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Non-steroidal anti-inflammatory drugs : aspirin & paracetamol…

- - - - NSAID + antiplatelet effect
      - Non selective COX inhibitor
        
        Acts irreversible by acetylating certain aa residue in COX proteins
    - - analgesic and antipyretic dose
        
        2.5g/day
      - anti-inflammatory dose
        
        5-8g/day (high)
      - Antiplatelet effect
        
        80-160 mg/day
        
        Decrease TXA2 by COX-1 platelet
        
        The slow release tablets hepatic first pass metabolism exceeds 90% -> allows marked effect on platelets in portal blood but limits the effect on endothel to mesenteric vessels.
        
        Good for prevention of AMI and stroke
    - - high dose
        
        displacement of other drugs
    - - hydrolyzed rapidly to free salicylate in plasma
      - upon first pass in the liver with the formed salicylate -> reversible COX inhibitor
    - - saturated with higher dose -> non-linear pharmacokinetics
      - Unchanged fraction of salicylate is excreted by the kidney depending on urinary pH
    - - Low dose
        
        may lead to uric acid retention by competitive inhibition of urate secretion in the proximal tubule
      - High dose
        
        increase renal urate excretion by inhibiting urate reabsorption
    - - Hepatic damage
      - Reye's syndrome
        
        hepatic failure
        
        encephalopathy in children with viral infection
      - Urate retention
      - Stimulation of the respiratory center
        
        respiratory alkalosis
    - - CNS symptoms
        
        Hearing disturbance
        
        Confusion
        
        signs of mild overdose
      - Metabolic disturbance
        
        Uncoupling of oxidative phosphorylation
        
        increased heat production
        
        Anaerobic metabolism
      - Acid-base metabolism
        
        Inhibiton of respiratory center
        
        respiratory alkalosis
        
        salicylate + formed pyruvate & lactate
        
        metabolic acidosis
      - Hemostatic problems
        
        Prolonged bleeding time
        
        reduced prothrombin levels
        
        bleeding -> hypovolemia
      - CV and respiratory problems
        
        Vasodilation
        
        Salt/water loss
        
        pulmonary edema
      - Treatment
        
        Gastric lavage w/ activated charcoal + NaHCO3 i.v to treat acidosis and enhance renal excretion of salicylate, cooling and dialysis
  - - - topically used antiseptic with food antifungal effect
    - - Used systemically
    - - Does not enter the grain -> no antipyretic effect
- - - - unless tehre is kidney or liver damage
  - - - causing non-linear pharmacokinetic with higher toxic metabolite
        
        liver cell necrosis
        
        renal tbular necrosis
        
        chronic overdose may cause analgesic nephropathy
  - - - Glu-6-P dehydrogenase insufficiency