Valganciclovir

What is Valganciclovir?

• Valganciclovir (VALCYTE) is a deoxynucleoside analogue cytomegalovirus (CMV) DNA polymerase inhibitor used to treat cytomegalovirus (CMV) infection in those with HIV/AIDS or following organ transplant.

Valganciclovir

Valganciclovir ball-and-stick

Valganciclovir

What are the uses of this medicine?

VALCYTE is a prescription antiviral medicine. In adults, VALCYTE tablets are used:

• to treat cytomegalovirus (CMV) retinitis in people who have acquired immunodeficiency syndrome (AIDS). When CMV virus infects the eyes, it is called CMV retinitis. If CMV retinitis is not treated, it can cause blindness.
• to prevent CMV disease in people who have received a kidney, heart, or kidney-pancreas transplant and who have a high risk for getting CMV disease.

In children, VALCYTE tablets or oral solution are used:

• to prevent CMV disease in children 4 months to 16 years of age who have received a kidney transplant and have a high risk for getting CMV disease.
• to prevent CMV disease in children 1 month to 16 years of age who have received a heart transplant and have a high risk for getting CMV disease.

• VALCYTE does not cure CMV retinitis.

How does this medicine work?

• Valganciclovir is an antiviral drug with activity against CMV.
• Valganciclovir is an L-valyl ester (prodrug) of ganciclovir that exists as a mixture of two diastereomers.
• After oral administration, both diastereomers are rapidly converted to ganciclovir by intestinal and hepatic esterases.
• Ganciclovir is a synthetic analogue of 2'-deoxyguanosine, which inhibits replication of human CMV in cell culture. ganciclovir is initially phosphorylated to ganciclovir monophosphate by the viral protein kinase, pUL97.
• Further phosphorylation occurs by cellular kinases to produce ganciclovir triphosphate.
• The virustatic activity of ganciclovir is due to inhibition of the viral DNA polymerase, pUL54 by ganciclovir triphosphate.

Who Should Not Use this medicine ?

This medicine cannot be used in patients who:

• had a serious allergic reaction to valganciclovir, ganciclovir or any of the ingredients of VALCYTE.

What drug interactions can this medicine cause?

• valganciclovir is rapidly and extensively converted to ganciclovir, drug-drug interactions associated with ganciclovir will be expected for VALCYTE.
• Seizures were reported in patients receiving ganciclovir and imipenem-cilastatin. Concomitant use is not recommended unless the potential benefits outweigh the risks.
• Cyclosporine or amphotericin B when coadministered with valganciclovir, the risk of nephrotoxicity may be increased. Monitor renal function.
• Mycophenolate mofetil (MMF) when coadministered with valganciclovir, the risk of hematological and renal toxicity may be increased. Monitor for ganciclovir and MMF toxicity.
• Due to potential for increased toxicity, consider for concomitant use of drugs associated with myelosuppression or nephrotoxicity with valganciclovir only if the potential benefits are judged to outweigh the risks.
• Ganciclovir coadministered with didanosine may increase didanosine levels. Monitor for didanosine toxicity (e.g., pancreatitis).
• coadministration with Probenecid may increase ganciclovir levels. Monitor for evidence of ganciclovir toxicity.

Is this medicine FDA approved?

• Valganciclovir was approved for medical use in 2001.

How should this medicine be used?

Recommended dosage: Recommended Dosage in Adult Patients with Normal Renal Function:

Treatment of CMV Retinitis:

• Induction: The recommended dosage is 900 mg (two 450 mg tablets) taken orally twice a day for 21 days.
• Maintenance: Following induction treatment, or in adult patients with inactive CMV retinitis, the recommended dosage is 900 mg (two 450 mg tablets) taken orally once a day.

Prevention of CMV Disease:

• For adult patients who have received a heart or kidney-pancreas transplant, the recommended dosage is 900 mg (two 450 mg tablets) taken orally once a day starting within 10 days of transplantation until 100 days post-transplantation.
• For adult patients who have received a kidney transplant, the recommended dosage is 900 mg (two 450 mg tablets) taken orally once a day starting within 10 days of transplantation until 200 days post-transplantation.

Recommended Dosage in Pediatric Patients:

Prevention of CMV Disease in Pediatric Kidney Transplant Patients:

• For pediatric kidney transplant patients 4 months to 16 years of age, the recommended dose once a day within 10 days of transplantation until 200 days post-transplantation according to dosage algorithm (note the calculation of creatinine clearance using a modified Schwartz formula in children).

Prevention of CMV Disease in Pediatric Heart Transplant Patients:

• For pediatric heart transplant patients 1 month to 16 years of age, the recommended dose once a day within 10 days of transplantation until 100 days post-transplantation according to dosage algorithm (note the calculation of creatinine clearance using a modified Schwartz formula in children).

