Details
| Stereochemistry | UNKNOWN |
| Molecular Formula | C19H18N4O2 |
| Molecular Weight | 334.3718 |
| Optical Activity | ( + ) |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
COC1=CC=C(C=C1)C2=NC3=C(N2)C=CC(=C3)C4=NNC(=O)CC4C
InChI
InChIKey=GLBJJMFZWDBELO-UHFFFAOYSA-N
InChI=1S/C19H18N4O2/c1-11-9-17(24)22-23-18(11)13-5-8-15-16(10-13)21-19(20-15)12-3-6-14(25-2)7-4-12/h3-8,10-11H,9H2,1-2H3,(H,20,21)(H,22,24)
DescriptionCurator's Comment: description was created based on several sources, including
http://www.ncbi.nlm.nih.gov/pubmed/1660359
Curator's Comment: description was created based on several sources, including
http://www.ncbi.nlm.nih.gov/pubmed/1660359
Pimobendan (INN, or pimobendane; tradenames Vetmedin, Acardi, and Heartmedin) is a veterinary medication. Under the trade name Acardi, it is available for human use in Japan. Usually, this medicine is used to treat acute heart failure and chronic heart failure (mild to moderate in severity). By increasing the calcium ion sensitivity to protein regulating myocardial contraction and also by inhibiting phosphodiesterase (PDE-III) activity, this medicine dilates the blood vessels and improves the symptoms of heart failure such as shortness of breath and difficulty in breathing. Pimobendan is metabolized into an active metabolite (desmethylpimobendan) by the liver. The parent compound, pimobendan, is a potent calcium sensitizer while desmethylpimobendan is a more potent phosphodiesterase III inhibitor. Pimobendan is 90–95% bound to plasma proteins in circulation. This may have implications in patients suffering from low blood protein levels (hypoproteinemia/hypoalbuminemia) and in patients that are on concurrent therapies that are also highly protein bound.
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| Differential modulation of cytokine production by drugs: implications for therapy in heart failure. | 1996 Dec |
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| The novel insulinotropic mechanism of pimobendan: direct enhancement of the exocytotic process of insulin secretory granules by increased Ca2+ sensitivity in beta-cells. | 1998 Mar |
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| Normalization of left ventricular parameters following combined pimobendan and carvedilol treatment in a case of unclassified cardiomyopathy with longstanding refractory status. | 2002 Dec |
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| Beta-blocker therapy combined with low-dose pimobendan in patients with idiopathic dilated cardiomyopathy and chronic obstructive pulmonary disease: report on two cases. | 2002 May |
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| Inotropic agents and immune modulation. | 2002 May |
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| A double-blind, randomized, placebo-controlled study of pimobendan in dogs with dilated cardiomyopathy. | 2002 May-Jun |
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| Combined endpoints: can we use them? | 2002 Oct 15 |
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| Mechanisms of action of novel cardiotonic agents. | 2002 Sep |
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| [Pharmacological treatment of heart failure]. | 2003 Apr |
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| Role of nonglycosidic inotropic agents: indications, ethics, and limitations. | 2003 Mar |
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| Inhibition and facilitation by pimobendan, a calcium sensitizer, of catecholamine secretion from bovine adrenal chromaffin cells. | 2003 Mar |
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| Plasma concentration profile of orally administered pimobendan and plasma brain natriuretic peptide level in patients with severe heart failure. | 2003 May |
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| [Inotropic agents]. | 2003 May |
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| [Roles of cytokines in the pathogenesis of heart failure]. | 2003 May |
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| Increased mitral valve regurgitation and myocardial hypertrophy in two dogs with long-term pimobendan therapy. | 2005 |
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| Pharmacokinetic characterization of transcellular transport and drug interaction of digoxin in Caco-2 cell monolayers. | 2005 Jan |
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| Efficacy and safet of pimobendan in canine heart failure caused by myxomatous mitral valve disease. | 2005 Mar |
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| Positive inotropic effect of purified green tea catechin derivative in guinea pig hearts: the measurements of cellular Ca2+ and nitric oxide release. | 2006 Dec 15 |
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| Pimobendan in heart failure therapy--a silver bullet? | 2006 Mar-Apr |
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| Preclinical dilated cardiomyopathy in the dobermann. | 2006 May 27 |
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| Beta-blockers use in patients with chronic obstructive pulmonary disease and concomitant cardiovascular conditions. | 2007 |
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| Effects of pimobendan for mitral valve regurgitation in dogs. | 2007 Apr |
