DiJoseph J F, Mir G N
Department of Gastrointestinal Pharmacology, William H. Rorer, Inc., Fort Washington, Pennsylvania.
Arch Int Pharmacodyn Ther. 1987 Aug;288(2):300-8.
Lidamidine, a new antidiarrheal agent, produced a dose-dependent increase in plasma glucose levels in fed rats. The hyperglycemic response was evident 10 min after oral administration of lidamidine and lasted for 4 hr. Lidamidine's effect was absent in alloxanized rats. Insulin administration prevented the hyperglycemia. Pretreatment with the alpha 2-adrenoceptor antagonists yohimbine or RX781094A blocked the hyperglycemic response, while prazosin, propranolol, and hexamethonium pretreatment had no effect. These results indicate that the hyperglycemic effect of lidamidine is primarily due to the activation of peripherally located alpha 2-adrenoceptors that inhibit the release of insulin from pancreatic beta-cells.
利达脒是一种新型止泻剂，可使进食大鼠的血糖水平呈剂量依赖性升高。口服利达脒10分钟后血糖升高反应明显，并持续4小时。在四氧嘧啶处理的大鼠中未观察到利达脒的作用。注射胰岛素可预防高血糖。用α2-肾上腺素能拮抗剂育亨宾或RX781094A预处理可阻断高血糖反应，而用哌唑嗪、普萘洛尔和六甲铵预处理则无作用。这些结果表明，利达脒的高血糖作用主要是由于激活了位于外周的α2-肾上腺素能受体，从而抑制了胰岛素从胰岛β细胞的释放。
