Cevimeline

Uncontrolled asthma, conditions wherein miosis is undesirable (e.g. narrow-angle glaucoma, acute iritis).

Patient with significant CV disease (e.g. MI, angina), history of cholelithiasis or nephrolithiasis; controlled asthma, COPD, chronic bronchitis. Patient with known or suspected CYP2D6 deficiency may be at increased risk of adverse effects due to reduced cevimeline metabolism. Pregnancy and lactation.

Significant: Parasympathomimetic effects (e.g. sweating [excessive cases may lead to dehydration], AV block, bradycardia, arrhythmia, hypotension or hypertension, lacrimation, tachycardia, respiratory distress, gastrointestinal spasm, diarrhoea, vomiting, tremors, confusion); visual effects (e.g. blurred vision, decreased visual acuity).
Gastrointestinal disorders: Nausea, dyspepsia, abdominal pain.
General disorders and administration site conditions: Fatigue, pain.
Musculoskeletal and connective tissue disorders: Back pain, arthralgia.
Nervous system disorders: Headache.
Renal and urinary disorders: Urinary tract infection.
Respiratory, thoracic and mediastinal disorders: Rhinitis, sinusitis, upper respiratory tract infection, cough, pharyngitis, bronchitis.
Skin and subcutaneous tissue disorders: Rash.

PO: C

This drug may cause visual disturbances (e.g. blurred vision) particularly at night, if affected, do not drive or operate machinery.

Risk of conduction disturbances with β-blockers. Additive effects with other parasympathomimetic agents. Decreased metabolism and increased plasma concentration with inhibitors of CYP2D6 and CYP3A3/4.

Decreased rate of absorption with food.

Description:
Overview: Cevimeline is a cholinergic agonist.
Mechanism of Action: Cevimeline selectively binds to muscarinic M₁ receptors, resulting in increased secretion of exocrine glands (e.g. salivary glands, sweat glands) and increased smooth muscle tone in gastrointestinal and urinary tracts.
Pharmacokinetics:
Absorption: Rapidly absorbed from the gastrointestinal tract. Food decreases rate of absorption. Time to peak plasma concentration: 1.5-2 hours.
Distribution: Volume of distribution: 6 L/kg. Plasma protein binding: <20%.
Metabolism: Metabolised in the liver by CYP2D6 and CYP3A3/4 isoenzymes into cis- and trans-sulfoxide, glucuronic acid conjugate, and N-oxide metabolites.
Excretion: Mainly via urine (84% after 24 hours; 97% after 7 days); faeces (0.5% after 7 days). Elimination half-life: 5 ± 1 hours.

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 25137844, Cevimeline. https://pubchem.ncbi.nlm.nih.gov/compound/Cevimeline. Accessed Oct. 27, 2025.

Store between 15-30°C.

Other Gastrointestinal Drugs

N07AX03 - cevimeline ; Belongs to the class of other parasympathomimetics.

Brayfield A, Cadart C (eds). Cevimeline Hydrochloride. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 06/10/2025.

Cevimeline Hydrochloride Capsule (Lupin Pharmaceuticals, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 23/10/2025.

Cevimeline Hydrochloride. UpToDate Lexidrug, AHFS DI (Adult and Pediatric) Online. American Society of Health-System Pharmacists, Inc. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 06/10/2025.

Cevimeline. UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 06/10/2025.

Evoxac Capsules (Daiichi Pharmaceutical Corporation). U.S. FDA. https://www.fda.gov. Accessed 06/10/2025.