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Valganciclovir

Pronouncation: (val-gan-sye-kloh-veer)
Class: Antiviral agent

Trade Names:
Valcyte
- Tablets 450 mg

Pharmacology

Feedback for Valganciclovir

As a treatment for...	Avg User Ratings [?]
Cytomegalovirus (CMV) Infection	Be the first to rate it 0 comments
CMV Retinitis	Be the first to rate it 0 comments

Compare with other drugs.

Valganciclovir is a prodrug of ganciclovir, which inhibits cytomegalovirus (CMV) replication by inhibition of viral DNA synthesis.

Pharmacokinetics

Absorption

Well absorbed from the GI tract. Bioavailability is about 60%. T _max is about 1 to 3 h. When administered with high-fat meal, AUC increased 30%, and C _max increased 14%. It should be administered with food.

Distribution

Valganciclovir is metabolized to ganciclovir. Protein binding of ganciclovir is about 1% to 2%. Vd of ganciclovir is about 0.703 L/kg.

Metabolism

Rapidly metabolized in the intestinal wall and liver to ganciclovir.

Elimination

Major route of elimination is by renal excretion. The t _½ is about 4.08 h (tablets) and about 3.81 h (IV).

Special Populations

Renal Function Impairment

Dosage reductions according to CrCl are required for valganciclovir.

Indications and Usage

Treatment of CMV retinitis in patients with AIDS; prevention of CMV disease in kidney, heart, and kidney-pancreas transplant patients at high risk (donor CMV seropositive/recipient CMV seronegative [D+/R-]).

Contraindications

Hypersensitivity to ganciclovir or valganciclovir.

Dosage and Administration

CMV Retinitis
Adults

PO 900 mg twice daily with food for 21 days. Following this induction phase, or in patients with inactive CMV retinitis, give 900 mg every day with food.

Decreased Renal Function
Induction (adults)

PO 900 mg twice daily (CrCl 60 mL/min or more); 450 mg twice daily (CrCl 40 to 59 mL/min); 450 mg every day (CrCl 25 to 39 mL/min); 450 mg every 2 days (CrCl 10 to 24 mL/min).

Maintenance (adults)

PO 900 mg/day (CrCl 60 mL/min or more); 450 mg every day (CrCl 40 to 59 mL/min); 450 mg every 2 days (CrCl 25 to 39 mL/min); 450 mg twice/wk (CrCl 10 to 24 mL/min).

Prevention of CMV Disease in Heart, Kidney, and Kidney-Pancreas Transplantation
Adults

PO 900 mg every day with food, starting within 10 days of transplantation until 100 days posttransplantation.

Storage/Stability

Store at controlled room temperature (59° to 86°F).

Drug Interactions

Interaction studies have not been conducted; however, because valganciclovir is converted to ganciclovir, interactions associated with ganciclovir are expected to occur for valganciclovir.

Amphotericin B, cyclosporine, nephrotoxic drugs

May increase serum creatinine.

Cytotoxic drugs

May increase the risk of toxicity.

Didanosine

Plasma levels of didanosine may be increased, while didanosine may decrease levels of ganciclovir.

Imipenem-cilastatin

May cause generalized seizures.

Probenecid

May reduce renal Cl and increase serum levels of ganciclovir.

Zidovudine

Both ganciclovir and zidovudine can cause granulocytopenia.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Hypertension (18%); hypotension (at least 5% or serious adverse reactions).

CNS

Headache (22%); insomnia (20%); peripheral neuropathy (9%); paresthesia (8%); dizziness, convulsions, depression, psychosis, hallucinations, confusion, agitation (at least 5% or serious adverse reactions).

Dermatologic

Dermatitis, pruritus, acne (at least 5% or serious adverse reactions).

EENT

Retinal detachment (15%); pharyngitis/nasopharyngitis, rhinorrhea (at least 5% or serious adverse reactions).

GI

Diarrhea (41%); nausea (30%); vomiting (21%); abdominal pain (15%); constipation, dyspepsia, abdominal distention, ascites (at least 5% or serious adverse reactions).

