PHAR 340 Lecture Notes - Lecture 6: Portal Vein, Biotransformation, Prodrug
21 Sep 2019
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Biotransformation of chemically inert compound to a chemically reactive radical e. g. with codeine and morphine. Give large amount of codeine, need to convert first, don"t get rush. Morphine: prescription, if could get this btc, would extract morphine and sell. Oral drugs (pills) pass directly to the liver. Everything dumps into portal vein, then to liver for effect, then systemic circ. Do blood sampling to figure out how much drug actually got into body. Po starts a 0, then peaks and troughs. Iv starts at max, then declines, larger area under curve, higher total exposure. Small area so can also precipitate so aren"t distributed. Create/unmask a chemical group (polar) that allows for phase ii. Conjugation reaction w/ endogenous substance, usually water soluble. With conjugated group, different 3d conformation so can"t interact w/ receptor. Drug could skip phase i (have oh already) then gets conjugated and excreted. Drug could be inactive, activated in liver, then conjugated and excreted.
