The pharmacokinetics of the NNRTI rilpivirine (RPV) in the presence of the antimycobacterial rifabutin.
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Study Design
A pharmacokinetic study (n=18) conducted by the manufacturer showed a decrease in rilpivirine AUC by 42% (90% CI, 35-48) for the 25mg QD dose, and a 16% (90% CI, 6-26) increase for the 50mg QD dose when co-administered with rifabutin 300mg QD.
Study Results
An earlier pharmacokinetic study conducted on rilpivirine as an investigational drug (TMC278) at a dose of 150mg QD also showed a similar decrease in AUC24h (0.54, 90%CI 0.50-0.58) when coadministered with rifabutin 300mg QD, compared to rilpivirine alone. However, AUC24h of rifabutin and metabolite 25-O-desacetyl-rifabutin were not affected by co-administration with rilpivirine (1.03, 90%CI 0.97-1.09 and 1.07, 90%CI 1.02-1.11, respectively).
Study Conclusions
***With rifabutin co-administration, the EDURANT (rilpivirine) dose should be increased to 50 mg (two tablets of 25 mg each) taken once daily with a meal. When rifabutin co-administration is stopped, the EDURANT (rilpivirine) dose should be decreased to 25 mg taken once daily with a meal. Likewise, if COMPLERA (emtricitabine, rilpivirine, tenofovir disoproxil fumarate) is administered with rifabutin, an additional 25mg tablet of rilpivirine once daily is recommended to be taken concomitantly with Complera with food, for the duration of co-administration with rifabutin.
References
Crauwels HM, van Huijkelom R, Stevens M, Mrus J, Hoetelmans RM. The pharmacokinetics of the nnrti rilpivirine (rpv) in the presence of the antimycobacterial rifabutin. International Aids Society Conference On Hiv Pathogenesis, Treatment, And Prevention. Kuala Lumpur, Malaysia . 7; June 2013.
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