6990-06-3

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Questions And Answer

• Mode of action

  Fusidic acid forms a stable complex with an elongation factor (EF-G) involved in translocation and with guanosine triphosphate (GTP), which provides energy for the translocation process. One round of translocation occurs, with hydrolysis of GTP, but the fusidic acid–EF-G–GDP complex cannot dissociate from the ribosome, thereby blocking further chain elongation and leaving peptidyl-tRNA in the P site.
  Although protein synthesis in Gram-negative bacilli–and, indeed, mammalian cells–is susceptible to fusidic acid, the antibiotic penetrates poorly into these cells and the spectrum of action is virtually restricted to Gram-positive bacteria, notably staphylococci. ;

• Structure

  Fusidic acid is a 3alpha-hydroxy steroid, an 11alpha-hydroxy steroid, a sterol ester, a steroid acid, an alpha,beta-unsaturated monocarboxylic acid and a steroid antibiotic. It is a conjugate acid of a fusidate. Fusidic acid has an asteroid-type structure, as do some other antibiotics produced by fungi, but does not possess any steroid activity. The structure is thought to be responsible for the steroid-like high penetration. ;

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