Drug Metabolism · Pharmacology

What is the primary goal of drug metabolism (biotransformation) in the body?

  1. To make the drug more lipid-soluble so that it is stored in body fat
  2. To increase the pharmacological activity of every drug so that smaller doses are needed
  3. To convert the drug into a more polar, water-soluble form for excretion
  4. To decrease the molecular weight of the drug before absorption
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Correct answer: To convert the drug into a more polar, water-soluble form for excretion

Most drugs are lipid-soluble and would be reabsorbed by the renal tubules if not metabolized. Biotransformation adds or exposes polar groups, making the metabolites water-soluble so they can be easily eliminated by the kidneys.

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