Drug Metabolism: Chemical and Enzymatic Aspects: Textbook by Jack P. Uetrecht

By Jack P. Uetrecht

So that it will comprehend drug metabolism at its so much primary point, pharmaceutical scientists needs to be in a position to examine drug compound buildings and are expecting attainable metabolic pathways with a view to keep away from the danger of inauspicious reactions that result in the withdrawal of a drug from the marketplace. This complete textbook will reduction in guiding scholars in the course of the popularity of the chemical underpinnings of drug metabolism. whereas there are lots of assets on hand for figuring out drug constitution, and different texts in terms of drug metabolism from a organic point of view, there isn't any different source at the moment to be had that hyperlinks either the chemical and organic terminology jointly in a transparent and concise language, written, to be available to be used within the lecture room, as an schooling device for educating drug improvement. Drug Metabolism: Chemical and Enzymatic elements explains, to lecturers and scholars alike, how a drug is metabolized, the aptitude results of the metabolites, broad fabric to assist comprehend drug metabolism inside of a organic context, and useful difficulties and solutions.

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Example text

For example, CYP2B6 catalyzes the 4-hydroxylation and the N-decholorethylation of the anticancer agents cyclophosphamide and ifosfamide (15), respectively, the 4-hydroxylation of the anesthetic agent propofol (16), and the methyl group hydroxylation of the antidepressant and antismoking agent bupropion (17) (Fig. 9). The O-deethylation of 7-ethoxy-4-trifluoromethylcoumarin has been the favored substrate to probe for CYP2B6 activity (18), but recent evidence indicates that it is not as selective for CYP2B6 as one would hope because both CYP1A2 and CYP2E1 also catalyze this reaction.

303 is the slope of the elimination curve. kinetics because therapeutic doses are generally low enough to allow this to be true, a few do not. , phenytoin and salicylate, can be particularly difficult in finding and maintaining a dose level that is therapeutic without being toxic. Volume of distribution, V D , is the proportionality constant that equates the amount of drug in the body (A) to its concentration in plasma (C) [Eq. 3)]. 3) From Eq. 3), V D is the apparent volume that a given amount of drug will occupy based on its plasma concentration.

In humans, the P450s are found throughout the body but the highest concentrations are localized in the body’s chemical factory—the liver. At the subcellular level, the P450s are found in the endoplasmic reticulum. Upon cellular homogenization followed by 100000 × g centrifugation, the P450s present in endoplasmic reticulum can be isolated as a subcellular fraction known as microsomes. This is the primary enzymatic preparation that has been utilized for the last several decades for in vitro drug metabolism studies.

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