This study evaluates the prophylactic effect of the peripherally-selective mu-opioid receptor agonist, loperamide, administered topically in a liposomal gel formulation on pain, inflammation, and disease progression in the adjuvant-induced model of experimental rheumatoid arthritis in female Lewis rats. In a randomized, blinded and controlled animal trial, AIA rats were divided into six groups ...

BACKGROUND Loperamide is used as an antidiarrheal drug and is available over-the-counter. It cannot pass the blood-brain barrier and it does not have a considerable abuse potential. It can lead to dangerous cardiac arrhythmia. CASE REPORT Herein, we report a 35-year-old man with a 13-year history of abusing opioids who had undergone detoxification for four times during this period. He underwe...

Abuse of over the counter drugs often gets overlooked by health care providers. Loperamide is one such over the counter drug that is often abused by drug addicts.We present here a case of a youngmale attaining euphoria from takingmassive doses of loperamide. He developed Torsades de Pointes and subsequent cardiac arrest. We found similarities in the progression of myocardial electrical conducti...

Cytochrome P450 3A4 (CYP3A4) is the major enzyme responsible for phase I drug metabolism of many anticancer agents. It is also a major route for metabolism of many drugs used by patients to treat the symptoms caused by cancer and its treatment as well as their other illnesses, for example, cardiovascular disease. To assess the ability to inhibit CYP3A4 of drugs most commonly used by our patient...

Pycnocycla spinosa Decne. ex Boiss. var. spinosa (Fam. Umbelliferae) is an essential oil-containing wild plant growing in central part of Iran. Hydroalcoholic extract of Pycnocycla spinosa has antispasmodic and antidiarrheal activity. The aim of this study was to further investigate antidiarrheal and small intestinal transit effect of P. spinosa extract for a comparison with loperamide and dicy...

P-glycoprotein (P-gp) and CYP3A (cytochrome P450 3A, generally; Cyp3a, rodent enzyme) in the intestine can attenuate absorption of orally administered drugs. While some suggest that P-gp enhances intestinal metabolism by CYP3A/Cyp3a during absorption of a dual substrate, others suggest that P-gp reduces the metabolism in the intestine when substrates are at subsaturating concentrations. Hence, ...