This document discusses eicosanoids, which are oxygenation products of arachidonic acid. It specifically focuses on prostaglandins and leukotrienes. Prostaglandins and leukotrienes are local hormones derived from arachidonic acid that have many functions, including roles in inflammation, smooth muscle tone, blood coagulation, reproduction, and GI secretion. The document outlines the pathways and enzymes involved in their biosynthesis, including the roles of cyclooxygenase and lipoxygenase. It also discusses the actions and clinical applications of various prostaglandins.

1. P ROSTAGLANDINS PG
L EUKOTRIENES LT
THROMBOXINE TX
DR MUSTANSAR

4. 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).

5. PROSTAGLANDINS & LEUKOTRIENES
 Localhormones - very active,many
functions..
 Autacoids from 20 C PUFA
Prostaglandins
Prostacyclin
Thromboxanes
Leukotrienes

6. FUNCTIONS
Inflammation
Smooth muscle tone
Blood coagulation
Reproduction
GI secretion

7. .
SYNTHES
. PHOSPHOLI
PIDS
IS PHOSPHOLIPASE A2
ARACHIDO
NIC ACID
CYCLOOXYGENASE 5 LIPOOXYGENASE
LT
PG G2
A4
LT
PG LT C4
ISOMERASE H2 THROMBOXANE
SYNTHASE B4 LT
D4
PGE2 PROSTACYCLINE
SYNTHASE
PG THROMBOX
D2 ANE A2
PG
PG
F2 I2

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

10. . 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

11. 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

12. ACTIONS
Inflammation
Most important
mediators..
Synthesised as per need.
NSAIDS

13. ACTIONS –SMOOTH MUSCLES
Blood vessels
Pg E2, Prostacycline -
vasodilatation
Thromboxane A2 –
constriction

14. Prostaglandi
ns

15. ACTIONS :SMOOTH MUSCLE
Bronchus
PgE2 •BRONCHO
DILATION
PgI2
PgF2α •CONSTRICT
TXA2 ION
LT

16. UTERUS
Both uterus &cervix
Cervical Initiation
ripening of Labour
•PgE2 •PgE1
•PgF2

17. ACTIONS
 GIT
MUCUS
HCO3-
ACID
Natural ulcer protectants..
NSAIDS..

18.  GIT
Cramps
Motilit Secretio
y n Diarrho
ea

19. RENAL
PgE2,Prostacyclin -protective..
PgE2,Pg
I2
RENAL
DIRECT ON
VASODILATA TUBULES
TION
RBF
DIURESIS
NATRIURESIS

20. COAGULATION
TXA PLATEL AGGREGATIO
ETS N
2
(-)
ENDOTHEL
PgI2 IUM AGGREGATIO
N

21. .
Pulmonary
vessels-
vasodilatation
CNS-
EYE-↓IOT Neurotransmit
ter

22. Clinical Application
 Female Reproductive Organ
 Male Reproductive System
 Inflammation & Immunity
 Gastrointestinal Tract
 Respiratory System
 Musculo skeletal
 Cardiovascular
 Glaucoma
 Kidney
 Cancer

24. Preparations &
Uses

25. Prostagln Preparation
PREPARATIONS
din
PgE₁ Misoprostol ,
Alprostadil,Latanopros
t
PgE₂ Rioprostil , Enprostil
Dinoprostone
PgF₂α Prostin
15Methyl Carboprost / Prostodin

26. USES
1.Obstetrics
Therapeutic abortion
PgE1/MISOPRO
STOL
Cervical ripening
PgE₁/PgE2
Severe Post partum hge
15METHYL
PgF2
im/PgE1
Rectal

27. 2.Peptic ulcer
PgE1/Misoprostol
PgE2/Enprostil,Rioprostil,Arbaprostil
3.Glaucoma : PgE1 / Latanoprost
4-PDA PgE1/Alprostadil
5-Primary pulmonary hypertention : PgI ₂

28. SUMMARY OF USES
Use Preparation
Abortion PgE1
Cervical PgE1 / E2
ripening
Peptic ulcer PgE1
Glaucoma PgE1-
Latanoprost
PPH PgI2

36. ADR
Vomiting,Diarrhoea,Abdo
minal cramps
Uterine cramps
Bronchospasm

37. LEUKOTRIENES

38. PHOSPHOLIPIDS
ARACHIDONIC
ACID
CYCLOOXYGE LIPOOXYGEN
NASE ASE
Zileuton
LEUKOTRI
ENES
LEUKOTRIE
Monteleuk NE
PROSTAGLANDINS
astZafirleu RECEPTOR
kast
Chromoglyc MAS
ate T
Nedochromi CEL
l L