Cevimeline


Concise Prescribing Info
Indications/Uses
Dry mouth associated with Sjogren syndrome.
Dosage/Direction for Use
Adult : PO 30 mg tid.
Dosage Details
Oral
Dry mouth associated with Sjogren’s syndrome
Adult: 30 mg tid.
Contraindications
Uncontrolled asthma, acute iritis, narrow-angle glaucoma.
Special Precautions
Patients with cardiovascular disease (e.g. MI, angina pectoris), controlled asthma, chronic bronchitis, COPD, history of nephrolithiasis or cholelithiasis. Pregnancy and lactation. CYP2D6 poor metabolisers.
Adverse Reactions
Significant: Parasympathomimetic effects (e.g. AV block, bradycardia, cardiac arrhythmia, hypotension, lacrimation, respiratory distress, tachycardia, tremor, vomiting).
Cardiac disorders: Palpitation, chest pain.
Gastrointestinal disorders: Nausea, abdominal pain, diarrhoea, salivary gland pain, excessive salivation.
General disorders and administration site conditions: Hyperhidrosis, back pain, fatigue, fever, malaise.
Metabolism and nutrition disorders: Loss of appetite.
Musculoskeletal and connective tissue disorders: Arthralgia, skeletal pain.
Nervous system disorders: Headache.
Psychiatric disorders: Insomnia.
Renal and urinary disorders: Frequent urination, UTI.
Respiratory, thoracic and mediastinal disorders: Rhinitis, sinusitis, upper respiratory tract infection, cough, bronchitis.
Skin and subcutaneous tissue disorders: Rash.
Vascular disorders: Hot flushes.
Patient Counseling Information
This drug may cause visual disturbances (e.g. blurred vision, decreased visual acuity, impaired depth perception), if affected, do not drive or operate machinery.
Drug Interactions
May increase risk of conduction disturbances and bronchoconstriction with concomitant use of β-adrenergic agonists. Additive effects with parasympathomimetic agents. Decreased metabolism and increased risk of adverse effects with inhibitors of CYP2D6 and CYP3A3/4.
Food Interaction
Decreased rate and extent of absorption with food.
Action
Description: Cevimeline is a cholinergic agonist that selectively binds to muscarinic receptors resulting in increased secretion of exocrine glands (e.g. salivary, sweat glands) and increased smooth muscle tone in gastrointestinal and urinary tracts.
Pharmacokinetics:
Absorption: Rapidly absorbed from the gastrointestinal tract. Decreased rate and extent of absorption with food. Time to peak plasma concentration: 1.5-2 hours.
Distribution: Volume of distribution: Approx 6 L/kg. Plasma protein binding: <20%.
Metabolism: Metabolised in the liver by CYP2D6 and CYP3A3/4 to cis and trans-sulfoxide, glucuronic acid conjugate, and N-oxide metabolites.
Excretion: Mainly via urine (84% in 24 hours; 97% in 7 days); faeces (approx 0.5% in 7 days). Elimination half-life: 5±1 hour.
Chemical Structure

Chemical Structure Image
Cevimeline

Source: National Center for Biotechnology Information. PubChem Database. Evoxac, CID=83898, https://pubchem.ncbi.nlm.nih.gov/compound/Evoxac (accessed on Mar. 25, 2020)

Storage
Store between 20-25°C.
ATC Classification
N07AX03 - cevimeline ; Belongs to the class of other parasympathomimetics.
References
Weber J, Keating GM. Cevimeline. Adis Data Information BV. 2008;68(12):1691-1698. Accessed 15/11/2019

Annotation of FDA Label for Cevimeline and CYP2D6. Pharmacogenomics Knowledgebase (PharmGKB). https://www.pharmgkb.org/. Accessed 15/11/2019.

Anon. Cevimeline. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 15/11/2019.

Anon. CYP2D6-Cevimeline (Pharmacogenomics). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 15/11/2019.

Buckingham R (ed). Cevimeline Hydrochloride. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 15/11/2019.

Cevimeline Capsule (Lupin Pharmaceuticals, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 15/11/2019.

Disclaimer: This information is independently developed by MIMS based on Cevimeline from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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