacipranThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Levomilnacipran.Approved
LevorphanolThe risk or severity of adverse effects can be increased when Levorphanol is combined with Nitrazepam.Approved
LidocaineThe risk or severity of adverse effects can be increased when Lidocaine is combined with Nitrazepam.Approved, Vet Approved
LithiumThe risk or severity of adverse effects can be increased when Lithium is combined with Nitrazepam.Approved
LofentanilThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Lofentanil.Illicit
LopinavirThe metabolism of Nitrazepam can be decreased when combined with Lopinavir.Approved
LoprazolamThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Loprazolam.Experimental
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Nitrazepam.Approved
LormetazepamThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Lormetazepam.Approved
LovastatinThe metabolism of Nitrazepam can be decreased when combined with Lovastatin.Approved, Investigational
LoxapineThe risk or severity of adverse effects can be increased when Loxapine is combined with Nitrazepam.Approved
LuliconazoleThe serum concentration of Nitrazepam can be increased when it is combined with Luliconazole.Approved
LumacaftorThe metabolism of Nitrazepam can be increased when combined with Lumacaftor.Approved
LurasidoneThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Lurasidone.Approved
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Nitrazepam.Approved, Vet Approved
MebicarThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Mebicar.Experimental
MedazepamThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Medazepam.Experimental
MedetomidineThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Medetomidine.Vet Approved
MefloquineThe therapeutic efficacy of Nitrazepam can be decreased when used in combination with Mefloquine.Approved
MelatoninThe risk or severity of adverse effects can be increased when Melatonin is combined with Nitrazepam.Approved, Nutraceutical, Vet Approved
MelperoneThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Melperone.Approved, Investigational
MepivacaineThe risk or severity of adverse effects can be increased when Mepivacaine is combined with Nitrazepam.Approved, Vet Approved
MeprobamateThe risk or severity of adverse effects can be increased when Meprobamate is combined with Nitrazepam.Approved, Illicit
MeptazinolThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Meptazinol.Experimental
MesoridazineThe risk or severity of adverse effects can be increased when Mesoridazine is combined with Nitrazepam.Approved, Investigational
MethadoneNitrazepam 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 Methadyl Acetate is combined with Nitrazepam.Approved, Illicit
MethapyrileneThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Methapyrilene.Withdrawn
MethaqualoneThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Methaqualone.Illicit, Withdrawn
MethohexitalThe risk or severity of adverse effects can be increased when Methohexital is combined with Nitrazepam.Approved
MethotrimeprazineNitrazepam may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.Approved
MethoxyfluraneThe risk or severity of adverse effects can be increased when Methoxyflurane is combined with Nitrazepam.Approved, Investigational, Vet Approved
MethylecgonineThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Methylecgonine.Experimental
MethylphenobarbitalThe risk or severity of adverse effects can be increased when Methylphenobarbital is combined with Nitrazepam.Approved
MetyrosineNitrazepam may increase the sedative activities of Metyrosine.Approved
MianserinThe therapeutic efficacy of Nitrazepam 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 Nitrazepam.Approved, Illicit
MifepristoneThe serum concentration of Nitrazepam can be increased when it is combined with Mifepristone.Approved, Investigational
MilnacipranThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Milnacipran.Approved
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Nitrazepam.Approved, Investigational
MirtazapineNitrazepam may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.Approved
MitotaneThe serum concentration of Nitrazepam can be decreased when it is combined with Mitotane.Approved
MolindoneThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Molindone.Approved
MorphineThe risk or severity of adverse effects can be increased when Morphine is combined with Nitrazepam.Approved, Investigational
