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flunitrazepam 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
diazepam derivatives	1202	1622-62-4

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: flunitrazepam flunidazepam fluridrazepam flunipam	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. Molecular weight: 313.29 Formula: C16H12FN3O3 CLOGP: 1.78 LIPINSKI: 0 HAC: 6 HDO: 0 TPSA: 78.49 ALOGS: -4.56 ROTB: 2

Molecule

Description

Molfile Inchi Smiles

Synonyms:

flunitrazepam
flunidazepam
fluridrazepam
flunipam

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.

Molecular weight: 313.29
Formula: C16H12FN3O3
CLOGP: 1.78
LIPINSKI: 0
HAC: 6
HDO: 0
TPSA: 78.49
ALOGS: -4.56
ROTB: 2

Drug dosage:

Dose	Unit	Route
1	mg	O
1	mg	P

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	80 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
t_half (Half-life)	25 hours	Lombardo F, Berellini G, Obach RS
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
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	0.50 %	Benet LZ, Broccatelli F, Oprea TI
fu (Fraction unbound in plasma)	0.17 %	Lombardo F, Berellini G, Obach RS
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.11 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
S (Water solubility)	0.00 mg/mL	Benet LZ, Broccatelli F, Oprea TI

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Approvals:

Date	Agency	Company	Orphan
Jan. 1, 1976	YEAR INTRODUCED

FDA Adverse Event Reporting System (Female)

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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
Intentional overdose	141.30	26.21	75	3770	74077	63411100
Neuroleptic malignant syndrome	125.09	26.21	41	3804	12015	63473162
Altered state of consciousness	112.40	26.21	46	3799	25184	63459993
Overdose	103.65	26.21	72	3773	115006	63370171
Suicide attempt	97.64	26.21	55	3790	60863	63424314
Salivary hypersecretion	87.35	26.21	28	3817	7638	63477539
Hepatic function abnormal	71.84	26.21	38	3807	37104	63448073
Psychiatric symptom	63.30	26.21	20	3825	5203	63479974
Extrapyramidal disorder	61.79	26.21	25	3820	13259	63471918
Toxicity to various agents	53.32	26.21	70	3775	247180	63237997

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FDA Adverse Event Reporting System (Male)

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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
Neuroleptic malignant syndrome	123.55	20.45	54	4057	17880	34934940
Hepatic function abnormal	77.71	20.45	54	4057	44309	34908511
Altered state of consciousness	76.27	20.45	42	4069	22851	34929969
Pneumonia aspiration	71.03	20.45	50	4061	41853	34910967
Rhabdomyolysis	69.12	20.45	60	4051	68103	34884717
Salivary hypersecretion	56.15	20.45	25	4086	8619	34944201
Asphyxia	55.00	20.45	23	4088	6812	34946008
Blood creatine phosphokinase increased	52.67	20.45	43	4068	44814	34908006
Water intoxication	42.98	20.45	10	4101	418	34952402
Overdose	42.69	20.45	53	4058	91006	34861814

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FDA Adverse Event Reporting System (Geriatric)

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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
Neuroleptic malignant syndrome	238.86	20.56	93	7765	27466	79709064
Altered state of consciousness	170.03	20.56	84	7774	43738	79692792
Hepatic function abnormal	142.38	20.56	89	7769	73018	79663512
Salivary hypersecretion	141.10	20.56	53	7805	14171	79722359
Intentional overdose	127.89	20.56	96	7762	105864	79630666
Pneumonia aspiration	114.19	20.56	75	7783	66892	79669638
Suicide attempt	104.19	20.56	77	7781	82855	79653675
Overdose	103.27	20.56	108	7750	184098	79552432
Psychiatric symptom	95.24	20.56	33	7825	7002	79729528
Blood creatine phosphokinase increased	93.59	20.56	66	7792	66024	79670506

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FDA Adverse Event Reporting System (Pediatric)

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Pharmacologic Action:

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Source	Code	Description
ATC	N05CD03	NERVOUS SYSTEM PSYCHOLEPTICS HYPNOTICS AND SEDATIVES Benzodiazepine derivatives
CHEBI has role	CHEBI:35474	anti-anxiety agents
CHEBI has role	CHEBI:35717	hypnotics
CHEBI has role	CHEBI:91016	GABAA receptor agonists
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

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Drug Use | Suggest Off label Use Form| |View source of the data|

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🐶 Veterinary Drug Use

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🐶 Veterinary products

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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)

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Orange Book exclusivity data (new drug applications)

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Gamma-aminobutyric acid receptor subunit alpha-1	Ion channel	P14867	GBRA1_HUMAN	ALLOSTERIC MODULATOR	Ki	8.28	IUPHAR	IUPHAR
Gamma-aminobutyric acid receptor subunit alpha-2	Ion channel	P47869	GBRA2_HUMAN	ALLOSTERIC MODULATOR	Ki	8.28	IUPHAR	IUPHAR
Gamma-aminobutyric acid receptor subunit alpha-3	Ion channel	P34903	GBRA3_HUMAN	ALLOSTERIC MODULATOR	Ki	7.80	IUPHAR	IUPHAR
Gamma-aminobutyric acid receptor subunit alpha-5	Ion channel	P31644	GBRA5_HUMAN	ALLOSTERIC MODULATOR	Ki	8.26	IUPHAR	IUPHAR
GABA-A receptor alpha-1/beta-2/gamma-2	Ion channel	P14867 P18507 P47870	GBRA1_HUMAN GBRG2_HUMAN GBRB2_HUMAN		Ki	8.70	WOMBAT-PK
GABA-A receptor alpha-2/beta-3/gamma-2	Ion channel	P18507 P28472 P47869	GBRG2_HUMAN GBRB3_HUMAN GBRA2_HUMAN		Ki	8.70	WOMBAT-PK
GABA-A receptor alpha-3/beta-3/gamma-2	Ion channel	P18507 P28472 P34903	GBRG2_HUMAN GBRB3_HUMAN GBRA3_HUMAN		Ki	8.35	WOMBAT-PK
GABA-A receptor alpha-5/beta-3/gamma-2	Ion channel	P18507 P28472 P31644	GBRG2_HUMAN GBRB3_HUMAN GBRA5_HUMAN		Ki	8.84	WOMBAT-PK
GABA-A receptor alpha-1/beta-2/gamma-3	Ion channel	P14867 P47870 Q99928	GBRA1_HUMAN GBRB2_HUMAN GBRG3_HUMAN		Ki	7.46	WOMBAT-PK
GABA-A receptor alpha-1/beta-3/gamma-2	Ion channel	P14867 P18507 P28472	GBRA1_HUMAN GBRG2_HUMAN GBRB3_HUMAN		Ki	8.47	WOMBAT-PK

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External reference:

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ID	Source
004091	NDDF
2951	INN_ID
3380	PUBCHEM_CID
387573007	SNOMEDCT_US
4193	IUPHAR_LIGAND_ID
4460	RXNORM
620X0222FQ	UNII
96237009	SNOMEDCT_US
C0016296	UMLSCUI
CHEBI:31622	CHEBI

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Pharmaceutical products:

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