Overview
| Generic Names: | PE2; Penciclovirum [INN-Latin] |
|---|---|
| Trade Names: | Denavir |
| PharmGKB Accession Id: | PA450839 |
Description
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 (source: Drug Bank)
Indication
Used to treat recurrent cold sores on the lips and face. (source: Drug Bank)
ATC Therapeutic Categories
- D06BB:Antivirals
- J05AB:Nucleosides and nucleotides excl. reverse transcriptase inhibitors
Pharmacology, Interactions, and Contraindications
Mechanism Of Action
Penciclovir has <i>in vitro</i> 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 <i>in vitro</i> inside HSV-infected cells for 10-20 hours, compared with 0.7-1 hour for acyclovir. <i>in vitro</i> 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. (source: Drug Bank)
Pharmacology
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. (source: Drug Bank)
Absorption, Distribution, Metabolism, Elimination & Toxicity
Biotransformation
Hepatic (source: Drug Bank)
Protein Binding
Less than 20%. (source: Drug Bank)
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. (source: Drug Bank)
Toxicity
Symptoms of overdose include headache, abdominal pain, increased serum lipase, nausea, dyspepsia, dizziness, and hyperbilirubinemia. (source: Drug Bank)
Isomeric SMILES Code:
c1nc2c(=O)[nH]c(nc2n1CCC(CO)CO)N (source: Drug Bank)
A list of non-curated publications that mention this drug along with other genes is available.
A list of non-curated publications that mention this drug along with other drugs is available.
Drug Interactions
| Drug | Description | |
|---|---|---|
| digoxin |
|
The multivalent agent decreases the effect of penicillamine (source: Drug Bank) |
| iron |
|
The multivalent agent decreases the effect of penicillamine (source: Drug Bank) |
| kaolin |
|
The multivalent agent decreases the effect of penicillamine (source: Drug Bank) |
Non-Curated Information
A list of non-curated publications that mention this drug along with other diseases is available.
Additional Datasets
These datasets are minimally curated and are sorted alphabetically by title.
LinkOuts
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Non-Curated Publications
A list of non-curated publications that mention this drug is available.