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Solutions For An Introduction to Medicinal Chemistry Chapter 11 Problem 7Q

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Solution 1

Two drugs are used in the treatment of attention deficit hyperactive disorder. These include; atomoxetine and methylphenidate. They are sold in the market as Strattera and Ritalin respectively. These drugs are largely excreted from the body as metabolites of their original molecular form.

The metabolism of atomoxetine occurs through the action of the cytochrome P450 enzyme CYP2D6. The dominant oxidative metabolite in atomoxetine is 4-hydroxyatomoxetine. In vivo method, the oxidative metabolite is glucuronidated and is excreted in the urine and feces as 4--hydroxyatomoxetine-O-glucuronide.

Methylphenidate gets metabolized within the liver as a biologically inactive metabolite known as ritalinic acid or a-phenyl-2piperidine acetic acid. The enzyme responsible for this metabolism is the carboxyl esterase CES1A1. As is the case with atomoxetine, these metabolites are what are primarily excreted from the body.

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Solutions For Problems in Chapter 11