Aciclovir (INN) (IPA: ) or acyclovir (USAN, former BAN) is a guanine analogue antiviral drug used most commonly for the treatment of herpes simplex virus infection. It is one of the most commonly-used antiviral drugs, and is most commonly marketed under the trade name Zovirax (GSK).
Aciclovir was seen as the start of a new era in antiviral therapy, as it is extremely selective and low in cytotoxicity. Pharmacologist Gertrude B. Elion was awarded the 1988 Nobel Prize in Medicine partly for the development of aciclovir.
Pharmacology
Mechanism of action
Aciclovir differs from previous
nucleoside analogues in that it contains only a partial
nucleoside structure – the sugar ring is replaced by an open-chain structure. It is selectively converted into a monophosphate form by viral
thymidine kinase, which is far more effective (3000 times) in phosphorylation than cellular thymidine kinase. Subsequently, the monophosphate form is further phosphorylated into the active triphosphate form, aciclo-GTP, by cellular
kinases. Aciclo-GTP is a very potent inhibitor of viral
DNA polymerase; it has approximately 100 times higher affinity to viral than cellular polymerase. Its monophosphate form also incorporates into the viral DNA, resulting in
chain termination. It has also been shown that the viral enzymes cannot remove aciclo-GMP from the chain, which results in inhibition of further activity of DNA polymerase. Aciclo-GTP is fairly rapidly metabolised within the cell, possibly by cellular
phosphatases.
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[ Aciclovir ]
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Acyclovir - Fact sheet for HIV and AIDS patients about this antiviral used to treat herpes genitalis, herpes simplex, and herpes zoster.
Acyclovir (Zovirax) - Patient information page about the use of this medication for HIV-related conditions.
DrugDigest: Acyclovir - Information on dosage, usage, side effects, interactions, and drug comparisons including generics when available.
DrugDigest: Zovirax - Information on dosage, usage, side effects, interactions, and drug comparisons including generics when available.
MedlinePlus Drug Information: Acyclovir - Advice for patients on this medication (brand name Zovirax) used to treat herpes infections.
Meta Description: [ Acyclovir ]
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Zovirax - Product information sheets from GlaxoSmithKline, providing prescribing information for acyclovir for administration orally, by injection, or as an ointment.
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