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Loperamide

Class
  • Synthetic piperidine derivative (opioid) antidiarrhoeal
Indications
Administration/Absorption
  • Oral
  • Not significantly absorbed from the gut
Dosage

Distribution
  • Does cross the blood-brain barrier
    • However it is immediately pumped back out into non–central nervous system (CNS) circulation by P-glycoprotein
    • This mechanism effectively shields the CNS from exposure (and thus risk of CNS addiction) to loperamide
  • NB many drugs are known to inhibit P-glycoprotein and may thus render the CNS vulnerable to opiate agonism by loperamide
Mechanism
Excretion
  • Unchanged in faeces
  • Half life 9.1 to 14.4 hours (average 10.8 hours)
Side effects
  • Abdominal pain and bloating, nausea, vomiting and constipation
Interactions
Contraindications

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