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NSAIDs

NSAIDs. What will be covered. Indications Mechanism of action Side Effects Contraindications Metabolism Pharmacokinetics. Indications. Analgesia Anti-inflammatory Anti-pyretic. Mechanism of Action. Leukotrienes. Lipo-oxygenase. Thromboxane. Phospholipids. Arachidonic acid.

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NSAIDs

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  1. NSAIDs

  2. What will be covered • Indications • Mechanism of action • Side Effects • Contraindications • Metabolism • Pharmacokinetics

  3. Indications Analgesia Anti-inflammatory Anti-pyretic

  4. Mechanism of Action Leukotrienes Lipo-oxygenase Thromboxane Phospholipids Arachidonic acid Tx Synthase Phospholipase A2 COX Prostaglandin A2 PG Synthase Prostaglandins

  5. Analgesia • Prostaglandins sensitize noiceptor endings to inflammatory mediators. • NSAIDs will prevent the noiceptor endings becoming sensitive to inflammatory mediators through the blockade of prostaglandin synthesis.

  6. Anti Inflammatory • When inflammatory cells are activated COX-2 is induced. • COX-2 initiates the eicosanoid mediators of inflammation. • Through the blockade of eicosanoid production NSAIDs reduce; vasodilation and therefore oedema and pain.

  7. Mechanism of Action Eicosanoids Leukotrienes Lipo-oxygenase Thromboxane Phospholipids Arachidonic acid Tx Synthase Phospholipase A2 COX Prostaglandin A2 PG Synthase Prostaglandins

  8. Anti Pyretic • IL-1, IL-6 and TNF function as endogenous pyrogen. • These cause the hypothalamus to raise the body temperature by releasing prostaglandins. • Through the blockade of prostaglandin production in the hypothalamus, the body temperature remains stable.

  9. Side Effects • Gastric Side Effects • PG E-2 decreases gastric acid secretion. • PG E-2 increases gastric mucus secretion. • If prostaglandins are inhibited, gastric acid secretion increases and gastric mucus secretion decreases. • This may lead to gastric ulcer formation.

  10. Side Effects • Renal Side Effects • NSAIDs do not have an effect on those with normal kidney function. • Those with poor kidney function can be affected by acute renal insufficiency, which is reversible on stopping the drug. • Neonates and the elderly are particularly effected. • The prostaglandins PG I-2 and PG E-2 have a role in vasodilation in response to angiotensin II and noradrenaline.

  11. Contra Indication and Cautions • Heart failure or pre-existing cardiac morbidity; NSAIDs should be used with caution due to their potential effects on kidney. • Hepatic impairment; increased risk of gastric irritation. • Pregnancy; manufacturers suggest that they shouldn’t be used. • Use in the third trimester can lead to premature closure of the ductusarteriosus leading to pulmonary hypertension.

  12. Metabolism and Pharmacokinetics • Metabolised in the liver by oxidation to non reactive species. • Excreted in urine • Ibuprofen and Diclofenac have a short half life of only 2-3 hours

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