Identification

Name
Flunitrazepam
Accession Number
DB01544
Type
Small Molecule
Groups
Approved, Illicit
Description

A benzodiazepine with pharmacologic actions similar to those of diazepam that can cause anterograde amnesia. Some reports indicate that it is used as a date rape drug and suggest that it may precipitate violent behavior. The United States Government has banned the importation of this drug. [PubChem]

Structure
Thumb
Synonyms
  • Flunitrazepamum
  • Rohypnol
External IDs
N05CD03 / RO 5-4200
International/Other Brands
Hipnosedon (Roche) / Hypnodorm (Alphapharm) / Narcozep (Roche) / Rohypnol (Roche) / Roipnol (Roche)
Categories
UNII
620X0222FQ
CAS number
1622-62-4
Weight
Average: 313.2832
Monoisotopic: 313.08626947
Chemical Formula
C16H12FN3O3
InChI Key
PPTYJKAXVCCBDU-UHFFFAOYSA-N
InChI
InChI=1S/C16H12FN3O3/c1-19-14-7-6-10(20(22)23)8-12(14)16(18-9-15(19)21)11-4-2-3-5-13(11)17/h2-8H,9H2,1H3
IUPAC Name
5-(2-fluorophenyl)-1-methyl-7-nitro-2,3-dihydro-1H-1,4-benzodiazepin-2-one
SMILES
CN1C2=C(C=C(C=C2)[N+]([O-])=O)C(=NCC1=O)C1=CC=CC=C1F

Pharmacology

Indication

For short-term treatment of severe insomnias, that are not responsive to other hypnotics.

Structured Indications
Not Available
Pharmacodynamics

Flunitrazepam is a powerful hypnotic drug that is a benzodiazepine derivative. It has powerful hypnotic, sedative, anxiolytic, and skeletal muscle relaxant properties. The drug is sometimes used as a date rape drug. In the United States, the drug has not been approved by the Food and Drug Administration for medical use, and is considered to be an illegal drug. It has however been approved in the United Kingdom and other countries.

Mechanism of action

Benzodiazepines bind nonspecifically to benzodiazepine receptors BNZ1, which mediates sleep, and BNZ2, which affects 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 the inhibitory neurotransmitter GABA to the site opens the chloride channel, resulting in a hyperpolarized cell membrane that prevents further excitation of the cell.

TargetActionsOrganism
ATranslocator protein
agonist
Human
AGamma-aminobutyric acid receptor subunit alpha-2
potentiator
Human
AGamma-aminobutyric acid receptor subunit alpha-4
agonist
Human
AGamma-aminobutyric acid receptor subunit alpha-5
potentiator
Human
AGamma-aminobutyric acid receptor subunit alpha-6
potentiator
Human
AGamma-aminobutyric acid receptor subunit alpha-3
potentiator
Human
UGamma-aminobutyric acid receptor subunit alpha-1
agonist
Human
UGamma-aminobutyric acid receptor subunit beta-3
agonist
Human
UGamma-aminobutyric acid receptor subunit gamma-2
agonist
Human
Absorption

50% (suppository) and 64-77% (oral)

Volume of distribution
Not Available
Protein binding
Not Available
Metabolism

Hepatic.

Route of elimination
Not Available
Half life

18-26 hours

Clearance
Not Available
Toxicity

Symptoms of overdose include confusion, coma, impaired coordination, sleepiness, and slowed reaction time.

