Walstad R A, Hellum K B
Acta Otolaryngol Suppl. 1984;407:50-4. doi: 10.3109/00016488409124965.
Successful treatment of respiratory tract infections with erythromycin may depend upon adequate penetration of the drug to the site of infection. The delivery of antibiotics into respiratory tract secretions is a simple passive diffusion process along a concentration gradient according to Fick's principle. A number of other factors including physicochemical characteristics of the drug and host defence mechanisms may further modify the tissue penetration. A common feature of penetration studies in respiratory tract infections is the wide range of results. This is due to the numerous variables involved in this kind of study. However, the studies performed at steady state, and after oral administration of erythromycin, show a rapid increase in drug concentrations in adenoid and tonsillar tissue homogenates and sustained levels equal to or higher than in serum. In secretions of the middle ear, paranasal sinuses and bronchiae the penetration and elimination of erythromycin is much slower. The drug levels were equal to--or in some cases even higher than--steady state serum concentrations. Fluctuations, however, were less pronounced. In lung tissue homogenates erythromycin concentrations higher than the serum levels have generally been found. In respiratory tract secretions and tissues the penetration of erythromycin is good. Sufficient levels are reached to inhibit in vitro the growth of most common pathogens involved in respiratory tract infections with the exception of some strains of Haemophilus influenzae.
用红霉素成功治疗呼吸道感染可能取决于药物充分渗透到感染部位。根据菲克原理,抗生素进入呼吸道分泌物是一个沿着浓度梯度的简单被动扩散过程。包括药物的物理化学特性和宿主防御机制在内的许多其他因素可能会进一步改变组织渗透。呼吸道感染渗透研究的一个共同特点是结果范围广泛。这是由于这类研究涉及众多变量。然而,在稳态下以及口服红霉素后进行的研究表明,腺样体和扁桃体组织匀浆中的药物浓度迅速增加,且持续水平等于或高于血清中的水平。在中耳、鼻窦和支气管分泌物中,红霉素的渗透和消除要慢得多。药物水平等于——在某些情况下甚至高于——稳态血清浓度。然而,波动不太明显。在肺组织匀浆中,通常发现红霉素浓度高于血清水平。在呼吸道分泌物和组织中,红霉素的渗透良好。除了一些流感嗜血杆菌菌株外,能达到足够的水平以在体外抑制呼吸道感染中最常见病原体的生长。