Drug Groups

approved; investigational

Description

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.

Indication

Valganciclovir is an antiviral medication used for the treatment of cytomegalovirus infections.

Pharmacology

Valganciclovir 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. After this, it (being an analogue of guanosine) gets incorporated into DNA and thus cannot be properly read by DNA polymerase. This results in the termination of the elongation of viral DNA.

Toxicity

It is expected that an overdose of valganciclovir could also possibly result in increased renal toxicity.

Affected Organisms

Biotransformation

Rapidly hydrolyzed in the intestinal wall and liver to ganciclovir. No other metabolites have been detected.

Absorption

Valganciclovir is well absorbed from the gastrointestinal tract and the absolute bioavailability from valganciclovir tablets (following administration with food) is approximately 60%.

Half Life

Approximately 4.08 hours. Increased in patients with renal function impairment.

Protein Binding

Plasma protein binding of ganciclovir is 1% to 2% over concentrations of 0.5 and 51 mg/mL.

Elimination

The major route of elimination of valganciclovir is by renal excretion as ganciclovir through glomerular filtration and active tubular secretion.

Distribution

* 0.703 ± 0.134 L/kg

Clearance

* 3.07+/- 0.64 mL/min/kg [IV administration]
* 5.3 L/hr [Patient with creatinine clearance of 70.4 mL/min]

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