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Prostaglandins & leukotrienes

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Prostaglandins & leukotrienes

  1. 1. Prostaglandins & Leukotrienes<br />Dr.Sangeetha Purushothaman<br />
  2. 2. Prostaglandins & Leukotrienes<br />Local hormones - very active,many functions..<br />Autacoids from 20 C PUFA<br /> Prostaglandins<br />Prostacyclin<br />Thromboxanes<br />Leukotrienes<br />
  3. 3. Functions <br />Inflammation<br />Smooth muscle tone<br />Blood coagulation<br />Reproduction <br />GI secretion<br />
  4. 4. .<br />. <br />SYNTHESIS<br />PHOSPHOLIPIDS<br />PHOSPHOLIPASE A2<br />ARACHIDONIC ACID<br />5 LIPOOXYGENASE<br />CYCLOOXYGENASE<br />LT A4<br />PG G2<br />PGH2<br />LT C4 <br />LT D4<br />LT B4<br />THROMBOXANE SYNTHASE<br />ISOMERASE<br />PROSTACYCLINE SYNTHASE<br />PGE2 PG D2 PG F2<br />THROMBOXANE A2<br />PG I2<br />
  5. 5. .<br />PHOSPHOLIPIDS<br />STEROIDS<br />PHOSPHOLIPASE A2<br />ARACHIDONIC ACID<br />ZILEUTON<br />NSAIDS<br />5 LIPOOXYGENASE<br />CYCLOOXYGENASE<br />LT A4<br />PG G2<br />PGH2<br />LT C4 <br />LT D4<br />LT B4<br />THROMBOXANE A2<br />PGE2 ,PG D2 ,PG F2<br />PG I2<br />
  6. 6. BIOSYNTHESIS OF PROSTAGLANDINS AND LEUKOTRIENES<br />Membrane phospholipid<br />Phospholipase A<br />Arachidonic acid<br />Cyclooxygenase<br />Lipoxygenase<br />PG G2<br />5HPETE<br />LTA4<br />PGH2<br />Prostacyclinsynthase<br />LTC4<br />LTB4<br />Thromboxanesynthase<br />Isomerases<br />PGI2<br />LTD4<br />PGE2<br />TXA2<br />6 keto PGF2α<br />PGD2<br />PGF2<br />TXB2<br />
  7. 7. BIOSYNTHESIS OF PROSTAGLANDINS<br /><ul><li>Enzyme is Cyclooxygenase(COX)</li></ul> COX 1-constitutive.<br /> COX 2-inducible<br /><ul><li>NSAIDS- Nonselective COX inhibitors.</li></ul>COXIBS - Selective COX inhibitors<br /><ul><li>Aspirin- Irreversible inhibition of COX</li></ul> Other NSAIDS- Reversible inhibition <br />
  8. 8. Actions <br /> Inflammation <br /> Most important mediators.. <br />Synthesised as per need.<br /> NSAIDS <br />
  9. 9. Actions –Smooth muscles<br />Blood vessels<br />Pg E2, Prostacycline - vasodilatation <br />Thromboxane A2 – constriction<br />
  10. 10. Actions :Smooth muscle <br />Bronchus<br />
  11. 11. Uterus <br />Both uterus &cervix<br />
  12. 12. Actions <br />GIT<br />Natural ulcer protectants..<br />NSAIDS..<br />
  13. 13. GIT<br />
  14. 14. RENAL<br />PgE2,Prostacyclin -protective..<br />
  15. 15. Coagulation <br />
  16. 16. ENDOTHELIUM<br />PG I₂<br />PLATELET<br />
  17. 17. .<br />Penile erection<br />Pulmonary vessels-vasodilatation<br />CNS-Neurotransmitter<br />EYE-↓IOT<br />
  18. 18. Preparations & Uses <br />
  19. 19. Preparations <br />
  20. 20. Uses <br />1.Obstetrics <br /> Therapeutic abortion <br />Cervical ripening<br />Severe Post partum hge<br />PgE1/MISOPROSTOL<br />PgE₁/PgE2<br />15METHYL PgF2im/PgE1 Rectal<br />
  21. 21. 2.Peptic ulcer<br /> PgE1/Misoprostol<br />PgE2/Enprostil,Rioprostil,Arbaprostil<br />3.Glaucoma : PgE1 / Latanoprost<br />4.Erectile dysfunction <br />5. PDA<br />6. Primary pulmonary hypertention: PgI₂<br />PgE1/Alprostadil<br />
  22. 22. Summary of uses<br />
  23. 23. ADR<br />Vomiting,Diarrhoea,Abdominal cramps<br />Uterine cramps<br />Bronchospasm<br />
  24. 24. LEUKOTRIENES<br />
  25. 25. PHOSPHOLIPIDS<br />ARACHIDONIC ACID<br />CYCLOOXYGENASE<br />LIPOOXYGENASE<br />Zileuton<br />LEUKOTRIENES<br />LEUKOTRIENE RECEPTOR<br />MonteleukastZafirleukast<br />PROSTAGLANDINS<br />MAST CELL<br />Chromoglycate<br />Nedochromil<br />

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