药品详细
Foscarnet (膦 )
化学结构式图
中文名
膦
英文名
Foscarnet
分子式
Not Available
化学名
phosphonoformic acid
分子量
Average: 126.0053
Monoisotopic: 125.971809718
Monoisotopic: 125.971809718
CAS号
63585-09-1
ATC分类
J05A Direct acting antivirals
药物类型
small molecule
阶段
商品名
Foscarmet;Foscavir;Triapten;
同义名
Carboxyphosphonic acid;Dihydroxyphosphinecarboxylic acid oxide;Forscarnet sodium;Foscarnet sodium;PFA;Phgosphonocarboxylic acid;Phosphonoformate;Phosphonoformic acid;
基本介绍
An antiviral agent used in the treatment of cytomegalovirus retinitis. Foscarnet also shows activity against human herpesviruses and HIV. [PubChem]
生产厂家
- Clinigen healthcare ltd
- Hospira inc
封装厂家
参考
| Synthesis Reference | Not Available |
| General Reference | Not Available |
剂型
| Form | Route | Strength |
|---|---|---|
| Injection, solution | Intravenous drip |
规格
| Unit description | Cost | Unit |
|---|---|---|
| Sodium phosphonoformate powder | 286.3 USD | g |
| Foscavir 24 mg/ml infus bottle | 0.43 USD | ml |
| Foscarnet 24 mg/ml infus bttl | 0.37 USD | ml |
化合物类型
| Type | small molecule |
| Classes |
|
| Substructures |
|
适应症
ANTIVIRALS 抗病毒;
药理
| 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. |
| Pharmacodynamics | 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 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. |
| 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%). |
| Volume of distribution | Not Available |
| Protein binding | 14-17% |
| Metabolism |
Not metabolized. |
| Route of elimination | Not Available |
| Half life | 3.3-6.8 hours |
| Clearance |
|
| Toxicity | Oral, rat LD50: >2,000 mg/kg. Signs of overdose include renal impairment. |
| Affected organisms |
|
| Pathways | Not Available |
理化性质
| Properties | |||||||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| State | solid | ||||||||||||||||||||||||||||||||||||
| Melting point | 88.06 oC | ||||||||||||||||||||||||||||||||||||
| Experimental Properties |
|
||||||||||||||||||||||||||||||||||||
| Predicted Properties |
|
||||||||||||||||||||||||||||||||||||
药物相互作用
| Drug | Interaction |
|---|---|
| Artemether | Additive QTc-prolongation may occur. Concomitant therapy should be avoided. |
| Ciprofloxacin | Increased risk of convulsions |
| Cyclosporine | Monitor for nephrotoxicity |
| Lumefantrine | Additive QTc-prolongation may occur. Concomitant therapy should be avoided. |
| Norfloxacin | Increased risk of convulsions |
| Ofloxacin | Increased risk of convulsions |
| Quinupristin | This combination presents an increased risk of toxicity |
| Tacrolimus | Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. |
| Thiothixene | May cause additive QTc-prolonging effects. Increased risk of ventricular arrhythmias. Consider alternate therapy. Thorough risk:benefit assessment is required prior to co-administration. |
| Toremifene | Additive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Consider alternate therapy. A thorough risk:benefit assessment is required prior to co-administration. |
| Trimipramine | Additive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution. |
| Voriconazole | Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP). |
| Vorinostat | Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP). |
| Ziprasidone | Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated. |
| Zuclopenthixol | Additive QTc prolongation may occur. Consider alternate therapy or use caution and monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP). |
食物相互作用
Not Available
收藏