19)NSAIDs

Question 1

Non-Steroidal Anti-Inflammatory Drugs

Answer 1

Provide symptomatic relief from pain + swelling

Question 2

Mechanism of action

Answer 2

• During trauma ⇢ Arachidonic acid is converted into ⇢ prostaglandin H2
• PH2 converted into ⇢ Prostaglandin E2/F2 ⇢ cause fever, enhanced pain + inflammation
• COX-1 + COX-2 enzymes responsible for production of PH2
• COX-1 ⇢ Physiological
• COX-2 ⇢ Inflammatory
• NSAIDs INHIBIT COX enzyme ⇢ inhibition of prostaglandins + thromboxane’s synthesis

Question 3

Classification

Answer 3

NON-SPECIFIC NSAID’s ⇢ Block COX-1 + COX-2

• Aspirin
• Ibuprofen
• Naproxen

Selective NSAID - Only block COX-2 - coxibs

• Celecoxib (CELERY)
• Parecoxib (Paranoia)
• Etoricoxib (tories)

Question 4

Pharmacokinetics

Answer 4

• Very good oral absorption
• Metabolised by liver
• Excreted via kidneys
• Aspirin ⇢ metabolised by hydrolysis + conjugation w/glucuronic acid

Question 5

Pharmacological effects

Answer 5

Non-specific

• Antipyretic - fever relief
• Analgesic - For mild - moderate pain
• Anti-inflammatory - for mild inflammation

Question 6

Side effects

Answer 6

• Anti-coagulant ⇢ bleeding easily
• Allergic reaction ⇢ skin rash
• Bronchospasm
• Gastric upset ⇢ ulcers, vomiting, haemorrhage
• Renal effect ⇢ renal failure, nephritis
• Rey’s syndrome ⇢ hepatic fatty degeneration + encephalopathy