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Antiallergic drugs

Antiallergic drugs. ALLERGIC REACTIONS. Frequency in Ukraine – 35-45 % from all adverse reactions of drugs Frequency in a world – 10-15 % of population 20 % healthy persons have got sensitization to drugs. ALLERGENS. Drugs. Food products. Dust with mites. Pollen of blooming

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Antiallergic drugs

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  1. Antiallergic drugs

  2. ALLERGIC REACTIONS • Frequency in Ukraine – 35-45 % from all adverse reactions of drugs • Frequency in a world – 10-15 % of population • 20 % healthy persons have gotsensitization to drugs

  3. ALLERGENS Drugs Food products Dust with mites Pollen of blooming plants Animals skin, hear, fur Wasp, bee

  4. Stevens-Johnson syndrome

  5. Exfoliate dermatitis (Laiell’s syndrome)

  6. Quincke's Oedema, Angioneurotic Oedema • oedema of the subcutaneous tissue, particularly of the lips, eyelids and genitalia, though any part of the body may be involved • The tongue and larynx may also be affected, it may be life threatening • Quincke's oedema may occur in urticaria, anaphylaxis, and serum sickness • Etiologic factors include medications (e.g. penicillin, aspirin, phenytoin) • infections and food related products for Quincke's oedema associated with urticaria

  7. Antiallergics –drugs which stabilize membranes of mast cells and basophiles • Cetotifen (Zaditen) – orally • Cromolin-sodium (Intal) – by inhalations • Nedocromil-sodium (Tailed) – by inhalations Leikotrien-inhibitor - Accolat

  8. Ketotifen (Zaditen), Cromolin-sodium (Intal), Nedocromil-sodium (Tilade),Accolat

  9. Antiallergics –drugs which stabilize membranes of mast cells and basophiles slow down releasing of mediators of hypersensitivity reaction Only for prophylaxis of allergic reactions

  10. Antihistamine drugs R1 CH3 CH2-CH2-N R1 CH3 Structure of nucleus of Н1 histamine-receptors antagonists (H1 histamine-blockers)

  11. Н1- ANTIHISTAMINES ACTION

  12. According to chemical structure blockers of Н1histamine-receptors are divided into derivatives of: 1) ethylendiamin (suprastin) 2) ethanolamin (dimedrol, klemastin) 3) piperasin (cetyrisin) 4) alkilamins (feniramin) 5) phenothiasin (diprasin, teralen) 6) oxycam (meloxycam, pyroxycam) 6) different structure (diasolin, peritol, fenkarol)

  13. Antihistamines • 1 generation: dimedrol(difenhydramine), suprastin, diprazin (pipolfen), fencarol, diazolin, peritol, tavegil (clemastin) • 2 generation: terfenadine, astemizol, loratadine (claritin) • 3 generation: cetirizin (zyrtec), fexofenadine (telfast)

  14. Comparative antiallergic activity Н1histamine blockers of 1st generation diprasine>tavegil>dimedrol>suprastin> fenkarol>diasoline Н1 histamine blockers of 2nd and 3rd generations cetirizine> terfenadine=fexofenadine> astemizole>loratadine

  15. Н1-histamine blockers of 1st generation

  16. Н1 histamine blockers of 2nd and 3rd generations

  17. Indications for administration of antihistamine drugs: 1. Nettle-rash 2. Hay fever 3. Vasomotor rhinitis 4. Contact dermatitis 5. Angioneurotic edema 6. Serum sickness 7. Anaphylactic shock 8. Others

  18. Side effects of Н1-histamine receptors blockers of 1st generation 1) Depression of CNS (disorders of coordination, increased tiredness, dizziness, tremor, euphoria, nervousness, insomnia) 2) Disturbance of GI functioning : decreasing of appetite, nausea, vomiting, pain in epigastria, constipation of diarrhea 3) As a result of M-cholinoblocking activity – dryness of mucous membranes, eye disorders - blurred vision, impotence, ischuria, tachycardia, headache, psychosis 4) in case of repeated administration - tachyphylaxis

