Содержание
- 2. Plan of lecture: Anti-inflammatory agents Anti-allergic drugs Immunomodulators
- 3. Inflammation Inflammation is a complex protective response of the organism to injury caused by damaging agents.
- 4. Mediators of inflammation Prostaglandins Bradykinin Serotonin Histamine Interleukins-2 – 6, 10, 12,13 Platelet activating factor Gamma-Interferon
- 5. The role of some prostaglandins in the body PGE 2 – vasodilation, bronchodilation, inhibition of gastric
- 6. Cyclo-oxygenase (COX) Exists in the tissue as constitutive isoform (COX-1). At site of inflammation, cytokines stim
- 7. NSAIDs – nonsteroidal anti-inflammatory drugs
- 8. 1. Nonsteroidal anti-inflammatory drugs (NSAIDs) Nonselective COX inhibitors 1. Salicylates *Acetylsalicylic acid (Aspirin) * Salicylamide 2.
- 9. Selective COX inhibitors Preferential COX-2 inhibitors Nimesulide Meloxicam Nabumeton Selective COX-2 inhibitors Celecoxib Parecoxib Rofecoxib NB!!!These
- 10. Mechanism of action of NSAIDs (Non-Steroidal Anti-Inflammatory Drugs) • Act by inhibiting CycloOXygenases (COX) => no
- 11. Mechanism of anti-inflammatory drugs’ action
- 12. Pharmacological effects of NSAIDs Anti-inflammatory Analgesic Antipyretic Antiplatelet (Aspirin) Closure of ductus arteriosus in newborn
- 13. Clinical uses of NSAIDs 1. Pain: headache, toothache, myalgia, backpain; 2. Fever; 3. Arthritises: rheumatiod arthritis,
- 15. Side effects of NSAIDs 1. GIT disturbances: epigastric pain, nausea, gastric peptic ulcer (especially aspirin), gastrointestinal
- 16. Contraindications A) Pregnancy B) Haemophilic patients C) Hypersensitivity reactions D) Viral infections mainly in children E)
- 17. Drugs interaction Potentiates the gastric irritant effect of alcohol Potentiates the hypoglycaemic effects of oral hypoglycaemic
- 18. The Salicylates - ASPIRIN Duration of action ~ 4 hr. Orally taken. Weak acid (pKa ~
- 19. ASPIRIN - Therapeutic Uses Antipyretic, analgesic. Anti-inflammatory: rheumatic fever, rheumatoid arthritis (joint dis), other rheumatological diseases.
- 20. Propionic acid derivatives IBUPROFEN: Pharmacokinetics Rapidly absorbed after oral ingestion. Half-life 1-2 hours Highly bound to
- 21. IBUPROFEN The same mechanism & pharmacological actions of aspirin Except that it is reversible inhibitor for
- 22. Clinical uses A) Analgesic B) Antipyretic C) Anti-inflammatory D)Acute gouty arthritis E) Patent ductus arteriosus
- 23. Preparations of Ibuprofen Oral preparations. Topical cream for osteoarthritis. A liquid gel for rapid relief of
- 24. Adverse effects 1.Gastric upset (less frequent than aspirin). 2.Fluid retention 3.Hypersensetivity reactions 4.Ocular disturbances 5.Rare hematologic
- 25. Contraindications 1. Peptic ulcer 2. Allergic patients to aspirin 3. Kidney impairment 4.Liver diseases 5.Pregnancy 6.Haemophilic
- 26. Piroxicam Mechanism of actions: A) Non-selective inhibitors to COX1 & COX2 B) Traps free radicals C)
- 27. Pharmacokinetics Well absorbed orally Half- Life 45 hours Given once daily
- 28. Adverse effects Less frequent gastric upset (20%). Dizziness. Tinnitus. Headache. Allergy.
- 29. Acetic acid derivatives DICLOFENAC Mechanism of action Non-selective inhibitor to COX1 & COX2. More potent as
- 30. Clinical uses DICLOFENAC A) Any inflammatory conditions B) Musculoskeletal pain C) Dysmenorrhoea D)Acute gouty arthritis E)
- 31. Adverse effects DICLOFENAC Gastric upset Renal impairment Elevation of serum aminotransferase Salt & water retention
- 32. Preparations of DICLOFENAC Diclofenac with misoprostol decreases upper gastrointestinal ulceration, but result in diarrhea. Diclofenac with
- 33. Selective COX 2 inhibitors Advantages: 1. Highly selective inhibitors to COX2 enzyme. 2. Potent anti-inflammatory. 3.
