Dosing & Uses
Dosage Forms & Strengths
tablet
- 5mg
- 7.5mg
Radiation-induced Xerostomia
5 mg PO q8hr; may titrate up to 10 mg PO q8hr; not to exceed 30 mg/day
Xerostomia Associated with SjÖgren's Syndrome
5 mg PO q6hr
Hepatic Impairment
Mild impairment (Child-Pugh score of 5-6): Dose reduction not necessary
Moderate impairment (Child-Pugh score of 7-9): 5 mg PO BID followed by adjustment based on therapeutic response and tolerability
Severe impairment (Child-Pugh score of 10-15): Not recommended
Safety & efficacy not established
Interactions
Interaction Checker
No Results

Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor

Adverse Effects
>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
Warnings
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 & Lactation
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.Pharmacology
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
Images
Patient Handout
Formulary
Adding plans allows you to compare formulary status to other drugs in the same class.
To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.
Adding plans allows you to:
- View the formulary and any restrictions for each plan.
- Manage and view all your plans together – even plans in different states.
- Compare formulary status to other drugs in the same class.
- Access your plan list on any device – mobile or desktop.