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Nitrazepam.Approved, Investigational
NalbuphineThe risk or severity of adverse effects can be increased when Nalbuphine is combined with Nitrazepam.Approved
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Nitrazepam.Approved
NefazodoneThe metabolism of Nitrazepam can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe metabolism of Nitrazepam can be decreased when combined with Nelfinavir.Approved
NetupitantThe serum concentration of Nitrazepam can be increased when it is combined with Netupitant.Approved
NevirapineThe metabolism of Nitrazepam can be increased when combined with Nevirapine.Approved
NilotinibThe metabolism of Nitrazepam can be decreased when combined with Nilotinib.Approved, Investigational
Nitrous oxideThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Nitrous oxide.Approved, Vet Approved
NorfluraneThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Norflurane.Investigational
NormethadoneThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Normethadone.Approved, Illicit
OlanzapineThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Olanzapine.Approved, Investigational
OlaparibThe metabolism of Nitrazepam can be decreased when combined with Olaparib.Approved
OndansetronThe risk or severity of adverse effects can be increased when Ondansetron is combined with Nitrazepam.Approved
OpiumThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Opium.Approved, Illicit
OrlistatThe serum concentration of Nitrazepam can be decreased when it is combined with Orlistat.Approved, Investigational
OrphenadrineNitrazepam may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
OsanetantThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Osanetant.Investigational
OsimertinibThe serum concentration of Nitrazepam can be increased when it is combined with Osimertinib.Approved
OxazepamThe risk or severity of adverse effects can be increased when Oxazepam is combined with Nitrazepam.Approved
OxethazaineThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Oxethazaine.Approved, Investigational
OxprenololThe risk or severity of adverse effects can be increased when Oxprenolol is combined with Nitrazepam.Approved
OxybuprocaineThe risk or severity of adverse effects can be increased when Oxybuprocaine is combined with Nitrazepam.Approved
OxycodoneThe risk or severity of adverse effects can be increased when Oxycodone is combined with Nitrazepam.Approved, Illicit, Investigational
OxymorphoneThe risk or severity of adverse effects can be increased when Oxymorphone is combined with Nitrazepam.Approved, Investigational, Vet Approved
PalbociclibThe serum concentration of Nitrazepam can be increased when it is combined with Palbociclib.Approved
PaliperidoneThe risk or severity of adverse effects can be increased when Paliperidone is combined with Nitrazepam.Approved
ParaldehydeNitrazepam may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.Approved, Investigational
ParoxetineThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Paroxetine.Approved, Investigational
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Nitrazepam.Approved
PenfluridolThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Penfluridol.Experimental
PentazocineThe risk or severity of adverse effects can be increased when Pentazocine is combined with Nitrazepam.Approved, Vet Approved
PentobarbitalThe metabolism of Nitrazepam can be increased when combined with Pentobarbital.Approved, Vet Approved
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Nitrazepam.Approved
PerazineThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Perazine.Investigational
PerospironeThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Perospirone.Approved
PerphenazineThe risk or severity of adverse effects can be increased when Perphenazine is combined with Nitrazepam.Approved
PethidineThe risk or severity of adverse effects can be increased when Pethidine is combined with Nitrazepam.Approved
PhenazocineThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Phenazocine.Experimental
PhenibutThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Phenibut.Experimental
PhenobarbitalThe metabolism of Nitrazepam can be increased when combined with Phenobarbital.Approved
PhenoperidineThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Phenoperidine.Experimental
PhenoxyethanolThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Phenoxyethanol.Approved
PhenytoinThe serum concentration of Phenytoin can be increased when it is combined with Nitrazepam.Approved, Vet Approved
