Phosphonoformate
Phosphonoformate Uses, Dosage, Side Effects, Food Interaction and all others data.
An antiviral agent used in the treatment of cytomegalovirus retinitis. Phosphonoformate also shows activity against human herpes viruses and HIV.
Phosphonoformate 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). Phosphonoformate does not require activation (phosphorylation) by thymidine kinase or other kinases and therefore is active in vitro against HSV TK deficient mutants and CMV UL97 mutants. Thus, HSV strains resistant to acyclovir or CMV strains resistant to ganciclovir may be sensitive to foscarnet. However, acyclovir or ganciclovir resistant mutants with alterations in the viral DNA polymerase may be resistant to foscarnet and may not respond to therapy with foscarnet. The combination of foscarnet and ganciclovir has been shown to have enhanced activity in vitro.
| Trade Name | Phosphonoformate |
| Availability | Prescription only |
| Generic | Foscarnet |
| Foscarnet Other Names | Carboxyphosphonic acid, Foscarmet, Phosphonoformate, Phosphonoformic acid, Phosphonomethanoic acid |
| Related Drugs | acyclovir, valacyclovir, Valtrex, Zovirax, famciclovir, ganciclovir ophthalmic, valganciclovir, Valcyte, Famvir, cidofovir |
| Type | |
| Formula | CH3O5P |
| Weight | Average: 126.0053 Monoisotopic: 125.971809718 |
| Protein binding | 14-17% |
| Groups | Approved |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Phosphonoformate is an antiviral used to treat CMV, HIV, and HSV infections.
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.
Phosphonoformate is also used to associated treatment for these conditions: Chickenpox, Cytomegalovirus Retinitis, Genital Herpes, Herpes Labialis, Herpetic whitlow
How Phosphonoformate works
Phosphonoformate 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.
Toxicity
Oral, rat LD50: >2,000 mg/kg. Signs of overdose include renal impairment.
Food Interaction
No interactions found.Phosphonoformate Drug Interaction
Moderate: furosemide, furosemide, valacyclovir, valacyclovir, voriconazole, voriconazoleMinor: sulfamethoxazole / trimethoprim, sulfamethoxazole / trimethoprimUnknown: lactobacillus acidophilus, lactobacillus acidophilus, ursodiol, ursodiol, loratadine, loratadine, meperidine, meperidine, acetaminophen, acetaminophen, valganciclovir, valganciclovir
Phosphonoformate Disease Interaction
Major: dehydration, electrolyte disturbances, renal dysfunctionModerate: hematologic toxicities
Elimination Route
Poorly absorbed after oral administration (bioavailability from 12 to 22%).
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]
Innovators Monograph
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