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

Stem definition	Drug id	CAS RN
diazepam derivatives	594	58-25-3

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: chlordiazepoxide chlordiazepoxide hydrochloride chloridazepoxide methaminodiazepoxide chlordiazepoxid chlorodiazepoxide chlordiazepoxide HCl	An anxiolytic benzodiazepine derivative with anticonvulsant, sedative, and amnesic properties. It has also been used in the symptomatic treatment of alcohol withdrawal. Molecular weight: 299.76 Formula: C16H14ClN3O CLOGP: 3.79 LIPINSKI: 0 HAC: 4 HDO: 1 TPSA: 53.14 ALOGS: -4.18 ROTB: 1 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

chlordiazepoxide
chlordiazepoxide hydrochloride
chloridazepoxide
methaminodiazepoxide
chlordiazepoxid
chlorodiazepoxide
chlordiazepoxide HCl

An anxiolytic benzodiazepine derivative with anticonvulsant, sedative, and amnesic properties. It has also been used in the symptomatic treatment of alcohol withdrawal.

Molecular weight: 299.76
Formula: C16H14ClN3O
CLOGP: 3.79
LIPINSKI: 0
HAC: 4
HDO: 1
TPSA: 53.14
ALOGS: -4.18
ROTB: 1

Status: OFP

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

Drug dosage:

Dose	Unit	Route
30	mg	O
50	mg	P

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	99 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
t_half (Half-life)	8.30 hours	Lombardo F, Berellini G, Obach RS
S (Water solubility)	2 mg/mL	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	14.30 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
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
CL (Clearance)	0.37 mL/min/kg	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	0.25 L/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.06 %	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
Feb. 24, 1960	FDA	VALEANT PHARM INTL

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
Cerebral venous thrombosis	218.08	23.17	43	3023	2031	63483925
Drug abuse	126.06	23.17	64	3002	72454	63413502
Bradyphrenia	91.80	23.17	27	3039	6953	63479003
Hyperreflexia	91.60	23.17	26	3040	5908	63480048
Thalamic infarction	81.78	23.17	15	3051	477	63485479
Drug interaction	76.42	23.17	73	2993	229058	63256898
Toxicity to various agents	69.90	23.17	72	2994	247178	63238778
Sopor	58.12	23.17	26	3040	22138	63463818
Intentional product misuse	57.28	23.17	36	3030	60881	63425075
Drug withdrawal syndrome	50.06	23.17	25	3041	27169	63458787

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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	192.31	28.70	98	1836	98998	34855999
Toxicity to various agents	180.06	28.70	120	1814	200242	34754755
Ventricular tachyarrhythmia	103.94	28.70	18	1916	356	34954641
Delusion of replacement	61.60	28.70	10	1924	131	34954866
Shoshin beriberi	44.41	28.70	7	1927	75	34954922
Overdose	44.10	28.70	38	1896	91021	34863976
Completed suicide	37.76	28.70	36	1898	98132	34856865
Tracheobronchitis	31.54	28.70	8	1926	1033	34953964

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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
Drug abuse	300.75	22.61	156	4248	162535	79577449
Cerebral venous thrombosis	200.09	22.61	43	4361	2710	79737274
Toxicity to various agents	199.85	22.61	173	4231	421367	79318617
Hyperreflexia	83.32	22.61	27	4377	8358	79731626
Bradyphrenia	77.01	22.61	27	4377	10613	79729371
Completed suicide	74.21	22.61	79	4325	245688	79494296
Intentional product misuse	72.69	22.61	52	4352	95113	79644871
Sopor	70.37	22.61	35	4369	32975	79707009
Thalamic infarction	65.15	22.61	15	4389	1292	79738692
Delusion of replacement	59.79	22.61	10	4394	159	79739825

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	N05BA02	NERVOUS SYSTEM PSYCHOLEPTICS ANXIOLYTICS Benzodiazepine derivatives
CHEBI has role	CHEBI:35474	anti-anxiety agents
CHEBI has role	CHEBI:35717	hypnotics
CHEBI has role	CHEBI:60807	anaesthestic adjuvant
FDA CS	M0002356	Benzodiazepines
FDA EPC	N0000175694	Benzodiazepine
MeSH PA	D000759	Adjuvants, Anesthesia
MeSH PA	D014151	Anti-Anxiety Agents
MeSH PA	D002491	Central Nervous System Agents
MeSH PA	D002492	Central Nervous System Depressants

