Dosing and uses of Pilocarpine PO, Salagen (pilocarpine)
Radiation-induced Xerostomia
5 mg PO TID; may titrate up to 10 mg PO TID; not to exceed 30 mg/d
Xerostomia Associated with SjÖgren's Syndrome
5 mg PO QId
Moderate hepatic insufficiency, regardless of indication
5 mg PO BID, then adjust dose according to treatment efficacy and patient's tolerability
Severe hepatic insufficiency (Child-Pugh score of 10-15)
Not recommended
Pediatric dosage forms and strengths
Not recommended
Pilocarpine PO, Salagen (pilocarpine) adverse (side) effects
>10%
Sweating (29%)
Headache (15%)
Flushing (8-13%)
Chills (3-15%)
1-10%
Nervousness (10%)
Nausea (6%)
Dizziness (>3%)
Asthenia (>3%)
Frequency not defined
Confusion
Hypotension
Hypertension
Bradycardia
Tachycardia
Increased airway resistance
Abdominal cramping
Diarrhea
Urinary frequency
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
CVD, cholelithiasis, biliary tract dz, COPD, chronic bronchitis, concomitant use of beta adrenergic agonist, renal insufficiency, PUD, Parkinson's, hyperthyroidism, urinary tract obstruction
May require up to 12 wk to determine if head/neck cancer pts will respond
Pregnancy and 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 of Pilocarpine PO, Salagen (pilocarpine)
Half-Life: 0.76-1.35 hr
Onset: initial response for xerostomia: 20 min
Duration: 3-5 hr (single dose), >10 hr (multiple dose)
Peak Plasma Time: 0.85-1.25 hr
Bioavailability: high fat meal decr rate & extent of absorption
Protein Bound: none
Mechanism of action
Cholinergic parasympathomimetic, incr salivation
