Tìm theo
Foscarnet
Các tên gọi khác (6 ) :
  • Carboxyphosphonic acid
  • Foscarmet
  • Foscarnet
  • Phosphonoformate
  • Phosphonoformic acid
  • Phosphonomethanoic acid
antiviral agents, reverse transcriptase inhibitors
Thuốc Gốc
Small Molecule
CAS: 63585-09-1
ATC: J05AD01
ĐG : AstraZeneca Inc. , http://www.astrazeneca.ca
CTHH: CH3O5P
PTK: 126.0053
An antiviral agent used in the treatment of cytomegalovirus retinitis. Foscarnet also shows activity against human herpesviruses and HIV. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
CH3O5P
Phân tử khối
126.0053
Monoisotopic mass
125.971809718
InChI
InChI=1S/CH3O5P/c2-1(3)7(4,5)6/h(H,2,3)(H2,4,5,6)
InChI Key
InChIKey=ZJAOAACCNHFJAH-UHFFFAOYSA-N
IUPAC Name
phosphonoformic acid
Traditional IUPAC Name
foscarnet
SMILES
OC(=O)P(O)(O)=O
Độ tan chảy
88.06 °C
Độ hòa tan
Complete
logP
-2.1
logS
-0.88
pKa (strongest acidic)
-0.096
PSA
94.83 Å2
Refractivity
19.07 m3·mol-1
Polarizability
7.89 Å3
Rotatable Bond Count
1
H Bond Acceptor Count
5
H Bond Donor Count
3
Physiological Charge
-3
Number of Rings
0
Bioavailability
1
Rule of Five
true
Dược Lực Học : 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.
Cơ Chế Tác Dụng : An antiviral agent used in the treatment of cytomegalovirus retinitis. Foscarnet also shows activity against human herpesviruses and HIV. [PubChem] 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.
Dược Động Học :
▧ Absorption :
Poorly absorbed after oral administration (bioavailability from 12 to 22%).
▧ Protein binding :
14-17%
▧ Metabolism :
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]
Độc Tính : Oral, rat LD50: >2,000 mg/kg. Signs of overdose include renal impairment.
Chỉ Định : 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.
Tương Tác Thuốc :
  • 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).
Liều Lượng & Cách Dùng : Injection, solution - Intravenous drip
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Foscavir
  • Công ty :
    Sản phẩm biệt dược : Triapten
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00529
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=3415
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507873
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00579
ChemSpider
http://www.chemspider.com/Chemical-Structure.3297.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0186-1906-01
PharmGKB
http://www.pharmgkb.org/drug/PA449706
Wikipedia
http://en.wikipedia.org/wiki/Foscarnet
RxList
http://www.rxlist.com/cgi/generic2/foscarnet.htm
Drugs.com
http://www.drugs.com/cdi/foscarnet.html
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