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 147,016 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Labetalol is a combined alpha- and beta-adrenoreceptor blocking agent. A loading dose may be used to antagonize sympathetic overactivity rapidly after surgery and be followed by a continuous infusion to achieve a stable effect. The haemodynamic effects and pharmacokinetics of this method of labetalol administration were studied in six rewarmed, extubated and sedated patients 15 +/- 2 h after aortobifemoral bypass surgery. Patients were monitored with radial and thermistor-tipped pulmonary artery catheters. Labetalol 1.5 mg kg-1 was injected i.v. over 5 min and a maintenance infusion of 0.2 mg kg-1 h-1 was started 30 min later and continued for 5.5 h. Within 5 min of the loading dose, i.v. labetalol induced significant (P less than 0.05) decreases in mean arterial pressure (-32 +/- 11%), in heart rate (-20 +/- 11%) and in cardiac index (-26 +/- 15%) that lasted throughout the infusion. Changes in systemic vascular resistance were not uniform, but an increase was not observed in any patient. Mean stroke volume index and ventricular filling pressures were not significantly affected by labetalol administration. The mean measured steady state plasma concentration (Css) (264 +/- 46 ng ml-1) was higher than predicted (170 ng ml-1) because the clearance (13.1 +/- 2.4 ml kg-1 min-1) was lower than that used to calculate the infusion rate. We conclude that labetalol is an effective antihypertensive agent in the postoperative period. A Css can be achieved rapidly by such i.v. administration and this offers the advantage of inducing rapid and stable haemodynamic effects.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Continuous i.v. infusion of labetalol for postoperative hypertension. Haemodynamic effects and plasma kinetics. 367 53

The antihypertensive effects of intravenous labetalol were evaluated in 59 patients with hypertensive crises or severe hypertension in need of rapid lowering of blood pressure in a multicenter study. Patients appearing with a supine diastolic blood pressure 125 mm Hg or greater, or a supine systolic blood pressure of more than 200 mm Hg received an initial mini-bolus injection (20 mg) of labetalol. This was followed by repeated incremental doses of 20 to 80 mg given at 10 minute intervals to achieve a supine diastolic blood pressure of less than 95 mm Hg or decrease 30 mm Hg or greater, or a satisfactory decrease in systolic blood pressure. Patients were stratified into those who had taken antihypertensive medication within 24 hours and those who had not. The initial mini-bolus injection caused rapid but not abrupt reduction in blood pressure; the baseline mean blood pressure decreased 23/14 mm Hg. Further injections were needed in the majority of patients (mean: 197 mg). The blood pressure reduction after the last dose of labetalol was 55/33 mm Hg. In pretreated patients and in those who had no medication for 24 hours prior to the intravenous labetalol, the response was similar. Heart rate decreased 10 beats per minute in the total population. In patients pretreated with beta-adrenergic blockers, blood pressure response was similar to that in the total group (59/35 versus 55/33 mm Hg), but heart rate remained essentially unchanged. The dose required to achieve the therapeutic effect was less in pretreated patients than in untreated patients, but the duration of action was shorter. No serious adverse effects were encountered even in patients with concomitant diagnoses of acute left ventricular failure, myocardial infarction, stable congestive heart failure, atrial fibrillation, angina pectoris, acute stroke, transient ischemic attack or encephalopathy. Labetalol is a safe and effective treatment for a rapid blood pressure reduction in hypertensive emergencies.
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PMID:Intravenous labetalol in the treatment of severe hypertension and hypertensive emergencies. 613 20

The cardinal haemodynamic disturbance in established hypertension is an increased total peripheral resistance and a subnormal blood flow, particularly during exercise. 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. Labetalol is a unique antihypertensive agent which induces both alpha- and beta-blockade. Numerous studies have shown that when labetalol is given intravenously to patients with mild to moderate essential hypertension, blood pressure falls within a few minutes-partly due to reduction in cardiac output and heart rate and partly due to reduction in total peripheral resistance. In most series the average reduction in blood pressure was 17 to 22%, the reduction in total peripheral resistance 11 to 14%, and the reduction in cardiac output 2 to 10%. Thus, the reduction in cardiac output with labetalol is less than that seen after single-dose injection of beta-blockers without intrinsic sympathomimetic activity. After intravenous injection, the blood pressure-lowering effect is most marked in the upright position and during muscular exercise when cardiac output is usually significantly reduced. Labetalol reduces blood pressure in severe hypertension. Intravenous doses of 0.2 to 0.8 mg/kg bodyweight reduce blood pressure by approximately 20%. This hypotensive effect is partly due to a reduction in total peripheral resistance and partly due to a fall in cardiac index. When the reduction in blood pressure is gradual and moderate (less than 20%), it is mainly produced by a reduction in total peripheral resistance. During long term use labetalol induces haemodynamic changes rather similar to those seen after bolus injection. However, during prolonged use there is a tendency to normalisation in cardiac output and stroke volume; the sustained decrease in blood pressure is mainly due to a reduction in total peripheral resistance. In a recent 6-year follow-up study where 15 patients were studied before treatment and after 1 and 6 years on long term labetalol treatment, a tendency to normalisation of central haemodynamics was found. Over the years total peripheral resistance was gradually reduced by 15 to 20% at rest as well as during exercise. Stroke volume gradually increased and after 6 years of treatment was approximately 10% higher than the pretreatment value. This compensated for the reduced heart rate and no significant reduction in cardiac output was seen either during exercise or at rest.(ABSTRACT TRUNCATED AT 400 WORDS)
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PMID:Pharmacology of combined alpha-beta-blockade. II. Haemodynamic effects of labetalol. 615 90

