药品详细
Penciclovir(喷昔洛韦)
化学结构式图
中文名
喷昔洛韦
英文名
Penciclovir
分子式
C10H15N5O3
化学名
2-amino-9-[4-hydroxy-3-(hydroxymethyl)butyl]-6,9-dihydro-3H-purin-6-one
分子量
Average: 253.2578
Monoisotopic: 253.117489371
Monoisotopic: 253.117489371
CAS号
39809-25-1
ATC分类
D06B 未知;J05A Direct acting antivirals
药物类型
small molecule
阶段
approved
商品名
Denavir;
同义名
PE2;Penciclovirum [INN-Latin];
基本介绍
Penciclovir is a guanine analogue antiviral drug used for the treatment of various herpesvirus infections. It is a nucleoside analogue which exhibits low toxicity and good selectivity. [Wikipedia]
生产厂家
- Novartis consumer health inc
封装厂家
参考
| Synthesis Reference | Not Available |
| General Reference | Not Available |
剂型
规格
化合物类型
| Type | small molecule |
| Classes |
|
| Substructures |
|
适应症
ANTIVIRALS 抗病毒;
药理
| Indication | Used to treat recurrent cold sores on the lips and face from various herpesvirus invections. |
| Pharmacodynamics | Penciclovir is the active metabolite of the oral product famciclovir. The more favorable results observed with topical penciclovir versus topical acyclovir for the treatment of herpes labialis may be due to the longer intracellular half-life of penciclovir in HSV-infected cells. The activated drug inhibits the viral DNA polymerase. This impairs the ability of the virus to replicate within the cell. |
| Mechanism of action | Penciclovir has in vitro activity against herpes simplex virus types 1 (HSV-1) and 2 (HSV-2). In cells infected with HSV-1 or HSV-2, viral thymidine kinase phosphorylates penciclovir to a monophosphate form. The monophosphate form of the drug is then converted to penciclovir triphosphate by cellular kinases. The intracellular triphosphate of penciclovir is retained in vitro inside HSV-infected cells for 10-20 hours, compared with 0.7-1 hour for acyclovir. in vitro studies show that penciclovir triphosphate selectively inhibits viral DNA polymerase by competing with deoxyguanosine triphosphate. Inhibition of DNA synthesis of virus-infected cells inhibits viral replication. In cells not infected with HSV, DNA synthesis is unaltered. Resistant mutants of HSV can occur from qualitative changes in viral thymidine kinase or DNA polymerase. The most commonly encountered acyclovir-resistant mutants that are deficient in viral thymidine kinase are also resistant to penciclovir. |
| Absorption | Measurable penciclovir concentrations were not detected in plasma or urine of healthy male volunteers (n= 12) following single or repeat application of the 1% cream at a dose of 180 mg penciclovir daily. |
| Volume of distribution | Not Available |
| Protein binding | Less than 20%. |
| Metabolism |
Hepatic
|
| Route of elimination | Not Available |
| Half life | 2 hours |
| Clearance | Not Available |
| Toxicity | Symptoms of overdose include headache, abdominal pain, increased serum lipase, nausea, dyspepsia, dizziness, and hyperbilirubinemia. |
| Affected organisms |
|
| Pathways | Not Available |
理化性质
| Properties | |||||||||||||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| State | solid | ||||||||||||||||||||||||||||||||||||||||||
| Experimental Properties |
|
||||||||||||||||||||||||||||||||||||||||||
| Predicted Properties |
|
||||||||||||||||||||||||||||||||||||||||||
药物相互作用
| Drug | Interaction |
|---|---|
| Aluminium | The multivalent agent decreases the effect of penicillamine |
| Attapulgite | The multivalent agent decreases the effect of penicillamine |
| Digoxin | The multivalent agent decreases the effect of penicillamine |
| Iron | The multivalent agent decreases the effect of penicillamine |
| Kaolin | The multivalent agent decreases the effect of penicillamine |
食物相互作用
Not Available
收藏