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 |
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.