Valganciclovir

Absorption

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

Toxicity

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

The Uses of Valganciclovir

Valganciclovir-d8, is the labeled analogue of Valganciclovir (V092000), a pro-drug of Ganciclovir, used in treatment of retro-virus.

The Uses of Valganciclovir

Antiviral.

Indications

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

Background

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.

Definition

ChEBI: The L-valinyl ester of ganciclovir, into which it is rapidly converted by intestinal and hepatic esterases. It is a synthetic analogue of 2'-deoxyguanosine.

Indications

Valganciclovir (Valcyte) is the L-valyl ester prodrug of ganciclovir.

brand name

Valcyte (Roche).

Pharmacokinetics

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.

Clinical Use

Oral valganciclovir is comparable to intravenous ganciclovir for the treatment and suppression of CMV retinitis in AIDS patients.

Drug interactions

Potentially hazardous interactions with other drugs
Antibacterials: increased risk of convulsions with imipenem-cilastatin.
Antivirals: possibly increased didanosine concentration; profound myelosuppression with zidovudine - avoid if possible.
Mycophenolate: possibly increased concentrations of both mycophenolic acid and ganciclovir.
Increased risk of myelosuppression with other myelosuppressive drugs.

Metabolism

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

Metabolism

Valganciclovir is well absorbed from the gastrointestinal tract and rapidly and extensively metabolised in the intestinal wall and liver to ganciclovir. Valganciclovir is eliminated in the urine as unchanged ganciclovir, mainly by glomerular filtration and also active tubular secretion.