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

Stem definition	Drug id	CAS RN
diazepam derivatives	703	1622-61-3

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: clonazepam lonazep klonopin	An anticonvulsant used for several types of seizures, including myotonic or atonic seizures, photosensitive epilepsy, and absence seizures, although tolerance may develop. It is seldom effective in generalized tonic-clonic or partial seizures. The mechanism of action appears to involve the enhancement of GAMMA-AMINOBUTYRIC ACID receptor responses. Molecular weight: 315.71 Formula: C15H10ClN3O3 CLOGP: 2.38 LIPINSKI: 0 HAC: 6 HDO: 1 TPSA: 87.28 ALOGS: -4.47 ROTB: 2 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

clonazepam
lonazep
klonopin

An anticonvulsant used for several types of seizures, including myotonic or atonic seizures, photosensitive epilepsy, and absence seizures, although tolerance may develop. It is seldom effective in generalized tonic-clonic or partial seizures. The mechanism of action appears to involve the enhancement of GAMMA-AMINOBUTYRIC ACID receptor responses.

Molecular weight: 315.71
Formula: C15H10ClN3O3
CLOGP: 2.38
LIPINSKI: 0
HAC: 6
HDO: 1
TPSA: 87.28
ALOGS: -4.47
ROTB: 2

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
8	mg	O
8	mg	P

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	98 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
t_half (Half-life)	38 hours	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	2.90 L/kg	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
CL (Clearance)	0.88 mL/min/kg	Lombardo F, Berellini G, Obach RS
EoM (Fraction excreted unchanged in urine)	0.50 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.42 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
fu (Fraction unbound in plasma)	0.15 %	Lombardo F, Berellini G, Obach RS
S (Water solubility)	0.10 mg/mL	Benet LZ, Broccatelli F, Oprea TI

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Approvals:

Date	Agency	Company	Orphan
June 4, 1975	FDA	ROCHE

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
Completed suicide	2406.03	10.16	2674	206929	142999	63136420
Toxicity to various agents	930.38	10.16	2325	207278	244925	63034494
Suicide attempt	771.40	10.16	978	208625	59940	63219479
Drug abuse	593.09	10.16	945	208658	71573	63207846
Contraindicated product administered	578.90	10.16	35	209568	217613	63061806
Synovitis	543.52	10.16	16	209587	186902	63092517
Intentional overdose	534.63	10.16	913	208690	73239	63206180
Suicidal ideation	504.29	10.16	809	208794	61612	63217807
Systemic lupus erythematosus	467.43	10.16	67	209536	208851	63070568
Somnolence	464.86	10.16	1471	208132	177214	63102205

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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
Drug abuse	1467.64	10.72	1691	109963	97405	34747872
Depression	977.42	10.72	1368	110286	95730	34749547
Completed suicide	875.33	10.72	1306	110348	96862	34748415
Toxicity to various agents	696.02	10.72	1789	109865	198573	34646704
Drug interaction	440.04	10.72	1650	110004	224296	34620981
Somnolence	434.06	10.72	1039	110615	110077	34735200
Coma	365.83	10.72	579	111075	45099	34800178
Sopor	363.25	10.72	305	111349	11831	34833446
Overdose	361.40	10.72	857	110797	90202	34755075
Suicidal ideation	311.10	10.72	503	111151	39885	34805392

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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
Completed suicide	3442.21	9.80	4114	255614	241653	79243007
Drug abuse	1906.51	9.80	2494	257234	160197	79324463
Toxicity to various agents	1629.25	9.80	3968	255760	417572	79067088
Respiratory arrest	836.30	9.80	984	258744	56566	79428094
Depression	827.51	9.80	2034	257694	214756	79269904
Suicide attempt	822.69	9.80	1174	258554	81758	79402902
Intentional overdose	797.75	9.80	1320	258408	104640	79380020
Somnolence	717.69	9.80	2051	257677	236930	79247730
Sopor	697.21	9.80	688	259040	32322	79452338
Cardio-respiratory arrest	653.86	9.80	1226	258502	107284	79377376

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FDA Adverse Event Reporting System (Pediatric)

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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
Tricuspid valve incompetence	33.98	29.35	12	321	61	89398

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Pharmacologic Action:

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Source	Code	Description
ATC	N03AE01	NERVOUS SYSTEM ANTIEPILEPTICS ANTIEPILEPTICS Benzodiazepine derivatives
CHEBI has role	CHEBI:35474	anti-anxiety agents
CHEBI has role	CHEBI:35623	anticonvulsants
CHEBI has role	CHEBI:50268	GABA modulators
FDA CS	M0002356	Benzodiazepines
FDA EPC	N0000175694	Benzodiazepine
MeSH PA	D000927	Anticonvulsants
MeSH PA	D002491	Central Nervous System Agents
MeSH PA	D018682	GABA Agents
MeSH PA	D018757	GABA Modulators

