Valcyte (valganciclovir HCl)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Valganciclovir, a prodrug of ganciclovir, is an antiviral agent; after in vivo conversion to an active metabolite, the drug is active against herpes viruses.
Valganciclovir, the l-valyl ester of ganciclovir, is an antiviral agent. Valganciclovir is a prodrug and exhibits no antiviral activity until converted by intestinal and hepatic esterases to ganciclovir and subsequently to the active form ganciclovir triphosphate.
Valganciclovir is commercially available as the hydrochloride salt and differs structurally from ganciclovir by the presence of the l-amino acid, valine, attached to the 2-hydroxyl group of the nucleoside and by the presence of the monohydrochloride salt. These structural modifications result in substantially increased GI absorption of valganciclovir relative to oral ganciclovir (no longer commercially available in the US), resulting in plasma ganciclovir concentrations comparable to those achieved with IV ganciclovir.
Valganciclovir is rapidly converted to ganciclovir in vivo and subsequently phosphorylated within cytomegalovirus (CMV)-infected cells to ganciclovir triphosphate. Since initial phosphorylation of ganciclovir depends largely on the presence of a viral kinase (pUL97), phosphorylation occurs preferentially in virus-infected cells. Ganciclovir triphosphate is a viral DNA polymerase inhibitor and exerts its antiviral activity on CMV by inhibiting the viral DNA polymerase.
Other mechanisms also are involved. For additional information, see Mechanism of Action in Ganciclovir 8:18.32.
The absolute bioavailability of ganciclovir following oral administration of valganciclovir is about 60%. Results from pharmacokinetic studies in adults indicate that oral administration of valganciclovir 900 mg once daily with food provides a mean area under the plasma concentration-time curve0-24 hour (AUC0-24 hour) for ganciclovir comparable to that following IV ganciclovir 5 mg/kg once daily. However, at these dosages, oral valganciclovir produces lower peak plasma ganciclovir concentrations than IV ganciclovir.
USES: Valganciclovir is an anti-viral drug. It is changed in the body to the active form of the drug called ganciclovir. It is used to prevent disease caused by a virus called cytomegalovirus (CMV) in people who have received organ transplants.
CMV disease can lead to serious infections in the body, including an infection in the eye, called CMV retinitis, that can cause blindness. Valganciclovir works by slowing the growth of the CMV virus. It helps prevent the spread of infection to other areas of the body.
Valganciclovir is also used to treat CMV retinitis in people with advanced HIV disease (AIDS). This medication helps control CMV retinitis and decrease the risk of blindness. Valganciclovir is not a cure for CMV disease.
Some people may have worsening CMV retinitis even with treatment. It is important to have your eyes checked regularly by your doctor.
Generic name: valganciclovir HCl
Pronunciation: (val-gan-SIGH-klow-veer)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
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Indications
The following indications are listed for Valcyte:
- Cmv Retinitis In Aids Patient
- Prevention Of Cmv Disease After Cardiac Transplantation
- Prevention Of Cmv Disease After Kidney Transplantation
- Prevention Of Cytomegalovirus Disease After Kidney-Pancreas Transplantation
Also known as: Cytomegalovirus Prophylaxis After Cardiac Transplantation, Cytomegalovirus Prophylaxis After Kidney Transplantation, Cytomegalovirus Prophylaxis After Kidney-Pancreas Transplantation, Cytomegalovirus Retinitis In Aids, Prevention Of Cmv Disease After Renal Transplantation.
Dosing
Dosage of valganciclovir hydrochloride is expressed in terms of valganciclovir.
Valganciclovir hydrochloride is administered orally as tablets or an oral solution and should be given with food.
Adults should receive valganciclovir tablets (not the oral solution). Valganciclovir tablets should not be broken or crushed.
Valganciclovir oral solution is the preferred dosage form for pediatric patients. Valganciclovir tablets should be used in pediatric patients only if the calculated dose is within 10% of the tablet strength (i.e., a single 450-mg tablet may be used if the calculated dose is 405-495 mg). (See Pediatric Dosage under Dosage and Administration: Dosage.)
Patients receiving valganciclovir should be adequately hydrated.
Females of childbearing potential should be tested for pregnancy prior to initiation of valganciclovir. (See Pregnancy under Warnings/Precautions: Specific Populations, in Cautions.)
Because of the mutagenic and/or carcinogenic potential of valganciclovir, the tablets, powder for oral solution, and reconstituted oral solutions of the drug should be handled carefully according to guidelines issued for cytotoxic drugs. (See Handling and Disposal under Warnings/Precautions: Other Warnings/Precautions, in Cautions.)
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No dosing information is available for this tab.
Drug interactions
No formal drug interaction studies have been performed using valganciclovir. However, valganciclovir is rapidly and extensively converted to ganciclovir and interactions reported with ganciclovir are expected to occur in patients receiving valganciclovir.