PimozideThe risk or severity of adverse effects can be increased when Pimozide is combined with Nitrazepam.Approved
PipamperoneThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Pipamperone.Approved, Investigational
PiritramideThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Piritramide.Investigational
PosaconazoleThe metabolism of Nitrazepam can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
PramipexoleNitrazepam may increase the sedative activities of Pramipexole.Approved, Investigational
PramocaineThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Pramocaine.Approved
PrazepamThe risk or severity of adverse effects can be increased when Prazepam is combined with Nitrazepam.Approved, Illicit
PregabalinThe therapeutic efficacy of Nitrazepam can be decreased when used in combination with Pregabalin.Approved, Illicit, Investigational
PrilocaineThe risk or severity of adverse effects can be increased when Prilocaine is combined with Nitrazepam.Approved
PrimidoneThe metabolism of Nitrazepam can be increased when combined with Primidone.Approved, Vet Approved
ProcaineThe risk or severity of adverse effects can be increased when Procaine is combined with Nitrazepam.Approved, Investigational, Vet Approved
ProchlorperazineThe risk or severity of adverse effects can be increased when Prochlorperazine is combined with Nitrazepam.Approved, Vet Approved
PromazineThe risk or severity of adverse effects can be increased when Promazine is combined with Nitrazepam.Approved, Vet Approved
PropanididThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Propanidid.Experimental
ProparacaineThe risk or severity of adverse effects can be increased when Proparacaine is combined with Nitrazepam.Approved, Vet Approved
PropofolThe risk or severity of adverse effects can be increased when Propofol is combined with Nitrazepam.Approved, Investigational, Vet Approved
PropoxycaineThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Propoxycaine.Approved
ProxibarbalThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Proxibarbal.Experimental
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Nitrazepam.Approved
PSD502The risk or severity of adverse effects can be increased when Nitrazepam is combined with PSD502.Investigational
QuazepamThe risk or severity of adverse effects can be increased when Quazepam is combined with Nitrazepam.Approved, Illicit
QuetiapineThe risk or severity of adverse effects can be increased when Quetiapine is combined with Nitrazepam.Approved
QuinisocaineThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Quinisocaine.Experimental
RacloprideThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Raclopride.Investigational
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Nitrazepam.Approved, Investigational
RemifentanilThe risk or severity of adverse effects can be increased when Remifentanil is combined with Nitrazepam.Approved
RemoxiprideThe risk or severity of adverse effects can be increased when Remoxipride is combined with Nitrazepam.Approved, Withdrawn
ReserpineThe risk or severity of adverse effects can be increased when Reserpine is combined with Nitrazepam.Approved, Investigational
RifabutinThe metabolism of Nitrazepam can be increased when combined with Rifabutin.Approved
RifampicinThe serum concentration of Nitrazepam can be decreased when it is combined with Rifampicin.Approved
RifapentineThe metabolism of Nitrazepam can be increased when combined with Rifapentine.Approved
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Nitrazepam.Approved, Investigational
RisperidoneThe risk or severity of adverse effects can be increased when Risperidone is combined with Nitrazepam.Approved, Investigational
RitanserinThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Ritanserin.Investigational
RomifidineThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Romifidine.Vet Approved
RopiniroleNitrazepam may increase the sedative activities of Ropinirole.Approved, Investigational
RopivacaineThe risk or severity of adverse effects can be increased when Ropivacaine is combined with Nitrazepam.Approved
RotigotineNitrazepam may increase the sedative activities of Rotigotine.Approved
RucaparibThe metabolism of Nitrazepam can be decreased when combined with Rucaparib.Approved, Investigational
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Nitrazepam.Approved
SaquinavirThe metabolism of Nitrazepam can be decreased when combined with Saquinavir.Approved, Investigational
