title: Drugs five years later: acyclovir.
abstract: In the 5 years since its release for clinical use, acyclovir (9-[2-hydroxyethoxymethyl]guanine) has proved to be a safe and effective agent for therapy of herpes simplex and varicella-zoster infections. The drug's availability in topical, oral, and intravenous preparations has allowed its use in a range of clinical situations. Acyclovir must be phosphorylated by viral thymidine kinase in infected cells, where it then acts to inhibit viral DNA replication specifically. Epstein-Barr virus and human cytomegalovirus infections do not seem to respond to acyclovir therapy, although in-vitro effects on these viruses may be seen. Acyclovir is well absorbed and distributed, with cerebrospinal fluid levels 50% that of plasma. Clearance is almost entirely by the renal route, with a half-life of 20 hours in the anuric patient. Acyclovir has an excellent safety profile, its major adverse effect being transient serum creatinine elevations during high-dose intravenous use. Major uses include treatment of primary and recurrent genital herpes and herpes encephalitis and prophyllaxis and therapy of mucocutaneous herpes and varicella-zoster infections in immunocompromised patients. Resistance to acyclovir in herpes simplex virus is rarely encountered and does not seem to be due to long-term chronic suppressive therapy.
authors.affiliation: Department of Medicine, Beth Israel Hospital, Harvard Medical School, Boston, Massachusetts.
authors.forename: D I
authors.initials: DI
authors.lastname: Dorsky
authors.forename: C S
authors.initials: CS
authors.lastname: Crumpacker
mesh_terms: D000212:Acyclovir / Q000009:adverse effects / Q000031:analogs & derivatives / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use; D002644:Chickenpox / Q000188:drug therapy; D004347:Drug Interactions; D004352:Drug Resistance, Microbial; D015774:Ganciclovir; D006561:Herpes Simplex / Q000188:drug therapy; D006562:Herpes Zoster / Q000188:drug therapy; D006564:Herpesviridae / Q000187:drug effects; D006801:Humans; D011183:Postoperative Complications / Q000517:prevention & control; D014180:Transplantation
chemical_list: D015774:Ganciclovir; D000212:Acyclovir