Racecadotril is an anti diarrheal drug which acts as a peripherally acting enkephalinase inhibitor and help to reduces the secretion of water and electrolytes into the intestine.
Infections of the gastro intestinal tract, especially infectious diarrhea, are among the most common debilitating infectious diseases, afflicting people of all ages around the world. Diarrhea can be defined as the passage of loose or watery stools, usually at least three times in a 24 hr period it may be accompanied by anorexia, nausea vomiting, abdominal cramps. It is not a disease but sign of some infections or gastro intestinal disorders.
Indication and Usage:
â It is used for the treatment of the acute and chronic diarrhea.
â Acute diarrhea usually lasts for a few days and is typically caused by an infection of some sort caused by bacteria, viruses or parasites.
â Chronic diarrhea persists longer than does acute diarrhea, generally longer than four weeks. Chronic diarrhea can indicate a serious disorder, such as ulcerative colitis or Crohn's disease.
Mechanism of Action:
Racecadotril increases the availability of endogenous opioids (enkephalins) by inhibiting the membrane-bound enkephalinase. These enkephalins activate Î´-opioid receptors in the GI tract. This leads to a reduction in cAMP mucosal levels, resulting in a reducted secretion of water and electrolytes in the intestinal lumen.
Common Bacteria, Viruses, and Parasites that Cause Diarrhea:
E. coli : E. coli are harmless and live in the intestines of healthy humans and animals. E. coli produces a powerful toxin that can cause a severe infection.
Salmonella :Salmonella is a bacteria that infects the intestines and causes diarrhea, fever, and abdominal cramps 12 to 72 hours after infection.
Rotavirus:Rotavirus is the most common cause of severe diarrhea among children. The disease is characterized by vomiting and watery diarrhea for three to eight days, and fever and abdominal pain occur frequently.
Giardia : Giardia lamblia has become recognized as one of the most common waterborne diseases in humans in the United States. Giardia is a tiny parasite that lives in the intestines of people and animals.
Absorption: Racecadotril is quickly absorbed orally. The inhibiting activity of the plasmatic encephalinase appears in 30 minute. The amplitude and the duration of action of the racecadotril are related to the administered dose. The peak concentration is of 2.5 hrs approximately and corresponds to an inhibition of 90% of the enzymatic activity for the administered dose of 1.5 mg/kg. The duration of inhibiting activity on the plasma encephalinase is of approximately 3 hours. The half life is 3-4 hours.
Distribution:The tissue distribution is weak; it accounts for only approximately 1% of the administered dose. The racecadotril is fixed at 90% on plasma proteins (mainly albumin). The bioavailability of Racecadotril is not modified by food, but the peak of activity is delayed for 1.5 hours approximately. Duration of 4 hours action close. It does not cross the hemato-encephalic barrier.
Metabolism:Racecadotril is a prodrug, which is rapidly absorbed after by oral income and hydrolyzed to thiorphan as active metabolites.
Elimination:Racecadotril is eliminated in the urine. The repeated administration of racecadotril does not modify its pharmacokinetic properties and does not involve accumulation in the body.
Renal way: Elimination in form of metabolites.
Fecal way: Elimination in the form of metabolite .
It is contra-indicated in the event of intolerance with fructose, malabsorption of glucose and galactose or of invert sugar-isomaltase deficit. It is contra-indicated in patients with known Hypersensitivity.
From the above discussion, it can be concluded that this Racecadotril used to treat acute and chronic diarrhea because this drug help to inhibit membrane-bound enkephalinase so inhibition of enkephalinase increase the availability of endogenous opioids( enkephalins) and this enkephalins activate Î´-opioid receptors in the GI tract. This leads to a reduction in cAMP mucosal levels, resulting in a reducted secretion of water and electrolytes in the intestinal lumen.
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