Valganciclovir 175865-59-5
175865-60-8

Valganciclovir

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.

Administration

Orally, available in 450 mg pink tablets. For patients who have received a transplant, the recommended dose is 900 mg once daily, starting within 10 days of transplantation and continuing until 100 days post transplantation. HIV patients might initially need to take the dose 900 mg twice daily for the first 3 weeks.

Pharmacokinetics

# Oral bioavailability is approximately 60%. Fatty foods significantly increase the bioavailability and the peak level in the serum. # It takes about 2 hours to reach maximum concentrations in the serum. # Valganciclovir is eliminated as ganciclovir in the urine, with a half-life of about 4 hours in people with normal kidney function. # The mechanism of this drug is activation via thymidine kinsase enzyme. The phosphotransferase enzyme can likewase activate valganciclovir.

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, a follow-up double-blind, controlled study of 30 patients was completed, and although data has not yet been released, according to the Virus Induced CNS Dysfunction Association, "the data Dr. Montoya presented at the 2008 International Conference on HHV-6&7 indicated that patients on Valcyte experienced significant cognitive improvement. ", especially for those with elevated antibody levels to HHV-6 and EBV (VCA and EA)

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    Systematic (IUPAC) name: 2-[(2-amino-6-oxo-6,9-dihydro-3H-purin-9-yl)methoxy]-3-hydroxypropyl (2S)-2-amino-3-methylbutanoate
    Valganciclovir CAS number: 175865-59-5
    175865-60-8
    ATC code: J05 AB14
    PubChem: 64147
    DrugBank:
    Formula: C14H22N6O5
    Molecular mass: 354.362 g/mol
    Valganciclovir Assay/Purity: Typically NLT 98%
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