Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0085580 (essential hypertension)
14,686 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The acute haemodynamic effects of the non-selective beta-adrenoceptor antiagonist pindolol which has considerable intrinsic sympathomimetic activity (ISA), were studied in 10 patients with essential hypertension for 24 h. One hour after oral dosing (10 mg), the drug reduced supine arterial pressure significantly. The maximum antihypertensive effect was observed after 3-4 h (-15 +/- 3%, P less than 0.001). The fall in arterial pressure was associated with a 25% reduction of systemic vascular resistance (P less than 0.001) after 24 h. By that time cardiac output was increased by 16 +/- 5% (P less than 0.05). Cardiac filling pressures and pulmonary artery pressure did not change. The vasodilator effect of pindolol cannot easily be explained by suppression of plasma renin activity since changes in arterial pressure and plasma renin were inversely correlated (r = -0.58, P less than 0.001). Despite the antihypertensive and vasodilator effect of pendolol, plasma noradrenaline did not rise. The rapid fall in arterial pressure and systemic vascular resistance may be explained by the absence of an initial reflex vasoconstriction which normally follows blockade of cardiac beta-receptors. This may be related to ISA on cardiac and vascular postsynaptic beta-receptors. Concomitant blockade of central and/or peripheral presynaptic beta-receptors is suggested by the absence of a rise in plasma noradrenaline and may contribute to the vasodilator action of pindolol.
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PMID:Direct 24-hour haemodynamic monitoring after starting beta-blocker therapy: studies with pindolol in hypertension. 610 Jul 55

Thirteen beta-blocking agents with different pharmacological properties were administered orally to 161 outpatients with essential hypertension for 5 weeks to assess their hemodynamic effects. Cardioselective ones, such as atenolol, metoprolol and acebutolol, reduced mean blood pressure (MBP) and the cardiac index. (CI) without any changes of the total peripheral resistance index. (TPRI). In the total 44 patients treated with these drugs, a positive correlation (r = 0.529, p less than 0.005) was found between the decrease in MBP and that of TPRI, but the decrease in MBP did not correlate with that of CI. Effects of non-cardioselective ones were classified arbitrarily into the following 3 patterns: 1) reduction of CI of more than 0.50 L/min/m2 and a slight increase of TPRI by more than 150 dyne . sec . cm-5 . m2 (nadolol, propranolol, o.prenolol and penbutolol), 2) reduction of TPRI by more than 150 dyne . sec . cm-5 . m2 (pindolol, bunitrolol and labetalol) and 3) the intermediate hemodynamic responses between the two patterns described above (carteolol, bupranolol and bufetolol). In all these 3 groups, the decrease in MBP correlated with that of TPRI (the first group, n = 45, r = 0.557, p less than 0.005; the second, n = 37, r = 0.525, p less than 0.005; the third, n = 35, r = 0.612, p less than 0.005), but did not correlate with the decrease of CI. These results suggest that the antihypertensive effects of beta-blocking agents mainly depend on the reduction of peripheral resistance, although their pharmacological properties are not uniform and their cardiodepressant effects are variable. Reduction of cardiac performance with these beta-blocking agents seemed to be a consequence of overall pharmacological actions including beta-receptor blockade, central effects and membrane stabilizing effects, and it may be antagonized by intrinsic sympathomimetic activity and the reduction in afterload for the heart. Vascular beta-receptor blocking action may play a part in decreasing the degree of reduction of the total peripheral resistance index, while their intrinsic sympathomimetic action on the vascular site may induce vasodilating effects.
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PMID:Possible significance of the pharmacological differentiation of beta-blocking agents in hemodynamic effects in essential hypertension. 613 16

In 8 ambulatory patients with stable essential hypertension (WHO grade I and II) the effects of a new beta-blocker with marked sympathomimetic activity on arterial blood pressure, creatinin clearance and renal plasma flow, as measured by total PAH clearance (constant infusion technique), were studied. In contrast to previous findings no significant reduction in creatinin clearance or renal blood flow was observed during a 3-5 weeks' observation period. The small reduction in calculated renal vascular resistance was not statistically significant. In addition to its postulated peripheral vasodilatory effect, bufuralol appears to interfere less than propranolol with renal hemodynamics and renal excretory function.
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PMID:[Bufuralol: do beta blockers reduce blood circulation in the kidneys?]. 613 56

Bucindolol is a newly developed, nonselective beta-adrenergic blocking agent with intrinsic sympathomimetic activity and direct vasodilator properties. In 14 patients with mild to moderate essential hypertension, the effects of bucindolol, hydrochlorothiazide and their combination on blood pressure (BP), heart rate (HR) and parameters of the renin-aldosterone system were compared with those after placebo. Bucindolol's antihypertensive effect was evident within the first hour after drug administration, maximal at 2 to 3 hours, and lasted for as long as 12 hours. Compared with placebo values (108 +/- 5 mm Hg), both bucindolol (97 +/- 9 mm Hg) and hydrochlorothiazide (99 +/- 10 mm Hg) alone significantly and comparably reduced the 12-hour averaged standing diastolic BP, with the combination resulting in approximately additive effects (91 +/- 9 mm Hg). Although bucindolol alone did not affect HR, it attenuated the hydrochlorothiazide-induced increase in HR. There was a tendency for bucindolol to decrease plasma renin activity. Except for transient postural hypotension in 2 patients, bucindolol was well tolerated.
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PMID:Bucindolol, a beta-adrenoceptor blocker with vasodilatory action: its effect in systemic hypertension. 614 80

