Mechanism of Action

Macrolides bind to the 50S ribosomal subunit of bacteria but not to the 80S mammalian ribosome; this accounts for its selective toxicity. Binding to the ribosome occurs at a site near peptidyltransferase, with a resultant inhibition of translocation, peptide bond formation, and release of oligopeptidyl tRNA. However, unlike chlo-ramphenicol, the macrolides do not inhibit protein synthesis by intact mitochondria, and this suggests that the mitochondrial membrane is not permeable to erythro-mycin.

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