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Cevimeline !

A muscarinic agonist taken by mouth to increase saliva in people with dry mouth from Sjögren disease.

Updated 2026-11-01

No structure of cevimeline bound to its receptor exists. The figure shows iperoxo, a potent research agonist, in the acetylcholine (orthosteric) pocket of the active human M3 muscarinic receptor, the subtype on glands, the eye and the bladder that cevimeline stimulates.

Target in 3D: Muscarinic M1 and M3 receptors. PDB structure 8E9Z (RCSB PDB, public domain). View the structure at RCSB PDB

Mechanism of action

Cevimeline preferentially activates M1 and M3 muscarinic receptors on salivary and tear glands, producing a long-lasting increase in saliva. Sjögren disease is an autoimmune disease that damages these glands; the drug works only while some gland tissue still functions.

  1. Activates M1 and M3 receptors on salivary glands
  2. Gland cells secrete more saliva
  3. Dry mouth eases while gland tissue remains

Pharmacokinetics

Absorption
Rapidly absorbed by mouth; food slows absorption
Metabolism
In the liver by CYP2D6 and CYP3A4
Half-life
About 5 hours

Indications

Adverse effects

Common

  • Excessive sweating
  • Nausea
  • Runny nose
  • Diarrhoea
  • Excess salivation and urinary frequency

Contraindications

  • Uncontrolled asthma
  • When miosis is undesirable: acute iritis or narrow-angle glaucoma
  • Hypersensitivity to cevimeline

Key interactions

Beta blockers
Possible heart conduction disturbances
CYP2D6 and CYP3A4 inhibitors
Slower metabolism and more side effects; caution also in people who lack CYP2D6 activity
Antimuscarinic drugs
Opposite effects

What is monitored

  • Heart rate and rhythm in heart disease
  • Breathing in asthma or COPD
  • Hydration if sweating is heavy

Administration and safety

  • Taken by mouth; food slows its absorption
  • Extra water is advised if sweating is heavy

Nursing care

  • Warn about blurred vision at night and driving
  • Teach to drink extra water if sweating heavily
  • Ask about asthma, glaucoma and heart disease before starting

Pregnancy and breastfeeding

No adequate studies in pregnant women; used only if the benefit justifies the risk.

Test yourself

Think of the answer, then tap the question to see it.

Which receptor subtypes does cevimeline prefer?

M1 and M3 muscarinic receptors.

Why must some salivary gland tissue remain for cevimeline to work?

It stimulates existing gland cells; it does not replace destroyed glands.

Which eye conditions are contraindications?

Acute iritis and narrow-angle glaucoma, where miosis is undesirable.

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← Back to the class: Muscarinic (cholinergic) agonists

Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.

Sources: DailyMed - CEVIMELINE HYDROCHLORIDE capsule (DailyMed (U.S. National Library of Medicine), 2026); Cevimeline: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2026); Goodman & Gilman's The Pharmacological Basis of Therapeutics, 14th ed., ch. 11 (McGraw Hill, 2023).

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Representative model, for educational purposes only.