Dosing and uses of Evoxac (cevimeline)
Adult dosage forms and strengths
capsule
- 30mg
Xerostomia
Indicated for xerostomia in patients with Sjogren's syndrome
30 mg PO TId
Pediatric dosage forms and strengths
Safety and efficacy not established
Evoxac (cevimeline) adverse (side) effects
>10%
Sweating (18.7%)
Nausea (13.8%)
Rhinitis (11.2%)
1-10%
Vomiting (4.6%)
Frequency not defined
Dizziness
Tremor
Bronchitis
Pharyngitis
Dyspepsia
Abdominal pain
Urinary tract infection
Back pain
Arthralgia
Warnings
Contraindications
Uncontrolled asthma, conditions in which miosis is undesirable (eg, narrow-angle glaucoma, acute iritis)
Hypersensitivity
Cautions
Controlled asthma, CVD, chronic bronchitis, COPD, history of nephrolithiasis
Pregnancy and lactation
Pregnancy category: C
Lactation: unknown whether distributed into breast milk, avoid or do not nurse
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Evoxac (cevimeline)
Mechanism of action
Muscarinic receptor agonist (quinuclidine derivative of acetylcholine), exhibits high binding affinity for muscarinic M3 receptors on lacrimal & salivary gland epithelium: incr salivation
Absorption
Bioavailability: Rapid absorption, food decrease rate of absorption
Peak Plasma Time: 1.5-2 hr
Distribution
Protein Bound: 20%
Vd: 6 L/kg
Metabolism
Metabolized by CYP3A4 and CYP2D6
Metabolites: cis- & trans-sulfoxide (inactive), glucuronic acid conjugate (inactive), N-Oxide (inactive)
Elimination
Half-Life: ~5 hr
Excretion: Urine 97%; feces 0.5%
