Pirenzepine (Gastrozepin), an M1 selective antagonist, is used in the treatment of peptic ulcers, as it reduces gastric acid secretion and reduces muscle spasm. It is in a class of drugs known as muscarinic receptor antagonists; acetylcholine is the neurotransmitter of the parasympathetic nervous system which initiates the rest-and-digest state (as opposed to fight-or-flight), resulting in an increase in gastric motility and digestion; whereas pirenzepine would inhibit these actions and cause decreased gastric motility leading to delayed gastric emptying and constipation.[1] It has no effects on the brain and spinal cord as it cannot diffuse through the blood–brain barrier.
Pirenzepine has been investigated for use in myopia control.[2][3]
It promotes the homodimerization or oligomerisation of M1 receptors.[4]
^Stolerman IP (2 August 2010). Encyclopedia of Psychopharmacology. Springer. p. 811. ISBN 978-3-540-68698-9. Retrieved 26 June 2013.
^Czepita D (2005). "[Fundamentals of modern treatment of myopia]". Annales Academiae Medicae Stetinensis. 51 (2): 5–9. PMID 16519089.
^Walline JJ, Lindsley KB, Vedula SS, Cotter SA, Mutti DO, Ng SM, Twelker JD (January 2020). "Interventions to slow progression of myopia in children". The Cochrane Database of Systematic Reviews. 1 (1): CD004916. doi:10.1002/14651858.CD004916.pub4. PMC 6984636. PMID 31930781.
^Pediani JD, Ward RJ, Godin AG, Marsango S, Milligan G (June 2016). "Dynamic Regulation of Quaternary Organization of the M1 Muscarinic Receptor by Subtype-selective Antagonist Drugs". The Journal of Biological Chemistry. 291 (25): 13132–13146. doi:10.1074/jbc.M115.712562. PMC 4933229. PMID 27080256.
Pirenzepine (Gastrozepin), an M1 selective antagonist, is used in the treatment of peptic ulcers, as it reduces gastric acid secretion and reduces muscle...
than the (–)-isomer at muscarinic receptors in the rat cerebral cortex. Pirenzepine Eveleigh P, Hulme EC, Schudt C, Birdsall NJ (April 1989). "The existence...
butylbromide and hydrobromide, ipratropium, tropicamide, cyclopentolate, pirenzepine and scopalamine. Muscarinic antagonists such as ipratropium bromide can...
natural tolerance of the gastric lining. Antimuscarinic drugs such as pirenzepine or H2 antihistamines can reduce acid secretion. Proton pump inhibitors...
proteins. There are other classification systems. For example, the drug pirenzepine is a muscarinic antagonist (decreases the effect of ACh), which is much...
years of age may slow the worsening of myopia. These treatments include pirenzepine gel, cyclopentolate eye drops, and atropine eye drops. While these treatments...
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