DENAVIR penciclovir cream

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

PENCICLOVIR (UNII: 359HUE8FJC) (PENCICLOVIR - UNII:359HUE8FJC)

Available from:

New American Therapeutics, Inc

INN (International Name):

PENCICLOVIR

Composition:

PENCICLOVIR 10 mg in 1 g

Prescription type:

PRESCRIPTION DRUG

Authorization status:

New Drug Application

Summary of Product characteristics

DENAVIR- PENCICLOVIR CREAM
NEW AMERICAN THERAPEUTICS, INC
----------
DENAVIR
BRAND OF
PENCICLOVIR CREAM, 1%
FOR DERMATOLOGIC USE ONLY
RX ONLY
PRESCRIBING INFORMATION
DESCRIPTION
_Denavir_ (penciclovir) cream 1% contains penciclovir, an antiviral
agent active against herpes viruses.
_Denavir_ is available for topical administration as a 1% white cream.
Each gram of _Denavir_ contains
10 mg of penciclovir and the following inactive ingredients:
cetomacrogol 1000 BP, cetostearyl
alcohol, mineral oil, propylene glycol, purified water and white
petrolatum.
Chemically, penciclovir is known as
9-[4-hydroxy-3-(hydroxymethyl)butyl]guanine. Its molecular
formula is C
H N O ; its molecular weight is 253.26. It is a synthetic acyclic
guanine derivative and
has the following structure:
Penciclovir is a white to pale yellow solid. At 20°C it has a
solubility of 0.2 mg/mL in methanol,
1.3 mg/mL in propylene glycol, and 1.7 mg/mL in water. In aqueous
buffer (pH 2) the solubility is
10.0 mg/mL.
Penciclovir is not hygroscopic. Its partition coefficient in
n-octanol/water at pH 7.5 is 0.024 (logP = -
1.62).
CLINICAL PHARMACOLOGY
MICROBIOLOGY
MECHANISM OF ANTIVIRAL ACTIVITY: The antiviral compound penciclovir
has _in vitro_ inhibitory 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 which, in turn, is converted
to penciclovir triphosphate by cellular kinases. _In vitro_ studies
demonstrate that penciclovir triphosphate
inhibits HSV polymerase competitively with deoxyguanosine
triphosphate. Consequently, herpes viral
®
10
15
5
3
DNA synthesis and, therefore, replication are selectively inhibited.
ANTIVIRAL ACTIVITY _IN VITRO_ AND _IN VIVO_: In cell culture studies,
penciclovir has antiviral activity against
HSV-1 and HSV-2. Sensitivity test results, expressed as the
concentration of the drug required to inhibit
growth of the virus by 50% (IC
) or 99% (IC
) in cell culture, vary depending upon a number