ACYCLOVIR ointment

Nazione: Stati Uniti

Lingua: inglese

Fonte: NLM (National Library of Medicine)

Principio attivo:

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

Commercializzato da:

ACTAVIS PHARMA, INC.

INN (Nome Internazionale):

acyclovir

Composizione:

acyclovir 50 mg in 1 g

Via di somministrazione:

TOPICAL

Tipo di ricetta:

PRESCRIPTION DRUG

Indicazioni terapeutiche:

Acyclovir Ointment 5% is indicated in the management of initial genital herpes and in limited non-lifethreatening mucocutaneous HSV infections in immunocompromised patients. Acyclovir Ointment 5% is contraindicated in patients who develop hypersensitivity to the components of the formulation.

Dettagli prodotto:

Each gram of Acyclovir Ointment 5% contains 50 mg acyclovir in a polyethylene glycol base. It is supplied as follows: Store at 15° to 25°C (59° to 77°F) in a dry place.

Stato dell'autorizzazione:

New Drug Application Authorized Generic

Scheda tecnica

ACYCLOVIR- ACYCLOVIR OINTMENT
ACTAVIS PHARMA, INC.
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PRESCRIBING INFORMATION
ACYCLOVIR
OINTMENT 5%
DESCRIPTION
Acyclovir 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 is a white to off-white crystalline powder with the
molecular formula C H N O and a
molecular weight of 225.20. 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 three 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 d