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JAC Advance Access published online on May 12, 2004
Journal of Antimicrobial Chemotherapy, doi:10.1093/jac/dkh244
© 2004 by The British Society for Antimicrobial Chemotherapy
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Leading article

Pharmacokinetics of valaciclovir

Conan MacDougall 1 B. Joseph Guglielmo 1*

1 Department of Clinical Pharmacy, School of Pharmacy, University of California, San Francisco, CA, USA

* To whom correspondence should be addressed. E-mail: bjg{at}itsa.ucsf.edu.


  Abstract

While active against Herpesviridae, oral aciclovir is limited by low and inconsistent bioavailability. Modification of aciclovir by valine esterification, producing valaciclovir, results in significant increases in systemic aciclovir plasma levels. The exact mechanism of increased absorption with valaciclovir is not fully determined but probably involves intestinal dipeptide transporters, followed by rapid ester hydrolysis in the small intestine and liver. The enhanced pharmacokinetics of valaciclovir have translated into improvements in clinical efficacy and patient convenience.

Key Words: Keywords: herpesviruses, bioavailability, absorption, aciclovir


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