Overview
DESCRIPTION Cevimeline is cis-2’-methylspiro {1-azabicyclo [2.2.2] octane-3, 5’ -[1,3] oxathiolane} hydrochloride, hydrate (2:1). Its molecular formula is C 10 H 17 NOS•HCl•½ H 2 O, and its structural formula is: Cevimeline hydrochloride, USP has a molecular weight of 244.79. It is a white to off white crystalline powder with a melting point range of 201°C and 203°C.
Mechanism of Action
CLINICAL PHARMACOLOGY Pharmacodynamics 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. Pharmacokinetics Absorption: After administration of a single 30 mg capsule, cevimeline was rapidly absorbed with a mean time to peak concentration of 1.5 hours to 2 hours. No accumulation of active drug or its metabolites was observed following multiple dose administration. When administered with food, there is a decrease in the rate of absorption, with a fasting T max of 1.53 hours and a T max of 2.86 hours after a meal; the peak concentration is reduced by 17.3%.
Indications
- INDICATIONS AND USAGE Cevimeline hydrochloride capsules are indicated for the treatment of symptoms of dry mouth in patients with Sjögren’s Syndrome.
Common Doses
- 30 mg
Dosage
DOSAGE AND ADMINISTRATION The recommended dose of cevimeline hydrochloride capsules is 30 mg taken three times a day. There is insufficient safety information to support doses greater than 30 mg tid. There is also insufficient evidence for additional efficacy of cevimeline hydrochloride at doses greater than 30 mg tid.
Contraindications
- CONTRAINDICATIONS Cevimeline is contraindicated in patients with uncontrolled asthma, known hypersensitivity to cevimeline, and when miosis is undesirable, e.g., in acute iritis and in narrow-angle (angle-closure) glaucoma.
Side Effects
- ADVERSE REACTIONS Cevimeline was administered to 1,777 patients during clinical trials worldwide, including Sjögren’s patients and patients with other conditions. In placebo-controlled Sjögren’s studies in the U.S., 320 patients received cevimeline doses ranging from 15 mg tid to 60 mg tid, of whom 93% were women and 7% were men. Demographic distribution was 90% Caucasian, 5% Hispanic, 3% Black and 2% of other origin. In these studies, 14.6% of patients discontinued treatment with cevimeline due to adverse events.
Interactions
- No major interactions listed on the FDA label. Always consult a healthcare professional.