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)

Drug-induced reduction of elevated blood pressure decreases cardiovascular mortality and morbidity in patients with moderate and severe hypertension. Furthermore, antihypertensive drug studies in mild hypertensive subjects (diastolic blood pressure 90 to 104 mm Hg) have shown protection against stroke, left ventricular hypertrophy, congestive heart failure and progression of renal damage, as well as improved patient longevity. The Hypertension Detection and Follow-up Program trial, recently carried out in the U.S., documented reduced coronary artery disease events (fatal and nonfatal) in special drug-treated patients with mild hypertension. From the standpoint of practical management and considering the ubiquity of essential hypertension, a modified stepped-care regimen advocating initial drug therapy with a beta blocker and addition of low-dose thiazide diuretic when necessary constitutes a judicious approach for widespread application. Although there are 8 orally active beta blockers currently approved in the U.S. for clinical use in systemic hypertension, only acebutolol possesses all of the salutary pharmacologic properties of cardioselectivity, intrinsic sympathomimetic activity and hydrophilicity, thereby making this compound an effective and safe beta-blocking agent for first-order management of a broad segment of the hypertensive population.
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PMID:Antihypertensive therapy and the concept of total cardiovascular protection. 288 51

The hemodynamic effects of oral bucindolol, a non-selective beta-adrenergic blocking agent with intrinsic sympathomimetic activity and direct vasodilating properties, were studied at rest and during handgrip exercise with a flotation-directed pulmonary artery catheter in 12 patients with mild to moderate essential hypertension. After the initial dose of 150 mg of bucindolol, blood pressure (BP) was significantly reduced and cardiac output was increased (from 5.9 +/- 0.8 to 6.8 +/- 1.6 liters/min) in the supine position and during exercise (p less than 0.05). Systemic vascular resistance was reduced (from 1,555 +/- 339 to 1,311 +/- 467 dynes s cm-5, p less than 0.01) at rest and without significant changes during exercise. There were increases in heart rate (13 +/- 13%, p less than 0.01) and right atrial (69 +/- 77%, p less than 0.05), pulmonary arterial (38 +/- 24 %, p less than 0.001) and pulmonary artery wedge pressures (62 +/- 46%, p less than 0.001) during exercise. Bucindolol did not change these variables at rest or during exercise. Bucindolol increased plasma norepinephrine levels both at rest (from 330 +/- 151 to 588 +/- 320 ng/liter, p less than 0.01) and during exercise (from 468 +/- 220 to 685 +/- 390 ng/liter, p less than 0.05). After 4 weeks of bucindolol with doses of 50 to 200 mg 3 times daily, BP was reduced in both supine and standing positions (mean arterial BP of 11 +/- 7% [p less than 0.001] and 11 +/- 6% [p less than 0.001], respectively), without changes in cardiac output, systemic vascular resistance or plasma norepinephrine level.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Efficacy of bucindolol in systemic hypertension. 289 Feb 92

1. Hypertension is associated with a distension of the large arteries and consequently a marked reduction in arterial compliance, which does not result merely from the mechanical effects of elevated arterial pressure but also from early functional and/or structural changes in the arterial walls. This suggests that one of the aims of antihypertensive therapy should be to reverse these arterial abnormalities in the hope of protecting the patient from the atherosclerotic complications of hypertension. 2. Studies have been carried out to compare the effects of equieffective antihypertensive doses of pindolol and propranolol on the arterial circulation in patients suffering from essential hypertension. After 3 months therapy pindolol produced a dilatation of the brachial artery with an increase in arterial compliance and blood flow. In contrast, propranolol, despite comparable antihypertensive effects, did not influence brachial artery circulation. 3. These different effects on the arterial circulation presumably reflect the differing pharmacological properties of the two beta-adrenoceptor antagonists and suggest that the intrinsic sympathomimetic activity of pindolol may be responsible for the qualitative differences in the arterial responses to the two drugs. 4. The results reviewed here reveal that even when two drugs of the same class are used to treat patients with essential hypertension the effects of these agents on arterial haemodynamics can vary greatly and are unrelated to the degree of blood pressure lowering. Thus, pindolol, in contrast to propranolol, not only lowers blood pressure but also reverses some of the changes in arterial haemodynamics which are characteristic of hypertensive disease.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Large arteries in hypertension: heterogeneous haemodynamic response to beta-adrenoceptor antagonists with and without intrinsic sympathomimetic activity. 289 24

