"I just wanted to tell you that loperamide WILL WORK": a web-based study of extra-medical use of loperamide.

AIMS: Many websites provide a means for individuals to share their experiences and knowledge about different drugs. Such User-Generated Content (UGC) can be a rich data source to study emerging drug use practices and trends. This study examined UGC on extra-medical use of loperamide among illicit opioid users. METHODS: A website that allows for the free discussion of illicit drugs and is accessible for public viewing was selected for analysis. Web-forum posts were retrieved using web crawlers and retained in a local text database. The database was queried to extract posts with a mention of loperamide and relevant brand/slang terms. Over 1290 posts were identified. A random sample of 258 posts was coded using NVivo to identify intent, dosage, and side-effects of loperamide use. RESULTS: There has been an increase in discussions related to loperamide's use by non-medical opioid users, especially in 2010-2011 Loperamide was primarily discussed as a remedy to alleviate a broad range of opioid withdrawal symptoms, and was sometimes referred to as "poor man's" methadone. Typical doses ranged 70-100mg per day, much higher than an indicated daily dose of 16mg. CONCLUSIONS: This study suggests that loperamide is being used extra-medically to self-treat opioid withdrawal symptoms. There is a growing demand among people who are opioid dependent for drugs to control withdrawal symptoms, and loperamide appears to fit that role. The study also highlights the potential of the Web as a "leading edge" data source in identifying emerging drug use practices.

Prospective randomized double-blind trial of racecadotril compared with loperamide in elderly people with gastroenteritis living in nursing homes.

AIM: Our aim was to compare the efficacy and tolerability of loperamide and racecadotril in elderly patients with acute diarrhea. RESEARCH DESIGN AND METHODS: We performed a randomized, prospective, double-blind, and parallel group design implemented in geriatric nursing homes in Catanzaro, Italy, from February 2008 to March 2009. Patients of both sexes were randomly allocated to receive either one tablet of racecadotril 100 mg every 8 h or two tablets of loperamide 2.0 mg followed by one tablet after each unformed stool, up to four tablets in any 24-h period. Patients were treated until recovery, defined as the production of two consecutive normal stools or no stool production for a period of 12 h. RESULTS: Normal stools were collected 36 +/- 4 h after the beginning of racecadotril and in 63 +/- 6 h from the beginning of loperamide administration (P < 0.01). The median time of abdominal pain in the intent-to-treat (ITT) population was 14 h for racecadotril and 28 h for loperamide. In the per-protocol (PP) population, the median time of abdominal pain was 14 h for racecadotril and 32 h for loperamide (P < 0.01). About the 50% of patients experienced at least one adverse event during the study: 12% in the racecadotril group and 60% in the loperamide group. The most frequently occurring adverse events were nausea and constipation. Genetic analysis did not report the presence of rapid or poor metabolizers. Pharmacoeconomic analysis performed at the end of our study documented an increase in costs in the loperamide group with respect to the racecadotril group (P < 0.01). CONCLUSIONS: Racecadotril is more effective than loperamide-probably due to drug interaction with loperamide-and it is not related to pharmacogenetic susceptibility. Racecadotril is also more cost effective than loperamide.

Possible therapeutic use of loperamide for symptoms of lactose intolerance.

OBJECTIVES: To examine a potential practical therapeutic use of loperamide (Lo) to decrease the symptoms of lactose intolerance. SUBJECTS AND METHODS: Nineteen (eight men, 11 women) healthy lactose maldigesters (18 of 19 with symptoms) underwent a 25 g lactose challenge on five separate days. Breath hydrogen was measured, areas under the curve (AUC) were calculated for 4 h, and 4 and 12 h symptom scores were recorded. After establishing baseline measurements, test doses of 4 mg, 8 mg and 12 mg Lo were randomly administered without placebo in a double-blind manner. As well, each subject received seven lactase tablets, in a random, unblinded manner. RESULTS: The median AUC and mean oral cecal transit time followed dose response expectations; however, only lactase treatment achieved significance. Nevertheless, 8 mg Lo significantly improved symptom scores, which were statistically indistinguishable from those of lactase. Four subjects complained of delayed constipation and cramps with various doses of Lo. CONCLUSIONS: Lo monotherapy for lactose intolerance is not economical and may have some side effects. However, Lo may be studied further as an adjunctive treatment of lactose intolerance in an effort to reduce the need for complete lactose digestion. Such a manoeuvre may allow rapid colonic adaptation, which in turn may be beneficial for prophylaxis for a number of colonic diseases.

Benefit/risk considerations with respect to OTC-descheduling of loperamide.

The main criteria to be considered for releasing an antidiarrhoeal from a prescription to an OTC-drug are guaranteed quality control, established efficacy and safety and the evaluation of the drug experience on major markets. Besides the considerable benefits from a socio-economic point of view, the risk for potential inappropriate use of loperamide (CAS 53179-11-6) as self-medication can be minimized by its use being avoided in children of 5 years of age or less (e.g. by making available a solid formulation only), by limiting the treatment duration to 48 h, and by contraindicating the use of the drug in cases of fever (> 38 degrees C) and/or blood in the stools. On the basis of a broad review loperamide can be considered to be efficacious in acute non-specific, acute functional and traveller's diarrhoea. The agent has a good safety profile if the mentioned restrictions are born in mind. Loperamide thus satisfies the OTC criteria.