[Effect of the molecular structure of azithromycin on pharmacokinetics and the antimicrobial activity].
Azithromycin possesses in position 9 of the lactone cycle a nitrogen atom which provides a second site of protonation. Hence, and compared to erythromycin, azithromycin is more stable in the gastric environment, enjoys improved digestive absorption and improved digestive toleration, displays much higher intracellular accumulation responsible for prolonged serum and tissue half-lives, which allows simplified therapeutic schedules. It is also postulated that improved activity against Gram negative isolates such as H. influenzae and B. catarrhalis results from the same structural particularities.
Département de Génétique et Microbiologie, CMU, Genève, Suisse.
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JC
Pechère
D000900:Anti-Bacterial Agents / Q000494:pharmacology*; D017963:Azithromycin / Q000097:blood / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D004917:Erythromycin / Q000737:chemistry*; D005260:Female; D016905:Gram-Negative Bacterial Infections / Q000188:drug therapy; D006801:Humans; D006863:Hydrogen-Ion Concentration; D066298:In Vitro Techniques; D008297:Male; D014066:Palatine Tonsil / Q000187:drug effects*; D010587:Phagocytosis / Q000502:physiology; D011467:Prostate / Q000187:drug effects*; D014599:Uterus / Q000187:drug effects*
D000900:Anti-Bacterial Agents; D004917:Erythromycin; D017963:Azithromycin
Effet de la structure moléculaire de l'azithromycine sur la pharmacocinétique et l'activité antimicrobienne.