CLASSIFICATION
1. NON SELECTIVE COX INHIBITORS:
a. Salycilates: Aspirin
b. Ibuprofen
c. Indomethacin
d. Diclofenac
f. Piroxicam
g. Mefenamic acid
2. SELECTIVE COX-2 INHIBITORS:
Celecoxib, Meloxicam
2. ANALGESIC, ANTIPYRETIC WITH POOR ANTI-
INFLAMMATORY ACTION: Paracetamol
Non-Steroidal Anti-inflammatory Drugs
(NSAIDs)
NSAIDs
• Mechanism of Action
• Inhibits cyclo-oxygenase enzyme = ↓↓ Prostaglandin synthesis
COX-I Most cells in the body
COX-II Inflammatory and immune cells
COX-III Hypothalamic temperature control center
NSAIDs that act on COX-I, COX-II & COX-III, more side
effects
Selective COX-II NSAIDs, less side effects
NSAIDs
Common Pharmacological Effects
• Analgesic (CNS and peripheral effect)
• Antipyretic (CNS effect)
• Anti-inflammatory (except Paracetamol)
• Antiplatelet effect:
– prevents platelet aggregation. ( Aspirin low dose)
Common Adverse Effects
• Gastritis and peptic ulceration with bleeding (inhibition of PG
+ other effects)
• Platelet Dysfunction
• Acute Renal Failure in susceptible persons
• Sodium+ water retention and edema
• Analgesic nephropathy
NSAIDs
ASPIRIN: Actions & Uses
Antiplatelet:
Prophylaxis of angina & myocardial infarction (MI)
Analgesic : Mild to moderate pain
Acute dental pain as in pulpitis, dentoalveolar abscess or post
dental surgical procedures.
Headache, musculoskeletal pain & arthritic pains
Anti-inflammatory: Rheumatic fever, rheumatoid arthritis,
Antipyretic : Fever
NSAIDs
Adv effects of Aspirin
Gastritis, Peptic ulcer & GI bleeding.
Reyes’ syndrome in children with viral fever
Salicylism:
 doses => Tinnitus, vertigo, vomiting &hearing
Contraindications:
• Bleeding disorders (Hemophilia),
• Peptic ulcer,
• Children with Viral fever,
• Hypersensitivity/bronchial asthma,
NSAIDs
INDOMETHACIN – Potent NSAID.
Non selective COX-inhibitor,
Inhibition of Phospholipase A & C,
↓ PMN migration.
Uses;
Acute gouty arthritis, ankylosing spondylitis, osteoarthritis,
Medical closure of Patent Ductus Arteriosus
Uterine relaxant ( tocolytic agent ).
NSAIDs
PARACETAMOL
• Antipyretic, Analgesic & Weak Anti-inflammatory
Uses: Fever, Headache, myalgias, etc.
Safe in patients with peptic ulcer, hemophilia, children with
viral fever, bronchial asthma
Adv effects:
Least GI and platelet effects
•  dosage = Hepatic damage due to accumulation of a toxic
metabolite, N-acetyl-benzoquinone
Antidotes: Acetylcysteine & Methionine
NSAIDs
SelectiveCOX-2 Inhibitors (COXIBs)
• Meloxicam, Celecoxib
• More selective inhibition of Cyclooxygenase-II enzyme
• Long duration of action
– given once or twice daily -- better patient compliance
• Least GI effects
Adverse effects:
• Thrombosis (Risk of myocardial infarction & stroke )
• Nephrotoxicity

4. NSAID

  • 1.
    CLASSIFICATION 1. NON SELECTIVECOX INHIBITORS: a. Salycilates: Aspirin b. Ibuprofen c. Indomethacin d. Diclofenac f. Piroxicam g. Mefenamic acid 2. SELECTIVE COX-2 INHIBITORS: Celecoxib, Meloxicam 2. ANALGESIC, ANTIPYRETIC WITH POOR ANTI- INFLAMMATORY ACTION: Paracetamol Non-Steroidal Anti-inflammatory Drugs (NSAIDs)
  • 2.
    NSAIDs • Mechanism ofAction • Inhibits cyclo-oxygenase enzyme = ↓↓ Prostaglandin synthesis COX-I Most cells in the body COX-II Inflammatory and immune cells COX-III Hypothalamic temperature control center NSAIDs that act on COX-I, COX-II & COX-III, more side effects Selective COX-II NSAIDs, less side effects
  • 3.
    NSAIDs Common Pharmacological Effects •Analgesic (CNS and peripheral effect) • Antipyretic (CNS effect) • Anti-inflammatory (except Paracetamol) • Antiplatelet effect: – prevents platelet aggregation. ( Aspirin low dose) Common Adverse Effects • Gastritis and peptic ulceration with bleeding (inhibition of PG + other effects) • Platelet Dysfunction • Acute Renal Failure in susceptible persons • Sodium+ water retention and edema • Analgesic nephropathy
  • 4.
    NSAIDs ASPIRIN: Actions &Uses Antiplatelet: Prophylaxis of angina & myocardial infarction (MI) Analgesic : Mild to moderate pain Acute dental pain as in pulpitis, dentoalveolar abscess or post dental surgical procedures. Headache, musculoskeletal pain & arthritic pains Anti-inflammatory: Rheumatic fever, rheumatoid arthritis, Antipyretic : Fever
  • 5.
    NSAIDs Adv effects ofAspirin Gastritis, Peptic ulcer & GI bleeding. Reyes’ syndrome in children with viral fever Salicylism:  doses => Tinnitus, vertigo, vomiting &hearing Contraindications: • Bleeding disorders (Hemophilia), • Peptic ulcer, • Children with Viral fever, • Hypersensitivity/bronchial asthma,
  • 6.
    NSAIDs INDOMETHACIN – PotentNSAID. Non selective COX-inhibitor, Inhibition of Phospholipase A & C, ↓ PMN migration. Uses; Acute gouty arthritis, ankylosing spondylitis, osteoarthritis, Medical closure of Patent Ductus Arteriosus Uterine relaxant ( tocolytic agent ).
  • 7.
    NSAIDs PARACETAMOL • Antipyretic, Analgesic& Weak Anti-inflammatory Uses: Fever, Headache, myalgias, etc. Safe in patients with peptic ulcer, hemophilia, children with viral fever, bronchial asthma Adv effects: Least GI and platelet effects •  dosage = Hepatic damage due to accumulation of a toxic metabolite, N-acetyl-benzoquinone Antidotes: Acetylcysteine & Methionine
  • 8.
    NSAIDs SelectiveCOX-2 Inhibitors (COXIBs) •Meloxicam, Celecoxib • More selective inhibition of Cyclooxygenase-II enzyme • Long duration of action – given once or twice daily -- better patient compliance • Least GI effects Adverse effects: • Thrombosis (Risk of myocardial infarction & stroke ) • Nephrotoxicity