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Rifamycins (rifampin, rifabutin, rifapentine)

Richard H Drew, PharmD, MS, FCCP, FIDP
Section Editor
Stephen B Calderwood, MD
Deputy Editor
Elinor L Baron, MD, DTMH


The rifamycins include rifampin, rifapentine, and rifabutin. Of these, rifampin is most commonly used, either as first-line therapy (in combination with other agents) for treatment of mycobacterial disease (including tuberculosis) [1] or for select invasive staphylococcal infections (as part of combination therapy) [2].

Rifamycins are moderate to potent inducers of drug metabolism, which can lead to reduced bioavailability and enhanced clearance of some coadministered medications. Such interactions may be delayed in onset but persist beyond rifamycin coadministration. Therefore, patients receiving any rifamycin should have their medication regimen analyzed carefully for drug interactions; this may be done by use of the Lexi-Interact program included within UpToDate.

Issues related to pharmacology of rifampin, rifabutin, and rifapentine will be reviewed here. Issues related to clinical use of rifampin and rifapentine are discussed separately. (See related topics.)


Rifampin is the most commonly used rifamycin for treatment of nontuberculous mycobacterial diseases, in combination with other agents [1]. It is also used for treatment of treatment of tuberculosis (active and latent infection) and for prophylaxis following exposure to Neisseria meningitidis or Haemophilus influenzae and as an adjunctive agent for treatment of select deep-seated staphylococcal infections. (See related topics.)

Mechanism of action — Rifampin is thought to inhibit bacterial DNA-dependent RNA polymerase, which appears to occur as a result of drug binding in the polymerase subunit deep within the DNA/RNA channel, facilitating direct blocking of the elongating RNA [3].

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Literature review current through: Dec 2017. | This topic last updated: Feb 09, 2017.
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