Pronunciation:

(pye loe KAR peen)

U.S. Brand Names:

Synonyms:

Generic Available:

Canadian Brand Names:

Use:

Ophthalmic: Management of chronic simple glaucoma, chronic and acute angle-closure glaucoma

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

Use - Unlabeled/Investigational:

Pregnancy Risk Factor:

Lactation:

Contraindications:

Warnings/Precautions:

Ophthalmic products: May cause decreased visual acuity, especially at night or with reduced lighting.

Oral tablets: Use caution with controlled asthma, chronic bronchitis or COPD; may increase airway resistance, bronchial smooth muscle tone, and bronchial secretions. Use caution with cholelithiasis, biliary tract disease, nephrolithiasis; adjust dose with moderate hepatic impairment.

Adverse Reactions:

Ophthalmic: Frequency not defined:

Cardiovascular: Hypertension, tachycardia

Gastrointestinal: Diarrhea, nausea, salivation, vomiting

Ocular: Burning, ciliary spasm, conjunctival vascular congestion, corneal granularity (gel 10%), lacrimation, lens opacity, myopia, retinal detachment, supraorbital or temporal headache, visual acuity decreased

Respiratory: Bronchial spasm, pulmonary edema

Miscellaneous: Diaphoresis

Oral (frequency varies by indication and dose):

>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%: Abnormal dreams, abnormal thinking, alopecia, angina pectoris, anorexia, anxiety, aphasia, appetite increased, arrhythmia, arthralgia, arthritis, bilirubinemia, body odor, bone disorder, bradycardia, breast pain, bronchitis, cataract, cholelithiasis, colitis, confusion, contact dermatitis, cyst, deafness, depression, dry eyes, dry mouth, dry skin, dyspnea, dysuria, ear pain, ECG abnormality, eczema, emotional lability, eructation, erythema nodosum, esophagitis, exfoliative dermatitis, eye hemorrhage, eye pain, gastritis, gastroenteritis, gastrointestinal disorder, gingivitis, glaucoma, hematuria, hepatitis, herpes simplex, hiccup, hyperkinesias, hypesthesia, hypoglycemia, hypotension, hypothermia, insomnia, intracranial hemorrhage, laryngismus, laryngitis, leg cramps, leukopenia, liver function test abnormal, lymphadenopathy, mastitis, melena, menorrhagia, metrorrhagia, migraine, moniliasis, myasthenia, MI, neck pain, photosensitivity reaction, nervousness, ovarian disorder, pancreatitis, paresthesia, parotid gland enlargement, peripheral edema, platelet abnormality, pneumonia, pyuria, salivary gland enlargement, salpingitis, seborrhea, skin ulcer, speech disorder, sputum increased, stridor, syncope, taste loss, tendon disorder, tenosynovitis, thrombocythemia, thrombocytopenia, thrombosis, tongue disorder, twitching, urethral pain, urinary impairment, urinary urgency, vaginal hemorrhage, vaginal moniliasis, vesiculobullous rash, WBC abnormality, yawning

Overdosage/Toxicology:

Drug Interactions:

Concurrent use with beta-blockers may cause conduction disturbances; pilocarpine may antagonize the effects of anticholinergic drugs

Ethanol/Nutrition/Herb Interactions:

Stability:

Gel: Store at room temperature of 2°C to 27°C (36°F to 80°F). Do not freeze; avoid excessive heat.

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

Mechanism of Action:

Pharmacodynamics/Kinetics:

Onset of action:

Ophthalmic: Miosis: 10-30 minutes; Intraocular pressure reduction: 1 hour

Oral: 20 minutes

Duration:

Ophthalmic: Miosis: 4-8 hours; Intraocular pressure reduction: 4-12 hours

Oral: 3-5 hours

Half-life elimination: Oral: 0.76-1.35 hours; increased with hepatic impairment

Excretion: Urine

Dosage:

Ophthalmic:

Glaucoma:

Solution: Instill 1-2 drops up to 6 times/day; adjust the concentration and frequency as required to control elevated intraocular pressure

Gel: Instill 0.5" ribbon into lower conjunctival sac once daily at bedtime

To counteract the mydriatic effects of sympathomimetic agents (unlabeled use): Solution: Instill 1 drop of a 1% solution in the affected eye

Oral: Xerostomia:

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

Sj&ouml;gren's syndrome: 5 mg 4 times/day

Dosage adjustment in hepatic impairment: Oral: Patients with moderate impairment: 5 mg 2 times/day regardless of indication; adjust dose based on response and tolerability. Do not use with severe impairment (Child-Pugh score 10-15).

Administration:

Oral: Avoid administering with high-fat meal. Fat decreases the rate of absorption, maximum concentration, and increases the time it takes to reach maximum concentration.

Ophthalmic: If both solution and gel are used, the solution should be applied first, then the gel at least 5 minutes later. Following administration of the solution, finger pressure should be applied on the lacrimal sac for 1-2 minutes.

Monitoring Parameters:

Patient Education:

Ophthalmic: Wash hands before using. Do not let tip of applicator touch eye; do not contaminate tip of applicator (may cause eye infection, eye damage, or vision loss). Sit or lie down. Open eye, look at ceiling, and instill prescribed amount of solution. Do not blink for 30 seconds, close eye and roll eye in all directions, and apply gentle pressure to inner corner of eye for 1-2 minutes. Temporary stinging or blurred vision may occur. You may experience altered dark adaptation; use caution when driving at night or in poorly lit environments. Report persistent pain, redness, burning, double vision, or severe headache. Pregnancy/breast-feeding precautions: Inform prescriber if you are pregnant. Breast-feeding is not recommended.

Nursing Implications:

Dental Health: Effects on Dental Treatment:

Dental Health: Vasoconstrictor/Local Anesthetic Precautions:

Mental Health: Effects on Mental Status:

Mental Health: Effects on Psychiatric Treatment:

Oncology: Emetic Potential:

Dosage Forms:

Gel, ophthalmic, as hydrochloride (Pilopine HS®): 4% (3.5 g) [contains benzalkonium chloride]

Solution, ophthalmic, as hydrochloride: 1% (15 mL); 2% (15 mL); 4% (15 mL); 6% (15 mL) [may contain benzalkonium chloride]

Isopto® Carpine: 1% (15 mL); 2% (15 mL, 30 mL); 4% (15 mL, 30 mL); 6% (15 mL); 8% (15 mL) [contains benzalkonium chloride]

Pilocar®: 0.5% (15 mL); 1% (1 mL, 15 mL); 2% (1 mL, 15 mL); 3% (15 mL); 4% (1 mL, 15 mL); 6% (15 mL) [contains benzalkonium chloride]

Tablet, as hydrochloride (Salagen®): 5 mg, 7.5 mg

International Brand Names: