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Pilocarpine is a drug used to treat dry mouth and glaucoma. It is a parasympathomimetic alkaloid obtained from the leaves of tropical American shrubs from the genus Pilocarpus. It is a non-selective muscarinic receptor agonist in the parasympathetic nervous system, which acts therapeutically at the muscarinic acetylcholine receptor M3 due to its topical application, e.g., in glaucoma and xerostomia.

Pilocarpine is available under several trade names such as: Diocarpine (Dioptic), Isopto Carpine (Alcon), Miocarpine (CIBA Vision), Ocusert Pilo-20 and -40 (Alza), Pilopine HS (Alcon), Salagen (MGI Pharma), Scheinpharm Pilocarpine (Schein Pharmaceutical), and Timpilo (Merck Frosst).

It is on the World Health Organization's List of Essential Medicines, a list of the most important medication needed in a basic health system.

Pilocarpine stimulates the secretion of large amounts of saliva and sweat. It is used to treat dry mouth (xerostomia), particularly in Sjögren's syndrome, but also as a side effect of radiation therapy for head and neck cancer.

It has also been used in the treatment of chronic open-angle glaucoma and acute angle-closure glaucoma for over 100 years. It acts on a subtype of muscarinic receptor (M3) found on the iris sphincter muscle, causing the muscle to contract -resulting in pupil contraction (miosis). Pilocarpine also acts on the ciliary muscle and causes it to contract. When the ciliary muscle contracts, it opens the trabecular meshwork through increased tension on the scleral spur. This action facilitates the rate that aqueous humor leaves the eye to decrease intraocular pressure.

In ophthalmology, pilocarpine is also used to reduce the possibility of glare at night from lights when the patient has undergone implantation of phakic intraocular lenses; the use of pilocarpine would reduce the size of the pupils, relieving these symptoms. The most common concentration for this use is pilocarpine 1%, the weakest concentration.

Adverse effects

Use of pilocarpine may result in a range of adverse effects, most of them related to its non-selective action as a muscarinic receptor agonist. Pilocarpine has been known to cause excessive salivation, sweating, bronchial mucus secretion, bronchospasm, bradycardia, vasodilation, and diarrhea. Eye drops can result in brow ache and chronic use in miosis.

Systemic injection of pilocarpine can compromise the blood brain barrier allowing pilocarpine to gain access to the brain which can lead to chronic epilepsy.

Preparation

Plants in the genus Pilocarpus are the only known sources of Pilocarpine, and commercial production is derived entirely from the leaves of Pilocarpus microphyllus (Maranham Jaborandi). This genus grows only in South America, and Pilocarpus microphyllus is native to several states in northern Brazil.

On Aug, 11, 2015: 350 people reported to have side effects when taking Pilocarpine hydrochloride. Among them, 3 people (0.86%) have Hallucination.