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Rifampin and other rifamycins

INTRODUCTION

The rifamycins include rifampin, rifapentine, and rifabutin. Of these, rifampin is the rifamycin most commonly used as first-line therapy in combination with other agents for the treatment of mycobacterial infections, including tuberculosis [1]. Rifapentine has an increased half-life compared to rifampin.

This topic will review issues related to the clinical use of rifampin and rifapentine. (For additional information (see "Rifampin (rifampicin): Patient drug information" and "Rifapentine: Drug information". The clinical settings in which rifampin may be used are discussed separately in the appropriate topic reviews.

RIFAMPIN

Rifampin is the rifamycin most commonly used as first-line therapy in combination with other agents for the treatment of mycobacterial infections, including tuberculosis [1]. It is also used as a prophylactic agent following exposures to Neisseria meningitidis and H. influenzae and for the prevention and treatment of deep-seated staphylococcal infections.

Mechanism of action — Rifampin is thought to inhibit bacterial DNA-dependent RNA polymerase, which is not a mechanism of action shared with other antibiotics. This effect on RNA polymerase appears to result from drug binding in the polymerase subunit deep within the DNA/RNA channel where direct blocking of the elongating RNA can occur [2].

Resistance — Resistance to rifampin arises due to missense mutations in the rpoB gene and occurs in a variety of bacteria including Mycobacterium tuberculosis, methicillin-resistant Staphylococcus aureus (MRSA), Streptococcus pneumoniae, and Rickettsiae [3-6]. Resistance has been demonstrated in many parts of the world. Cross-resistance to rifabutin or rifapentine depends upon the mutation type.
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References Top
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