Tag Archives: morphine

VIVA SCENE: PARACETAMOL Vs MORPHINE CENTRAL MOA

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PARACETAMOL:

Central action via COX 3 inhibition which is associated with decreased brain PGE2 levels. It also modulates endogenous cannabinoid system

MORPHINE:

Morphine work by stimulating presynaptic Gi-protein-coupled MOP and KOP opioid receptors. Binding of the ligand causes the following events:

> Closure of voltage-gated Ca2+ channels

> Decreased cAMP production

> Stimulation of K+ efflux from the cell

> Hyperpolarisation of the cell membrane.

> This leads to decreased excitability of the cell and therefore decreased neurotransmitter release and pain transmission

Morphine and Hydromorphone

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  • Morphine is metabolised via hepatic system and excreted by renal system
  • It can get accumulated in hepatic/renal dysfunction and obesity
  • Morphine has 2 metabolites:
  • Morphine 6 glucoronide- Active metabolite: responsible for analgesia and sedation
  • Morphine 3 glucoronide: Can cause seizures
  • Morphine has histamine releasing property
  • Hydromorphone is more potent than morphine
  • Hydromorphone doesnt have active metabolites
  • Hydromorphone lacks histamine release