Contraindications
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Known hypersensitivity to pilocarpine.
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Uncontrolled asthma.
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Patients in whom miosis is undesirable (e.g., those with acute iritis, angle-closure glaucoma).
Warnings/Precautions
Warnings
Cardiovascular Effects
Risk of altered cardiac conduction and/or heart rate. Patients with clinically important cardiovascular disease may be unable to compensate for transient changes in hemodynamics or heart rhythm induced by pilocarpine.
Use with caution and under close medical supervision in patients with a history of cardiovascular disease (e.g., angina pectoris, MI).
Ocular Effects
Blurred vision reported with ophthalmic formulations. May result in impaired depth perception and decreased visual acuity, especially at night and in patients with central lens changes; may impair ability to drive at night or perform hazardous activities in reduced lighting. (See Advice to Patients.)
Pulmonary Effects
May increase airway resistance, bronchial smooth muscle tone, and bronchial secretions. Use with caution and under close medical supervision in patients with controlled asthma, chronic bronchitis, or COPD.
General Precautions
Parasympathomimetic Effects
Possible exaggeration of parasympathomimetic effects (e.g., headache, visual disturbance, lacrimation, sweating, respiratory distress, GI spasm, nausea, vomiting, diarrhea, AV block, tachycardia, bradycardia, hypotension, hypertension, shock, mental confusion, cardiac arrhythmia, tremors).
Sweating is the most common adverse effect. Excessive sweating may cause dehydration. (See Advice to Patients.)
Biliary Effects
Use with caution in patients with known or suspected cholelithiasis or biliary tract disease.
Contraction of gallbladder or biliary smooth muscle could precipitate complications (e.g., cholecystitis, cholangitis, biliary obstruction) in patients with cholelithiasis.
Renal Effects
May increase ureteral smooth muscle tone, and theoretically cause renal colic or ureteral reflux in patients with nephrolithiasis.
CNS Effects
Dose-related CNS effects reported; use caution in patients with underlying cognitive or psychiatric disturbances.
Specific Populations
Pregnancy
No adequate and well-controlled studies in pregnant women; fetotoxicity and developmental abnormalities reported in animal studies.
Use during pregnancy only if potential benefit justifies potential risk to the fetus.
Lactation
Not known whether pilocarpine is distributed into human milk; discontinue nursing or the drug.
Pediatric Use
Safety and efficacy not established in children.
Geriatric Use
In patients ≥65 years of age with head and neck cancer, adverse effects generally similar to those observed in younger adults.
In patients ≥65 years of age with Sjögren syndrome, increased incidence of urinary frequency, diarrhea, and dizziness reported compared with younger patients.
Hepatic Impairment
Clearance decreased in patients with hepatic impairment. (See Special Populations under Pharmacokinetics.) Dosage reduction required in patients with moderate hepatic impairment. (See Hepatic Impairment under Dosage and Administration.)
Renal Impairment
Pharmacokinetics not substantially altered in patients with renal impairment (mean Clcr 25.4 mL/minute; range 9.8–40.8 mL/minute).
Common Adverse Effects
Radiation-induced dry mouth: Sweating, nausea, rhinitis, diarrhea, chills, flushing, urinary frequency, dizziness, asthenia, headache, dyspepsia, lacrimation, edema.
Dry mouth secondary to Sjögren syndrome: Sweating, urinary frequency, nausea, flushing, rhinitis, diarrhea, headache, flu syndrome, dyspepsia, dizziness.
