Pilocarpine is sometimes used immediately beforecertain types of corneal grafts andcataract surgery.[21][22] It is also used prior to YAG laser iridotomy. In ophthalmology, pilocarpine is also used to reduce symptomatic glare at night from lights when the patient has undergone implantation ofphakic intraocular lenses; the use of pilocarpine would reduce the size of the pupils, partially relieving these symptoms.[dubious –discuss] The most common concentration for this use is pilocarpine 1%.[citation needed] Pilocarpine is shown to be just as effective asapraclonidine in preventing intraocular pressure spikes afterlaser trabeculoplasty.[23]
Use of pilocarpine may result in a range of adverse effects, most of them related to itsnon-selective action as a muscarinic receptor agonist. Systemic (oral) pilocarpine has been known to cause excessive salivation, sweating, bronchialmucus secretion,bronchospasm,bradycardia,vasodilation, anddiarrhea. Eye drops can result in browache and chronic use inmiosis. It can also cause temporary blurred vision or darkness of vision, temporary shortsightedness,hyphema and retinal detachment.
Pilocarpine is a drug that acts as a muscarinic receptor agonist. It acts on a subtype of muscarinic receptor (M3) found on theiris sphincter muscle, causing the muscle to contract - resulting in pupil constriction (miosis). Pilocarpine also acts on theciliary muscle and causes it to contract. When the ciliary muscle contracts, it opens thetrabecular meshwork through increased tension on thescleral spur. This action facilitates the rate thataqueous humor leaves theeye to decreaseintraocular pressure. Paradoxically, when pilocarpine induces this ciliary muscle contraction (known as anaccommodative spasm) it causes the eye'slens to thicken and move forward within the eye. This movement causes the iris (which is located immediately in front of the lens) to also move forward, narrowing theAnterior chamber angle. Narrowing of the anterior chamber angle increases the risk of increasedintraocular pressure.[26]
Plants in the genusPilocarpus are the only known sources of pilocarpine, and commercial production is derived entirely from the leaves ofPilocarpus microphyllus (Maranham Jaborandi). This genus grows only in South America, andPilocarpus microphyllus is native to several states in northern Brazil.[27]
Pilocarpine is extracted from the leaves ofPilocarpus microphyllus in a multi-step process : the sample is moistened with dilutesodium hydroxide to transform the alkaloid into its free-base form then extracted usingchloroform or a suitable organic solvent. Pilocarpine can then be further purified by re-extracting the resulting solution with aqueoussulfuric acid then readjusting the pH to basic usingammonia and a final extraction by chloroform.[28][29][30]
Pilocarpine is used to induce chronicepilepsy inrodents, commonlyrats, as a means to study the disorder's physiology and to examine different treatments.[31][32] Smaller doses may be used to induce salivation in order to collect samples ofsaliva, for instance, to obtain information aboutIgA antibodies.
^Gornitsky M, Shenouda G, Sultanem K, Katz H, Hier M, Black M, et al. (July 2004). "Double-blind randomized, placebo-controlled study of pilocarpine to salvage salivary gland function during radiotherapy of patients with head and neck cancer".Oral Surgery, Oral Medicine, Oral Pathology, Oral Radiology, and Endodontics.98 (1):45–52.doi:10.1016/j.tripleo.2004.04.009.PMID15243470.
^"Glaucoma and ocular hypertension. NICE guideline 81". National Institute for Health and Care Excellence. November 2017. Retrieved19 September 2019.Ocular hypertension... alternative options include carbonic anhydrase inhibitors such as brinzolamide or dorzolamide, a topical sympathomimetic such as apraclonidine or brimonidine tartrate, or a topical miotic such as pilocarpine, given either as monotherapy or as combination therapy.
^Lusthaus J, Goldberg I (March 2019). "Current management of glaucoma".The Medical Journal of Australia.210 (4):180–187.doi:10.5694/mja2.50020.PMID30767238.S2CID73438590.Pilocarpine is no longer routinely used for long term IOP control due to a poor side effect profile
^Hamilton R (2015).Tarascon Pocket Pharmacopoeia 2015 Deluxe Lab-Coat Edition. Jones & Bartlett Learning. p. 415.ISBN978-1-284-05756-0.
^Rosin A (1991). "[Pilocarpine. A miotic of choice in the treatment of glaucoma has passed 110 years of use]".Oftalmologia (in Romanian).35 (1):53–55.PMID1811739.
^Holmstedt B, Wassén SH, Schultes RE (January 1979). "Jaborandi: an interdisciplinary appraisal".Journal of Ethnopharmacology.1 (1):3–21.doi:10.1016/0378-8741(79)90014-x.PMID397371.
^World Health Organization (2019).World Health Organization model list of essential medicines: 21st list 2019. Geneva: World Health Organization.hdl:10665/325771. WHO/MVP/EMP/IAU/2019.06. License: CC BY-NC-SA 3.0 IGO.
^"Pilocarpine".MedLinePlus. U.S. National Library of Medicine.Archived from the original on 6 March 2010.
^Yang WF, Liao GQ, Hakim SG, Ouyang DQ, Ringash J, Su YX (March 2016). "Is Pilocarpine Effective in Preventing Radiation-Induced Xerostomia? A Systematic Review and Meta-analysis".International Journal of Radiation Oncology, Biology, Physics.94 (3):503–511.doi:10.1016/j.ijrobp.2015.11.012.hdl:10722/229069.PMID26867879.
^Károly N (2018).Immunohistochemical investigations of the neuronal changes induced by chronic recurrent seizures in a pilocarpine rodent model of temporal lobe epilepsy (Thesis). University of Szeged.doi:10.14232/phd.9734.
