Cholinergic Agonist

Treatment of symptoms of dry mouth in patients with Sjögren's syndrome

C

There are no adequate or well-controlled studies in pregnant women. Use only if potential benefit justifies potential risk to the fetus. Excretion in breast milk is unknown/not recommended.

Known hypersensitivity to cevimeline; uncontrolled asthma; narrow-angle glaucoma; acute iritis; other conditions where miosis is undesirable

May alter cardiac conduction and/or heart rate; use caution in patients with significant cardiovascular disease, including angina, myocardial infarction, or conduction disturbances. Cevimeline has the potential to increase bronchial smooth muscle tone, airway resistance, and bronchial secretions; use with caution in patients with controlled asthma, COPD, or chronic bronchitis. May cause decreased visual acuity (particularly at night and in patients with central lens changes) and impaired depth perception. Patients should be cautioned about driving at night or performing hazardous activities in reduced lighting. May cause a variety of parasympathomimetic effects, which may be particularly dangerous in elderly patients; excessive sweating may lead to dehydration in some patients.

>10%:

Central nervous system: Headache (14%; placebo 20%)

Gastrointestinal: Nausea (14%), diarrhea (10%)

Respiratory: Rhinitis (11%), sinusitis (12%), upper respiratory infection (11%)

Miscellaneous: Increased sweating (19%)

1% to 10%:

Cardiovascular: Peripheral edema, chest pain, edema, palpitation

Central nervous system: Dizziness (4%), fatigue (3%), pain (3%), insomnia (2%), anxiety (1%), fever, depression, migraine, hypoesthesia, vertigo

Dermatologic: Rash (4%; placebo 6%), pruritus, skin disorder, erythematous rash

Endocrine & metabolic: Hot flashes (2%)

Gastrointestinal: Dyspepsia (8%; placebo 9%), abdominal pain (8%), vomiting (5%), excessive salivation (2%), constipation, salivary gland pain, dry mouth, sialoadenitis, gastroesophageal reflux, flatulence, ulcerative stomatitis, eructation, increased amylase, anorexia, tooth disorder

Genitourinary: Urinary tract infection (6%), vaginitis, cystitis

Hematologic: Anemia

Local: Abscess

Neuromuscular & skeletal: back pain (5%), arthralgia (4%), skeletal pain (3%), rigors (1%), hypertonia, tremor, myalgia, hyporeflexia, leg cramps

Ocular: Conjunctivitis (4%), abnormal vision, eye pain, eye abnormality, xerophthalmia

Otic: Ear ache, otitis media

Respiratory: Coughing (6%), bronchitis (4%), pneumonia, epistaxis

Miscellaneous: Flu-like syndrome, infection, fungal infection, allergy, hiccups

<1% (limited to important or life-threatening symptoms): Syncope, malaise, substernal chest pain, abnormal ECG, hypertension, hypotension, arrhythmia, T wave inversion, angina, myocardial infarction, pericarditis, pulmonary embolism, peripheral ischemia, thrombophlebitis, vasculitis, dysphagia, enterocolitis, gastric ulcer, gastrointestinal hemorrhage, ileus, melena, mucositis, esophageal stricture, esophagitis, peptic ulcer, stomatitis, tongue discoloration, tongue ulceration, hypothyroidism, thrombocytopenic purpura, thrombocytopenia, anemia, eosinophilia, granulocytopenia, leukopenia, leukocytosis, lymphadenopathy, cholelithiasis, increased transaminases, arthropathy, avascular necrosis (femoral head), bursitis, costochondritis, synovitis, tendonitis, tenosynovitis, coma, dyskinesia, dysphonia, aggravated multiple sclerosis, neuralgia, neuropathy, paresthesia, agitation, confusion, depersonalization, emotional lability, manic reaction, paranoia, somnolence, hyperkinesia, hallucination, fall, sepsis, bronchospasm, nasal ulcer, pleural effusion, pulmonary fibrosis, systemic lupus erythematosus, alopecia, dermatitis, eczema, photosensitivity reaction, dry skin, skin ulceration, bullous eruption, deafness, motion sickness, parosmia, taste perversion, blepharitis, cataract, corneal ulceration, diplopia, glaucoma, anterior chamber hemorrhage, retinal disorder, scleritis, tinnitus, epididymitis, menstrual disorder, genital pruritus, dysuria, hematuria, renal calculus, abnormal renal function, decreased urine flow, postural hypotension, aphasia, convulsions, paralysis, gingival hyperplasia, intestinal obstruction, bundle branch block, increased CPK, electrolyte abnormality, aggressive behavior, delirium, impotence, apnea, oliguria, urinary retention, lymphocytosis

Symptoms of toxicity may include headache, visual disturbances, lacrimation, sweating, gastrointestinal spasm, nausea, vomiting, diarrhea, A-V block, mental confusion, tremor, cardiac depression, bradycardia, tachycardia, or bronchospasm. Atropine may be of value as an antidote, and epinephrine may be required for bronchoconstriction. Additional treatment is supportive. The effect of hemodialysis is unknown.

CYP2D6 and CYP3A3/4 substrate

Decreased effect: Anticholinergic agents (atropine, TCA's, phenothiazines) may antagonize the effects of cevimeline

Store at 25°C (77°F)

Binds to muscarinic (cholinergic) receptors, causing an increase in secretion of exocrine glands (including salivary glands)

Distribution: V_d: 6 L/kg

Protein binding: <20%

Metabolism: Hepatic, via CYP2D6 and CYP3A3/4

Half-life: 5 hours

Time to peak: 1.5-2 hours

Elimination: In urine, as metabolites and unchanged drug

Adults: Oral: 30 mg 3 times/day

Elderly: No specific dosage adjustment is recommended; however, use caution when initiating due to potential for increased sensitivity

Take with or without food

No information available to require special precautions

No effects or complications reported

May be taken with or without food; take with food if medicine causes upset stomach. May cause decreased visual acuity (particularly at night and in patients with central lens changes) and impaired depth perception; patients should be cautioned about driving at night or performing hazardous activities in reduced lighting.

Capsule: 30 mg