Pharmacokinetics of penciclovir after oral administration of its prodrug famciclovir to horses.
Abstract: We investigated the pharmacokinetics of penciclovir after oral administration of its prodrug famciclovir to horses. Following an oral dose of famciclovir at 20 mg/kg, maximum plasma concentrations of penciclovir occurred between 0.75 and 1.5 hr (mean 0.94 + or - 0.38 hr) after dosing and were in the range 2.22 to 3.56 microg/ml (mean 2.87 + or - 0.61 microg/ml). The concentrations of penciclovir declined in a biphasic manner after the peak concentration was attained. The mean half-life of the rapid elimination phase was 1.73 + or - 0.34 hr whereas that of the slow elimination phase was 34.34 + or - 13.93 hr. These pharmacokinetic profiles observed were similar to those of another antiherpesvirus drug, acyclovir, previously reported in horses following oral dosing of its prodrug valacyclovir.
Publication Date: 2009-12-04 PubMed ID: 19959884DOI: 10.1292/jvms.09-0350Google Scholar: Lookup
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- Journal Article
Summary
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The research article explores the reaction of horses to the oral intake of the drug famciclovir, which is converted into its active form, penciclovir, in the body. It delves into the time it takes to reach maximum plasma concentrations and its elimination phase duration.
Research Process
- The research focused on studying the pharmacokinetics of penciclovir, a drug used against the herpes virus, in horses after they are orally administered its prodrug, famciclovir.
- Famciclovir was given orally to the horses at the dose of 20mg/kg.
- The maximum plasma concentrations of penciclovir were then observed to occur between 0.75 and 1.5 hr after dosing.
- The range of the maximum plasma concentrations of penciclovir was between 2.22 and 3.56 microg/ml.
Findings
- The study found that the concentration of penciclovir declined in a biphasic manner after peaking.
- The study noticed a rapid elimination phase with a mean half-life of approximately 1.73 hours. This is the period in which the concentration of the drug decreased rapidly in plasma.
- Following the rapid elimination phase, there was a slow elimination phase which had a mean half-life of approximately 34.34 hours. Here, the concentration of the drug decreased in plasma at a slower pace.
- The pharmacokinetic profiles, the body’s effect on the drug in terms of absorption, distribution, metabolism, and excretion, which were observed in this study, were matched with the profiles of valacyclovir-acyclovir anti-herpes virus drug treatment in horses that was previously reported.
Implications
- The findings imply that the prodrug famciclovir is converted into the active drug penciclovir upon oral administration and absorption.
- The established behavior of the absorption and elimination of penciclovir could be instrumental in determining the appropriate dosage and frequency for horses to effectively alleviate herpes virus symptoms.
Cite This Article
APA
Tsujimura K, Yamada M, Nagata S, Yamanaka T, Nemoto M, Kondo T, Kurosawa M, Matsumura T.
(2009).
Pharmacokinetics of penciclovir after oral administration of its prodrug famciclovir to horses.
J Vet Med Sci, 72(3), 357-361.
https://doi.org/10.1292/jvms.09-0350 Publication
Researcher Affiliations
- Epizootic Research Center, Equine Research Institute, Japan Racing Association, 1400-4 Shiba, Shimotsuke, Tochigi 329-0412, Japan. koji_tsujimura@jra.go.jp
MeSH Terms
- 2-Aminopurine / administration & dosage
- 2-Aminopurine / analogs & derivatives
- 2-Aminopurine / blood
- 2-Aminopurine / pharmacokinetics
- Acyclovir / analogs & derivatives
- Acyclovir / blood
- Acyclovir / pharmacokinetics
- Administration, Oral
- Animals
- Antiviral Agents / blood
- Antiviral Agents / pharmacokinetics
- Area Under Curve
- Famciclovir
- Guanine
- Half-Life
- Herpesviridae Infections / drug therapy
- Herpesviridae Infections / veterinary
- Herpesvirus 1, Equid / drug effects
- Horse Diseases / drug therapy
- Horse Diseases / virology
- Horses
Citations
This article has been cited 2 times.- Ishii H, Shibuya M, Kusano K, Sone Y, Kamiya T, Wakuno A, Ito H, Miyata K, Sato F, Kuroda T, Yamada M, Leung GN. Generic approach for the discovery of drug metabolites in horses based on data-dependent acquisition by liquid chromatography high-resolution mass spectrometry and its applications to pharmacokinetic study of daprodustat.. Anal Bioanal Chem 2022 Nov;414(28):8125-8142.
- Carmichael RJ, Whitfield C, Maxwell LK. Pharmacokinetics of ganciclovir and valganciclovir in the adult horse.. J Vet Pharmacol Ther 2013 Oct;36(5):441-9.
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