Source: Medicines Authority (MT) Revision Year: 2021 Publisher: AGEPHA Pharma s.r.o, Diaฤพniฤnรก cesta 5, Senec, 903 01, Slovakia
Pharmacotherapeutic group: Ophthalmologicals, antiinfectives, antivirals, Aciclovir
ATC-Code: S01AD03
Aciclovir is a purine nucleoside analogue and shows in vitro high activity against herpes simplex virus type 1 and 2, as well as against the Varicella-Zoster virus.
In the Herpes infected cells, aciclovir is phosphorylated to monophosphate by viral thymidine kinase in a first step. In further steps, it is converted to di- and triphosphate with participation of the cell’s own enzyme. On the one hand, Acyclovir triphosphate inhibits the viral DNA polymerase and on the other hand it gets integrated into the viral DNA instead of deoxyguanosine triphosphate which results in a disruption of the viral DNA synthesis.
Due to the fact that aciclovir is preferentially taken up by Herpes infected cells and the selective conversionto the active triphosphate form, there is low toxicity to human cells that are not affected by the virus.
Aciclovir is rapidly absorbed by the corneal epithelium and the superficial ocular tissues, penetrates into the aqueous humor and reaches there a therapeutic level of about 7.5 mol/l.
It has not been possible to detect aciclovir in the blood by existing methods after topical application to the eye. However, trace quantities may be measured in the urine. These levels are not clinically significant.
Aciclovir is metabolized by the enzyme aldehyde dehydrogenase to 9-Carboxymethoxymethylguanin.
Aciclovir is excreted via the kidneys, both by glomerular filtration and tubular secretion.
The results of a wide range of mutagenicity tests in vitro and in vivo indicate that aciclovir does not pose a genetic risk to man.
Aciclovir was not found to be carcinogenic in long-term studies in the rat and the mouse. Largely reversible adverse effects on spermatogenesis in association with overall toxicity in rats and dogs have been reported only at doses of aciclovir greatly in excess of those employed therapeutically. Two-generation studies in mice did not reveal any effect of orally administered aciclovir on fertility.
Systemic administration of aciclovir in internationally accepted standard tests did not produce embryotoxic or teratogenic effects in rabbits, rats or mice.
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