Loperamide

PHARMACOLOGY

This is primarily a mu opioid receptor agonist which acts locally to reduce intestinal motility but does not cross blood/brain barrier. Used to treat diarrhoea, to reduce fecal output and to relieve symptoms of abdominal cramping

Time to peak: up to 24 h
Plasma ½ life: 11 h

DOSING

  • 4 mg initially followed by 2 mg after each loose stool PO (max 16 mg/day)
  • In cases of ongoing diarrhoea (and where overflow diarrhoea and other treatable conditions have been ruled out) a regular dose may be needed bid
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  • 10-20 kg: 1 mg tid
  • 20-30 kg: 2 mg bid
  • More than 30 kg: 2 mg tid

UNWANTED EFFECTS

  • Constipation and overflow diarrhoea
  • Drowsiness
  • Dry mouth
  • Nausea and vomiting
  • Rarely hyperglycemia

NOTE

This information is drawn from a number of sources (see below). The reader is encouraged to access these and other relevant literature for more detail. As always, sound clinical judgment should be used in individual clinical cases. In particular, it should be remembered that there may be significant variation in the pharmokinetics of a drug resulting from a number of factors, including the individual patient’s metabolism/disease status and how the medication has been formulated.

SOURCES/REFERENCES

  1. Brunton LL, Lazo JS, Parker KL, editors. Goodman and Gilman’s: the pharmacological basis of therapeutics. 11th ed. McGraw-Hill Professional; 2006.
  2. Twycross R, Wilcock A. Palliative care formulary. 3rd ed. Radcliffe Medical Press Ltd; 2008.
  3. Repchinsky C, editor. Compendium of pharmaceuticals and specialties (CPS): the Canadian drug reference for health professionals. 44th ed. Canadian Pharmacists Association; 2009.
  4. Goldman A, Hain R, Liben S. Oxford textbook of palliative care for children. 1st ed. Oxford University Press; 2006.
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