Pilocarpine Hydrochloride

What it is and how it works

Mechanism of Action Pilocarpine hydrochloride is a direct acting cholinergic parasympathomimetic agent which acts through direct stimulation of muscarinic receptors and smooth muscle such as the iris and secretory glands. Pilocarpine contracts the ciliary muscle, causing increased tension on the scleral spur and opening of the trabecular meshwork spaces to facilitate outflow of aqueous humor. Outflow resistance is reduced, lowering intraocular pressure (IOP). Pilocarpine also produces miosis through contraction of the iris sphincter muscle. Miosis relieves appositional angle narrowing and closure, which lowers IOP in certain types of angle-closure glaucoma.

Indications

Pilocarpine hydrochloride ophthalmic solution is indicated for the: Pilocarpine hydrochloride ophthalmic solution is a muscarinic cholinergic agonist indicated for: The reduction of elevated intraocular pressure (IOP) in patients with open-angle glaucoma or ocular hypertension. The management of acute angle-closure glaucoma. The prevention of postoperative elevated IOP associated with laser surgery. The induction of miosis. Reduction of Elevated Intraocular Pressure (IOP) in Patients with Open-Angle Glaucoma or Ocular Hypertension Management of Acute Angle-Closure Glaucoma Prevention of Postoperative Elevated IOP Associated with Laser Surgery Induction of Miosis

Dosage and administration (summary)

Instill one drop in the eye(s) up to four times daily. Reduction of Elevated Intraocular Pressure (IOP) in Patients with Open-Angle Glaucoma or Ocular Hypertension One drop of pilocarpine hydrochloride ophthalmic solution 1%, 2% or 4% should be applied topically in the eye(s) up to four times daily. Pilocarpine-naïve patients should be started on the 1% concentration as higher concentrations are often not tolerated initially. The frequency of instillation and concentration of pilocarpine hydrochloride are determined by the severity of the elevated intraocular pressure and miotic response of the patient.

Contraindications

None. None.

Warnings and precautions

Poor illumination: Exercise caution in night driving and other hazardous occupations in poor illumination. Pre-existing retinal disease: Rare cases of retinal detachment have been reported; a thorough examination of the retina including funduscopy is advised in all patients prior to the initiation of therapy. Iritis: Caution is advised in patients with iritis. Congenital glaucoma: Caution is advised in pediatric patients with primary congenital glaucoma for control of IOP as cases of a paradoxical increase in IOP have been reported.

Pregnancy

Pregnancy Pregnancy Category C. Animal reproduction studies have not been conducted with pilocarpine hydrochloride. It is also not known whether pilocarpine hydrochloride can cause fetal harm when administered to a pregnant woman or can affect reproduction capacity.

Storage and supply

Pilocarpine Hydrochloride Ophthalmic Solution USP, 1% , 2% and 4% is supplied sterile in natural low density polyethylene plastic bottles and natural low density polyethylene tips with dark green high density polyethylene caps.

Source: Pilocarpine Hydrochloride (Pilocarpine Hydrochloride) — US FDA prescribing information, 2021-01-03, DailyMed. Summarised and shortened; the full label governs. Iranian registration, indications and labelling may differ.