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