Peyrière H, Branger B, Bengler C, Vécina F, Pinzani V, Hillaire-Buys D, Blayac J P
Centre régional de pharmacovigilance, hôpital Saint-Charles, CHU, 300, rue Auguste-Broussonnet, 34295 Montpellier, France. je;eme[
Rev Med Interne. 2001 Mar;22(3):297-303. doi: 10.1016/s0248-8663(00)00332-5.
We report three cases of neurotoxicity in patients with renal failure, treated with Zelitrex (valacyclovir).
The patients are two women and a man, aged 76 +/- 4.6 years, who presented acute mental confusion during a treatment with valacyclovir. In two cases, the patients previously had altered renal function and were under peritoneal dialysis. In the last case, the patient had simultaneous neurotoxicity and acute renal failure. After the discontinuation of the drug, the outcome was favourable in all cases.
Our cases focus attention on the possible neurotoxicity of valacyclovir, which is an amino acid ester prodrug of acyclovir, rapidly and almost completely hydrolysed to acyclovir prior to systemic exposure. The bioavailability of valacyclovir is 54% compared to approximately 20% for oral acyclovir and may account for unexpected overdoses, which may lead to serious neurological toxicity.
我们报告了3例肾衰竭患者使用Zelitrex（伐昔洛韦）治疗后出现神经毒性的病例。
患者为2名女性和1名男性，年龄76±4.6岁，在接受伐昔洛韦治疗期间出现急性精神错乱。其中2例患者先前肾功能已改变，正在接受腹膜透析。最后1例患者同时出现神经毒性和急性肾衰竭。停药后，所有病例预后良好。
我们的病例使人们关注伐昔洛韦可能存在的神经毒性，伐昔洛韦是阿昔洛韦的氨基酸酯前药，在全身暴露前迅速且几乎完全水解为阿昔洛韦。伐昔洛韦的生物利用度为54%，而口服阿昔洛韦约为20%，这可能导致意外过量用药，进而可能引发严重的神经毒性。
