Ganciclovir (injection)
Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]
Overview
Ganciclovir INN /ɡænˈsaɪkləvɪər/ or DHPG (9-(1,3-dihydroxy-2-propoxymethyl)guanine) is an antiviral medication used to treat or prevent cytomegalovirus (CMV) infections. Ganciclovir sodium is marketed under the trade names Cytovene and Cymevene (Roche). Ganciclovir for ocular use is marketed under the trade name Vitrasert (Bausch & Lomb). A prodrug form with improved oral bioavailability (valganciclovir) has also been developed.
Category
Antiviral
US Brand Names
VITRASERT®,ZIRGAN®
FDA Package Insert
Description | Clinical Pharmacology | Microbiology | Indications and Usage | Contraindications | Warnings and Precautions | Adverse Reactions | Drug Interactions | Clinical Studies | Dosage and Administration | How Supplied | Labels and Packages
Mechanism of action
Ganciclovir is a synthetic analogue of 2′-deoxy-guanosine. It is first phosphorylated to ganciclovir monophosphate by a viral kinase encoded by the cytomegalovirus (CMV) gene UL97 during infection. Subsequently, cellular kinases catalyze the formation of ganciclovir diphosphate and ganciclovir triphosphate, which is present in 10-fold greater concentrations in CMV or herpes simplex virus (HSV)-infected cells than uninfected cells.
Ganciclovir triphosphate is a competitive inhibitor of deoxyguanosine triphosphate (dGTP) incorporation into DNA and preferentially inhibits viral DNA polymerases more than cellular DNA polymerases. In addition, ganciclovir triphosphate serves as a poor substrate for chain elongation, thereby disrupting viral DNA synthesis by a second route.