Labetalol in Essential Hypertension

Larochelle, Pierre; Hamet, Pavel; Hoffman, Brian B.; Küchel, Otto; McKenzie, J. K.; Mitenko, Paul A.; Ri, Ogilvie; Ruedy, John

doi:10.1097/00005344-198011000-00005

Cited by 6 publications

(4 citation statements)

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“…A further increase in the dose to an average of 1,000 mg/day at the end of the 12th week had no additional blood pressure-lowering effect. In agreement with previous investigators, we were unable to detect an alteration of the body weight [20] and of the plasma renin [15,18] after chronic labetalol treatment. Other authors, however, found a marked increased of body weight and a suppression of plasma renin in consequence of an expansion of the extracellular fluid volume during labetalol administration [27].…”

Section: Discussionsupporting

confidence: 93%

“…In the first four weeks of treatment, labetalol administered at a dose of 400 mg/day had a slight effect on the ambulant blood pressure in the lying position. However, labetalol already showed a marked blood pressure-lowering action on the blood pressure in the standing position in the second week, probably as an expression of its e-receptor-blocking properties [15,27]. An increase in the dosage to an average of 850 mg labetalol/day at the end of the eighth week led to a further lowering of blood pressure in which a preferential lowering of the orthostatic blood pressue could no longer be recognized.…”

Section: Discussionmentioning

confidence: 98%

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Sympathetic nervous activity and the pressor effect of noradrenaline under chronic?-?-adrenoceptor blockade with labetalol in hypertension

et al. 1983

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In 14 patients with essential hypertension, the influence of the alpha- and beta-adrenoceptor blocking drug labetalol on blood pressure, heart rate, plasma renin, plasma noradrenaline and pressor effect of exogenous noradrenaline was investigated during long-term treatment. During the initial four weeks of treatment, labetalol at a dose of 400 mg/day showed a slight effect only on supine blood pressure, whereas upright blood pressure was already lowered effectively after the second week of treatment (p less than 0.01). An increase in the mean dose to 850 mg/day had an additional blood pressure-lowering effect (p less than 0.001), whereby a preferential decrease of the orthostatic blood pressure was no longer apparent. Further increase in the mean dose to 1,000 mg/day at the end of the 12th week did not have an additional blood pressure-lowering effect. Body weight, plasma renin and plasma noradrenaline remained unchanged on labetalol treatment in the lowest and the highest dose. There was, however, an increased pressor effect of exogenous noradrenaline, i.e. an alpha-adrenoceptor antagonistic effect of labetalol was not detectable under these conditions. The cause of the increased pressor effect was a reduced elimination of noradrenaline from plasma, which is probably the consequence of an inhibition of the uptake 1 process by labetalol. During long-term treatment with the doses administered, the blood pressure-lowering effect of labetalol appears essentially to be the expression of the beta-adrenoceptor blocking properties of the drug.

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Section: Discussionsupporting

confidence: 93%

Section: Discussionmentioning

confidence: 98%

Sympathetic nervous activity and the pressor effect of noradrenaline under chronic?-?-adrenoceptor blockade with labetalol in hypertension

et al. 1983

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“…In addition, a majority of studies comparing labetalol to placebo have shown a significant antihypertensive effect of labetalol when compared to placebo [58][59][60][61]. Most comparative studies comparing labetalol to diuretics in management of hypertension have shown labetalol to be equivalent or superior to thiazide diuretics [62,63].…”

Section: Essential Hypertenisonmentioning

confidence: 99%

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

Frishman

1988

Cardiovasc Drug Ther

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Labetalol, a combined alpha-beta-adrenergic antagonist, is one of the new group of beta-adrenergic blockers reduces peripheral and coronary vascular resistances while preserving cardiac output. Unlike alpha-adrenergic blockers, labetalol tends to reduce heart rate during rest and exercise. The drug is a potent antihypertensive agent which has been used by mouth and by vein to treat mild, moderate, and severe hypertension, including hypertensive emergencies. Labetalol has a hemodynamic profile which makes it an attractive agent for treating myocardial ischemia. The drug reduces blood pressure, left ventricular wall tension, heart rate, and contractility while preserving or even augmenting coronary blood flow. Studies with labetalol in hypertensive patients with angina have shown it to be more effective than placebo in reducing angina attacks and blood pressure while improving exercise tolerance. The drug appears to have antianginal and antihypertensive effects comparable to atenolol and propranolol. Side effects of treatment are observed and most are related to alpha- and beta-adrenergic blockade. Labetalol also appears to be effective for treatment of normotensive patients with angina and for silent myocardial ischemia. It has no apparent effects on serum lipids and lipoproteins. Labetalol appears to be a useful drug for treating the hypertensive heart and its many complications.

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“…Therefore, serum CPK levels and muscle cramps appear mostly to be related to ISA. Labetalol, a/3-adrenoceptor blocker without ISA but with MSA and a-blocking action, is reported to elevate the serum CPK levels [16], so some unknown pharmacological action of /3-adrenoceptor blockers may contribute to muscle cramps and/or serum CPK levels.…”

Section: Discussionmentioning

confidence: 99%

Muscle cramps and elevated serum creatine phosphokinase levels induced by ?-adrenoceptor blockers

Imai

Watanabe

Hashimoto

et al. 1995

Eur J Clin Pharmacol

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We have assessed the propensity of beta-adrenoceptor blockers to cause muscle cramps and to raise the serum creatine phosphokinase (CPK) level in 78 patients with essential hypertension. After a control period, a beta-adrenoceptor blocker without intrinsic sympathomimetic activity (ISA; propranolol, metoprolol or arotinolol) was administered for three months. Thereafter, the patients were randomised to receive a beta-adrenoceptor blocker with ISA (pindolol or carteolol) for three months or a beta-adrenoceptor blocker without ISA for a further three months. This pattern was continued until all beta-adrenoceptor blockers had been given. At the end of each period, CPK and CPK-MB levels were measured. Of the 78 subjects, muscle cramps occurred in 27 during treatment with pindolol and 32 during treatment with carteolol. No complaints were made by subjects treated with propranolol and arotinolol, but muscle cramps were reported in 2 treated with metoprolol. While muscle cramps were caused both by pindolol and carteolol in 16 subjects, they were caused by either of these drugs in the remainder of the subjects. Muscle cramp occurred mainly in the calves when the patients were in bed at night. Serum CPK and CPK-MB levels increased significantly during treatment with pindolol (control period vs pindolol, CPK = 96 vs 133 IU.ml-1, CPK-MB = 14 vs 18 IU.ml-1) or carteolol (CPK = 117 IU.ml-1, CPK-MB = 18 IU.ml-1) while the levels during treatment with propranolol, arotinolol and metoprolol did not change from those in the control period.(ABSTRACT TRUNCATED AT 250 WORDS)

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Labetalol in Essential Hypertension

Cited by 6 publications

References 0 publications

Sympathetic nervous activity and the pressor effect of noradrenaline under chronic?-?-adrenoceptor blockade with labetalol in hypertension

Sympathetic nervous activity and the pressor effect of noradrenaline under chronic?-?-adrenoceptor blockade with labetalol in hypertension

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

Muscle cramps and elevated serum creatine phosphokinase levels induced by ?-adrenoceptor blockers

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