Cevimeline

Mechanism-of-action class: Cholinergic Muscarinic Agonists.

• Cevimeline hydrochloride capsules are indicated for the treatment of symptoms of dry mouth in patients with Sjögren’s Syndrome.

• 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.contraindicated

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.

Cardiovascular Disease Cevimeline can potentially alter cardiac conduction and/or heart rate. Patients with significant cardiovascular disease may potentially be unable to compensate for transient changes in hemodynamics or rhythm induced by cevimeline. Cevimeline should be used with caution and under close medical supervision in patients with a history of cardiovascular disease evidenced by angina pectoris or myocardial infarction. Pulmonary Disease Cevimeline can potentially increase airway resistance, bronchial smooth muscle tone, and bronchial secretions. Cevimeline should be administered with caution and with close medical supervision to patients with controlled asthma, chronic bronchitis, or chronic obstructive pulmonary disease. Ocular Ophthalmic formulations of muscarinic agonists have been reported to cause visual blurring which may result in decreased visual acuity, especially at night and in patients with central lens changes, and to cause impairment of depth perception. Caution should be advised while driving at night or performing hazardous activities in reduced lighting.

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. The following adverse events associated with muscarinic agonism were observed in the clinical trials of cevimeline in Sjögren’s syndrome patients: Adverse Event Cevimeline 30 mg (tid) n n is the total number of patients exposed to the dose at any time during the study. = 533 Placebo (tid) n = 164 Excessive Sweating 18.7% 2.4% Nausea 13.8% 7.9% Rhinitis 11.2% 5.4% Diarrhea 10.3% 10.3% Excessive Salivation 2.2% 0.6% Urinary Frequency 0.9% 1.8% Asthenia 0.5% 0.0% Flushing 0.3% 0.6% Polyuria 0.1% 0.6% In addition, the following adverse events (≥ 3% incidence) were reported in the Sjögren’s clinical trials: Adverse Event Cevimeline 30 mg (tid) n n is the total number of patients exposed to the dose at any time during the study.

MANAGEMENT OF OVERDOSE Management of the signs and symptoms of acute overdosage should be handled in a manner consistent with that indicated for other muscarinic agonists: general supportive measures should be instituted. If medically indicated, atropine, an anti-cholinergic agent, may be of value as an antidote for emergency use in patients who have had an overdose of cevimeline. If medically indicated, epinephrine may also be of value in the presence of severe cardiovascular depression or bronchoconstriction. It is not known if cevimeline is dialyzable.

• Jan 11, 2000NDANDA020989Cosette
• Jul 8, 2013ANDAANDA091591Hikma
• Jun 4, 2014ANDAANDA203775Rising
• Dec 30, 2016ANDAANDA204746Novel Labs Inc
• Apr 6, 2023ANDAANDA216682Rubicon Research
• Apr 18, 2023ANDAANDA215056Aurobindo Pharma
• Nov 8, 2023ANDAANDA218290Bionpharma
• Sep 20, 2024ANDAANDA206808Macleods Pharms Ltd

1. 1Drug Ineffective2077.8%
2. 2Headache1726.5%
3. 3Nausea1636.2%
4. 4Diarrhoea1616.1%
5. 5Fatigue1535.8%
6. 6Dyspnoea1375.2%
7. 7Pain1274.8%
8. 8Arthralgia1184.5%
9. 9Fall1084.1%
10. 10Off Label Use1074.1%
11. 11Malaise973.7%
12. 12Dizziness943.6%
13. 13Vomiting933.5%
14. 14Pneumonia873.3%
15. 15Dry Mouth863.3%

The 6 most recently updated of 6 ClinicalTrials.gov registrations naming Cevimeline as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Evaluation of BTV100 in Subjects With Dry Eye Disease
  Recruiting · Phase 2 · Interventional · 120 enrolled · BioTheraVision, Inc.
  NCT06543303updated 2025-01-22
• Efficacy of Cevimeline Versus Pilocarpine in the Secretion of Saliva
  Completed · Interventional · 15 enrolled · University of Kentucky
  NCT01690052updated 2018-06-04
• Crossover Bioequivalence Study of Cevimeline 30 mg Capsules Under Fasted Conditions
  Completed · Early phase 1 · Interventional · 26 enrolled · Roxane Laboratories
  NCT01903122updated 2018-01-23
• Crossover Bioequivalence Study of Cevimeline 30 mg Capsules Under Fed Conditions
  Completed · Early phase 1 · Interventional · 27 enrolled · Roxane Laboratories
  NCT01903109updated 2018-01-23
• Study of the Effectiveness of Cevimeline on Oral Health in Patients With Radiation Induced Xerostomia
  Completed · Phase 4 · Interventional · 54 enrolled · American Academy of Otolaryngology-Head and Neck Surgery Foundation
  NCT00466388updated 2014-05-22
• Cevimeline in Treating Patients With Dry Mouth Caused by Radiation Therapy for Head and Neck Cancer
  Completed · Phase 3 · Interventional · Daiichi Sankyo
  NCT00017511updated 2012-05-16

CPIC-curated drug–gene pairs for Cevimeline. Levels describe the strength of curated evidence and guideline status — never a recommendation to test or to adjust therapy.

• CYP2D6CPIC B/C (provisional)FDA label: Actionable PGx

Frequently asked questions

How does Cevimeline work?

Mechanism-of-action class: Cholinergic Muscarinic Agonists.

What is Cevimeline used for?

According to FDA labeling, Cevimeline carries indications including: Cevimeline hydrochloride capsules are indicated for the treatment of symptoms of dry mouth in patients with Sjögren’s Syndrome.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Cevimeline?

Cevimeline is classified as Other parasympathomimetics, Cholinergic Receptor Agonist, Cholinergic Muscarinic Agonists, Pupillary Constriction, Salivation Stimulation.

What are the brand names for Cevimeline?

Cevimeline is marketed under brand names including Evoxac.

What are the contraindications for Cevimeline?

Cevimeline labeling lists contraindications including: 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.. Always consult the full prescribing information and a clinician.