Cevimeline

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
  • Substrate of
  • Drug Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

North America

Canada: Evoxac; USA: Evoxac.

Asia

Japan: Evoxac, Saligren.

Drug combinations

Chemistry

Cevimeline Hydrochloride: C~10~H~17~NOS HCl .½H~2~O. Mw: 244.78. (1) Spiro[1-azabicyclo[2.2.2]octane-3,5′-[1,3]oxathiolane], 2′-methyl-, hydrochloride, hydrate (2:1), cis-; (2)(±)-cis-2-Methylspiro[1,3-oxathiolane-5,3′-quinuclidine] hydrochloride, hemihydrate. CAS-153504-70-2; CAS-107233-08-9 (cevimeline)(1997).

Pharmacologic Category

Parasympathomimetic (Cholinergic) Agents. (ATC-Code: N07AX03).

Mechanism of action

Binds to muscarinic (cholinergic) receptors, causing an increase in secretion of exocrine glands (including salivary glands) and increased gastrointestinal and urinary tract smooth muscle tone. Pharmacologically similar to pilocarpine.

Therapeutic use

Dry mouth in Sjögren’s syndrome.

Pregnancy and lactiation implications

No adequate studies in pregnant women. Use only if potential benefit justifies potential risk to the fetus. Use not recommended during lactation.

Unlabeled use

Contraindications

Hypersensitivity to cevimeline or any component of the formulation. Uncontrolled asthma. Narrow-angle glaucoma. Acute iritis. Other conditions where miosis is undesirable.

Warnings and precautions

May cause a variety of parasympathomimetic effects, which may be particularly dangerous in elderly patients (excessive sweating may lead to dehydration in some patients). May cause decreased visual acuity (particularly at night and in central lens changes) and impaired depth perception. Use with caution in history of biliary stones (may induce smooth muscle spasms, precipitating cholangitis, cholecystitis, or biliary obstruction in susceptible patients). Use with caution in significant cardiovascular disease (including angina, myocardial infarction, or conduction disturbances; may alter cardiac conduction and/or heart rate). Use with caution in history of nephrolithiasis (may induce smooth muscle spasms, precipitating renal colic or ureteral reflux in susceptible patients). Use with caution in controlled asthma, chronic obstructive pulmonary disease, or chronic bronchitis (may increase bronchial smooth muscle tone, airway resistance, and bronchial secretions). Patients with a known or suspected deficiency of CYP2D6 may be at higher risk of adverse effects.

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