Drug interaction studies with ganciclovir were performed in patients with normal renal function. In patients with renal impairment, concomitant use of valganciclovir and other drugs eliminated by renal excretion may result in increased concentrations of ganciclovir and the concomitant drug and such patients should be closely monitored for toxicity associated with ganciclovir and the concomitant drug.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
Valganciclovir is contraindicated in patients who have had a clinically important hypersensitivity reaction (e.g., anaphylaxis) to valganciclovir, ganciclovir, or any ingredient in the formulation.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
Adverse effects occurring in 20% or more of adults receiving valganciclovir include diarrhea, pyrexia, fatigue, nausea, tremor, neutropenia, anemia, leukopenia, thrombocytopenia, headache, insomnia, urinary tract infection, and vomiting.
Adverse effects occurring in 20% or more of pediatric patients receiving valganciclovir include diarrhea, pyrexia, upper respiratory tract infection, urinary tract infection, vomiting, neutropenia, leukopenia, and headache.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
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Safety and efficacy of valganciclovir have not been established in pediatric patients younger than 1 month of age.
Use of valganciclovir for the prevention of CMV disease in pediatric heart transplant recipients 1 month to 16 years of age is based on safety and pharmacokinetic data from 2 studies in pediatric solid organ transplant recipients and is supported by efficacy data from studies in adult solid organ transplant recipients.
Use of valganciclovir for the prevention of CMV disease in pediatric kidney transplant recipients 4 months to 16 years of age is based on safety, tolerability, and pharmacokinetic data from 2 open-label studies in solid organ transplant recipients in this age group and is supported by efficacy data from studies in adult solid organ transplant recipients.
Safety and efficacy of valganciclovir have not been established for prevention of CMV disease in pediatric heart transplant recipients younger than 1 month of age, pediatric kidney transplant recipients younger than 4 months of age, or pediatric liver transplant recipients of any age.
The safety profile of valganciclovir in pediatric patients generally is similar to that observed in adults. However, upper respiratory tract infection, pyrexia, nasopharyngitis, anemia, abdominal pain, and neutropenia have been reported more frequently in pediatric patients than in adults.
In animal studies, ganciclovir caused maternal and fetal toxicity, embryofetal mortality, and teratogenicity. Valganciclovir is expected to have reproductive toxicity similar to ganciclovir. (See Teratogenesis under Warnings/Precautions: Warnings, in Cautions.)
Data are not available regarding use of valganciclovir in pregnant women to establish the presence or absence of drug-associated risk. An ex vivo placental model indicates that ganciclovir crosses the human placenta by passive diffusion and is not saturable over a concentration range of 1-10 mg/mL.
Although most maternal CMV infections are asymptomatic or may be associated with a self-limited mononucleosis-like syndrome, CMV infections in pregnant immunocompromised patients (e.g., those with human immunodeficiency virus (HIV) infection and acquired immunodeficiency syndrome (AIDS), transplant recipients) may be symptomatic and result in substantial maternal morbidity and mortality. Perinatal transmission of CMV from infected mothers to their neonates can occur resulting in congenital CMV infection and disease. (See Congenital Cytomegalovirus Disease under Uses: Treatment of Cytomegalovirus Infection and Disease.)
Females of childbearing potential should undergo pregnancy testing before initiation of valganciclovir. In addition, pregnancy should be avoided in female patients receiving valganciclovir and in females with male partners receiving valganciclovir.
Females of childbearing potential should be advised to use an effective method of contraception during and for at least 30 days after valganciclovir therapy and male patients should be advised to use a reliable method of barrier contraception during and for at least 90 days after valganciclovir therapy.
It is not known whether valganciclovir or ganciclovir is distributed into human milk, affects the breast-fed infant, or affects milk production. Animal data from studies using ganciclovir indicate that the drug is distributed into milk of lactating rats.
Because of the potential for serious adverse effects in nursing infants, valganciclovir is not recommended in breast-feeding women. HIV-infected mothers should be instructed not to breast-feed their infants because of the risk of transmission of HIV.
Dosage of valganciclovir for geriatric patients should be selected with caution, usually starting at the low end of the dosage range, because of age-related decreases in hepatic, renal, and/or cardiac function. Renal function should be assessed before and during valganciclovir therapy and appropriate dosage adjustments made as necessary. (See Geriatric Use under Warnings/Precautions: Specific Populations, in Cautions.)
Safety and efficacy of valganciclovir have not been specifically evaluated in geriatric patients 65 years of age or older and there were insufficient numbers of individuals in this age group in clinical studies to determine whether they respond differently than younger adults. Pharmacokinetics of the drug have been not studied in geriatric patients.
Because geriatric individuals frequently have decreased renal function and because valganciclovir is substantially excreted by the kidneys, particular attention should be paid to assessing renal function before and during valganciclovir therapy in this age group. If evidence of renal impairment exists or develops, appropriate dosage adjustments should be made. In general, dosage should be selected carefully, usually starting at the low end of the dosage range, taking into account the greater frequency of decreased hepatic, renal, and/or cardiac function and of concomitant disease and drug therapy observed in the elderly.
ICD codes
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Last reviewed · Source: First Databank (FDB) drug data
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