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

Stem definition	Drug id	CAS RN
antihistaminics	671	15686-51-8

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: clemastine meclastine clemastine fumarate	A histamine H1 antagonist used as the hydrogen fumarate in hay fever, rhinitis, allergic skin conditions, and pruritus. It causes drowsiness. Molecular weight: 343.90 Formula: C21H26ClNO CLOGP: 5.45 LIPINSKI: 1 HAC: 2 HDO: 0 TPSA: 12.47 ALOGS: -5.93 ROTB: 6 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

clemastine
meclastine
clemastine fumarate

A histamine H1 antagonist used as the hydrogen fumarate in hay fever, rhinitis, allergic skin conditions, and pruritus. It causes drowsiness.

Molecular weight: 343.90
Formula: C21H26ClNO
CLOGP: 5.45
LIPINSKI: 1
HAC: 2
HDO: 0
TPSA: 12.47
ALOGS: -5.93
ROTB: 6

Status: OFP

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

Drug dosage:

Dose	Unit	Route
2	mg	O
2	mg	P

ADMET properties:

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Property	Value	Reference
EoM (Fraction excreted unchanged in urine)	5 %	Benet LZ, Broccatelli F, Oprea TI
BA (Bioavailability)	37 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
S (Water solubility)	2.30 mg/mL	Benet LZ, Broccatelli F, Oprea TI
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.39 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

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Approvals:

Date	Agency	Company	Orphan
Feb. 25, 1977	FDA

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
Leukopenia	103.21	25.74	75	6304	77215	63405428
Erythema	95.10	25.74	102	6277	175649	63306994
Cytokine release syndrome	81.46	25.74	36	6343	14278	63468365
Toxic epidermal necrolysis	75.61	25.74	41	6338	25293	63457350
General physical health deterioration	67.96	25.74	92	6287	201310	63281333
Hydronephrosis	67.79	25.74	29	6350	10633	63472010
Dyspnoea	66.86	25.74	180	6199	661133	62821510
Tooth erosion	65.66	25.74	14	6365	459	63482184
Allergy test positive	61.89	25.74	14	6365	606	63482037
Pulpitis dental	51.29	25.74	13	6366	915	63481728

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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
Cytokine release syndrome	80.45	23.77	43	3930	22834	34930124
Pyrexia	63.16	23.77	125	3848	332888	34620070
Pulpitis dental	50.09	23.77	12	3961	590	34952368
Toxic epidermal necrolysis	47.59	23.77	30	3943	21616	34931342
Chills	42.31	23.77	49	3924	80994	34871964
Leukopenia	41.49	23.77	43	3930	62813	34890145
Febrile neutropenia	38.18	23.77	61	3912	136788	34816170
SARS-CoV-2 sepsis	36.04	23.77	7	3966	125	34952833
Long QT syndrome	31.88	23.77	12	3961	2791	34950167
Mantle cell lymphoma stage III	31.46	23.77	5	3968	25	34952933

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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
Leukopenia	124.60	21.16	107	9523	116406	79618352
Toxic epidermal necrolysis	112.60	21.16	69	9561	44512	79690246
Cytokine release syndrome	109.96	21.16	63	9567	35935	79698823
Pulpitis dental	101.70	21.16	25	9605	1288	79733470
Erythema	100.43	21.16	129	9501	223161	79511597
Pyrexia	63.84	21.16	203	9427	678506	79056252
Chills	61.86	21.16	86	9544	160148	79574610
General physical health deterioration	61.33	21.16	115	9515	275123	79459635
Tooth erosion	59.54	21.16	13	9617	395	79734363
Drug reaction with eosinophilia and systemic symptoms	58.64	21.16	54	9576	64190	79670568

