Opioids contribute to 70% of the negative health impact associated with drug use disorders. A new opioid withdrawal protocol using over-the-counter medications loperamide and P-glycoprotein inhibitor (omeprazole) was described by Dr Al Garhy previously. In this article successful protocol, evidenced Clinical Opiate Withdrawal Scale, is discussed in a case series.

An investigation was made of the effect of changing mean transit time (MTT) by administration of drugs which affect colonic motility on faecal microbial mass in man. Senokot was used to accelerate and codeine and/or loperamide to prolong transit in subjects maintained on a constant high fibre diet. Doses of Senokot or codeine/loperamide were adjusted to halve or double transit time measured dur...

The purpose of this study is to examine the gastrointestinal disorders after injection of vinblastine (2 mg kg-1 b.w. i.v.) in rats. Animals were divided into two equal groups: Group 1 was considered as a control group (NaCl, 0.9%). Group 2 was treated with intravenous injection of vinblastine for 7 days. Loperamide (2 mg kg-1) was injected in a saline solution subcutaneously to induce constipa...

We investigated the laxative and anti-diarrheal activity of polycarbophil, an insoluble hydrophilic polymer, in comparison with other agents used for treating functional bowel disorder (FBD). In naive rats, polycarbophil (500 mg/kg) increased fecal weight and water contents without producing diarrhea. Carboxymethylcellulose (CMC) did not produce evident changes in bowel movement. Picosulfate ma...

A facile synthesis for novel loperamide analogs as potential μ opioid receptors is described. The synthetic procedure for compound 5, which contains two 4-phenyl piperidine scaffolds, was optimized, and this compound was synthesized in excellent yield. We also describe a mild and highly efficient protocol for the synthesis of compounds 6 and 7.

The effects of KW-5092, [1-[2-[[[5-(piperidinomethyl)-2- furanyl]methyl]amino]ethyl]-2-imidazolidinylidene]propanedinitr ile fumarate, on the loperamide- or clonidine-induced delayed propulsion were determined in rats and compared with those of other gastroprokinetic agents. Administration of loperamide (0.3 mg/kg, s.c.) or clonidine (0.01 mg/kg, s.c.) induced delay of the evacuation time of th...

[(11)C]Loperamide has been proposed for imaging P-glycoprotein (P-gp) function with positron emission tomography (PET), but its metabolism to [N-methyl-(11)C] N-desmethyl-loperamide ([(11)C]dLop; [(11)C]3) precludes quantification. We considered that [(11)C]3 might itself be a superior radiotracer for imaging brain P-gp function and therefore aimed to prepare [(11)C]3 and characterize its effic...