SarilumabThe therapeutic efficacy of Nitrazepam can be decreased when used in combination with Sarilumab.Approved
SecobarbitalThe risk or severity of adverse effects can be increased when Secobarbital is combined with Nitrazepam.Approved, Vet Approved
SepranoloneThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Sepranolone.Investigational
SertindoleThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Sertindole.Approved, Investigational, Withdrawn
SertralineThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Sertraline.Approved
SevofluraneThe risk or severity of adverse effects can be increased when Sevoflurane is combined with Nitrazepam.Approved, Vet Approved
SildenafilThe metabolism of Nitrazepam can be decreased when combined with Sildenafil.Approved, Investigational
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Nitrazepam.Approved
SiltuximabThe serum concentration of Nitrazepam can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Nitrazepam can be increased when it is combined with Simeprevir.Approved
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Nitrazepam.Approved
St. John's WortThe serum concentration of Nitrazepam can be decreased when it is combined with St. John's Wort.Investigational, Nutraceutical
StiripentolThe serum concentration of Nitrazepam 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 Nitrazepam.Approved, Investigational
SulfisoxazoleThe metabolism of Nitrazepam can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
SulpirideThe risk or severity of adverse effects can be increased when Sulpiride is combined with Nitrazepam.Approved, Investigational
SultoprideThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Sultopride.Experimental
SuvorexantNitrazepam may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.Approved
TandospironeThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Tandospirone.Investigational
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Nitrazepam.Approved
TeduglutideThe serum concentration of Nitrazepam can be increased when it is combined with Teduglutide.Approved
TelaprevirThe metabolism of Nitrazepam can be decreased when combined with Telaprevir.Approved, Withdrawn
TelithromycinThe metabolism of Nitrazepam can be decreased when combined with Telithromycin.Approved
TemazepamThe risk or severity of adverse effects can be increased when Temazepam is combined with Nitrazepam.Approved
TetracaineThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Tetracaine.Approved, Vet Approved
TetracosactideTetracosactide may increase the hepatotoxic activities of Nitrazepam.Approved
TetrahydropalmatineThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Tetrahydropalmatine.Investigational
TetrodotoxinThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Tetrodotoxin.Investigational
ThalidomideNitrazepam may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.Approved, Investigational, Withdrawn
ThiamylalThe risk or severity of adverse effects can be increased when Thiamylal is combined with Nitrazepam.Approved, Vet Approved
ThiopentalThe risk or severity of adverse effects can be increased when Thiopental is combined with Nitrazepam.Approved, Vet Approved
ThioridazineThe risk or severity of adverse effects can be increased when Thioridazine is combined with Nitrazepam.Approved, Withdrawn
ThiothixeneThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Thiothixene.Approved
TiaprideThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Tiapride.Approved, Investigational
TiclopidineThe metabolism of Nitrazepam can be decreased when combined with Ticlopidine.Approved
TiletamineThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Tiletamine.Vet Approved
TilidineThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Tilidine.Experimental
TocilizumabThe serum concentration of Nitrazepam can be decreased when it is combined with Tocilizumab.Approved
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Nitrazepam.Approved, Investigational
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with Nitrazepam.Approved, Investigational
Trans-2-PhenylcyclopropylamineThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Trans-2-Phenylcyclopropylamine.Experimental
TranylcypromineThe risk or severity of adverse effects can be increased when Tranylcypromine is combined with Nitrazepam.Approved
TrazodoneThe risk or severity of adverse effects can be increased when Trazodone is combined with Nitrazepam.Approved, Investigational
TriazolamThe risk or severity of adverse effects can be increased when Triazolam is combined with Nitrazepam.Approved
