Sedatives and Hypnotics · Pharmacology

Why does Diazepam have a much longer duration of action than its initial half-life suggests?

  1. It binds irreversibly to the GABA-A receptor and cannot dissociate
  2. It inhibits its own metabolism by suppressing hepatic CYP3A4 activity
  3. It is converted into active metabolites with very long half-lives
  4. It is excreted unchanged by the lungs over several days
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Correct answer: It is converted into active metabolites with very long half-lives

Diazepam is metabolized by the liver into several active metabolites, including nordiazepam (desmethyldiazepam), which has a half-life of over 100 hours. This results in cumulative effects and prolonged sedation, especially with repeated dosing.

Difficulty: Medium Question 14 of 20

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