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Jakarta, 28 Dec 2009

The Importance of NSAIDs Enteropathy

The Importance of NSAIDs Enteropathy


The deleterious effects of non-steroidal anti-inflammatory drugs (NSAIDs) on the stomach and duodenum are well established and reported. However, the effects of these agents on the more distal portions of the small intestine (NSAIDs-enteropathy) is not as widely publicised despite the fact that the small bowel is more susceptible to the damaging effects of NSAIDs than the stomach.1,2
There are many reasons for the low awareness of NSAID enteropathy. The single most important reason for underestimating the clinical importance of NSAIDs enteropathy is the difficulty in making a diagnosis.
The condition is usually asymptomatic and diagnosis has until recently, only been possible with the use of tests that are not widely available such as Cr-EDTA tests, indium-labelled leucocyte technique, faecal calprotectin measurements, enteroscopy and the latest capsule endoscopy technique.3   

However, the most important factor is that pharmaceutical companies with invested interest in “gastroprotective” agents drove the recognition of the side effects of NSAIDs on the gastrointestinal tract.

It is important to note that it has been shown beyond any reasonable doubt that selective COX-1 inhibition does not lead to gastrointestinal damage. But in contrast with prevailing theories about the “housekeeping” function of COX-1 and role of COX-2 in inflammation, it is clear that selective COX-2 inhibition (not COX-1 inhibition) leads to small bowel damage (stomach is apparently unaffected).

The pathogenesis of NSAID induced gastrointestinal damage can now be viewed as the combination of COX-1 inhibition (restricting mucosal blood flow), COX-2 inhibition (through an unknown “immunological” mechanism), and the topical effect of NSAIDs.4 Together these cause a breach in mucosal integrity. In the stomach this exposes the mucosa to acid and pepsin causing erosions and ulcers with Helicobacter pylori playing an additional part. In the small bowel the permeability increase exposes the mucosa to bile acids and bacteria, which results in inflammation, erosions, and ulcers.

Mucosta® is an anti gastritis and gastropathy drug with Rebamipide as it’s active ingredient. The molecular weight of Rebamipide is 370.79. Mucosta® is classified as anti-inflammatory, anti free-radical drug. As anti-inflammation drug, Mucosta® suppress inflammation process due to the release of inflammatory cytokine, such as IL-8, TNF-α, IL-1ß. By inhibiting the release of free radical, superoxide (O2-) and also scavenge hydroxyl radical (OH-) Mucosta® shows its action as anti free-radical.

Mucosta® , a prostaglandin-inducing gastroprotective drug, promotes the synthesis of endogen prostaglandin which helps to reduce the recurrences of ulcer, improve gastroduodenal mucosal defense against aggressive factor, like gastric acid, infection due to H. pylori, NSAIDs, and other stressors.

Mucosta® is indicated in the treatment of gastritis, gastropathy (due to NSAIDs, steroid, or antibiotics), gastric ulcer, and to overcome acute gastroduodenal mucosal lesions due to administration of NSAIDs, steroid, or antibiotics. Mucosta® has strong penetration into gastrointestinal mucosal with minimal systemic effect. Mucosta® does not interact and does not interfere with the absorption of other drugs which often given together (NSAIDs, antibiotics) . In that way, Mucosta® does not affect the effectiveness of those drugs.  

Mucosta® is effective, not only to prevent gastric mucosal injuries (gastropathy), but in small intestinal (enteropathy) as well.
Mucosta® is the first choice medication for NSAID gastropathy and enteropathy.

Reference :

  1. Smale S, Tibble J, Sigthorsson G, et al. Epidemiology and differential diagnosis of NSAID-induced injury to the mucosa of the small intestine. Best Pract Res Clin Gastroenterol 2001 ;15 :723-38.
  2. Fortun PJ, Hawkey CJ. Nonsteroidal anti-inflammatory drugs and the small intestine. Curr Opin Gastroenterol 2005 ;21 :169-75.
  3. Adebayo D, Bjarnason I. Is non-steroidal anti-inflammatory drug (NSAID) enteropathy clinically more important than NSAID gastropathy ? Postgrad Med J 2006;82:186-191.
  4. Whittle BJR. Mechanisms underlying intestinal injury induced by anti-inflammatory COX inhibitors. Eur J Pharmacol 2004;500:427-39.



Philip Darmawan, MD., MKT.
Medical Advisor
pdsony@ho.otsuka.co.id

 
     
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