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

The objective of this placebo controlled double-blind multicentre (six centres) trial was to investigate the safety and efficacy of ICI 141,292 (Visacor), a new selective beta 1-adrenoceptor antagonist with modest intrinsic sympathomimetic activity (ISA), in hypertensive patients. Fifty-nine patients with mild essential hypertension were randomized to two of five treatment alternatives (placebo, 50 mg, 100 mg 200 mg or 300 mg of ICI 141,292) each given once daily for 2 weeks with a 4 week placebo period before (run in) and in between (wash out) active periods. Thus, each of the five treatments was evaluated in 20-24 patients. After 2 weeks (24 h after last dose) the reduction in recumbent blood pressure for all doses except 50 mg of ICI 141,292 was statistically significant and in the order of 6/4 mm Hg. Standing systolic blood pressure was reduced in a dose-dependent way but only significant for 200 mg of ICI 141,292 (8 mm Hg). Heart rate changes (delta) less than 4 beats/min) were not statistically significant for any dose. It is concluded that ICI 141,292 was well tolerated and had a significant but weak antihypertensive effect which might be explained by too much beta 1-adrenoceptor ISA.
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PMID:Initial clinical experience with ICI 141,292 (Visacor), a new selective beta 1-adrenoceptor blocker with ISA--a multicentre trial in 59 patients. 615 75

Carvedilol (BM 14190) is a new antihypertensive compound which combines beta-adrenoceptor blocking and precapillary vasodilating properties but is devoid of intrinsic sympathomimetic activity. The acute and long-term effects on blood pressure and regional haemodynamics (forearm plethysmography) were studied with carvedilol 25 mg b.i.d. or 50 mg b.i.d. Comparisons were made with propranolol 80 mg b.i.d. in a randomized double-blind placebo controlled trial comprised of 30 patients with essential hypertension. After a four-week placebo period active therapy was given for four weeks. Carvedilol administered acutely reduced blood pressure at both doses, delta 13/6 mmHg (P less than 0.001/P less than 0.01) and 17/10 mmHg (P less than 0.001/P less than 0.01). Resistance in the forearm fell significantly with the higher dose. This was in contrast to propranolol which only reduced heart rate acutely, and as expected caused a rise in forearm resistance. After four weeks both compounds had reduced blood pressure significantly and to the same extent. Blood flow was still significantly reduced with propranolol in contrast to the findings with carvedilol. We conclude that carvedilol given orally has a useful antihypertensive effect both acutely and during prolonged treatment. It is well tolerated and its haemodynamic profile is attractive.
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PMID:Haemodynamic effects of carvedilol, a new beta-adrenoceptor blocker and precapillary vasodilator in essential hypertension. 615 80

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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PMID:Labetalol: a review of its pharmacology, pharmacokinetics, clinical uses and adverse effects. 631 May 29

Eight out-patients with essential hypertension participated in a comparative, placebo-controlled study with a cross-over design. Pindolol and propranolol were administered orally in doses of 20.0 +/- 3.13 mg/d (mean +/- SEM) and 125.0 +/- 19.17 mg/d respectively. Pindolol reduced mean blood pressure by 11.9 mmHg; pre-ejection period index by 8.1 msec; total peripheral resistance by 3.1 mmHg min/L; and limb vascular resistance by 3.28 mmHg min 100 g/ml. Heart rate, cardiac output, plasma renin activity and urinary norepinephrine excretion rate were not altered by pindolol. Propranolol reduced mean blood pressure by 14.0 mmHg; heart rate by 9.1 beats/min; cardiac output by 0.57 L/min; limb blood flow by 1.06 ml/100 g.min; and plasma renin activity by 1.44 ng/ml/h; and increased pre-ejection period index by 8.7 msec. Total peripheral resistance, limb vascular resistance and urinary norepinephrine excretion rate were not altered by propranolol. It was concluded that: (1) the drugs, pindolol and propranolol, are equally effective as antihypertensive agents; (2) heart function and plasma renin activity are decreased by propranolol and unaltered by pindolol; (3) total peripheral resistance is decreased by pindolol and unaltered by propranolol; and (4) these findings may be explained by the intrinsic sympathomimetic activity exhibited by pindolol only.
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PMID:A comparative study on the effects of pindolol and propranolol on systemic and cardiac haemodynamics in hypertensive patients. 638 72

Guanethidine (G) is currently used in the treatment of essential hypertension. Acetaldehyde (A), acrolein (AR), formaldehyde (F) and propionaldehyde (P) are constituents of cigarette smoke and (A) is also an intermediate oxidative metabolite of ethanol. These aldehydes are known to produce sympathomimetic effects by the release of NE from adrenergic neurons and to exert cardioinhibitory effects. The type of predominant effect is dose-dependent. This study was undertaken to determine if these aldehydes result in sympathomimetic effects in the presence of G (15 mg/kg iv) in anesthetized rats. G enhanced the pressor responses to A and P in dose ranges of 5-20 and 5-10 mg/kg respectively. However, AR and F at dose ranges of 0.05-5 and 0.1-10 mg/kg, respectively, elicited only depressor responses after G. Thus, A and P exerted greater sympathomimetic effects through the release of intraneuronal NE in the presence of G. The adrenergic neuronal blocking action of G changes the blood pressure effects of AR and F. When these two compounds are administered in the absence of G, they cause predominant pressor effects, whereas in the presence of G a depressor response is noted. This depressor response is possibly by vagal stimulation and/or direct vasodilation.
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PMID:Effects of intravenous acetaldehyde, acrolein, formaldehyde and propionaldehyde on arterial blood pressure following acute guanethidine treatment. 687 72


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