ラット血漿中カルベジロール濃度に及ぼすメトクロプラミドと臭化プロパンテリンの影響

概要

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We investigated the effects of metoclopramide and propantheline bromide on the bioavailability of carvedilol in rats. To determine the concentration-time profile of plasma carvedilol, the blood samples were obtained from the tail vein after the simultaneous administration of 20 mg/kg carvedilol either with or without 5 mg/kg metoclopramide and 15 mg/kg propantheline bromide. The plasma carvedilol concentrations were significantly higher than the controls at 15 min. - I hr and 3,4 hr, and the drug pharmacokinetic parameters time to C_<max> (T_<max>) was 0.45 time shorter, while the absorption rate constant (Ka) and area under the concentration-time curve (AUC_<0-24>) were 2.5 and 1.5 times higher after the oral administration of carvedilol with metoclopramide. The rate of bioavailability for carvedilol was accelerated by metoclopramide which stimulates gastric emptying. In contrast, the plasma carvedilol concentrations and T_<max>, AUC_<0-24> did not change after the single intraperitoneal administration of carvedilol with the oral administration of metoclopramide. Conversely, propantheline bromide, which delays gastric emptying , slowed absorption, but not according the AUC_<0-24> of carvedilol. Other similar pharmacokinetic interaction probably occur since carvedilol are poorly absorbed from the stomach and numerous therapeutic agents influence gastrointestinal motility.
日本医療薬学会の論文
1999-04-10