Eicosanoids Pharmacology

1. Ecosanoids
Immunity PGE2
MyeloidDrieved Suppresive T Cells
Dendretic (antigen presenting) cels
Natural killer cells
supression
Thrombosis
Clotting
endothelium
PGI2
platelets aggregation
vasodilatation
TXA2 Platelets
Ca+2
vasoconstriction
platelets aggregation
balanced PGI2 & TXA2
Platelets
PGE2
platelets aggregation
vasodilatation
Kidney
PGI2
PGE2
vasodilatation Renal Blood Flow
Angiotensin 2
GFR
sympathetic activity
stimulated by
opposing vasoconstriction of norepinephrine
GIT
renin Na+ excretion Cl reabsorption
B.P.
PGI2
PGE2
mucous thickening,turnover,blood flow&Hco3- HCl
PGF2alpha contaction darrhea & spasm maintain peristalsis
Uterus
contraction oxytocin sensitivity
softening cervix facilitating sperm movement
Respiratory tract
PGE2
PGF2
potent bronchodilatation
potent bronchoconstriction
Inflammation
PGE2
PGD2
Fever,Stupor,Erythema,Wheel formation
capillary permeabiity
Temperature PEG2
Fever causing cytokine(IL-1)
hypothalamus temperature
M.O. growth Repair
NSAIDs
Nonselective
Cox inhibitors
Salicylate,mefenamic acid
Diclophenac,piroxicam
Indomethacin,Ibuprofen
Selective Cox
2 inhibitors
celecoxib, meloxicam
safe to ulcerative stomach
NOT safe to
stomach,kidner
children
Reye syndrome
Brain&liver dysfunction
pain,fever,inflammation
Cox3(dark horse)
Inhibitor
poor anti-inflammatory,analgesic,antipyretic
by viral infection
little efect on coc1&2
ex: paracetamol & dipyrone
safe to children
Biosynthesis
acting central
acting central&peripheral
PG catabolism
rapidly removed from circulation
90%of metabolism in liver