Drug Groups

approved

Description

Cevimeline is a parasympathomimetic and muscarinic agonist, with particular effect on M3 receptors. It is indicated by the Food and Drug Administration for the treatment of dry mouth associated with Sj?gren's syndrome. [Wikipedia]

Indication

For the treatment of symptoms of dry mouth in patients with Sjögren's Syndrome.

Pharmacology

Cevimeline is a cholinergic agonist which binds to muscarinic receptors. Muscarinic agonists in sufficient dosage can increase secretion of exocrine glands, such as salivary and sweat glands and increase tone of the smooth muscle in the gastrointestinal and urinary tracts.

Affected Organisms

Biotransformation

Primarily hepatic, isozymes CYP2D6 and CYP3A4 are responsible for the metabolism of cevimeline. Approximately 44.5% of the drug is converted to cis and trans-sulfoxide, 22.3% to glucuronic acid conjugate, and 4% to N-oxide of cevimeline. Approximately 8% of the trans-sulfoxide metabolite is then converted into the corresponding glucuronic acid conjugate.

Absorption

Rapidly absorbed with peak concentration after 1.5 to 2 hours

Half Life

5 ± 1 hours

Protein Binding

< 20%

Elimination

After 24 hours, 84% of a 30 mg dose of cevimeline was excreted in urine.

Distribution

* 6 L/kg

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