- 34. Selective Cox 2 inhibitors 5. Lower incidence of gastric upset. 6. No effect on platelet aggregation
- 35. Selective Cox 2 inhibitors 9- They are recommended in postoperative patients undergoing bone repair. 10- Also,
- 36. SAIDs – steroidal anti-inflammatory drugs
- 37. Steroidal anti-inflammatory drugs 1. Short-acting glucocorticoids (natural) Hydrocortisone Cortisone 2. Intermediate-acting glucocorticoids Prednisone Prednisolone Methylprednisolone Triamcinolone
- 40. Phospholipids Arachidonic acids Lipoxygenase Cycylooxygenase Leukotriene Prostaglandins, Thromboxane, Prostacyclins. Phospholipase A2 Corticosteroids MECHANISM OF ACTION OF
- 41. Clinical uses of SAIDs Adrenal insufficiency Arthrities Collagen diseases (systemic lupus erhymatosis, scleroderma) Bronchial asthma Severe
- 42. Main side effects of SAIDs Susceptibility to infections Delayed healing of wounds Osteoporosis Growth retardation in
- 43. ANTI-ALLERGIC DRUGS
- 44. Allergy An allergy is a hypersensitivity disorder of the immune system. Allergic reactions occur when a
- 45. mild/cutaneous mild to moderate severe/ anaphylactic erythema, urticaria, and/or itching skin reactions, tachycardia, dysrhythmias, moderate hypotension,
- 46. Histamine exerts its effects on many tissues and organs: It is not a drug but is
- 47. Pathophysiological Actions of Histamine Cellular mediator of immediate hypersensitivity reaction and acute inflammatory response Anaphylaxis Seasonal
- 48. Pharmacological Effects of Histamine Ranges from mild allergic symptoms to anaphylactic shock Involves both the H1
- 49. (Oedema of Quincke, Stevence-Johnson syndrome)
- 53. Antiallergic drugs 1. Antihistaminics 2. Corticosteroids 3. Mast cell stabilisers 4.Antileukotriene drugs
- 54. histaglobulin
- 58. Histamine-related Drugs Mast Cell Stabilizers (Cromolyn Na, Nedocromil –Tilade -, Albuterol) H1 Receptor Antagonists (1st and
- 59. First Generation ANTIHISTAMINE Agents Ethanolamines: DIPHENHYDRAMINE (Benadryl) CLEMASTINE (Tavist) Ethylenediamine:TRIPELENNAMINE Alkylamine:CHLORPHENIRAMINE (Chlortrimeton) Phenothiazine:PROMETHAZINE (Phenergan) Piperazines: HYDROXYZINE
- 60. Uses: Adjunctive in anaphylaxis and other cases where histamine release can occur (H2 antagonist, and epinephrine
- 61. First Generation Agents Adverse Effects: Sedation (Paradoxical Excitation in children) Dizziness Fatigue Tachydysrhythmias in overdose -
- 62. Drug interactions: Additive with classical antimuscarinics Potentiate CNS depressants opioids sedatives general and narcotic analgesics alcohol
- 63. Uses Antiallergy Examples CETIRIZINE (ZYRTEC) FEXOFENADINE (ALLEGRA) LORATADINE (CLARITIN) DESLORATADINE (CLARINEX- FDA APPROVED IN 2002) LORATADINE
- 65. Histamine H1- Antagonists First Generation: !!!Sedating!!! Second Generation: !!!Non sedating!!!
- 66. Advantages of 2nd generation antihistaminics Higher H1 selectivity, absence of anticholinergic side effects Absence of inhibitory
- 67. Mast cell stabilisers Cromolyn sodium (Sodium cromoglycate) Nedocromil sodium Ketotifen Corticosteroids (vide supra)
- 69. Antileukotriene drugs Montelukast Zafirlukast Mechanism: competitive block of LT1 receptors Clinical use: bronchial asthma
- 71. Immunomodulators
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