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Valaciclovir (INN) or valacyclovir (USAN) is an antiviral drug used in the management of herpes simplex and herpes zoster (shingles). It is a prodrug, being converted in vivo to aciclovir. It is marketed by GlaxoSmithKline under the trade name Valtrex.
Pharmacology
Mechanism of action
Valaciclovir is a prodrug that is converted by esterases to the active drug aciclovir via hepatic first-pass metabolism. Aciclovir is selectively converted into a monophosphate form by viral thymidine kinase, which is far more effective (3000 times) in phosphorylation than cellular thymidine kinase. Subsequently, the monophosphate form is further phosphorylated into the active triphosphate form, aciclo-GTP, by cellular kinases. Aciclo-GTP is a very potent inhibitor of viral DNA polymerase; it has approximately 100 times higher affinity to viral than cellular polymerase. Its monophosphate form also incorporates into the viral DNA, resulting in chain termination. It has also been shown that the viral enzymes cannot remove aciclo-GMP from the chain, which results in inhibition of further activity of DNA polymerase. Aciclo-GTP is fairly rapidly metabolised within the cell, possibly by cellular phosphatases.Microbiology
Aciclovir, the active metabolite of valaciclovir, is active against most species in the herpesvirus family. In descending order of activity:O'Brien JJ, Campoli-Richards DM. Acyclovir. An updated review of its antiviral activity, pharmacokinetic properties and therapeutic efficacy. Drugs 1989;37(3):233-309. PMID 2653790- Herpes simplex virus type I (HSV-1)
- Herpes simplex virus type II (HSV-2)
- Varicella zoster virus (VZV)
- Epstein-Barr virus (EBV)
- Cytomegalovirus (CMV)
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DrugDigest: Valtrex - Information on dosage, usage, side effects, interactions, and drug comparisons.
Valtrex - Valtrex is indicated for the treatment or suppression of genital herpes for adults with normal immune systems. (Valacyclovir)
Meta Description: [ Genital Herpes information – learn about the herpes virus and treatment options to reduce your number of outbreaks and lower your risk of spreading herpes to a partner. ]
Valtrex - a.k.a. Valacyclovir HCL.
Valtrex ( valcyclovir HCl ) - Contains information about genital herpes and treatment options from Glaxo Wellcome.
Meta Description: [ Genital herpes information from VALTREX, the once-daily herpes medication approved to reduce the number of outbreaks and reduce the risk of spreading in appropriate patients. ]
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