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Famciclovir/Penciclovir

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Antiviral Chemotherapy 5

Part of the book series: Advances in Experimental Medicine and Biology ((AEMB,volume 458))

Abstract

Since the early 1980’s, the gold standard for treatment for both varicella zoster (VZV) and herpes simplex virus (HSV-1, HSV-2) infections has been acyclovir. In general, the clinical significance of acyclovir’s impact on clinical outcomes has been directly proportional to the severity of the natural history of disease. Unfortunately, acyclovir’s limitations are governed by poor oral absorption with a bioavailability of about 15% along with maintenance of plasma antiviral activity in accordance with a short plasma T1/2 of 2.5 hours. Accordingly, novel approaches to address these limitations were required. Fam-ciclovir is the oral prodrug of the antiviral nucleoside deoxyguanosine analog, penciclovir. Famciclovir is characterized by its high rate of absorption and rapid conversion to the active compound, penciclovir. Penciclovir triphosphate, the active intracellular nucleotide has a prolonged intracellular T1/2. Studies performed to date have shown these agents to be both effective and safe and in most cases, more conveniently dosed compared with acyclovir. Famciclovir has shown significant benefits in both active treatment and suppression of genital herpes infections in normal and immunocompromised hosts. Moreover, in the US, the currently approved dosing regimen of famciclovir for the treatment of herpes zoster (shingles) is 500 mg tid for 7 days, while for episodic treatment of recurrent genital herpes, it is 125 mg bid for 5 days.1 Famciclovir is also effective for treatment of first episode genital herpes at a dose of 250 mg tid for 5 or 10 days and is used in chronic suppression of recurrences at a dose of 250 mg bid. Penciclovir is being developed in its own right as both an intravenous and topical formulation. Parenteral penciclovir (5 mg per kg intravenously [IV] every 8 hours for 5 days) is effective against recurrent genital herpes, although this is an impractical regimen for this indication.2 More importantly, penciclovir IV (5 mg/kg) every 12 hours was also equally effective compared with penciclovir IV 8 hourly or acyclovir IV (5 mg/kg) every 8 hours in the treatment of herpes simplex infections in immunocompromised hosts, offering a significant dosing reduction in the hospital setting.3 Penciclovir 1% cream is also effective in reducing the duration and severity of herpes labialis when used early and frequently (every 2 hours) at the onset of either symptoms or signs of an active episode,4 and is the treatment of choice for herpes labialis according to the Medical Letter. In fact, it is the only antiviral which has clearly shown benefits in this clinical setting in large, placebo-controlled trials and is the only product licensed for this indication in the US.

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Authors and Affiliations

  1. Department of Pharmacology and Therapeutics Faculty of Medicine, The University of British Columbia and Viridae Clinical Sciences Incorporated, Vancouver, British Columbia, Canada

    Stephen L. Sacks & Bruce Wilson

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  1. Stephen L. Sacks
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  2. Bruce Wilson
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Editors and Affiliations

  1. Macfarlane Burnet Centre for Medical Research, Fairfield, Victoria, Australia

    John Mills

  2. University of California, San Francisco, San Francisco, California, USA

    Paul A. Volberding

  3. University of Washington, Seattle, Washington, USA

    Lawrence Corey

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Sacks, S.L., Wilson, B. (1999). Famciclovir/Penciclovir. In: Mills, J., Volberding, P.A., Corey, L. (eds) Antiviral Chemotherapy 5. Advances in Experimental Medicine and Biology, vol 458. Springer, Boston, MA. https://doi.org/10.1007/978-1-4615-4743-3_13

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  • DOI: https://doi.org/10.1007/978-1-4615-4743-3_13

  • Publisher Name: Springer, Boston, MA

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  • Online ISBN: 978-1-4615-4743-3

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