ANTIINFLAMMATORY DRUGS

1
ANTI-INFLAMMATORY DRUGS

• Time course of inflammation
• Acute vs chronic inflammation
• Non-steroidal anti-inflammatory drugs
• Corticosteroid anti-inflammatory drugs

2
TIME COURSE OF INFLAMMATION

• _________/ /__________________________
• 0 1 4 5 6 7 Days
• Mediator release
• Microvascular effects
• Cellular accumulation and activation
• Systemic effects
• Repair and healing

3
ACUTE AND CHRONIC INFLAMMATION

• 1. ACUTE
• Benefits - defence, preparation for repair
• Harmful effects
• - swelling
• - hypersensitivity (eg hay fever)
• Short term
• Mainly neutrophils active

4
ACUTE AND CHRONIC INFLAMMATION

• 2. CHRONIC
• No benefit
• Persistent
• May develop from acute
• ? fibroblasts ? ? scar tissue
• (eg in bowel, kidney)
• Mainly lymphocytes and macrophages

5
ANTI-INFLAMMATORY DRUGS

• Uses ? pain, ? chronic inflamm.
• conditions
• Actions ? enzyme formation or action, which ?
  chemical mediators of inflammation

6
MECHANISM OF ACTION

• cell membrane phospholipids
• corticosteroids
• arachidonic acid
• NSAIDs
• leukotrienes prostaglandins(PG)

7
NSAIDs

• Aspirin, ibuprofen ? PG
• Effects ? inflammation, ? pain
• ? fever
• Side-effects ? gastric bleeding
• (?gastric acid, and ? mucus)
• ? platelet aggregation
• !! Paracetamol - only blocks PG in CNS (not
  anti-inflammatory)

8
CORTICOSTEROIDS

• Adrenal cortex hormones (glucocorticoids - eg
  hydrocortisone, prednisolone)
• Action normal -ve feedback control of inflamm.
  mediators
• ? arachidonic acid formation
• ? all aspects of inflammation due to PGs and
  leukotrienes

9
CORTICOSTEROIDS

• More effective than NSAIDs
• Also ? autoimmune reactions
• Side effects
• ? response to infection
• ? glucocorticoid synthesis (-ve feedback on
  pituitary and hypothalamus
• hyperglycemia, osteoporosis