![]() ![]() ![]() This can be potentiated by concurrent use of CYP 3A4 inhibitors or P-glycoprotein inhibitors, such as the widely available OTC antihistamine cimetidine (Tagamet). When taken at supertherapeutic doses (above 200mg daily), however, people may experience clinically-significant CNS effects similar to an opioid intoxication: miosis, sedation, respiratory depression. These qualities led to the common assertion that loperamide had no potential for abuse. The absorbed drug is subjected to first pass metabolism (liver metabolizes majority of drug) primarily by CYP 3A4 and concentrations in the CNS kept even lower due to active efflux of the drug by P-glycoprotein transporters. Loperamide is a synthetic mu-opioid receptor agonist with a bioavailability (amount actually absorbed that enters bloodstream) of <2% when taken orally at therapeutic doses of 8-16mg daily. At costs around $10 for 200 tablets, loperamide is a significantly cheaper and infinitely more legal option than heroin or illicitly-acquired opioid analgesics, and has the added benefit of being undetectable on routine toxicology screening. Loperamide, a seemingly-innocuous anti-diarrheal agent on the WHO list of essential medications has becoming increasingly used as a substitute for opioid analgesics and a means of managing withdrawal symptoms. Answer: The increasing rates of opioid addiction and simultaneously increasing barriers to acquiring licit opioid analgesics have forced many patients to seek alternative means managing their addiction. ![]()
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