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20 patients (12 female) with moderately severe essential hypertension [blood pressure during placebo treatment 181 +/- 6 (systolic), 107 +/- 3 (diastolic)] completed a double-blind, cross-over dose-titrated comparison of labetalol and methyldopa. Both drugs reduced lying and standing arterial blood pressure to a similar extent, although only labetalol reduced heart rate. Compliance was high (greater than 95%) with both drugs, and the incidence of subjective adverse effects was similar.

1 Twenty patients with essential hypertension completed a double-blind, dose-tritrated, cross-over comparison of methyldopa and labetalol. 2 Average lying BPs (systolic/diastolic) were reduced by 28/15 mmHg with methyldopa and by 23/15 mmHg with labetalol. 3 Average standing BPs (systolic/diastolic) were reduced by 29/14 mmHg with methyldopa and by 29/15 mmHg with labetalol. 4 Both lying and standing heart rates were reduced with labetalol. 5 It is concluded that the antihypertensive properties of labetalol and methyldopa are similar but that larger patient populations are needed to study the relative incidence of subjective adverse effects.

1 Mean steady‐state plasma concentrations of labetalol (labetalol Css) in 17 hypertensive patients undergoing chronic treatment with this drug, have been examined in relation to dose, fall in BP, and beta‐ blockade. 2 A significant relationship (rs = 0.81, P less than 0.001) was observed between labetalol Css and daily dose. 3 No correlation was found between labetalol Css and antihypertensive response. 4 In thirteen patients, there seemed to be significant relationship between labetalol Css and beta‐blockade (rs = 0.72, P less than 0.005). In three patients, the degree of beta‐blockade was disproportionate to the drug concentration.