flunitrazepam Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| diazepam derivatives | 1202 | 1622-62-4 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
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.
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 1 | mg | O |
| 1 | mg | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 0.00 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 0.50 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 0.11 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 80 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 1.90 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 1.40 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.17 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 25 hours | Lombardo F, Berellini G, Obach RS |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 1, 1976 | YEAR INTRODUCED |
FDA Adverse Event Reporting System (Female)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Overdose | 171.40 | 118.67 | 41 | 179 | 19866 | 2337999 |
| Intentional overdose | 154.30 | 118.67 | 34 | 186 | 11287 | 2346578 |
FDA Adverse Event Reporting System (Male)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Toxicity to various agents | 135.25 | 76.80 | 41 | 180 | 29100 | 1717460 |
| Overdose | 105.39 | 76.80 | 30 | 191 | 16671 | 1729889 |
| Rhabdomyolysis | 102.79 | 76.80 | 27 | 194 | 11063 | 1735497 |
| Neuroleptic malignant syndrome | 100.71 | 76.80 | 21 | 200 | 3127 | 1743433 |
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | N05CD03 | NERVOUS SYSTEM PSYCHOLEPTICS HYPNOTICS AND SEDATIVES Benzodiazepine derivatives |
| CHEBI has role | CHEBI:35717 | sedative |
| CHEBI has role | CHEBI:91016 | GABAA receptor agonist |
| CHEBI has role | CHEBI:35474 | anxiolytic drug |
| MeSH PA | D014151 | Anti-Anxiety Agents |
| MeSH PA | D002491 | Central Nervous System Agents |
| MeSH PA | D002492 | Central Nervous System Depressants |
| MeSH PA | D018682 | GABA Agents |
| MeSH PA | D018757 | GABA Modulators |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D011619 | Psychotropic Drugs |
| MeSH PA | D014149 | Tranquilizing Agents |
Drug Use (View source of the data)
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 1.89 | Basic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Gamma-aminobutyric acid receptor subunit alpha-3 | Ion channel | ALLOSTERIC MODULATOR | Ki | 7.80 | IUPHAR | IUPHAR | |||
| Gamma-aminobutyric acid receptor subunit alpha-5 | Ion channel | ALLOSTERIC MODULATOR | Ki | 8.26 | IUPHAR | IUPHAR | |||
| Gamma-aminobutyric acid receptor subunit alpha-1 | Ion channel | ALLOSTERIC MODULATOR | Ki | 8.28 | IUPHAR | IUPHAR | |||
| Gamma-aminobutyric acid receptor subunit alpha-2 | Ion channel | ALLOSTERIC MODULATOR | Ki | 8.28 | IUPHAR | IUPHAR | |||
| GABA-A receptor alpha-2/beta-3/gamma-2 | Ion channel | Ki | 8.70 | WOMBAT-PK | |||||
| GABA A receptor alpha-3/beta-2/gamma-2 | Ion channel | Ki | 8.82 | WOMBAT-PK | |||||
| GABA-A receptor alpha-3/beta-3/gamma-2 | Ion channel | Ki | 8.35 | WOMBAT-PK | |||||
| GABA A receptor alpha-3/beta-2/gamma-3 | Ion channel | Ki | 7.50 | WOMBAT-PK | |||||
| GABA A receptor alpha-5/beta-2/gamma-2 | Ion channel | Ki | 9 | WOMBAT-PK | |||||
| GABA A receptor alpha-5/beta-2/gamma-3 | Ion channel | Ki | 8.42 | WOMBAT-PK | |||||
| GABA A receptor alpha-5/beta-3/gamma-3 | Ion channel | Ki | 8.42 | WOMBAT-PK | |||||
| GABA-A receptor alpha-1/beta-2/gamma-3 | Ion channel | Ki | 7.46 | WOMBAT-PK | |||||
| GABA-A receptor alpha-1/beta-3/gamma-2 | Ion channel | Ki | 8.47 | WOMBAT-PK | |||||
| GABA-A receptor alpha-5/beta-3/gamma-2 | Ion channel | Ki | 8.84 | WOMBAT-PK | |||||
| GABA-A receptor alpha-1/beta-2/gamma-2 | Ion channel | Ki | 8.70 | WOMBAT-PK | |||||
| GABA-A receptor; anion channel | Ion channel | IC50 | 8.82 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D005445 | MESH_DESCRIPTOR_UI |
| N0000166924 | NUI |
| C0016296 | UMLSCUI |
| D01230 | KEGG_DRUG |
| 620X0222FQ | UNII |
| 2951 | INN_ID |
| 96237009 | SNOMEDCT_US |
| 4460 | RXNORM |
| 387573007 | SNOMEDCT_US |
| 004091 | NDDF |
| CHEMBL13280 | ChEMBL_ID |
| DB01544 | DRUGBANK_ID |
| CHEBI:31622 | CHEBI |
| 3380 | PUBCHEM_CID |
| 4193 | IUPHAR_LIGAND_ID |
Pharmaceutical products:
None