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外観
白色～うすい褐色、結晶～粉末
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溶解性
ぎ酸及び酢酸(100)に溶けやすく、エタノール(95)にやや溶けにくく、メタノールに溶けにくく、水及びジエチルエーテルにほとんど溶けない。
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効能
強心薬, ホスホジエステラーゼ阻害薬
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商品名
アカルディ (日本ベーリンガーインゲルハイム)
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説明
Pimobendan, a novel cardiotonic vasodilator, was introduced in Japan for the
treatment of acute and mild to moderate chronic heart failure. It is a
phosphodiesterase Ⅲ inhibitor and is able to enhance sensitization of myocardial
contractile regulatory protein to calcium ions. The combination of these effects
contribute to its inotropic activity. In patients with severe congestive heart failure,
orally administered pimobendan improves cardiac index, stroke volume index,
pulmonary wedge pressure, and systemic and pulmonary vascular resistance.
Pimobendan is reported to be well tolerated and largely devoid of the proarrhythmic
effects of classical phosphodiesterase Ill inhibitors. Studies also suggested that
combination of the inotropic agent pimobendan with an ACE inhibitor such as
enalapril may be superior to monotherapy for heart failure patients.
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化学的特性
White Solid
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使用
Pimobendan is a cardiotonic agent. The study of the cardiotonic mechanism of Pimobendan using ventricular muscles from rabbits and guinea pigs suggests that Pimobendan acts by inhibiting phosphodiesterase III and potassium channel. The potent venodilating action of Pimobendan makes it a suitable treatment option for patients with congestive heart failure (CHF) as it also improves systemic vasoconstriction.
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定義
ChEBI: Pimobendan is a pyridazinone and a member of benzimidazoles. It has a role as a cardiotonic drug, a vasodilator agent and an EC 3.1.4.* (phosphoric diester hydrolase) inhibitor.
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生物活性
Pimobendan is an inhibitor of phosphodiesterase 3 (PDE3; IC50 = 0.32 μM for guinea pig cardiac enzyme) that is selective for PDE3 over PDE1, PDE2, and PDE4 (IC50s = >30 μM). It is also a calcium sensitizer, decreasing the concentration of calcium required for half-maximal contractile force in isolated, skinned porcine ventricular fibers. Pimobendan increases the force of contraction in electrically-stimulated isolated guinea pig papillary muscles with an EC50 value of 6 μM, indicating positive inotropic effects. It increases survival time in dogs with congestive heart failure due to myxomatous mitral valve disease when administered in combination with angiotensin-converting enzyme inhibitors and furosemide . Formulations containing pimobendan have been used in the treatment of heart failure in dogs.
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作用機序
The mechanism of mild mitral regurgitation (MR) in dogs treated with Pimobendan is a dual mechanism of action, which enhances myocardial contractility by increasing calcium sensitisation of troponin C and promotes vasodilatation by inhibiting PDEIII.
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副作用
The most common side effects include gastrointestinal effects such as decreased appetite, and diarrhea. Other possible side effects include lethargy and difficulty breathing This short-acting medication should stop working within 24 hours, although effects can be longer in pets with liver or kidney disease.
