Metabolic fate of radioactive acyclovir in humans

Paulo De Miranda, Steven S. Good, Harvey C. Krasny, James D. Connor, Oscar L. Laskin, Paul S. Lietman

Research output: Contribution to journalArticlepeer-review

29 Scopus citations


The metabolic fate and the kinetics of elimination of [8-14C]acyclovir in plasma and blood was investigated in five cancer patients. Doses of 0.5 and 2.5 mg/kg were administered by one-hour intravenous infusion. Radioactivity was distributed nearly equally in blood and plasma. The plasma and blood concentration-time data were defined by a two-compartment open pharmacokinetic model. The overall mean acyclovir plasma half-life and total body clearance ± SD were 2.1 ± 0.5 hours and 297 ± 53 ml/min/1.73 m2. Binding of acyclovir to plasma proteins was 15.4 ± 4.4 percent. The radioactive dose was excreted predominantly in the urine (71 to 99 percent) with less than 2 percent excretion in the feces and only trace amounts of radioactivity in the expired air. Reverse-phase high-performance liquid chromatography indicated that 9-carboxymethoxymethylguanine was the only significant urinary metabolite of acyclovir accounting for 8.5 to 14.1 percent of the dose. A minor metabolite (<0.2 percent of dose) had the retention time of 8-hydroxy-9-(2-hydroxyethoxymethyl)guanine. Unchanged urinary acyclovir ranged from 62 to 91 percent of the dose. There was no indication of acyclovir cleavage to guanine. The renal clearances of acyclovir were three times higher than the corresponding creatinine clearances.

Original languageEnglish (US)
Pages (from-to)215-220
Number of pages6
JournalThe American journal of medicine
Issue number1 PART 1
StatePublished - Jul 20 1982

ASJC Scopus subject areas

  • Medicine(all)


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