Cevimeline Hydrochloride

(USAN, rINNM)
Synonyms: AF-102; AF-102B; Céviméline, Chlorhydrate de; Cevimelini Hydrochloridum; FKS-508; Hidrocloruro de cevimelina; SND-5008; SNI-2011; SNK-508. (±)cis-2-Methylspiro[1,3-oxathiolane-5,3′quinuclidine] hydrochloride hemihydrate.
Cyrillic synonym: Цевимелина Гидрохлорид.

💊 Chemical information

Chemical formula: C10H17NOS,HCl, H2O = 244.8.
CAS — 107233-08-9 (cevimeline); 153504-70-2 (cevimeline hydrochloride).

💊 Adverse Effects, Treatment, and Precautions

As for Neostigmine. Sweating is a common problem with cevimeline; patients who sweat excessively should be advised to drink extra fluids to avoid dehydration. The manufacturer recommends that cevimeline should not be given when miosis is undesirable such as in patients with acute iritis or angle-closure glaucoma. Blurred vision may affect the performance of skilled tasks. In addition cevimeline should be given with care to those with renal calculi or with biliary-tract disorders. It should also be used with caution in patients deficient in the cytochrome P450 isoenzyme CYP2D6 who may be at a higher risk of adverse effects.

💊 Interactions

As for Neostigmine. Drugs which inhibit cytochrome P450 isoenzymes CYP2D6, CYP3A3, or CYP3A4 inhibit the metabolism of cevimeline.

💊 Pharmacokinetics

After oral doses cevimeline is absorbed from the gastrointestinal tract; peak concentrations are reached in 1.5 to 2 hours. The rate and extent of absorption are decreased when given with food. Cevimeline is less than 20% bound to plasma proteins. It is metabolised in the liver by cytochrome P450 isoenzymes CYP2D6, CYP3A3, and CYP3A4. Cevimeline is primarily excreted in the urine, mainly as metabolites; about 0.5% of a dose is excreted in the faeces.

💊 Uses and Administration

Cevimeline is a selective muscarinic M1 agonist used to improve the symptoms of dry mouth in patients with Sjögren’s syndrome. It is given as the hydrochloride by mouth in doses of 30 mg 3 times daily.

Dementia.

Muscarinic M1 agonists such as cevimeline have proved unsuccessful in relieving the symptoms of Alzheimer’s disease.

💊 Preparations

Proprietary Preparations

USA: Evoxac.
Published March 02, 2019.