Cytochrome P-450 metabolic-intermediate complex formation and induction by macrolide antibiotics; a new class of agents

Xenobiotica. 1982 Nov;12(11):687-99. doi: 10.3109/00498258209038944.


1. By several criteria, macrolide antibiotics constitute a new class of nitrogenous cytochrome P-450 metabolic-intermediate complex-forming compounds. 2. Macrolide antibiotic metabolic-intermediate complexes are only formed in livers induced with phenobarbital or with the macrolide antibiotics themselves. The extent of metabolic-intermediate complex formation in microsomes from phenobarbital-induced rats is lower than that seen for members of the amphetamine and SKF 525-A classes of compounds. 3. Cytochrome P-450 induced by macrolide antibiotics, of which troleandomycin is the most potent, is extensively sequestered as a metabolic intermediate complex in vivo. 4. Cytochrome P-450 induced by troleandomycin differs, using several criteria, from those induced by phenobarbital, beta-naphthoflavone or SKF 525-A, and those present in uninduced rats.

MeSH terms

  • Animals
  • Anti-Bacterial Agents / metabolism*
  • Anti-Bacterial Agents / pharmacology
  • Benzoflavones / pharmacology
  • Cytochrome P-450 Enzyme System / metabolism*
  • Enzyme Induction / drug effects
  • Female
  • In Vitro Techniques
  • Male
  • Microsomes, Liver / metabolism
  • Phenobarbital / pharmacology
  • Proadifen / pharmacology
  • Rabbits
  • Rats
  • Rats, Inbred Strains
  • Species Specificity
  • Troleandomycin / pharmacology
  • beta-Naphthoflavone


  • Anti-Bacterial Agents
  • Benzoflavones
  • beta-Naphthoflavone
  • Cytochrome P-450 Enzyme System
  • Proadifen
  • Troleandomycin
  • Phenobarbital