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 Flunitrazepam is combined with 7-Nitroindazole.Experimental
AbirateroneThe serum concentration of Flunitrazepam can be increased when it is combined with Abiraterone.Approved
AcepromazineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Acepromazine.Approved, Vet Approved
AceprometazineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Aceprometazine.Approved
AdipiplonThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Adipiplon.Investigational
AgomelatineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Agomelatine.Approved, Investigational
AlaproclateThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Alaproclate.Experimental
AlfaxaloneThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Alfaxalone.Vet Approved
AlfentanilThe risk or severity of adverse effects can be increased when Alfentanil is combined with Flunitrazepam.Approved, Illicit
AllopregnanoloneThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Allopregnanolone.Investigational
AlphacetylmethadolThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Alphacetylmethadol.Experimental, Illicit
AlphaprodineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Alphaprodine.Illicit
AlprazolamThe risk or severity of adverse effects can be increased when Alprazolam is combined with Flunitrazepam.Approved, Illicit, Investigational
Ambroxol acefyllinateThe therapeutic efficacy of Flunitrazepam can be decreased when used in combination with Ambroxol acefyllinate.Experimental
AminophyllineThe therapeutic efficacy of Flunitrazepam can be decreased when used in combination with Aminophylline.Approved
AmiodaroneThe metabolism of Flunitrazepam can be decreased when combined with Amiodarone.Approved, Investigational
AmisulprideThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Amisulpride.Approved, Investigational
AmitriptylineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Amitriptyline.Approved
AmobarbitalThe risk or severity of adverse effects can be increased when Amobarbital is combined with Flunitrazepam.Approved, Illicit
AmoxapineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Amoxapine.Approved
AmperozideThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Amperozide.Experimental
AprepitantThe serum concentration of Flunitrazepam 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 Flunitrazepam.Approved, Investigational
ArmodafinilThe metabolism of Flunitrazepam can be decreased when combined with Armodafinil.Approved, Investigational
ArticaineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Articaine.Approved
AsenapineThe risk or severity of adverse effects can be increased when Asenapine is combined with Flunitrazepam.Approved
AtazanavirThe metabolism of Flunitrazepam can be decreased when combined with Atazanavir.Approved, Investigational
AtomoxetineThe metabolism of Flunitrazepam can be decreased when combined with Atomoxetine.Approved
AzaperoneThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Azaperone.Vet Approved
AzelastineFlunitrazepam may increase the central nervous system depressant (CNS depressant) activities of Azelastine.Approved
AzithromycinThe metabolism of Flunitrazepam can be decreased when combined with Azithromycin.Approved
BaclofenThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Baclofen.Approved
BarbitalThe risk or severity of adverse effects can be increased when Barbital is combined with Flunitrazepam.Illicit
BenperidolThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Benperidol.Investigational
BenzocaineThe risk or severity of adverse effects can be increased when Benzocaine is combined with Flunitrazepam.Approved
Benzyl alcoholThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Benzyl alcohol.Approved
BoceprevirThe metabolism of Flunitrazepam can be decreased when combined with Boceprevir.Withdrawn
BortezomibThe metabolism of Flunitrazepam can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Flunitrazepam can be decreased when it is combined with Bosentan.Approved, Investigational
BrexpiprazoleThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Brexpiprazole.Approved
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Flunitrazepam.Approved
BromazepamThe risk or severity of adverse effects can be increased when Bromazepam is combined with Flunitrazepam.Approved, Illicit
BromisovalThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Bromisoval.Experimental
BromperidolThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Bromperidol.Investigational
BrompheniramineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Brompheniramine.Approved
BrotizolamThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Brotizolam.Approved, Withdrawn
BupivacaineThe risk or severity of adverse effects can be increased when Bupivacaine is combined with Flunitrazepam.Approved, Investigational
BuprenorphineFlunitrazepam 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 Flunitrazepam.Approved, Investigational
ButabarbitalThe risk or severity of adverse effects can be increased when Butabarbital is combined with Flunitrazepam.Approved, Illicit
ButacaineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Butacaine.Vet Approved
ButalbitalThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Butalbital.Approved, Illicit
ButambenThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Butamben.Approved
ButethalThe risk or severity of adverse effects can be increased when Butethal is combined with Flunitrazepam.Approved, Illicit
ButorphanolThe risk or severity of adverse effects can be increased when Butorphanol is combined with Flunitrazepam.Approved, Illicit, Vet Approved
CaffeineThe metabolism of Flunitrazepam can be decreased when combined with Caffeine.Approved
CanertinibThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Canertinib.Investigational
CapecitabineThe metabolism of Flunitrazepam can be decreased when combined with Capecitabine.Approved, Investigational
CarbamazepineThe metabolism of Flunitrazepam can be increased when combined with Carbamazepine.Approved, Investigational
CarbinoxamineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Carbinoxamine.Approved
CarfentanilThe risk or severity of adverse effects can be increased when Carfentanil is combined with Flunitrazepam.Illicit, Vet Approved
CarisoprodolThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Carisoprodol.Approved
CeritinibThe serum concentration of Flunitrazepam can be increased when it is combined with Ceritinib.Approved
CetirizineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Cetirizine.Approved
Chloral hydrateThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Chloral hydrate.Approved, Illicit, Vet Approved
ChloramphenicolThe metabolism of Flunitrazepam 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 Flunitrazepam.Approved, Illicit
ChlormezanoneThe risk or severity of adverse effects can be increased when Chlormezanone is combined with Flunitrazepam.Approved, Withdrawn
ChloroprocaineThe risk or severity of adverse effects can be increased when Chloroprocaine is combined with Flunitrazepam.Approved
ChlorphenamineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Chlorphenamine.Approved
ChlorpromazineThe risk or severity of adverse effects can be increased when Chlorpromazine is combined with Flunitrazepam.Approved, Vet Approved
ChlorprothixeneThe risk or severity of adverse effects can be increased when Chlorprothixene is combined with Flunitrazepam.Approved, Withdrawn
ChlorzoxazoneThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Chlorzoxazone.Approved
CholecalciferolThe metabolism of Flunitrazepam can be decreased when combined with Cholecalciferol.Approved, Nutraceutical
CimetidineThe metabolism of Flunitrazepam can be decreased when combined with Cimetidine.Approved
CinchocaineThe risk or severity of adverse effects can be increased when Cinchocaine is combined with Flunitrazepam.Approved, Vet Approved
CitalopramThe metabolism of Flunitrazepam can be decreased when combined with Citalopram.Approved
ClarithromycinThe metabolism of Flunitrazepam can be decreased when combined with Clarithromycin.Approved
ClemastineThe metabolism of Flunitrazepam can be decreased when combined with Clemastine.Approved
ClidiniumThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Clidinium.Approved
ClobazamThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Clobazam.Approved, Illicit
clomethiazoleThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with clomethiazole.Investigational
ClomipramineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Clomipramine.Approved, Vet Approved
ClonazepamThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Clonazepam.Approved, Illicit
ClonidineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Clonidine.Approved
ClopenthixolThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Clopenthixol.Experimental
ClopidogrelThe metabolism of Flunitrazepam can be decreased when combined with Clopidogrel.Approved, Nutraceutical
ClorazepateThe risk or severity of adverse effects can be increased when Clorazepate is combined with Flunitrazepam.Approved, Illicit
ClothiapineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Clothiapine.Experimental
ClotrimazoleThe metabolism of Flunitrazepam can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Clozapine.Approved
CobicistatThe metabolism of Flunitrazepam can be decreased when combined with Cobicistat.Approved
CocaineThe risk or severity of adverse effects can be increased when Cocaine is combined with Flunitrazepam.Approved, Illicit
CodeineThe risk or severity of adverse effects can be increased when Codeine is combined with Flunitrazepam.Approved, Illicit
ConivaptanThe serum concentration of Flunitrazepam can be increased when it is combined with Conivaptan.Approved, Investigational
CrisaboroleThe metabolism of Flunitrazepam can be decreased when combined with Crisaborole.Approved
CrizotinibThe metabolism of Flunitrazepam can be decreased when combined with Crizotinib.Approved
CyclizineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Cyclizine.Approved
CyclobenzaprineThe risk or severity of adverse effects can be increased when Cyclobenzaprine is combined with Flunitrazepam.Approved
CyclosporineThe metabolism of Flunitrazepam can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
CyproheptadineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Cyproheptadine.Approved
Cyproterone acetateThe serum concentration of Flunitrazepam can be decreased when it is combined with Cyproterone acetate.Approved, Investigational
DabrafenibThe serum concentration of Flunitrazepam can be decreased when it is combined with Dabrafenib.Approved
DantroleneThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Dantrolene.Approved
DapiprazoleThe risk or severity of adverse effects can be increased when Dapiprazole is combined with Flunitrazepam.Approved
DapoxetineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Dapoxetine.Investigational
DarunavirThe metabolism of Flunitrazepam can be decreased when combined with Darunavir.Approved
DasatinibThe serum concentration of Flunitrazepam can be increased when it is combined with Dasatinib.Approved, Investigational
DeferasiroxThe serum concentration of Flunitrazepam can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe metabolism of Flunitrazepam can be decreased when combined with Delavirdine.Approved
DeramciclaneThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Deramciclane.Investigational
DesfluraneThe risk or severity of adverse effects can be increased when Desflurane is combined with Flunitrazepam.Approved
DesipramineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Desipramine.Approved
DesloratadineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Desloratadine.Approved, Investigational
DesvenlafaxineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Desvenlafaxine.Approved
DetomidineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Detomidine.Vet Approved
DexbrompheniramineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Dexbrompheniramine.Approved
DexmedetomidineThe risk or severity of adverse effects can be increased when Dexmedetomidine is combined with Flunitrazepam.Approved, Vet Approved
DextromoramideThe risk or severity of adverse effects can be increased when Dextromoramide is combined with Flunitrazepam.Experimental, Illicit
DextropropoxypheneThe risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Flunitrazepam.Approved, Illicit, Withdrawn
DezocineThe risk or severity of adverse effects can be increased when Dezocine is combined with Flunitrazepam.Approved
DiazepamThe risk or severity of adverse effects can be increased when Diazepam is combined with Flunitrazepam.Approved, Illicit, Vet Approved
Diethyl etherThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Diethyl ether.Experimental
DifenoxinThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Difenoxin.Approved, Illicit
DihydrocodeineThe risk or severity of adverse effects can be increased when Dihydrocodeine is combined with Flunitrazepam.Approved, Illicit
DihydroergotamineThe metabolism of Flunitrazepam can be decreased when combined with Dihydroergotamine.Approved
DihydroetorphineThe risk or severity of adverse effects can be increased when Dihydroetorphine is combined with Flunitrazepam.Experimental, Illicit
DihydromorphineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Dihydromorphine.Experimental, Illicit
DiltiazemThe metabolism of Flunitrazepam can be decreased when combined with Diltiazem.Approved
DimenhydrinateThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Dimenhydrinate.Approved
DiphenhydramineThe risk or severity of adverse effects can be increased when Diphenhydramine is combined with Flunitrazepam.Approved
DiphenoxylateThe risk or severity of adverse effects can be increased when Diphenoxylate is combined with Flunitrazepam.Approved, Illicit
DixyrazineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Dixyrazine.Experimental
DoramectinThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Doramectin.Vet Approved
DosulepinThe metabolism of Flunitrazepam can be decreased when combined with Dosulepin.Approved
DoxepinThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Doxepin.Approved
DoxorubicinThe metabolism of Flunitrazepam can be decreased when combined with Doxorubicin.Approved, Investigational
DoxycyclineThe metabolism of Flunitrazepam can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Flunitrazepam.Approved, Vet Approved
DPDPEThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with DPDPE.Investigational
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Flunitrazepam.Approved, Illicit
DronedaroneThe metabolism of Flunitrazepam can be decreased when combined with Dronedarone.Approved
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Flunitrazepam.Approved, Vet Approved
DrotebanolThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Drotebanol.Experimental, Illicit
DuloxetineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Duloxetine.Approved
DyclonineThe risk or severity of adverse effects can be increased when Dyclonine is combined with Flunitrazepam.Approved
DyphyllineThe therapeutic efficacy of Flunitrazepam can be decreased when used in combination with Dyphylline.Approved
EcgonineThe risk or severity of adverse effects can be increased when Ecgonine is combined with Flunitrazepam.Experimental, Illicit
EcopipamThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Ecopipam.Investigational
EfavirenzThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Efavirenz.Approved, Investigational
EltanoloneThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Eltanolone.Investigational
EnfluraneThe risk or severity of adverse effects can be increased when Enflurane is combined with Flunitrazepam.Approved, Vet Approved
EntacaponeThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Entacapone.Approved, Investigational
EnzalutamideThe serum concentration of Flunitrazepam can be decreased when it is combined with Enzalutamide.Approved
ErythromycinThe metabolism of Flunitrazepam can be decreased when combined with Erythromycin.Approved, Vet Approved
EscitalopramThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Escitalopram.Approved, Investigational
Eslicarbazepine acetateThe metabolism of Flunitrazepam can be decreased when combined with Eslicarbazepine acetate.Approved
EsomeprazoleThe metabolism of Flunitrazepam can be decreased when combined with Esomeprazole.Approved, Investigational
EstazolamThe risk or severity of adverse effects can be increased when Estazolam is combined with Flunitrazepam.Approved, Illicit
EszopicloneThe risk or severity of adverse effects can be increased when Eszopiclone is combined with Flunitrazepam.Approved
EthanolFlunitrazepam 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 Flunitrazepam.Approved, Illicit, Withdrawn
EthosuximideThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Ethosuximide.Approved
EthotoinThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Ethotoin.Approved
Ethyl carbamateThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Ethyl carbamate.Withdrawn
Ethyl chlorideThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Ethyl chloride.Experimental
Ethyl loflazepateThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Ethyl loflazepate.Approved, Illicit
EthylmorphineThe risk or severity of adverse effects can be increased when Ethylmorphine is combined with Flunitrazepam.Approved, Illicit
EtidocaineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Etidocaine.Approved
EtifoxineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Etifoxine.Withdrawn
EtizolamThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Etizolam.Approved
EtomidateThe risk or severity of adverse effects can be increased when Etomidate is combined with Flunitrazepam.Approved
EtoperidoneThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Etoperidone.Approved
EtorphineThe risk or severity of adverse effects can be increased when Etorphine is combined with Flunitrazepam.Illicit, Vet Approved
EtravirineThe metabolism of Flunitrazepam can be decreased when combined with Etravirine.Approved
EzogabineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Ezogabine.Approved
FelbamateThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Felbamate.Approved
FencamfamineThe risk or severity of adverse effects can be increased when Fencamfamine is combined with Flunitrazepam.Approved, Illicit, Withdrawn
FentanylThe risk or severity of adverse effects can be increased when Fentanyl is combined with Flunitrazepam.Approved, Illicit, Investigational, Vet Approved
FexofenadineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Fexofenadine.Approved
FlibanserinThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Flibanserin.Approved
FloxuridineThe metabolism of Flunitrazepam can be decreased when combined with Floxuridine.Approved
FluanisoneThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Fluanisone.Experimental
FluconazoleThe metabolism of Flunitrazepam can be decreased when combined with Fluconazole.Approved
FludiazepamThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Fludiazepam.Approved, Illicit
FlunarizineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Flunarizine.Approved
FluorouracilThe metabolism of Flunitrazepam can be decreased when combined with Fluorouracil.Approved
FluoxetineThe metabolism of Flunitrazepam can be decreased when combined with Fluoxetine.Approved, Vet Approved
FlupentixolThe risk or severity of adverse effects can be increased when Flupentixol is combined with Flunitrazepam.Approved, Withdrawn
FluphenazineThe risk or severity of adverse effects can be increased when Fluphenazine is combined with Flunitrazepam.Approved
FlurazepamThe risk or severity of adverse effects can be increased when Flurazepam is combined with Flunitrazepam.Approved, Illicit
FluspirileneThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Fluspirilene.Approved
