Difference between revisions of "Loperamide"
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| − | '''Loperamide''' ({{pron-en|loʊˈpɛrəmaɪd}}) a synthetic [[piperidine]] derivative,<ref>[http://www.cancer.gov/Templates/drugdictionary.aspx?CdrID=41911 US National Cancer Institute, Drug Dictionary]</ref> is an opioid [[medication|drug]] effective against [[diarrhea]] resulting from [[gastroenteritis]] or [[inflammatory bowel disease]]. In most countries it is available generically and under brand names such as '''Lopex''', '''Imodium''', '''Dimor''', '''Fortasec''' and '''Pepto''' Diarrhea Control. It was | + | '''Loperamide''' ({{pron-en|loʊˈpɛrəmaɪd}}) a synthetic [[piperidine]] derivative,<ref>[http://www.cancer.gov/Templates/drugdictionary.aspx?CdrID=41911 US National Cancer Institute, Drug Dictionary]</ref> is an opioid [[medication|drug]] effective against [[diarrhea]] resulting from [[gastroenteritis]] or [[inflammatory bowel disease]]. In most countries it is available generically and under brand names such as '''Lopex''', '''Imodium''', '''Dimor''', '''Fortasec''' and '''Pepto''' Diarrhea Control. It was developed at [[Janssen Pharmaceutica]].{{Citation needed|date=May 2010}} |
==History== | ==History== | ||
| Line 44: | Line 44: | ||
==Contraindications== | ==Contraindications== | ||
| − | The use of Loperamide (Imodium) in children under 2 years is not recommended. There have been rare reports of fatal [[paralytic ileus]] associated with [[abdominal distention]]. Most of these reports occurred in the setting of acute [[dysentery]], overdose, and with very young children less than two years of age.<ref>http://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?id=6651</ref> | + | The use of Loperamide (Imodium) in children under 2 years is not recommended. There have been rare reports of fatal [[paralytic ileus]] associated with [[abdominal distention]]. Most of these reports occurred in the setting of acute [[dysentery]], overdose, and with very young children less than two years of age.<ref>http://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?id=6651</ref> In 1990, all |
| + | pediatric formulations of the antidiarrheal loperamide (Imodium and others) were banned in [[Pakistan]].<ref>http://www.essentialdrugs.org/edrug/archive/199708/msg00056.php</ref> | ||
Treatment should be avoided in the presence of [[fever]] or if the stool is bloody ([[dysentery]]).<ref name="Butler2008">{{Cite journal|author=Butler T |title=Loperamide for the treatment of traveler's diarrhea: broad or narrow usefulness? |journal=Clinical Infectious Diseases |volume=47 |issue=8 |pages=1015–6 |year=2008 |month=October |pmid=18781871 |doi=10.1086/591704}}</ref> It is of no value in diarrhoea caused by [[cholera]], [[Shigella]] or [[Campylobacter]].<ref name="Butler2008"/> Treatment is not recommended for patients that could suffer detrimental effects from rebound [[constipation]]. If there is a suspicion of diarrhea associated with organisms that can penetrate the intestinal walls, such as [[Escherichia coli O157:H7|E. coli O157:H7]] or [[salmonella]], loperamide is [[contraindicated]]. | Treatment should be avoided in the presence of [[fever]] or if the stool is bloody ([[dysentery]]).<ref name="Butler2008">{{Cite journal|author=Butler T |title=Loperamide for the treatment of traveler's diarrhea: broad or narrow usefulness? |journal=Clinical Infectious Diseases |volume=47 |issue=8 |pages=1015–6 |year=2008 |month=October |pmid=18781871 |doi=10.1086/591704}}</ref> It is of no value in diarrhoea caused by [[cholera]], [[Shigella]] or [[Campylobacter]].<ref name="Butler2008"/> Treatment is not recommended for patients that could suffer detrimental effects from rebound [[constipation]]. If there is a suspicion of diarrhea associated with organisms that can penetrate the intestinal walls, such as [[Escherichia coli O157:H7|E. coli O157:H7]] or [[salmonella]], loperamide is [[contraindicated]]. | ||
Revision as of 15:38, 20 September 2010
| File:Loperamide.svg | |
| File:Loperamide2mg.JPG | |
| Systematic (IUPAC) name | |
|---|---|
|
4-[4-(4-chlorophenyl)-4-hydroxypiperidin-1-yl]- N,N-dimethyl-2,2-diphenylbutanamide | |
| Clinical data | |
| Pregnancy category |
|
| Routes of administration | oral, insufflation |
| Legal status | |
| Legal status |
|
| Pharmacokinetic data | |
| Bioavailability | Not significantly absorbed from the gut |
| Protein binding | 97% |
| Metabolism | hepatic |
| Biological half-life | 9.1 to 14.4 hours (average 10.8 hours) |
| Identifiers | |
| CAS Number | 53179-11-6 34552-83-5 (with HCl) |
| ATC code | A07DA03 (WHO) A07DA05 |
| PubChem | CID 3955 |
| DrugBank | APRD00275 |
| ChemSpider | 3818 |
| Chemical data | |
| Formula | C29H33ClN2O2 |
| Molar mass | 477.037 g/mol (513.506 with HCl)[[Script error: No such module "String".]] |
| (verify) | |
Loperamide (pronounced /loʊˈpɛrəmaɪd/) a synthetic piperidine derivative,[2] is an opioid drug effective against diarrhea resulting from gastroenteritis or inflammatory bowel disease. In most countries it is available generically and under brand names such as Lopex, Imodium, Dimor, Fortasec and Pepto Diarrhea Control. It was developed at Janssen Pharmaceutica.[citation needed]
Contents
History
Loperamide was approved in the United States by the FDA in 1976, when it was also placed on schedule V. It was descheduled in 1982, and became available over the counter in 1988.[3]
Mechanism of action
Loperamide is an opioid-receptor agonist and acts on the μ-opioid receptors in the myenteric plexus of the large intestine; by itself it does not affect the central nervous system like other opioids.