Tricaine methanesulfonateThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Tricaine methanesulfonate.Vet Approved
TrichloroethyleneThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Trichloroethylene.Approved
TrifluoperazineThe risk or severity of adverse effects can be increased when Trifluoperazine is combined with Nitrazepam.Approved
TrifluperidolThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Trifluperidol.Experimental
TriflupromazineThe risk or severity of adverse effects can be increased when Triflupromazine is combined with Nitrazepam.Approved, Vet Approved
Valproic AcidThe risk or severity of adverse effects can be increased when Valproic Acid is combined with Nitrazepam.Approved, Investigational
VemurafenibThe serum concentration of Nitrazepam can be decreased when it is combined with Vemurafenib.Approved
VenlafaxineThe metabolism of Nitrazepam can be decreased when combined with Venlafaxine.Approved
VeraliprideThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Veralipride.Experimental
VerapamilThe metabolism of Nitrazepam can be decreased when combined with Verapamil.Approved
VincristineThe excretion of Vincristine can be decreased when combined with Nitrazepam.Approved, Investigational
Vinyl etherThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Vinyl ether.Experimental
VoriconazoleThe metabolism of Nitrazepam can be decreased when combined with Voriconazole.Approved, Investigational
VortioxetineThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Vortioxetine.Approved
XenonThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Xenon.Experimental
XylazineThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Xylazine.Vet Approved
YohimbineThe therapeutic efficacy of Nitrazepam can be decreased when used in combination with Yohimbine.Approved, Vet Approved
ZaleplonThe risk or severity of adverse effects can be increased when Zaleplon is combined with Nitrazepam.Approved, Illicit, Investigational
ZimelidineThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Zimelidine.Withdrawn
ZiprasidoneThe metabolism of Nitrazepam can be decreased when combined with Ziprasidone.Approved
ZolazepamThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Zolazepam.Vet Approved
ZolpidemNitrazepam may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.Approved
ZopicloneThe risk or severity of adverse effects can be increased when Zopiclone is combined with Nitrazepam.Approved
ZotepineThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Zotepine.Approved, Investigational
ZuclopenthixolThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Zuclopenthixol.Approved, Investigational
Food Interactions
  • Avoid alcohol.
  • Avoid excessive quantities of coffee or tea (Caffeine).
  • Take with food.

References

General References
  1. Rickels K: The clinical use of hypnotics: indications for use and the need for a variety of hypnotics. Acta Psychiatr Scand Suppl. 1986;332:132-41. [PubMed:2883820]
  2. Robertson MD, Drummer OH: Postmortem drug metabolism by bacteria. J Forensic Sci. 1995 May;40(3):382-6. [PubMed:7782744]
  3. Oelschlager H: [Chemical and pharmacologic aspects of benzodiazepines]. Schweiz Rundsch Med Prax. 1989 Jul 4;78(27-28):766-72. [PubMed:2570451]
  4. Podhorna J, Krsiak M: Behavioural effects of a benzodiazepine receptor partial agonist, Ro 19-8022, in the social conflict test in mice. Behav Pharmacol. 2000 Apr;11(2):143-51. [PubMed:10877119]
  5. Nowakowska E, Chodera A: Studies on the involvement of opioid mechanism in the locomotor effects of benzodiazepines in rats. Pharmacol Biochem Behav. 1991 Feb;38(2):265-6. [PubMed:1676167]
External Links
Human Metabolome Database
HMDB0015534
KEGG Drug
D00531
KEGG Compound
C07487
PubChem Compound
4506
PubChem Substance
46505806
ChemSpider
4350
BindingDB
50020856
ChEBI
7581
ChEMBL
CHEMBL13209
Therapeutic Targets Database
DAP000691
PharmGKB
PA10242
Wikipedia
Nitrazepam
ATC Codes
N05CD02 — Nitrazepam
AHFS Codes
  • 28:24.08 — Benzodiazepines

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
2CompletedTreatmentEpilepsies / Infantile Spasms (IS)1
3CompletedTreatmentSleep Initiation and Maintenance Disorders1
3TerminatedTreatmentAnxiety Disorders / Dementias / Depression / Psychosomatic Disorders / Schizophrenic Disorders1
4RecruitingTreatmentEpilepsies1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
TabletOral10 mg
TabletOral5 mg
Prices
Unit descriptionCostUnit
Mogadon 10 mg Tablet0.24USD tablet
Mogadon 5 mg Tablet0.16USD tablet