Genitourinary

UTI, renal impairment, dysuria, decreased CrCl (at least 5% or serious adverse reactions).

Hematologic

Neutropenia (27%); anemia (26%); leukopenia (14%); thrombocytopenia (including life-threatening bleeding) (6%); pancytopenia, bone marrow depression, aplastic anemia (at least 5% or serious adverse reactions).

Hepatic

Abnormal hepatic function (at least 5% or serious adverse reactions).

Metabolic-Nutritional

Hyperkalemia, hypokalemia, hypomagnesemia, hyperglycemia, decreased appetite, dehydration, hypophosphatemia, hypocalcemia (at least 5% or serious adverse reactions).

Musculoskeletal

Back pain, arthralgia, muscle cramps, limb pain (at least 5% or serious adverse reactions).

Respiratory

Upper respiratory tract infection, cough, dyspnea, pleural effusion (at least 5% or serious adverse reactions).

Miscellaneous

Pyrexia (31%); tremors (28%); graft rejection (24%); catheter-related infections (3%); hypersensitivity, fatigue, pain, edema, peripheral edema, weakness, local and systemic infections and sepsis, postoperative pain, wound infection and complications, increased wound drainage, wound dehiscence (at least 5% or serious adverse reactions).

Precautions

Warnings

Toxicity includes granulocytopenia, anemia, and thrombocytopenia. In animal studies, ganciclovir was carcinogenic, teratogenic, and caused aspermatogenesis.

Pregnancy

Category C .

Lactation

Undetermined; however, the CDC recommends that HIV-infected mothers not breast-feed infants to avoid risk of HIV transmission.

Children

Safety and efficacy not established.

Renal Function

Use with caution and adjust dosage.

Contact with skin

If broken or crushed tablet comes in contact with skin or mucus membranes, wash thoroughly with soap and water and rinse eyes thoroughly with plain water.

Cytopenia

Severe leukopenia, neutropenia, bone marrow depression, and aplastic anemia have been reported; therefore, use with caution in patients with preexisting cytopenias, or those who have received or are receiving myelosuppressive drugs or irradiation.

Overdosage

Symptoms

Pancytopenia, bone marrow depression, medullary aplasia, leukopenia, neutropenia, granulocytopenia, hepatitis, liver function disorder, worsening of hematuria, acute renal failure, elevated creatinine, abdominal pain, diarrhea, vomiting, generalized tremor, convulsion.

Patient Information

Advise patient to read patient information leaflet before beginning therapy and with each refill.
Warn patient that valganciclovir tablets cannot be substituted for ganciclovir capsules on a one-to-one basis.
Review dosing schedule with patient.
Instruct patient to take each dose with food to maximize absorption into the body.
Advise patient not to chew, crush, break, or split tablets. If direct contact with broken or crushed tablets occurs, advise patient to wash thoroughly with soap and water and rinse eyes thoroughly with plain water.
Advise patient that if a dose is missed to take as soon as remembered and to take the next dose at the usual time. However, if it is nearing the time for the next dose, to skip the dose and take the next dose at the regularly scheduled time.
Advise patient that this drug is not a cure for CMV retinitis and that retinitis may continue to progress during or following treatment.
Advise patient that valganciclovir is converted to ganciclovir in the body and that it may cause infertility and birth defects. Advise men to use barrier contraception during and for at least 90 days following treatment and women to use effective contraception during treatment.
Advise men that drug may cause temporary or permanent infertility.
Advise patient that drug may cause sedation, dizziness and/or confusion and to use caution while performing tasks requiring alertness, including driving and operating machinery.
Advise patient to immediately report any of the following to health care provider: fever or other signs of infection, sore throat, unusual bruising or bleeding.
Advise patient that diarrhea, nausea, vomiting, and headache are common side effects and to inform health care provider if they occur and are intolerable.
Advise HIV-infected mothers not to breast-feed infants to avoid risk of HIV transmission to the infant.
Remind patient that office visits, ophthalmic examinations, and laboratory tests will be required to monitor therapy and to keep appointments.