| Item |
Information |
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Drug Groups
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approved |
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Description
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A guanosine analog that acts as an antimetabolite. Viruses are especially susceptible. Used especially against herpes. [PubChem] |
| Indication |
For the treatment and management of herpes zoster (shingles), genital herpes, and chickenpox |
| Pharmacology |
Aciclovir (INN) or acyclovir (USAN, former BAN) is a synthetic deoxyguanosine analog and it is the prototype antiviral agent that is activated by viral thymidine kinase. The selective activity of aciclovir is due to its affinity for the thymidine kinase enzyme encoded by HSV and VZV. |
| Toxicity |
Aciclovir may cause nephrotoxicity (crystallization of aciclovir within renal tubules, elevation of serum creatinine, transient), and neurotoxicity (coma, hallucinations, lethargy, seizures, tremors). Nephrotoxicity and neurotoxicity usually resolve after cessation of aciclovir therapy. However, there is no well-defined relationship between aciclovir concentrations in the blood and these adverse effects. |
| Affected Organisms |
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| Biotransformation |
Hepatic, the only major urinary metabolite that has been detected is 9-carboxymethoxymethylguanine. |
| Absorption |
Oral: bioavailability 10 to 20% |
| Half Life |
2.5-3.3 hours |
| Protein Binding |
9%-33% |
| Elimination |
Acyclovir is cleared renally. |
| References |
| • |
O'Brien JJ, Campoli-Richards DM: Acyclovir. An updated review of its antiviral activity, pharmacokinetic properties and therapeutic efficacy. Drugs. 1989 Mar;37(3):233-309.
[Pubmed]
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| External Links |
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