ジルチアゼムに関する薬物相互作用の研究(第4報)ジルチアゼムの吸収促進作用と種々の薬物の初回通過代謝との関係

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Alterations in bioavailability of several drugs other than propranolol after the coadministration of diltiazem were investigated in dog and human. Diltiazem did not promote the bioavailability of dipyridamole and furosemide, but the plasma levels of diazepam and its metabolite, desmethyl-diazepam were remarkably increased by the coadministration of diltiazem in dog. On diltiazem-diazepam interaction in human, there was no significant observation. This species difference may be explained by the difference in metabolizing activity for diazepam in dog and human. Several other drugs were tested in dog and it was found that relationship between absolute availability of drugs and the promoting effect of diltiazem was significant. Namely, diltiazem enhanced the absorption of drugs with absolute availability less than 20%, indicating that underlying mechanisms were related to their first pass metabolism. It is considered that such a diltiazem interaction would be advantageous to reduce inter-individual variation in pharmacological effect and also to reduce doses of coadministrated drugs with high liver clearance.
公益社団法人日本薬学会の論文
1983-05-25