Expert Opin Drug Saf. 2012 May;11(3):357-60. doi: 10.1517/14740338.2012.672972. Epub 2012 Mar 15.
Currently, five nucleos(t)ide analogs (NAs) are approved for the treatment of chronic hepatitis B (CHB) infection. They are lamivudine, adefovir dipivoxil, telbivudine, entecavir (ETV) and tenofovir disoproxil fumarate (TDF). Two of them, ETV and TDF, are recommended as first-line treatment options. Their main advantages include excellent tolerability, antiviral potency and a high genetic barrier to resistance within medium duration treatment periods (2 - 6 years). In most patients, NAs need to be administered on a long-term basis. Several studies suggest that NAs long-term administration have been associated with low rates of serious adverse events (AEs), including lactic acidosis, renal function impairment, osteopenia and osteoporosis. Discontinuations due to AEs tended to be low in published randomized clinical trial and in the experience in clinical practice. NAs long-term use appears to be safe and effective; and in patients with advanced liver disease, despite preliminary concerning reports, their short-term use also appears to be safe and effective. Although major AEs are infrequent, they can be initially clinically silent yet lead to serious medical problems, therefore, a proactive surveillance and their prompt management is recommended.
目前，有五种核苷（酸）类似物（NAs）被批准用于治疗慢性乙型肝炎（CHB）感染。它们是拉米夫定、阿德福韦酯、替比夫定、恩替卡韦（ETV）和富马酸替诺福韦二吡呋酯（TDF）。其中两种，ETV 和 TDF，被推荐作为一线治疗选择。它们的主要优点包括良好的耐受性、抗病毒效力和在中程治疗期间（2-6 年）具有很高的遗传耐药屏障。在大多数患者中，NAs 需要长期使用。多项研究表明，NA 的长期使用与严重不良事件（AE）的低发生率相关，包括乳酸酸中毒、肾功能损害、骨密度降低和骨质疏松症。在已发表的随机临床试验和临床实践经验中，因 AE 而停药的比例较低。NA 的长期使用似乎是安全有效的；在晚期肝病患者中，尽管有初步令人担忧的报告，但他们的短期使用似乎也是安全有效的。尽管主要的 AE 并不常见，但它们最初可能在临床上没有症状，但会导致严重的医疗问题，因此建议进行主动监测并及时处理。
