ACYCLOVIR ointment

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

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

Available from:

Mylan Institutional Inc.

INN (International Name):

ACYCLOVIR

Composition:

ACYCLOVIR 50 mg in 1 g

Administration route:

TOPICAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

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.

Product summary:

Each gram of Acyclovir Ointment USP, 5% contains acyclovir USP, 50 mg in a polyethylene glycol base. Acyclovir Ointment USP, 5% is an opaque white to off-white ointment available as follows: 51079-550-68 carton of two 5 g tubes Store at 20° to 25°C (68° to 77°F). [See USP Controlled Room Temperature.] Store in a dry place. Manufactured for: Mylan Institutional Inc. Rockford, IL 61103 U.S.A. Manufactured by: Mylan Institutional Inc. Sugar Land, TX 77478 U.S.A. Revised: 7/2018 ACYCO:5G:R4 1343.4 [pharma code: 3434]

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

ACYCLOVIR- ACYCLOVIR OINTMENT
MYLAN INSTITUTIONAL INC.
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DESCRIPTION
Acyclovir ointment, USP is a synthetic nucleoside analogue active
against herpes viruses.
Acyclovir ointment 5% is a formulation for topical administration.
Each gram of acyclovir
ointment 5% contains 50 mg of acyclovir in a polyethylene glycol (PEG)
base.
Acyclovir, USP is a white to off-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 9-
[(2-Hydroxyethoxy)methyl]guanine; 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
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 inhibit by 50% the growth of
virus i