Pronunciation: PYE-loe-KAR-peen HYE-droe-KLOR-ide
Class: Cholinergic agent, Ophthalmic agent, miotic and antiglaucoma
- Solution, ophthalmic 1%
- Solution, ophthalmic 2%
- Solution, ophthalmic 4%
- Solution, ophthalmic 0.5%
- Solution, ophthalmic 1%
- Solution, ophthalmic 2%
- Solution, ophthalmic 3%
- Solution, ophthalmic 4%
- Solution, ophthalmic 6%
- Gel, ophthalmic 4%
- Tablets 5 mg
- Tablets 7.5 mg
Decreases IOP by constricting pupil and stimulating ciliary muscles to open trabecular meshwork spaces and facilitate outflow of aqueous humor.PO
Stimulates exocrine glands including mucous cells of respiratory tract and salivary glands in oral cavity.
T max is 0.85 to 1.25 h. C max is 15 to 41 ng/mL. AUC is 33 to 108 h•ng/mL. High-fat meals decreased the rate of absorption.
Limited information available; however, its thought to occur at neuronal synapses and probably in the plasma.
Urine (as unchanged pilocarpine, minimal active/inactive degradation products). Half-life is 0.76 to 1.35 h.
3 to 5 h.
Special PopulationsRenal Function Impairment
No effect on pilocarpine pharmacokinetics.Hepatic Function Impairment
In patients with mild to moderate hepatic function impairment, pilocarpine Cl is decreased, resulting in an increase in the pilocarpine C max and half-life.Gender
Elderly women had C max and AUC approximately twice that of elderly and younger men.
Indications and UsageOphthalmic gel
To control IOP.Ophthalmic solution
Management of glaucoma, especially open-angle glaucoma; management of acute (closed-angle) glaucoma alone and in combination with other cholinergic agent or carbonic anhydrase inhibitors.PO
Treatment of xerostomia (dry mouth) in patients with malfunctioning salivary glands because of radiotherapy for cancer of head and neck; relief of dry mouth in patients with Sjögren syndrome.
Relief of dry mouth in patients with graft-vs-host disease (PO); keratoconjunctivitis sicca (dry eye syndrome).
When miosis is undesirable (eg, acute iritis, narrow-angle glaucoma); hypersensitivity to any component of the product.PO
Dosage and AdministrationAdults
PO Titrate dosage based on therapeutic response and tolerance. To reduce the incidence and severity of adverse reactions, use the lowest effective dose. Do not exceed a maximum of 10 mg/dose or 30 mg daily.Radiation-Induced Xerostomia
PO 5 mg 3 times daily. If no response, increase dosage to 10 mg 3 times daily. Continue uninterrupted for at least 12 wk before assessing for full therapeutic benefit (max, 30 mg/day).Sjögren Syndrome
PO 5 mg 4 times daily. Continue uninterrupted for at least 6 wk before assessing for full therapeutic benefit.Glaucoma
Ophthalmic solution Instill 1 to 2 drops in affected eye(s) up to 4 times daily. More concentrated solutions are sometimes used.Adults
Ophthalmic gel Apply one-half inch ribbon in lower conjunctival sac of affected eye(s) once daily at bedtime.Hepatic Function Impairment
PO Moderate hepatic function impairment: Start with 5 mg twice daily, adjusting the dose based on therapeutic response and tolerability. Avoid use in patients with severe hepatic function impairment.
- Administration with a high-fat meal reduces pilocarpine absorption.
- Give medication with food if GI distress occurs.
- To avoid contamination, do not touch tip of container to any surface. Replace cap after administration.
- During acute phase, the mitotic agent must be instilled into the unaffected eye to prevent an attack of angle-closure glaucoma.
Store at controlled room temperature (59° to 86°F).Ophthalmic gel
Store at 36° to 80°F. Avoid excessive heat. Do not freeze.
