Rifampin: mechanisms of action and resistance.

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Wehrli W

Rifampin: mechanisms of action and resistance.

Rev Infect Dis. 1983 Jul-Aug;5 Suppl 3:S407-11.

PubMed ID

6356275 [ View in PubMed

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Abstract

Rifampin specifically inhibits bacterial RNA polymerase, the enzyme responsible for DNA transcription, by forming a stable drug-enzyme complex with a binding constant of 10(-9) M at 37 C. The corresponding mammalian enzymes are not affected by rifampin. Bacterial resistance to rifampin is caused by mutations leading to a change in the structure of the beta subunit of RNA polymerase. Such resistance is not an all-or-nothing phenomenon; rather, a large number of RNA polymerases with various degrees of sensitivity to rifampin have been found. No strict correlation exists between enzyme sensitivity and MIC values, since inhibition of RNA synthesis does not always show up to the same extent in the two different test systems used for the determination of these values.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Rifampicin	DNA-directed RNA polymerase subunit beta	Protein	Escherichia coli (strain K12)	Yes	Inhibitor	Details