Valganciclovir

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Valganciclovir
Systematic (IUPAC) name
2-[(2-amino-6-oxo-3,6-dihydro-9H-purin-9-yl) methoxy]-3-hydroxypropyl (2S)-2-amino-3- methylbutanoate
Identifiers
CAS number	175865-59-5
ATC code	J05AB14
PubChem	64147
Chemical data
Formula	C14H22N6O5
Mol. mass	354.362 g/mol
Pharmacokinetic data
Bioavailability	60%
Protein binding	1-2%
Metabolism	Hydrolysed to ganciclovir
Half life	4 hours
Excretion	Renal
Therapeutic considerations
Pregnancy cat.	C(US)
Legal status	POM(UK) ℞-only(US)
Routes	Oral

Valganciclovir hydrochloride (Valcyte, manufactured by Roche) is an antiviral medication used to treat cytomegalovirus infections. As the L-valyl ester of ganciclovir, it is actually a prodrug for ganciclovir. After oral administration, it is rapidly converted to ganciclovir by intestinal and hepatic esterases.

Contents 1 Administration 2 Pharmacokinetics 3 Side effects 4 Alternative uses 5 References

[edit] Administration

Orally, available in 450 mg pink tablets. Dosing is calculated to provide appropriate doses of ganciclovir; 900 mg of valganciclovir orally every 12 hours is equivalent to 5 mg per kilogram of body weight of intravenous ganciclovir, also every 12 hours.

[edit] Pharmacokinetics

1. Oral bioavailability is approximately 60%. Fatty foods significantly increase the bioavailability and the peak level in the serum.
2. It takes about 2 hours to reach maximum concentrations in the serum.
3. Valganciclovir is eliminated as ganciclovir in the urine, with a half-life of about 4 hours in people with normal kidney function.

[edit] Side effects

• Blood: neutropenia, anemia, low platelets. Myelosuppression is one of the main side effects that may limit prolonged use of valganciclovir.
• Gastrointestinal: diarrhea, nausea, vomiting, abdominal pain.
• Central nervous system: fever, headache, insomnia, paresthesia, and peripheral neuropathy.
• Ocular: retinal detachment

[edit] Alternative uses

It has been proposed that valganciclovir could be used in the treatment of chronic fatigue syndrome, following some reported success in 9 out of 12 patients at Stanford University in California, although further research is required [1]. A study is planned at Stanford for early 2007. [2]

[edit] References

1. Kogelnik AM et al Use of valganciclovir in patients with elevated antibody titers against Human Herpesvirus-6 (HHV-6) and Epstein-Barr Virus (EBV) who were experiencing central nervous system dysfunction including long-standing fatigue. J Clin Virol. 2006;37(S1):S33-S38.
2. Paltiel AD et al Preevaluation of clinical trial data: the case of preemptive cytomegalovirus therapy in patients with human immunodeficiency virus. Clin Infect Dis. 2001;32(5):783-93.
3. Pescovitz MD et al Valganciclovir results in improved oral absorption of ganciclovir in liver transplant recipients. Antimicrob Agents Chemother. 2000;44(10):2811-5.
4. Reusser P. Antiviral therapy: current options and challenges. Schweiz Med Wochenschr. 2000;130(4):101-12.
5. Sugawara M, Huang W, Fei YJ, et al. Transport of valganciclovir, a ganciclovir prodrug, via peptide transporters PEPT1 and PEPT2. J Pharm Sci. 2000;89(6):781-9.

v • d • e Antivirals, other than for HIV (primarily J05, also S01AD and D06BB) Anti-herpesvirus (DNA, I) purine analogue (guanine) (Aciclovir, Famciclovir, Ganciclovir, Penciclovir, Valaciclovir, Valganciclovir) • Vidarabine pyrimidine analogue (uridine) (Idoxuridine, Trifluridine) • Cidofovir Docosanol • Fomivirsen • Foscarnet • Tromantadine HPV/MC (DNA, I) Imiquimod • Podophyllotoxin Hepatitis B (DNA, VII) Adefovir • Clevudine • Interferon alfa-2b • Pegylated interferon alfa-2a • Entecavir • Lamivudine • Telbivudine • Tenofovir† Hepatitis C (RNA, IV) Pegylated interferon alpha • Ribavirin • Taribavirin† • Boceprevir† Picornavirus (RNA, IV) Pleconaril† Anti-influenza agents (RNA, V) Arbidol adamantane derivatives/M2 inhibitors (Amantadine, Rimantadine) neuraminidase inhibitors (Oseltamivir, Zanamivir, Peramivir†) HIV (Reverse, VI) See HIV pharm Other antiviral agents general (Inosine, Interferon) †Undergoing clinical trials, not FDA approved.