口服抗病毒新药——缬更昔洛韦

A new oral antiviral drug——valganciclovir

缬更昔洛韦 (valganciclovir)是抗病毒药更昔洛韦的前体药物 ,用于治疗AIDS病人发生的巨细胞病毒 (CMV)视网膜炎。缬更昔洛韦口服后迅速吸收 ,并水解为更昔洛韦 ,其口服给药的生物利用度较高 (60 % )。试验表明 ,口服缬更昔洛韦 (90 0mg)与静脉注射更昔洛韦 (5mg·kg-1) ,bid,3wk后改为 qd ,治疗 1 60例AIDS病人发生的CMV视网膜炎有相同疗效 ,且耐受性相似。缬更昔洛韦维持治疗中最常见的不良反应为中性粒细胞减少症、贫血、胃肠道反应 (腹泻、恶心、呕吐 )、发热。

Valganciclovir is a prodrug of ganciclovir which has been developed for the treatment of cytomegalovirus(CMV) retinitis in patients with AIDS. Oral valganciclovir is rapidly absorbed and hydrolysed to ganciclovir. The bioavailab ility of oral valganciclovir is higher. A single, randomised, nonblind study ind icated that oral valganciclovir(900 mg, bid for 3 wk then 900 mg, qd) and intrav enous ganciclovir(5 mg·kg -1 , bid for 3 wk then 5 mg·kg -1 , qd) wer e equally effective in the treatment of newly diagnosed CMV retinitis in 160 patients with AIDS, and wi th similar tolerability profile. During maintenance therapy with valganciclovir, the most commnly reported adverse reactions included neutropenia, anemia, gastr ointestinal(including diarrhoea, nausea, and vomiting), fever, headache, and ins omnia.