pilocarpine (Rx)

>10%

Sweating (29%)

Headache (11%)

Flushing (8-13%)

Dizziness (5-12%)

Chills (3-15%)

Nausea (6-15%)

Urinary frequency (9-12%)

Rhinitis (5-14%)

Diaphoresis (29-68%)

1-10%

Pain (4%)

Asthenia (>3%)

Dyspepsia (7%)

Vomiting (3-4%)

Hypertension (3%)

Lacrimation (6%)

Amblyopia (4%)

Frequency Not Defined

Confusion

Hypotension

Bradycardia

Tachycardia

Increased airway resistance

Diarrhea

Bladder tightness

Decreased visual acuity

Contraindications

Uncontrolled asthma, anterior eye inflammation, any time miosis in undesirable (eg, narrow-angle glaucoma, acute iritis)

Hypersensitivity

Cautions

Patients with significant cardiovascular disease may be unable to compensate for transient changes in hemodynamics or rhythm induced by therapy; pulmonary edema has been reported as a complication of pilocarpine toxicity from high ocular doses given for acute angle-closure glaucoma; pilocarpine should be administered with caution in and under close medical supervision of patients with significant cardiovascular disease

Therapy has been reported to increase airway resistance, bronchial

smooth muscle tone, and bronchial secretions; therapy should be administered with caution to and under close medical supervision in patients with controlled asthma, chronic

bronchitis, or chronic obstructive pulmonary disease requiring pharmacotherapy

Pilocarpine toxicity is characterized by exaggeration of parasympathomimetic

effects, which may include: headache, visual disturbance, lacrimation, sweating, respiratory distress, gastrointestinal spasm, nausea, vomiting, diarrhea, atrioventricular block, tachycardia,

bradycardia, hypotension, hypertension, shock, mental confusion, cardiac arrhythmia, and tremors

Dose-related cardiovascular pharmacologic effects of pilocarpine include hypotension, hypertension, bradycardia, and tachycardia

Drug should be administered with caution to patients with known or suspected cholelithiasis or biliary tract disease; contractions of gallbladder or biliary smooth muscle could precipitate

complications including cholecystitis, cholangitis, and biliary obstruction

Pilocarpine may increase ureteral smooth muscle tone and could theoretically precipitate renal colic (or "ureteral reflux"), particularly in patients with nephrolithiasis

Cholinergic agonists may have dose-related central nervous system effects; this should be considered when treating patients with underlying cognitive or psychiatric disturbances

Pregnancy Category: C

Lactation: unknown if drug is distributed into breast milk; use caution

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.

Mechanism of Action

Cholinergic parasympathomimetic with predominant muscarinic action; increases secretion of exocrine glands (sweat, lacrimal, salivary, intestinal, pancreatic glands, and mucous cells of the respiratory tract may be stimulated

Tone and mobility of gallbladder, biliary duct, and urinary tract may be increased

Pharmacokinetics

Half-Life: 0.76-1.35 hr

Onset: 20 min (initial response for xerostomia)

Duration: 3-5 hr (single dose), >10 hr (multiple dose)

Peak plasma time: 0.85-1.25 hr

Bioavailability: High fat meal decreases rate & extent of absorption

Protein bound: None