Add time:07/15/2019 Source:sciencedirect.com
Publisher SummaryThis chapter explains the nomenclature, synthesis, methods of analysis, and pharmacology of pirenzepine dihydrochloride. Pirenzepine is a tricyclic compound, but its physico-chemical properties differ considerably from those of other tricyclic compounds that are used as centrally acting drugs. The crystal structure of pirenzepine monohydrate free base was studied by Ruzic-Toros and Kojec-Prodic. Stability of pirenzepine depends on both moisture contents and pH and the effect of the moisture contents could be minimized by adjusting to optimum pH. The marked physicochemical properties of pirenzepine result in the drug being highly hydrophilic at physiological pH. Pretreatment of healthy volunteers with therapeutic doses of pirenzepine over 5 days showed no significant effect on the absorption, distribution or elimination of antipyrine. Pirenzepine was shown by Dal Monte to be effective in the maintenance treatment of duodenal ulcers to prevent ulcer recurrence when given in oral doses of 100 mg daily for one year.
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