valgansiklovir适应症

Valganciclovir hydrochloride tablets () are the levalyl ester (prodrug) of ganciclovir. After oral administration, it is rapidly converted into ganciclovir by esterases in the small intestine and liver. Ganciclovir is a synthetic 2’-deoxyguanosine monophosphate analog that inhibits herpesvirus replication in vitro and in vivo. Susceptible human viruses include human cytomegalovirus (HCMV), herpes simplex virus-1 and herpes simplex virus-2 (HSV-1, HSV-2), human herpesvirus-6, 7, 8 (HHV-6, 7, 8), Epstein-Barr virus, varicella-zoster virus (VZV), and hepatitis B virus. 

In cells infected by cytomegalovirus (CMV), ganciclovir is first phosphorylated by the viral protein kinase UL97 into ganciclovir monophosphate, and then further phosphorylated by intracellular protein kinases into ganciclovir triphosphate, and then slowly metabolized within the cell. After removal of extracellular ganciclovir, the observed half-life of ganciclovir in HSV- or HCMV-infected cells was 18 hours and 6 to 24 hours, respectively. Since the phosphorylation process relies heavily on viral protein kinases, ganciclovir phosphorylation occurs preferentially in virus-infected cells. Ganciclovir inhibits viral activity mainly by inhibiting the synthesis of viral DNA: (a) Competitively inhibits viral DNA polymerase, preventing deoxyguanosine triphosphate from binding to DNA; (b) Ganciclovir triphosphate binds to viral DNA to terminate or limit the elongation of the viral DNA chain. 

Valganciclovir Hydrochloride Tablets (valgansiklovir) Indications: Valganciclovir Hydrochloride Tablets (valgansiklovir) are suitable for the treatment of cytomegalovirus (CMV) retinitis in patients with acquired immunodeficiency syndrome (AIDS), and Valganciclovir Hydrochloride Tablets () are suitable for the prevention of CMV infection in high-risk solid organ transplant patients.