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  • Pathways of arachidonic acid (AA) release and metabolism.

prostaglandinsPG  leukotrienesLT thromboxinesTX prostaglandinsPG leukotrienesLT thromboxinesTX Presentation Transcript

  • P ROSTAGLANDINS PGL EUKOTRIENES LTTHROMBOXINE TXDR MUSTANSAR
  • 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).
  • PROSTAGLANDINS & LEUKOTRIENES  Localhormones - very active,many functions..  Autacoids from 20 C PUFA Prostaglandins Prostacyclin Thromboxanes Leukotrienes
  • FUNCTIONS Inflammation Smooth muscle tone Blood coagulation Reproduction GI secretion
  • .SYNTHES . PHOSPHOLI PIDSIS PHOSPHOLIPASE A2 ARACHIDO NIC ACID CYCLOOXYGENASE 5 LIPOOXYGENASE LT PG G2 A4 LT PG LT C4ISOMERASE H2 THROMBOXANE SYNTHASE B4 LT D4 PGE2 PROSTACYCLINE SYNTHASE PG THROMBOX D2 ANE A2 PG PG F2 I2
  • Pathways of arachidonic acid (AA) releaseand metabolism.
  • . PHOSPHO LIPIDS STEROIDS PHOSPHOLIPASE A2 NSAIDS ARACHIDO ZILEUTON NIC ACID CYCLOOXYGENASE 5 LIPOOXYGENASE LT A4 PG G2 PGH2 LT C4 LT B4 LT D4 PGE2 THROMB ,PG D2 OXANE A2 ,PG F2 PG I2
  • BIOSYNTHESIS OFPROSTAGLANDINS 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
  • ACTIONSInflammation Most important mediators.. Synthesised as per need. NSAIDS
  • ACTIONS –SMOOTH MUSCLESBlood vessels Pg E2, Prostacycline - vasodilatation Thromboxane A2 – constriction
  • Prostaglandins
  • ACTIONS :SMOOTH MUSCLEBronchus PgE2 •BRONCHO DILATION PgI2 PgF2α •CONSTRICT TXA2 ION LT
  • UTERUSBoth uterus &cervix Cervical Initiation ripening of Labour •PgE2 •PgE1 •PgF2
  • ACTIONS GIT MUCUS HCO3- ACIDNatural ulcer protectants..NSAIDS..
  •  GIT CrampsMotilit Secretio y n Diarrho ea
  • RENALPgE2,Prostacyclin -protective.. PgE2,Pg I2 RENAL DIRECT ON VASODILATA TUBULES TION RBF DIURESIS NATRIURESIS
  • COAGULATION TXA PLATEL AGGREGATIO ETS N 2 (-) ENDOTHELPgI2 IUM AGGREGATIO N
  • . Pulmonary vessels- vasodilatation CNS- EYE-↓IOT Neurotransmit ter
  • Clinical Application Female Reproductive Organ Male Reproductive System Inflammation & Immunity Gastrointestinal Tract Respiratory System Musculo skeletal Cardiovascular Glaucoma Kidney Cancer
  • Preparations &Uses
  • Prostagln PreparationPREPARATIONSdinPgE₁ Misoprostol , Alprostadil,Latanopros tPgE₂ Rioprostil , Enprostil DinoprostonePgF₂α Prostin15Methyl Carboprost / Prostodin
  • USES1.ObstetricsTherapeutic abortion PgE1/MISOPRO STOLCervical ripening PgE₁/PgE2Severe Post partum hge 15METHYL PgF2 im/PgE1 Rectal
  • 2.Peptic ulcer PgE1/Misoprostol PgE2/Enprostil,Rioprostil,Arbaprostil3.Glaucoma : PgE1 / Latanoprost4-PDA PgE1/Alprostadil5-Primary pulmonary hypertention : PgI ₂
  • SUMMARY OF USESUse PreparationAbortion PgE1Cervical PgE1 / E2ripeningPeptic ulcer PgE1Glaucoma PgE1- LatanoprostPPH PgI2
  • ADRVomiting,Diarrhoea,Abdo minal crampsUterine crampsBronchospasm
  • LEUKOTRIENES
  • PHOSPHOLIPIDS ARACHIDONIC ACIDCYCLOOXYGE LIPOOXYGEN NASE ASE Zileuton LEUKOTRI ENES LEUKOTRIE Monteleuk NEPROSTAGLANDINS astZafirleu RECEPTOR kast Chromoglyc MAS ate T Nedochromi CEL l L