Smee D F, Matthews T R
Antimicrob Agents Chemother. 1986 Jul;30(1):117-21. doi: 10.1128/AAC.30.1.117.
The metabolism of ribavirin to its mono-, di-, and triphosphate derivatives was examined in uninfected and respiratory syncytial virus-infected cells. The degree of phosphorylation was dose dependent upon extracellular ribavirin concentration. The major species formed was the triphosphate, with mono- and diphosphates being approximately 12 and 4% of the triphosphate, respectively. Amounts of triphosphate formed in infected cells were up to 2.6-fold greater than those in uninfected cells. Upon drug removal, ribavirin triphosphate degradation was very rapid, with decay half-lives of 70 to 100 min. Actinomycin D inhibited triphosphate production and also neutralized the antiviral effect of ribavirin.
在未感染和呼吸道合胞病毒感染的细胞中检测了利巴韦林向其一磷酸、二磷酸和三磷酸衍生物的代谢情况。磷酸化程度取决于细胞外利巴韦林的浓度。形成的主要产物是三磷酸形式,一磷酸和二磷酸分别约占三磷酸的12%和4%。感染细胞中形成的三磷酸量比未感染细胞中的多2.6倍。去除药物后,利巴韦林三磷酸的降解非常迅速,衰变半衰期为70至100分钟。放线菌素D抑制三磷酸的产生,也中和了利巴韦林的抗病毒作用。