Pharmacokinetics of Moxonidine After Single and Repeated Daily Doses in Healthy Volunteers

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Abstract
The pharmacokinetics of the centrally acting alpha‐2 agonist moxonidine were investigated in 12 healthy male subjects after single and repeated oral doses (q12h for five days) of moxonidine 0.2 mg. Plasma concentration‐time data followed the general characteristics of a one‐compartment model with first‐order absorption. Peak plasma concentrations of 1.29 ± 0.32 ng/mL were achieved 0.74 ± 0.35 hours after ingestion of a 0.2‐mg tablet. The terminal half‐life of elimination was 2.12 ± 0.58 hours. The oral clearance (CL/F) amounted to 830 ± 171 mL/min with renal elimination being the major route of elimination. No significant differences in pharmacokinetic parameters could he observed following repeated dosing over five days.