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NSAIDS Non Steroidal Anti-inflammatory Drugs

  1. 1. NSAIDS (NON-STEROIDAL ANTI-INFLAMMATORY DRUGS) NSAIDS are the drugs that reduce inflammation, pain & fever by inhibiting the synthesis of prostaglandins & related compounds. NSAID inhibits cyclooxygenase 1 or 2 or both enzymes. NSAIDS have three major actions:  Analgesic  Antipyretic  Anti-inflammatory Uses: • Postoperative Pain • Menstrual Pain • Myalgia/Neuralgia • Headache/Backache • Pyrexia(Fever) • Osteoarthritis • Rheumatoid Arthritis • Anti-platelet
  2. 2. There are two forms of cyclooxygenase, cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2). COX-1: Produced by normal cells & tissues, maintains homeostasis COX-2: Induced by inflammed cells, mediates inflammation
  3. 3. Functions Of Prostaglandins • Directly Cause Pain • Enhances Pain Inducing Effects Of Bradykinin • Induces Fever Functions Of Thromboxanes • Cause platelets to aggregate • Causes vasoconstriction • Enhances function of inflammatory cells Functions Of Histamines • Causes tissue congestion & swelling • Causes bronchoconstriction • Causes sneezing, watery eyes, itching • Causes pressure & pain Functions Of Leukotrienes • Increases vessel permiability and leakiness • Stimulates platelet aggregation
  4. 4. Pain & Fever during Inflammation Pain: PGE2 sensitize nerve terminal to the action of bradykinin, PG, histamine and other local mediators released from inflamed tissue & cause pain. Fever: Pyrogen, Cytokine (WBC), IL and chemical mediators are activated during inflammation, infection and diseases condition which stimulate PG synthesis in hypothalamus and temperature set up point is raised. Analgesic, Anti-pyretic & Anti-inflammatory action is due to inhibition of inflammatory mediators; prostaglandins, histamines, thromboxanes and leukotrienes.
  5. 5. Inflammation is the body’s response towards injurious stimulus. It is a protective response involving immune cells and chemical mediators. Inflammatory response includes calor (warmth), dolor (pain), rubor (redness), and tumor (swelling). Why inflammation should be controlled? Inflammation can exaggerate & become harmful Extremely inconvenience to patient To reduce the symptoms like fever & pain
  6. 6. Non-Selective COX inhibitors • Aspirin • Ibuprofen • Flurbiprofen • Naproxen • Mephenamic acid • Piroxicam • Ketolorac • Indomethacin • Phenylbutazone
  7. 7. Preferential COX-2 Inhibitors • Nimesulide • Meloxicam • Etodolac • Diclofenac • Aceclofenac Selective COX-2 Inhibitors • Celecoxib • Etoricoxib • Parecoxib Analgesic but poor anti-inflamatory • Paracetamol (Acetaminophen) • Metamizol • Nefopam
  8. 8. ASPIRIN (ACETYLSALICYLIC ACID) MOA: Aspirin is non selective inhibitor of cox enzymes and supress prostaglandin synthesis. Indication: • Mild to moderate pain (headache, backache, joint pain, toothache, dysmenorrhoea) Aspirin 600mg=Codeine 60mg=Morphine 6mg • Antipyretic in fevers • Anti inflammatory in acute rheumatic fever, rheumatoid arthritis, osteoarthritis • Antiplatelet agent in atherosclerotic diseases, post-operative, myocardial infarction, post stroke patients • Aspirin is prescribed in a small dose as a means to lower the risk of heart attack (prevents clotting action of platelets) • Dose: 300-600mg TDS analgesic, antipyretic & anti- inflammatory action 75-150mg OD myocardial infarction/stroke
  9. 9. Adverse effects • Gastric mucosal damage, peptic ulcer • Hypersensitivity • Salicylism—dizziness, tinnitus, vertigo, reversible impairment of hearing and vision, excitement and mental confusion, hyperventilation and electrolyte imbalance. • Liver injury • Acute salicylate poisoning Contraindication • Peptic ulcer • Bleeding disorder • Hypersensitivity to NSAIDs • Under 12 children • Liver disease • Pregnancy and lactation • Chickenpox of influenza infection
  10. 10. PARACETAMOL (ACETAMINOPHEN) MOA: Paracetamol inhibits the synthesis of prostaglandins in the CNS by inhibiting COX 1 & 2 enzymes in the brain. Thus it inhibits prostaglandin synthesis in hypothalamus & temperature set up point is reduced. It also increases pain threshold & reduces pain. It has less effect on COX enzyme in peripheral tissues, which account for their weak anti-inflammatory activity. Indications: Over The Counter (OTC) drug for: • Fever • Headache • Musculoskeletal Pain • Dysmenorrhoea • Osteoarthritis Dose: Adult 325-1000mg 4-6 hourly or SOS (650mg rectally) Child 10-15mg/kg 4-6 hourly; Safe in Pregnancy!
