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Antimicrob Agents Chemother. 2010 Dec;54(12):5399-402. doi: 10.1128/AAC.00840-10. Epub 2010 Sep 20.
Adverse effects have limited the clinical use of telithromycin. Preferential inhibition of the nicotinic acetylcholine receptors (nAChR) at the neuromuscular junction (α3β2 and NMJ), the ciliary ganglion of the eye (α3β4 and α7), and the vagus nerve innervating the liver (α7) could account for the exacerbation of myasthenia gravis, the visual disturbance, and the liver failure seen with telithromycin use. The studies presented here enable the prediction of expected side effects of macrolides in development, such as solithromycin (CEM-101).
不良反应限制了泰利霉素的临床应用。在神经肌肉接头(α3β2 和 NMJ)、眼睫状神经节(α3β4 和 α7)和支配肝脏的迷走神经(α7)中,优先抑制烟碱型乙酰胆碱受体(nAChR),可能导致重症肌无力、视觉障碍和泰利霉素使用时出现的肝衰竭恶化。这里介绍的研究可以预测大环内酯类药物(如 CEM-101)在开发过程中的预期副作用。