Gene/Protein Disease Symptom Drug Enzyme Compound
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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)

Although there are many classes of drugs, including cardiac glycosides, sympathomimetic inotropes, beta-adrenergic antagonists, angiotensin-converting enzyme inhibitors (ACE inhibitors) and spironolactone etc. used for the treatment of heart failure, the morbidity and mortality rates of patients after these treatments are not ameliorated. Chronic administration of Sympathomimetic inotropes also increased the arrhythmogenic effects. Consequently, improvement of treatment for heart failure remains a major medical challenge for the coming years. In this present experiment, the novel Na(+)-K(+) ATPase inhibitor AT-11 was characterized for its inotropic and toxic properties. Comparing AT-11 with ouabain, we found that AT-11 concentration-dependently increased contractility in guinea pig heart preparations, and the safety index of AT-11 was better than ouabain in vitro. In the in vivo study, AT-11 was also safer than ouabain at the equieffective dose. Moreover, AT-11 slowed heart rate more than ouabain did. This may be due to a larger AT-11-induced increase in vagal reflex than with ouabain and an indirect decrease in sympathetic tone to prevent Ca(2+) overload.
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PMID:Pharmacological profile of the new inotropic agent AT-11. 1803 38

Toborinone is an inotropic agent with a moderate coronary vasodilatory action, but lacking direct chronotropic action, under development by Otsuka. A marketing application has been filed in Japan [269634], and it has entered phase III trials in the US for the treatment of cardiac failure [170668]. The effects of toborinone in 48 patients with moderate to severe CHF have been evaluated in a multicenter, double-blind study. Patients received either placebo or 1.25, 2.5, 5 or 10 microg/kg/min toborinone via a 6-h infusion. Based on efficacy criteria (25% increase in cardiac index and/or 25% decrease in pulmonary capillary wedge pressure), 25, 58, 92 and 100% of patients receiving 1.25, 2.5, 5 or 10 microg/kg/min toborinone, respectively, had a clinically significant improvement in hemodynamic status after 6 h of infusion, compared to only 17% of patients taking placebo [284078]. A phase I trial of toborinone in 20 healthy Japanese volunteers showed that the drug was well-tolerated. Another phase I trial in 10 patients with congestive heart failure showed that the drug improved ventricular performance without sympathomimetic stimulation of the myocardium [279819]. In anesthetized dogs, the cardiovascular effects of toborinone were unaffected by procainamide and lidocaine, suggesting that it can be used clinically with these antiarrhythmic agents for the treatment of heart failure [175267]. Toborinone did not aggravate adverse effects such as arrhythmias, and can be combined with ACE inhibitors, nitrates and diuretics for the treatment of heart failure [175268].
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PMID:Toborinone Otsuka Pharmaceutical Co Ltd. 1846 98

Agina pectoris is a discomfort in the chest or adjacent areas caused by myocardial ischemia. It is most commonly caused by the inability of narrowed atherosclerotic coronary arteries to supply adequate oxygen to the heart under conditions of increase demand. This review article will focus in the medical treatment of chronic stable angina, with a focus in new strategies or medications. Treatment by revascularization techniques will not be discussed in this article. The goal of treatment is to improve quality of life, decrease cardiovascular events and mortality. All patients should be evaluated for reversible causes of their angina, such as anemia, hyperthyroidism, sympathomimetic drugs and hypertension. Sublingual nitroglycerin should be used for immediate relief of symptoms. In general, all patients should be on aspirin (ASA) unless they are allergic or other contraindications, if so; clopidogrel should be added to the therapy. In addition to the antiplatelet therapy, which decreases mortality, patients should be started on beta blockers and nitrates. If there is no improvement in symptoms then a calcium channel blockers of the dihydropyridine family should be added. Patients with Diabetes Mellitus and/or left ventricular systolic dysfunction should be also started on angiotensin converting enzyme inhibitors. If the patient continues with limiting angina, ranolazine should be started and finally enhanced external counterpulsation should be considered in those patients who have not responded to maximal drug therapy.
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PMID:Management of chronic stable angina pectoris. 1940 May 28

In rats with relatively mild chronic heart failure (CHF) there was an increase in plasma LDL levels. In turn, in severe CHF it was revealed a significant decrease in total cholesterol concentration due to LDL levels decline. ACE inhibitors (captopril, enalapril and lisinopril) and the most selective beta1-adrenoblockers (metoprolol, nebivolol) had not any significant influence on plasma lipids. Less selective and especially nonselective beta-adrenoblockers pindolol and propranolol brought up the atherogenic potential of plasma because of HDL levels reduction in mild CHF whereas in case of severe model--due to the trends toward decrease in HDL concentration and toward increase in LDL levels. Lipophilic ACE-inhibitors and beta-adrenoblockers without intrinsic sympathomimetic activity improved survival in rats with mild CHF to the equal extent. On the contrary in severe CHF beta-adrenoblockers, especially non-selective, had an advantage over ACE inhibitors on the survival effect.
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PMID:[Plasma lipid spectrum and survival in rats with heart failure varied by severity under the influence of neurohormonal modulators]. 2434 Jun 20


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