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

@article{Brogden2012LabetalolAR,
  title={Labetalol: A Review of its Pharmacology and Therapeutic Use in Hypertension},
  author={Rex N. Brogden and Rennie C. Heel and Trevor M. Speight and Graeme S. Avery},
  journal={Drugs},
  year={2012},
  volume={15},
  pages={251-270}
}
SummarySynopsis: Labetalol1 is an orally active adrenoceptor blocking drug which is a competitive antagonist at both α- and β-adrenoceptor sites. Its β-blocking effects resemble those of propranolol, but its overall haemodynamic effects are akin to those of a comination of propranolol and an α-adrenoceptor blocking drug such as phenoxybenzamine. Unlike with conventional β -adrenoceptor blocking drugs, acute administration of labetalol reduces peripheral vascular resistance and blood pressure… Expand
Pharmacology of labetalol in experimental animals.
TLDR
On the basis of this profile, it is proposed that labetalol lowers blood pressure in human subjects by three independent mechanisms: (1) beta blockade, (2) alpha blockade, and (3) direct vasodilatation. Expand
Adrenoceptor Blocking Drugs: Clinical Pharmacology and Therapeutic Use
TLDR
The principal usefulness of α-adrenoceptor antagonists is in the management of phaeochromocytoma — preoperative preparation, prevention of paroxysmal hypertension during surgery and prolonged treatment of cases not amenable to surgery, as potentially they may cause serious adverse reactions. Expand
Anti-anginal and beta-adrenoceptor blocking drugs
TLDR
This chapter provides an overview of the adverse effects of anti-anginal and beta-adrenoceptor blocking drugs, and peyronie's disease of the penis has now been observed several times in patients taking beta- adrenergic blockers. Expand
Labetalol: an alpha- and beta-adrenoceptor blocking drug.
TLDR
Side effects typical of beta-blockers are less prominent with labetalol in the usual antihypertensive doses, however, occasional mild vasodilating, alpha-blocking, and other nonspecific effects are best managed with careful dose titration. Expand
Mechanism of antihypertensive action of dilevalol compared with that of "cardioselective" beta-blocking agents.
TLDR
The main mechanism of antihypertensive action for dilevalol is vasodilation, in contrast to the cardioselective agents, which is beta blockade. Expand
β-Adrenergic blocking agents with α-adrenergic blocking and vasodilator activity (survey)
~o types of adrenerBic blocking agents are eurrently being used for the treatment of cardiovascular diseases: ~-adrenergic blockers (~-AB) and ~-adrenergic blockers (~-AB). The principalExpand
Combined effects of phenoxybenzamine and propranolol in hypertensive rats.
TLDR
The results did not support the above hypothesis, at least when the blockade was caused with PBZ and PPL, and the combined treatment increased side-effects, typically seen as urinary incontinence. Expand
Pharmacology of Combined α-β-Blockade II
TLDR
The spontaneously occurring changes in central haemodynamics have been followed in young males with essential hypertension over a 17-year period: a gradual increase in total peripheral resistance and blood pressure, and a gradual fall in cardiac output and stroke volume, have been demonstrated. Expand
Continuous i.v. infusion of labetalol for postoperative hypertension. Haemodynamic effects and plasma kinetics.
TLDR
It is concluded that labetalol is an effective antihypertensive agent in the postoperative period and can be achieved rapidly by such i.v. administration as offers the advantage of inducing rapid and stable haemodynamic effects. Expand
A comparison and an investigation of a potential synergistic effect of labetalol and bethanidine in patients with mild hypertension.
TLDR
The effects of labetalol, bethanidine and combined treatment with both drugs were compared in a within-patient randomized cross-over study in mild essential hypertension and no evidence of synergism was observed. Expand
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References

SHOWING 1-10 OF 98 REFERENCES
Treatment of hypertension with labetalol.
TLDR
Raynaud's phenomenon, which had complicated previous beta-blocker therapy in some patients, improved with labetalol and reduced heart rate in patients who were not on previous or concomitant beta- blocker therapy. Expand
Labetalol (AH5158), a competitive alpha- and beta-receptor blocking drug, in the management of hypertension.
TLDR
In a direct comparison with intravenous propranolol, labetalol was less effective in lowering plasma angiotensin II, but more effective in reducing blood pressure, and was similarly effective in controlling a hypertensive crisis following clonidine withdrawal. Expand
The effects of oral AH 5158, a combined α and β-adrenoceptor antagonist, in healthy volunteers.
TLDR
It is concluded that the pharmacological profile of this combined α- and β-adrenoceptor antagonism suggests a potential therapeutic role as an antihypertensive drug. Expand
Hemodynamic Effects of Labetalol, an Alpha and Beta Adrenergic Blocking Agent, in Hypertensive Subjects
TLDR
It is indicated that labetalol is an antihypertensive drug that exerts both alpha and beta adrenergic blocking properties and deserves further clinical trials in the treatment of hypertension and angina pectoris. Expand
THE EFFECT OF LABETALOL IN THE TREATMENT OF SEVERE DRUG‐RESISTANT HYPERTENSION
TLDR
Twenty‐two hypertensive patients from a large clinic, who were resistant to conventional therapy, were entered into this study and it was suggested that, if blood pressure control is not achieved with a thiazide diuretic and a beta‐ blocking drug, then labetalol should be introduced and the beta‐blocking drug should be withdrawn. Expand
Effects of intravenous labetalol on blood pressure, angiotensin II and aldosterone in hypertension: comparison with propranolol.
TLDR
In a cross-over comparison in five patients against 10 mg of propranolol intravenously, labetalol was more effective in lowering blood pressure, but less effective in lowered pulse rate or plasma angiotensin II. Expand
Controlled comparison of labetalol and propranolol in the management of severe hypertension.
TLDR
Labetalol, in conjunction with diuretic therapy, was at least as effective in lowering blood pressure in patients with severe hypertension, and initially induced a number of side-effects, predominantly related to alpha-adrenoreceptor blockade, which disappeared by the end of the trial. Expand
Acute effect of intravenous labetalol in the treatment of systemic arterial hypertension.
TLDR
Labetalol reduced the blood pressure when administered intravenously and thus merits further investigation as a treatment for acute hypertensive crises. Expand
LABETALOL COMPARED WITH PRINDOLOL PLUS HYDRALLAZINE IN THE TREATMENT OF HYPERTENSION: A DOUBLE‐BLIND CROSS‐OVER STUDY
TLDR
Labetalol is a useful hypotensive drug with effect similar to that of a combination of a beta‐adrenoceptor blocking drug and a vasodilator. Expand
Intravenous labetalol in hypertensive patients treated with beta-adrenoreceptor-blocking drugs.
TLDR
It is concluded that intravenous labetalol at a dose of 2 mg/kg is safe and effective in rapidly reducing blood pressure in patients already receiving beta-adrenoreceptor-blocking drugs. Expand
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