PILOCARPINE Eye drops Ref.[7850] Active ingredients: Pilocarpine

Source: Medicines & Healthcare Products Regulatory Agency (GB)  Revision Year: 2016  Publisher: Martindale Pharmaceuticals Ltd, T/a Martindale Pharma, Bampton Road, Harold Hill, Romford, RM3 8UG

Pharmacodynamic properties

Pharmacotherapeutic group: parasympathomimetics
ATC code: S01EB01

Pilocarpine is an alkaloid of natural plant origin, which is a direct-acting cholinergic agonist. It acts primarily at muscarinic receptor sites both peripherally and centrally, affecting smooth muscle, the cardiovascular system and exocrine glands.

The precise mechanism by which pilocarpine reduces intra-ocular pressure has not been established, though it is believed to involve direct stimulation of the longitudinal muscle of the ciliary body, which in turn affects the scleral spur, widening the trabecular spaces and allowing for increased aqueous flow. Pilocarpine may also decrease aqueous formation with long term administration. Due to its activity at the muscarinic receptor sites of the ciliary muscles and iris sphincter, pilocarpine causes varying degrees of accommodation spasm and pupillary constriction.

Paediatric population

There are literature reports of the ocular use of pilocarpine in concentrations up to 2% in patients aged 1 month and older. However, information on the dose and strength used is limited. Safety data do not suggest any significant safety issues in children, or any difference between the safety profiles of pilocarpine in children and adults.

Pharmacokinetic properties

Onset of miosis after topical administration of a 1% solution of pilocarpine hydrochloride or nitrate to the conjunctival sac occurs within 10-30 minutes, with maximal effect within 30 minutes. Miosis usually persists for 4-8 hours, rarely, up to 20 hours. Reduction of intra-ocular pressure is evident within 60 minutes, peaks within 75 minutes and, depending on the concentration of pilocarpine used, persists for 4-14 hours. Spasms of accommodation commence in about 15 minutes and persist for 2-3 hours.

Preclinical safety data

None available.

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