- Cyclooxygenase(COX) inhibition is recognized as the most important mechanism of action.
- COX is an enzyme that is responsible for the formation of prostaglandins and thromboxane.
- Prostaglandins are the main mediators of inflammation alongwith leukotrienes
- Thromboxane is a potent vasoconstrictor,released from platelets,increases platelet aggregation.
- Leukotriene is another mediator of inflammation which is released from leukocytes,they are produced by enzyme lipooxygenase(LOX)
- NSAIDS can only inhibit COX enzyme,they cant inhibit LOX enzyme.whereas glucocorticoids can inhibit all inflammatory mediators.
- There are two types of COX enxymes,COX1 & COX 2.
- COX1 is seen in almost all tissues whereas COX 2 is found in inflammed tissues
- NSAIDS action-
- Analgesic
- Anti Inflammatory
- Anti Pyretic
- Anti Thrombotic
- NSAIDS Side effects due to PG synthesis inhibition-
- Causes gastric erosion- * inhibit synthesis of gastroprotective PGs
2. Bleeding tendencies- Due to inhibition of thromboxane synthesis
3. Exacerbation of asthmatic reactions-Asthmatic patients are more prone to leukotrienes,which are bronchoconstrictors.As NSAIDS inhibit PG synthesis all arachidonic acid is used to form leukotrienes.
4. Causes sodium & water retention.
5. Prolongation of labour
- Contraindicated in-
- Asthmatic patients
- Pregnant ladies in 3rd trimester
- Liver insufficiency
- Gastric ulcers
- 1 week before surgeries
- Cautiously used in diabetics
- Piroxicam- Non selective COX inhibitor.Potent anti inflammatory and potent analgesic.Prolongs bleeding time.Causes gastric discomfort
Brand name-Dolonex 10,20 mg caps.
- Ketorolac- Non selective COX inhibitor.Potent analgesic and modest anti inflammatory.Not to be used for more than 5days
Brand name-Ketorol 10 mg tab.
- Other non selective COX inhibitors-ibuprofen;indomethacin
- Nimesulide-Preferential COX 2 inhibitor. Doesn't exacerbate asthmatic attacks, preferred NSAID in asthmatic patients.Hepatic toxic.Gastrointestinal disturbances.Not to be given to children and pregnant ladies.
Brand name-Nimegesic100mg tab.
- Paracetamol-Potent analgesic.Mild anti inflammatory.Gastric erosion is rare. Doesn't prolong bleeding time.contraindicated in liver insufficiency.
Brand name-Crocin 0.5,1 mg tab.
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