替诺福韦:核苷酸管理模拟人类免疫缺陷病毒感染。
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安东尼奥由于T, Park-Wyllie LY,曾
替诺福韦:核苷酸管理模拟人类免疫缺陷病毒感染。
药物治疗。2003年1月;23 (1):29-43。
- PubMed ID
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12523458 (在PubMed]
- 文摘
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替诺福韦disoproxil延胡索酸酯,无环核苷酸磷酸腺苷的模拟,是最近的抗逆转录病毒阿森纳。转换后替诺福韦二酯水解,随后由细胞酶磷酸化形成主动替诺福韦二磷酸抗逆转录病毒活动是必要的。初步数据显示,替诺福韦司他夫定的是安全和有效的,当你给结合拉米夫定,依法韦伦antiretroviral-naive患者的治疗。在antiretroviral-experienced患者中,泰诺福韦的稳定背景抗逆转录病毒疗法导致大约0.6 log10拷贝/毫升减少病毒载量相对于安慰剂。延长随访表明,这种病毒可能是持久的。体外,重组人类免疫缺陷病毒(HIV)表达K65R突变显示3-4-fold增加50%抑制浓度的替诺福韦与野生型相比。体内,这种突变到目前为止似乎很少发生病毒学反应和相关变量。响应率,替诺福韦随胸苷的数量和模式模拟突变出现在开始治疗之前用这个代理。替诺福韦在患者似乎是一个良好的代理进行预处理和先进的疾病。主要副作用是胃肠道出现在自然和包括恶心、呕吐和腹泻。 In animals, osteomalacia and nephrotoxicity have occurred with tenofovir at exposures much higher than those observed in humans. Although no patient had to discontinue therapy as a result of elevated creatinine levels or hypophosphatemia through 58 weeks of treatment, the toxicities associated with long-term tenofovir therapy in humans are unknown. Concomitant administration of tenofovir and didanosine increases the area under the concentration-time curve of the latter by 44-60%; monitoring for signs and symptoms of didanosine toxicity is recommended. The approved dosage of tenofovir is 300 mg (one tablet) once/day with meals. Given the ease of administration and relative safety from the perspectives of adverse effects and drug interactions, tenofovir has the potential to assume a large role in the treatment of patients with HIV infection.
beplay体育安全吗DrugBank数据引用了这篇文章
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药物 酶 类 生物 药理作用 行动 替诺福韦disoproxil 腺苷酸激酶2,线粒体 蛋白质 人类 未知的底物细节 替诺福韦disoproxil 腺苷酸激酶4,线粒体 蛋白质 人类 未知的底物细节 - 药物反应
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反应 细节
