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曲伐沙星对刚地弓形虫具有活性。

Trovafloxacin is active against Toxoplasma gondii.

作者信息

Khan A A, Slifer T, Araujo F G, Remington J S

机构信息

Department of Immunology and Infectious Diseases. Palo Alto Medical Foundation, California 94301, USA.

出版信息

Antimicrob Agents Chemother. 1996 Aug;40(8):1855-9. doi: 10.1128/AAC.40.8.1855.

Abstract

Drugs currently used for treatment of toxoplasmosis in pregnant women, congenital infections, immunocompromised patients, and patients with the ocular disease are not always effective or may be dangerous to use; therefore, there is a need for more-effective and less-toxic drugs. Recently, we examined a group of fluoroquinolones for in vitro and in vivo activities against Toxoplasma gondii. Among those examined in vitro (ciprofloxacin, fleroxacin, ofloxacin, temafloxacin, and trovafloxacin), only trovafloxacin significantly inhibited intracellular replication of T. gondii without significant toxicity for host cells. In a murine model of acute toxoplasmosis, 100 or 200 mg of trovafloxacin per kg of body weight per day for 10 days protected 100% of infected mice against death. A dose of 50 mg/kg/day protected 90% of the mice, and a dose of 25 mg/kg/day effected prolongation of time to death. The other fluoroquinolones did not have such in vivo activities. These results indicate that trovafloxacin may be useful for treatment of toxoplasmosis in humans.

摘要

目前用于治疗孕妇弓形虫病、先天性感染、免疫功能低下患者以及眼部疾病患者的药物并非总是有效,或者使用起来可能存在危险;因此,需要更有效且毒性更低的药物。最近,我们研究了一组氟喹诺酮类药物对刚地弓形虫的体外和体内活性。在体外研究的药物(环丙沙星、氟罗沙星、氧氟沙星、替马沙星和曲伐沙星)中,只有曲伐沙星能显著抑制弓形虫在细胞内的复制,且对宿主细胞无明显毒性。在急性弓形虫病的小鼠模型中,每天每千克体重给予100或200毫克曲伐沙星,连续给药10天,可使100%的感染小鼠免于死亡。50毫克/千克/天的剂量可保护90%的小鼠,25毫克/千克/天的剂量可延长死亡时间。其他氟喹诺酮类药物没有这种体内活性。这些结果表明,曲伐沙星可能对治疗人类弓形虫病有用。

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Trovafloxacin is active against Toxoplasma gondii.曲伐沙星对刚地弓形虫具有活性。
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