PHAR 340 Lecture Notes - Lecture 6: Cytochrome P450, Portal Vein, Lipid Bilayer
23 Dec 2018
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Aka biotransformation, enzyme-cat conversion of drugs to their metabolites. Role: incr water solubility of a drug to encourage excretion + act of prodrug (biotransf of chem inert comp to a chem reactive radical ex. codeine morphine) Liver: primary site, high conc of enzymes + blood flow. Oral drug absorbed in gi tract into portal vein liver systemic circ, affects bioavailability. First pass: give 200 mg via iv and measure blood levels then give it orally, area b/n the curves=ba. Oral route most of drug is usually eliminated so have larger bio availability if administered any other way (iv, subcutaneous, intramuscular, ect) Phase i: create/unmask a chem group for biotransf to active compound. Phase ii: conjugation rxs w an endogenous sub, form readily excretable metabolites (rarely active) Phase i rxs oxidation rxs: loss of e-, o is incorp into drug, primary oc causes part of molecule to be lost.
