ACYCLOVIR ointment

Land: Vereinigte Staaten

Sprache: Englisch

Quelle: NLM (National Library of Medicine)

Wirkstoff:

ACYCLOVIR (UNII: X4HES1O11F) (ACYCLOVIR - UNII:X4HES1O11F)

Verfügbar ab:

TOLMAR Inc.

INN (Internationale Bezeichnung):

ACYCLOVIR

Zusammensetzung:

ACYCLOVIR 50 mg in 1 g

Verabreichungsweg:

TOPICAL

Verschreibungstyp:

PRESCRIPTION DRUG

Anwendungsgebiete:

Acyclovir Ointment, 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, 5% is contraindicated in patients who develop hypersensitivity to the components of the formulation.

Produktbesonderheiten:

Each gram of Acyclovir Ointment USP, 5% contains 50 mg acyclovir in a polyethylene glycol base. It is supplied as follows: 15-g tubes (NDC 63646-300-15) 30-g tubes (NDC 63646-300-30) Store at 20° - 25°C (68° - 77°F); excursions permitted to 15° - 30°C (59° - 86°F) [see USP Controlled Room Temperature] in a dry place. To report SUSPECTED ADVERSE REACTIONS contact Tolmar, Inc. at 1-888-865-6277 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. Manufactured and Distributed by: Tolmar, Inc. Fort Collins, CO 80526 04005027 Rev. 3 03/18

Berechtigungsstatus:

Abbreviated New Drug Application

Fachinformation

ACYCLOVIR- ACYCLOVIR OINTMENT
TOLMAR INC.
----------
ACYCLOVIR OINTMENT USP, 5%
RX ONLY
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.
ANTIVIRAL ACTIVITIES
The quantitative relationship between the _in vitro_ susceptibility of
herpes viruses to
8
11
5
3
antivirals and the clinical response to therapy has not been
established in humans, and
virus sensitivity testing has not been standardized. Sensitivity
testing results, expressed
as the concentration of drug required to