  19. Properties of Н1- histamine receptors blockers of 2nd and 3rd generations: 1) Blockage Н1-histamine receptors 2) Stabilizing mast cells 3) Decreasing histamine secretion 4) Possessing anti-inflammatory activity

  20. Advantages of Н1-histamine receptors blockers of 2nd and 3rd generations over classical Н1-antagonists 1) High specificity and affinity to Н1-receptors 2) Short onset 3) Long duration of action (over 24 hours) 4) Absence of blockade of other types of receptors 5) No penetrable through HEB in therapeutic doses 6) Absence of tachyphylaxis

  21. Anti-inflammatory drugs (GCS and NSAIDs)

  22. Groups of anti-inflammatory agents and mechanism of action:1) nonsteroidal anti-inflammatory drugs – NSAIDs, 2) glucocorticosteroids (GCS) - Phospholipids Arachidonic acid Cyclic endoperoxydases glucocorticosteroids L Phospholipase А2 - Cyclooxygenases (COG-1, COG-2, COG-3) NSAIDs ProstaglandinsThromboxan InflammationPainFeverVasoconstriction Increasing of platelets aggregation - - depressing effect - stimulating effect +

  23. Classification of nonsteroid anti-inflammatory drugs according to mechanism of action: • Selective inhibitors of COG-1 (acetylsalicylic acid in small doses) • II.Nonselective inhibitors of COG-1 and COG-2 (most of NSAIDs) • III.Drugs with dominant influence on COG-2 • (meloxycam, nimesulid) • IV.High selective inhibitors of COG-2 • (celecoxyb,rofecoxyb)

  24. Properties of nonsteroidal anti-inflammatory drugs • Anti-inflammatory action • indometacyn>diclofenac>meloxycam>nimesulid>pyroxycam>ketoprofen>naproxen>butadion>ibuprofen>acetylsalicylic acid • Analgesic action • Antipyretic action

  25. Indications for administration of nonsteroidal anti-inflammatory drugs 1. Rheumatism 2. Infectious-allergic myocarditis 3. Rheumatoid polyarthritis 4. System lupus erythematosus 5. Anchilizing spondilitis (Bechterev’s disease) 6. Gout 7. Deformating osteoarthrosis(DOA) 8. Thrombophlebitis 9. Inflammation diseases of connective tissue, osseous-muscular system 10. Neuralgia 11. Meningoencephalitis 12. Chronic bronchitis 13. Virus hepatitis

  26. Rheumatoid diseases

  27. Doses in which NSAIDs are used as anti-inflammatory agents Meloxicam 0,0075-0,015 0,0125-0,05 1 1 Rofecoxib

  28. Acetylsalicylic acid

  29. Aspirin С

  30. Aspirin

  31. Butadion

  32. Indometacin (methyndol)

  33. Ibuprofen (brufen)

  34. Piroxicam

  35. Sodium diclofenac

  36. Voltaren

  37. Diclofenac-sodium

  38. Іndometacin

  39. Nimesulid, Meloxicam

  40. Celecoxib, Rofecoxib

  41. Side effects of nonsteroid anti-inflammatory drugs

  42. Prevention of development of GI complications while administering NSAIDs: 1) Administer simultaneously with gastric protectors sucralfat, misoprostol, ranitidin, famotidin, omeprasol 2) Create and introduce NSAIDs which selectively inhibit COG-2 meloxycam, nimesulid, rofecoxib, celecoxib

  43. Directions of medical treatment ofrheumatoid diseases: • NSAIDswith the aim of depression of inflammatory process, pain, rigidness of muscles and joints, but don’t effect the currency of disease • 2) Basis drugs(disease modifying) • Methotrexat, hydroxychloroquin, sulfasalazin, gold containing drugs, penicillamin, • purin derivatives (asathioprin and mercaptopurin) • Alkilying drugs (chlorbutin and cyclophosphamid), • cyclosporin • 3) GCSare administered if there’s a lack of effect of NSAIDs and basis drugs in case of very severe currency of inflammatory process

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