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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:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	2.30 mg/mL	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	5 %	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
BA (Bioavailability)	37 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Approvals:

Date	Agency	Company	Orphan
Feb. 25, 1977	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
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
Angioedema	49.57	25.74	40	6339	47925	63434718
Sepsis	47.17	25.74	67	6312	153056	63329587
Mucosal inflammation	46.10	25.74	38	6341	46890	63435753
Drug reaction with eosinophilia and systemic symptoms	43.21	25.74	32	6347	33804	63448839
Periodontitis	42.52	25.74	15	6364	3288	63479355
Tachycardia	39.81	25.74	54	6325	118102	63364541
Anaphylactic shock	38.64	25.74	26	6353	23607	63459036
Drug ineffective	37.84	25.74	30	6349	1044735	62437908
Feeling hot	37.82	25.74	35	6344	50319	63432324
Sensory disturbance	37.67	25.74	21	6358	13651	63468992
Stevens-Johnson syndrome	37.37	25.74	26	6353	24924	63457719
Nail toxicity	35.48	25.74	8	6371	341	63482302
Lymphocytosis	33.47	25.74	12	6367	2755	63479888
Circulatory collapse	33.18	25.74	23	6356	21915	63460728
Chills	32.54	25.74	48	6331	113330	63369313
Urticaria	31.15	25.74	58	6321	165744	63316899
Blood lactate dehydrogenase increased	29.82	25.74	22	6357	23094	63459549
Leukocytosis	29.73	25.74	23	6356	25912	63456731
Neutropenia	28.93	25.74	58	6321	174947	63307696
Venous thrombosis limb	28.85	25.74	11	6368	2997	63479646
Thrombocytopenia	28.54	25.74	53	6326	151104	63331539
Febrile neutropenia	28.19	25.74	46	6333	118403	63364240
Lymphangiectasia	27.24	25.74	5	6374	74	63482569
Polyneuropathy	26.15	25.74	17	6362	14572	63468071

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
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
Lacrimal duct neoplasm	31.46	23.77	5	3968	25	34952933
Conjunctivitis	30.63	23.77	17	3956	9688	34943270
Drug therapeutic incompatibility	30.44	23.77	6	3967	116	34952842
Herpes zoster reactivation	30.24	23.77	7	3966	296	34952662
Guillain-Barre syndrome	28.82	23.77	14	3959	6073	34946885
Polyneuropathy	28.67	23.77	19	3954	14877	34938081
Fibrin D dimer increased	27.07	23.77	12	3961	4232	34948726
Drug reaction with eosinophilia and systemic symptoms	26.22	23.77	25	3948	32987	34919971
Cancer fatigue	26.20	23.77	5	3968	81	34952877
Neutropenia	26.13	23.77	56	3917	156722	34796236
Infusion related reaction	25.86	23.77	31	3942	53026	34899932

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
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
Allergy test positive	57.08	21.16	14	9616	714	79734044
Angioedema	56.37	21.16	57	9573	75978	79658780
Periodontitis	56.33	21.16	21	9609	4475	79730283
Polyneuropathy	52.47	21.16	34	9596	24117	79710641
Stevens-Johnson syndrome	50.20	21.16	40	9590	39126	79695632
Hydronephrosis	49.17	21.16	29	9601	17425	79717333
Febrile neutropenia	47.10	21.16	93	9537	230906	79503852
Lymphocytosis	44.83	21.16	18	9612	4675	79730083
Anaphylactic shock	44.51	21.16	36	9594	35960	79698798
Dyspnoea	44.13	21.16	212	9418	856813	78877945
Sepsis	43.93	21.16	99	9531	269329	79465429
Circulatory collapse	43.07	21.16	36	9594	37632	79697126
Neutropenia	41.75	21.16	101	9529	287609	79447149
Feeling hot	39.27	21.16	42	9588	59692	79675066
Tachycardia	39.19	21.16	74	9556	177694	79557064
Conjunctivitis	38.93	21.16	29	9601	25686	79709072
Tumour lysis syndrome	36.25	21.16	27	9603	23912	79710846
SARS-CoV-2 sepsis	35.40	21.16	7	9623	129	79734629
Anaemia	34.53	21.16	125	9505	444890	79289868
Mucosal erosion	33.39	21.16	12	9618	2306	79732452
Sensory disturbance	32.19	21.16	21	9609	15056	79719702
Venous thrombosis limb	32.17	21.16	14	9616	4443	79730315
Leukocytosis	31.14	21.16	32	9598	43423	79691335
Bronchospasm	31.02	21.16	25	9605	24834	79709924
Guillain-Barre syndrome	30.91	21.16	17	9613	8948	79725810
Thrombocytopenia	30.13	21.16	85	9545	265174	79469584
Urticaria	30.09	21.16	68	9562	185133	79549625
C-reactive protein increased	28.78	21.16	54	9576	128973	79605785
Nail toxicity	28.56	21.16	7	9623	356	79734402
Blood lactate dehydrogenase increased	28.35	21.16	29	9601	39141	79695617
Drug therapeutic incompatibility	28.09	21.16	6	9624	164	79734594
Infusion related reaction	27.34	21.16	75	9555	230162	79504596
Lymphangiectasia	24.49	21.16	5	9625	109	79734649
Tryptase increased	24.48	21.16	7	9623	646	79734112
Arthralgia	24.40	21.16	20	9610	571783	79162975
Mucosal inflammation	23.96	21.16	37	9593	75543	79659215
Fibrin D dimer increased	23.38	21.16	14	9616	8640	79726118
Torsade de pointes	23.20	21.16	19	9611	19293	79715465
B-lymphocyte count decreased	22.95	21.16	8	9622	1406	79733352
Pain	22.88	21.16	31	9599	703771	79030987
Long QT syndrome	22.50	21.16	12	9618	5943	79728815
Neisseria infection	22.38	21.16	5	9625	169	79734589
Electrocardiogram T wave biphasic	22.08	21.16	5	9625	180	79734578

