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Loperamide

Introduction to Loperamide

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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.

Using Loperamide

Ways of Administration

Effects of Loperamide

Combinations with Loperamide

Different Uses for Loperamide


Pharmacology of Loperamide

LD50 (mg/kg) (as the hydrochloride) [1] :
Mice : 105 orally, 28 intraperitoneally, 75 subcutaneously
Rat : 185 orally

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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) [2]
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.
[1]

The Dangers of Loperamide


Physical Health Risks

<Physical Problem 1 - Please Identify and Add Others As Necessary>

<Physical Problem 2 - Please Identify and Add Others As Necessary>


Overdose


Reported Deaths


Mental Health Risks

<Mental Health Risk 1 - Please Identify and Add Others As Necessary>

<Mental Health Risk 2 - Please Identify and Add Others As Necessary>


Side Effects


Addiction

Physical Addiction

Mental Addiction


Producing/Growing Loperamide


Forms of Loperamide


United Nations

USA

EU

Other Countries


History of Loperamide


More Loperamide Sections




The Latest Loperamide Threads






References


[1]Merck Index, fifteenth edition (2013)
[2]Calculated from Atomic Weights of the Elements, 2007
[3] A Web-Based Study of Self-Treatment of Opioid Withdrawal Symptoms with Loperamide.
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