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It is a calcium sensitizer and a selective inhibitor of phosphodiesterase 3 (PDE3) with positive inotropic and vasodilator effects. Pimobendan is used in the management of heart failure in dogs, most commonly caused by myxomatous mitral valve disease (also previously known as endocardiosis), or dilated cardiomyopathy. [3]
PDE3 inhibitors are indicated as inotropics for the therapy of acute heart failure if catecholamines are ineffective. [2] Well controlled studies have shown that these drugs generally increase mortality , [ 3 ] when used for the therapy of acute heart failure, so they have to be applied under close observation.
The term inotropic state is most commonly used in reference to various drugs that affect the strength of contraction of heart muscle. However, it can also refer to pathological conditions. For example, enlarged heart muscle can increase inotropic state, whereas dead heart muscle can decrease it.
Their inotropic properties make cardiactonic agents critical in addressing inadequate perfusion, and acute heart failure conditions including cardiogenic shock, as well as for long-term management of heart failure. These conditions arise when the heart's ability to meet the body's needs is compromised.
enalapril – ACE-inhibitor used to treat high blood pressure and heart failure; enrofloxacin – Broad spectrum antibiotic (Gram-positive and -negative) -- not recommended for streptococci, or anaerobic bacteria; equine chorionic gonadotropin – gonadotropic hormone used to induce ovulation in livestock prior to artificial insemination
PDE3 enzymes are involved in regulation of cardiac and vascular smooth muscle contractility. Molecules that inhibit PDE3 were originally investigated for the treatment of heart failure, but, because of unwanted arrhythmic side-effects, they are not studied for that indication any longer.
Istaroxime is a positive inotropic agent [2] that mediates its action through inhibition of sodium/potassium adenosine triphosphatase (Na+/K+ ATPase). [7] Na+/K+ ATPase inhibition increases intracellular sodium levels, which reverses the driving force of the sodium/calcium exchanger, inhibiting calcium extrusion and possibly facilitating calcium entry., [5] [8]
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