Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Pivot Concepts:
Gene/Protein
Disease
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Drug
Enzyme
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Target Concepts:
Gene/Protein
Disease
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Drug
Enzyme
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Query: EC:3.4.15.1 (
ACE
)
18,300
document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)
516 patients with New York Heart Association class III and IV heart failure despite treatment with diuretics and
angiotensin converting enzyme
inhibitors were randomised in a double-blind between-group comparison to xamoterol 200 mg (352) or placebo (164) twice daily for 13 weeks. There was no difference between the treatments in loss of clinical signs. Visual analogue scale and Likert scores indicated that breathlessness was less severe with xamoterol, but there was no difference in exercise duration or total work done.
Xamoterol
reduced maximum exercise heart rate and systolic blood pressure, did not affect the number of ventricular premature beats after exercise, showed no arrhythmogenic activity, and had variable (agonist and antagonist) effects on 24 h heart rate. On intention-to-treat analysis 32 (9.1%) patients in the xamoterol group and 6 (3.7%) patients in the placebo group died within 100 days of randomisation (p = 0.02).
...
PMID:Xamoterol in severe heart failure. The Xamoterol in Severe Heart Failure Study Group. 197 33
Xamoterol
('Corwin', 'Carwin', 'Corwil', 'Xamtol', ICI118, 587)*, a partial beta-agonist, has beneficial effects in patients with mild to moderate heart failure. In acute haemodynamic studies in more severe heart failure some patients have shown negative inotropic and chronotropic effects, although treatment with a partial agonist should protect the heart against excessive stimulation, while providing a baseline level of sympathetic drive. This study examined the effects of oral xamoterol in patients with moderate to severe heart failure. Ten patients were studied, nine with ischaemic heart disease. All but one were in New York Heart Association (NYHA) functional Class III. Other treatment, including
angiotensin converting enzyme
(
ACE
) inhibitors, was continued. The patients underwent a standard bicycle exercise test, and the following day cardiac catheterization was performed to obtain measurements of ventricular size (by cineangiography) and pressures during the cardiac cycle. The patients began treatment with xamoterol 200 mg b.d. in addition to their baseline therapy, and this was continued for an average of 9 weeks, after which the exercise test and the haemodynamic investigations were repeated. At baseline, all patients had a raised left ventricular end-diastolic pressure (LVEDP) and nine had a low election fraction, raised end-systolic and end-diastolic volume indices and reduced left ventricular (+) dP/dtmax
Xamoterol
produced a marked reduction in left ventricular filling pressure, a fall in end-systolic volume index and improvements in T1, (+) dP/dtmax and (dP/dt)/DP40 with no change in mean aortic pressure. Duration of exercise increased in four patients, and did not change in the other four tested.(ABSTRACT TRUNCATED AT 250 WORDS)
...
PMID:Clinical experience of therapy with xamoterol in patients with severe systolic and diastolic dysfunction. 197 87
1. Current therapy of heart failure leaves much to be desired. Not all patients respond, and many agents lose their effects with time. 2. Newer agents may be effective but toxic, and some which have a beneficial action when given intravenously have proved disappointing when used orally. 3. The value of digoxin in patients in sinus rhythm is open to debate, and diuretics, although useful acutely in reducing fluid overload, do not appear to improve prognosis. 4. Vasodilators increase effort capacity and reduce symptoms, possibly conferring some long-term benefit, and
angiotensin converting enzyme
(
ACE
) inhibitors improve symptoms and decrease mortality in a wide range of patients. 5. Positive inotropes may be effective in the short term, but they increase myocardial oxygen demand and show tachyphylaxis with no prognostic benefit. 6.
Xamoterol
(Corwin, Carwin, Corwil, Xamtol, ICI 118,587) is a partial sympathetic agonist with approximately 50% of the activity of a pure agonist, which provides inotropic support at rest, and protection against excess sympathetic activity on exercise. 7. It is compatible with other therapies and has shown no serious toxicity. 8. It should be considered at present as an adjunct to diuretic and/or
ACE
inhibitor therapy, although it may be useful alone; its role will become clearer as its effects on mortality are established.
...
PMID:The management of heart failure and the scope for new therapies: what role for xamoterol? 257 56
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