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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
MeSH PA	D018494	Histamine Agents
MeSH PA	D006633	Histamine Antagonists
MeSH PA	D006634	Histamine H1 Antagonists
MeSH PA	D018377	Neurotransmitter Agents

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

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
Ocular hypertension	contraindication	4210003	DOID:9282
Peptic ulcer	contraindication	13200003	DOID:750
Hyperthyroidism	contraindication	34486009	DOID:7998
Hypertensive disorder	contraindication	38341003	DOID:10763
Chronic idiopathic constipation	contraindication	82934008
Bladder outflow obstruction	contraindication	236645006
Benign prostatic hyperplasia	contraindication	266569009
Retention of urine	contraindication	267064002
Angle-closure glaucoma	contraindication	392291006	DOID:13550

🐶 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:

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
5-hydroxytryptamine receptor 6	GPCR	P50406	5HT6R_HUMAN		Ki	7.44	DRUG MATRIX
Alpha-2B adrenergic receptor	GPCR	P18089	ADA2B_HUMAN		Ki	6.85	DRUG MATRIX
D(3) dopamine receptor	GPCR	P35462	DRD3_HUMAN		Ki	8.60	DRUG MATRIX
Histamine H2 receptor	GPCR	P25021	HRH2_HUMAN		Ki	6.44	DRUG MATRIX
Muscarinic acetylcholine receptor M1	GPCR	P11229	ACM1_HUMAN		Ki	7.80	WOMBAT-PK
Muscarinic acetylcholine receptor M3	GPCR	P20309	ACM3_HUMAN		Ki	8.08	DRUG MATRIX
Muscarinic acetylcholine receptor M4	GPCR	P08173	ACM4_HUMAN		Ki	8.56	DRUG MATRIX
Muscarinic acetylcholine receptor M5	GPCR	P08912	ACM5_HUMAN		Ki	8.22	DRUG MATRIX
Alpha-2C adrenergic receptor	GPCR	P18825	ADA2C_HUMAN		Ki	7.85	DRUG MATRIX
Sodium-dependent dopamine transporter	Transporter	Q01959	SC6A3_HUMAN		Ki	6.27	DRUG MATRIX
Cytochrome P450 2D6	Enzyme	P10635	CP2D6_HUMAN		Ki	5.70	WOMBAT-PK
Alpha-1D adrenergic receptor	GPCR	P25100	ADA1D_HUMAN		Ki	7.82	DRUG MATRIX
Cytochrome P450 2C19	Enzyme	P33261	CP2CJ_HUMAN		IC50	6.22	DRUG MATRIX
Solute carrier family 22 member 1	Transporter	O15245	S22A1_HUMAN		IC50	5.31	CHEMBL
Muscarinic acetylcholine receptor M2	GPCR	P08172	ACM2_HUMAN		Ki	6.70	WOMBAT-PK
Transmembrane protein 97	Enzyme	Q5BJF2	TMM97_HUMAN		Ki	7.60	CHEMBL
Alpha-1B adrenergic receptor	GPCR		ADA1B_RAT		Ki	7.39	DRUG MATRIX
5-hydroxytryptamine receptor 1B	GPCR		5HT1B_RAT		Ki	6.66	DRUG MATRIX
Membrane-associated progesterone receptor component 1	Membrane receptor		PGRC1_RAT		Ki	6.35	DRUG MATRIX
Alpha-1A adrenergic receptor	GPCR		ADA1A_RAT		IC50	7.28	CHEMBL

External reference:

ID	Source
4019681	VUID
N0000147773	NUI
D00666	KEGG_DRUG
14976-57-9	SECONDARY_CAS_RN
142430	RXNORM
4018759	VANDF
4019681	VANDF
C0008929	UMLSCUI
CHEBI:3738	CHEBI
CHEMBL1626	ChEMBL_ID
DB00283	DRUGBANK_ID
CHEMBL1200795	ChEMBL_ID
D002974	MESH_DESCRIPTOR_UI
26987	PUBCHEM_CID
6063	IUPHAR_LIGAND_ID
2231	INN_ID
95QN29S1ID	UNII
224	MMSL
4464	MMSL
d00780	MMSL
003410	NDDF
004441	NDDF
372744005	SNOMEDCT_US
45218006	SNOMEDCT_US
83968007	SNOMEDCT_US

Pharmaceutical products:

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