Foscarnet
  • Inhibits viral DNA polymerase, RNA. polymerase, HIV reverse transcriptase. Phosphorylation step not required for drug activation.
  • In vitro activity against HSV, VZV, HIV, hepatitis B. virus, HHV-6,Epstein-Barr virus, and CMV.
  • Foscarnet resistance: DNA polymerase gene point mutation, typically following prolonged administration; mutations may also occur in HIV-1 reverse transcriptase
  • Only available by IV route of administration.
  • Clearance: primarily renal; dosage adjustment required based on creatinine clearance.

 Foscarnet: Clinical Use

  • CMV retinitis, acyclovir-resistant HSV;
  • Foscarnet is as effective as ganciclovir in treating CMV retinitis in patients with AIDS; however, patients survived longer, perhaps because of foscarnet's anti-HIV activity.
  • foscarnet superior to vidarabine in treatment of acyclovir-resistant human simplex viral infections

Forcarnet: Adverse Reactions 

  • Significant renal side effects: real insufficiency, hypocalcemia, hypercalcemia, hypophosphatemia, hyperphosphatemia, hypomagnesemia (these effects are due to foscarnet's ability to bind divalent ions).
  • Lack of hematologic abnormalities allows foscarnet use in combination with myelosuppressive agents such as zidovudine.
  • Slow infusion rates and saline hydration protect against nephrotoxicity and electrolyte imbalances.
  • Genital ulcerations
  • CNS toxicities: headache, seizures, hallucinations
  • Coadministration with pentamidine increases hypocalcemia and renal toxicity