Fluticasone propionateThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Fluticasone propionate.Approved
FluvastatinThe metabolism of Flunitrazepam can be decreased when combined with Fluvastatin.Approved
FluvoxamineThe metabolism of Flunitrazepam can be decreased when combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe metabolism of Flunitrazepam can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Flunitrazepam can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe serum concentration of Fosphenytoin can be increased when it is combined with Flunitrazepam.Approved
FospropofolThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Fospropofol.Approved, Illicit
Fusidic AcidThe serum concentration of Flunitrazepam 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 Flunitrazepam.Approved, Investigational
Gabapentin EnacarbilThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Gabapentin Enacarbil.Approved
Gamma Hydroxybutyric AcidThe risk or severity of adverse effects can be increased when Gamma Hydroxybutyric Acid is combined with Flunitrazepam.Approved, Illicit
GemfibrozilThe metabolism of Flunitrazepam can be decreased when combined with Gemfibrozil.Approved
GepironeThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Gepirone.Investigational
GlutethimideThe risk or severity of adverse effects can be increased when Glutethimide is combined with Flunitrazepam.Approved, Illicit
GuanfacineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Guanfacine.Approved, Investigational
HalazepamThe risk or severity of adverse effects can be increased when Halazepam is combined with Flunitrazepam.Approved, Illicit, Withdrawn
HaloperidolThe risk or severity of adverse effects can be increased when Haloperidol is combined with Flunitrazepam.Approved
HalothaneThe risk or severity of adverse effects can be increased when Halothane is combined with Flunitrazepam.Approved, Vet Approved
HeroinThe risk or severity of adverse effects can be increased when Heroin is combined with Flunitrazepam.Approved, Illicit
HexobarbitalThe risk or severity of adverse effects can be increased when Hexobarbital is combined with Flunitrazepam.Approved
HyaluronidaseThe therapeutic efficacy of Flunitrazepam can be decreased when used in combination with Hyaluronidase.Approved, Investigational
HydrocodoneFlunitrazepam 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 Flunitrazepam.Approved, Illicit
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Flunitrazepam.Approved
IdelalisibThe serum concentration of Flunitrazepam can be increased when it is combined with Idelalisib.Approved
IloperidoneThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Iloperidone.Approved
ImatinibThe metabolism of Flunitrazepam can be decreased when combined with Imatinib.Approved
ImipramineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Imipramine.Approved
IndalpineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Indalpine.Investigational, Withdrawn
IndinavirThe metabolism of Flunitrazepam can be decreased when combined with Indinavir.Approved
IndiplonThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Indiplon.Investigational
IrbesartanThe metabolism of Flunitrazepam can be decreased when combined with Irbesartan.Approved, Investigational
IrinotecanThe serum concentration of the active metabolites of Irinotecan can be increased when Irinotecan is used in combination with Flunitrazepam.Approved, Investigational
IsavuconazoniumThe metabolism of Flunitrazepam can be decreased when combined with Isavuconazonium.Approved, Investigational
IsofluraneThe risk or severity of adverse effects can be increased when Isoflurane is combined with Flunitrazepam.Approved, Vet Approved
IsoniazidThe metabolism of Flunitrazepam can be decreased when combined with Isoniazid.Approved
IsradipineThe metabolism of Flunitrazepam can be decreased when combined with Isradipine.Approved
ItraconazoleThe metabolism of Flunitrazepam can be decreased when combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Flunitrazepam 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 Flunitrazepam.Approved, Vet Approved
KetazolamThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Ketazolam.Approved
KetobemidoneThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Ketobemidone.Approved
KetoconazoleThe metabolism of Flunitrazepam can be decreased when combined with Ketoconazole.Approved, Investigational
LamotrigineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Lamotrigine.Approved, Investigational
LeflunomideThe metabolism of Flunitrazepam can be decreased when combined with Leflunomide.Approved, Investigational
LevetiracetamThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Levetiracetam.Approved, Investigational
LevobupivacaineThe risk or severity of adverse effects can be increased when Levobupivacaine is combined with Flunitrazepam.Approved
LevocabastineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Levocabastine.Approved
LevocetirizineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Levocetirizine.Approved
LevodopaThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Levodopa.Approved
Levomethadyl AcetateThe risk or severity of adverse effects can be increased when Levomethadyl Acetate is combined with Flunitrazepam.Approved
LevomilnacipranThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Levomilnacipran.Approved
LevorphanolThe risk or severity of adverse effects can be increased when Levorphanol is combined with Flunitrazepam.Approved
LidocaineThe metabolism of Flunitrazepam can be decreased when combined with Lidocaine.Approved, Vet Approved
LithiumThe risk or severity of adverse effects can be increased when Lithium is combined with Flunitrazepam.Approved
LobeglitazoneThe metabolism of Flunitrazepam can be decreased when combined with Lobeglitazone.Approved
LofentanilThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Lofentanil.Illicit
LopinavirThe metabolism of Flunitrazepam can be decreased when combined with Lopinavir.Approved
LoprazolamThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Loprazolam.Experimental
LoratadineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Loratadine.Approved
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Flunitrazepam.Approved
LormetazepamThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Lormetazepam.Approved
LosartanThe metabolism of Flunitrazepam can be decreased when combined with Losartan.Approved
LovastatinThe metabolism of Flunitrazepam can be decreased when combined with Lovastatin.Approved, Investigational
LoxapineThe risk or severity of adverse effects can be increased when Loxapine is combined with Flunitrazepam.Approved
LuliconazoleThe serum concentration of Flunitrazepam can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of Flunitrazepam can be decreased when it is combined with Lumacaftor.Approved
LurasidoneThe risk or severity of adverse effects can be increased when Lurasidone is combined with Flunitrazepam.Approved
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Flunitrazepam.Approved, Vet Approved
ManidipineThe metabolism of Flunitrazepam can be decreased when combined with Manidipine.Approved
MaprotilineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Maprotiline.Approved
MebicarThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Mebicar.Experimental
MeclizineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Meclizine.Approved
MedazepamThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Medazepam.Experimental
MedetomidineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Medetomidine.Vet Approved
MelatoninThe risk or severity of adverse effects can be increased when Melatonin is combined with Flunitrazepam.Approved, Nutraceutical, Vet Approved
MelperoneThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Melperone.Approved
MepivacaineThe risk or severity of adverse effects can be increased when Mepivacaine is combined with Flunitrazepam.Approved, Vet Approved
MeprobamateThe risk or severity of adverse effects can be increased when Meprobamate is combined with Flunitrazepam.Approved, Illicit
MeptazinolThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Meptazinol.Experimental
MesoridazineThe risk or severity of adverse effects can be increased when Mesoridazine is combined with Flunitrazepam.Approved
MetaxaloneThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Metaxalone.Approved
MethadoneFlunitrazepam 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 Flunitrazepam.Approved, Illicit
MethapyrileneThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Methapyrilene.Withdrawn
MethaqualoneThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Methaqualone.Illicit, Withdrawn
MethocarbamolThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Methocarbamol.Approved, Vet Approved
MethohexitalThe risk or severity of adverse effects can be increased when Methohexital is combined with Flunitrazepam.Approved
MethotrimeprazineFlunitrazepam 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 Flunitrazepam.Approved, Vet Approved
MethsuximideThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Methsuximide.Approved
MethylecgonineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Methylecgonine.Experimental
MethylphenobarbitalThe risk or severity of adverse effects can be increased when Methylphenobarbital is combined with Flunitrazepam.Approved
MetyrosineFlunitrazepam may increase the sedative activities of Metyrosine.Approved
MexiletineThe metabolism of Flunitrazepam can be decreased when combined with Mexiletine.Approved
MidazolamThe risk or severity of adverse effects can be increased when Midazolam is combined with Flunitrazepam.Approved, Illicit
MidostaurinThe metabolism of Flunitrazepam can be decreased when combined with Midostaurin.Approved
MifepristoneThe serum concentration of Flunitrazepam can be increased when it is combined with Mifepristone.Approved, Investigational
MilnacipranThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Milnacipran.Approved
