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Pilocarpine
Pronunciation
U.S. Brand Names
Generic Available
Canadian Brand Names
Synonyms
Pharmacological Index
Use
Pregnancy Risk Factor
Contraindications
Warnings/Precautions
Adverse Reactions
Overdosage/Toxicology
Drug Interactions
Stability
Mechanism of Action
Pharmacodynamics/Kinetics
Usual Dosage
Dietary Considerations
Administration
Monitoring Parameters
Mental Health: Effects on Mental Status
Mental Health: Effects on Psychiatric Treatment
Dental Health: Local Anesthetic/Vasoconstrictor Precautions
Dental Health: Effects on Dental Treatment
Patient Information
Nursing Implications
Dosage Forms
References

Pronunciation
(pye loe KAR peen)

U.S. Brand Names
Adsorbocarpine® Ophthalmic; Akarpine® Ophthalmic; Isopto® Carpine Ophthalmic; Ocusert Pilo-20® Ophthalmic; Ocusert Pilo-40® Ophthalmic; Pilagan® Ophthalmic; Pilocar® Ophthalmic; Pilopine HS® Ophthalmic; Piloptic® Ophthalmic; Pilostat® Ophthalmic; Salagen® Oral

Generic Available

Yes: Solution


Canadian Brand Names
Minims® Pilocarpine

Synonyms
Pilocarpine Hydrochloride; Pilocarpine Nitrate

Pharmacological Index

Cholinergic Agonist; Ophthalmic Agent, Antiglaucoma; Ophthalmic Agent, Miotic


Use

Ophthalmic: Management of chronic simple glaucoma, chronic and acute angle-closure glaucoma; counter effects of cycloplegics

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


Pregnancy Risk Factor

C


Contraindications

Acute inflammatory disease of anterior chamber, hypersensitivity to pilocarpine or any component


Warnings/Precautions

Use with caution in patients with corneal abrasion, CHF, asthma, peptic ulcer, urinary tract obstruction, Parkinson's disease, or narrow-angle glaucoma


Adverse Reactions

>10%: Ocular: Blurred vision, miosis

1% to 10%:

Central nervous system: Headache

Genitourinary: Polyuria

Local: Stinging, burning

Ocular: Ciliary spasm, retinal detachment, browache, photophobia, acute iritis, lacrimation, conjunctival and ciliary congestion early in therapy

Miscellaneous: Hypersensitivity reactions

<1%: Hypertension, tachycardia, nausea, vomiting, diarrhea, salivation, diaphoresis


Overdosage/Toxicology

Symptoms of overdose include bronchospasm, bradycardia, involuntary urination, vomiting, hypotension, tremors

Atropine is the treatment of choice for intoxications manifesting with significant muscarinic symptoms. Atropine I.V. 2-4 mg every 3-60 minutes (or 0.04-0.08 mg I.V. every 5-60 minutes if needed for children) should be repeated to control symptoms and then continued as needed for 1-2 days following the acute ingestion. Epinephrine 0.1-1 mg S.C. may be useful in reversing severe cardiovascular or pulmonary sequel.


Drug Interactions

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


Stability

Refrigerate gel; store solution at room temperature of 8°C to 30°C (46°F to 86°F) and protect from light


Mechanism of Action

Directly stimulates cholinergic receptors in the eye causing miosis (by contraction of the iris sphincter), loss of accommodation (by constriction of ciliary muscle), and lowering of intraocular pressure (with decreased resistance to aqueous humor outflow)


Pharmacodynamics/Kinetics

Ophthalmic instillation:

Miosis: Onset of effect: Within 10-30 minutes; Duration: 4-8 hours

Intraocular pressure reduction: Onset of effect: 1 hour required; Duration: 4-12 hours

Ocusert® Pilo application:

Miosis: Onset of effect: 1.5-2 hours

Reduced intraocular pressure: Onset: Within 1.5-2 hours; miosis within 10-30 minutes; Duration: ~1 week


Usual Dosage

Adults:

Nitrate solution: Shake well before using; instill 1-2 drops 2-4 times/day

Hydrochloride solution:

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

To counteract the mydriatic effects of sympathomimetic agents: Instill 1 drop of a 1% solution in the affected eye

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

Ocular systems: Systems are labeled in terms of mean rate of release of pilocarpine over 7 days; begin with 20 mcg/hour at night and adjust based on response

Oral: 5 mg 3 times/day, titration up to 10 mg 3 times/day may be considered for patients who have not responded adequately


Dietary Considerations

No data reported


Administration

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

Intraocular pressure, funduscopic exam, visual field testing


Mental Health: Effects on Mental Status

None reported


Mental Health: Effects on Psychiatric Treatment

Pilocarpine may antagonize the effects of anticholinergics and produce cardiac conduction abnormalities in patients receiving beta-blockers


Dental Health: Local Anesthetic/Vasoconstrictor Precautions

No information available to require special precautions


Dental Health: Effects on Dental Treatment

No effects or complications reported


Patient Information

Use as often as recommended. Ophthalmic: Wash hands before using. 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. Do not let tip of applicator touch eye or contaminate tip of applicator. 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. Breast-feeding precautions: Consult prescriber if breast-feeding.


Nursing Implications

Usually causes difficulty in dark adaptation; advise patients to use caution while night driving or performing hazardous tasks in poor illumination; finger pressure should be applied to lacrimal sac for 1-2 minutes after instillation to decrease risk of absorption and systemic reactions. Assure the patient or a caregiver can adequately administer ophthalmic medication dosage form.


Dosage Forms

Gel: 4% (3.5 g)

Solution, as hydrochloride: 0.25% (15 mL); 0.5% (15 mL, 30 mL); 1% (1 mL, 2 mL, 15 mL, 30 mL); 2% (1 mL, 2 mL, 15 mL, 30 mL); 3% (15 mL, 30 mL); 4% (1 mL, 2 mL, 15 mL, 30 mL); 6% (15 mL, 30 mL); 8% (2 mL); 10% (15 mL)

Solution, as nitrate: 1% (15 mL); 2% (15 mL); 4% (15 mL)

Ocusert® Pilo-20: Releases 20 mcg/hour for 1 week

Ocusert® Pilo-40: Releases 40 mcg/hour for 1 week

Tablet: 5 mg


References

Jacobs CD and van der Pas M, "A Multicenter Maintenance Study of Oral Pilocarpine Tablets for Radiation-Induced Xerostomia," Oncology, 1996, 10(3 Suppl):16-20.

Johnson JT, Ferretti GA, Nethery WJ, et al, "Oral Pilocarpine for Postirradiation Xerostomia in Patients With Head and Neck Cancer," N Engl J Med, 1993, 329(6):390-5.

LeVeque FG, Montgomery M, Potter D, et al, "A Multicenter, Randomized, Double-Blind, Placebo-Controlled, Dose-Titration Study of Oral Pilocarpine for Treatment of Radiation-Induced Xerostomia in Head and Neck Cancer Patients," J Clin Oncol, 1993, 11(6):1124-31.

Rieke JW, Hafermann MD, Johnson JT, et al, "Oral Pilocarpine for Radiation-Induced Xerostomia: Integrated Efficacy and Safety Results From Two Prospective Randomized Clinical Trials," Int J Radiat Oncol Biol Phys, 1995, 31(3):661-9.

Schuller DE, Stevens P, Clausen KP, et al, "Treatment of Radiation Side Effects With Oral Pilocarpine," J Surg Oncol, 1989, 42(4):272-6.


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