It works by decreasing the activity of the myenteric plexus, which, like morphine, decreases the tone of the longitudinal smooth muscles but increases tone of circular smooth muscles of the intestinal wall. This increases the amount of time substances stay in the intestine, allowing for more water to be absorbed out of the fecal matter. Loperamide also decreases colonic mass movements and suppresses the gastrocolic reflex.[4]
Loperamide molecules do not cross the blood-brain barrier in significant amounts, and, thus, it has no analgesic or euphoric properties. Any that do cross the blood-brain barrier are quickly exported from the brain by P-glycoprotein (Pgp), also known as multidrug resistance protein (MDR1). Tolerance in response to long-term use has not been reported.
However, loperamide has been shown to cause a mild physical dependence during preclinical studies, specifically in mice, rats, and rhesus monkeys. Symptoms of mild opiate withdrawal have been observed following abrupt discontinuation of long-term therapy with loperamide.[5][6]
Contraindications
The use of Loperamide (Imodium) in children under 2 years is not recommended. There have been rare reports of fatal paralytic ileus associated with abdominal distention. Most of these reports occurred in the setting of acute dysentery, overdose, and with very young children less than two years of age.[7] In 1990, all pediatric formulations of the antidiarrheal loperamide (Imodium and others) were banned in Pakistan.[8]
Treatment should be avoided in the presence of fever or if the stool is bloody (dysentery).[9] It is of no value in diarrhoea caused by cholera, Shigella or Campylobacter.[9] Treatment is not recommended for patients that could suffer detrimental effects from rebound constipation. If there is a suspicion of diarrhea associated with organisms that can penetrate the intestinal walls, such as E. coli O157:H7 or salmonella, loperamide is contraindicated.
Effectiveness
Studies have shown loperamide to be more effective than diphenoxylate, attapulgite or bismuth subsalicylate for the treatment of acute diarrhea. For the treatment of chronic diarrhea, loperamide was found to be as effective as, or slightly more so than, diphenoxylate.[3]
Crossing the blood-brain barrier
Concurrent administration of P-glycoprotein inhibitors such as quinidine and its other isomer quinine (although much higher doses must be used), PPIs like omeprazole (Prilosec OTC), venlafaxine (Effexor), and even black pepper (piperine as the active ingredient) could potentially allow loperamide to cross the blood-brain barrier. It should however be noted that only quinidine with loperamide was found to produce respiratory depression, indicative of central opioid action.[10]
See also
- Simethicone - an anti-flatulent frequently combined with Loperamide in medications
- Gastroenteritis
- Traveler's diarrhea
References
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de:Loperamides:Loperamida fa:لوپرامید fr:Lopéramide hr:Loperamid it:Loperamide hu:Loperamid nl:Loperamide ja:ロペラミド pl:Loperamid pt:Loperamida ru:Лоперамид sv:Loperamid
yi:לאפעראמיד- ↑ "Loperamide Hydrochloride." DailyMed.
- ↑ US National Cancer Institute, Drug Dictionary
- ↑ 3.0 3.1 "www.imodium.com" (PDF). Retrieved 2010-07-27.
- ↑ Katzung, Bertram G. Basic and Clinical Pharmacology, 9th ed. (2004). ISBN 0-07-141092-9[page needed]
- ↑ Yanagita T, Miyasato K, Sato J (1979). "Dependence potential of loperamide studied in rhesus monkeys". NIDA Research Monograph. 27: 106–13. PMID 121326.
- ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
- ↑ http://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?id=6651
- ↑ http://www.essentialdrugs.org/edrug/archive/199708/msg00056.php
- ↑ 9.0 9.1 Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
- ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
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