Valacyclovir: Difference between revisions
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==US Brand Names== | ==US Brand Names== | ||
VALTREX<sup>®</sup> | VALTREX<sup>®</sup>, VALACYCLOVIR<sup>®</sup>, VALACYCLOVIR HYDROCHLORIDE<sup>®</sup> | ||
==FDA Package Insert== | ==FDA Package Insert== | ||
Revision as of 19:34, 5 January 2014
Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Sheng Shi, M.D. [2]
Overview
Valaciclovir (INN) or valacyclovir (USAN) is an antiviral drug used in the management of herpes simplex, herpes zoster (shingles), and herpes B. It is a prodrug, being converted [in vivo] error: {{lang}}: text has italic markup (help) to aciclovir. It is marketed by GlaxoSmithKline under the trade names Valtrex and Zelitrex. Valaciclovir has been available as a generic drug in the U.S. since November 25, 2009.[1]
Category
Antiviral
US Brand Names
VALTREX®, VALACYCLOVIR®, VALACYCLOVIR HYDROCHLORIDE®
FDA Package Insert
Description | Clinical Pharmacology | Microbiology | Indications and Usage | Contraindications | Warnings and Precautions | Adverse Reactions | Overdosage | Clinical Studies | Dosage and Administration | How Supplied | Labels and Packages
Mechanism of Action
Valacyclovir is a nucleoside analogue DNA polymerase inhibitor. Valacyclovir hydrochloride is rapidly converted to acyclovir which has demonstrated antiviral activity against HSV types 1 (HSV─1) and 2 (HSV─2) and VZV both in cell culture and in vivo.
The inhibitory activity of acyclovir is highly selective due to its affinity for the enzyme thymidine kinase (TK) encoded by HSV and VZV. This viral enzyme converts acyclovir into acyclovir monophosphate, a nucleotide analogue. The monophosphate is further converted into diphosphate by cellular guanylate kinase and into triphosphate by a number of cellular enzymes. In biochemical assays, acyclovir triphosphate inhibits replication of herpes viral DNA.
This is accomplished in 3 ways: 1) competitive inhibition of viral DNA polymerase, 2) incorporation and termination of the growing viral DNA chain, and 3) inactivation of the viral DNA polymerase. The greater antiviral activity of acyclovir against HSV compared with VZV is due to its more efficient phosphorylation by the viral TK.
References
- ↑ Ahmed, Rumman (2009-11-27). "Ranbaxy Launches Generic Valtrex in U.S." The Wall Street Journal. Retrieved 2010-01-16.