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Functional Disorders of the Stomach and Duodenum
Published in Kevin W. Olden, Handbook of Functional Gastrointestinal Disorders, 2020
The selective muscarinic antagonist pirenzepine, which selectively bonds to the M1 muscarinic receptor, has been evaluated in NUD. In one study (43), pirenzepine produced improvement in symptoms in approximately one-quarter of dyspeptic patients, but its usefulness is limited by its significant side-effect profile. The synthetic prostaglandin misoprostol’s usefulness in NUD is also severely limited by its side-effect profile, which actually tends to worsen symptoms in NUD patients (44).
Evaluation of Anti-ulcer Potential of Sphenodesme involucrata var. paniculata (C.B. Clarke) Munir Leaves on Various Gastric Aggressive Factors
Published in Parimelazhagan Thangaraj, Phytomedicine, 2020
P. S. Sreeja, K. Arunachalam, Parimelazhagan Thangaraj
Sodium nitroprusside- and FK409-like NO donors were also used in the ulcer treatment, which was to exert their activity through minimizing the gastric secretion by acting on the Cyclic Guanosine Monophosphate Pathway (cGMP) (Lanas 2008). Anti-muscarinie is another class of anti-ulcer drug with an anti-secretary property by inhibiting the vagal stimulation and blocking the M1 muscarinic receptor. Pirenzepine is a popularly used anti-muscarinie drug, but this also coupled with various side effects to humans, including, dry mouth, blurred vision, tachycardia, and photobia (Singh et al. 2018).
Cholinergic Antagonists
Published in Sahab Uddin, Rashid Mamunur, Advances in Neuropharmacology, 2020
Vishal S. Gulecha, Manoj S. Mahajan, Aman Upaganlawar, Abdulla Sherikar, Chandrashekhar Upasani
A tricyclic antimuscarinic drug, pirenzepine, is an M1-receptor selective agent (Caulfield and Birdsall, 1998). It has a higher affinity for M1 receptors, specifically in the cerebral cortex and sympathetic ganglia. Pirenzepine shows minimal binding toward involuntary muscles (cardiac and smooth muscle) and glands at very low concentration. The drug is responsible for blocking the excitatory postsynaptic potential (EPSP) due to binding of ACh and other cholinergic agonists at ganglionic M1 receptor thereby altering the functions of these M1 receptors (Eglen et al., 1996; Caulfield and Birdsall, 1998). Pirenzepine, at low concentration, reduces the secretion of gastric acid and muscle spasm; therefore, it is used in the management of peptic ulcer. Pirenzepine also showed the contraction of lower esophageal sphincter due to blockade of ganglionic receptors (Wellstein and Pitschner, 1988). Adverse effects such as dry mouth, distorted visualization, and central muscarinic disturbances of other anti-mucarinics are observed to a lower extent with pirenzepine at therapeutic concentration. At a curative dose (100–150 mg/day), pirenzepine cure the duodenal and gastric ulcers as cimetidine and ranitidine which are H2-receptor blockers (Carmine and Brogden, 1985; Tryba and Cook, 1997).
Optical and pharmacological strategies of myopia control
Published in Clinical and Experimental Optometry, 2018
Pirenzepine is a selective anti‐muscarinic agent with a high affinity for the M1 and M4 receptors. A distinct benefit of pirenzepine compared to the non‐selective anti‐muscarinic atropine is that it is less likely to cause cycloplegia and mydriasis and was therefore considered as an alternative myopia control treatment. Pirenzepine has been reported to reduce form deprivation myopia and eye enlargement in the animal model1996 and there have been a handful of clinical trials which have demonstrated myopia control effects of pirenzepine in children.2005 A two‐year randomised clinical trial involved children 8–12-years receiving two per cent pirenzipine gel applied twice daily for two years. At the end of the treatment period, a reduction in myopia progression was measured in children who were treated with pirenzipine compared to the placebo‐treated group (Table 4).