TABLE 1

List of reported rifampin drug-drug interactions with either intravenously or orally administered CYP3A4 victim drugs

Details of the references are listed in the supplemental data.

Intravenous Induction DDI DatasetOral Induction DDI Dataset
Victim DrugEHaAUC Fold ChangeReferenceVictim DrugfmCYP3A4bAUC Fold ChangeReference
Alfentanil0.322.7Kharasch et al., 2004Alfentanil0.8721.9Kharasch et al., 2004
Alfentanil0.322.8Kharasch et al., 1997Alprazolam0.808.5Schmider et al., 1999
Alfentanil0.322.3Phimmasone et al., 2001Atorvastatin0.775.1Backman et al., 2005
Cyclosporine0.191.4Hebert et al., 1992Cyclosporine0.713.7Hebert et al., 1992
Midazolam0.542.1Phimmasone et al., 2001Midazolam0.947.2Adams et al., 2005
Midazolam0.541.5Link et al., 2008Midazolam0.948.0Chung et al., 2006
Midazolam0.541.9Kharasch et al., 2004Midazolam0.9419.1Eap et al., 2004
Midazolam0.542.6Kharasch et al., 1997Midazolam0.9414.5Gorski et al., 2003
Midazolam0.542.2Gorski et al., 2003Midazolam0.9417.7Gurley et al., 2006
Midazolam0.541.9Yu et al., 2004Midazolam0.9419.0Kharasch et al., 2004
Midazolam0.542.3Yu et al., 2004Midazolam0.9414.6Floyd et al., 2003
Midazolam0.542.3Yu et al., 2004Nifedipine0.7112.2Holtbecker et al., 1996
Midazolam0.541.8Floyd et al., 2003Quinidine0.766.0Twum-Barima et al., 1981
Midazolam0.542.3Eeckhoudt et al., 2001Quinidine0.768.8Damkier et al., 1999
Nifedipine0.541.4Holtbecker et al., 1996Repaglinide0.494.9Bidstrup et al., 2004
Quinidine0.213.7Twum-Barima et al., 1981Repaglinide0.492.4Niemi et al., 2000
Tacrolimus0.031.5Hebert et al., 1999Repaglinide0.491.5Hatorp et al., 2003
Verapamil0.641.2Barbarash et al., 1988Tacrolimus0.993.1Hebert et al., 1999
Triazolam0.9220.0Villikka et al., 1997
Verapamil0.3015.4Barbarash et al., 1988
Zolpidem0.603.6Villikka et al., 1997
  • a Hepatic extraction ratio calculated from reported intravenous clearance data (Gertz et al., 2010).

  • b Fraction metabolized by CYP3A4. Values were collected from the literature (Houston and Galetin, 2008; Shou et al., 2008) (alfentanil, verapamil).