Paracetamol Flashcards
Mechanism
Not fully known but some thoughts:
An indirect inhibitory effect on COX-2 in the CNS by reducing the availability of essential co-substrates.
Has some COX-3 activity - NOT IMPORTANT
Uses
Reduce pain , Antipyretic (reduce fever),
Overdose
metabolism paracetamol is normally conjugated with glucuronic acid and sulphate.
When toxic doses of paracetamol are taken (10-15g), these pathways become saturated, leading to metabolism by cyP450 enzymes (CYP2E1). = Production of toxic N-acetyl-p-benzoquinone, which can be inactivated by glutathione. However, once glutathione is depleted, N-acetyl-p-benzoquinone causes liver and kidney necrosis.
Irreversible liver damage usually reaches its peak by 72-96 hours
TREATMENT:
N-acetylcysteine must be administered within 8-10 hours of ingestion = speeds the replenishment of glutathione
IF liver damage too severe liver need replacing
Common brand names
Calpol
Co codamol = codeine + paracetomal