ACYCLOVIR ointment

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

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

Available from:

Glenmark Pharmaceuticals Inc., USA

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 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 USP in a polyethylene glycol base. Acyclovir ointment USP, 5% is a white to off-white translucent ointment. It is supplied as follows: Store at 20° to 25°C (68° to 77°F); excursions permitted to 15° to 30°C (59° to 86°F) [See USP Controlled Room Temperature]. Manufactured by: Glenmark Pharmaceuticals Ltd. Colvale-Bardez, Goa 403 513, India Manufactured for: Glenmark Pharmaceuticals Inc., USA Mahwah, NJ 07430 Questions? 1 [phone] www.glenmarkpharma.com/usa September 2016

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

ACYCLOVIR- ACYCLOVIR OINTMENT
GLENMARK PHARMACEUTICALS INC., USA
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ACYCLOVIR OINTMENT USP, 5%
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, USP 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 225.2 g/mol. 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, USP 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 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