Comparative Pharmacology
Head-to-head clinical analysis: CIDOFOVIR versus VITRASERT.
Peer-Reviewed Evidence
Head-to-head clinical analysis: CIDOFOVIR versus VITRASERT.
CIDOFOVIR vs VITRASERT
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Cidofovir is a nucleotide analog that inhibits viral DNA polymerase by competing with deoxycytidine triphosphate for incorporation into viral DNA, resulting in chain termination and inhibition of viral replication.
Vitrasert (ganciclovir implant) releases ganciclovir, a nucleoside analog that inhibits cytomegalovirus (CMV) replication by competitively inhibiting viral DNA polymerase (UL54) after intracellular phosphorylation to ganciclovir triphosphate. This results in chain termination and viral DNA synthesis inhibition.
5 mg/kg intravenously once weekly for 2 weeks, then 5 mg/kg every 2 weeks. Administer with probenecid 2 g orally 3 hours before dose, then 1 g at 2 and 8 hours after dose. Hydrate with 1 L normal saline before infusion.
Intravitreal implant containing 0.59 mg fluocinolone acetonide; inserted into the vitreous cavity; releases drug over approximately 36 months; no systemic dosing.
None Documented
None Documented
Clinical Note
moderateCidofovir + Teriflunomide
"The serum concentration of Teriflunomide can be increased when it is combined with Cidofovir."
Clinical Note
moderateTenofovir disoproxil + Cidofovir
"Tenofovir disoproxil may decrease the excretion rate of Cidofovir which could result in a higher serum level."
Terminal elimination half-life is approximately 2.5 hours. However, the intracellular half-life of the active diphosphate metabolite is >48 hours, supporting once-weekly dosing.
Terminal half-life of 2.8 hours following intravitreal injection; sustained local levels for 2-3 weeks.
Renal excretion of unchanged drug via glomerular filtration and tubular secretion accounts for approximately 90% of the administered dose. Biliary/fecal elimination is minimal (<5%).
Primarily biliary/fecal (approximately 90%) with minimal renal excretion (<10% unchanged in urine).
Category D/X
Category C
Antiviral
Antiviral