Pharmacology notes

Apr 15th, 2015
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Pharmacology Semester 1 page 1 of 5By Duy Thai: www.geocities.com/d.thaiENZYMES AS SITES OF DRUG ACTION IIAspirin Aspirin is an example of a drug which acts as an irreversible enzyme inhibitor. It inhibits the cyclo-oxygenase enzyme in the production of prostinoids. Production of arachidonic acid metabolites:PhospholipidAspirinirreversiblyinhibits cyclooxygenasePhospholipase A2Arachidonic acidCyclo-oxygenaseLipoxygenasesPGG2LeukotrienesLipoxinsPGH2ProstacyclinsProstaglandinsThromboxanePhospholipase A2 is not a good target because arachidonic acid is widely used for many important processes in allcells of the body. Arachidonic acid can act as a second messenger to regulate the function of protein kinases.The prostinoids (prostacyclin, prostaglandin, thromboxane) have many actions: Control vascular homeostasis Cellular proliferation Immune and inflammatory mediators ReproductionAspirin (acetyl salicylic acid) irreversibly inhibits cyclo-oxygenase by the following mechanism:Acetyl salicylic acidSalicylic acidCyclo-oxygenaseAcetylated cyclo-oxygenaseThe acetylated cyclo-oxygenase is non-functional, and remains that way.A byproduct, salicylic acid, is a reversible inhibitor of cyclo-oxygenase, although much weaker than aspirin.Clinical uses of aspirin Mild analgesic Anti pyretic Anti inflammatory agent Used in the prevention of acute myocardial infarctionsAcute myoca

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