Lafutidine, a newly developed antiulcer drug, elevates postprandial intragastric pH and increases plasma calcitonin gene-related peptide and somatostatin concentrations in humans: comparisons with famotidine.
Lafutidine, a newly developed histamine H(2)-receptor antagonist, inhibits daytime (i.e., postprandial) as well as nighttime gastric acid secretion in clinical studies. It also has gastroprotective activity that particularly affects mucosal blood flow in rats. This study focused on the efficacy of lafutidine on plasma concentrations of gastrointestinal peptides in humans. Six healthy male volunteers aged 23-32 years without Helicobacter pylori infection were orally administered either 10 mg lafutidine, 20 mg famotidine, or water only (control) 30 min after a standard meal (650 kcal). Plasma concentrations of lafutidine and famotidine were highest from 90 to 150 min after administration. Intragastric pH was elevated after both lafutidine and famotidine compared with the control. Plasma concentrations of calcitonin gene-related peptide (CGRP) and somatostatin were significantly increased after lafutidine at 60 and 90 min. We concluded that lafutidine increases plasma concentrations of CGRP and somatostatin in humans, which may result in inhibition of postprandial acid secretion and gastroprotective activity.
Shimatani
Tomohiko
T
Department of General Medicine, Hiroshima University Hospital, 1-2-3 Kasumi, Minami-ku, Hiroshima 734-8551, Japan. tshima@hiroshima-u.ac.jp
Inoue
Masaki
M
Kuroiwa
Tomoko
T
Xu
Jing
J
Nakamura
Masuo
M
Tazuma
Susumu
S
Ikawa
Kazuro
K
Morikawa
Norifumi
N
D000081:Acetamides / Q000494:pharmacology*; D000284:Administration, Oral; D000328:Adult; D015415:Biomarkers / Q000097:blood; D015740:Calcitonin Gene-Related Peptide / Q000097:blood*; D018592:Cross-Over Studies; D015738:Famotidine / Q000494:pharmacology*; D005500:Follow-Up Studies; D005744:Gastric Acid / Q000378:metabolism; D005745:Gastric Acidity Determination; D005753:Gastric Mucosa / Q000378:metabolism; D006635:Histamine H2 Antagonists / Q000494:pharmacology*; D006801:Humans; D006863:Hydrogen-Ion Concentration / Q000187:drug effects; D007124:Immunoenzyme Techniques; D008297:Male; D010880:Piperidines / Q000494:pharmacology*; D019518:Postprandial Period / Q000187:drug effects / Q000502:physiology*; D011446:Prospective Studies; D011725:Pyridines / Q000494:pharmacology*; D012016:Reference Values; D013004:Somatostatin / Q000097:blood*; D013270:Stomach / Q000187:drug effects*
D000081:Acetamides; D015415:Biomarkers; D006635:Histamine H2 Antagonists; D010880:Piperidines; D011725:Pyridines; C076948:lafutidine; D013004:Somatostatin; D015738:Famotidine; D015740:Calcitonin Gene-Related Peptide