Home » Drug Information » FDA Approved Drugs » 2002
Medical Areas: Gastroenterology | Family Medicine
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Aciphex (rabeprazole sodium)
The following drug information is obtained from various newswires, published
medical journal articles, and medical conference presentations.
Company: Elan Pharmaceuticals
Approval Status: Approved February 2002
Treatment Area: Symptomatic gastroesophageal reflux disease
In February 2002, the indications for Aciphex were expanded to
include the treatment of patients with symptomatic gastroesophageal
reflux disease (GERD). Aciphex, a proton pump inhibitor, can now be
used for the treatment of daytime and nighttime heartburn and other
symptoms associated with GERD.
Individuals with symptomatic GERD often suffer from heartburn,
belching and regurgitation (when digestive acid moves back up the
esophagus). In contrast to those with erosive GERD, patients with
symptomatic GERD do not have evidence of erosion to the esophagus.
Heartburn, which affects over 60 million Americans on a monthly
basis, is the most common symptom of symptomatic GERD.
Prior to this new indication, Aciphex was approved for the
healing of erosive GERD, the maintenance of healed erosive GERD,
and the healing of duodenal ulcers. Aciphex is also used for the
treatment of pathological hypersecretory conditions, such as
Two multicenter, double-blind, placebo-controlled trials
evaluating Aciphex were conducted in the United States. The trials
included 316 subjects with daytime and nighttime heartburn who did
not have esophageal erosions. Subjects received either Aciphex 10
mg, Aciphex 20 mg or placebo, and they were given a diary to keep
track of their GERD symptoms. Subjects returned for assessment at
week two and four.
Trials results demonstrated that the percentage of
heartburn-free daytime and/or nighttime periods was significantly
greater with Aciphex 20 mg than with placebo. Additionally, daily
antacid consumption was significantly reduced with Aciphex versus
placebo over four weeks of treatment.
Treatment with rabeprazole has been generally well tolerated in
both short-term and long-term trials.
In the two US trials, the most common adverse events potentially
related to Aciphex 20 mg (and occurring at greater than 2%
frequency) were abdominal pain, diarrhea and headache.
Mechanism of Action
Rabeprazole belongs to a class of antisecretory compounds
(substituted benzimidazole proton-pump inhibitors) that do not
exhibit anticholinergic or histamine H2-receptor antagonist
properties, but suppress gastric acid secretion by inhibiting the
gastric H+, K+ ATPase at the secretory surface of the gastric
parietal cell. Because this enzyme is regarded as the acid (proton)
pump within the parietal cell, rabeprazole has been characterized
as a gastric proton-pump inhibitor. Rabeprazole blocks the final
step of gastric acid secretion.
In gastric parietal cells, rabeprazole is protonated,
accumulates, and is transformed to an active sulfenamide. When
studied in vitro, rabeprazole is chemically activated at pH 1.2
with a half-life of 78 seconds. It inhibits acid transport in
porcine gastric vesicles with a half-life of 90 seconds. (from
Aciphex Prescribing Information)
Aciphex is referred to as Pariet outside of the United States.
Aciphex was discovered and developed by Eisai, and it is
co-marketed in the United States by Eisai and Janssen
For additional information on Aciphex, please visit the product
web site at www.aciphex.com.
Individuals interested in learning more about GERD can obtain
information from the National Institute of Diabetes and Digestive and