  11. 11. Paracetamol is Safe and Well Tolerated! Adverse Effects Over doses causes: • Liver & kidney damage • Gastric irritation, mucosal erosion & bleeding • Rashes • Nausea, Vomiting and Sweating Contraindication • Hypersensitivity • Peptic ulcer • Abuse of alcohol
  12. 12. NIMESULIDE MOA: Nimesulide is an anti-inflammatory, analgesic, and antipyretic that selectively inhibits COX-2 and weakly inhibits PG synthesis. Indications: Short-lasting painful inflammatory conditions/sports injuries • Sinusitis • Dental surgery • Bursitis • Fever Dose: 100mg BD • Low backache • Dysmenorrhoea • Postoperative pain • Osteoarthritis
  13. 13. Adverse Effects • Gastrointestinal (epigastralgia, heart burn, nausea, loose motions) • Dermatological (rash, pruritus) • Central (somnolence, dizziness) • Hepatic Failure Contraindication • Liver toxicity/ Hepatic failure on long term use • Pregnancy & Breastfeeding • Children under 12 years of age
  14. 14. IBUPROFEN MOA: Ibuprofen inhibits the COX enzymes and supresses the synthesis of prostaglandins which are mediators of pain, inflammation, and fever. It also inhibits the thromboxane A2 which stimulates platelets aggregation & formation of blood clot. Indications: Over The Counter (OTC) Drug • Fever • Dysmenorrhoea • Osteoarthritis • Rheumatoid arthritis • Musculoskeletal disorders • Headache, Backache, Toothache • Postpartum and Postoperative pain Dose: 400-800mg TDS (children 20mg/kg/day)
  15. 15. Adverse Effects: • Gastric discomfort, nausea and vomiting • Gastric erosion and occult blood loss • Dizziness, blurring of vision, tinnitus • Rashes, itching and other hypersensitivity Contraindication: • Peptic ulcer • Pregnancy & Lactation • Children under 7 years • Hypersensitivity
  16. 16. DICLOFENAC SODIUM MOA: Diclofenac inhibits the synthesis of prostaglandins by inhibiting COX enzymes and leucocyte migration. It is somewhat COX-2 selective so it has better anti-inflammatory action. It is also a potent analgesic preferred in mild to moderate pain. Indications: • Quick relief of pain and edema, Toothache • Rheumatoid arthritis, Osteoarthritis • Dysmenorrhoea (menstrual pain) • Bursitis (pain in shoulder, hip and elbow) • Ankylosing spondylitis (inflammation in vertebra) • Postoperative or post-traumatic pain and inflammation • Ocular inflammation and pain Dose: 50mg TDS, 75mg deep i.m
  17. 17. Adverse effects: • Epigastric pain, nausea, headache, dizziness • Rashes • Gastric ulceration and bleeding • Hepatic and Renal damage Contraindications: • Peptic ulcer • Children under 7 years of age • Kidney disease • Liver disease • Inflammatory bowel disease • Patients with bleeding disorder Aceclofenac: Similar in action with Diclofenac with fewer side effects and better tolerability. Dose: 100mg BD
  18. 18. NSAIDS USES DOSE Ketorolac Postoperative pain, inflammation 15-30mg i.m or i.v Indomethacin Acute GOUT, Rheumatoid arthritis, Ankylosing spodylitis 25-50mg TDS Naproxen Rheumatoid arthritis, Ankylosing spodylitis 250-500mg BD Piroxicam Osteoarthritis, Rheumatoid arthritis, Ankylosing spodylitis 10-20mg OD Mefenamic acid Muscle, Joint, Tissue Pain Dysmenorrhoea, Rheumatoid arthritis, Osteoarthritis 250-500mg TDS Celecoxib Selective COX-2 Inhibitors Anti-inflammatory ” 100-200mg OD-BD Etoricoxib 60-120mg OD

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