Rifampicin and Rifabutin

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Chapter: Pharmaceutical Microbiology : Mechanisms of action of antibiotics and synthetic anti-infective agents

Rifampicin acts on the β subunit of RNA polymerase. Binding of just one molecule of rifampicin inhibits the initiation stage of transcription in which the first nucleotide is incorporated in the RNA chain.


Rifampicin And Rifabutin

 

 

Rifampicin acts on the β subunit of RNA polymerase. Binding of just one molecule of rifampicin inhibits the initiation stage of transcription in which the first nucleotide is incorporated in the RNA chain. Once started, transcription itself is not inhibited. It has been suggested that the structure of rifampicin resembles that of two adenosine nucleotides in RNA; this may form the basis of the binding of the antibiotic to the β subunit. One problem is the rapid development of resistance in organisms due to alterations in the amino acids comprising one particular region of the β subunit. These changes do not affect the activity of the polymerase but render it insensitive to rifampicin. The action of rifampicin is specific for the microbial RNA polymerase, the mammalian version being unaffected. Rifabutin, which has enhanced activity against Mycobacterium avium complex, is thought to act in the same way as rifampicin.

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