Pharmacology · single question

Drug metabolization (biotransformation) by the liver will make the drug:

  1. More fat-soluble
  2. More pharmacologically active
  3. More lipophilic
  4. More water-soluble
Show answer and explanation

Correct answer: D. More water-soluble

  • A. INCORRECT — Drugs are typically already fat-soluble when absorbed; metabolism CONVERTS them to water-soluble metabolites for renal excretion.
  • B. INCORRECT — Most drug metabolism results in INACTIVE metabolites (detoxification). Some prodrugs are activated by metabolism, but this is the exception, not the rule.
  • C. INCORRECT — Lipophilicity (fat-solubility) is DECREASED by hepatic metabolism; increased water solubility is the goal.
  • D. CORRECT — Hepatic drug metabolism (Phase I and Phase II reactions) converts lipophilic drugs into more water-soluble (hydrophilic) metabolites that can be excreted by the kidneys. This is the primary purpose of biotransformation.

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