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Flunitrazepam.Approved, Investigational
MirtazapineFlunitrazepam may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.Approved
MitotaneThe serum concentration of Flunitrazepam can be decreased when it is combined with Mitotane.Approved
MoclobemideThe metabolism of Flunitrazepam can be decreased when combined with Moclobemide.Approved
ModafinilThe metabolism of Flunitrazepam can be decreased when combined with Modafinil.Approved, Investigational
MolindoneThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Molindone.Approved
MorphineThe risk or severity of adverse effects can be increased when Morphine is combined with Flunitrazepam.Approved, Investigational
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Flunitrazepam.Approved, Investigational
NalbuphineThe risk or severity of adverse effects can be increased when Nalbuphine is combined with Flunitrazepam.Approved
NefazodoneThe metabolism of Flunitrazepam can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe metabolism of Flunitrazepam can be decreased when combined with Nelfinavir.Approved
NetupitantThe serum concentration of Flunitrazepam can be increased when it is combined with Netupitant.Approved
NevirapineThe metabolism of Flunitrazepam can be increased when combined with Nevirapine.Approved
NicardipineThe metabolism of Flunitrazepam can be decreased when combined with Nicardipine.Approved
NicotineThe metabolism of Flunitrazepam can be decreased when combined with Nicotine.Approved
NilotinibThe metabolism of Flunitrazepam can be decreased when combined with Nilotinib.Approved, Investigational
NitrazepamThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Flunitrazepam.Approved
Nitrous oxideThe risk or severity of adverse effects can be increased when Nitrous oxide is combined with Flunitrazepam.Approved, Vet Approved
NorfluraneThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Norflurane.Investigational
NormethadoneThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Normethadone.Approved, Illicit
NortriptylineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Nortriptyline.Approved
OlanzapineThe risk or severity of adverse effects can be increased when Olanzapine is combined with Flunitrazepam.Approved, Investigational
OlaparibThe metabolism of Flunitrazepam can be decreased when combined with Olaparib.Approved
OlopatadineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Olopatadine.Approved
OmeprazoleThe metabolism of Flunitrazepam can be decreased when combined with Omeprazole.Approved, Investigational, Vet Approved
OndansetronThe risk or severity of adverse effects can be increased when Ondansetron is combined with Flunitrazepam.Approved
OpiumThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Opium.Approved, Illicit
OrphenadrineFlunitrazepam may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
OsanetantThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Osanetant.Investigational
OsimertinibThe serum concentration of Flunitrazepam 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 Flunitrazepam.Approved
OxethazaineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Oxethazaine.Investigational
OxprenololThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Oxprenolol.Approved
OxybuprocaineThe risk or severity of adverse effects can be increased when Oxybuprocaine is combined with Flunitrazepam.Approved
OxycodoneThe risk or severity of adverse effects can be increased when Oxycodone is combined with Flunitrazepam.Approved, Illicit, Investigational
OxymorphoneThe risk or severity of adverse effects can be increased when Oxymorphone is combined with Flunitrazepam.Approved, Investigational, Vet Approved
PalbociclibThe serum concentration of Flunitrazepam 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 Flunitrazepam.Approved
PantoprazoleThe metabolism of Flunitrazepam can be decreased when combined with Pantoprazole.Approved
ParaldehydeFlunitrazepam may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.Approved
ParoxetineThe metabolism of Flunitrazepam can be decreased when combined with Paroxetine.Approved, Investigational
Peginterferon alfa-2bThe serum concentration of Flunitrazepam can be increased when it is combined with Peginterferon alfa-2b.Approved
PenfluridolThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Penfluridol.Experimental
PentazocineThe risk or severity of adverse effects can be increased when Pentazocine is combined with Flunitrazepam.Approved, Vet Approved
PentobarbitalThe metabolism of Flunitrazepam can be increased when combined with Pentobarbital.Approved, Vet Approved
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Flunitrazepam.Approved
PerazineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Perazine.Investigational
PerospironeThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Perospirone.Approved
PerphenazineThe risk or severity of adverse effects can be increased when Perphenazine is combined with Flunitrazepam.Approved
PethidineThe risk or severity of adverse effects can be increased when Pethidine is combined with Flunitrazepam.Approved
PhenazocineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Phenazocine.Experimental
PhenibutThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Phenibut.Experimental
PhenobarbitalThe metabolism of Flunitrazepam can be increased when combined with Phenobarbital.Approved
PhenoperidineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Phenoperidine.Experimental
PhenoxyethanolThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Phenoxyethanol.Approved
PhenytoinThe serum concentration of Phenytoin can be increased when it is combined with Flunitrazepam.Approved, Vet Approved
PimozideThe risk or severity of adverse effects can be increased when Pimozide is combined with Flunitrazepam.Approved
PipamperoneThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Pipamperone.Approved
PipotiazineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Pipotiazine.Approved
PiritramideThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Piritramide.Investigational
PizotifenThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Pizotifen.Approved
PomalidomideThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Pomalidomide.Approved
PosaconazoleThe metabolism of Flunitrazepam can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
PramipexoleFlunitrazepam may increase the sedative activities of Pramipexole.Approved, Investigational
PramocaineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Pramocaine.Approved
PrazepamThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Prazepam.Approved, Illicit
PregabalinThe risk or severity of adverse effects can be increased when Pregabalin is combined with Flunitrazepam.Approved, Illicit, Investigational
PrilocaineThe risk or severity of adverse effects can be increased when Prilocaine is combined with Flunitrazepam.Approved
PrimidoneThe metabolism of Flunitrazepam 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 Flunitrazepam.Approved, Investigational, Vet Approved
ProchlorperazineThe risk or severity of adverse effects can be increased when Prochlorperazine is combined with Flunitrazepam.Approved, Vet Approved
PromazineThe risk or severity of adverse effects can be increased when Promazine is combined with Flunitrazepam.Approved, Vet Approved
PromethazineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Promethazine.Approved
PropanididThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Propanidid.Experimental
ProparacaineThe risk or severity of adverse effects can be increased when Proparacaine is combined with Flunitrazepam.Approved, Vet Approved
PropofolThe risk or severity of adverse effects can be increased when Propofol is combined with Flunitrazepam.Approved, Investigational, Vet Approved
PropoxycaineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Propoxycaine.Approved
ProtriptylineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Protriptyline.Approved
ProxibarbalThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Proxibarbal.Experimental
PSD502The risk or severity of adverse effects can be increased when Flunitrazepam is combined with PSD502.Investigational
PyrimethamineThe metabolism of Flunitrazepam can be decreased when combined with Pyrimethamine.Approved, Vet Approved
QuazepamThe serum concentration of Flunitrazepam can be increased when it is combined with Quazepam.Approved, Illicit
QuetiapineThe risk or severity of adverse effects can be increased when Quetiapine is combined with Flunitrazepam.Approved
QuinineThe metabolism of Flunitrazepam can be decreased when combined with Quinine.Approved
QuinisocaineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Quinisocaine.Experimental
RacloprideThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Raclopride.Investigational
RamelteonThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Ramelteon.Approved, Investigational
RanolazineThe metabolism of Flunitrazepam can be decreased when combined with Ranolazine.Approved, Investigational
RemifentanilThe risk or severity of adverse effects can be increased when Remifentanil is combined with Flunitrazepam.Approved
RemoxiprideThe risk or severity of adverse effects can be increased when Remoxipride is combined with Flunitrazepam.Approved, Withdrawn
ReserpineThe risk or severity of adverse effects can be increased when Reserpine is combined with Flunitrazepam.Approved
RifabutinThe metabolism of Flunitrazepam can be increased when combined with Rifabutin.Approved
RifampicinThe metabolism of Flunitrazepam can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Flunitrazepam can be increased when combined with Rifapentine.Approved
RisperidoneThe risk or severity of adverse effects can be increased when Risperidone is combined with Flunitrazepam.Approved, Investigational
RitanserinThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Ritanserin.Investigational
RitonavirThe metabolism of Flunitrazepam can be decreased when combined with Ritonavir.Approved, Investigational
RomifidineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Romifidine.Vet Approved
RopiniroleFlunitrazepam may increase the sedative activities of Ropinirole.Approved, Investigational
RopivacaineThe risk or severity of adverse effects can be increased when Ropivacaine is combined with Flunitrazepam.Approved
RotigotineFlunitrazepam may increase the sedative activities of Rotigotine.Approved
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Flunitrazepam.Approved
SaquinavirThe metabolism of Flunitrazepam can be decreased when combined with Saquinavir.Approved, Investigational
ScopolamineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Scopolamine.Approved
SecobarbitalThe metabolism of Flunitrazepam can be increased when combined with Secobarbital.Approved, Vet Approved
SepranoloneThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Sepranolone.Investigational
SertindoleThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Sertindole.Approved, Withdrawn
SertralineThe metabolism of Flunitrazepam can be decreased when combined with Sertraline.Approved
SevofluraneThe risk or severity of adverse effects can be increased when Sevoflurane is combined with Flunitrazepam.Approved, Vet Approved
SildenafilThe metabolism of Flunitrazepam can be decreased when combined with Sildenafil.Approved, Investigational
SiltuximabThe serum concentration of Flunitrazepam can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Flunitrazepam can be increased when it is combined with Simeprevir.Approved
SorafenibThe metabolism of Flunitrazepam can be decreased when combined with Sorafenib.Approved, Investigational
St. John's WortThe serum concentration of Flunitrazepam can be decreased when it is combined with St. John's Wort.Nutraceutical
StiripentolThe serum concentration of Flunitrazepam 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 Flunitrazepam.Approved, Investigational
SulfadiazineThe metabolism of Flunitrazepam can be decreased when combined with Sulfadiazine.Approved, Vet Approved
SulfamethoxazoleThe metabolism of Flunitrazepam can be decreased when combined with Sulfamethoxazole.Approved
SulfisoxazoleThe metabolism of Flunitrazepam 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 Flunitrazepam.Approved
SultoprideThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Sultopride.Experimental
SuvorexantFlunitrazepam may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.Approved
TandospironeThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Tandospirone.Investigational
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Flunitrazepam.Approved
TasimelteonThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Tasimelteon.Approved
TeduglutideThe serum concentration of Flunitrazepam can be increased when it is combined with Teduglutide.Approved
TelaprevirThe metabolism of Flunitrazepam can be decreased when combined with Telaprevir.Withdrawn
TelithromycinThe metabolism of Flunitrazepam can be decreased when combined with Telithromycin.Approved
TemazepamThe risk or severity of adverse effects can be increased when Temazepam is combined with Flunitrazepam.Approved
Tenofovir disoproxilThe metabolism of Flunitrazepam can be decreased when combined with Tenofovir disoproxil.Approved, Investigational
TeriflunomideThe serum concentration of Flunitrazepam can be decreased when it is combined with Teriflunomide.Approved
TetrabenazineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Tetrabenazine.Approved
TetracaineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Tetracaine.Approved, Vet Approved
TetrahydropalmatineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Tetrahydropalmatine.Investigational
TetrodotoxinThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Tetrodotoxin.Investigational
ThalidomideFlunitrazepam may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.Approved, Investigational, Withdrawn
TheophyllineThe therapeutic efficacy of Flunitrazepam can be decreased when used in combination with Theophylline.Approved
ThiamylalThe risk or severity of adverse effects can be increased when Thiamylal is combined with Flunitrazepam.Approved, Vet Approved
ThiopentalThe risk or severity of adverse effects can be increased when Thiopental is combined with Flunitrazepam.Approved, Vet Approved
ThioridazineThe risk or severity of adverse effects can be increased when Thioridazine is combined with Flunitrazepam.Withdrawn
ThiotepaThe metabolism of Flunitrazepam can be decreased when combined with Thiotepa.Approved
ThiothixeneThe risk or severity of adverse effects can be increased when Thiothixene is combined with Flunitrazepam.Approved
TiagabineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Tiagabine.Approved
TiaprideThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Tiapride.Approved, Investigational
TicagrelorThe metabolism of Flunitrazepam can be decreased when combined with Ticagrelor.Approved
TiclopidineThe metabolism of Flunitrazepam can be decreased when combined with Ticlopidine.Approved
TiletamineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Tiletamine.Vet Approved
TilidineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Tilidine.Experimental
TizanidineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Tizanidine.Approved
TocilizumabThe serum concentration of Flunitrazepam can be decreased when it is combined with Tocilizumab.Approved
TolbutamideThe metabolism of Flunitrazepam can be decreased when combined with Tolbutamide.Approved
TolcaponeThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Tolcapone.Approved, Withdrawn
TopiramateThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Topiramate.Approved
TopiroxostatThe metabolism of Flunitrazepam can be decreased when combined with Topiroxostat.Approved
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with Flunitrazepam.Approved, Investigational
Trans-2-PhenylcyclopropylamineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Trans-2-Phenylcyclopropylamine.Experimental
TranylcypromineThe risk or severity of adverse effects can be increased when Tranylcypromine is combined with Flunitrazepam.Approved
TrazodoneThe risk or severity of adverse effects can be increased when Trazodone is combined with Flunitrazepam.Approved, Investigational
TriazolamThe risk or severity of adverse effects can be increased when Triazolam is combined with Flunitrazepam.Approved
Tricaine methanesulfonateThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Tricaine methanesulfonate.Vet Approved
TrichloroethyleneThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Trichloroethylene.Experimental
TrifluoperazineThe risk or severity of adverse effects can be increased when Trifluoperazine is combined with Flunitrazepam.Approved
TrifluperidolThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Trifluperidol.Experimental
TriflupromazineThe risk or severity of adverse effects can be increased when Triflupromazine is combined with Flunitrazepam.Approved, Vet Approved
TrimethoprimThe metabolism of Flunitrazepam can be decreased when combined with Trimethoprim.Approved, Vet Approved
TrimipramineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Trimipramine.Approved
TriprolidineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Triprolidine.Approved
Valproic AcidThe risk or severity of adverse effects can be increased when Valproic Acid is combined with Flunitrazepam.Approved, Investigational
ValsartanThe metabolism of Flunitrazepam can be decreased when combined with Valsartan.Approved, Investigational
VemurafenibThe serum concentration of Flunitrazepam can be increased when it is combined with Vemurafenib.Approved
VenlafaxineThe metabolism of Flunitrazepam can be decreased when combined with Venlafaxine.Approved
VeraliprideThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Veralipride.Experimental
VerapamilThe metabolism of Flunitrazepam can be decreased when combined with Verapamil.Approved
VigabatrinThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Vigabatrin.Approved
Vinyl etherThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Vinyl ether.Experimental
VoriconazoleThe metabolism of Flunitrazepam can be decreased when combined with Voriconazole.Approved, Investigational
VortioxetineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Vortioxetine.Approved
XenonThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Xenon.Experimental
XylazineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Xylazine.Vet Approved
YohimbineThe therapeutic efficacy of Flunitrazepam can be decreased when used in combination with Yohimbine.Approved, Vet Approved
ZafirlukastThe metabolism of Flunitrazepam can be decreased when combined with Zafirlukast.Approved, Investigational
ZaleplonThe risk or severity of adverse effects can be increased when Zaleplon is combined with Flunitrazepam.Approved, Illicit, Investigational
ZiconotideThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Ziconotide.Approved
ZimelidineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Zimelidine.Withdrawn
ZiprasidoneThe metabolism of Flunitrazepam can be decreased when combined with Ziprasidone.Approved
ZolazepamThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Zolazepam.Vet Approved
ZolpidemFlunitrazepam may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.Approved
ZonisamideThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Zonisamide.Approved, Investigational
ZopicloneThe risk or severity of adverse effects can be increased when Zopiclone is combined with Flunitrazepam.Approved
ZotepineThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Zotepine.Approved
ZucapsaicinThe metabolism of Flunitrazepam can be decreased when combined with Zucapsaicin.Approved
ZuclopenthixolThe risk or severity of adverse effects can be increased when Zuclopenthixol is combined with Flunitrazepam.Approved, Investigational
Food Interactions
  • Avoid alcohol.
  • Avoid excessive quantities of coffee or tea (Caffeine).
  • Avoid taking with grapefruit juice.
  • Take with food.

