Valganciclovir hydrochloride: Difference between revisions
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Valganciclovir is an L-valyl ester (prodrug) of [[ganciclovir]] that exists as a mixture of two diastereomers. After oral administration, both diastereomers are rapidly converted to [[ganciclovir]] by intestinal and hepatic esterases. [[ganciclovir]] is a synthetic analogue of 2'-[[deoxyguanosine]], which inhibits replication of human CMV in cell culture and in vivo. | Valganciclovir is an L-valyl ester (prodrug) of [[ganciclovir]] that exists as a mixture of two diastereomers. After oral administration, both diastereomers are rapidly converted to [[ganciclovir]] by intestinal and hepatic esterases. [[ganciclovir]] is a synthetic analogue of 2'-[[deoxyguanosine]], which inhibits replication of human CMV in cell culture and in vivo. | ||
In CMV-infected cells [[ganciclovir]] is initially phosphorylated to [[ganciclovir]] monophosphate by the viral protein kinase, pUL97. Further phosphorylation occurs by cellular kinases to produce [[ganciclovir]] triphosphate, which is then slowly metabolized intracellularly (half-life 18 hours). As the phosphorylation is largely dependent on the viral kinase, phosphorylation of [[ganciclovir]] occurs preferentially in virus-infected cells. The virustatic activity of [[ganciclovir]] is due to inhibition of the viral DNA polymerase, pUL54, synthesis by [[ganciclovir]] triphosphate. | In CMV-infected cells [[ganciclovir]] is initially phosphorylated to [[ganciclovir]] monophosphate by the viral protein kinase, pUL97. Further phosphorylation occurs by cellular kinases to produce [[ganciclovir]] triphosphate, which is then slowly metabolized intracellularly (half-life 18 hours). As the phosphorylation is largely dependent on the viral kinase, phosphorylation of [[ganciclovir]] occurs preferentially in virus-infected cells. The virustatic activity of [[ganciclovir]] is due to inhibition of the viral DNA polymerase, pUL54, synthesis by [[ganciclovir]] triphosphate.<ref>{{Cite web | last = |first =|title =http://www.accessdata.fda.gov/drugsatfda_docs/label/2010/021304s008,022257s003lbl.pdf | url =http://www.accessdata.fda.gov/drugsatfda_docs/label/2010/021304s008,022257s003lbl.pdf|publisher =|date = | accessdate = }}</ref> | ||
==References== | ==References== | ||
Revision as of 23:45, 2 January 2014
Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Sheng Shi, M.D. [2]
Overview
Valganciclovir (Valcyte, manufactured by Hoffmann–La Roche, and also known as Cymeval, Valcyt, Valixa, Darilin, Rovalcyte, Patheon, and Syntex) is an antiviral medication used to treat cytomegalovirus infections. As the L-valyl ester of ganciclovir, it is actually a prodrugfor ganciclovir. After oral administration, it is rapidly converted to ganciclovir by intestinal and hepatic esterases.
Category
Antiviral
US Brand Names
VALCYTE®
FDA Package Insert
Description | Clinical Pharmacology | Microbiology | Indications and Usage | Contraindications | Warnings and Precautions | Adverse Reactions | Overdosage | Clinical Studies | Dosage and Administration | Directions For Use | How Supplied | Labels and Packages
Mechanism of Action
Valganciclovir is an L-valyl ester (prodrug) of ganciclovir that exists as a mixture of two diastereomers. After oral administration, both diastereomers are rapidly converted to ganciclovir by intestinal and hepatic esterases. ganciclovir is a synthetic analogue of 2'-deoxyguanosine, which inhibits replication of human CMV in cell culture and in vivo.
In CMV-infected cells ganciclovir is initially phosphorylated to ganciclovir monophosphate by the viral protein kinase, pUL97. Further phosphorylation occurs by cellular kinases to produce ganciclovir triphosphate, which is then slowly metabolized intracellularly (half-life 18 hours). As the phosphorylation is largely dependent on the viral kinase, phosphorylation of ganciclovir occurs preferentially in virus-infected cells. The virustatic activity of ganciclovir is due to inhibition of the viral DNA polymerase, pUL54, synthesis by ganciclovir triphosphate.[1]
References
- ↑ "http://www.accessdata.fda.gov/drugsatfda_docs/label/2010/021304s008,022257s003lbl.pdf" (PDF). External link in
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