Bisoprolol is a beta 1-adrenoceptor antagonist with no partial agonist (intrinsic sympathomimetic) activity or membrane stabilising (local anaesthetic) activity. The oral bioavailability of bisoprolol is high (90%) and the drug has a long elimination half-life which allows once-daily administration; in addition, it is hepatically and renally cleared in equal proportions. In non-comparative studies, and comparative trials, bisoprolol proved effective, and as efficacious as atenolol, low doses of metoprolol, diuretics and nifedipine SR in hypertension, and atenolol and verapamil in stable angina pectoris. Bisoprolol has been well tolerated in most patients. Thus, bisoprolol is an effective alternative to other beta-adrenoceptor antagonists in patients with mild to moderate essential hypertension or stable angina pectoris. Furthermore, its unique pharmacokinetic properties may offer advantages in selected patients. However, the results of further comparative studies with established agents in the treatment of hypertension and angina pectoris are still awaited so that a final assessment of the relative place in therapy of bisoprolol in these disease states may be made.
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PMID:Bisoprolol. A preliminary review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in hypertension and angina pectoris. 290 20

Sotalol is a beta-adrenoceptor blocking agent devoid of intrinsic sympathomimetic activity, membrane stabilising actions and cardioselectivity. It lengthens repolarisation and the effective refractory period in all cardiac tissues independently of its antiadrenergic properties. Combining Class II and Class III antiarrhythmic properties, sotalol can be given either intravenously or orally and its pharmacokinetic properties permit long dosing (once or twice daily) intervals. Controlled and uncontrolled studies have established the efficacy of sotalol in mild-to-moderate essential hypertension and in angina of effort. Sotalol reduces anginal frequency and glyceryl trinitrate (nitroglycerin) consumption and increases exercise capacity during treadmill stress tests. In addition, although there is evidence that the drug reduces reinfarction rate in survivors of acute infarction, the data for reduction in sudden death rates in these patients are not as compelling as for other beta-blockers. However, comparative and additional long term studies are required before an accurate assessment of the use of sotalol in these disorders can be made. When used in the treatment of mild-to-moderate hypertension sotalol is more effective than placebo and comparable to other beta-blockers in reducing elevated blood pressures. In addition, a synergistic antihypertensive response is achieved when sotalol is combined with hydrochlorothiazide. Still, additional well-controlled comparative studies are required before the value of sotalol relative to other drug treatment regimens in the management of hypertension can be made. In preliminary studies sotalol appeared effective in most forms of supraventricular tachyarrhythmias with its effects being similar to those of other beta-blockers. However, preliminary data indicate that sotalol is likely to be more effective than than conventional beta-blockers in converting atrial flutter and fibrillation to sinus rhythm and maintaining stability post-conversion. Sotalol also appears to be a promising agent in the control of ventricular arrhythmias. In suppressing premature ventricular contractions it is at least as effective as procainamide. In ventricular tachycardia and fibrillation, intravenous sotalol (1.5 mg/kg), prevents reinduction by programmed electrical stimulation in 40 to 50% of cases if double stimuli are used. Both prevention of reinducible arrhythmia and the suppression of spontaneous arrhythmias on Holter recordings are predictive of a long term favourable clinical outcome. In patients with reduced ejection fractions, sotalol depresses ventricular function less than conventional beta-blockers.(ABSTRACT TRUNCATED AT 400 WORDS)
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PMID:Sotalol. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic use. 331 21

1. In recent years evidence has accumulated which indicates that although various beta-adrenoceptor antagonists are equally effective in lowering blood pressure in patients with essential hypertension the mechanisms of action of the different drugs are heterogeneous. 2. Pindolol, a beta-adrenoceptor antagonist with pronounced intrinsic sympathomimetic activity (ISA) appears, to some extent, to act via peripheral vascular mechanisms. 3. Following prolonged treatment with pindolol in essential hypertension peripheral vascular resistance at maximal vasodilatation has been found to be decreased compared with the pretreatment values suggesting that the structural vascular changes characteristic of established hypertension may be reversible.
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PMID:Reversibility of structural changes in the resistance vessels in hypertension: a review of studies with pindolol. 332 35

1. Haemodynamic changes during the onset of the antihypertensive action of pindolol, 10 mg twice daily, and propranolol, 80 mg three times daily, were studied for 24 h in two groups of 10 patients with uncomplicated essential hypertension. 2. Baseline haemodynamics were not different between the two groups. 3. Pindolol, with considerable intrinsic sympathomimetic activity (ISA) exerted its maximal antihypertensive efficacy within 3-4 after dosing (-15 +/- 3%, mean +/- s.e. mean, P less than 0.001). This effect was maintained for 24 h. 4. After propranolol, which is devoid of ISA, arterial pressure fell more gradually, but after 24 h the two drugs shared an equal antihypertensive effect. 5. Cardiac output rose after pindolol by 16 +/- 5% (P less than 0.01). It decreased transiently by 16 +/- 6% (P less than 0.01) 1-4 h after propranolol. At that time vascular resistance had risen by 18 +/- 5% (P less than 0.001). 6. The onset of the antihypertensive action of the two drugs was associated with reductions in vascular resistance. Since reflex vasoconstriction did not occur after pindolol, vascular resistance was always lower on this drug than on propranolol (-29 +/- 4%, P less than 0.001 vs -15 +/- 5%, P less than 0.01). 7. Cardiac filling pressures, pulmonary artery pressure and pulmonary vascular resistance did not change after pindolol but they rose after propranolol. 8. During the onset of the vasodilator and antihypertensive effects of the two beta-adrenoceptor blockers heart rate, stroke volume and cardiac output rose, despite cardiac beta-adrenoceptor blockade, suggesting a reduction of parasympathetic tone and an increase in venous return.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Comparison of the onset of the antihypertensive action of pindolol and propranolol. A 24 h haemodynamic study. 332 34

