Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: UMLS:C0018801 (heart failure)
 72,216 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Xamoterol has been shown in large, double-blind studies to produce benefit in patients with heart failure. Ischaemic heart disease is the commonest cause of heart failure in the Western World and many patients with heart failure also have angina pectoris (Califf et al., 1982). In view of the known anti-ischaemic effects of xamoterol, we analysed the results of a subgroup of 269 patients with heart failure but without chest pain as a limiting factor on exercise to compare the efficacy of xamoterol in such patients with that of the total group. There were no differences in exercise heart rate, exercise tolerance and symptoms in patients without chest pain compared with the total group. Xamoterol is probably, therefore, acting through myocardial mechanisms other than an anti-ischaemic effect.
 ...
PMID:Xamoterol in mild to moderate heart failure: a subgroup analysis of patients with cardiomegaly but no concomitant angina pectoris. 257 58

Xamoterol 200 mg twice daily was given for 2 months to nine patients with severe heart failure already being treated with angiotensin converting enzyme (ACE) inhibitors. Left ventricular end-diastolic pressure fell from 28 to 13 mmHg and end-systolic volume fell from 115 to 106 ml m-2; indices of contractility improved and ejection fraction rose from 33 to 38%. The time constant of ventricular relaxation, T1, improved from 62 to 44 ms. Exercise tolerance improved. Thus, in this group of patients with severe heart failure, xamoterol produced benefits in systolic and diastolic function. There were no adverse effects.
 ...
PMID:The efficacy and safety of chronic oral administration of xamoterol to patients with severe heart failure treated with ACE inhibitors. 257 63

This study was designed to assess the efficacy of xamoterol in 14 patients with mild to moderate heart failure over a period of 18 months. A beneficial effect on exercise capacity and a lowering of heart rate on exercise was sustained, and ejection fraction did not change, although some deterioration may be expected over this length of time in patients with heart failure. Xamoterol is safe and effective, and its benefits are maintained over at least 18 months.
 ...
PMID:Long-term efficacy of xamoterol (a beta 1-adrenoceptor partial agonist) in patients with mild to moderate heart failure. 257 65

Xamoterol has been shown to reduce the frequency of oedema and lung crepitations in heart failure. We examined its effects on blood pressure and renal function in healthy volunteers. Systolic blood pressure rose, sodium and chloride excretion increased and there was a strong correlation in individual subjects between rises in systolic blood pressure and in sodium excretion. Although no changes in glomerular filtration rates were seen, changes sufficient to explain the observed rise in sodium excretion are well within the experimental error of this study. Xamoterol may increase sodium excretion by an action on renal haemodynamics.
 ...
PMID:Effects of xamoterol on sodium excretion in volunteers. 257 66

The effects of xamoterol (200 mg twice a day) in 21 patients with left ventricular dysfunction were studied in a double blind, randomised, crossover, placebo controlled trial with treatment periods of four weeks. Most patients had moderate heart failure (New York Heart Association class II), all had ischaemic heart disease, a history of a myocardial infarction, and symptoms of dyspnoea on exertion. Patients were assessed in terms of exercise duration (bicycle ergometer), clinical signs of heart failure, symptoms and activities, and ejection fraction. Xamoterol increased exercise duration (mean (SD] (from 445 (8) seconds to 484 (8) seconds) and ejection fraction (from 41.9 (1.3)% to 46.6 (1.3)%) and reduced the signs and symptoms of heart failure. The results of this study show that xamoterol is a safe and effective treatment for left ventricular dysfunction resulting from ischaemic heart disease.
 ...
PMID:Effects of xamoterol, a beta 1 adrenoceptor partial agonist, in patients with ischaemic dysfunction of the left ventricle. 257 49

The clinical efficacy of xamoterol, alpha beta 1-adrenoceptor partial agonist, was determined in a multicentre double-blind, randomized, parallel group study of 240 patients with mild to moderate heart failure. At entry, 62% of patients were receiving diuretics (thiazides, or loop diuretics at a dose no greater than the equivalent of 80 mg of frusemide); 32% were taking nitrate formulations and 14% digoxin for control of atrial fibrillation. Assessments were carried out after a 1-week placebo run-in and after 3 months of treatment with either xamoterol or placebo. 198 patients completed the study of whom 186 had valid exercise tests. Mean exercise duration increased by 7% after placebo and by 19% after xamoterol during a progressive treadmill exercise protocol. Xamoterol significantly reduced peak exercise heart rate compared with placebo. Subjectively, there was improvement in breathlessness on the visual analogue scale after treatment with xamoterol compared with placebo, but no change in fatigue. We conclude that xamoterol produces sustained improvement in symptoms and exercise duration in mild to moderate heart failure.
 ...
PMID:Clinical efficacy of xamoterol, a beta 1-adrenoceptor partial agonist, in mild to moderate heart failure. U.K. Xamoterol Study Group. 257 8

