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Pharmacology · single question

Which medication produces the most clinically significant ACTIVE METABOLITES?

  1. Diazepam
  2. Atorvastatin
  3. Lisinopril
  4. Amoxicillin
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Correct answer: A. Diazepam

Diazepam is metabolized to desmethyldiazepam (nordazepam) — an active metabolite with a half-life of 36-200 hours, causing prolonged sedative effects.
  • A. CORRECT. Diazepam produces desmethyldiazepam (nordazepam) — a potent, long-acting active metabolite (t½ 36-200h). This explains why benzodiazepines accumulate with repeated dosing, especially in elderly patients and those with liver disease.
  • B. Atorvastatin does have active metabolites but diazepam is the classic textbook example with the most clinically significant long-lasting active metabolites.
  • C. Lisinopril is itself active (not a prodrug) and does not rely on metabolites for its ACE-inhibiting effect.
  • D. Amoxicillin is not significantly metabolized to active metabolites — it is excreted largely unchanged in the urine.

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