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

Stem definitionDrug idCAS RN
antihistaminics 671 15686-51-8

Description:

MoleculeDescription

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:

DoseUnitRoute
2 mg O
2 mg P

ADMET properties:

PropertyValueReference
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:

DateAgencyCompanyOrphan
Feb. 25, 1977 FDA

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Leukopenia 84.10 23.96 64 5259 67464 50532337
Dyspnoea 75.01 23.96 172 5151 547436 50052365
General physical health deterioration 72.80 23.96 82 5241 142352 50457449
Erythema 72.64 23.96 83 5240 146331 50453470
Tooth erosion 65.69 23.96 14 5309 437 50599364
Allergy test positive 61.43 23.96 13 5310 392 50599409
Pulpitis dental 52.10 23.96 13 5310 820 50598981
Cytokine release syndrome 45.90 23.96 21 5302 8613 50591188
Mucosal inflammation 45.47 23.96 36 5287 40106 50559695
Periodontitis 42.92 23.96 15 5308 3054 50596747
Drug reaction with eosinophilia and systemic symptoms 42.24 23.96 30 5293 28394 50571407
Angioedema 40.99 23.96 33 5290 37643 50562158
Toxic epidermal necrolysis 40.38 23.96 26 5297 20966 50578835
Anaphylactic shock 36.40 23.96 24 5299 20131 50579670
Nail toxicity 35.32 23.96 8 5315 332 50599469
Chills 32.21 23.96 45 5278 96642 50503159
Tachycardia 31.12 23.96 45 5278 99718 50500083
Venous thrombosis limb 29.83 23.96 11 5312 2611 50597190
Feeling hot 29.81 23.96 28 5295 39174 50560627
Circulatory collapse 29.45 23.96 21 5302 19979 50579822
Postpartum haemorrhage 26.18 23.96 9 5314 1745 50598056
Sensory disturbance 26.13 23.96 16 5307 11813 50587988
Febrile neutropenia 26.11 23.96 41 5282 97626 50502175
Polyneuropathy 25.76 23.96 16 5307 12115 50587686
Cerebral hypoperfusion 25.01 23.96 6 5317 321 50599480
Drug ineffective 24.83 23.96 30 5293 819303 49780498

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Cytokine release syndrome 76.75 22.36 35 3363 13084 29558045
Pyrexia 47.87 22.36 103 3295 287519 29283610
Chills 43.52 22.36 47 3351 71253 29499876
Toxic epidermal necrolysis 41.77 22.36 26 3372 18127 29553002
Febrile neutropenia 40.89 22.36 57 3341 112183 29458946
SARS-CoV-2 sepsis 36.07 22.36 7 3391 123 29571006
Long QT syndrome 34.29 22.36 12 3386 2246 29568883
Pulpitis dental 33.64 22.36 8 3390 377 29570752
Lacrimal duct neoplasm 31.41 22.36 5 3393 25 29571104
Mantle cell lymphoma stage III 31.41 22.36 5 3393 25 29571104
Herpes zoster reactivation 30.97 22.36 7 3391 263 29570866
Fibrin D dimer increased 30.63 22.36 12 3386 3076 29568053
Drug therapeutic incompatibility 30.52 22.36 6 3392 113 29571016
Polyneuropathy 29.46 22.36 18 3380 12134 29558995
Cancer fatigue 28.11 22.36 5 3393 53 29571076
Leukopenia 27.87 22.36 33 3365 55170 29515959
Immune effector cell-associated neurotoxicity syndrome 26.64 22.36 9 3389 1515 29569614
Drug reaction with eosinophilia and systemic symptoms 25.52 22.36 23 3375 27969 29543160
Conjunctivitis 25.07 22.36 14 3384 7984 29563145
Hypothalamo-pituitary disorder 23.88 22.36 7 3391 742 29570387
Scrotal pain 23.46 22.36 7 3391 789 29570340
Neutropenia 22.70 22.36 48 3350 131663 29439466
Electrocardiogram T wave biphasic 22.52 22.36 5 3393 173 29570956

