Gv. Ohning et al., Rabeprazole produces rapid, potent, and long-acting inhibition of gastric acid secretion in subjects with Helicobacter pylori infection, ALIM PHARM, 14(6), 2000, pp. 701-708
Aim: To compare acid inhibiting activity and duration of action of differen
t doses of rabeprazole, a substituted benzimidazole characterized as a high
ly potent and irreversible H+, K+-ATPase inhibitor, administered for 7 days
to subjects infected with Helicobacter pylori.
Methods: A total of 38 subjects (mean age 39.3 years) were enrolled in a si
ngle-centre, double-blind, randomized, crossover study. All subjects were c
onfirmed positive for H. pylori by C-14 urea breath test and ELISA serologi
es. Subjects were divided into two groups of 19 to receive two doses of rab
eprazole, either 5 and 20 mg or 10 and 40 mg, and placebo, given in random
order daily in the morning for 7 days. Peptone-stimulated acid, pH, and gas
trin measurements were made for 24 h after the 1st dose and for 48 h after
the 7th dose.
Results: Peptone-stimulated acid secretion rates were decreased from 12.5 t
o 6.7, 4.0, 1.5, and 0.26 h after initial 5, 10, 20, and 40 mg doses, respe
ctively; to 7.3, 4.3, 2.1, and 1.2 mmol/h 23 h after the initial dose; and
to 2.4, 2.6, 0.6, and 0.8 mmol/h 23 h after the 7th dose. After 48 h, stimu
lated acid secretion had recovered less than 40% for all treatment groups c
ompared to placebo. Median intragastric pH also increased from 2.0 with pla
cebo to 4.9, 6.2, 6.6 and 6.9 during the 24-h period after the 7th dose of
5, 10, 20, and 40 mg. The 20 mg dose of rabeprazole produced equivalent aci
d inhibition to the 40 mg dose with less increase in plasma gastrin.
Conclusion: Rabeprazole in doses from 5 to 40 mg was a highly effective inh
ibitor of gastric acid secretion in subjects infected with H. pylori. The i
nhibition was rapid, dose-related, and long-acting, with less than 50% reco
very of acid by 48 h after the 7th dose. The optimal acid inhibitory dose i
n these subjects appeared to be 20 mg daily, however 5 mg and 10 mg doses p
roduced potent inhibition of gastric acid secretion.