The effects of acebutolol (with intrinsic sympathomimetic activity (ISA] and metoprolol (without ISA) on arm blood pressure, ankle systolic blood pressure, claudication distances (CD) and maximal walking distances (MWD) were compared in patients with essential hypertension and intermittent claudication. Fourteen patients participated in a long-term, open, randomized cross-over study. After randomization the patients received either acebutolol, 200 mg b.i.d., or metoprolol, 100 mg b.i.d. After eight weeks the drugs were shifted and after another eight weeks they were withdrawn. Arm and ankle blood pressure, CD and MWD were determined before randomization and after 4, 8, 12 and 16 weeks, and again 4-6 weeks after withdrawal of the drugs. The arm blood pressure was reduced by 20/13 mmHg after acebutolol and by 22/21 mmHg after metoprolol. In spite of a significant decrease in arm blood pressure there were no significant changes in ankle blood pressure, CD or MWD after the two drugs. After withdrawal of the drugs and after the arm blood pressure had returned to the control value no significant changes were seen in CD, MWD or ankle blood pressure. It is concluded that beta-blockers have no deleterious effect on CD, MWD or ankle blood pressure in patients with hypertension and intermittent claudication. No effect of ISA was demonstrated.
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PMID:The effects of acebutolol and metoprolol on walking distances and distal blood pressure in hypertensive patients with intermittent claudication. 351 64

This study re-examines the proposal that beta-adrenoceptor blockers with intrinsic sympathomimetic activity decrease plasma noradrenaline levels. Thirteen patients (aged 29-65 years) with uncomplicated essential hypertension were randomly allocated to a three period, double-blind cross-over trial. The treatment periods, each of 3 weeks duration, were composed of placebo, pindolol (5 mg twice daily) and metoprolol (100 mg twice daily), dispensed in identical capsules. At the end of each treatment period, patients were exercised on a bicycle ergometer to a predetermined workload. Blood pressure and heart rate were measured before, immediately on completion of exercise and after 10 min post-exercise rest. Blood samples for plasma noradrenaline and adrenaline determination were also collected at these times. Blood pressures were similar during treatment with pindolol and metoprolol. As expected, heart rate was consistently lower during metoprolol treatment. Basal, pre-exercise plasma noradrenaline and adrenaline were similar at the end of each treatment period. However, the increase following exercise was significantly greater during metoprolol treatment. The post-exercise increase during pindolol treatment was indistinguishable from that in the placebo period. These findings, in a randomised placebo-controlled study, therefore demonstrate that pindolol does not influence basal or exercise-stimulated plasma noradrenaline and adrenaline concentrations. This is best explained by a lack of effect of pindolol on the plasma clearance of catecholamines, which is impaired by beta-adrenoceptor blockers devoid of intrinsic sympathomimetic activity.
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PMID:Plasma catecholamines following exercise in hypertensives treated with pindolol: comparison with placebo and metoprolol. 374 14

In a double-blind, comparative study metoprolol (100 to 300 mg/day) or pindolol (5 to 15 mg/day) was given in randomized order to 39 patients with uncomplicated essential hypertension. Peripheral hemodynamics were studied by noninvasive means after an initial 6-week placebo period and again after 6 weeks and 6 months of active treatment. Three patients withdrew from the trial during the 6-week period of active treatment. Heart rate during exercise on an ergometric bicycle to a predetermined workload indicated that the degree of beta-adrenoceptor blockade was identical during treatment with either metoprolol or pindolol. Both agents also reduced resting blood pressure to the same extent. Heart rate at rest fell considerably more during metoprolol than pindolol therapy, while vascular resistance was reduced by pindolol but not by metoprolol. This indicates that the antihypertensive effect of metoprolol can be ascribed mainly to cardiac mechanisms; in contrast, pindolol appears to lower blood pressure primarily through vascular effects. Studies at maximal dilatation showed that pindolol, but not metoprolol, reduced resistance at maximal dilatation after 6 months of treatment, indicating that a reversal of the structural vascular changes had occurred. The hemodynamic differences between the 2 agents can probably be explained by the fact that pindolol with its intrinsic sympathomimetic activity acts as a partial agonist causing active stimulation of vascular beta 2 adrenoceptors and relaxation of resistance vessels.
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PMID:Hemodynamics of metoprolol and pindolol in systemic hypertension with particular reference to reversal of structural vascular changes. 394 48


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