Pilocarpine Hydrochloride

Brand names: Salagen
Drug class: Antineoplastic Agents

Usage of Pilocarpine Hydrochloride

Radiation-induced Dry Mouth

Symptomatic treatment of radiation-induced dry mouth (xerostomia) in patients with head and neck cancer.

Dry Mouth Secondary to Sjögren Syndrome

Symptomatic treatment of dry mouth in patients with Sjögren syndrome.

There are few comparative studies of pilocarpine and cevimeline (a similar muscarinic agonist). Although both drugs can increase salivary flow and improve symptoms of dry mouth, adverse effects may differ based on differences in selectivity and affinity for muscarinic receptors. (See Actions.)

Relate drugs

How to use Pilocarpine Hydrochloride

Administration

Oral Administration

Administer orally 3–4 times daily.

Dosage

Available as pilocarpine hydrochloride; dosage expressed in terms of the salt.

Adults

Radiation-induced Dry Mouth Oral

Initially, 5 mg 3 times daily; titrate dosage based on therapeutic response and tolerance.

Usual dosage range is 15–30 mg daily given in divided doses (not to exceed 10 mg per dose).

Adverse effects are dose related; use lowest effective and tolerated dosage for maintenance therapy.

At least 12 weeks of continuous therapy may be necessary to achieve therapeutic benefit.

Dry Mouth Secondary to Sjögren Syndrome Oral

Recommended dosage is 5 mg 4 times daily. To minimize incidence of sweating, some clinicians recommend initiating therapy at a low dosage (e.g., 2 mg once or twice daily), then gradually increasing up to 5 mg 3 or 4 times daily.

In clinical studies, a therapeutic effect was observed by 6 weeks of treatment.

Prescribing Limits

Adults

Radiation-induced Dry Mouth Oral

Do not exceed 10 mg per dose.

Special Populations

Hepatic Impairment

Mild hepatic impairment: No dosage adjustment required.

Moderate hepatic impairment: Reduce initial dosage to 5 mg twice daily regardless of indication; adjust subsequent dosage based on response and tolerability. (See Hepatic Impairment under Cautions.)

Severe hepatic impairment: Use not recommended.

Renal Impairment

Manufacturer makes no specific dosage recommendations.

Geriatric Patients

Manufacturer makes no specific dosage recommendations.

Warnings

Contraindications

  • Known hypersensitivity to pilocarpine.
  • Uncontrolled asthma.
  • 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.

    What other drugs will affect Pilocarpine Hydrochloride

    Specific Drugs

    Drug

    Interaction

    Comments

    Antimuscarinic agents (e.g., atropine, ipratropium)

    Potential for antagonism of antimuscarinic effects

    β-Adrenergic blocking agents

    Possible cardiac conduction disturbances

    Caution is advised if used concomitantly

    Parasympathomimetic agents

    Possible additive effects

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