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Valacyclovir is a nucleoside analogue antiviral agent and prodrug of acyclovir which is used in therapy of herpes simplex and varicella-zoster virus infections. Valacyclovir val ay sye' kloe vir, which is sometimes spelled valaciclovir, is an acyclic purine nucleoside analogue, the L-valyl ester prodrug of acyclovir that once absorbed, is rapidly converted to acyclovir, its active moiety. Valacyclovir has greater oral bioavailability than acyclovir and has similar activity against herpes viruses, including herpes simplex 1 and 2, cytomegalovirus, Epstein-Barr virus and varicella-zoster. Once converted to acyclovir, the drug is phosphorylated intracellularly by viral kinases. The resultant triphosphate competes with guanosine for incorporation into viral DNA, blocking viral DNA polymerase activity. Because its activation requires the presence of viral kinases, valacyclovir is only activated in virally infected cells. Valacyclovir is indicated for therapy of mucocutaneous and genital herpes simplex infections, both type 1 and 2 and for herpes zoster.
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