Bethanidine Dose, Plasma Levels, and Antihypertensive Effects

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Abstract
Bethanidine dose, plasma levels and hypotensive effects were evaluated in 12 hypertensive patients. Diuretic therapy with benzthiazide was started 2 wk before and continued during the study. Bethanidine was given 3 times daily. After 2-12 mo. of therapy in 11 of the patients, the mean standing diastolic pressure was reduced from 112 to 91 mm Hg. The mean total daily bethanidine dose was 79 mg (range 30-150 mg). The mean plasma bethanidine was 0.65 .mu.M (range 0.1-2.8 .mu.M), which correlated with the bethanidine dose. There was less correlation between dose and antihypertensive effect. The effects of sudden withdrawal from chronic bethanidine dosing were observed in 6 patients. The orthostatic effect of bethanidine was lost within 12 h, but the half-time of elimination of bethanidine from plasma was 39 h. Based upon the present findings, recommendations are presented for initiation and maintenance of antihypertensive therapy with bethanidine.