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	D04AA14	DERMATOLOGICALS ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC. ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC. Antihistamines for topical use
ATC	R06AA04	RESPIRATORY SYSTEM ANTIHISTAMINES FOR SYSTEMIC USE ANTIHISTAMINES FOR SYSTEMIC USE Aminoalkyl ethers
ATC	R06AA54	RESPIRATORY SYSTEM ANTIHISTAMINES FOR SYSTEMIC USE ANTIHISTAMINES FOR SYSTEMIC USE Aminoalkyl ethers
CHEBI has role	CHEBI:37955	H1 receptor antagonists
CHEBI has role	CHEBI:48876	muscarinic antagonists
CHEBI has role	CHEBI:50857	anti-allergic drugs
CHEBI has role	CHEBI:59683	antipruritic drugs
MeSH PA	D018926	Anti-Allergic Agents
MeSH PA	D000982	Antipruritics
MeSH PA	D003879	Dermatologic Agents

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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
Dermatographic urticaria	indication	7632005	DOID:743
Vasomotor rhinitis	indication	8229003	DOID:4730
Allergic rhinitis	indication	61582004
Nasal discharge	indication	64531003
Nasal congestion	indication	68235000
Sneezing	indication	76067001
Urticaria	indication	126485001
Itching of skin	indication	418363000
Allergic conjunctivitis	indication	473460002	DOID:11204
Anaphylaxis Adjunct	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	9.7	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
Histamine H1 receptor	GPCR	P35367	HRH1_HUMAN	ANTAGONIST	Ki	8.59	WOMBAT-PK	CHEMBL
D(1A) dopamine receptor	GPCR	P21728	DRD1_HUMAN		Ki	6.12	DRUG MATRIX
D(2) dopamine receptor	GPCR	P14416	DRD2_HUMAN		Ki	7.35	DRUG MATRIX
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN		Ki	7.16	DRUG MATRIX
Sigma non-opioid intracellular receptor 1	Membrane receptor	Q99720	SGMR1_HUMAN		Ki	7.85	DRUG MATRIX
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		Ki	7.92	WOMBAT-PK
Sodium-dependent noradrenaline transporter	Transporter	P23975	SC6A2_HUMAN		Ki	5.51	DRUG MATRIX
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN		Ki	8.04	DRUG MATRIX
5-hydroxytryptamine receptor 2B	GPCR	P41595	5HT2B_HUMAN		Ki	7.64	DRUG MATRIX
5-hydroxytryptamine receptor 2C	GPCR	P28335	5HT2C_HUMAN		Ki	7.28	DRUG MATRIX

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External reference:

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ID	Source
003410	NDDF
004441	NDDF
142430	RXNORM
14976-57-9	SECONDARY_CAS_RN
2231	INN_ID
224	MMSL
26987	PUBCHEM_CID
372744005	SNOMEDCT_US
4018759	VANDF
4019681	VUID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Clemastine Fumarate	HUMAN PRESCRIPTION DRUG LABEL	1	0093-0308	TABLET	2.68 mg	ORAL	ANDA	13 sections
Clemastine Fumarate	HUMAN PRESCRIPTION DRUG LABEL	1	0093-0308	TABLET	2.68 mg	ORAL	ANDA	13 sections
Clemastine Fumarate	HUMAN PRESCRIPTION DRUG LABEL	1	51655-425	TABLET	2.68 mg	Oral	ANDA	12 sections
Clemastine Fumarate	HUMAN PRESCRIPTION DRUG LABEL	1	54838-514	SYRUP	0.67 mg	ORAL	ANDA	17 sections
Clemastine Fumarate	HUMAN OTC DRUG LABEL	1	54868-5913	TABLET	1.34 mg	ORAL	ANDA	14 sections
CLEMASTINE FUMARATE	HUMAN PRESCRIPTION DRUG LABEL	1	62135-713	SYRUP	0.67 mg	ORAL	ANDA	12 sections
Clemastine Fumarate	HUMAN OTC DRUG LABEL	1	68151-2456	TABLET	1.34 mg	ORAL	ANDA	14 sections
Clemastine Fumarate	HUMAN PRESCRIPTION DRUG LABEL	1	73308-358	SYRUP	0.67 mg	ORAL	ANDA	17 sections
Clemastine Fumarate	HUMAN PRESCRIPTION DRUG LABEL	1	73308-358	SYRUP	0.67 mg	ORAL	ANDA	17 sections

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