Labetalol: A Review of Its Pharmacology, Pharmacokinetics, Clinical Uses and Adverse Effects

  title={Labetalol: A Review of Its Pharmacology, Pharmacokinetics, Clinical Uses and Adverse Effects},
  author={E P Maccarthy and Saul S. Bloomfield},
  journal={Pharmacotherapy: The Journal of Human Pharmacology and Drug Therapy},
  • E. MaccarthyS. Bloomfield
  • Published 1983
  • Biology, Medicine
  • Pharmacotherapy: The Journal of Human Pharmacology and Drug Therapy
Labetalol is a combined alpha‐ and beta‐adenoceptor blocking agent for oral and intravenous use in the treatment of hypertension. It is a nonselective competitive antagonist at beta‐adrenoceptors and a competitive antagonist of postsynaptic alpha1‐adrenoceptors. Labetalol is more potent at beta than at alpha1 adrenoceptors in man; the ratio of beta‐alpha antagonism is 3:1 after oral and 6.9:1 after intravenous administration. 

Labetalol. A reappraisal of its pharmacology, pharmacokinetics and therapeutic use in hypertension and ischaemic heart disease.

With its broad scope of therapeutic use in hypertension labetalol remains an important therapeutic option, and the drug may well find an additional place in the treatment of myocardial ischaemia if further evidence confirms encouraging preliminary findings.

Survey of Pharmacological Activity and Pharmacokinetics of Selected β-Adrenergic Blockers in Regard to Their Stereochemistry

It could be shown that the activity in the arylaminoethanol and aryloxyaminopropanol group of β-blockers is higher in their (–)-enantiomers as compared with the (+)- enantiomers.

Rising Multiple‐Dose Pharmacokinetics of Labetalol in Hypertensive Patients

The steady‐state plasma drug concentrations are predictable from the pharmacokinetic data and are in good agreement with the observed values.

Single dose pharmacokinetics and pharmacodynamics of oral oxazepam during concomitant administration of propranolol and labetalol.

The oral kinetics of oxazepam after a single 15 mg oral dose was investigated in six healthy volunteers before and during concomitant administration of the beta-adrenoceptor antagonists propranolol and labetalol and it was found that postural sway was affected significantly only by the combination of oxAZepam and proPRanolol.

Labetalol overdose successfully treated with amrinone and alpha-adrenergic receptor agonists.

This case suggests that amrinone may be effective adjunctive therapy for beta-adrenergic receptor blocker overdoses by reversing their negative inotropic effects.

Development and Evaluation of a Physiologically Based Pharmacokinetic Model of Labetalol in Healthy and Diseased Populations

The presented model provides useful quantitative estimates of drug dosing in patients fighting against severe chronic diseases and the disposition of labetalol after IV and oral administration occurring in patients with the hepatic and renal disease was predicted.

The use of intravenous labetalol in the setting of rapid atrial fibrillation secondary to methamphetamine use

Combination alpha and beta blockade using labetalol may be an effective and safe treatment option in patients with methamphetamine associated supraventricular tachydysrhythmias.

Pharmacokinetics and pharmacodynamics of dilevalol

Dilevalol caused significant cardiac β‐blockade for more than 24 hours, but these effects were not altered by cimetidine, and the pharmacokinetic changes are consistent with a decrease in first‐pass extraction of a high clearance drug.

Stereochemical facets of clinical β-blockers: An overview.

This review provides details of stereo-selectivity in the pharmacological behavior of some of β-blockers and their metabolites and highlights the distinction between the therapeutic behavior of the racemic mixtures and pure enantiomers.

Comparative evaluation of efficacy and safety of methyldopa and labetalol in pregnancy-induced hypertension: A meta-analysis

Labetalol is more efficacious and safer as compared to methyldopa, and there was no significant difference in the prevalence of the other maternal side effects.



Labetalol, a new alpha- and beta-adrenoreceptor blocking agent, in hypertension.

It can be concluded that labetalol offers a useful anti-hypertensive effect and that this compound is well tolerated.

The treatment of hypertension by labetalol‐a new alpha‐ and beta‐adrenoreceptor blocking agent

A significant reduction in hypertension was achieved with relatively few adverse reactions and the combination of alpha and beta blockers in labetalol with their mutually opposing characteristics offers an interesting and promising approach to the control of hypertension.

A pilot trial of labetalol (AH 5158A): a combined alpha and beta blocker in treatment of hypertension.

Adequate control of blood pressure was achieved in all nine patients and the only side-effect of note was postural hypotension which necessitated withdrawal of the drug in one patient.

Labetalol: A Review of its Pharmacology and Therapeutic Use in Hypertension

Labetalol may be particularly useful in some patients whose blood pressure is not adequately controlled by β-adrenoceptor blocking drugs alone or combined with a diuretic, but possibly at the expense of a postural hypotensive effect.

Assessment of alpha- and beta-adrenoceptor blocking actions of labetalol.

Isoprenaline dose-response curves plotting increases in heart rate before and after labetalol are suggestive of competitive antagonism at beta-adrenoceptor sites. Phenylephrine dose-response curves


Labetalol is an effective antihypertensive agent, but side effects are common and it has few advantages over drugs presently available.

Pharmacokinetics and pharmacodynamic studies of labetalol in hypertensive subjects.

Plasma levels correlated poorly with the acute effect on BP, raising the possibility of labetalol acting in a deep tissue compartment or alternatively an active metabolite contributing to its effect.

Double-blind trial of labetalol.

A new anti-hypertensive agent (labetalol) with alpha- and beta-adrenoreceptor-blocking properties has been assessed in 30 patients in a general practice, with significant reduction in blood pressure and pulse rate and side-effects were generally mild.

LABETALOL AND BENDROFLUAZIDE: comparison of their antihypertensive effects

The plasma levels of labetalol showed a significant correlation with changes in blood pressure, and plasma level determinations of this drug may be of value in the management of patients who receive antihypertensive agents.