References

Synthesis Reference

Kariss, J. and Newmark, H.L.; U.S. Patent 3,116,203; December 31, 1963; assigned to Hoffmann-la Roche Inc.
 Kariss, J. and Newmark, H.L.; US. Patent 3,123,529; March 3,1964; assigned to Hoffmann-La Roche Inc. 
Keiler, O., Steiger, N. and Sternbach, L.H.; U.S. Patent 3,203,990; August 31, 1965; assigned to Hoffmann-La Roche Inc.

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. 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]
  5. Tokunaga S, Takeda Y, Shinomiya K, Hirase M, Kamei C: Effects of some H1-antagonists on the sleep-wake cycle in sleep-disturbed rats. J Pharmacol Sci. 2007 Feb;103(2):201-6. Epub 2007 Feb 8. [PubMed:17287588]
External Links
Human Metabolome Database
HMDB15510
KEGG Drug
D01230
PubChem Compound
3380
PubChem Substance
46504553
ChemSpider
3263
BindingDB
25878
ChEBI
31622
ChEMBL
CHEMBL13280
Therapeutic Targets Database
DAP000931
PharmGKB
PA164781320
Wikipedia
Flunitrazepam
ATC Codes
N05CD03 — Flunitrazepam
AHFS Codes
Not Available
PDB Entries
Not Available
FDA label
Not Available
MSDS
Not Available

Clinical Trials

Clinical Trials
Not Available

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)166-167 °CKariss, J. and Newmark, H.L.; U.S. Patent 3,116,203; December 31, 1963; assigned to Hoffmann-la Roche Inc.
 Kariss, J. and Newmark, H.L.; US. Patent 3,123,529; March 3,1964; assigned to Hoffmann-La Roche Inc. 
Keiler, O., Steiger, N. and Sternbach, L.H.; U.S. Patent 3,203,990; August 31, 1965; assigned to Hoffmann-La Roche Inc.
logP2.06HANSCH,C ET AL. (1995)
Predicted Properties
PropertyValueSource
Water Solubility0.00858 mg/mLALOGPS
logP2.2ALOGPS
logP2.55ChemAxon
logS-4.6ALOGPS
pKa (Strongest Basic)1.7ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area78.49 Å2ChemAxon
Rotatable Bond Count2ChemAxon
Refractivity82.55 m3·mol-1ChemAxon
Polarizability29.6 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9922
Blood Brain Barrier+0.973
Caco-2 permeable+0.5257
P-glycoprotein substrateSubstrate0.6717
P-glycoprotein inhibitor INon-inhibitor0.6428
P-glycoprotein inhibitor IINon-inhibitor0.9094
Renal organic cation transporterNon-inhibitor0.713
CYP450 2C9 substrateNon-substrate0.7621
CYP450 2D6 substrateNon-substrate0.8932
CYP450 3A4 substrateSubstrate0.725
CYP450 1A2 substrateNon-inhibitor0.5691
CYP450 2C9 inhibitorNon-inhibitor0.5163
CYP450 2D6 inhibitorNon-inhibitor0.8776
CYP450 2C19 inhibitorInhibitor0.5957
CYP450 3A4 inhibitorInhibitor0.5626
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.5555
Ames testAMES toxic0.9108
CarcinogenicityNon-carcinogens0.7209
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.8125 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9869
hERG inhibition (predictor II)Non-inhibitor0.8074
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)MSsplash10-01p9-2393000000-5d873203e4acf1211838
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/MSsplash10-03di-0009000000-d3cdbd0e6db0ff7d3658
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-02t9-0098000000-ed4fc29ca5e103e7e7ac
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-014i-0292000000-910e58767edf9829ae76
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-000i-0590000000-f32a6119c0a1af4b09f1
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-03di-0009000000-0917b69ebd96bce7d228
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-03di-0009000000-52198b26a21902b1164d
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-02t9-0095000000-6905e6ef41a999c5c6bb
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-014r-0291000000-05daa60855227774f98a
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-01p9-0590000000-1dc724d4ffca2a0dcc87
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0230-0970000000-c801330e64d95e44fce8
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-00si-1920000000-6d855cf670784a504122
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-001i-2910000000-ab0a5646c93755d78538
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0gx0-3900000000-0e0998c190e076f40d1b

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 / Fluorobenzenes / Aryl fluorides / Tertiary carboxylic acid amides / Lactams / Ketimines / Propargyl-type 1,3-dipolar organic compounds / Organic oxoazanium compounds / Azacyclic compounds
show 5 more
Substituents
1,4-benzodiazepine / Alpha-amino acid or derivatives / Nitroaromatic compound / Fluorobenzene / Halobenzene / Aryl fluoride / Aryl halide / Monocyclic benzene moiety / Benzenoid / Tertiary carboxylic acid amide
show 23 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
Not Available

