| Loperamide and P-glycoprotein inhibition: assessment of the clinical relevance. | |
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MedLine Citation:
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PMID: 20604828 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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OBJECTIVES: Loperamide is a peripherally acting mu opioid receptor agonist and an avid substrate for P-glycoprotein. This may give rise to drug-drug interactions and increased risk for central adverse effects. The objective of this study was to re-evaluate the predictability of non-clinical data using loperamide as a probe P-glycoprotein substrate. We searched the literature for papers containing data on drug-drug interactions of loperamide-containing products in humans. We also reviewed the internal worldwide safety database of Johnson & Johnson for spontaneous case reports suggestive of a central opioid effect after coadministration of loperamide with a P-glycoprotein inhibitor or substrate. KEY FINDINGS: Only one of the ten studies in our review supported the finding that inhibition of P-glycoprotein is associated with clinically relevant signs or symptoms of central nervous system (CNS) depression/opioid toxicity of loperamide. None of the 25 spontaneous case reports of interest were suggestive of signs or symptoms of CNS depression/opioid toxicity due to coadministration of loperamide and a P-glycoprotein inhibitor or substrate. SUMMARY: Based on a review of the literature and a cumulative review of the spontaneous case reports, there is insufficient evidence that an interaction between loperamide and a P-glycoprotein inhibitor or substrate is associated with clinical symptoms of CNS depression/opioid toxicity when loperamide is taken at the recommended dose. |
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Authors:
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Joris Vandenbossche; Maarten Huisman; Yimei Xu; Dawn Sanderson-Bongiovanni; Paul Soons |
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Publication Detail:
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Type: Journal Article; Review |
Journal Detail:
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Title: The Journal of pharmacy and pharmacology Volume: 62 ISSN: 2042-7158 ISO Abbreviation: J. Pharm. Pharmacol. Publication Date: 2010 Apr |
Date Detail:
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Created Date: 2010-07-07 Completed Date: 2011-01-14 Revised Date: 2011-09-13 |
Medline Journal Info:
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Nlm Unique ID: 0376363 Medline TA: J Pharm Pharmacol Country: England |
Other Details:
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Languages: eng Pagination: 401-12 Citation Subset: IM |
Affiliation:
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Clinical Pharmacology, Johnson & Johnson Pharmaceutical Research & Development, Beerse, Belgium. jvdbossc@its.jnj.com |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Analgesics, Opioid
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adverse effects* Central Nervous System / drug effects* Drug Interactions* Humans Loperamide / adverse effects* P-Glycoprotein / antagonists & inhibitors* |
| Chemical | |
Reg. No./Substance:
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0/Analgesics, Opioid; 0/P-Glycoprotein; 53179-11-6/Loperamide |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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