Coppolino Giuseppe, Simeoni Mariadelina, Summaria Chiara, Postorino Maria Concetta, Rivoli Laura, Strazzulla Alessio, Torti Carlo, Fuiano Giorgio
Department of Medical and Surgical Sciences, Unit of Nephrology and Dialysis, University-Hospital "Magna Graecia", Via Michele Torcia, 4, 88100, Catanzaro, Italy,
J Nephrol. 2015 Aug;28(4):393-402. doi: 10.1007/s40620-015-0214-0. Epub 2015 Jun 9.
Tenofovir is a nucleotide acting both as an inhibitor of human immunodeficiency (HIV) reverse transcriptase and as a competitor for hepatitis B virus (HBV) RNA-directed DNA polymerase. Approved worldwide in 2001, tenofovir is used as a component of highly active antiretroviral therapy (HAART) in patients with HIV infection. Since 2008, it has also been indicated for treatment of chronic HBV infection or HIV/HBV co-infection. The aim of the treatment consists in suppressing viral replication, thus reducing hepatic complications and improving patient survival. Furthermore, tenofovir could represent an effective therapeutic option in lamivudine-resistant HBV patients. Tenofovir is eliminated unchanged through urine via glomerular filtration (80%) and proximal tubular secretion (20%). Thus, alterations in renal clearance may interfere with tenofovir pharmacokinetics and systemic drug concentrations, modifying the therapeutic response. Hence, a renal overload of tenofovir in patients with a pre-existing kidney impairment could result in a worsening of renal function. Following a brief introduction on HBV infection and its therapeutic options, we review the latest evidence, to our knowledge, on renal toxicity of tenofovir in HBV patients and on drug management.
替诺福韦是一种核苷酸,它既是人类免疫缺陷病毒(HIV)逆转录酶的抑制剂,也是乙型肝炎病毒(HBV)RNA定向DNA聚合酶的竞争剂。2001年在全球获批,替诺福韦被用作HIV感染患者高效抗逆转录病毒治疗(HAART)的一个组成部分。自2008年以来,它也被用于治疗慢性HBV感染或HIV/HBV合并感染。治疗的目的在于抑制病毒复制,从而减少肝脏并发症并提高患者生存率。此外,替诺福韦可能是拉米夫定耐药的HBV患者的一种有效治疗选择。替诺福韦通过肾小球滤过(80%)和近端肾小管分泌(20%)经尿液以原形排出。因此,肾脏清除率的改变可能会干扰替诺福韦的药代动力学和全身药物浓度,改变治疗反应。因此,已有肾脏损害的患者中替诺福韦的肾脏负荷过重可能会导致肾功能恶化。在对HBV感染及其治疗选择进行简要介绍之后,我们综述了据我们所知关于替诺福韦对HBV患者的肾脏毒性以及药物管理的最新证据。