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Pinaverium bromide: A calcium channel blocker acting selectively on the gastrointestinal tract
Author(s) -
Christen Mme MarieOdile,
Tassig JeanPierre
Publication year - 1989
Publication title -
drug development research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.582
H-Index - 60
eISSN - 1098-2299
pISSN - 0272-4391
DOI - 10.1002/ddr.430180202
Subject(s) - antagonist , pharmacology , chemistry , gastrointestinal tract , irritable bowel syndrome , ammonium bromide , in vivo , channel blocker , calcium , motility , calcium channel , medicine , biochemistry , receptor , biology , pulmonary surfactant , genetics , microbiology and biotechnology
Evidence is reviewed which indicates that pinaverium bromide (PB) relaxes gatrointestinal (GI) structures mainly by specifically inhibiting Ca +2 influx through potential‐dependent channels that exist on the surface membranes of smooth muscle cells. Its in vivo selectivity for the GI tract appears to be due mainly to its pharmacokinetic properties. Because of its low absorption, typical for quarternary ammonium compounds, and its efficient hepato‐biliary excertion, most of the orally‐administered dose of PB remains in the GI tract. Other mechanisms possibly related to its selectivity, and comparisons between the actions of PB and those Ca 2+ ‐antagonists, are also disussed. PB is the only Ca 2+ ‐antagonist currently registered for treatment of functional intestinal disorders (e.g., irritable bowel syndrome). A major advantage of orally‐administered PB is that it does not elicit adverse systemic (e.g., cardiovasular) side‐effects at doses that effectively relieve GI spasm, pain, and abnormal motility.