Effects of labetalol and propranolol on blood pressure at rest and during isometric and dynamic exercise

Nyberg, G.; Vedin, A; Wilhelmsson, Claes

doi:10.1007/bf00605625

Cited by 8 publications

(2 citation statements)

References 9 publications

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“…81 The influence of intravenous labetalol and propranolol on the blood pressure response to isometric and dynamic exercise was examined in a study of young normotensive subjects. 86 Labetalol, but not propranolol, significantly decreased the hypertensive response to exercise. In another study labetalol, but not propranolol, reduced the hypertensive response to orgasm in female subjects.a7 The increase in blood pressure due to psychic stress is also re- duced by labetalol, and this effect is attributed to its alpha-adrenoceptor blocking property.88 During dynamic forearm exercise, labetalol produced a decrease in forearm blood flow and an increase in calculated vascular ~esistance.~~ In this study, however, labetalol produced a decrease in forearm oxygen uptake that suggested an increase in mechanical efficiency.…”

Section: Hemodynamic Effectsmentioning

confidence: 82%

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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Section: Hemodynamic Effectsmentioning

confidence: 82%

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

1983

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“…Isometric exercise, such as sustained handgrip, is a potent stimulus for both systolic and diastolic bloodpressure rises. /?-blockers have previously been found not to attenuate the blood-pressure rise during handgrip (1 1); however, a single-dose study with labetalol showed such attenuation in both normotensive and hypertensive subjects (13).…”

Section: Introductionmentioning

confidence: 95%

Effects of labetalol and propranolol on the peripheral circulation in hypertensive patients

Nyberg

Berglund

1982

Journal of Internal Medicine

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ABSTRACT. Eleven patients with essential hypertension participated in a double–blind cross–over comparison of labetalol (L) and propranolol (P). Each drug was given for 5–8 weeks. The dose reducing the supine diastolic blood pressure when given b.d. to or below 90 mm Hg was titrated out. At the end of each period, isometric exercise (sustained handgrip) and calf plethysmography were performed. L (mean daily dose 636 mg) was slightly more effective in lowering supine and standing blood pressure than P (mean dose 276 mg). There was no significant difference between the drugs in their effect on the blood–pressure response to handgrip. However, compared with no treatment, L attenuated the blood–pressure rise at near–maximal handgrip; this has not been reported with other β–blockers. Resting vascular resistance and basal vascular tone were significantly lower (20%, p < 0.05) during treatment with labetalol than when the patients were taking propranolol. – The differences may be explained by the α–receptorblocking action of labetalol.

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Drugs Acting on Multiple Receptors: β-Blockers with Additional Properties

Sponer¹,

Bartsch²,

Hooper³

1990

Pharmacology of Antihypertensive Therapeutics

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Effects of labetalol and propranolol on blood pressure at rest and during isometric and dynamic exercise

Cited by 8 publications

References 9 publications

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

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

Effects of labetalol and propranolol on the peripheral circulation in hypertensive patients

Drugs Acting on Multiple Receptors: β-Blockers with Additional Properties

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