Clarithromycin

Clarithromycin is a macrolide antibiotic that functions by inhibiting bacterial protein synthesis. Clarithromycin binds to the 50S subunit of the bacterial ribosome, preventing peptide chain elongation and thereby suppressing bacterial growth^[1]. Clarithromycin is used to treat upper respiratory tract infections, such as community-acquired pneumonia, acute exacerbation of chronic bronchitis, and sinusitis^[2]. Clarithromycin also has anti-inflammatory and immunomodulatory properties, making it a potential treatment for certain non-infectious diseases like diffuse panbronchiolitis^[3]. Clarithromycin shows promise in combating cancer development and resistance^[4]

In vitro, treatment of rat hippocampal CA3 pyramidal neurons with Clarithromycin (3–300μM) significantly increases neuronal excitability in a dose-dependent manner. Clarithromycin can inhibit the amplitude and frequency of GABA-mPSCs^[5]. When combined with Ceftazidime (0.5MIC), Clarithromycin (0.5–2MIC) significantly enhances the bactericidal effect of Ceftazidime against Pseudomonas aeruginosa^[6].

In vivo, daily intraperitoneal injections of Clarithromycin (100mg/kg) in combination with Cisplatin (5mg/kg) are administered to BALB/c nude mice with ovarian tumor xenografts. Clarithromycin significantly reduces tumor volume and weight and enhances the antitumor effect of Cisplatin^[7]. Daily intraperitoneal injections of Clarithromycin (20mg/kg) are given to 5- to 6-week-old Cricetidae. Clarithromycin significantly reduces arthritis onset and shortens recovery time induced by Borrelia burgdorferi^[8].

References:
[1] Schlossberg D. Azithromycin and clarithromycin. Med Clin North Am. 1995 Jul;79(4):803-15.
[2] Williams KN, Bishai WR. Clarithromycin extended-release in community-acquired respiratory tract infections. Expert Opin Pharmacother. 2005 Dec;6(16):2867-76.
[3] Ando M, Ono T, Usagawa Y, et al. The development of diffuse panbronchiolitis during the treatment with long-term, low-dose clarithromycin for chronic sinusitis. J Infect Chemother. 2019 Feb;25(2):147-150.
[4] Petroni G, Bagni G, Iorio J, et al. Clarithromycin inhibits autophagy in colorectal cancer by regulating the hERG1 potassium channel interaction with PI3K. Cell Death Dis. 2020 Mar 2;11(3):161.
[5] Bichler EK, Elder CC, García PS. Clarithromycin increases neuronal excitability in CA3 pyramidal neurons through a reduction in GABAergic signaling. J Neurophysiol. 2017 Jan 1;117(1):93-103.
[6] Bui KQ, Banevicius MA, Nightingale CH, et al. In vitro and in vivo influence of adjunct clarithromycin on the treatment of mucoid Pseudomonas aeruginosa. J Antimicrob Chemother. 2000 Jan;45(1):57-62.
[7] Zhou B, Xia M, Wang B, et al. Clarithromycin synergizes with cisplatin to inhibit ovarian cancer growth in vitro and in vivo. J Ovarian Res. 2019 Nov 8;12(1):107.
[8] Alder J, Mitten M, Jarvis K, et al. Efficacy of clarithromycin for treatment of experimental Lyme disease in vivo. Antimicrob Agents Chemother. 1993 Jun;37(6):1329-33.

Clarithromycin是一种大环内酯类抗生素，通过抑制细菌蛋白质合成发挥作用，与细菌核糖体的50S亚基结合，阻止肽链延长，从而抑制细菌生长^[1]。Clarithromycin可用于治疗社区获得性肺炎、慢性支气管炎急性发作和鼻窦炎等上呼吸道感染^[2]。Clarithromycin具有抗炎和免疫调节作用，可用于治疗某些非感染性疾病，如弥漫性泛细支气管炎^[3]。Clarithromycin还具有对抗癌症发展和耐药的潜力^[4]。

在体外，Clarithromycin（3–300μM）处理大鼠海马CA3区锥体神经元，显著增加神经元的兴奋性，且呈剂量依赖性效应。Clarithromycin可抑制GABA-mPSCs的幅度和频率 ^[5]。Clarithromycin（0.5–2MIC）与Ceftazidime（0.5MIC）联合处理铜绿假单胞菌，Clarithromycin显著增强Ceftazidime杀菌效果^[6]。

在体内，Clarithromycin（100mg/kg）联合Cisplatin（5mg/kg）每天一次腹腔注射，用于处理卵巢肿瘤异种移植BALB/c裸鼠。Clarithromycin显著减少了卵巢肿瘤的体积和重量，并增强了Cisplatin的抗肿瘤效果^[7]。Clarithromycin（20mg/kg）每日一次腹腔注射，用于处理5至6周龄的Cricetidae。Clarithromycin显著减少了由Borrelia burgdorferi诱导的关节炎发作，并缩短了恢复时间^[8]。