Cidofovir

Products

Cidofovir was initially marketed in many countries as an infusion concentrate under the brand name Vistide (Gilead). It was approved in many countries in 1997 and had not been available since 2014. In 2017, a concentrate for the preparation of an infusion solution was approved (Sidovis).

Structure and properties

Cidofovir (C8H14N3O6P, Mr = 279.2 g/mol) is present in the drug as cidofovir dihydrate, a white crystalline powder that is soluble in water. It is an analog of cytidine and an acyclic nucleoside phosphonate. See also under the article Nucleic acids.

Effects

Cidofovir (ATC J05AB12) has antiviral properties against human cytomegalovirus (HCMV). It is a prodrug and is phosphorylated in the cell to the active ingredient cidofovir diphosphate. Cidofovir inhibits viral DNA synthesis by inhibiting viral HCMV DNA polymerase. Incorporation of the wrong substrate results in chain termination.

Indications

As a second-line agent for the treatment of cytomegalovirus retinitis (CMV retinitis) in adults with AIDS without renal dysfunction.

Dosage

According to the SmPC. The drug is administered as an intravenous infusion. To reduce the risk of nephrotoxicity, probenecid must be administered orally with each infusion. In addition, intravenous prehydration with saline is performed.

Contraindications

  • Hypersensitivity
  • In patients in whom probenecid or sulfonamides are contraindicated.
  • Renal insufficiency
  • Concurrent administration of other nephrotoxic agents.
  • Direct injection into the eye

For complete precautions, see the drug label.

Interactions

Drug-drug interactions have been described with tenofovir. Probenecid is susceptible to interactions.

Adverse effects

The most common potential adverse effects include:

  • Neutropenia
  • Headache
  • Nausea, vomiting
  • Hair loss, skin rash
  • Proteinuria, creatinine increase in the blood.
  • Weakness, fever

Cidofovir is nephrotoxic and can often lead to renal failure.