Ritonavir has minimal impact on the pharmacokinetic disposition of a single dose of bupropion administered to human volunteers

J Clin Pharmacol. 2006 May;46(5):567-76. doi: 10.1177/0091270006286981.


A drug-drug interaction study was conducted to determine whether ritonavir (200 mg; 4 doses over 2 days) alters the pharmacokinetic disposition of bupropion (75 mg; once) coadministered to 7 healthy volunteers in a placebo-controlled 2-way crossover study. Serum samples collected from 0 to 24 hours after bupropion administration were assayed for concentrations of bupropion and metabolites (hydroxybupropion, threohydrobupropion, and erythrohydrobupropion). Derived pharmacokinetic parameters were compared between placebo/bupropion and ritonavir/bupropion trials by paired t test. The effect of ritonavir on most pharmacokinetic parameters was minimal (<20% mean change). The only parameters that showed a statistically significant effect were threohydrobupropion area under the blood concentration curve (14% +/- 5% decrease, mean +/- SE; P = .04) and erythrohydrobupropion time-to-maximal serum concentration (161% +/- 92% increase, P = .03), suggesting that ritonavir may inhibit the carbonyl reductase enzyme responsible for formation of these metabolites. These findings indicate that short-term ritonavir dosing has only minimal impact on the pharmacokinetic disposition of a single dose of bupropion in healthy volunteers.

Publication types

  • Randomized Controlled Trial
  • Research Support, N.I.H., Extramural

MeSH terms

  • Adult
  • Antidepressive Agents, Second-Generation / blood
  • Antidepressive Agents, Second-Generation / pharmacokinetics*
  • Antiviral Agents / blood
  • Antiviral Agents / pharmacokinetics*
  • Bupropion / analogs & derivatives
  • Bupropion / blood
  • Bupropion / pharmacokinetics*
  • Cross-Over Studies
  • Drug Interactions
  • Humans
  • Male
  • Ritonavir / blood
  • Ritonavir / pharmacokinetics*


  • Antidepressive Agents, Second-Generation
  • Antiviral Agents
  • hydrobupropion
  • Bupropion
  • Ritonavir
  • radafaxine