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Pilocarpine (Systemic)

Pronunciation

(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

Pharmacology

Binds to muscarinic (cholinergic) receptors, causing an increase in secretion of exocrine glands (such as salivary and sweat glands) and increase tone of smooth muscle in gastrointestinal and urinary tracts

Excretion

Urine

Onset of Action

20 minutes; Maximum effect: 1 hour

Time to Peak

Serum: 0.85 to 1.25 hours (increased to 1.47 hours with a high-fat meal)

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

Clearance decreased ~30% in patients with mild to moderate impairment, resulting in an increase in Cmax and half-life.

Special Populations: Gender

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

Use: Labeled Indications

Xerostomia: Treatment of symptoms of dry mouth from salivary gland hypofunction caused by radiotherapy for cancer of the head and neck; treatment of symptoms of dry mouth in patients with Sjögren syndrome.

Contraindications

Hypersensitivity to pilocarpine or any component of the formulation; uncontrolled asthma; when miosis is undesirable (eg, acute iritis, angle-closure glaucoma)

Dosing: Adult

Xerostomia: Oral:

Associated with head and neck cancer: Initial: 5 mg 3 times daily; may titrate dose based on response and tolerability; usual dosage range: 15 to 30 mg/day; maximum: 10 mg/dose

Sjögren syndrome: 5 mg 4 times daily

Dosing: Geriatric

Refer to adult dosing.

Dosing: Renal Impairment

There are no dosage adjustments provided in the manufacturer’s labeling.

Dosing: Hepatic Impairment

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

Moderate impairment (Child-Pugh score 7 to 9): Initial: 5 mg twice daily; adjust dose based on response and tolerability.

Severe impairment (Child-Pugh score 10 to 15): Use is not recommended.

Administration

Avoid administering with high-fat meal. Ensure adequate water intake (dehydration may develop with use).

Storage

Store at 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

>10%:

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

Warnings/Precautions

Disease-related concerns:

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

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

• Hepatic impairment: Use with caution in patients with moderate impairment; dosage adjustment recommended; use is not recommended in patients with severe impairment.

• Nephrolithiasis: Use caution in patients with a history of nephrolithiasis; may induce smooth muscle spasms, precipitating renal colic or ureteral reflux in patients with nephrolithiasis.

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

Pregnancy Risk Factor

C

Pregnancy Considerations

Adverse events have been 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, loss of strength and energy, chills, rhinorrhea, or polyuria. Have patient report immediately to prescriber severe dizziness, passing out, shortness of breath, excessive weight gain, swelling of arms or legs, tachycardia, bradycardia, abnormal heartbeat, severe nausea, severe vomiting, vision changes, eye pain, severe eye irritation, severe headache, sweating a lot, severe diarrhea, confusion, or tremors (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.

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