Clemastine

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Inhibits
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Bulgaria: Clemastin, Tavegyl; Czech Republic: Tavegyl; Denmark: Tavegyl; Estonia: Tavegyl; Germany: Tavegil; Lithuania: Clemastinum, Tavegyl; Netherlands: Tavegyl; Poland: Clemastinum; Portugal: Tavegyl, Tavist; Romania: Tavegyl; Slovakia: Tavegyl; Slovenia: Tavegyl; Spain: Tavegil; Sweden: Tavegyl; UK: Tavegil.

North America

Canada: Tavist; USA: Clemastine, Tavist.

Latin America

Brazil: Agasten; Mexico: Tavist.

Asia

Japan: Alagyl, Benanzyl, Cle mamallet, Clemanil, Fuluminol, Inbestan, Kinotomin, Mallermin F, Marsthine, Masletine, Tavegyl, Telgin G, Xolamin.

Drugs Combination

Clemastine, Acetaminophen, and Pseudoephedrine

Drug combinations

Chemistry

Clemastine Fumarate: C~21~H~26~ClNO C~4~H~4~O~4~. Mw: 459.96. (1) Pyrrolidine, 2-[2-[1-(4-chlorophenyl)-1-phenylethoxy]ethyl]-1-methyl-, [R-(R*,R*)]-, (E)-2-butenedioate (1:1); (2)(+)-(2R)-2-[2-[[(R)-p-Chloro-α-methyl-α-phenylbenzyl]oxy]ethyl]-1-methylpyrrolidine fumarate (1:1). CAS-14976-57-9; CAS-15686-51-8 (clemastine)(1977).

Pharmacologic Category

First Generation Antihistamines; Histamine H~1~ Antagonist. (ATC-Code: D04AA14; R06AA04).

Mechanism of action

Competes with histamine for H~1~-receptor sites on effector cells in the gastrointestinal tract, blood vessels, and respiratory tract. Suppresses flare and pruritus that accompany the endogenous release of histamine. Has anticholinergic and sedative effects. Antihistamines do not block the stimulating effect of histamine on gastric acid secretion, which is mediated by H~2~-receptors of the parietal cells.

Therapeutic use

Perennial and seasonal allergic rhinitis. Other allergic symptoms including urticaria.

Pregnancy and lactiation implications

No evidence of fetal harm revealed in reproduction studies in animals. Use during pregnancy only when clearly needed. Distributed into milk (use with caution).

Unlabeled use

Contraindications

Hypersensitivity to clemastine or any component of the formulation. Narrow-angle glaucoma.

Warnings and precautions

May cause CNS depression. Use with caution in history of asthma, cardiovascular disease (including hypertension and ischemic heart disease), or increased intraocular pressure. Use with caution in prostatic hyperplasia and/or genitourinary obstruction, or pyloroduodenal obstruction (including stenotic peptic ulcer). Use with caution in thyroid dysfunction. Effects may be potentiated when used with other sedative drugs or ethanol. Use with caution in the elderly (may be more sensitive to adverse effects).

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