|
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. |
|
Copyright © 1978-2000 Lexi-Comp Inc. All Rights Reserved
|