A-Z Drug Facts > Pilocarpine

Pilocarpine

Pronouncation: (pie-low-CAR-peen)
Class: Ophthalmic, Antiglaucoma, Mouth and throat product Pilocarpine Hydrochloride

Trade Names:
Isopto-Carpine
- Solution 1%
- Solution 2%
- Solution 4%

Trade Names:
Pilocar
- Solution 0.5%
- Solution 1%
- Solution 2%
- Solution 4%
- Solution 6%

Trade Names:
Piloptic-1/2
- Solution 0.5%

Trade Names:
Piloptic-1
- Solution 1%

Trade Names:
Piloptic-2
- Solution 2%

Trade Names:
Piloptic-3
- Solution 3%

Trade Names:
Piloptic-4
- Solution 4%

Trade Names:
Piloptic-6
- Solution 6%

Trade Names:
Pilopine HS
- Gel 4%

Trade Names:
Salagen
- Tablets 5 mg
- Tablets 7.5 mg

Minims-Pilocarpine (Canada)

Pharmacology

Ophthalmic

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.

Pharmacokinetics

Absorption

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.

Metabolism

Limited information available; however, its thought to occur at neuronal synapses and probably in the plasma.

Elimination

Urine (as unchanged pilocarpine, minimal active/inactive degradation products). Half-life is 0.76 to 1.35 h.

Onset

20 min.

Peak

1 h.

Duration

3 to 5 h.

Special Populations

Gender

Elderly females had C _max and AUC approximately twice that of elderly, young males.

Indications and Usage

Ophthalmic

Treatment of chronic simple glaucoma, chronic angle-closure glaucoma, acute angle-closure glaucoma, pre- and postoperative management of intraocular tension, treatment of mydriasis.

PO

Treatment of xerostomia in patients with malfunctioning salivary glands because of radiotherapy for cancer of head and neck, relieve dry mouth in patients with Sjogren syndrome.

Unlabeled Uses

Relief of dry mouth in patients with graft-vs-host disease (PO).

Contraindications

Hypersensitivity; conditions in which cholinergic effects such as constriction are undesirable. Oral use also contraindicated in uncontrolled asthma, acute iritis, narrow-angle glaucoma, acute inflammatory disease of anterior segment of eye.

Dosage and Administration

Solution
Adults

Instill 1 to 2 drops of 1% or 2% solution in affected eye(s) 6 times or less/day. More concentrated solutions are sometimes used.

Gel
Adults

Apply 0.5-inch ribbon in lower conjunctival sac of affected eye(s) once daily at bedtime.

PO
Adults

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.

Radiation-induced Xerostomia Adults

PO 5 mg 3 times daily. If no response, increase dose to 10 mg 3 times daily. Continue uninterrupted for at least 12 wk before assessing for full therapeutic benefit.

Sjogren Syndrome Adults

PO 5 mg 4 times daily. Continue uninterrupted for at least 6 wk before assessing for full therapeutic benefit.

General Advice

PO

• Administration with a high-fat meal reduces pilocarpine absorption.
• Give medication with food if GI distress occurs.

Ophthalmic

• To avoid contamination, do not touch tip of container to any surface. Replace cap after administration.

Storage/Stability

PO

Store at controlled room temperature (59° to 86°F).

Ophthalmic

Store at room temperature; protect from freezing.

Drug Interactions

Anticholinergics

May antagonize action of pilocarpine (PO, ophthalmic).

Beta-blockers

Potential for cardiac conduction disturbances with oral pilocarpine.

Parasympathomimetics

Additive pharmacologic effects and increased toxicity possible.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Transient hypertension; tachycardia; edema; palpitations.

CNS

Chills; headache; dizziness; asthenia.

Dermatologic

Excessive sweating; flushing.

EENT

Transient stinging and burning, tearing, ciliary spasm, conjunctival vascular congestion, temporal, periorbital, or supraorbital headache, superficial keratitis-induced myopia, blurred vision, poor dark adaptation, conjunctival hyperemia, reduced visual acuity in poor illumination, lens opacity, subtle corneal granularity, conjunctival irritation, ciliary spasm, precipitation of angle closure, irritation, corneal abrasion, visual impairment (ophthalmic); rhinitis (PO).

GI

Excessive salivation; nausea; vomiting; diarrhea dyspepsia; abdominal pain.

Genitourinary

Urinary frequency (PO).

Respiratory

Bronchial spasm; pulmonary edema; rhinitis; sinusitis; pharyngitis; increased coughing; increases airway resistance; bronchial smooth muscle tone; bronchial secretions.

Special Senses

Lacrimation; amblyopia; conjunctivitis; abnormal vision; excessive salivation.

Precautions

Pregnancy

Category C .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Elderly

Elderly patients also may be at increased risk for certain adverse reactions during therapy, including diarrhea, urinary frequency, and dizziness.

Special Risk Patients

Use oral pilocarpine with caution in acute cardiac failure, bronchial asthma, peptic ulcer, hypertension, hyperthyroidism, retinal disease, GI or biliary tract spasm or obstruction, urinary tract obstruction, Parkinson disease, angina pectoris, MI, chronic bronchitis, chronic obstructive pulmonary disease, underlying psychiatric disorders.

Overdosage

Symptoms

Salivation, lacrimation, nausea, vomiting, diarrhea, cramping, sweating, frequent urination, bradycardia, asystole, death (PO).

Patient Information

• For treatment of glaucoma, emphasize need to adhere to medical regimen to prevent blindness.
• 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, altered distance vision and night vision; patient should use caution while night driving or performing hazardous tasks.
• 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.

• PO
• Advise patients to drink additional water or noncaffeinated fluids during therapy.
• Tell patients using oral form to report the following symptoms to health care provider: sweating, nausea, nasal congestion, chills, flushing, frequent urination, dizziness, weakness, headache, indigestion, tearing, diarrhea, fluid retention.

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