Pilocarpine, Pilocarpine Hydrochloride, Pilocarpine Nitrate
Drug class: Antineoplastic Agents
Usage of Pilocarpine, Pilocarpine Hydrochloride, Pilocarpine Nitrate
Open-angle Glaucoma
Reduction of elevated intraocular pressure (IOP) in patients with primary open-angle (chronic simple, noncongestive) glaucoma.
May use concomitantly with other miotics, sympathomimetic agents, β-adrenergic blocking agents, carbonic anhydrase inhibitors, or hyperosmotic agents.
Angle-closure Glaucoma
Reduction of IOP in the emergency treatment of acute (congestive) angle-closure glaucoma prior to surgery. Because it may preclude successful surgery, do not use for long periods prior to surgical treatment.
Lack of response may be caused by paralysis of the iris sphincter by the extremely high IOP; systemic administration of acetazolamide or hyperosmotic solutions (e.g., glycerin or mannitol) may be required.
Ocular Surgery
Reduction of IOP and protection of the lens by causing miosis prior to goniotomy or iridectomy, including laser iridectomy.
May use to control glaucoma which persists after surgery.
Ophthalmologic Examinations
Production of miosis to counteract mydriatic effects of sympathomimetic agents (e.g., phenylephrine) after ophthalmoscopic examinations in glaucoma patients.
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How to use Pilocarpine, Pilocarpine Hydrochloride, Pilocarpine Nitrate
Administration
Ophthalmic Administration
Avoid contamination of the solution or gel container.
Ophthalmic solutions are preferred when an acute reduction in IOP and/or an intense miotic effect are necessary (e.g., prior to surgery, following ophthalmologic examinations).
Tonometric measurements recommended before and during therapy.
Ophthalmic SolutionApply topically to the conjunctival sac of affected eye(s) as directed by clinician, usually 3–4 times daily; more frequent administration may be necessary in some patients. Not for injection.
Following topical instillation, apply finger pressure on the lacrimal sac for 1–2 minutes to minimize drainage into nose and throat and reduce risk of absorption and systemic reactions. Remove excess solution around the eye with a tissue and rinse off any medication on hands immediately.
Ophthalmic GelApply topically to the lower conjunctival sac of affected eye(s) once daily at bedtime.
Measure IOP just before next dose following initiation of therapy to ensure adequate control of IOP throughout the 24-hour dosing interval.
If used concomitantly with ophthalmic solutions, instill solutions first and apply gel ≥5 minutes later.
Dosage
Available as pilocarpine hydrochloride; dosage expressed in terms of the salt.
Adjust concentration and frequency of solution instillation according to patient requirements and response, as determined by tonometric readings.
In patients with heavily pigmented irides, higher solution concentrations may be required.
Adjust dosage of ophthalmic gel based on periodic tonometric readings.
Adults
Open-Angle Glaucoma Ophthalmic1–2 drops of a 1–4% solution in the eye(s) every 4–12 hours. Solution concentrations >4% are only occasionally more effective than lower concentrations.
Apply a 1.3-cm (0.5-inch) ribbon of a 4% gel into lower conjunctival sac once daily at bedtime.
Acute Angle-Closure Glaucoma Ophthalmic1 drop of a 2% solution in the affected eye every 5–10 minutes for 3–6 doses, followed by 1 drop every 1–3 hours until pressure is controlled. To prevent a bilateral attack, 1 drop of a 1–2% solution in the unaffected eye every 6–8 hours.
Ocular Surgery Iridectomy Ophthalmic1 drop of a 2% solution 4 times immediately prior to iridectomy has been used.
Congenital Glaucoma (Goniotomy) Ophthalmic1 drop of a 2% solution every 6 hours prior to surgery has been used.
May use a 2% solution to fill the gonioscopic lens prior to goniotomy, or may administer 1 drop of a 2% solution every 6 hours plus 3 times in the 30 minutes immediately preceding goniotomy, with or without concomitant administration of acetazolamide.
Ophthalmologic Examinations Ophthalmic1 drop of a 1% solution in the affected eye(s).
Warnings
Contraindications
Warnings/Precautions
Sensitivity Reactions
HypersensitivityAllergic conjunctivitis, dermatitis, or keratitis reported occasionally with miotics; these reactions are usually alleviated by changing to another miotic. In some instances, allergic reactions may be caused by preservatives in the preparations.
General Precautions
Ocular EffectsRetinal detachment reported rarely; use with extreme caution, if at all, in patients with a history or risk of retinal detachment, especially those who are young or aphakic. Carefully examine retinal periphery at least annually to detect an impending detachment.
Use with caution in patients with corneal abrasion to avoid excessive penetration and systemic toxicity.
Possible spasm of accommodation and poor vision in dim light, particularly in geriatric patients and patients with lens opacities. (See Advice to Patients.)
Follicular conjunctival hypertrophy may occur with prolonged therapy.
Possible transient increase in IOP even when the angle is open. In some patients with angle-closure glaucoma receiving miotics, IOP may be increased and acute attacks may be precipitated.
Possible corneal opacities.
Regular slit-lamp examinations recommended; discontinue therapy, at least temporarily, if iris cysts, iritis, syneChiae, or lens opacities occur.
Specific Populations
PregnancyCategory C.
LactationNot known whether pilocarpine is distributed into milk. Use with caution.
Pediatric UseSafety and efficacy not established.
Geriatric UseReduced visual acuity in dim light frequently experienced in geriatric patients.
Common Adverse Effects
Ocular irritation (burning or discomfort), lacrimation, temporal or periorbital headache, painful ciliary or accommodative spasm, blurred vision or myopia, conjunctival vascular congestion, superficial keratitis, poor vision in dim light.
What other drugs will affect Pilocarpine, Pilocarpine Hydrochloride, Pilocarpine Nitrate
Specific Drugs
Drug
Interaction
Comments
Ocular hypotensive agents
Additive IOP lowering effects
Used to therapeutic advantage
Anticholinesterase miotics
Competitive inhibition of miotic effect and presumably IOP-lowering effect
Concomitant administration generally not recommended
Some clinicians recommend administration of pilocarpine at onset of long-acting anticholinesterase therapy followed by gradual taper of pilocarpine so that antagonism between the drugs allows full effects of the anticholinesterase to be obtained gradually
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