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贝达喹啉的作用机制是什么? 1

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贝达喹啉是一种二芳基喹啉抗生素,用于治疗耐多药结核病(MDR-TB)。它通过抑制结核分枝杆菌的ATP合成酶来发挥作用,从而消耗细菌的能量。与其他抗结核药物不同,贝达喹啉的作用机制使其对耐多药结核分枝杆菌有效。

结核病的背景

结核病(TB)是一种由结核分枝杆菌(MTB)引起的传染病,通常影响肺部和其他身体部位。潜伏性结核病没有症状,但约10%的潜伏感染会发展为活动性疾病,如果不及时治疗,将导致大约一半的患者死亡。活动性TB的典型症状包括慢性咳嗽、含血的痰、发热、盗汗和消瘦。贝达喹啉通过抑制结核分枝杆菌的ATP合成酶,阻断细菌的能量供应,从而发挥抗菌作用。

贝达喹啉的应用

贝达喹啉可用于成人耐多药结核病(MDR-TB)的联合治疗。它通过特异性地抑制结核分枝杆菌的ATP合酶发挥作用,对耐药和非耐药结核分枝杆菌均有效。动物实验和临床试验证实了贝达喹啉对结核的有效性和安全性。贝达喹啉的最低抑菌浓度(MIC)为0.002-0.06μg/ml,对结核分枝杆菌具有抑制作用。

参考文献

[1]. Jang JC, et al. Bedaquiline susceptibility test for totally drug-resistant tuberculosis Mycobacterium tuberculosis. J Microbiol. 2017 Apr 20.

[2]. Pang Y, et al. In Vitro Activity of Bedaquiline against Nontuberculous Mycobacteria in China. Antimicrob Agents Chemother. 2017 Apr 24;61(5).

[3]. Chahine EB, et al. Bedaquiline: a novel diarylquinoline for multidrug-resistant tuberculosis. Ann Pharmacother. 2014 Jan;48(1):107-15.

[4]. "Bedaquiline Fumarate". The American Society of Health-System Pharmacists. Archived from the original on 20 December 2016. Retrieved 8 December 2016.

[5]. Diacon AH, Pym A, Grobusch M, et al. "The diarylquinoline TMC207 for multidrug-resistant tuberculosis". N Engl J Med. 360(23):2397–405.

[6]. "Bedaquiline". Archived from the original on 20 May 2013. Retrieved 28 April 2014.

[7]. "Sirturo: Clinical Pharmacology". Archived from the original on 28 February 2015. Retrieved 28 April 2014.

[8]. The selection and use of essential medicines: Twentieth report of the WHO Expert Committee 2015 (including 19th WHO Model List of Essential Medicines and 5th WHO Model List of Essential Medicines for Children) (PDF). World Health Organization. 2015. p.vii, 29. ISBN 9789241209946. Archived (PDF) from the original on 20 December 2016. Retrieved 10 December 2016.

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