Zevin Cream

A white cream with specific odor.
Each 100 g contains: Aciclovir 5 g.

Pharmacology: Pharmacodynamics: ZEVIN (Aciclovir) is a synthetic acyclic nucleoside analogue with in vitro inhibitory activity against herpes simplex type 1 and 2 (HSV-1 and HSV-2), varicella-zoster, Epstein-Barr, and cytomegalovirus. In cell cultures, the inhibitory activity of aciclovir for herpes simplex virus is highly selective.
Mechanism of action: Aciclovir is converted to aciclovir monophosphate, a nucleotide, by herpes simplex virus (HSV)-coded thymidine kinase. Aciclovir monophosphate is converted to the diphosphate by cellular guanylate kinase and to the triphosphate by a number of cellular enzymes. Aciclovir triphosphate interferes with HSV DNA polymerase and inhibits viral DNA replication. The triphosphate can be incorporated into growing chains of DNA by viral DNA polymerase, resulting in termination of the DNA chain. Since aciclovir is preferentially taken up and selectively converted to the active triphosphate form by HSV-infected cells, it is much less toxic to normal uninfected cells.
Pharmacokinetics: Aciclovir is a synthetic nucleoside analogue antiviral drug. It is converted to aciclovir triphosphate, which is the pharmacological active form of the drug in infected cells. It has antiviral activity against herpes simplex virus type 1 and 2, varicella zoster, Epstein-Barr virus, and cytomegalovirus.
Aciclovir is poorly absorbed following oral administration, with peak plasma levels occurring in 1.7 hours. Aciclovir is metabolized in liver.
Plasma protein-binding is low. The half-life is 3.3 hours. Approximately 14% of total dose is excreted unchanged in urine.
Absorption of aciclovir is usually slight following topical application to intact skin. In disease skin (Herpes zoster), moderate plasma concentrations up to 0.28 μg/ml have been reported in patients with normal renal function.
Approximately 9% of the total daily dose may be excreted in the urine.

For the treatment of Herpes simplex virus infection of the skin, including initial and recurrent genital herpes and herpes labialis.

Apply ZEVIN CREAM five times daily at approximately four hourly intervals. ZEVIN should be applied to lesions as early as possible after the start of an infection. Treatment should be continued for 5 days. If healing has not occurred, treatment may be continued for up to 10 days and for recurrent episodes, this should preferably be during the prodromal period or when the lesions first appear.

Overdosage of aciclovir may cause renal dysfunction and eventually renal failure and anuria, according to the precipitation of aciclovir crystals in the renal tubules. If acute renal failure and anuria occur, dosage of the drug should be adjusted and hemodialysis considered until the renal function is restored.

ZEVIN is contraindicated in patients known to be hypersensitive to aciclovir or propylene glycol.

Should avoid sexual contact while visible lesions are present because of the risk of infecting intimate partners.
Should be cautious not to exceed the prescribed dosage.
Do not apply to the mucous membrane eg. in the mouth, eyes, or vagina, as it may be irritant. Particular care should be taken to avoid accidental introduction into the eyes.

Use in pregnancy: Limited data are available on the use of aciclovir in pregnancy.
Caution should therefore be exercised by balancing the potential benefits of treatment against any possible hazard.
Use in lactation: Limited data indicate that aciclovir is distributed into milk following systemic administration. Caution is therefore advised if ZEVIN is to be administered to a nursing woman.

Transient burning or stinging following application of aciclovir cream may occur.
Erythema or mild drying and flaking of the skin have been reported in a small proportion of patients.

Concomitant administration of probenecid and aciclovir has reportedly increased the mean plasma half-life and area under the plasma concentration time curve (AUC) and decreased urinary excretion and renal clearance of aciclovir. This interaction may result from the competitive inhibition of the renal secretion of aciclovir by probenecid.

Store below 30°C. The shelf life period is 3 years.

Topical Antivirals

D06BB03 - aciclovir ; Belongs to the class of topical antivirals used in the treatment of dermatological diseases.

B