May antagonize action of pilocarpine (PO, ophthalmic).Beta-blockers
Potential for cardiac conduction disturbances with oral pilocarpine.Food (high-fat meal)
Decreases the rate of pilocarpine absorption.Parasympathomimetics
Additive pharmacologic effects and increased toxicity possible.
Laboratory Test Interactions
None well documented.
Hypertension (3%); palpitations, tachycardia (1% to 2%).
Asthenia, dizziness (12%); headache (11%); somnolence, tremor (1% to 2%). Ophthalmic: Periorbital or temporal headache.
Sweating (68%); flushing (13%); pruritus, rash (1% to 2%).
Rhinitis (14%); amblyopia (4%); abnormal vision, blurred vision, conjunctivitis, epistaxis, tinnitus, voice alteration (1% to 2%).Ophthalmic
Burning or discomfort; ciliary spasm; conjunctival vascular congestion; induced myopia; lacrimation; lens opacity; reduced visual acuity; retinal detachment; superficial keratitis.
Nausea (15%); diarrhea, dyspepsia (7%); vomiting (4%); increased salivation (3%); constipation, dysphagia, flatulence, glossitis, stomatitis, taste perversion (1% to 2%).
Urinary frequency (12%); urinary incontinence, urinary tract infection, vaginitis (1% to 2%).
Allergic reaction (1% to 2%).
Abnormalities including chemistry, hematology, and urinalysis (1% to 2%).
Back pain, myalgias (1% to 2%).
Increased cough, sinusitis (1% to 2%); bronchial spasm, pulmonary edema.
Chills (15%); edema (5%); pain (4%); accidental injury, face edema, fever (1% to 2%).
Category C .
Safety and efficacy not established.
Elderly patients also may be at increased risk for certain adverse reactions during therapy, including diarrhea, urinary frequency, and dizziness.
Dose reduction may be needed in patients with hepatic function impairment.
Special Risk Patients
Use with caution in patients with known or suspected cholelithiasis or biliary tract disease, nephrolithiasis, or underlying cognitive or psychiatric disturbances.
Dose-related CV effects include bradycardia, hypertension, hypotension, and tachycardia.
May cause difficulty in dark adaptation; therefore, caution is needed in night driving and in other hazardous situations in poor illumination.
Pilocarpine can increase airway resistance, bronchial smooth muscle tone, and bronchial secretions. Use with caution in patients with controlled asthma, chronic bronchitis, or COPD requiring treatment.
Ophthalmic preparations can cause visual blurring, which may result in decreased visual acuity, especially at night and in patients with central lens changes. Advise patients to use caution while driving at night or when performing hazardous activities in reduced lighting.
Bronchial constriction in asthmatic patients, death, exaggerated parasympathomimetic effects including AV block, bradycardia, cardiac arrhythmias, diarrhea, GI spasm, headache, hypertension, hypotension, lacrimation, mental confusion, nausea, respiratory distress, salivation, shock, sweating, tachycardia, tremors, visual disturbances, and vomiting.
- For treatment of glaucoma, emphasize need to adhere to medical regimen to prevent blindness.
- Advise patients that their vision may be impaired, affecting their ability to drive safely.
- Explain that long-term therapy may be required.
- Instruct patient to wash hands thoroughly before and after using ophthalmic preparation.
- Review proper procedure for administration of ophthalmic preparations.
- Explain that ophthalmic preparations may sting upon instillation, especially with first few doses.
- Tell patient to discard solution after expiration date.
- Explain that medication may cause headache or brow ache and that because of blurring and altered distance vision and night vision, to use caution while night driving or performing hazardous tasks in poor lighting.
- Explain that during acute phases, a miotic (agent that causes pupil to constrict) also must be instilled into unaffected eye to prevent occurrence of angle-closure glaucoma.
- Advise patients to drink additional water or noncaffeinated fluids during therapy.
- Tell patients to report the following symptoms to health care provider: chills, diarrhea, dizziness, fluid retention, flushing, frequent urination, headache, indigestion, nasal congestion, nausea, sweating, tearing, weakness.
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