Administration:

• Adults should only take VALCYTE tablets. Children may take either VALCYTE tablets or oral solution.
• Take VALCYTE with food.
• Do not break or crush VALCYTE tablets. Avoid contact with your skin or eyes. If you come in contact with the contents of the tablet or oral solution, wash your skin well with soap and water or rinse your eyes well with plain water.
• If your child is prescribed VALCYTE for oral solution, your pharmacist will give you oral dosing dispensers to measure your child's dose of VALCYTE for oral solution. To be sure you receive the prescribed dose, it is important to use the dispenser provided to you. See the detailed INSTRUCTIONS FOR USE below for information about how to take VALCYTE for oral solution. Ask your pharmacist if you have any questions. If you lose or damage your oral dispensers and cannot use them, contact your pharmacist.
• If you take too much VALCYTE, call your healthcare provider or go to the nearest hospital emergency room right away.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Tablets: 450 mg.

Oral Solution: 50 mg per mL.

This medicine is available in fallowing brand namesː

• VALCYTE

What side effects can this medication cause?

The most common side effects of this medicine include: The most common side effects of VALCYTE in children include:

• diarrhea
• fever
• upper respiratory tract infection
• urinary tract infection
• vomiting
• low white blood cell counts in blood tests
• headache

The most common side effects of VALCYTE in adults include:

• diarrhea
• fever
• fatigue
• nausea
• shaky movements (tremors)
• low white cell, red cell and platelet cell counts in blood tests
• headache
• sleeplessness
• urinary tract infection
• vomiting

VALCYTE may cause serious side effects, including:

• Blood and bone marrow problems
• Kidney failure
• Fertility problems
• Birth defects
• Cancer

What special precautions should I follow?

• VALCYTE can cause seizures, dizziness, and confusion. You should not drive a car or operate machinery until you know how VALCYTE affects you.
• Acute renal failure may occur in elderly patients (with or without reduced renal function), patients who receive concomitant nephrotoxic drugs, or inadequately hydrated patients. Use with caution in elderly patients or those taking nephrotoxic drugs, reduce dosage in patients with renal impairment, and monitor renal function.
• Severe leukopenia, neutropenia, anemia, thrombocytopenia, pancytopenia, and bone marrow failure including aplastic anemia have been reported in patients treated with VALCYTE or ganciclovir. VALCYTE should also be used with caution in patients with pre-existing cytopenias and in patients receiving myelosuppressive drugs or irradiation.
• Based on animal data and limited human data, VALCYTE at the recommended human doses may cause temporary or permanent inhibition of spermatogenesis in males, and may cause suppression of fertility in females. Advise patients that fertility may be impaired with use of VALCYTE.
• Ganciclovir may cause fetal toxicity when administered to pregnant women based on findings in animal studies. Females of reproductive potential should be advised to use effective contraception during treatment and for at least 30 days following treatment with VALCYTE because of the potential risk to the fetus. Similarly, males should be advised to use condoms during and for at least 90 days following treatment with VALCYTE.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• Hematological toxicity
• Hepatotoxicity
• Renal toxicity
• Gastrointestinal toxicity
• Neurotoxicity

Management of overdosage:

• Ganciclovir is dialyzable, dialysis may be useful in reducing serum concentrations in patients who have received an overdose of VALCYTE.
• Adequate hydration should be maintained.
• The use of hematopoietic growth factors should be considered.

Can this medicine be used in pregnancy?

• After oral administration, valganciclovir (prodrug) is converted to ganciclovir (active drug) and, therefore, VALCYTE is expected to have reproductive toxicity effects similar to ganciclovir.
• Advise pregnant women of the potential risk to the fetus.

Can this medicine be used in children?

• VALCYTE for oral solution and tablets are indicated for the prevention of CMV disease in pediatric kidney transplant patients 4 months to 16 years of age and in pediatric heart transplant patients 1 month to 16 years of age at risk for developing CMV disease.
• The safety and efficacy of VALCYTE for oral solution and tablets have not been established in children for prevention of CMV disease in pediatric liver transplant patients, in kidney transplant patients less than 4 months of age, in heart transplant patients less than 1 month of age, in pediatric AIDS patients with CMV retinitis, and in infants with congenital CMV infection.

What are the active and inactive ingredients in this medicine?

• Active ingredient: valganciclovir hydrochloride
• Inactive ingredients for tablets: microcrystalline cellulose, povidone K-30, crospovidone, and stearic acid. The film-coating applied to the tablets contains Opadry Pink®.
• Inactive ingredients for oral solution: sodium benzoate, fumaric acid, povidone K-30, sodium saccharin, mannitol and tutti-frutti flavoring.

Who manufactures and distributes this medicine?

• VALCYTE is a registered trademark of Hoffmann-La Roche Inc.

• Distributed by:

Genentech USA, Inc. A Member of the Roche Group 1 DNA Way South San Francisco, CA

What should I know about storage and disposal of this medication?

• Store VALCYTE tablets at room temperature between 68°F to 77°F (20°C to 25°C).
• Store VALCYTE for oral solution in the refrigerator between 36°F to 46°F (2°C to 8°C), for no longer than 49 days.
• Do not freeze.
• Do not keep VALCYTE that is out of date or that you no longer need.

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Drugs for Herpes Virus

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Acyclovir, Cidofovir, Famciclovir, Foscarnet, Ganciclovir, Valacyclovir, Valganciclovir

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• Dailymed label info on Valganciclovir
• FDA Valganciclovir

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