DAVID I. DORSKY, M.D., Ph.D.; CLYDE S. CRUMPACKER, M.D.
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.
DORSKY DI, CRUMPACKER CS. Drugs Five Years Later: Acyclovir. Ann Intern Med. ;107:859–874. doi: 10.7326/0003-4819-107-6-859
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Published: Ann Intern Med. 1987;107(6):859-874.
Infectious Disease, Prevention/Screening.
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Print ISSN: 0003-4819 | Online ISSN: 1539-3704
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