Species differences in the disposition of acyclovir

摘要: The disposition of acyclovir was investigated in several species. drug well distributed into all the tissues, including brain, mice and rats. Binding to plasma proteins 36 percent or lower. After intravenous bolus dosing (20 mg/kg) dogs, concentration-time profile, determined by radioimmunoassay, showed a biphasic decline with half-life elimination phase 2.3 +/- 0.1 hours. volume distribution (Vd beta) 1.2 0.2 liters/kg indicated tissues. Marked species differences were observed gastrointestinal absorption biotransformation acyclovir. Oral produced better dogs than rats rhesus monkeys. More 95 radioactivity urine derived from 14C-acyclovir parenteral dose recovered as unchanged mice, rats, dogs. Minor urinary metabolites characterized high-performance liquid chromatography 9-carboxymethoxymethylguanine (CMMG) 8-hydroxy-9-(2-hydroxyethoxymethyl)guanine. In other species--guinea pig, rabbit, monkey--up 40 consisted these metabolites.