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Loperamide
Loperamide is an opioid antidiarrheal sold under the brand name Imodium[1]. It is also commonly used to alive symptoms of opioid withdrawal, dubbed the "Poor Man's Methadone"[2]. Loperamide cannot effectively cross the Blood Brain Barrier but when used in large enough doses or in combination with P-glycoprotein inhibitor like Quinidine, enough of the drug can cross the blood brain barrier in order to illicit central morphine-like effects[3][4][5]. Loperamide taken with quinidine was found to produce respiratory depression as well as some of the recreational effects typical of other opioids. When taken at high doses Loperamide has been shown to be cardiotoxic, causing arrhythmia, and can be fatal[3].
- ↑ Drugs.com International brands for loperamide Archived 23 September 2015 at the Wayback Machine Page accessed 4 September 2015
- ↑ Stanciu CN, Gnanasegaram SA (2017). "Loperamide, the "Poor Man's Methadone": Brief Review". Journal of Psychoactive Drugs. 49 (1): 18–21. doi:10.1080/02791072.2016.1260188. PMID 27918873. S2CID 31713818.
- ↑ 3.0 3.1 Sadeque AJ, Wandel C, He H, Shah S, Wood AJ (September 2000). "Increased drug delivery to the brain by P-glycoprotein inhibition". Clinical Pharmacology and Therapeutics. 68 (3): 231–7. doi:10.1067/mcp.2000.109156. PMID 11014404. S2CID 38467170.
- ↑ Yanagita T, Miyasato K, Sato J (1979). "Dependence potential of loperamide studied in rhesus monkeys". NIDA Research Monograph. 27: 106–13. PMID 121326.
- ↑ Nakamura H, Ishii K, Yokoyama Y, Motoyoshi S, Suzuki K, Sekine Y, et al. (November 1982). "[Physical dependence on loperamide hydrochloride in mice and rats]". Yakugaku Zasshi (in Japanese). 102 (11): 1074–85. doi:10.1248/yakushi1947.102.11_1074. PMID 6892112.