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J.Health Sci., 51(2), 257-262, 2005
Comparison of the Effects of Cetraxate and its Major Metabolite
on Human Plasma Gastrin, Somatostatin, Calcitonine
Gene-Related Peptide and Substance P in Human Plasma
Fumihiko Katagiri,* Shin Inoue, Yuhki Sato, Hiroki Itoh, and Masaharu Takeyama
Department of Clinical Pharmacy, Oita University Hospital, 1-1, Idaigaoka, Hasama-machi, Oita, 879-5593, Japan
Cetraxate hydrochloride (cetraxate), an antiulcer
drug, produces a dose related increase in mucosal blood
flow. We have reported that cetraxate increases plasma
calcitonin gene-related peptide (CGRP) and substance
P in healthy human subjects (J. Pharm.
Pharmacol., 56, p. 557, 2004). Cetraxate is rapidly metabolized to
tranexamic acid in plasma. We investigated the effect
of tranexamic acid on human plasma CGRP, substance
P, gastrin and somatostatin. Tranexamic acid at a dose
of 500 mg or placebo was orally administered in five
healthy male volunteers. The blood samples were taken
before and at 20, 40, 60, 90, 120, 180 and 240 min after
administrations, followed by the extracting procedure,
and submitted to the high sensitive enzyme
immunoassay system for CGRP and substance P as previously
developed. Single administration of tranexamic acid
caused significant increases of plasma CGRP
concentration at 60-90 min compared with placebo, but the
level-time profile was a little different from that of
cetraxate. Tranexamic acid had no significant effect
on plasma gastrin, somatostatin and substance P
levels compared with placebo. In this study, we thought
that the gastroprotective effect of cetraxate might not
be due to plasma metabolite, tranexamic acid, but
direct stimulation of gastric mucosa.
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