Pechère J C
Département de Génétique et Microbiologie, CMU, Genève, Suisse.
Pathol Biol (Paris). 1995 Jun;43(6):483-7.
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.
阿奇霉素在内酯环的9位含有一个氮原子，该氮原子提供了第二个质子化位点。因此，与红霉素相比，阿奇霉素在胃环境中更稳定，具有更好的消化吸收和消化耐受性，表现出更高的细胞内蓄积，这导致血清和组织半衰期延长，从而可以简化治疗方案。还据推测，对革兰氏阴性菌如流感嗜血杆菌和卡他莫拉菌的活性提高也源于相同的结构特性。
