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02 NSAIDhdjjdhshbjjsuehujairhjahdhs.pptx
- 3. OBJECTIVES At the end of the lecture the students should : Define NSAIDs Describe the classification of this group of drugs Describe the general mechanism of actions Define the following terms : Analgesic Antipyretics
- 4. OBJECTIVES ( CONTINUE) Anti-inflammatory Anti-platelet o Describe the general pharmacological actions Describe the general therapeutic uses Describe the general adverse effects Describe the general contraindications Know some examples of each group of NSAIDs Know the difference between the selective & non-selective NSAIDs
- 5. CLASSIFICATION OF NSAIDS Non-Selective COXs Inhibitor Selective COX2 Inhibitor
- 6. NON- SLECTIVE -NON -STEROIDAL ANTI-INFLAMMATORY DRUGS Are group of drugs that share in common the capacity to induce the following actions : Analgesic Antipyretic Anti-inflammatory Anti-platelet Actions on the kidney
- 8. ANTIPYRETIC Drug that lower the elevated body temperature to normal.
- 9. PHARMACOKINETIC Oral administration Most NSAIDs are weak acid (absorbed well in stomach and intestinal mucosa) 95% bound to plasma-protein (high bioavailability) Most metabolized in liver (oxidation & conjugation)
- 10. DISCUSS
- 11. MECHANISM OF ACTION OF N-NSAIDS
- 14. MECHANISM OF ACTION Analgesic Centrally inhibition of COX enzymes in CNS periperally Anti- Inflammatory action Antipyretic Centrally inhibition of COX enzymes in CNS inhibition of interleukin-1 Anti-Inflam. Peripherally inhibition of COX enzymes Antioxidant effect
- 15. ( CONTINUE) Effect on platelets Inhibit platelet aggregation through inhibition the synthesis of TXA2 ( inhibit cox-1)
- 16. ACTIONS ON THE KIDNEY Salt &water retention & may cause edema ( inhibit synthesis of PGE2 & PGI2 that are responsible for maintaining renal blood flow) Hyperkalemia Interstitial nephritis ( except aspirin)
- 17. RESPIRATORY ACTIONS ( SPECIFIC FOR ASPIRIN) Therapeutic doses aspirin elevates CO2 & increased respiration High doses acts directly on the respiratory center resulting in hyperventilation & respiratory alkalosis Toxic doses , central respiratory paralysis & respiratory acidosis ( continued production of CO2)
- 19. Antipyretic Analgesic (Type of pain?) Headache, Migraine, Dental pain Common cold.
- 20. CONTINUE Rheumatic / Rheumatoid arthritis / myositis or other forms of inflammatory conditions. Dysmenrrhea
- 21. ADVERSE EFFECTS SHARED BY N-NSAIDS GIT upsets ( nausea, vomiting) GIT bleeding & ulceration Bleeding Hypersensitivity reaction Inhibition of uterine contraction Salt & water retention
- 23. CLINICAL USES Acute rheumatic fever Low doses reduce the incidence of myocardial infarction & unstable angina ( cardioprotective)
- 25. ( CONTINUE) Chronic gouty arthritis with large doses Chronic use of small doses of aspirin reduces the incidence of colorectal cancer
- 26. CONTINUE External applications : Salicylic acid is used topically to treat corns Methyl salicylate ( oil of wintergreen ) is used as counter irritant
- 27. Adverse Effects Related to (A) Therapeutic Doses Of Aspirin Nausea & vomiting Hypersensitivity ( Aspirin asthma) Acute Gouty arthritis Reye's syndrome
- 28. ( B) LARGE DOSES OR CHRONIC USE OF ASPIRIN Salicylism ( ringing of ear( tinnitus) , vertigo) Hyperthermia Gastric ulceration & bleeding Respiratory depression & uncompensated respiratory & metabolic acidoses
- 29. ADVERSE EFFECTS RELATED TO HIGH DOSES
- 30. CONTRAINDICATIONS Peptic ulcer Pregnancy Hemophilic patients Patients taking anticoagulants Children with viral infections Gout ( small doses )
- 31. PARACETAMOL IS commonly used as analgesic antipyretic
- 32. THERAPEUTIC APPLICATIONS OF PARACETAMOL AS ANALGESIC & ANTIPYRETIC
- 33. In patients with : Peptic or gastric ulcers. Bleeding tendency. Allergy to aspirin. Viral infections especially in children . During Pregnancy.
- 34. ADVERSE EFFECTS Mainly on liver due to its active metabolite ( N-acetyl-p-benzoquinone) Therapeutic doses elevate liver enzymes Large doses cause liver & kidney necrosis Treatment Of toxicity of paracetamol by : N- acetylcysteine ( SH- donor to neutralize the toxic metabolite
- 35. DICLOFENAC Clinical uses o Long-term use in treatment of rheumatoid arthritis , osteoarthritis & ankylosing spondylitis o Analgesic o Antipyretic o Acute gouty arthritis o Locally to prevent post-opthalmic inflammation
- 36. PREPARATIONS OF DICLOFENAC Diclofenac with misoprostol decreases upper gastrointestinal ulceration ,but result in diarrhea. Diclofenac with omeprazole to prevent recurrent bleeding. .1% opthalmic preparation for postoperative opthalmic inflammation. A topical gel 3% for solar keratoses. Rectal suppository as analgesic
- 37. CONTINUE Oral mouth wash. Intramuscular preparations.
- 38. SELECTIVE COX-2 INHIBITORS General advantages : o Potent anti-inflammatory o Antipyretic & analgesic o Lower incidence of gastric upset o No effect on platelet aggregation ( COX-1)
- 39. GENERAL ADVERSE EFFECTS Renal toxicity Dyspepsia & heartburn Allergy Cardiovascular ( do not offer the cardioprotective effects of non- selective group).
- 40. GENERAL CLINICAL USES Rheumatoid arthritis Osteoarthritis Acute gouty arthritis Acute musculoskeletal pain Ankylosing spondylitis Dysmenorrhea
- 41. CONTINUE They are recommended in postoperative patients undergoing bone repair. Indicated in primary familial adenomatous polyposis,
- 42. CELECOXIB Half-life 11 hours Food decrease its absorption Highly bound to plasma proteins
- 43. CLINICAL USES & ADVERSE EFFECTS Discussed before
- 44. DRUG INTERACTIONS With warfarin potentiate its actions through interfering with its metabolism.
- 45. SUMMARY NSAIDs are group of drugs that have analgesic , antipyretic , anti-platelet & anti-inflammatory effects. They are classified according to their action on COX-enzymes into non-selective that inhibit both COX-1 & COX-2 & selective that inhibit only COX-2 enzymes. They are sharing in common therapeutic uses as analgesic to relief mild to moderate pain not visceral pain , reducing high body temperature, preventing clot formation , so aspirin can be used as prophylaxis in ischemic heart disease.
- 46. SUMMARY ( CONTINUE) As anti-inflammatory in rheumatic , rheumatoid arthritis, desmenrrhea and other inflammatory conditions including muscles or bones. The common adverse effects includes : gastric upset ( nausea, vomiting ,gastric ulceration or bleeding). Allergy Edema They are contraindicated mainly in patients with peptic ulcer , bleeding tendency or in pregnancy .
- 47. SUMMARY ( CONTINUE) Selective COX-2 inhibitors as celecoxib are potent anti-inflammatory & analgesic ,but have no anti-platelet effect & less gastric upset. They can be used in patients with gastric ulcer , haemophilia . Their common adverse is mainly on kidney & cardiovascular system.
- 48. THANK YOU