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Name: Foscarnet
PubChem Compound ID: 169569
Description: An antiviral agent used in the treatment of cytomegalovirus retinitis. Foscarnet also shows activity against human herpesviruses and HIV.
Molecular formula: CH12Na3O11P
Molecular weight: 300.042 g/mol
34156-56-4; D02267; Trisodium phosphonoformte hexahydrate; Dihydroxyphosphinecarboxylic acid oxide trisodium salt hexahydrate; Formic acid, phosphono-, trisodium salt, hexahydrate; Foscarnet sodium hydrate; Foscarnet; Foscavir; Foscavir (TN); Phosphinecarboxylic acid, dihydroxy-, oxide, trisodium salt, hexahydrate.
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Name: Foscarnet
Name (isomeric): DB00529
Drug Type: small molecule
Description: An antiviral agent used in the treatment of cytomegalovirus retinitis. Foscarnet also shows activity against human herpesviruses and HIV.
Phosphonoformate; Forscarnet sodium; Carboxyphosphonic acid; Foscarnet sodium; Dihydroxyphosphinecarboxylic acid oxide; Phgosphonocarboxylic acid; PFA; Phosphonoformic acid
Brand: Triapten, Foscavir, Foscarmet
Category: Antiviral Agents, Reverse Transcriptase Inhibitors
CAS number: 63585-09-1
Indication: For the treatment of CMV retinitis in patients with acquired immunodeficiency syndrome (AIDS) and for treatment of acyclovir-resistant mucocutaneous HSV infections in immunocompromised patients.
Foscarnet is an organic analogue of inorganic pyrophosphate that inhibits replication of herpes viruses in vitro including cytomegalovirus (CMV) and herpes simplex virus types 1 and 2 (HSV-1 and HSV-2). Foscarnet does not require activation (phosphorylation) by thymidine kinase or other kinases and therefore is active in vitro against HSV TK...
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Mechanism of Action: Foscarnet exerts its antiviral activity by a selective inhibition at the pyrophosphate binding site on virus-specific DNA polymerases at concentrations that do not affect cellular DNA polymerases.
Absorption: Poorly absorbed after oral administration (bioavailability from 12 to 22%).
Protein binding: 14-17%
Biotransformation: Not metabolized.
Half Life: 3.3-6.8 hours
Clearance: 2.13 +/- 0.71 mL/min/kg [patients had normal renal function (CrCl > 80 mL/min] 68 +/- 8 mL/min/kg [CrCl was 50-80 mL/min] 34 +/- 9 mL/min/kg [CrCl was 25-49 mL/min] 20 +/- 4 mL/min/kg [CrCl was 10 - 24 mL/min]
Toxicity: Oral, rat LD50: >2,000 mg/kg. Signs of overdose include renal impairment.
Affected organisms: Human Herpes Virus
Drug interaction:
ThiothixeneMay cause additive QTc-prolonging effects. Increased risk of ventricular arrhythmias. Consider alternate therapy. Thorough risk:benefit assessment is required prior to co-administration.
VorinostatAdditive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
OfloxacinIncreased risk of convulsions
NorfloxacinIncreased risk of convulsions
ZiprasidoneAdditive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
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