Pharmacokinetics of moxonidine after single and repeated daily doses in healthy volunteers.

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 be observed following repeated dosing over five days.