Comparison of labetalol with other anti‐hypertensive drugs.

Abstract

1 The anti‐hypertensive effects of labetalol have been compared and contrasted with other groups of anti‐hypertensive drugs in this review of the published literature. 2 The data show that the pharmacological and haemodynamic profile of labetalol in man is distinctly different from that of other specific anti‐hypertensive agents; namely the properties of competitive alpha‐and beta‐adrenoceptor blockade leading to haemodynamic effects of reduced blood pressure and peripheral vascular resistance with little accompanying changes in resting heart rate or cardiac output. 3 The anti‐hypertensive effects of labetalol are dose related. In fixed dose comparative studies equivalent anti‐ hypertensive effects to those of labetalol have been shown for individual drugs of the beta‐adrenoceptor‐blocking and diuretic groups. In dose titration studies, equivalent anti‐hypertensive effects at given doses of labetalol have been demonstrated for drugs of the following types: beta‐adrenoceptor blockers, beta‐blockers plus diuretics, methyldopa, adrenergic neurone blockers and the combination of beta‐blockers plus a peripheral vasodilator. 4 Comparing side‐effect liabilities, it is clear that quantitatively labetalol produces no greater burden of side‐effects than drugs of the beta‐adrenoceptor‐ blocking group. Qualitative differences, however, do exist; in particular, symptomatic postural hypotension is dose related and is more likely to occur when excessive doses (greater than 2 g daily) are used.

Labetalol: the nineteen‐eighties.

“…These various studies generally confirm the consensus of earlier reports showing that blood pressure reduction is mainly due to reduced peripheral resistance, with little accompanying change in resting heart rate or cardiac output (Prichard & Richards, 1982). Significant lowering of plasma renin and aldosterone was also confirmed (Fagard et al, 1982).…”

“…Cardiac output was not significantly altered in these acute studies. Cohn et al (1982) (Prichard & Richards, 1982). Significant lowering of plasma renin and aldosterone was also confirmed (Fagard et al, 1982).…”

Properties of labetalol, a combined ?-and ?-blocking agent, relevant to the treatment of myocardial ischemia

“…Labetalol, in both fixed and individually titrated doses, has been used outside the United States since 1975 for the management of mild, moderate, and severe hypertension [52][53][54][55]. A number of investigators using labetalol have reported the drug to be at least as effective in lowering blood pressure as a wide range of other antihypertensive drugs.…”

“…Multiple reports identify the nature and frequency of side effects with labetalol [1,54,68,75,89,90]. Side effects are generally mild and self-limited.…”

Combined α/β‐Blockade: An Underused Approach to the Treatment of Resistant Hypertension

“…Earlier studies did not find the antihypertensive effect of combined //β‐blockade with labetalol to be significantly greater than that of β‐blocker monotherapy 15 . However, labetalol is lipophilic and subject to considerable first‐pass hepatic metabolism, with low bioavailability in the range of 25% to 33%, and with considerable interindividual variation in bioavailability 16,17 .…”