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Talk:Loperamide: Difference between revisions
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==Pharmacology== | ==Pharmacology== | ||
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Loperamide is an [[opioid]]-[[receptor]] [[agonist]] and acts on the μ-opioid receptors in the myenteric plexus of the large intestine. Loperamide works like [[morphine]], decreasing the activity of the myenteric plexus, which decreases the tone of the longitudinal and circular smooth muscles of the intestinal wall. It is considered to have a low abuse potential because of substantial first-pass metabolism and P-glycoprotein-mediated efflux at the level of the blood-brain barrier. Central nervous system opioid effects are not observed after therapeutic [[oral]] dosing because of poor bioavailability and minimal central nervous system penetration. However, central nervous system opioid effects do occur after supratherapeutic oral doses.<ref name="Loperamide Death">Loperamide Abuse Associated With Cardiac Dysrhythmia and Death. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/27140747</ref> | Loperamide is an [[opioid]]-[[receptor]] [[agonist]] and acts on the μ-opioid receptors in the myenteric plexus of the large intestine. Loperamide works like [[morphine]], decreasing the activity of the myenteric plexus, which decreases the tone of the longitudinal and circular smooth muscles of the intestinal wall. It is considered to have a low abuse potential because of substantial first-pass metabolism and P-glycoprotein-mediated efflux at the level of the blood-brain barrier. Central nervous system opioid effects are not observed after therapeutic [[oral]] dosing because of poor bioavailability and minimal central nervous system penetration. However, central nervous system opioid effects do occur after supratherapeutic oral doses.<ref name="Loperamide Death">Loperamide Abuse Associated With Cardiac Dysrhythmia and Death. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/27140747</ref> | ||