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13 Cards in this Set

  • Front
  • Back

Eicosanoids

Prostaglandins


Thromboxanes


Leukotrines

Phospholipase A2

Converts phospholipids in plasma membrane into arachidonic acid

PGE2

Increases thermostatic set point in hypothalamus - induces fever

2 actions of cyclooxygenase

1. Endoperoxidase synthase action


2. Peroxidase action



Converts arachidonic acid to prostaglandin H2

COX 1

Maintains tissue homeostasis


Housekeeping enzyme


Narrow binding pocket

COX 2

Induced by inflammation, mediates inflammation


Wide binding pocket

NSAIDs general action

Inhibits COX, mostly endoperoxidase synthase activity


Inhibits AA --> PGG2

Salicylates (aspirin)

Inhibits COX 1 preferentially


Protein bound serum albumin


Effects are dose dependent



Side effect: GI bleeding



Contraindications: displaces warfarin

Paracetamol

Possible COX 1/2 inhibition


Mild analgesic


Weak antipyretic


Weak anti-inflammatory



Side effects: saturates liver enzymes, CYP450 used instead creating toxic NAPQI



Contraindications: anti-epileptics

Ibuprofen

Inhibits COX 1+2


Anti-inflammatory


Antipyretic


Analgesic


Vasodilation



Side effects: mild



Contraindications: asthma (bronchoconstriction)

Meloxicam

Selective COX 2 inhibitor


Neuroblastoma treatment


Neuropsychiatric disorders

Celecoxib

Selective COX 2 inhibitor


Neuroblastoma treatment


Neuropsychiatric disorders

Cortisol

Anti-inflammatory actions


Stimulates production of Annexin 1 (lipocortin) which blocks PLA2