ACYCLOVIR ointment

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

acyclovir (UNII: X4HES1O11F) (acyclovir - UNII:X4HES1O11F)

Available from:

E. Fougera & Co. a division of Fougera Pharmaceuticals Inc.

INN (International Name):

acyclovir

Composition:

acyclovir 50 mg in 1 g

Administration route:

TOPICAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Acyclovir ointment USP 5% is indicated in the management of initial genital herpes and in limited non- life-threatening mucocutaneous Herpes simplex virus infections in immunocompromised patients. Acyclovir ointment USP 5% is contraindicated in patients who develop hypersensitivity to the components of the formulation.

Product summary:

Each gram of Acyclovir Ointment USP 5% contains 50 mg acyclovir in a polyethylene glycol base. It is supplied as follows: Store at 20°-25°C (68°-77°F) [see USP Controlled Room Temperature]. Store in a dry place. 400214C R12/15 #285

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

ACYCLOVIR- ACYCLOVIR OINTMENT
E. FOUGERA & CO. A DIVISION OF FOUGERA PHARMACEUTICALS INC.
----------
FOUGERA
ACYCLOVIR OINTMENT USP 5%
FOR TOPICAL USE ONLY.
Rx only
PRESCRIBING INFORMATION
DESCRIPTION
Acyclovir is a synthetic nucleoside analogue active against herpes
viruses. Acyclovir
ointment USP 5% is a formulation for topical administration. Each gram
of acyclovir
ointment USP 5% contains 50 mg of acyclovir in a polyethylene glycol
(PEG) base.
Acyclovir is a white, crystalline powder with the molecular formula C
H
N O and a
molecular weight of 225. The maximum solubility in water at 37°C is
2.5 mg/mL. The
pka's of acyclovir are 2.27 and 9.25.
The chemical name of acyclovir is
2-amino-1,9-dihydro-9-[(2-hydroxyethoxy)methyl]-6_H_-
purin-6-one; it has the following structural formula:
VIROLOGY
MECHANISM OF ANTIVIRAL ACTION: Acyclovir is a synthetic purine
nucleoside analogue
with _in vitro_ and _in vivo_ inhibitory activity against herpes
simplex virus types 1 (HSV-1), 2
(HSV-2), and varicella-zoster virus (VZV).
The inhibitory activity of acyclovir is highly selective due to its
affinity for the enzyme
thymidine kinase (TK) encoded by HSV and VZV. This viral enzyme
converts acyclovir
into acyclovir monophosphate, a nucleotide analogue. The monophosphate
is further
converted into diphosphate by cellular guanylate kinase and into
triphosphate by a
number of cellular enzymes. _In vitro_, acyclovir triphosphate stops
replication of herpes
viral DNA. This is accomplished in 3 ways: 1) competitive inhibition
of viral DNA
polymerase, 2) incorporation into and termination of the growing viral
DNA chain, and 3)
inactivation of the viral DNA polymerase. The greater antiviral
activity of acyclovir against
HSV compared to VZV is due to its more efficient phosphorylation by
the viral TK.
®
8
11
5
3
ANTIVIRAL ACTIVITIES: The quantitative relationship between the _in
vitro_ susceptibility of
herpes viruses to antivirals and the clinical response to therapy has
not been established
in humans, and virus sensitivity testing ha