Xamoterol is a partial beta 1 adrenoceptor agonist with positive inotropic properties. Treatment with xamoterol and digoxin was compared in 19 patients with cardiac failure (NYHA class II-III). The study consisted of a short-term and a long-term phase. The former was a randomized, double-blind, crossover study with 6-week treatment periods. In the 15 patients who completed this phase, there was no significant difference between exercise duration on digoxin and on xamoterol. Exercise duration increased on digoxin by 27% and on xamoterol by 17% relative to baseline. Comparing digoxin and xamoterol, maximum exercise heart rate (p less than 0.001), blood pressure (p less than 0.01), and the pressure-rate product during maximum exercise were significantly lower on xamoterol treatment. The systolic time interval was shorter on digoxin than on xamoterol (p less than 0.001). No changes occurred in the echocardiographic parameters. After the short-term study, 13 patients were followed 3-6 months on the drug to which they had responded best (digoxin 7, xamoterol 6). The results of the short-term study were maintained during this period. In conclusion, we found that xamoterol may be an alternative to digoxin in patients with mild to moderate heart failure.
 ...
PMID:Digoxin and xamoterol in patients with moderate chronic heart failure. A double-blind, randomized, controlled study. 257 83

The ideal sympathomimetic derivative should possess the positive inotropic and relaxing effects of catecholamines whilst remaining free of their side-effects. Theoretically, such properties could be present in beta 1-adrenoceptor partial agonists. Xamoterol (ICI 118,587, Corwin; ISA 43 p. 100) seems to be the most promising beta 1 partial agonist. The aim of the study was to determine if the beneficial effects of Xamoterol were maintained during long term administration. Xamoterol (200 mg twice dialy) was administered to 14 patients with anterior myocardial infarction and moderate heart failure (class II-III NYHA). After 3 months' therapy, left ventricular function improved as indicated by reduction in left ventricular (LV) end-diastolic pressure (23 +/- 5 to 16 +/- 5 mm Hg; P less than 0.0005), LV end-diastolic volume (153 to 140 ml/m2; P less than 0.05) and in LV end-systolic volume especially in 11 patients with a control end-systolic volume less than 100 ml/m2 (- 15 p. 100; P less than 0.05). LV inotropic state was also enhanced as indicated by 21 p. 100 increases in EMax, the maximal LV pressure/volume ratio (P less than 0.02) and 20 p. 100 increases in the ratio end-systolic stress/ end-systolic volume (P less than 0.02). Myocardial oxygen consumption was unchanged, global lactate extraction fraction increased from 20 +/- 18 to 33 +/- 14 p. 100 (P less than 0.05) and LV alanine release was reduced (-1.7 to -0.2 muMol/min; P less than 0.05). The rate of LV pressure fall accelerated from 57 to 52 ms (P less than 0.05) and the mean diastolic wall stress was reduced by 35 p. 100 (P less than 0.05), reflecting the improvement in LV relaxation and diastolic function. Thus, the beneficial effects of Xamoterol were maintained after prolonged therapy particularly in patients with class II-III heart failure; patients in class IV benefited less from this therapy. No tachyphylaxis or side-effects were observed.
 ...
PMID:[Role of adrenergic beta receptor partial agonists in left ventricular failure of ischemic origin. Value of xamoterol (ICI 118,587, Corwin)]. 286 23

1. Xamoterol is a cardioselective beta-adrenoceptor partial agonist which may have a role in the management of cardiac failure. Excretion is mainly by the renal route. 2. The kinetics of a single 200 mg oral dose of xamoterol were studied in eight elderly (age 67-82 years) volunteers, eight young (age 21-43 years) volunteers; eight patients with mild to moderate cardiac failure and eight age and sex matched controls. 3. Elderly volunteers had a significantly longer time to reach peak concentration (mean +/- s.e. mean 2.1 +/- 0.2 vs 1.1 +/- 0.1 h) and elimination half-life time (27.0 +/- 2.8 vs 16.4 +/- 3.1 h) compared with young volunteers. The renal clearance of xamoterol was lower in the elderly (115 +/- 12 vs 185 +/- 19 ml min-1) and showed a significant correlation with creatinine clearance (r = 0.85, P less than 0.001). 4. There was no significant difference in any of the pharmacokinetic parameters measured in patients with cardiac failure compared with healthy age and sex matched controls. 5. These results suggest that the maintenance dose of xamoterol could be reduced in elderly patients in relation to impairment of renal function.
 ...
PMID:The effect of age and cardiac failure on xamoterol pharmacokinetics. 289 12

Xamoterol is a partial agonist at the beta 1-adrenoceptor. Haemodynamic studies indicate that xamoterol moderately increases myocardial contractility, improves diastolic relaxation and lowers left ventricular filling pressure at rest and during moderate exercise. At higher levels of sympathetic activity (e.g. strenuous exercise) it produces negative chronotropic responses whilst the reduced filling pressure is maintained. Studies in patients with mild to moderate chronic heart failure demonstrate an advantage for xamoterol 200mg twice daily over placebo and digoxin with respect to improvement in exercise capacity and symptoms. In limited trials to date the initial response seems to be maintained during periods of up to 12 months. Preliminary small studies suggest that xamoterol is useful in the treatment of some patients with angina pectoris, sinoatrial disease or postural hypotension, although further studies are needed to confirm its clinical role in such patients. Xamoterol appears to be generally well tolerated, but deleterious effects in a small number of patients with asthma, or severe heart failure due to dilated cardiomyopathy indicate the need for cautious use of xamoterol in patients with these diseases. Thus, xamoterol is a promising addition to the drugs available to the physician for treating patients with mild to moderate heart failure although further controlled studies are required to clearly establish its precise role.
 ...
PMID:Xamoterol. A preliminary review of its pharmacodynamic and pharmacokinetic properties, and therapeutic use. 290 65


<< Previous 1 2 3 4 5 Next >>