Apo-Nitrazepam 10 mg Tablet0.13USD tablet
Nitrazadon 10 mg Tablet0.11USD tablet
Sandoz Nitrazepam 10 mg Tablet0.11USD tablet
Apo-Nitrazepam 5 mg Tablet0.09USD tablet
Nitrazadon 5 mg Tablet0.08USD tablet
Sandoz Nitrazepam 5 mg Tablet0.08USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)225 °CPhysProp
logP2.25HANSCH,C ET AL. (1995)
logS-3.8ADME Research, USCD
Predicted Properties
PropertyValueSource
Water Solubility0.0299 mg/mLALOGPS
logP1.95ALOGPS
logP2.55ChemAxon
logS-4ALOGPS
pKa (Strongest Acidic)11.9ChemAxon
pKa (Strongest Basic)2.61ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area87.28 Å2ChemAxon
Rotatable Bond Count2ChemAxon
Refractivity79.22 m3·mol-1ChemAxon
Polarizability27.59 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9925
Blood Brain Barrier+0.9802
Caco-2 permeable+0.5176
P-glycoprotein substrateSubstrate0.5785
P-glycoprotein inhibitor INon-inhibitor0.8782
P-glycoprotein inhibitor IINon-inhibitor0.9205
Renal organic cation transporterNon-inhibitor0.8307
CYP450 2C9 substrateNon-substrate0.7695
CYP450 2D6 substrateNon-substrate0.8583
CYP450 3A4 substrateSubstrate0.6725
CYP450 1A2 substrateInhibitor0.7569
CYP450 2C9 inhibitorNon-inhibitor0.6133
CYP450 2D6 inhibitorNon-inhibitor0.8986
CYP450 2C19 inhibitorInhibitor0.5682
CYP450 3A4 inhibitorInhibitor0.6791
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.5645
Ames testNon AMES toxic0.9132
CarcinogenicityNon-carcinogens0.7197
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.5397 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9904
hERG inhibition (predictor II)Non-inhibitor0.8498
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Mass Spectrum (Electron Ionization)MSsplash10-0zgi-2490000000-84b5bf7df62c745f8414
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-QFT , negativeLC-MS/MSsplash10-001i-0090000000-8f7713c4e618326c1d9b
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-0udi-0090000000-d514d232dff7c473d32f
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-0udi-0090000000-e2a1a64f13da7ed85586
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-0uk9-0190000000-f22bb948e3a20dfd2bff
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-006x-0980000000-f78bdd1a7e391dbaad48
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-014l-0920000000-d334a1a23130e08b3d55
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-014i-1900000000-3808670d5ccc91bd0e38
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-0uxu-3900000000-1fc08ceb9c88d5c734ca
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-0udi-5900000000-cbcd46c7ea13a9ff18cb
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-00lr-0090000000-bc49e652f5e2e4f4b760
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-001i-0090000000-c63c1250878b61e6d0da
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-001i-0090000000-02d4e0b73c57e157d6b0
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0019-0090000000-6623ad5dc09e01b5a573
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-000i-0390000000-38d5874ebcc0e05f411c
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-053r-0970000000-ce2d7caefc3860d70fa4
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-053r-0930000000-670ac85a651f0faf0d7d
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0udi-1900000000-f96a507afa68e1b3a438
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0udi-2900000000-c9082e2a3a5a56cfe408
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0udi-3900000000-310a824d6452fa47d987
MS/MS Spectrum - , positiveLC-MS/MSsplash10-001i-0190000000-6d4a0096179c1ef67c5a
1H NMR Spectrum1D NMRNot Applicable
13C NMR Spectrum1D NMRNot Applicable

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 / Nitroaromatic compounds / Benzene and substituted derivatives / Secondary carboxylic acid amides / Lactams / Ketimines / Propargyl-type 1,3-dipolar organic compounds / Organic oxoazanium compounds / Azacyclic compounds / Organopnictogen compounds
show 4 more
Substituents
1,4-benzodiazepine / Alpha-amino acid or derivatives / Nitroaromatic compound / Monocyclic benzene moiety / Benzenoid / Carboxamide group / Ketimine / Lactam / C-nitro compound / Organic nitro compound
show 18 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
C-nitro compound, 1,4-benzodiazepinone (CHEBI:7581)

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. Podhorna J, Krsiak M: Behavioural effects of a benzodiazepine receptor partial agonist, Ro 19-8022, in the social conflict test in mice. Behav Pharmacol. 2000 Apr;11(2):143-51. [PubMed:10877119]
