Pharmacokinetics of Acyclovir, Antivirus Agent

Abstract

The pharmacokinetics of acyclovir (ACV) was studied in 8 healthy male volunteers. Half of the men were given 5 mg/kg (group 1) and half were given 10 mg/kg (group 2). ACV was dissolved in 180 ml of saline and intravenously perfused for one hour. At the end of the perfusion group 1 and group 2 respectively demonstrated: mean half life value of slow phase (t_1/2 β) of 2.50 and 2.45 hr, and mean area under the plasma concentration-time curve (AUC^∞₀) of 71.6 and 131.3 μmol h/1. Combined data from both groups revealed: mean volume of distribution at the steady state (V_dss) of 47.0 1, a mean whole body clearance of 336.6 ml/min. The mean renal clearance was 242.4 and 221.7 ml/min as determined by the area method and elimination rate method, respectively. These clearances exceeded the normal glomerular filtration rate, indiccating renal secretion of ACV in addition to glomerular filtration. The mean urinary elimination of unchanged ACV was 62.8 and 72.3% of the administered dose within 6 and 48 ht after infusion started, respectively. No clinical or laboratory evidence of toxicity was noted in the 8 subjects examined.