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What Is Relistor (Methylnaltrexone)? Why Do Opioids Cause Constipation?

is approved Relistor was approved for the treatment of opioid -induced constipation in the following countries: *In April, 2008 - approved by Health Canada. *In April, 2008 - approved by the US Food and Drug Administration (FDA). *In July, 2008 - approved by the European Commission (EMEA), representing 27 countries. How does methylnaltrexone work? *Opioids stop pain but also numb the digestive tract and reduce digestive secretions An opioid, such as morphine, kills pain by numbing the receptors in the brain. However, it also numbs the receptors in the digestive system. If the nerves in the digestive system are numbed, the muscles there will not propel undigested food and stools (it will not push the food and feces along properly). The slower the food moves through your digestive tract, the more water the colon will absorb from food. Consequently, the stools (feces) become dry and hard, leading to constipation. Opioids also cause contractions in the jenunum - the middle of the small intestine - to increase. These contractions are non-propulsive ones; they do not push the food forward. Opioids also numb the stomach to some extent, slowing down the digestive system even longer. Opioids reduce digestive secretions as well. This decreases a person"s urge to defecate (the urge to poo is much weaker). If somebody delays going to the toilet the stools will continue losing water and become harder and drier, resulting in constipation. *Relistor (Methylnaltrexone) blocks the numbing in the intestines Methylnaltrexone binds to those receptors in the gut, blocking morphine"s effects on them - so that they are not numbed any more. This means that the muscles in the gut can react normally again. *Relistor (Methylnaltrexone) does not block the opioids" painkilling effects Methylnaltrexone does not cross the brain barrier - it does not enter the brain. Morphine"s painkilling effects inside the brain continue to work. Morphine"s effects on the receptors inside the brain are what give it, and all other opioids, their painkilling qualities. If methylnaltrexone did enter the brain it would be useless because it would neutralize all morphine"s effects, including its painkilling ones - the patient would be in pain again. How effective is Relistor? Two Randomized, double-blind, placebo-controlled clinical studies In a double-blind clinical study, neither the doctor nor patient knows who is receiving the real drug, and who is getting the placebo. In a placebo-controlled clinical trial, some patients receive a placebo, others receive the real drug (Relistor), and the results are compared. In a randomized clinical trial, the patients are selected randomly (by chance) to receive either Relistor or a placebo. *62% of patients receiving Relistor in one clinical study, and 48% of patients in the other study had a bowel movement (went to the toilet successfully) within 4 hours of the first injection. *30% of patients receiving Relistor reported a bowel movement within 30 minutes of a dose of Relistor in both studies. Written by Christian Nordqvist Copyright: Medical News Today Not to be reproduced without permission of Medical News Today

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Skipjimroo commented:

My god... Please, for the love of all that is holy, master the art of the paragraph and then repost this mess.

That is all.

22.02.2010


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