Thirteen patients with mild essential hypertension, mean age 44 years (range 21-59), were studied during "stress" before and after postsynaptic alpha-adrenoceptor blockade and combined postsynaptic alpha- and non-selective beta-adrenoceptor blockade. Loud broad band noise (100 dBA for 10 min) was used as the stress stimulus. Exposure to noise caused a significant increase in systolic (7%, p less than 0.05), diastolic (9%, p less than 0.01) and mean arterial pressure (6%, p less than 0.01). The blood pressure elevation was caused by an increase in total peripheral resistance (12%, p less than 0.05). There was no significant change in heart rate, stroke volume or cardiac output. The blood pressure response during noise stimulation was not affected by postsynaptic alpha-adrenoceptor blockade (prazosin, 2 mg orally). The hemodynamic reaction pattern, however, was totally reversed. Thus, the cardiac output increased significantly (9%, p less than 0.05), while the total peripheral resistance tended to decrease. Combined postsynaptic alpha- and non-selective beta-adrenoceptor blockade (labetalol, 200 mg orally) inhibited the increase in systolic blood pressure caused by noise, while the diastolic and mean arterial pressures still increased significantly (5%, p less than 0.01). Labetalol effectively blocked the stress-induced increase in total peripheral resistance and there was no significant increase in cardiac output after combined alpha- and beta-adrenoceptor blockade. Exposure to noise caused a significant increase in circulating noradrenaline (20%, p less than 0.05). Plasma adrenaline and plasma renin activity were not affected by noise stimulation. These results suggest that blood pressure elevation is essential during "stress" but that the hemodynamic pattern causing blood pressure elevation may vary and may be affected by pharmacological blockade of various parts of the sympathetic nervous system.
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PMID:Circulatory effects of noise. 633 82

Labetalol is a competitive antagonist of alpha 1-, beta 1-, and beta 2-adrenergic receptors. The hemodynamic effects of the drug include reduced blood pressure, heart rate, and peripheral resistance, with little change in resting cardiac output or stroke volume. In open trials and controlled studies, labetalol was an effective antihypertensive. Labetalol compared favorably with beta-blockers alone or in combination with vasodilators, for the treatment of hypertension. Reductions in heart rate are less pronounced with labetalol as compared with propranolol. Labetalol produces rapid reductions in blood pressure when administered intravenously for severe hypertension. The most frequent adverse reactions to the drug include fatigue, postural symptoms, headache, and gastrointestinal complaints. Labetalol may prove advantageous when vasodilation in addition to beta-blockade is desired, or for selected patients experiencing adverse effects attributable to beta-blockade. Until the clinical profile of labetalol is better defined, the use of the drug should be limited.
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PMID:Labetalol. 635 58

Long-term therapy with oral labetalol, an alpha- and beta-blocking agent, has been shown to effectively lower blood pressure and heart rate without decreasing cardiac output. We examined the hemodynamic effects of the acute intravenous administration of labetalol in nine hypertensive patients. Labetalol (0.6 +/- 0.1 mg/kg) promptly reduced arterial pressure, heart rate, and systemic vascular resistance without change in stroke volume. Heart rate responses to passive tilt and the Valsalva maneuver were significantly blunted. With isometric exercise, heart rate and mean arterial pressure increased significantly during labetalol therapy but less than in the pre-labetalol phase. In eight patients oral labetalol therapy was continued for six weeks (mean dose 1,050 +/- 105 mg/day), and hemodynamic evaluation was repeated. During oral labetalol therapy, decreases in arterial pressure and heart rate were sustained. Systemic vascular resistance was reduced in five of the eight patients. Hemodynamic responses to tilt, Valsalva maneuver, and handgrip were similar to those during intravenous administration. Coronary blood flow decreased, but coronary as well as pulmonary vascular resistances were unchanged. These data show the efficacy of intravenously administered labetalol in lowering blood pressure and systemic vascular resistance promptly. With long-term oral therapy, decreases in blood pressure are sustained. Labetalol does not appear to have significant effects on pulmonary or coronary vascular resistances.
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PMID:Systemic, pulmonary, and coronary hemodynamic effects of labetalol in hypertensive subjects. 663 39

