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Prostaglandins

Prostaglandins. Glutathione S -transferase. LTB 4. LTC 4. LTD 4. LTE 4. Biosynthesis. Membrane phospholipids. Phospholipase A 2. LTA 4. Arachidonic acid. Cyclooxygenase. PGG 2. PG hydroperoxidase. PGH 2. PGD 2. PGD 2 synthase. PGI 2 synthase. PGE 2. TXA 2 synthase. PGF 2a.

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Prostaglandins

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  1. Prostaglandins

  2. Glutathione S-transferase LTB4 LTC4 LTD4 LTE4 Biosynthesis Membrane phospholipids Phospholipase A2 LTA4 Arachidonic acid Cyclooxygenase PGG2 PG hydroperoxidase PGH2 PGD2 PGD2 synthase PGI2 synthase PGE2 TXA2 synthase PGF2a PGI2 (PC) TXA2

  3. Pharmacological actions CVS • PGE2 & PGI2 causes vasodilation • PGI2 is more potent hypotensive than PGE2 • PGE2 & PGI2 continually produced in ductus arteriosus during foetal life and keep it patent • PGF2α & TXA2 are the vasoconstrictors and has a little effect on BP, heart rate & cardiac contractility

  4. Platelets • PGE1 & PGI2 effectively inhibit platelet aggregation • TXA2 is potent platelet aggregators • COX-1 enzyme normally controls the physiological conditions but during any injury COX-2 activity will be very high INFLAMMATION

  5. Uterus • PGE2 and PGF2αuniformly contract pregnant as well as non pregnant uterus • Potency rate is high with PGF2α DYSMENORRHOEA- UTERINE CONTRACTIONS

  6. Bronchial smooth muscles • PGE1, PGE2, PGI2 & PGD2 causes relaxation of bronchial smooth muscles • PGF2α, TXA2 & LTs causes broncho constriction IMBALANCE CAUSES ASTHMA

  7. GIT • PGE2 & PGl2 reduces the acid secretion & increases the mucus production & increases the mucosal blood flow ANTIULCEROGENIC

  8. Eye • PGF2α & PGE2 lower the intraocular pressure by increasing the uveo-scleral outflow Used in GLAUCOMA

  9. Bone metabolism: plays some role in osteoporosis that mainly occur during the menopause INCREASES BONE RESORPTION • PGE2 facilitates the release of growth hormone, TSH, ACTH, LH, FSH • PGE2 and PGI2 sensitise pain receptors at efferent nerve endings to mediate the pain

  10. Prostaglandin analogues • PGE1- Misoprostol, Alprostadil • PGE2- Dinoprostone, Enaprostil • PGF2α- Carboprost, Latanoprost, Bimatoprost • PGI2- Epoprostenol, Iloprost

  11. Uses Abortion • PGE2 (dinoprostone), PGE1 (misoprostol) & PGF2α (carboprost) Cervical Priming • PGE2 (dinoprostone) & PGF2α(carboprost) Healing of peptic ulcer • PGE1 (misoprostol)

  12. To prevent platelet aggregation • PGI2 (Epoprostenol) For patency of ductus arteriosus • PGE1 (Alprostadil), PGI2 (Epoprostenol) For treatment of glaucoma • PGF2α (Latanoprost, Bimatoprost) Peripheral vascular diseases • PGE1 & PGI2 are usefull… Male impotence • (Alprostadil)PGE1

  13. Side effects Hypotension Diarrhoea (PGE1)- increase the water & electrolyte secretions Bronchoconstriction Fever Anaphylactic shock- Cardiovascular collapse (Carboprost) DOSE RELATED

  14. Overall uses • Abortion- mainly second trimester • Cervical priming- Facilitation of labour • Healing of peptic ulcer- Anti-ulcerogenic • Prevents platelet aggregation- Renal dialysis & cardiopulmonary bypass • Glaucoma- Facilitates aqueous humour drainage • Male impotence- Erection • Peripheral vascular diseases

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