PROSTAGLANDINS

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PROSTAGLANDINS :

PROSTAGLANDINS Dr. Akanksha G. William 24 Jan. 2011

Overview :

Overview History Classification & Nomenclature Synthesis Physiological actions Pharmacological uses Adverse effect Individual drugs

History :

History 1930 Kurzrok & Lieb 1935 von Euler coined the term PROSTAGLANDINS 1962 Samuelsson, Bergstorm et al. elucidated structures of PGE1 & PG F 2 α 1964 Bergstorm - Biosynthesis of PGE 2 from AA

1970 Von Euler Nobel Prize:

1970 Von Euler Nobel Prize

1982 BERGSTORM & SAMELSON :

1982 BERGSTORM & SAMELSON

Arachidonic Acid:

Arachidonic Acid

Slide 7:

CYP FREE RADICAL AA LOX ETHANOL AMIDE COX

Synthesis :

Synthesis

NOMENCLATURE :

NOMENCLATURE PGE 2 Vascular GIT Lungs

PGF2α:

PGF 2 α Vascular s mooth muscles Git Bronchi Uterus

PGD2:

PGD 2

Cyclo OXygenase:

C yclo OX ygenase COX 1 house keeping (almost all cells) COX 2 inflammatory (brain & kidney ) COX 3 unknown (# paracetamol )

Prostanoids :

Prostanoids PGE 2 PGI 2 PGD 2 PGF 2 α TXA 2

Physiological role of PG E2:

Physiological role of PG E 2 VASODILATOR Maintains ductus arteriosus Helps in maintaining placental blood flow

Clinical Significance(C/S):

Clinical Significance(C/S) Alprostadil

Slide 18:

Renal vasodilatation Na + /water K + excretion Chloride reabsorption Antagonizes action of ADH Renin release Hyperprostaglandin E syndrome/Bartter

Bartter Syndrome:

Bartter Syndrome

Erectile dysfunction :

Erectile dysfunction

Slide 21:

Maintain normal renal flow Blood pressure Continued blockade leads to hypertension Blunts the affect of diuretics

UTERUS:

UTERUS Contracts the uterus Softening of cervix Facilitates sperm movement

C/S:

C/S Dysmenorrhoea Augmentation of labour Convert oxytocin resistant uterus into oxytocin sensitive Cervical ripening

C/S:

C/S MTP Dinaprost Cx ripening II trimester abortion mensural regulation ADR severe mensural cramps heavy mensural bleeding

Slide 25:

Misoprostol orally active( 400mcg ) used along with methotrexate and mefepristone ( ectopic )

Smooth Muscle :

Smooth Muscle Bronchodilator Relaxes smooth muscles

C/S:

C/S

GIT:

GIT Contracts longitudinal muscles mucus production blood flow Helps in ulcer healing

Role in inflammation :

Role in inflammation Vasodilatation Chemotaxis Permeability Exudation Lysosomal degradation

CNS:

CNS Sensitizes nerves to pain Rise on body temperature Sedation Rigidity

HORMONAL :

HORMONAL Helps in the release of anterior pituitary hormones Mobilizes calcium from the bones

PGI2:

PGI 2 Inhibitor of platelet aggregator Mild bronchodilator Inhibits histamine release Evokes renin release Produced by vascular endothelium Maintains patency of ductus arteriosus Hypotensive (more thanPGE 2 )

PGI2 Analogues:

PGI 2 Analogues TREPROSTINIL ILOPROST PVD Pul . Hypertension ( Combination with PGE 2 )

PGF2ά:

PGF 2 ά Contracts the human uterus Bronchoconstriction Contracts longitudnal muscles Induces ocluar inflammation Decreases iot by increasing US outflow Increases in HepatoRenal Syndrome

C/S :

C/S PPH II trimester abortions Glaucoma ADR Cvs collapse anahpylaxis Pulmonary hypertension discolouration

TXA2:

TXA 2

Slide 37:

Produced by platelets Potent inducer of platelet aggregation Constituent of release reaction Renal vasoconstriction Bronchoconstriction

PGD2:

PGD 2 Anti platelet aggregartory Bronchoconstrictor Evokes renin release Mainly secreted by mast cells Constituent of slow release substance of anaphylaxis Slowly metabolised

Receptors :

Receptors Receptor Sub type Primary coupling PGD 2 DP 1 ↑c A mp PGD 2 DP 2 ↑Ca PGE 2 EP 1 ↓↑----- PGE 2 EP 2 ↑c A mp PGE 2 EP 3A-D ↓c A mp ↑c A mp ↑ PLC PGE 2 EP 4 ↑c A mp PGF 2 α FP A,B ↓↑ PGI 2 IP ↑c A mp

Thank You:

Thank You