Source: Medicines and Medical Devices Safety Authority (NZ) Revision Year: 2023 Publisher: AFT Pharmaceuticals Ltd, Level 1, 129 Hurstmere Road, Takapuna, Auckland, 0622, New Zealand Phone: 0800 423 823 Email: customer.service@aftpharm.com
Aciclovir is an antiviral agent which is active in vitro against Herpes simplex virus (HSV) types I and II. However, the relationship between in vitro sensitivity of herpes viruses to aciclovir and clinical response to therapy has yet to be established. Aciclovir needs to be phosphorylated to the active compound, aciclovir triphosphate, in order to become active against the virus. Such conversion is very limited in normal cells and in addition cellular DNA polymerase is not very sensitive to the active compound. However, in infected cells HSV or VZV-coded thymidine kinase facilitates the conversion of aciclovir to aciclovir monophosphate which is then converted to aciclovir triphosphate by cellular enzymes. Aciclovir triphosphate acts as an inhibitor of, and substrate for, the herpes-specified DNA polymerase, preventing further viral DNA synthesis.
Aciclovir is absorbed through the corneal epithelium and superficial ocular tissues, and achieves significant concentrations in aqueous humour. Small quantities (2-16% of the applied dose) appear in the urine. In animalstudieslow levels of aciclovir could be detected in blood after topical application to the eye.
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.
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