Acyclovir: mechanism of action, pharmacokinetics, safety and clinical applications

Pharmacotherapy. 1983 Sep-Oct;3(5):275-83. doi: 10.1002/j.1875-9114.1983.tb03274.x.


Acyclovir is a new antiviral drug that acts as a specific inhibitor of herpesvirus DNA polymerase. It shows good in vitro activity against herpes simplex and varicella-zoster viruses. The drug may be administered topically to the skin, intravenously, orally, or topically to the eye (only topical and intravenous preparations are currently available). Acyclovir kinetics are described by a two-compartment open model. The drug and its metabolites are excreted by the kidney via glomerular filtration and tubular secretion. Dosage adjustment is required in patients with renal failure. Safety and tolerance studies in animals and humans have shown acyclovir to be very well tolerated. The most important adverse effect is crystalluria and elevated serum creatinine related to bolus intravenous administration. Other reported adverse effects include infusion site inflammation and rash. Topical acyclovir is effective for treating initial genital herpes and mucocutaneous herpes in the compromised host, but has not been shown to be clinically useful for recurrent labial or genital herpes. Intravenous acyclovir is effective for mucocutaneous herpes infections in the compromised host and initial genital herpes in the normal host; it is being evaluated for the treatment of herpes simplex virus encephalitis and varicella-zoster infections. An investigational oral preparation may prove to be effective therapy for both initial and recurrent genital herpes. Acyclovir therapy does not eliminate latent virus or prevent subsequent recurrences.

Publication types

  • Clinical Trial
  • Review

MeSH terms

  • Acyclovir / metabolism
  • Acyclovir / pharmacology
  • Acyclovir / therapeutic use*
  • Administration, Topical
  • Animals
  • Chemical Phenomena
  • Chemistry
  • Clinical Trials as Topic
  • Female
  • Herpes Genitalis / drug therapy
  • Herpes Simplex / drug therapy*
  • Humans
  • Kidney / metabolism
  • Kidney Diseases / metabolism
  • Kinetics
  • Male


  • Acyclovir