Metoprolol kinetics and dose response in hypertensive patients

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Abstract
The kinetics and dose-response characteristics of metoprolol were examined in a series of hypertensive patients. In 14 the elimination half-life of metoprolol after single 100/mg doses (4.1 .+-. 0.6 h) was prolonged (P < 0.05) after 6-12 wk of therapy (5.6 .+-. 0.7 h). In 5 patients receiving 100 mg twice daily evidence of nonlinear metoprolol kinetics emerged, because the area under the concentration-time curve at steady state was 86.8% more (P < 0.02) than predicted from a single dose. Kinetic data from single doses of metoprolol appear to be a poor predictor of steady-state kinetics. Single metoprolol dosage induced a fall (P < 0.01) in blood pressure with pretreatment levels (163/108), reaching a minimum at 5 h (133/89). During long-term therapy incremental doses of metoprolol between 100 and 600 mg/day in 34 hypertensive patients caused a relatively horizontal dose-response curve at doses > 200 mg/day.

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