  4. Tanaka M, Suemaru K, Watanabe S, Cui R, Li B, Araki H: Comparison of short- and long-acting benzodiazepine-receptor agonists with different receptor selectivity on motor coordination and muscle relaxation following thiopental-induced anesthesia in mice. J Pharmacol Sci. 2008 Jul;107(3):277-84. Epub 2008 Jul 5. [PubMed:18603831]
  5. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Potentiator
General Function
Inhibitory extracellular ligand-gated ion channel activity
Specific Function
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
Gene Name
GABRA2
Uniprot ID
P47869
Uniprot Name
Gamma-aminobutyric acid receptor subunit alpha-2
Molecular Weight
51325.85 Da
References
  1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090]
  2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [PubMed:18384456]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Potentiator
General Function
Inhibitory extracellular ligand-gated ion channel activity
Specific Function
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
Gene Name
GABRA3
Uniprot ID
P34903
Uniprot Name
Gamma-aminobutyric acid receptor subunit alpha-3
Molecular Weight
55164.055 Da
References
  1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090]
  2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [PubMed:18384456]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Potentiator
General Function
Inhibitory extracellular ligand-gated ion channel activity
Specific Function
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
Gene Name
GABRA4
Uniprot ID
P48169
Uniprot Name
Gamma-aminobutyric acid receptor subunit alpha-4
Molecular Weight
61622.645 Da
References
  1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090]
  2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [PubMed:18384456]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Potentiator
General Function
Transporter activity
Specific Function
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
Gene Name
GABRA5
Uniprot ID
P31644
Uniprot Name
Gamma-aminobutyric acid receptor subunit alpha-5
Molecular Weight
52145.645 Da
References
  1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090]
  2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [PubMed:18384456]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Potentiator
General Function
Inhibitory extracellular ligand-gated ion channel activity
Specific Function
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
Gene Name
GABRA6
Uniprot ID
Q16445
Uniprot Name
Gamma-aminobutyric acid receptor subunit alpha-6
Molecular Weight
51023.69 Da
References
  1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090]
  2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [PubMed:18384456]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Potentiator
General Function
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]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Other/unknown
General Function
Voltage-gated sodium channel activity
Specific Function
Mediates the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein forms a...
Gene Name
SCN1A
Uniprot ID
P35498
Uniprot Name
Sodium channel protein type 1 subunit alpha
Molecular Weight
228969.49 Da
References
  1. 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]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
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. 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
Inhibitor
General Function
Steroid hydroxylase activity
Specific Function
Metabolizes several precarcinogens, drugs, and solvents to reactive metabolites. Inactivates a number of drugs and xenobiotics and also bioactivates many xenobiotic substrates to their hepatotoxic ...
Gene Name
CYP2E1
Uniprot ID
P05181
Uniprot Name
Cytochrome P450 2E1
Molecular Weight
56848.42 Da
References
  1. Tassaneeyakul W, Birkett DJ, Miners JO: Inhibition of human hepatic cytochrome P4502E1 by azole antifungals, CNS-active drugs and non-steroidal anti-inflammatory agents. Xenobiotica. 1998 Mar;28(3):293-301. [PubMed:9574817]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
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. Mahar Doan KM, Humphreys JE, Webster LO, Wring SA, Shampine LJ, Serabjit-Singh CJ, Adkison KK, Polli JW: Passive permeability and P-glycoprotein-mediated efflux differentiate central nervous system (CNS) and non-CNS marketed drugs. J Pharmacol Exp Ther. 2002 Dec;303(3):1029-37. [PubMed:12438524]

Drug created on August 29, 2007 11:49 / Updated on January 19, 2018 10:56