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[Valaciclovir].

B Lebrun-Vignes1

  • 1Service de Pharmacologie, Centre Régional de Pharmacovigilance, Groupe Hospitalier Pitié-Salpêtrière, 47, boulevard de l'Hôpital, 75013 Paris, France. benedicte.lebrun-vignes@psl.ap-hop-paris.fr

Annales De Dermatologie Et De Venereologie
|July 19, 2002
PubMed
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Valaciclovir, an oral prodrug of acyclovir, demonstrates superior bioavailability for treating herpes virus infections. It is effective for genital herpes, shingles, and preventing cytomegalovirus infections, with good tolerance but potential neurological side effects at high doses.

Area of Science:

  • Pharmacology and Virology
  • Antiviral Drug Development

Background:

  • Valaciclovir is an oral prodrug of acyclovir, designed to enhance oral bioavailability.
  • Its antiviral efficacy is attributed to the active metabolite, acyclovir, primarily targeting herpes viruses.

Purpose of the Study:

  • To evaluate the pharmacokinetic profile and therapeutic efficacy of valaciclovir compared to acyclovir.
  • To assess valaciclovir's effectiveness in various herpes virus infections and patient populations.

Main Methods:

  • Pharmacokinetic studies in healthy volunteers, HIV-infected individuals, elderly patients, and patients with hepatic or renal impairment.
  • Clinical trials comparing valaciclovir to acyclovir for treating first-episode and recurrent genital herpes, herpes zoster, and preventing cytomegalovirus (CMV) infections.

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Main Results:

  • Valaciclovir significantly increases acyclovir bioavailability (3-5 fold) compared to oral acyclovir.
  • Equivalent efficacy to acyclovir in treating genital herpes, with simpler dosing regimens.
  • Effective in preventing post-herpetic neuralgia and CMV infections in immunocompromised patients.
  • Dose adjustment is necessary for renal function, but not hepatic failure.

Conclusions:

  • Valaciclovir offers improved oral bioavailability and convenient dosing for herpes virus infections.
  • It is effective in treating genital herpes, preventing recurrences, and managing herpes zoster.
  • Valaciclovir is also indicated for CMV prophylaxis in specific immunocompromised populations.
  • Generally good tolerance, with neurological side effects noted at high doses.