valganciclovir

Contraindicated in:

Hypersensitivity to valganciclovir or ganciclovir;
Hemodialysis;
Undergoing liver transplantation;
OB:
Pregnancy
;
Lactation: Lactation.

Use Cautiously in:

Renal impairment (↓ dose if CCr <60 mL/min);
Pre-existing bone marrow depression
;
Previous or concurrent myelosuppressive drug therapy or radiation therapy
;
Rep:
Women of reproductive potential and men with female partners of reproductive potential
;
Pedi: Children <4 mo (safety and effectiveness not established);
Geri: Age-related ↓ in renal function requires dosage ↓ in older adults.

Adv. Reactions/Side Effects ⬆ ⬇

GI: abdominal pain, diarrhea, nausea, vomiting

GU: ↓fertility, renal impairment

Hemat: anemia, APLASTIC ANEMIA, NEUTROPENIA, PANCYTOPENIA, THROMBOCYTOPENIA

Neuro: headache, insomnia, agitation, ataxia, confusion, dizziness, hallucinations, paresthesia, peripheral neuropathy, psychosis, sedation, SEIZURES

Misc: fever, HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS), INFECTION, MALIGNANCY

Interactions ⬆ ⬇

Drug-drug:

↑risk of hematologic toxicity with zidovudine.
Probenecid may ↑ levels and risk of toxicity.
Patients with renal impairment may experience accumulation of metabolites of mycophenolate.

Drug-Food:

Food ↑ absorption.

Availability ⬆ ⬇

(Generic available)

Tablets: 450 mg
Oral solution tutti-frutti flavor: 50 mg/mL

Route/Dosage ⬆ ⬇

Treatment of CMV Disease

PO (Adults ): Induction: 900 mg twice daily for 21 days; Maintenance treatment or patients with inactive CMV retinitis: 900 mg once daily.

Renal Impairment

(Adults ): CCr 40–59 mL/min: Induction: 450 mg twice daily for 21 days. Maintenance treatment or patients with inactive CMV retinitis: 450 mg once daily. CCr 25–39 mL/min: Induction: 450 mg once daily for 21 days. Maintenance treatment or patients with inactive CMV retinitis: 450 mg every 2 days. CCr 10–24 mL/min: Induction: 450 mg every 2 days for 21 days. Maintenance treatment or patients with inactive CMV retinitis: 450 mg twice weekly.

Prevention of CMV Disease in Transplant Patients

PO (Adults ): Kidney/pancreas or heart transplant: 900 mg once daily, starting 10 days prior to transplant and continued for 100 days after; Kidney transplant: 900 mg once daily, starting 10 days prior to transplant and continued for 200 days after.
PO (Children 4 mo–16 yr): Kidney transplant: Dose is based on body surface area (BSA) and CCr. Dose = 7 × BSA × CCr (see prescribing information for equations used for BSA and CCr); all calculated doses should be rounded to nearest 25 mg (max = 900 mg) and administered as oral solution; should be started 10 days prior to transplant and continued for 200 days after.
PO (Children 4 mo–16 yr): Heart transplant: Dose is based on BSA and CCr. Dose = 7 × BSA × CCr (see prescribing information for equations used for BSA and CCr); all calculated doses should be rounded to nearest 25 mg (max = 900 mg) and administered as oral solution; should be started 10 days prior to transplant and continued for 100 days after.

Renal Impairment

PO (Adults ): CCr 40–59 mL/min: 450 mg once daily; CCr 25–39 mL/min: 450 mg every 2 days; CCr 12–24 mL/min: 450 mg twice weekly.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Valganciclovir is a prodrug, which is rapidly converted to ganciclovir by intestinal and hepatic enzymes. CMV virus converts ganciclovir to its active form (ganciclovir phosphate) inside host cell, where it inhibits viral DNA polymerase.

Therapeutic effects:

Antiviral effect directed preferentially against CMV-infected cells.

Classifications ⬆ ⬇

Therapeutic Classification: antivirals

Pharmacokinetics ⬆ ⬇

Absorption: 59% absorbed following oral administration, rapidly converted to ganciclovir.

Distribution: Widely distributed to tissues, including CSF.

Metabolism/Excretion: Rapidly converted to ganciclovir; ganciclovir is mostly excreted by the kidneys.

Half-Life: 4.1 hr (intracellular half-life of ganciclovir phosphate is 18 hr).

Time/Action Profile ⬆ ⬇

(ganciclovir plasma concentrations)

ROUTE	ONSET	PEAK	DURATION
PO	rapid	2 hr	12–24 hr

Patient/Family Teaching ⬆ ⬇

Explain the purpose and side effects of valganciclovir. Instruct patient to take with food, as directed. Take missed doses as soon as remembered, unless almost time for next dose; do not double doses. Advise patient to read Patient Information before starting therapy and with each Rx refill in case of changes.
Instruct patient on proper handling and to avoid direct contact of skin or mucous membranes with any broken or crushed tablet, powder for oral solution, or reconstituted oral solution. Keep valganciclovir out of children's reach.
Advise patient to maintain adequate hydration to avoid renal toxicity.
Explain need for continued medical follow-up to assess effectiveness and possible side effects of medication. Regular blood counts and eye exams will be needed.
Inform patient that valganciclovir is not a cure for CMV retinitis. Progression of retinitis may continue in immunocompromised patients during and following therapy. Advise patients to have regular ophthalmic exams at least every 4–6 wk. Duration of therapy for CMV prevention is based on the duration and degree of immunosuppression.
May cause seizures, sedation, dizziness, ataxia, and/or confusion. Caution patient not to drive or do other activities requiring alertness until response to medication is known.
Advise patient to promptly report unexplained weight loss, persistent weakness and fatigue, swollen lymph nodes, abnormal bleeding, unusual pain or bruising, or new lumps to health care provider.
Advise patient to notify health care provider if fever; chills; sore throat; other signs of infection; bleeding gums; bruising; petechiae; or blood in urine, stool, or emesis occurs. Caution patient to avoid crowds and persons with known infections. Instruct patient to use soft toothbrush and electric razor. Patient should be cautioned not to drink alcoholic beverages or take products containing aspirin or NSAIDs.
Caution patient to use sunscreen and protective clothing to prevent photosensitivity reactions.
Advise patient to notify health care provider of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care provider before taking other medications.
Rep:
May cause fetal harm. Advise women of reproductive potential to use effective contraception during and for ≥30 days following therapy and to avoid breastfeeding. Advise men with female partners of reproductive potential to use a barrier method of contraception during and for ≥90 days following therapy. Advise patient to notify health care provider immediately if pregnancy is suspected. May cause temporary or permanent infertility in men and women.

section name header

Indications ⬇

Contraind./Precautions ⬆ ⬇