Targets

Details
1. Translocator protein
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Agonist
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. Katz Y, Weizman R, Weizman A, Gavish M: Disulfiram and diethyldithiocarbamate are competitive inhibitors at the peripheral benzodiazepine receptor. J Pharmacol Exp Ther. 1992 Jul;262(1):394-7. [PubMed:1320691]
  2. Papadopoulos V, Berkovich A, Krueger KE, Costa E, Guidotti A: Diazepam binding inhibitor and its processing products stimulate mitochondrial steroid biosynthesis via an interaction with mitochondrial benzodiazepine receptors. Endocrinology. 1991 Sep;129(3):1481-8. [PubMed:1651852]
  3. Papadopoulos V, Nowzari FB, Krueger KE: Hormone-stimulated steroidogenesis is coupled to mitochondrial benzodiazepine receptors. Tropic hormone action on steroid biosynthesis is inhibited by flunitrazepam. J Biol Chem. 1991 Feb 25;266(6):3682-7. [PubMed:1847384]
  4. Awad M, Gavish M: Solubilization of peripheral-type benzodiazepine binding sites from cat cerebral cortex. J Neurochem. 1989 Jun;52(6):1880-5. [PubMed:2723642]
  5. Gandolfo P, Patte C, Leprince J, Thoumas JL, Vaudry H, Tonon MC: The stimulatory effect of the octadecaneuropeptide (ODN) on cytosolic Ca2+ in rat astrocytes is not mediated through classical benzodiazepine receptors. Eur J Pharmacol. 1997 Mar 19;322(2-3):275-81. [PubMed:9098698]
  6. Poisnel G, Dhilly M, Le Boisselier R, Barre L, Debruyne D: Comparison of five benzodiazepine-receptor agonists on buprenorphine-induced mu-opioid receptor regulation. J Pharmacol Sci. 2009 May;110(1):36-46. [PubMed:19443999]
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. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
  3. Oelschlager H: [Chemical and pharmacologic aspects of benzodiazepines]. Schweiz Rundsch Med Prax. 1989 Jul 4;78(27-28):766-72. [PubMed:2570451]
  4. Oblak AL, Gibbs TT, Blatt GJ: Reduced GABAA receptors and benzodiazepine binding sites in the posterior cingulate cortex and fusiform gyrus in autism. Brain Res. 2011 Mar 22;1380:218-28. doi: 10.1016/j.brainres.2010.09.021. Epub 2010 Sep 19. [PubMed:20858465]
  5. You H, Kozuska JL, Paulsen IM, Dunn SM: Benzodiazepine modulation of the rat GABAA receptor alpha4beta3gamma2L subtype expressed in Xenopus oocytes. Neuropharmacology. 2010 Nov;59(6):527-33. doi: 10.1016/j.neuropharm.2010.07.011. Epub 2010 Jul 16. [PubMed:20638393]
  6. Skilbeck KJ, O'Reilly JN, Johnston GA, Hinton T: Antipsychotic drug administration differentially affects [3H]muscimol and [3H]flunitrazepam GABA(A) receptor binding sites. Prog Neuropsychopharmacol Biol Psychiatry. 2008 Feb 15;32(2):492-8. Epub 2007 Oct 10. [PubMed:17976880]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Agonist
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. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
  3. Oblak AL, Gibbs TT, Blatt GJ: Reduced GABAA receptors and benzodiazepine binding sites in the posterior cingulate cortex and fusiform gyrus in autism. Brain Res. 2011 Mar 22;1380:218-28. doi: 10.1016/j.brainres.2010.09.021. Epub 2010 Sep 19. [PubMed:20858465]
  4. You H, Kozuska JL, Paulsen IM, Dunn SM: Benzodiazepine modulation of the rat GABAA receptor alpha4beta3gamma2L subtype expressed in Xenopus oocytes. Neuropharmacology. 2010 Nov;59(6):527-33. doi: 10.1016/j.neuropharm.2010.07.011. Epub 2010 Jul 16. [PubMed:20638393]
  5. Skilbeck KJ, O'Reilly JN, Johnston GA, Hinton T: Antipsychotic drug administration differentially affects [3H]muscimol and [3H]flunitrazepam GABA(A) receptor binding sites. Prog Neuropsychopharmacol Biol Psychiatry. 2008 Feb 15;32(2):492-8. Epub 2007 Oct 10. [PubMed:17976880]
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. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
  3. Oblak AL, Gibbs TT, Blatt GJ: Reduced GABAA receptors and benzodiazepine binding sites in the posterior cingulate cortex and fusiform gyrus in autism. Brain Res. 2011 Mar 22;1380:218-28. doi: 10.1016/j.brainres.2010.09.021. Epub 2010 Sep 19. [PubMed:20858465]
  4. You H, Kozuska JL, Paulsen IM, Dunn SM: Benzodiazepine modulation of the rat GABAA receptor alpha4beta3gamma2L subtype expressed in Xenopus oocytes. Neuropharmacology. 2010 Nov;59(6):527-33. doi: 10.1016/j.neuropharm.2010.07.011. Epub 2010 Jul 16. [PubMed:20638393]
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. Santhakumar V, Hanchar HJ, Wallner M, Olsen RW, Otis TS: Contributions of the GABAA receptor alpha6 subunit to phasic and tonic inhibition revealed by a naturally occurring polymorphism in the alpha6 gene. J Neurosci. 2006 Mar 22;26(12):3357-64. [PubMed:16554486]
  2. You H, Kozuska JL, Paulsen IM, Dunn SM: Benzodiazepine modulation of the rat GABAA receptor alpha4beta3gamma2L subtype expressed in Xenopus oocytes. Neuropharmacology. 2010 Nov;59(6):527-33. doi: 10.1016/j.neuropharm.2010.07.011. Epub 2010 Jul 16. [PubMed:20638393]
  3. Skilbeck KJ, O'Reilly JN, Johnston GA, Hinton T: Antipsychotic drug administration differentially affects [3H]muscimol and [3H]flunitrazepam GABA(A) receptor binding sites. Prog Neuropsychopharmacol Biol Psychiatry. 2008 Feb 15;32(2):492-8. Epub 2007 Oct 10. [PubMed:17976880]
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. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
  3. You H, Kozuska JL, Paulsen IM, Dunn SM: Benzodiazepine modulation of the rat GABAA receptor alpha4beta3gamma2L subtype expressed in Xenopus oocytes. Neuropharmacology. 2010 Nov;59(6):527-33. doi: 10.1016/j.neuropharm.2010.07.011. Epub 2010 Jul 16. [PubMed:20638393]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Agonist
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. Hadingham KL, Garrett EM, Wafford KA, Bain C, Heavens RP, Sirinathsinghji DJ, Whiting PJ: Cloning of cDNAs encoding the human gamma-aminobutyric acid type A receptor alpha 6 subunit and characterization of the pharmacology of alpha 6-containing receptors. Mol Pharmacol. 1996 Feb;49(2):253-9. [PubMed:8632757]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Agonist
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. Hadingham KL, Garrett EM, Wafford KA, Bain C, Heavens RP, Sirinathsinghji DJ, Whiting PJ: Cloning of cDNAs encoding the human gamma-aminobutyric acid type A receptor alpha 6 subunit and characterization of the pharmacology of alpha 6-containing receptors. Mol Pharmacol. 1996 Feb;49(2):253-9. [PubMed:8632757]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Agonist
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. Hadingham KL, Garrett EM, Wafford KA, Bain C, Heavens RP, Sirinathsinghji DJ, Whiting PJ: Cloning of cDNAs encoding the human gamma-aminobutyric acid type A receptor alpha 6 subunit and characterization of the pharmacology of alpha 6-containing receptors. Mol Pharmacol. 1996 Feb;49(2):253-9. [PubMed:8632757]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
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. 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
Glucuronosyltransferase activity
Specific Function
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds.Its unique specificity for 3,4-catechol estrogens and estriol su...
Gene Name
UGT2B7
Uniprot ID
P16662
Uniprot Name
UDP-glucuronosyltransferase 2B7
Molecular Weight
60694.12 Da
References
  1. Thomassin J, Tephly TR: Photoaffinity labeling of rat liver microsomal morphine UDP-glucuronosyltransferase by [3H]flunitrazepam. Mol Pharmacol. 1990 Sep;38(3):294-8. [PubMed:2119476]
  2. Cheng Z, Rios GR, King CD, Coffman BL, Green MD, Mojarrabi B, Mackenzie PI, Tephly TR: Glucuronidation of catechol estrogens by expressed human UDP-glucuronosyltransferases (UGTs) 1A1, 1A3, and 2B7. Toxicol Sci. 1998 Sep;45(1):52-7. [PubMed:9848110]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
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]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Exhibits a high coumarin 7-hydroxylase activity. Can act in the hydroxylation of the anti-cancer drugs cyclophosphamide and ifosphamide. Competent in the metabolic activation of aflatoxin B1. Const...
Gene Name
CYP2A6
Uniprot ID
P11509
Uniprot Name
Cytochrome P450 2A6
Molecular Weight
56501.005 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
CYP2B6
Uniprot ID
P20813
Uniprot Name
Cytochrome P450 2B6
Molecular Weight
56277.81 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
CYP2C9
Uniprot ID
P11712
Uniprot Name
Cytochrome P450 2C9
Molecular Weight
55627.365 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
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]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Steroid binding
Specific Function
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform glucuronidates bilirubin IX-alpha to form both the...
Gene Name
UGT1A1
Uniprot ID
P22309
Uniprot Name
UDP-glucuronosyltransferase 1-1
Molecular Weight
59590.91 Da
References
  1. Cheng Z, Rios GR, King CD, Coffman BL, Green MD, Mojarrabi B, Mackenzie PI, Tephly TR: Glucuronidation of catechol estrogens by expressed human UDP-glucuronosyltransferases (UGTs) 1A1, 1A3, and 2B7. Toxicol Sci. 1998 Sep;45(1):52-7. [PubMed:9848110]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Retinoic acid binding
Specific Function
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. Isoform 2 lacks transferase activity but acts as a negative reg...
Gene Name
UGT1A3
Uniprot ID
P35503
Uniprot Name
UDP-glucuronosyltransferase 1-3
Molecular Weight
60337.835 Da
References
  1. Cheng Z, Rios GR, King CD, Coffman BL, Green MD, Mojarrabi B, Mackenzie PI, Tephly TR: Glucuronidation of catechol estrogens by expressed human UDP-glucuronosyltransferases (UGTs) 1A1, 1A3, and 2B7. Toxicol Sci. 1998 Sep;45(1):52-7. [PubMed:9848110]

Drug created on July 31, 2007 07:10 / Updated on October 02, 2017 05:00