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Open-label, single-sequence, add-on drug interaction study in healthy subjects
Rilpivirine 25mg once daily, designated in this study as TMC278, was given to HIV-negative subjects on stable methadone maintenance therapy. The active from of methadone, R-methadone, experienced a decrease in the mean Cmin, Cmax, and AUC by 22%, 14%, and 16% respectively as compared with methadone alone.
The addition on rilpivirine in standard doses to stable methadone maintenance regimens lead to the decrease of both R- and S-methadone (R-methadone is the active form). The exposure of rilpivirine in these patients remained in the expected range. While no dose adjustments of either drug are recommended, it is important to watch for methadone withdrawal symptoms when administering these agents concomitantly. Methadone dose adjustments may be needed.
Crauwels, H., Van Heeswijk, R. P. G., Vandevoorde, A., McNeeley, D. F., Bue. Pharmacokinetic interaction study between tmc278, a next-generation nnrti, and methadone. International Aids Conference. Vienna, Austria. XVIII; July 2010.