RABIPRAZOLE AND ZINC CARNOSIN

JUSTIFICATION RATIONALE

A revolutionary discovery by Barry J. Marshall and J. Robin Warren so changed

our thinking about what causes ulcers that their research was rewarded the 2005
Nobel Prize in Physiology or Medicine. Contrary to popular belief, ulcers are not
caused only by stress, spicy foods and lifestyle mismanagement, but rather by
stomach infection with the bacterium Helicobacter pylori. This bacterium is the
culprit in nearly 80% of stomach ulcers and in more than 90% of ulcers in the
duodenum, the first portion of the small intestine.

Infection with H. pylori often causes no symptoms; it can cause gastritis, or

chronic inflammation of the lower stomach wall. This in turn results in increased
acid production from the non-infected upper stomach, which creates favorable
conditions for the erosion or ulceration of the mucosal lining in the stomach or
duodenum.

Most of the remaining ulcers are associated with the widespread use of pain
relievers known as nonsteroidal anti-inflammatory drugs, or NSAIDs. 1 Cells in the
stomach lining require chemicals known as prostaglandins to produce a thick
coating of gelatinous mucus. This mucosal lining acts as a natural defense by
keeping acid contained in digestive juices from burning the stomach wall and by
preventing harmful bacteria from entering the bloodstream or lymphatic system.
NSAIDs block the production of prostaglandins, thus relieving pain and
inflammation but also leaving the stomach lining susceptible to ulceration and
invasion by H. pylori.

When the upper region of the stomach is also infected with H. pylori, the resulting
inflammation sets the stage for stomach cancer or a specific type of stomach
lymphoma. Eradicating H. pylori is therefore important not only to avoid ulcers,
but also to lower the risk of developing malignant tumors.

Fortunately, scientists have identified novel nutraceuticals that provide

synergistic support for stomach health and integrity by relieving inflammation,
promoting tissue repair, and supporting the body’s defenses against H. pylori.
One of these remedies—a complex of zinc and carnosine—was previously
available only in Japan as a prescription drug for ulcers, but is now readily
accessible as a dietary supplement in the United States. Together, these natural
agents can serve as the foundation of a strategy to safely and effectively relieve
chronic gastric distress and restore stomach health and comfort.

Rabiprazole is fourth generation proton pump inhibitor. Its efficacy and safety has
already been clinically proven and established. USFDA approved indications are
very wide that none other proton pump inhibitors have got permission till now. It
is given for the treatment of duodenal ulcer, maintenance, Gastroesophageal
Reflux Disease (GERD), short-term treatment, Gastric ulcers, Helicobacter pylori
and Symptomatic GERD.

Activation time in minute of rabiprazole is just 1.3 whereas other proton pump
inhibitor’s activation time is 2.8 of Omeprazole, 2.0 of lansaprazole, 4.6 of
pantoprazole. Percentage of acid inhibiton within 10 minutes of rabiprazole is
100% whereas, 47% of Omeprazole, 66% of lansaprazole and 20% of
pantoprazole.

There is no food interaction with rabiprazole in comparison with other proton

pump inhibitors. Rabiprazole is safe for pregnant lady because it comes under
USFDA approved pregnancy category B. Daily dose of rabiprazole is just 20 mg
or 10 mg once but omeprazole is given 20 mg twice a day, lansaprazole 15 mg
twice a day or 30 mg once and pantoprazole is given 40 mg in a day.

Animal studies have offered clues as to the mechanism by which the zinc-
carnosine complex helps relieve stomach inflammation associated with H. pylori
infection. The zinc-carnosine complex acts as a scavenger to consume a
harmful agent called monochloramine that is released by H. pylori bacteria.
Monochloramine contributes to injury of the stomach’s lining. By
neutralizing this harmful agent, zinc-carnosine thereby reduces
inflammation of the stomach lining, prevents invasion by white blood cells,
and averts erosion of epithelial cells lining the stomach. 9,10 Other researchers
have similarly found that zinc-carnosine helps protect against gastritis
induced by monochloramine released by H. pylori, and also helps heal
existing stomach lesions related to the effects of H. pylori.

For example, in rats that are prone to develop stomach ulcers, zinc-carnosine
accelerated healing of these ulcers by increasing production of insulin-like
growth factor-1 (IGF-1), a natural defense known to promote gastric epithelial
wound repair. By stimulating IGF-1 production, zinc-carnosine was similarly
found to protect rabbit stomach cells in the laboratory, thereby promoting healing
of stomach lesions.

Zinc-carnosine has also been shown to enhance healing of the stomach

epithelial lining, by inhibiting production of pro-inflammatory interleukin-8 and by
preventing inflammatory white blood cells from adhering to epithelial cells.
Additionally, scientists have noted that zinc-carnosine decreases the
activation of nuclear factor-kappa beta (NFkB), a powerful inflammatory
mediator that scientists believe plays a role in numerous chronic disease
states such as cancer and arthritis. Scientists believe that strategies to reduce
the activity of NFkB may benefit the entire body by helping to avert such diverse
conditions as cancer, diabetes, and heart disease. (See “What Is Nuclear Factor-
Kappa Beta?” Life Extension, July 2006.) Zinc-carnosine is thus emerging as a
powerful anti-inflammatory agent offering specialized protection for the stomach.
Hence, FDC of rabiprazole and zinc carnosin would be highly efficacious and
safer combination to treat ulcers of any etiology whether eosophageal ulcer,
gastric ulcer or duodenal ulcer.

REFERRENCE

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