Drug Groups

approved

Description

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

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

External Links