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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
Alcohol withdrawal delirium	indication	8635005
Irritable bowel syndrome	indication	10743008	DOID:9778
Peptic ulcer	indication	13200003	DOID:750
Anxiety	indication	48694002
General anesthesia	indication	50697003
Severe anxiety (panic)	indication	80583007
Alcohol withdrawal syndrome	indication	191480000
Mixed anxiety and depressive disorder	indication	231504006
Local anesthesia	indication	386761002
Preoperative Anxiety	indication

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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	4.79	Basic
pKa2	4.13	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-2/beta-3/gamma-2	Ion channel	P18507 P28472 P47869	GBRG2_HUMAN GBRB3_HUMAN GBRA2_HUMAN	POSITIVE ALLOSTERIC MODULATOR	Ki	6.34	WOMBAT-PK	CHEMBL
GABA-A receptor alpha-3/beta-3/gamma-2	Ion channel	P18507 P28472 P34903	GBRG2_HUMAN GBRB3_HUMAN GBRA3_HUMAN	POSITIVE ALLOSTERIC MODULATOR	Ki	6.56	WOMBAT-PK	CHEMBL
GABA-A receptor alpha-5/beta-3/gamma-2	Ion channel	P18507 P28472 P31644	GBRG2_HUMAN GBRB3_HUMAN GBRA5_HUMAN	POSITIVE ALLOSTERIC MODULATOR	Ki	6.50	WOMBAT-PK	CHEMBL
GABA-A receptor alpha-1/beta-2/gamma-2	Ion channel	P14867 P18507 P47870	GBRA1_HUMAN GBRG2_HUMAN GBRB2_HUMAN	POSITIVE ALLOSTERIC MODULATOR	Ki	6.25	WOMBAT-PK	CHEMBL
GABA-A receptor alpha-1/beta-3/gamma-2	Ion channel	P14867 P18507 P28472	GBRA1_HUMAN GBRG2_HUMAN GBRB3_HUMAN		Ki	6.25	CHEMBL
Cholecystokinin receptor	GPCR	P32238 P32239	CCKAR_HUMAN GASR_HUMAN		IC50	4	CHEMBL
Histamine H1 receptor	GPCR	P35367	HRH1_HUMAN		Ki	6.68	DRUG MATRIX
Thyrotropin-releasing hormone receptor	GPCR	P34981	TRFR_HUMAN		Ki	6.54	WOMBAT-PK
Thyrotropin-releasing hormone receptor	GPCR		TRFR_RAT	ANTAGONIST	Ki	4.82	IUPHAR
Cholinesterase	Enzyme		CHLE_HORSE		Ki	6.52	CHEMBL

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External reference:

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ID	Source
001454	NDDF
001455	NDDF
1049	INN_ID
203173	RXNORM
2712	PUBCHEM_CID
3370	IUPHAR_LIGAND_ID
372866006	SNOMEDCT_US
3903	MMSL
4017780	VUID
4017780	VANDF

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Chlordiazepoxide and Amitriptyline Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	2	0378-0211	TABLET, FILM COATED	5 mg	ORAL	ANDA	25 sections
Chlordiazepoxide and Amitriptyline Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	2	0378-0211	TABLET, FILM COATED	5 mg	ORAL	ANDA	25 sections
Chlordiazepoxide and Amitriptyline Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	2	0378-0211	TABLET, FILM COATED	5 mg	ORAL	ANDA	25 sections
Chlordiazepoxide and Amitriptyline Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	2	0378-0277	TABLET, FILM COATED	10 mg	ORAL	ANDA	25 sections
Chlordiazepoxide and Amitriptyline Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	2	0378-0277	TABLET, FILM COATED	10 mg	ORAL	ANDA	25 sections
Chlordiazepoxide and Amitriptyline Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	2	0378-0277	TABLET, FILM COATED	10 mg	ORAL	ANDA	25 sections
Chlordiazepoxide and Amitriptyline Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	2	42571-302	TABLET	12.50 mg	ORAL	ANDA	24 sections
Chlordiazepoxide and Amitriptyline Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	2	42571-302	TABLET	12.50 mg	ORAL	ANDA	24 sections
Chlordiazepoxide and Amitriptyline Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	2	42571-303	TABLET	25 mg	ORAL	ANDA	24 sections
Chlordiazepoxide and Amitriptyline Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	2	42571-303	TABLET	25 mg	ORAL	ANDA	24 sections

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