Valganciclovir



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
O5 
Mol. mass 354.362 g/mol
Pharmacokinetic data
Bioavailability 60%
Protein binding 1-2%
ganciclovir
Half life 4 hours
Excretion Renal
Therapeutic considerations
Pregnancy cat.

C(US)

Legal status

-only(US)

Routes Oral

Valganciclovir hydrochloride (Valcyte, manufactured by Roche) is an antiviral medication used to treat cytomegalovirus infections. As the L-valyl esterases.

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.

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.

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

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]

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.
 
This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Valganciclovir". A list of authors is available in Wikipedia.