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flurazepam 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| diazepam derivatives | 1218 | 17617-23-1 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A benzodiazepine derivative used mainly as a hypnotic.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 30 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 500 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 0.10 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 1.10 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 83 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | EIF2AK3,GRK2,PDK1,PDK2,PDK4 | 5 | |||
| kinase-selectivity-class | PDK4 | 1 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| April 7, 1970 | FDA |
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 |
|---|---|---|---|---|---|---|
| Sopor | 762.65 | 42.56 | 171 | 2601 | 24473 | 90601202 |
| Drug abuse | 502.91 | 42.56 | 158 | 2614 | 82189 | 90543486 |
| Intentional self-injury | 290.34 | 42.56 | 82 | 2690 | 29252 | 90596423 |
| Intentional overdose | 252.53 | 42.56 | 98 | 2674 | 93736 | 90531939 |
| Suicide attempt | 243.49 | 42.56 | 90 | 2682 | 75309 | 90550366 |
| Toxicity to various agents | 148.41 | 42.56 | 98 | 2674 | 287748 | 90337927 |
| Bradyphrenia | 125.96 | 42.56 | 32 | 2740 | 7580 | 90618095 |
| Somnolence | 88.10 | 42.56 | 63 | 2709 | 209021 | 90416654 |
| Substance abuse | 76.15 | 42.56 | 20 | 2752 | 5386 | 90620289 |
| Coma | 69.51 | 42.56 | 37 | 2735 | 72595 | 90553080 |
| Mydriasis | 67.57 | 42.56 | 23 | 2749 | 14989 | 90610686 |
| Drug interaction | 60.65 | 42.56 | 57 | 2715 | 276396 | 90349279 |
| Hypokinesia | 51.43 | 42.56 | 19 | 2753 | 15678 | 90609997 |
| Altered state of consciousness | 51.00 | 42.56 | 23 | 2749 | 31509 | 90594166 |
| Sedation | 44.54 | 42.56 | 24 | 2748 | 48147 | 90577528 |
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 |
|---|---|---|---|---|---|---|
| Drug abuse | 216.73 | 34.95 | 95 | 1461 | 104676 | 42515103 |
| Sopor | 155.72 | 34.95 | 44 | 1512 | 13158 | 42606621 |
| Intentional self-injury | 149.58 | 34.95 | 44 | 1512 | 15158 | 42604621 |
| Psychomotor hyperactivity | 62.71 | 34.95 | 21 | 1535 | 10937 | 42608842 |
| Suicide attempt | 55.48 | 34.95 | 29 | 1527 | 46071 | 42573708 |
| Feelings of worthlessness | 50.75 | 34.95 | 9 | 1547 | 315 | 42619464 |
| Coma | 48.70 | 34.95 | 28 | 1528 | 53526 | 42566253 |
| Toxicity to various agents | 48.33 | 34.95 | 50 | 1506 | 229086 | 42390693 |
| Abulia | 43.96 | 34.95 | 9 | 1547 | 681 | 42619098 |
| Obsessive-compulsive disorder | 38.87 | 34.95 | 13 | 1543 | 6730 | 42613049 |
| Restless legs syndrome | 38.02 | 34.95 | 14 | 1542 | 9600 | 42610179 |
FDA Adverse Event Reporting System (Geriatric)
| 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 |
|---|---|---|---|---|---|---|
| Sopor | 855.52 | 35.24 | 211 | 3994 | 36335 | 110548759 |
| Drug abuse | 659.73 | 35.24 | 248 | 3957 | 177163 | 110407931 |
| Intentional self-injury | 442.19 | 35.24 | 126 | 4079 | 37303 | 110547791 |
| Suicide attempt | 228.66 | 35.24 | 100 | 4105 | 103294 | 110481800 |
| Intentional overdose | 220.11 | 35.24 | 105 | 4100 | 132396 | 110452698 |
| Toxicity to various agents | 171.37 | 35.24 | 143 | 4062 | 480412 | 110104682 |
| Bradyphrenia | 154.12 | 35.24 | 43 | 4162 | 11685 | 110573409 |
| Coma | 95.33 | 35.24 | 58 | 4147 | 117811 | 110467283 |
| Drug interaction | 69.52 | 35.24 | 90 | 4115 | 500093 | 110085001 |
| Somnolence | 63.87 | 35.24 | 67 | 4138 | 297382 | 110287712 |
| Hypokinesia | 57.64 | 35.24 | 24 | 4181 | 21802 | 110563292 |
| Substance abuse | 55.37 | 35.24 | 20 | 4185 | 12443 | 110572651 |
| Mydriasis | 53.96 | 35.24 | 23 | 4182 | 22134 | 110562960 |
| Psychomotor hyperactivity | 52.55 | 35.24 | 22 | 4183 | 20255 | 110564839 |
| Altered state of consciousness | 45.61 | 35.24 | 28 | 4177 | 57598 | 110527496 |
| Feelings of worthlessness | 44.98 | 35.24 | 9 | 4196 | 581 | 110584513 |
| Hypotension | 39.47 | 35.24 | 71 | 4134 | 523778 | 110061316 |
| Bradykinesia | 39.42 | 35.24 | 15 | 4190 | 10773 | 110574321 |
