Loperamide <Insert brief 3 line introduction here>
Introduction to Loperamide
Loperamide is a piperidine derivative, opioid agonist thought to have a low potential for central nervous effects. It was launched by Janssen Pharmaceutica in 1973. On release loperamide was classified in the US as a schedule II narcotic, before transfer to to schedule V in 1977. In November 1982 loperamide was removed from schedule V or 'decontrolled'.
This appears to have been based on initial, preclinical studies indicative of dependence and withdrawal in animal studies. The consensus of later studies was that loperamide has a low potential for abuse, based on an apparent lack of central nervous effects.
Loperamide's primary indications lie in the symptomatic treatment of some forms of diarrhoea and gastrointestinal inflammation. In this context it is included in the World Health Organization's List of Essential Medicines (for basic healthcare systems).
Web and internet forum based discussion of loperamide seems to be focused on two topics related to opioid use; its application in the management of withdrawal and its potential for central nervous effects. Appearing in threads or posts on various forums as early as 2005, there appears to have been a sustained increase in interest in loperamide.
Ways of Administration
Effects of Loperamide
Combinations with Loperamide
Different Uses for Loperamide
Pharmacology of Loperamide
LD50 (mg/kg) (as the hydrochloride)  :
Mice : 105 orally, 28 intraperitoneally, 75 subcutaneously
Rat : 185 orally
Chemistry of Loperamide
Column 1 Column 2 Systematic(IUPAC) name: 4-[4-(4-Chlorophenyl)-4-hydroxypiperidin-1-yl]-N,N-dimethyl-2,2-diphenylbutanamide Synonyms: 4-(4-Chlorophenyl)-4-hydroxy-N,N-dimethyl-α,α-diphenyl-1-piperidinebutanamide, 4-(p-Chlorophenyl)-4-hydroxy-N,N-dimethyl-α,α-diphenyl-1-piperidinebutyramide; PJ-185, R-18553, Arret, Blox, Brek, Dissenten, Fortasec, Imodium, Imosec, Imossel, Lopermid, Lopemin, Loperyl, Suprasec, Tebloc (hydrochloride) Molecular Formula: C29H33ClN2O2, C29H33ClN2O2.HCl (hydrochloride) Molar mass: 477.04 g/mol, 513.50 g/mol (hydrochloride)  CAS Registry Number: 53179-11-6, 34552-83-5 (hydrochloride) Melting Point: 222-223°C (hydrochloride) Boiling Point: 647.2 °C at 760 mmHg (Predicted) Flash Point: no data Solubility: Hydrochloride 1.4 mg/mL (water, pH 1.7), 0.08 mg/mL (citrapte-phosphate pH 6.1), <0.01 mg/mL (citrate-phosphate pH 7.9), 286 mg/mL (methanol), 53.7 mg/mL (ethanol), 11.1 mg/mL (isopropanol), 351 mg/mL (dichloromethane), 2.0 mg/mL (acetone), 0.35 mg/mL (ethyl acetate), < 0.01 mg/mL (diethyl ether), <0.01 mg/mL (hexane), 0.01 mg/mL (toluene), 103 mg/mL (dimethylformamide), 3.2 mg/mL (tetrahydrofuran), 0.20 mg/mL (4-methyl-2-pentanone), 56.4 mg/mL (propylene glycol), 14.0 mg/mL (polyethylene glycol 400), 205 mg/mL (dimethylsulfoxide), 1.8 (2-butanone); freely soluble in chloroform; slightly soluble in dilute acids; practically insoluble in water at physiological pH (0.002%). Additionnal data: pKa 8.66 Notes: Hydrochloride crystallized from isopropanol; stable, can be stored for several years under normal conditions; not hygroscopic; not affected by light.
The Dangers of Loperamide
Physical Health Risks
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Mental Health Risks
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Forms of Loperamide
Legal Status of Loperamide
History of Loperamide
More Loperamide SectionsLoperamide
Merck Index, fifteenth edition (2013)
Calculated from Atomic Weights of the Elements, 2007
 A Web-Based Study of Self-Treatment of Opioid Withdrawal Symptoms with Loperamide.