Drug reference

Ganciclovir

Antiviral

AntiviralATC J05AB06

CDSCO approvedSchedule HATC J05AB06

EXCRETION

—

not curated

INTERACTIONS

12 major

SEVERE in our sources

PREGNANCY

Manufacturer advises avoid.

FDA category + note

Top interactionssee all 12 →

MaribavirSevereTextbookHarrison 22e · unknown
AdalimumabSevereDatabaseDDInter
CertolizumabSevereDatabaseDDInter
CidofovirSevereDatabaseDDInter

Mechanism

Ganciclovir is a guanosine nucleoside analogue that requires initial phosphorylation by viral UL97 protein kinase (in CMV-infected cells) followed by cellular kinases to form the active triphosphate. Ganciclovir triphosphate competitively inhibits viral DNA polymerase and is incorporated into viral DNA, causing premature chain termination. Its dependence on viral UL97 kinase for activation provides selectivity for CMV-infected cells, though this also means resistance commonly arises through UL97 mutations.

Indications

Initial treatment of CMV infectionall herpesviruses (especially CMV)CMV retinitisother CMV syndromes in patients with AIDS or recipients of solid-organ transplantsprophylaxis of CMV infections in transplant recipientspreemptive therapy of CMV infections in transplant recipientsHSV keratitis (ophthalmic gel)chronic HBV infection (reduces HBV DNA levels and aminotransferase levels, but not approved for this indication)herpes simplex keratitiscytomegalovirus retinitisviral conjunctivitis (off-label)prophylaxis and treatment of severe CMV infections (pneumonia, colitis, retinitis) in immunocompromised patients (AIDS, transplant recipient)Treatment of CMV-related CNS infections

Dosing

Adult: Inosine pranobex p. 670 has been used by mouth for herpes simplex infections; its effectiveness remains unproven. Cytomegalovirus infection Ganciclovir p. 674 is related to aciclovir but it is more active against cytomegalovirus (CMV); it is also much more toxic than aciclovir and should therefore be prescribed only when the potential beneﬁt outweighs the risks.…
Renal adjustment: Doses should be adjusted in patients with renal insufficiency.

Pharmacokinetics

Half-life

2 to 4 h (plasma elimination); >24 h (intracellular ganciclovir triphosphate); 23 to 26 h (vitreous fluid)

Bioavailability

6% to 9% (oral)

Protein binding

1–2%

Excretion

Over 90% eliminated unchanged by renal excretion

Contraindications

Concomitant use with zidovudine (particularly during initial ganciclovir therapy) due to profound myelosuppression

Side effects

Common

neutropenia (15% to 40%)thrombocytopenia (5% to 20%)headache (5% to 15%)behavioral changes (5% to 15%)infusion-related phlebitisazotemiaanemiarashfeverliver function test abnormalitiesnauseavomitingeosinophiliapunctate keratopathyconjunctival hyperemianeuropsychiatric disturbancesGastrointestinal side effects (nausea, vomiting, diarrhea, abdominal pain) (~20%)

Serious

Profound myelosuppression
myelosuppression (principal dose-limiting toxicity)
persistent fatal neutropenia
convulsions
coma
bone marrow depression (systemic toxicity)
Granulocytopenia and thrombocytopenia (20–25%)
Retinal detachment (reported in some patients treated for CMV retinitis, causal relationship unclear)