Comparative trial of labetalol and acebutolol, alone or associated with dihydralazine, in treatment of essential hypertension.

Thibonnier, Marc; Lardoux,; Corvol, Pierre

doi:10.1111/j.1365-2125.1980.tb01081.x

Cited by 15 publications

(2 citation statements)

References 10 publications

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“…A between-patient study in 40 patients found that labetalol 400-800 mg daily was more effective than acebutolol 400-800 mg daily but the combination of acebutolol 800 mg daily plus dihydrallazine 25 or 50 mg twice daily was similar in effect to labetalol up to 800 mg twice daily. In this study a correlation between the initial renin levels and response to acebutolol was noted but there was no such correlation for the response to labetalol (Thibonnier et al, 1980). Labetalol and methyldopa or sympathetic inhibitory drugs Prichard and Boakes (1976) have reported a longterm study largely with patients already under treatment with existing anti-hypertensive drugs.…”

Section: Labetalol and 0-blockers Plus Hydrallazinementioning

confidence: 58%

“…In this study a correlation between the initial renin levels and response to acebutolol was noted but there was no such correlation for the response to labetalol (Thibonnier et al, 1980). Labetalol and methyldopa or sympathetic inhibitory drugs Prichard and Boakes (1976) have reported a longterm study largely with patients already under treatment with existing anti-hypertensive drugs.…”

Section: Labetalol and 0-blockers Plus Hydrallazinementioning

confidence: 91%

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Comparison of labetalol with other anti‐hypertensive drugs.

Prichard¹,

Richards²

1982

Brit J Clinical Pharma

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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.

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Section: Labetalol and 0-blockers Plus Hydrallazinementioning

confidence: 58%

Section: Labetalol and 0-blockers Plus Hydrallazinementioning

confidence: 91%

Comparison of labetalol with other anti‐hypertensive drugs.

Prichard¹,

Richards²

1982

Brit J Clinical Pharma

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The Combined Alpha‐ and Beta‐Adrenergic Blocker Labetalol and Propranolol in the Treatment of High Blood Pressure: Similarities and Differences

Weber

Drayer

Kaufman

1984

The Journal of Clinical Pharma

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Labetalol, an agent with both alpha- and beta-adrenoreceptor blocking properties, and the beta blocker propranolol were each given for one month to groups of 15 patients with essential hypertension. With either treatment, 11 of the 15 patients experienced decreased supine diastolic blood pressure to less than 90 mm Hg without evidence of fluid retention. Propranolol significantly increased plasma concentrations of uric acid and potassium, whereas labetalol significantly increased plasma concentration of high-density lipoproteins (HDL) and decreased the total cholesterol:HDL ratio; neither drug significantly changed renal function. During three additional months of labetalol treatment, there was a slight tendency to orthostatic decreases in systolic blood pressure as compared with the values after the initial month. Labetalol had variable effects on plasma renin activity and aldosterone excretion, but within individual patients the values were constant; there were close correlations between changes measured after one month and after four months for both renin (r = 0.86) and aldosterone (r = 0.94). The manifestations of labetalol's alpha-blocking component appeared to be a small postural effect on systolic blood pressure and an increase in plasma HDL.

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

1983

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Labetalol is a combined alpha- and beta-adrenoceptor blocking agent for oral and intravenous use in the treatment of hypertension. It is a nonselective antagonist at beta-adrenoceptors and a competitive antagonist of postsynaptic alpha 1-adrenoceptors. Labetalol is more potent at beta that at alpha 1 adrenoceptors in man; the ratio of beta-alpha antagonism is 3:1 after oral and 6.9:1 after intravenous administration. Labetalol is readily absorbed in man after oral administration, but the drug, which is lipid soluble, undergoes considerable hepatic first-pass metabolism and has an absolute bioavailability of approximately 25%. There are no active metabolites, and the elimination half-life of the drug is approximately 6 hours. Unlike conventional beta-adrenoceptor blocking drugs without intrinsic sympathomimetic activity, labetalol, when given acutely, produces a decrease in peripheral vascular resistance and blood pressure with little alteration in heart rate or cardiac output. However, like conventional beta-blockers, labetalol may influence the renin-angiotensin-aldosterone system and respiratory function. Clinical studies have shown that the antihypertensive efficacy of labetalol is superior to placebo and to diuretic therapy and is at least comparable to that of conventional beta-blockers, methyldopa, clonidine and various adrenergic neuronal blockers. Labetalol administered alone or with a diuretic is often effective when other antihypertensive regimens have failed. Studies have shown that labetalol is effective in the treatment of essential hypertension, renal hypertension, pheochromocytoma, pregnancy hypertension and hypertensive emergencies. In addition, preliminary studies indicate that labetalol may be of value in the management of ischemic heart disease. The most troublesome side effect of labetalol therapy is posture-related dizziness. Other reported side effects of the drug include gastrointestinal disturbances, tiredness, headache, scalp tingling, skin rashes, urinary retention and impotence. Side effects related to the beta-adrenoceptor blocking effect of labetalol, including asthma, heart failure and Raynaud's phenomenon, have been reported in rare instances.

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Comparative trial of labetalol and acebutolol, alone or associated with dihydralazine, in treatment of essential hypertension.

Cited by 15 publications

References 10 publications

Comparison of labetalol with other anti‐hypertensive drugs.

Comparison of labetalol with other anti‐hypertensive drugs.

The Combined Alpha‐ and Beta‐Adrenergic Blocker Labetalol and Propranolol in the Treatment of High Blood Pressure: Similarities and Differences

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

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