País: Austrália
Língua: inglês
Origem: Department of Health (Therapeutic Goods Administration)
aciclovir
GlaxoSmithKline Australia Pty Ltd
Registered
1 ZOVIRAX ® TABLETS AND ZOVIRAX ® DISPERSIBLE TABLETS NAME OF THE DRUG: Aciclovir _Chemical name:_ 9-((2-hydroxyethoxy)methyl)guanine _Chemical Structure _ N HN N N O H 2 N O HO _ _ _CAS Number_: 59277-89-3 DESCRIPTION: Aciclovir is a synthetic acyclic purine nucleoside analogue. It is a white crystalline powder slightly soluble in water and practically insoluble in most organic solvents. The chemical structure of aciclovir is: Each Zovirax tablet contains 200 mg, 400 mg or 800 mg of aciclovir. Zovirax Dispersible Tablets (200 mg, 400 mg and 800 mg) contain the excipients cellulose- microcrystalline, aluminium magnesium silicate, sodium starch glycollate, povidone, magnesium stearate, Opadry Complete film coating system White Y-1-7000 and macrogol 8000. Zovirax 200 mg Tablets contain the excipients cellulose-microcrystalline, lactose monohydrate, magnesium stearate, povidone and sodium starch glycollate. Zovirax 400 mg and 800 mg Tablets contain the excipients cellulose-microcrystalline, magnesium stearate, povidone and sodium starch glycollate. PHARMACOLOGY: MICROBIOLOGY: Aciclovir is an antiviral agent which is active _in vitro_ against _Herpes simplex_ virus (HSV) types I and II and _Varicella _ _zoster_ virus (VZV), the latter being considerably less sensitive. The relationship between the level of _ in vitro_ sensitivity of herpes viruses to aciclovir and clinical response to therapy has not been adequately established. Development of resistance by HSV to aciclovir has been documented. 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 2 triphosphate by cellular enzymes. Aciclovir triphosphate acts as an inhibitor of, and substrate for Leia o documento completo