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

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Disease	Relation	SNOMED_ID	DOID
Myoclonic seizure	indication	37356005
Atonic seizure	indication	42365007
Absence seizure	indication	79631006
Lennox-Gastaut syndrome	indication	230418006
Panic disorder	indication	371631005	DOID:594
Akathisia	off-label use	285145004
Manic Bipolar Disorder Adjunct Treatment	off-label use
Suicidal thoughts	contraindication	6471006
Alcohol intoxication	contraindication	25702006
Depressive disorder	contraindication	35489007

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	10.65	acidic
pKa2	1.65	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
GABA-A receptor alpha-1/beta-2/gamma-2	Ion channel	P14867 P18507 P47870	GBRA1_HUMAN GBRG2_HUMAN GBRB2_HUMAN	POSITIVE ALLOSTERIC MODULATOR	Ki	8.07	WOMBAT-PK	CHEMBL
GABA-A receptor; anion channel	Ion channel	O00591 O14764 P14867 P18505 P18507 P28472 P31644 P34903 P47869 P47870 P48169 P78334 Q16445 Q8N1C3 Q99928 Q9UN88	GBRP_HUMAN GBRD_HUMAN GBRA1_HUMAN GBRB1_HUMAN GBRG2_HUMAN GBRB3_HUMAN GBRA5_HUMAN GBRA3_HUMAN GBRA2_HUMAN GBRB2_HUMAN GBRA4_HUMAN GBRE_HUMAN GBRA6_HUMAN GBRG1_HUMAN GBRG3_HUMAN GBRT_HUMAN		Ki	9.07	CHEMBL
GABA-A receptor; anion channel	Ion channel		GBRP_RAT GBRB1_RAT GBRD_RAT GBRG2_RAT GBRA5_RAT GBRA3_RAT GBRG1_RAT GBRA2_RAT GBRA4_RAT GBRG3_RAT GBRA6_RAT GBRA1_RAT GBRB3_RAT GBRB2_RAT Q91ZM7_RAT GBRE_RAT		IC50	8.77	CHEMBL
GABA-A receptor; anion channel	Ion channel		GBRA1_BOVIN GBRB1_BOVIN GBRA2_BOVIN GBRA3_BOVIN GBRA4_BOVIN GBRG2_BOVIN		Ki	9.07	CHEMBL

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External reference:

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ID	Source
001635	NDDF
1345	MMSL
202585	RXNORM
2765	INN_ID
2802	PUBCHEM_CID
377	MMSL
387383007	SNOMEDCT_US
4017791	VUID
4017791	VANDF
4477	MMSL

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Clonazepam	HUMAN PRESCRIPTION DRUG LABEL	1	0093-0832	TABLET	0.50 mg	ORAL	ANDA	20 sections
Clonazepam	HUMAN PRESCRIPTION DRUG LABEL	1	0093-0832	TABLET	0.50 mg	ORAL	ANDA	20 sections
Clonazepam	HUMAN PRESCRIPTION DRUG LABEL	1	0093-0832	TABLET	0.50 mg	ORAL	ANDA	20 sections
Clonazepam	HUMAN PRESCRIPTION DRUG LABEL	1	0093-3212	TABLET	1 mg	ORAL	ANDA	20 sections
Clonazepam	HUMAN PRESCRIPTION DRUG LABEL	1	0093-3212	TABLET	1 mg	ORAL	ANDA	20 sections
Clonazepam	HUMAN PRESCRIPTION DRUG LABEL	1	0093-3212	TABLET	1 mg	ORAL	ANDA	20 sections
Clonazepam	HUMAN PRESCRIPTION DRUG LABEL	1	0093-3213	TABLET	2 mg	ORAL	ANDA	20 sections
Clonazepam	HUMAN PRESCRIPTION DRUG LABEL	1	0093-3213	TABLET	2 mg	ORAL	ANDA	20 sections
Clonazepam	HUMAN PRESCRIPTION DRUG LABEL	1	0093-3213	TABLET	2 mg	ORAL	ANDA	20 sections
Clonazepam	HUMAN PRESCRIPTION DRUG LABEL	1	0093-9290	TABLET, ORALLY DISINTEGRATING	0.13 mg	ORAL	ANDA	27 sections

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