Labetalol was used to treat systemic hypertension (systolic blood pressure above 150 mmHg) in 11 patients with acute myocardial infarction; its haemodynamic effects and tolerance were studied. Increasing doses of labetalol were infused to lower systolic blood pressure to less than 130 mmHg; the optimal rate was then maintained for one hour (mean rate: 2.3 mg/min). Haemodynamic variables were measured before, during, and after labetalol infusion. Labetalol lowered blood pressure in all patients; this effect was related to a decrease both in total systemic resistance (17.7 to 14 IU) and in cardiac index (3.1 to 2.7 1/min per m2); the stroke index remained unchanged and the heart rate was reduced (94 to 81 beats/min). There was no significant change in the mean pulmonary wedge pressure; it was decreased, however, in the six patients with an initial pressure greater than 15 mmHg. The double product was greatly decreased (16 497 to 8598 mmHg x beats per min), which is favourable in acute myocardial infarction. We conclude that labetalol is a drug of choice to treat hypertension in acute myocardial infarction because it is very effective; its haemodynamic effects are likely to reduce myocardial oxygen requirements and suggest that labetalol administration does not worsen moderate left sided heart failure. The drug, however, may reduce the cardiac output.
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PMID:Treatment of hypertension in acute stage of myocardial infarction. Haemodynamic effects of labetalol. 684 14

Aortic rigidity, plasma noradrenaline and adrenaline, and hemodynamic parameters were measured in 48 essential hypertensive patients, 25 younger than 45 (Group I) and 23 of 45 years and over (Group II). Aortic rigidity was determined by the ratio of pulse pressure over stroke volume. Aortic rigidity and hemodynamic parameters were also determined after combined alpha-beta receptor blockade induced by Labetalol (mg 100 IV) or by Propranolol (mg 10 IV) plus Phentolamine (mg 10 IV). The aortic rigidity index was significantly higher in Group II, systolic arterial pressure being significantly higher. All other data, including plasma noradrenaline and adrenaline, were not significantly different in the two groups. In Group II a significant correlation (r = 0.62) was noted between aortic rigidity indexes and plasma noradrenaline values. The alpha-beta receptor blockade induced a decrease of aortic rigidity particularly in Group II, owing to a more marked decrease of systolic arterial pressure. A highly significant correlation was noted in Group II between the changes in aortic rigidity index and the basal plasma noradrenaline levels (r = 0.81). Therefore, the aortic rigidity in essential hypertensive patients older than 45 is influenced by the sympathetic nervous system activity, as judged by plasma noradrenaline levels. This influence seems related to an increase with age of aortic responsiveness to sympathetic stimulation.
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PMID:Aortic rigidity and plasma catecholamines in essential hypertensive patients. 711 58

Basal hemodynamics and plasma catecholamines were measured in 10 patients with systolic hypertension, 7 males and 3 females, aged 38-69 years (Group 1), and in 10 patients with systolic and diastolic hypertension, 7 males and 3 females, aged 40-65 years (Group 2); the same measurements were repeated after acute pharmacological alpha and beta-blockade with Labetalol, 100 mg iv, or Propranolol, 10 mg iv, plus Phentolamine, 10 mg iv. In patients of Group 1 plasma noradrenaline was inversely related to systolic arterial pressure and to stroke index and was directly related to heart rate. In patients of Group 2 plasma noradrenaline was directly related to systolic arterial pressure. After acute alpha and beta-blockade the degree of reduction of systolic arterial pressure was directly related to basal plasma noradrenaline in both groups; systolic arterial pressure was reduced to normotensive levels in 5 patients of Group 1 who had high basal plasma noradrenaline values. These results confirm some of our previous findings and suggest that in some patients with systolic hypertension adrenergic activity is increased and may have a significant role in maintaining high blood pressure values.
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PMID:Adrenergic activity in systolic hypertension. 711 59

Central haemodynamic changes and regional blood flow were studied using the microsphere technique, during labetalol-induced hypotension in dogs anaesthetized with pentobarbitone and fentanyl. Labetalol 15 mg kg-1 decreased mean arterial pressure from an average of 88 mm Hg to 47 mm Hg. Mean pulmonary arterial pressure was unchanged. Cardiac output was reduced by decrease in stroke volume, while heart rate remained unchanged. Myocardial blood flow decreased approximately in parallel with left ventricular work. Perfusion of the brain and kidneys was unchanged.
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PMID:Haemodynamic effects of labetalol-induced hypotension in the anaesthetized dog. 724 22


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