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Prostaglanden feb (2014)

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Prostaglanden feb (2014)

  1. 1. Prostaglandins & Leukotrienes DR MUSTANSAR
  2. 2. Eicosanoids The eicosanoids are a group of signaling sub-stances that arise from the C-20 fatty acid arachidonic acid and therefore usually contain 20 C atom (Greek eicosa=20). As mediators, they influence a large number of physiological
  3. 3. Introduction  Eicosanoids (20 carbons) are found in the animal kingdom and a variety of plants.  The eicosanoids are oxygenation products of acid arachidonic (AA) polyunsaturated fatty acid.  Acid arachidonic is released from membrane by phospholipase A2 (PLA2).
  4. 4. Prostaglandins & Leukotrienes  Local hormones - very active,many functions..  Autacoids from 20 C PUFA Prostaglandins Prostacyclin Thromboxanes Leukotrienes
  5. 5. Functions  Inflammation  Smooth muscle tone  Blood coagulation  Reproduction  GI secretion
  6. 6. . . SYNTHESI S PHOSPHOLIPI DS PHOSPHOLIPASE A2 ARACHIDON IC ACID CYCLOOXYGENASE 5 LIPOOXYGENASE LT A4 PG G2 PGH ISOMERASE PGE2 PG D2 PG F2 2 THROMBOXANE SYNTHASE PROSTACYCLINE SYNTHASE PG I2 THROMBOXA NE A2 LT B4 LT C4 LT D4
  7. 7. Pathways of arachidonic acid (AA) release and metabolism.
  8. 8. . PHOSPHOLI PIDS STEROIDS PHOSPHOLIPASE A2 NSAIDS ARACHIDON IC ACID CYCLOOXYGENASE ZILEUTON 5 LIPOOXYGENASE LT A4 PG G2 PGH2 PGE2 ,PG D2 ,PG F2 LT B4 THROMBO XANE A2 PG I2 LT C4 LT D4
  9. 9. BIOSYNTHESIS OF PROSTAGLANDINS  Enzyme is Cyclo oxygenase(COX) COX 1-constitutive. COX 2-inducible  NSAIDS- Nonselective COX inhibitors. COXIBS - Selective COX inhibitors  Aspirin- Irreversible inhibition of COX Other NSAIDS- Reversible inhibition
  10. 10. Actions Inflammation Most important mediators.. Synthesised as per need. NSAIDS
  11. 11. Actions –Smooth muscles Blood vessels Pg E2, Prostacycline - vasodilatation Thromboxane A2 – constriction
  12. 12. Prostaglandins
  13. 13. Actions :Smooth muscle Bronchus PgE2 • BRONCHO DILATION PgI2 PgF2α • CONSTRICTI ON TXA2 LT
  14. 14. Uterus Both uterus &cervix Cervical ripening Initiation of Labour • PgE2 • PgE1 • PgF2
  15. 15. Actions  GIT MUCUS HCO3ACID Natural ulcer protectants.. NSAIDS..
  16. 16.  GIT Motility Secretio n Cramps Diarrhoe a
  17. 17. RENAL PgE2,Prostacyclin -protective.. PgE2,PgI 2 RENAL VASODILATATI ON DIRECT ON TUBULES RBF DIURESIS NATRIURESIS
  18. 18. Coagulation TXA 2 PgI2 PLATELE TS AGGREGATIO N ENDOTHELI UM (-) AGGREGATION
  19. 19. . Pulmonary vesselsvasodilatation EYE-↓IOT CNSNeurotransmitte r
  20. 20. Clinical Application  Female Reproductive Organ  Male Reproductive System  Inflammation & Immunity  Gastrointestinal Tract  Respiratory System  Musculo skeletal  Cardiovascular  Glaucoma  Kidney  Cancer
  21. 21. Preparations & Uses
  22. 22. Preparations Prostaglnd Preparation in PgE₁ Misoprostol , Alprostadil,Latanoprost PgE₂ Rioprostil , Enprostil Dinoprostone PgF₂α Prostin 15Methyl Carboprost / Prostodin PgF₂α
  23. 23. Uses 1.Obstetrics Therapeutic abortion Cervical ripening PgE1/MISOPROST OL PgE₁/PgE2 Severe Post partum hge 15METHYL PgF2 im/PgE1 Rectal
  24. 24. 2.Peptic ulcer PgE1/Misoprostol PgE2/Enprostil,Rioprostil,Arbaprostil 3.Glaucoma : PgE1 / Latanoprost 4-PDA PgE1/Alprostadil ₂ 5-Primary pulmonary hypertention : PgI
  25. 25. Summary of uses Use Abortion Cervical ripening Peptic ulcer Glaucoma PPH PDA Preparation PgE1 PgE1 / E2 PgE1 PgE1-Latanoprost PgI2 PgE1
  26. 26. ADR  Vomiting,Diarrhoea,Abdominal cramps  Uterine cramps  Bronchospasm
  27. 27. LEUKOTRIENES
  28. 28. PHOSPHOLIPIDS ARACHIDONIC ACID LIPOOXYGENA SE CYCLOOXYGEN ASE Zileuton PROSTAGLANDINS LEUKOTRIE NES LEUKOTRIENE Monteleuka RECEPTOR stZafirleuka st Chromoglyca MAS te T Nedochromil CELL

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