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轻度慢性阻塞性肺疾病急性加重期时地红霉素和红霉素的肺内浓度

Pulmonary concentrations of dirithromycin and erythromycin during acute exacerbation of mild chronic obstructive pulmonary disease.

作者信息

Matera M G, Tufano M A, Polverino M, Rossi F, Cazzola M

机构信息

Istituto di Farmacologia e Tossicologia, Seconda Università Napoletana, Napoli, Italy.

出版信息

Eur Respir J. 1997 Jan;10(1):98-103. doi: 10.1183/09031936.97.10010098.

Abstract

We compared the concentrations of dirithromycin and erythromycin at steady state in serum and the intrapulmonary region in patients suffering from acute exacerbation of mild chronic obstructive pulmonary disease. Twenty patients received dirithromycin, 500 mg given orally once daily for five consecutive days. The other 20 patients were treated with erythromycin base, which was administered orally four times daily at a total daily dose of 1000 mg for seven days. All patients were divided into eight groups, with five subjects in each group, according to sampling times (2, 4, 8, and hrs after the last dose) and treatment. After the erythromycin treatment mean serum concentrations were higher than those of dirithromycin treatment mean serum concentrations were higher than those of dirithromycin for upto 4 hours, but they were undetectable 24 hours after the last dose. At all time periods, the concentrations of dirithromycin in bronchial secretion, bronchial mucosa and epithelial lining fluid were greater than the concentration in serum. Concentrations of erythromycin were always lower than those of dirithromycin in the explored pulmonary sites. Our data demonstrated that a five day course of 500 mg of dirithromycin once daily induced higher concentrations and longer persistence in the various potential sites of pulmonary infection than a seven day course of 250 mg of erythromycin every 6 hrs. The shorter duration of therapy and the once daily dosing with good efficacy against common respiratory pathogens would be advantageous for patients and would be likely to promote better patient compliance and acceptability.

摘要

我们比较了患有轻度慢性阻塞性肺疾病急性加重期患者血清和肺内区域中地红霉素和红霉素的稳态浓度。20名患者接受地红霉素治疗,每日口服500mg,连续服用5天。另外20名患者接受红霉素碱治疗,每日口服4次,总日剂量为1000mg,共7天。根据采样时间(最后一剂后2、4、8和小时)和治疗情况,将所有患者分为8组,每组5名受试者。红霉素治疗后,平均血清浓度在长达4小时内高于地红霉素治疗后的平均血清浓度,但在最后一剂后24小时检测不到。在所有时间段,支气管分泌物、支气管黏膜和上皮衬液中地红霉素的浓度均高于血清中的浓度。在探索的肺部部位,红霉素的浓度始终低于地红霉素。我们的数据表明,与每6小时服用250mg红霉素共7天的疗程相比,每日一次服用500mg地红霉素共5天的疗程在肺部感染的各个潜在部位诱导出更高的浓度和更长的持续时间。较短的治疗疗程和每日一次给药且对常见呼吸道病原体有良好疗效,对患者有利,可能会提高患者的依从性和接受度。

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