| Abulia | 37.81 | 35.24 | 9 | 4196 | 1304 | 110583790 |
| Obsessive-compulsive disorder | 37.41 | 35.24 | 13 | 4192 | 7228 | 110577866 |
| Overdose | 37.03 | 35.24 | 45 | 4160 | 233749 | 110351345 |
| Muscle rigidity | 36.60 | 35.24 | 18 | 4187 | 24013 | 110561081 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | N05CD01 | NERVOUS SYSTEM PSYCHOLEPTICS HYPNOTICS AND SEDATIVES Benzodiazepine derivatives |
| FDA CS | M0002356 | Benzodiazepines |
| MeSH PA | D002492 | Central Nervous System Depressants |
| MeSH PA | D006993 | Hypnotics and Sedatives |
| MeSH PA | D011619 | Psychotropic Drugs |
| MeSH PA | D014151 | Anti-Anxiety Agents |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018682 | GABA Agents |
| MeSH PA | D018757 | GABA Modulators |
| CHEBI has role | CHEBI:35469 | antidepressant |
| CHEBI has role | CHEBI:35474 | anxiolytic drug |
| CHEBI has role | CHEBI:35476 | antipsychotic agent |
| CHEBI has role | CHEBI:35623 | anticonvulsant |
| CHEBI has role | CHEBI:35717 | sedative |
| CHEBI has role | CHEBI:91016 | GABA<small><sub>A</sub></small> receptor agonist |
| FDA EPC | N0000175694 | Benzodiazepine |
Related Drugs by ATC class:
N05CD Benzodiazepine derivatives 14 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Insomnia | indication | 193462001 | |
| Suicidal thoughts | contraindication | 6471006 | |
| Disorder of lung | contraindication | 19829001 | DOID:850 |
| Borderline personality disorder | contraindication | 20010003 | DOID:10930 |
| Alcohol intoxication | contraindication | 25702006 | |
| Shock | contraindication | 27942005 | |
| Depressive disorder | contraindication | 35489007 | |
| Substance abuse | contraindication | 66214007 | |
| Psychotic disorder | contraindication | 69322001 | |
| Sleep apnea | contraindication | 73430006 | DOID:0050847 |
| Decreased respiratory function | contraindication | 80954004 | |
| Kidney disease | contraindication | 90708001 | DOID:557 |
| Hypoalbuminemia | contraindication | 119247004 | |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Sleep automatism | contraindication | 247962006 | |
| Pregnancy, function | contraindication | 289908002 | |
| Coma | contraindication | 371632003 | |
| Breastfeeding (mother) | contraindication | 413712001 | |
| Porphyria | contraindication | 418470004 | |
| Behavioral Disorders | contraindication |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 8.24 | Basic |
| pKa2 | 1.92 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| GABA-A receptor alpha-1/beta-2/gamma-2 | Ion channel | POSITIVE ALLOSTERIC MODULATOR | IC50 | 8.10 | WOMBAT-PK | CHEMBL | |||
| Solute carrier family 22 member 2 | Transporter | IC50 | 4.22 | WOMBAT-PK |
External reference:
| ID | Source |
|---|---|
| 4019763 | VUID |
| N0000147854 | NUI |
| D00329 | KEGG_DRUG |
| 1172-18-5 | SECONDARY_CAS_RN |
| 4017827 | VANDF |
| 4019763 | VANDF |
| C0016375 | UMLSCUI |
| CHEBI:5128 | CHEBI |
| FL7 | PDB_CHEM_ID |
| CHEMBL3989724 | ChEMBL_ID |
| CHEMBL968 | ChEMBL_ID |
| DB00690 | DRUGBANK_ID |
| D005479 | MESH_DESCRIPTOR_UI |
| 3393 | PUBCHEM_CID |
| 7188 | IUPHAR_LIGAND_ID |
| 2551 | INN_ID |
| IHP475989U | UNII |
| 4501 | RXNORM |
| 4752 | MMSL |
| 70 | MMSL |
| d00238 | MMSL |
| 001463 | NDDF |
| 004584 | NDDF |
| 19403009 | SNOMEDCT_US |
| 27928002 | SNOMEDCT_US |
| 387109000 | SNOMEDCT_US |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Flurazepam | HUMAN PRESCRIPTION DRUG LABEL | 1 | 21695-363 | CAPSULE | 30 mg | ORAL | ANDA | 19 sections |
| Flurazepam | HUMAN PRESCRIPTION DRUG LABEL | 1 | 52959-236 | CAPSULE | 30 mg | ORAL | ANDA | 19 sections |
| Flurazepam Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 54868-0092 | CAPSULE | 15 mg | ORAL | ANDA | 14 sections |
| Flurazepam Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 54868-0093 | CAPSULE | 30 mg | ORAL | ANDA | 14 sections |
| Flurazepam Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 62135-736 | CAPSULE | 15 mg | ORAL | ANDA | 20 sections |
| Flurazepam Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 62135-737 | CAPSULE | 30 mg | ORAL | ANDA | 20 sections |