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多西环素

Doxycycline.

作者信息

Cunha B A, Sibley C M, Ristuccia A M

出版信息

Ther Drug Monit. 1982;4(2):115-35. doi: 10.1097/00007691-198206000-00001.

Abstract

The chemistry, mode of action, antimicrobial activity, pharmacokinetics, and therapeutic efficacy of doxycycline are reviewed. Doxycycline displays excellent activity against gram-positive and gram-negative aerobic and anaerobic pathogens. The oral absorption of doxycycline is rapid and virtually complete and is not significantly decreased by food. Moreover, serum concentrations of doxycycline following oral and intravenous (i.v.) administration are comparable. Because of the prolonged half-life of doxycycline, once daily administration is possible. Tissue penetration of doxycycline is excellent. Levels within the therapeutic range have been found in most organs and tissues, including kidney, lung, gallbladder, prostate, intestinal tract, myocardium, sinus secretions, tonsil, aqueous humor, and female reproductive tissue. Doxycycline does not accumulate in patients with renal insufficiency and is not removed from the blood to any great extent during hemodialysis. Extensive clinical investigation has shown doxycycline to be highly effective in infections of the respiratory tract, including atypical pneumonias; skin and soft tissue; genitourinary infection including gonorrhea, syphilis, nonspecific urethritis, and prostatitis; intraabdominal infection due to trauma, sepsis, or surgery; and cholera. Evidence also suggests that doxycycline will prove effective in the treatment of Legionnaires' disease. In addition, placebo-controlled clinical trials suggest doxycycline is effective in the prevention of traveler's diarrhea.

摘要

本文综述了多西环素的化学性质、作用方式、抗菌活性、药代动力学和治疗效果。多西环素对革兰氏阳性和革兰氏阴性需氧及厌氧病原体均表现出优异的活性。多西环素口服吸收迅速且几乎完全,食物对其吸收无显著影响。此外,口服和静脉注射多西环素后的血清浓度相当。由于多西环素半衰期较长,每日给药一次即可。多西环素的组织穿透力极佳。在大多数器官和组织中,包括肾脏、肺、胆囊、前列腺、肠道、心肌、鼻窦分泌物、扁桃体、房水和女性生殖组织,均发现其水平处于治疗范围内。肾功能不全患者体内多西环素不会蓄积,血液透析过程中也不会大量清除。广泛的临床研究表明,多西环素在呼吸道感染(包括非典型肺炎)、皮肤和软组织感染、泌尿生殖系统感染(包括淋病、梅毒、非特异性尿道炎和前列腺炎)、因创伤、败血症或手术引起的腹腔内感染以及霍乱的治疗中高度有效。有证据还表明,多西环素在治疗军团病方面将被证明有效。此外,安慰剂对照临床试验表明,多西环素在预防旅行者腹泻方面有效。

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