Erythromycin lactobionate

Erythromycin lactobionate is a water-soluble ester derivative of erythromycin and belongs to the macrolide antibiotics^[1]. Erythromycin lactobionate has a broad spectrum of antibacterial activity, effective against Streptococcus pneumoniae, Streptococcus pyogenes, Staphylococcus aureus, and some atypical pathogens such as Mycoplasma pneumoniae and Chlamydia pneumoniae^[2]. The mechanism of action of Erythromycin lactobionate involves binding to the 50S subunit of the bacterial ribosome, inhibiting protein synthesis, and thus exerting a bacteriostatic effect^[3]. Due to Erythromycin lactobionate good water solubility, Erythromycin lactobionate is commonly used for intravenous or intramuscular injection, especially for patients who cannot take oral medications. Additionally, Erythromycin lactobionate is used in ophthalmic and otic preparations^[4]

In vitro, Erythromycin lactobionate (2.5, 5.0, 25mg/mL) treatment of the rat skeletal muscle cell line (L6) for 1 hour can cause endoplasmic reticulum dilation and cytoplasmic bubbling, and even extensive cytoplasmic membrane damage^[5]. Erythromycin lactobionate (10-300µM) can significantly inhibit neurogenic and drug-induced contractions of the longitudinal and circular muscles of the guinea pig small intestine^[6].

In vivo, Erythromycin lactobionate (50mg/kg and 100mg/kg) administered intraperitoneally twice daily for 14 days in specific pathogen-free mice significantly increased the survival rate of mice infected with Pseudomonas aeruginosa^[7]. A single subcutaneous injection of Erythromycin lactobionate (50mg/kg) in middle cerebral artery occlusion (MCAO) rat models significantly reduced infarct volume and edema index and improved neurological deficit scores^[8].

References:
[1] Periti P, Mazzei T, Mini E, et al. Adverse effects of macrolide antibacterials. Drug Saf. 1993 Nov;9(5):346-64.
[2] Brittain DC. Erythromycin. Med Clin North Am. 1987 Nov;71(6):1147-54.
[3] Saltzman L, Apirion D. Binding of erythromycin to the 50S ribosomal subunit is affected by alterations in the 30S ribosomal subunit. Mol Gen Genet. 1976 Feb 2;143(3):301-6.
[4] Tschida SJ, Guay DR, Straka RJ, et al. QTc-interval prolongation associated with slow intravenous erythromycin lactobionate infusions in critically ill patients: a prospective evaluation and review of the literature. Pharmacotherapy. 1996 Jul-Aug;16(4):663-74.
[5] Laska DA, Williams PD, White SL, et al. In vitro correlation of ultrastructural morphology and creatine phosphokinase release in L6 skeletal muscle cells after exposure to parenteral antibiotics. In Vitro Cell Dev Biol. 1990 Apr;26(4):393-8.
[6] Minocha A, Galligan JJ. Erythromycin inhibits contractions of nerve-muscle preparations of the guinea pig small intestine. J Pharmacol Exp Ther. 1991 Jun;257(3):1248-52.
[7] Hirakata Y, Kaku M, Tomono K, et al. Efficacy of erythromycin lactobionate for treating Pseudomonas aeruginosa bacteremia in mice. Antimicrob Agents Chemother. 1992 Jun;36(6):1198-203.
[8] Katayama Y, Inaba T, Nito C, et al. Neuroprotective effects of erythromycin on ischemic injury following permanent focal cerebral ischemia in rats. Neurol Res. 2016 Mar;38(3):275-84.

Erythromycin lactobionate是红霉素的水溶性酯衍生物，属于大环内酯类抗生素^[1]。Erythromycin lactobionate具有广泛的抗菌谱，对肺炎链球菌、化脓性链球菌、金黄色葡萄球菌以及一些非典型病原体如肺炎支原体和肺炎衣原体等均有效^[2]。Erythromycin lactobionate的作用机制是与细菌核糖体的50S亚基结合，抑制蛋白质合成，从而发挥抑菌作用^[3]。由于Erythromycin lactobionate的水溶性好，常用于静脉或肌肉注射给药，尤其适用于不能口服药物的患者，此外，Erythromycin lactobionate还用于眼科和耳科制剂中^[4]。

在体外，Erythromycin lactobionate（2.5、5.0、25mg/mL）处理大鼠骨骼肌细胞系（L6）1小时，Erythromycin lactobionate可引起内质网扩张和细胞质起泡，甚至是广泛的细胞质膜损伤^[5]。Erythromycin lactobionate（10-300μM）可显著抑制豚鼠小肠纵肌和环肌神经介导和药物诱导收缩^[6]。

在体内，Erythromycin lactobionate（50mg/kg和100mg/kg）每天两次腹腔注射，用于处理特定病原体自由小鼠，持续14天。Erythromycin lactobionate显著提高了感染铜绿假单胞菌（Pseudomonas aeruginosa）小鼠的存活率^[7]。Erythromycin lactobionate（50mg/kg）单次皮下注大脑中动脉闭塞（MCAO）大鼠模型，Erythromycin lactobionate显著降低降低梗死体积、水肿指数，并改善神经功能缺损评分^[8]。