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Leukopenia 92.09 21.30 86 7944 101156 64389546
Pulpitis dental 86.45 21.30 21 8009 998 64489704
Erythema 78.35 21.30 106 7924 186964 64303738
Cytokine release syndrome 74.87 21.30 41 7989 20788 64469914
Toxic epidermal necrolysis 73.76 21.30 50 7980 37116 64453586
Chills 62.38 21.30 81 7949 137183 64353519
Tooth erosion 59.56 21.30 13 8017 382 64490320
Allergy test positive 58.29 21.30 13 8017 423 64490279
Drug reaction with eosinophilia and systemic symptoms 56.99 21.30 50 7980 54167 64436535
Periodontitis 53.62 21.30 20 8010 4139 64486563
Polyneuropathy 52.41 21.30 32 7998 19862 64470840
General physical health deterioration 51.95 21.30 92 7938 204333 64286369
Dyspnoea 48.69 21.30 197 7833 718477 63772225
Angioedema 47.66 21.30 48 7982 61773 64428929
Febrile neutropenia 47.09 21.30 84 7946 187573 64303129
Anaphylactic shock 42.37 21.30 33 7997 30295 64460407
Pyrexia 41.69 21.30 158 7872 558486 63932216
Circulatory collapse 37.23 21.30 32 7998 33700 64457002
SARS-CoV-2 sepsis 35.35 21.30 7 8023 126 64490576
Stevens-Johnson syndrome 34.81 21.30 31 7999 34218 64456484
Feeling hot 34.35 21.30 35 7995 45628 64445074
Venous thrombosis limb 33.78 21.30 14 8016 3823 64486879
Bronchospasm 31.17 21.30 24 8006 21658 64469044
Tachycardia 30.11 21.30 61 7969 149518 64341184
Tumour lysis syndrome 29.00 21.30 22 8008 19418 64471284
Nail toxicity 28.48 21.30 7 8023 349 64490353
Drug therapeutic incompatibility 28.34 21.30 6 8024 152 64490550
Neutropenia 26.94 21.30 78 7952 239546 64251156
Fibrin D dimer increased 26.20 21.30 14 8016 6751 64483951
Anaemia 25.63 21.30 104 7926 378576 64112126
Guillain-Barre syndrome 24.62 21.30 14 8016 7621 64483081
Lymphocytosis 24.53 21.30 11 8019 3633 64487069
Torsade de pointes 24.48 21.30 19 8011 17344 64473358
Mucosal inflammation 23.93 21.30 34 7996 62550 64428152
Long QT syndrome 23.83 21.30 12 8018 5127 64485575
Sensory disturbance 22.06 21.30 16 8014 13192 64477510
Electrocardiogram T wave biphasic 21.93 21.30 5 8025 180 64490522

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
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|

DiseaseRelationSNOMED_IDDOID
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 levelDissociation constantType (acidic/basic)
pKa1 9.7 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Histamine H1 receptor GPCR ANTAGONIST Ki 8.59 WOMBAT-PK CHEMBL
D(2) dopamine receptor GPCR Ki 7.35 DRUG MATRIX
Alpha-2A adrenergic receptor GPCR Ki 7.16 DRUG MATRIX
Sigma non-opioid intracellular receptor 1 Membrane receptor Ki 7.85 DRUG MATRIX
Potassium voltage-gated channel subfamily H member 2 Ion channel Ki 7.92 WOMBAT-PK
Sodium-dependent noradrenaline transporter Transporter Ki 5.51 DRUG MATRIX
5-hydroxytryptamine receptor 2A GPCR Ki 8.04 DRUG MATRIX
5-hydroxytryptamine receptor 2B GPCR Ki 7.64 DRUG MATRIX
5-hydroxytryptamine receptor 2C GPCR Ki 7.28 DRUG MATRIX
5-hydroxytryptamine receptor 6 GPCR Ki 7.44 DRUG MATRIX
Alpha-2B adrenergic receptor GPCR Ki 6.85 DRUG MATRIX
D(3) dopamine receptor GPCR Ki 8.60 DRUG MATRIX
Histamine H2 receptor GPCR Ki 6.44 DRUG MATRIX
Muscarinic acetylcholine receptor M1 GPCR Ki 7.80 WOMBAT-PK
Muscarinic acetylcholine receptor M2 GPCR Ki 6.70 WOMBAT-PK
Muscarinic acetylcholine receptor M3 GPCR Ki 8.08 DRUG MATRIX
Muscarinic acetylcholine receptor M4 GPCR Ki 8.56 DRUG MATRIX
Muscarinic acetylcholine receptor M5 GPCR Ki 8.22 DRUG MATRIX
Alpha-2C adrenergic receptor GPCR Ki 7.85 DRUG MATRIX
Sodium-dependent dopamine transporter Transporter Ki 6.27 DRUG MATRIX
Cytochrome P450 2D6 Enzyme Ki 5.70 WOMBAT-PK
Alpha-1D adrenergic receptor GPCR Ki 7.82 DRUG MATRIX
Cytochrome P450 2C19 Enzyme IC50 6.22 DRUG MATRIX
Solute carrier family 22 member 1 Transporter IC50 5.31 CHEMBL
D(1A) dopamine receptor GPCR Ki 6.12 DRUG MATRIX
Transmembrane protein 97 Enzyme Ki 7.60 CHEMBL
Alpha-1B adrenergic receptor GPCR Ki 7.39 DRUG MATRIX
5-hydroxytryptamine receptor 1B GPCR Ki 6.66 DRUG MATRIX
Membrane-associated progesterone receptor component 1 Membrane receptor Ki 6.35 DRUG MATRIX
Alpha-1A adrenergic receptor GPCR IC50 7.28 CHEMBL

External reference:

IDSource
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:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
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 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