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. 2021 Aug 17;65(9):e0104321.
doi: 10.1128/AAC.01043-21. Epub 2021 Aug 17.

Model-Based Comparative Analysis of Rifampicin and Rifabutin Drug-Drug Interaction Profile

Vianney Tuloup  1   2 , Mathilde France  1 , Romain Garreau  1   2 , Nathalie Bleyzac  1 , Laurent Bourguignon  1   2   3 , Michel Tod  1   2   3 , Sylvain Goutelle  1   2   3
Affiliations

Model-Based Comparative Analysis of Rifampicin and Rifabutin Drug-Drug Interaction Profile

Vianney Tuloup et al. Antimicrob Agents Chemother. .

Abstract

Rifamycins are widely used for treating mycobacterial and staphylococcal infections. Drug-drug interactions (DDI) caused by rifampicin (RIF) are a major issue. We used a model-based approach to predict the magnitude of DDI with RIF and rifabutin (RBT) for 217 cytochrome P450 (CYP) substrates. On average, DDI caused by low-dose RIF were twice as potent as those caused by RBT. Contrary to RIF, RBT appears unlikely to cause severe DDI, even with sensitive CYP substrates.

Keywords: drug-drug interaction; pharmacokinetics; rifabutin; rifampicin.

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Figures

FIG 1
FIG 1
Predicted versus observed AUC ratio of substrate drugs for DDI caused by rifampicin and rifabutin reported in the literature. The solid line is the line of identity (y = x). The dotted line is y = 0.5x, and the combined dashed and dotted line is y = 2x. Abbreviations: RBT300, rifabutin at 300 mg/day (red circles); RIF600, rifampicin at 600 mg/day (cyan circles).
FIG 2
FIG 2
Box plot of predicted AUC ratios for 217 drug-drug interactions between CYP substrates and rifamycin agents. Abbreviations: RIF 600; rifampicin at 600 mg/day; RBT 300, rifabutin at 300 mg/day.
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References

    1. Niemi M, Backman JT, Fromm MF, Neuvonen PJ, Kivistö KT. 2003. Pharmacokinetic interactions with rifampicin. Clin Pharmacokinet 42:819–850. 10.2165/00003088-200342090-00003. - DOI - PubMed
    1. Crabol Y, Catherinot E, Veziris N, Jullien V, Lortholary O. 2016. Rifabutin: where do we stand in 2016? J Antimicrob Chemother 71:1759–1771. 10.1093/jac/dkw024. - DOI - PubMed
    1. Horne DJ, Spitters C, Narita M. 2011. Experience with rifabutin replacing rifampin in the treatment of tuberculosis. Int J Tuber Lung Dis 15:1485–1490. 10.5588/ijtld.11.0068. - DOI - PMC - PubMed
    1. Gonzalez-Montaner LJ, Natal S, Yongchaiyud P, Olliaro P, Abbate E, Mosca C, Casado G, Di Lonardo M, Gerhart-Filho G, Betjel I, Ferreira-Lima S, Narinho AP, Lopez R, Carlos-Moreira A, Santana A, Filho AC, Magahaes M, Marinho A, Cavabarra-Cardoso N, Branao-Montero R, Prijanonda B, Nuchprayoon C, Punnotok J, Chakorn T, Carpentieri M, Dolfi L, Maniero A. 1994. Rifabutin for the treatment of newly-diagnosed pulmonary tuberculosis: a multinational, randomized, comparative study versus rifampicin. Tuber Lung Dis 75:341–347. 10.1016/0962-8479(94)90079-5. - DOI - PubMed
    1. Albano M, Karau MJ, Greenwood-Quaintance KE, Osmon DR, Oravec CP, Berry DJ, Abdel MP, Patel R. 2019. In vitro activity of rifampin, rifabutin, rifapentine, and rifaximin against planktonic and biofilm states of staphylococci isolated from periprosthetic joint infection. Antimicrob Agents Chemother 63:e00959-19. 10.1128/AAC.00959-19. - DOI - PMC - PubMed