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药品详细

Famciclovir (泛昔洛韦 )

化学结构式图
中文名
泛昔洛韦
英文名
Famciclovir
分子式
Not Available
化学名
2-[(acetyloxy)methyl]-4-(2-amino-9H-purin-9-yl)butyl acetate
分子量
Average: 321.3318
Monoisotopic: 321.143704121
CAS号
104227-87-4
ATC分类
J05A Direct acting antivirals;S01A 抗感染药
药物类型
small molecule
阶段
商品名
Famvir;
同义名
Famciclovirum [INN-Latin];FCV;
基本介绍

Famciclovir is a guanine analogue antiviral drug used for the treatment of various herpes virus infections, most commonly for herpes zoster (shingles). It is a prodrug form of penciclovir with improved oral bioavailability. Famciclovir is marketed under the trade name Famvir (Novartis).

生产厂家
  • Novartis pharmaceuticals corp
  • Teva pharmaceuticals usa
封装厂家
参考
Synthesis Reference Not Available
General Reference Not Available
剂型
Form Route Strength
Tablet Oral
规格
Unit description Cost Unit
Famvir 500 mg tablet 14.39 USD tablet
Famciclovir 500 mg tablet 11.67 USD tablet
Famvir 250 mg tablet 7.16 USD tablet
Famvir 125 mg tablet 6.59 USD tablet
Famciclovir 250 mg tablet 5.81 USD tablet
Famciclovir 125 mg tablet 5.34 USD tablet
化合物类型
Type small molecule
Classes
  • Purines and Purine Derivatives
Substructures
  • Carboxylic Acids and Derivatives
  • Acetates
  • Aliphatic and Aryl Amines
  • Ethers
  • Pyrimidines and Derivatives
  • Imidazoles
  • Heterocyclic compounds
  • Aromatic compounds
  • Purines and Purine Derivatives
  • Cyanamides
适应症
ANTIVIRALS 抗病毒;
药理
Indication For the treatment of acute herpes zoster (shingles). Also for the treatment or suppression of recurrent genital herpes in immunocompetent patients and treatment of recurrent mucocutaneous herpes simplex infections in HIV infected patients.
Pharmacodynamics Famciclovir is a prodrug that undergoes rapid biotransformation to the active antiviral compound penciclovir. Penciclovir is an anti-viral drug which has inhibitory activity against herpes simplex virus types 1 (HSV-1) and 2 (HSV-2) and varicella zoster virus (VZV). Therefore, herpes viral DNA synthesis and replication are selectively inhibited.
Mechanism of action Famciclovir undergoes rapid biotransformation to the active antiviral compound penciclovir, which has inhibitory activity against herpes simplex virus types 1 (HSV-1) and 2 (HSV-2) and varicella zoster virus (VZV). In cells infected with HSV-1, HSV-2 or VZV, viral thymidine kinase phosphorylates penciclovir to a monophosphate form that, in turn, is converted to penciclovir triphosphate by cellular kinases. In vitro studies demonstrate that penciclovir triphosphate inhibits HSV-2 DNA polymerase competitively with deoxyguanosine triphosphate. Consequently, herpes viral DNA synthesis and, therefore, replication are selectively inhibited.
Absorption 77 %
Volume of distribution
  • 1.08卤0.17 L/kg [healthy male subjects following a single intravenous dose of penciclovir at 400 mg administered as a 1-hour intravenous infusion]
Protein binding 20-25%
Metabolism

Hepatic
Route of elimination Active tubular secretion contributes to the renal elimination of penciclovir.
Half life 10 hours
Clearance
  • 36.6 +/- 6.3 L/hr [healthy male]
  • 0.48 +/- 0.09 L/hr/kg [healthy male]
Toxicity Symptoms of overdose include constipation, diarrhea, dizziness, fatigue, fever, headache, nausea, and vomiting.
Affected organisms
  • Human Herpes Virus
Pathways Not Available
理化性质
Properties
State solid
Melting point 102-104 oC
Experimental Properties
Property Value Source
logP 0.6 PhysProp
Predicted Properties
Property Value Source
water solubility 1.32e+00 g/l ALOGPS
logP 0.13 ALOGPS
logP -0.48 ChemAxon Molconvert
logS -2.39 ALOGPS
pKa ChemAxon Molconvert
hydrogen acceptor count 6 ChemAxon Molconvert
hydrogen donor count 1 ChemAxon Molconvert
polar surface area 122.22 ChemAxon Molconvert
rotatable bond count 9 ChemAxon Molconvert
refractivity 81.54 ChemAxon Molconvert
polarizability 32.83 ChemAxon Molconvert
药物相互作用
食物相互作用
  • Take without regard to meals.

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