Studies on the Active Form of Oral Gefarnate

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This paper describes a possibility that a metabolite of orally administered gefarnate (GF), an antiulcerative agent, is an acting substance, instead of GF.<BR>When GF was orally administered in rabbits or rats, its metabolites, farnesylacetic acid (FAA), geraniol etc. were clearly detected in portal or lymphatic flow, while mother compound GF was not detectable. FAA revealed about 100 times potent increase in the O<SUB>2</SUB> consumption of mitochondria of rat liver than that of GF. When FAA (4 mg/kg) was intraperitoneally administered in rats, it showed a potent inhibitory effect on the stress ulcer, while oral administrations (1-260mg/ kg) were inactive or slightly adverse.<BR>These findings may be related to the assumption that FAA, a main metabolite, acts as a main pharmacologically active substance, but when it was directly applied to the surface of gastric mucosa with higher concentrations, it may inhibit the cellular respiration.
一般社団法人日本臨床薬理学会の論文