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Pilocarpine (Systemic)



(pye loe KAR peen)

Index Terms

  • Pilocarpine HCl
  • Pilocarpine Hydrochloride

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Tablet, Oral, as hydrochloride:

Salagen: 5 mg

Salagen: 7.5 mg [contains fd&c blue #2 aluminum lake]

Generic: 5 mg, 7.5 mg

Brand Names: U.S.

  • Salagen

Pharmacologic Category

  • Cholinergic Agonist



Onset of Action

20 minutes; Maximum effect: 1 hour

Duration of Action

3 to 5 hours

Half-Life Elimination

0.76 to 1.35 hours; Mild to moderate hepatic impairment: 2.1 hours

Special Populations: Hepatic Function Impairment

In patients with mild to moderate hepatic function impairment, pilocarpine Cl is decreased, resulting in an increase in the pilocarpine Cmax and half-life.

Special Populations: Gender

Elderly women had Cmax and AUC approximately twice that of elderly and younger men.

Use: Labeled Indications

Symptomatic treatment of xerostomia caused by salivary gland hypofunction resulting from radiotherapy for cancer of the head and neck or Sjögren's syndrome


Hypersensitivity to pilocarpine or any component of the formulation; uncontrolled asthma; angle-closure glaucoma, severe hepatic impairment

Dosing: Adult

Xerostomia: Oral:

Following head and neck cancer: 5 mg 3 times/day, titration up to 10 mg 3 times/day may be considered for patients who have not responded adequately; do not exceed 2 tablets/dose

Sjögren's syndrome: 5 mg 4 times/day

Dosing: Geriatric

Refer to adult dosing.

Dosing: Renal Impairment

No dosage adjustment necessary.

Dosing: Hepatic Impairment

Mild impairment (Child-Pugh score 5-6): No dosage adjustment necessary.

Moderate impairment (Child-Pugh score 7-9): 5 mg twice daily regardless of indication; adjust dose based on response and tolerability

Severe impairment (Child-Pugh score >10): Not recommended.


Avoid administering with high-fat meal.

Dietary Considerations

Avoid taking with a high-fat meal.


Store at controlled room temperature of 15°C to 30°C (59°F to 86°F).

Drug Interactions

Acetylcholinesterase Inhibitors: May enhance the adverse/toxic effect of Cholinergic Agonists. Monitor therapy

Beta-Blockers: May enhance the adverse/toxic effect of Cholinergic Agonists. Of particular concern are the potential for cardiac conduction abnormalities and bronchoconstriction. Management: Administer these agents in combination with caution, and monitor for conduction disturbances. Avoid methacholine with any beta blocker due to the potential for additive bronchoconstriction. Monitor therapy

Cimetropium: Cholinergic Agonists may diminish the anticholinergic effect of Cimetropium. Monitor therapy

Adverse Reactions


Cardiovascular: Flushing (8% to 13%)

Central nervous system: Chills (3% to 15%), dizziness (5% to 12%), headache (11%)

Gastrointestinal: Nausea (6% to 15%)

Genitourinary: Urinary frequency (9% to 12%)

Neuromuscular & skeletal: Weakness (2% to 12%)

Respiratory: Rhinitis (5% to 14%)

Miscellaneous: Diaphoresis (29% to 68%)

1% to 10%:

Cardiovascular: Edema (<1% to 5%), facial edema, hypertension (3%), palpitation, tachycardia

Central nervous system: Pain (4%), fever, somnolence

Dermatologic: Pruritus, rash

Gastrointestinal: Diarrhea (4% to 7%), dyspepsia (7%), vomiting (3% to 4%), constipation, flatulence, glossitis, salivation increased, stomatitis, taste perversion

Genitourinary: Vaginitis, urinary incontinence

Neuromuscular & skeletal: Myalgias, tremor

Ocular: Lacrimation (6%), amblyopia (4%), abnormal vision, blurred vision, conjunctivitis

Otic: Tinnitus

Respiratory: Cough increased, dysphagia, epistaxis, sinusitis

Miscellaneous: Allergic reaction, voice alteration

<1% (Limited to important or life-threatening): Abnormal dreams, alopecia, angina pectoris, anorexia, anxiety, arrhythmia, body odor, bone disorder, cholelithiasis, colitis, confusion, dry eyes, dry mouth, ECG abnormality, myasthenia, photosensitivity reaction, nervousness, pancreatitis, paresthesia, salivary gland enlargement, sputum increased, taste loss, tongue disorder, urinary impairment, urinary urgency, yawning


Disease-related concerns:

• Cardiovascular disease: Use with caution in patients with cardiovascular disease; may have difficulty compensating for transient changes in hemodynamics or rhythm induced by pilocarpine.

• Cholelithiasis: Use caution with cholelithiasis or biliary tract disease.

• Hepatic impairment: Adjust dose with moderate hepatic impairment; contraindicated in severe impairment.

• Nephrolithiasis: Use caution in patients with a history of nephrolithiasis.

• Respiratory disorders: Use caution with controlled asthma, chronic bronchitis, or COPD; may increase airway resistance, bronchial smooth muscle tone, and bronchial secretions.

Monitoring Parameters

Intraocular pressure, funduscopic exam, visual field testing

Pregnancy Risk Factor


Pregnancy Considerations

Adverse events were observed in some animal reproduction studies.

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience flushing, sweating a lot, nausea, or polyuria. Have patient report immediately to prescriber severe dizziness, passing out, shortness of breath, excessive weight gain, swelling of arms or legs, tachycardia, arrhythmia, severe nausea, severe vomiting, vision changes, eye pain, severe eye irritation, severe headache, or severe loss of strength and energy (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.