Skip Navigation LinksHome > March 2013 - Volume 28 - Issue 2 > Effects of desvenlafaxine on the pharmacokinetics of desipra...
International Clinical Psychopharmacology:
doi: 10.1097/YIC.0b013e32835c1f49
Original Articles

Effects of desvenlafaxine on the pharmacokinetics of desipramine in healthy adults

Nichols, Alice I.a; Madelyn, Abella; Chen, Yangb; Behrle, Jessica A.a; Frick, Glena; Paul, Jeffreya

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The results of two single-center, two-period, open-label trials that evaluated the effects of multiple doses of desvenlafaxine on the pharmacokinetics of desipramine, a cytochrome P450 (CYP) 2D6 enzyme substrate, are presented. Healthy individuals aged 18–45 years were administered a single oral dose of 50 mg desipramine with and without 100 mg daily (n=34) or 400 mg daily (n=23) desvenlafaxine for 5 days. After coadministration of 100 mg desvenlafaxine, desipramine exposure, measured by peak plasma concentration (C max) and total area under the plasma concentration-versus-time curve (AUC), showed minimal increases of 25 and 17%, respectively; coadministration of 400 mg desvenlafaxine resulted in a 52% increase in desipramine C max and a 90% increase in AUC. For the 100 mg dose, the geometric least squares mean ratios and 90% confidence intervals (CIs) for desipramine AUC (117%; 90% CI 110–125%), 2-hydroxydesipramine AUC (114%; 90% CI 110–119%), and C max (110%; 90% CI 104–116%) were all within the 80–125% interval, showing the bioequivalence for AUC between desipramine administered alone and in combination with 100 mg desvenlafaxine. These results indicate that desvenlafaxine is a relatively weak inhibitor of CYP2D6 and that desvenlafaxine 100 mg, twice the recommended therapeutic dose of 50 mg, is unlikely to cause drug–drug interactions with CYP2D6 substrates.

© 2013 Lippincott Williams & Wilkins, Inc.


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