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. 2010 Jan;23(1):14–34. doi: 10.1128/CMR.00034-09

TABLE 2.

Significant rifampin drug interactions with antimicrobial agentsa

Antimicrobial Interaction(s) Recommendation Description Reference(s)
Antibiotics
    Atovaquone ↓Css 54% Contraindicated Combination not recommended 6, 104
    Clarithromycin ↓CL 90% No dosage adjustment Despite reduced levels, still effective with Mycobacterium avium complex treatment 257
    Dapsone ↓Css 7- to 10-fold No dosage adjustment Effective combination for leprosy 125, 127, 275
    Doxycycline Cmax 60-70% No dosage adjustment Effective combination for Brucella 54
    Linezolid Cmax 41%, ↓Cmin 59% No dosage adjustment Gut P glycoprotein metabolism; concern for decreased levels clinically 76, 98
    Moxifloxacin ↓AUC 31%, ↓Cmax 32% No dose adjustment recommended Reduced glucuronidation; concern for levels of moxifloxacin 184
    Metronidazole ↓AUC 33%, ↑CL 44% No dose adjustment recommended 67
Antifungals
    Caspofungin Cmin 31% Raise caspofungin dose to 70 mg i.v. daily 233
    Fluconazole ↓AUC 22%, ↓Cmax 17%, ↑CL 30% Consider raising fluconazole dose Would increase dose if used together 192
    Itraconazole Undetectable levels (case report) Combination not recommended 71
    Ketoconazole ↓AUC, ↓Cmax (levels not available) Combination not recommended 68
    Voriconazole ↓AUC 93%, ↓Cmax 96% Contraindicated 99
    Posaconazole ↓AUC, ↓Cmax (levels not available) Combination not recommended Warning in package insert, no clinical data 221
HIV medications
    NRTI
        Zidovudine ↓AUC 47%, ↓Cmax 43% No dose adjustment recommended 97
    NNRTI
        Delavirdine ↑CL 27-fold, ↓Cmax 92%, undetectable Cmin Contraindicated No longer manufactured 33
        Efavirenz ↓AUC 22%, ↓Cmax 24%, ↓Cmin 25% Consider raising efavirenz dose to 800 mg/day if patient wt >60 kg Therapeutic drug monitoring may be warranted to avoid toxicity 39, 40, 157, 196
        Etravirine No information available, likely significant ↓AUC and ↓Cmax Contraindicated 134
        Nevirapine ↓AUC 46%, ↓Cmax 42%, ↓Cmin 53% Contraindicated Failure of therapy 35, 207
    CCR5 antagonist
        Maraviroc Ratio of maraviroc PK parameters with rifampin to those without rifampin was Cmin of 0.22 (90% CI, 0.17-0.28), AUC of 0.368 (90% CI, 0.328-0.413), and Cmax of 0.335 (90% CI, 0.260-0.431) If used without a strong CYP3A inhibitor, raise maraviroc dose to 600 mg p.i. b.i.d. Must balance with ritonavir usage 271
If used with a strong CYP3A inhibitor, 300 mg p.o. b.i.d.
    Integrase inhibitor
        Raltegravir ↓AUC 40%, ↓Cmax 38%, ↓Cmin 61% Consider raising raltegravir dose to 800 mg p.o. b.i.d. 52
    Protease inhibitors
        Amprenavir ↓AUC 82%, ↓Cmax 70%, ↓Cmin 92% Contraindicated No longer formulated 203
        Atazanavir ↓AUC 53%, ↓Cmax 72%, ↓Cmin 98% Contraindicated Ritonavir does not improve levels 2, 111, 161
        Darunavir No information available, likely significant ↓AUC and ↓Cmax Contraindicated 166
        Fosamprenavir Administration with amprenavir; ↓AUC 82%, ↓Cmax 70%, ↓Cmin 92% Contraindicated Prodrug of amprenavir 203
        Indinavir ↓AUC 92%, ↓Cmax 87% Contraindicated 42, 136
        Lopinavir-ritonavir Concentrations of lopinavir, ↓AUC 75%, ↓Cmin 99% Contraindicated Ritonavir boosting did not increase levels 166, 209
        Nelfinavir ↓AUC 83%, ↓Cmax 76% Contraindicated 142
        Ritonavir ↓AUC 35%, ↓Cmax 25%, ↓Cmin 49% Contraindicated 166, 209
        Saquinavir ↓AUC 70%, ↓Cmax 65% Contraindicated Ritonavir boosting did not increase 210
        Tipranavir No information available; likely significant ↓AUC and ↓Cmax Contraindicated     levels 142
a

Abbreviations: AUC, area under curve; Cmax, concentration maximum; Cmin, concentration minimum; p.o., oral; CL, clearance; Css, steady-state concentration; i.v., intravenous; NRTI, nucleoside reverse transcriptase inhibitor; NNRTI, nonnucleoside reverse transcriptase inhibitor; PK, pharmacokinetic; ↑, increase; ↓, decrease.