Cidofovir, brand name Vistide, is a topical or injectable Antiviral drug medication primarily used as a treatment for cytomegalovirus (CMV) retinitis (an infection of the retina of the eye) in people with AIDS.[
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Cidofovir was approved for medical use in 1996.
Medical use
DNA virus
Its only indication that has received regulatory approval worldwide is cytomegalovirus retinitis.[ Cidofovir has also shown efficacy in the treatment of aciclovir-resistant HSV infections.]
It first received FDA approval on 26 June 1996,[ and EMA approval on 23 April 1997.]
It has been used topically to treat warts.
Other
It has been suggested as an antitumour agent, due to its suppression of FGF2.
Administration
Cidofovir is only available as an intravenous formulation. Cidofovir is to be administered with probenecid which decreases side effects to the kidney.
Side effects
The major dose-limiting side effect of cidofovir is nephrotoxicity (i.e., kidney damage).[
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Whereas uncommon side effects include: anaemia and elevated liver enzymes and rare side effects include: tachycardia and Fanconi syndrome.[ Probenecid (a uricosuric drug) and intravenous saline should always be administered with each cidofovir infusion to prevent this nephrotoxicity.]
Contraindications
Hypersensitivity to cidofovir or probenecid (as probenecid needs to be given concurrently to avoid nephrotoxicity).[
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Interactions
It is known to interact with nephrotoxic agents (e.g. amphotericin B, foscarnet, IV aminoglycosides, IV pentamide, vancomycin, tacrolimus, non-steroid anti-inflammatory drugs, etc.) to increase their nephrotoxic potential.[
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Mechanism of action
Its active metabolite, cidofovir diphosphate, inhibits viral replication by selectively inhibiting viral DNA polymerases.[ It also inhibits human polymerases, but this action is 8–600 times weaker than its actions on viral DNA polymerases.][ It also incorporates itself into viral DNA, hence inhibiting viral DNA synthesis during reproduction.][
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It possesses in vitro activity against the following viruses:
History
Cidofovir was discovered at the Institute of Organic Chemistry and Biochemistry, Prague, by Antonín Holý, and developed by Gilead Sciences
Synthesis
Cidofovir can be synthesized from a pyrimidone derivative and a protecting group derivative of glycidol.
See also