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| [Combined therapy with weight loss and amiodarone improved cardiac function in a patient with idiopathic dilated cardiomyopathy complicated with severe obesity: a case report]. | 2007 Aug |
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| Translational medicine with a capital T, troponin T, that is. | 2007 Jul 20 |
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| Knock-in mouse model of dilated cardiomyopathy caused by troponin mutation. | 2007 Jul 20 |
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| Comparative adverse cardiac effects of pimobendan and benazepril monotherapy in dogs with mild degenerative mitral valve disease: a prospective, controlled, blinded, and randomized study. | 2007 Jul-Aug |
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| [Calcium sensitizer agents in heart failure therapy]. | 2007 May 28 |
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| [Phosphodiesterase III inhibitor--characteristics, mechanisms of action, pharmacokinetics, indications, contraindications, clinical trials, and side effects]. | 2007 May 28 |
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| [Calcium sensitizer: characteristics, mechanisms of action, pharmacokinetics, indication, contraindication, clinical data, and side effects]. | 2007 May 28 |
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| Treatment options in myocarditis: what we know from experimental data and how it translates to clinical trials. | 2007 Sep |
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| The value added by measuring myocardial contractility 'in vivo' in safety pharmacological profiling of drug candidates. | 2007 Sep-Oct |
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| Effect of short-term treatment with meloxicam and pimobendan on the renal function in healthy beagle dogs. | 2008 Apr |
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| Defining the binding site of levosimendan and its analogues in a regulatory cardiac troponin C-troponin I complex. | 2008 Jul 15 |
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| The role of cardiac troponin T quantity and function in cardiac development and dilated cardiomyopathy. | 2008 Jul 9 |
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| Effect of pimobendan on case fatality rate in Doberman Pinschers with congestive heart failure caused by dilated cardiomyopathy. | 2008 Jul-Aug |
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| Validity, reliability, and responsiveness of the Kansas City Cardiomyopathy Questionnaire in anemic heart failure patients. | 2008 Mar |
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| Concerns about "Comparative adverse cardiac effects of pimobendan and benazepril monotherapy in dogs with mild degenerative mitral valve disease". | 2008 Mar-Apr |
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| Alterations in vasomotor control of coronary resistance vessels in remodelled myocardium of swine with a recent myocardial infarction. | 2008 May |
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| Canine heart disease: progress and promise. | 2008 Nov |
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| Treatment of congestive heart failure in dogs. | 2008 Oct 25 |
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| A QUEST begins. | 2008 Sep-Oct |
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| Effect of pimobendan or benazepril hydrochloride on survival times in dogs with congestive heart failure caused by naturally occurring myxomatous mitral valve disease: the QUEST study. | 2008 Sep-Oct |
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| Cardiac sarcoidosis culminating in severe biventricular failure. | 2009 |
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| Effect of pimobendan on echocardiographic values in dogs with asymptomatic mitral valve disease. | 2009 Mar-Apr |
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| Evaluation of pimobendan and N-terminal probrain natriuretic peptide in the treatment of pulmonary hypertension secondary to degenerative mitral valve disease in dogs. | 2009 Nov-Dec |
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| A randomized, double-blind, placebo-controlled study to determine the effects of valsartan on exercise time in patients with symptomatic heart failure with preserved ejection fraction. | 2009 Oct |
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| Acute effect of pimobendan and furosemide on the circulating renin-angiotensin-aldosterone system in healthy dogs. | 2009 Sep-Oct |
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| Assessment of the pharmacological effects of inotropic drugs on left ventricular pressure and contractility: an evaluation of the QA interval as an indirect indicator of cardiac inotropism. | 2009 Sep-Oct |
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| Sarcomere control mechanisms and the dynamics of the cardiac cycle. | 2010 |
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| Patients' self-assessed functional status in heart failure by New York Heart Association class: a prognostic predictor of hospitalizations, quality of life and death. | 2010 Feb |
Sample Use Guides
Acute heart failure: usually for adults, one capsule (2.5 mg of pimobendan) once daily
Chronic heart failure (mild to moderate in severity): usually for adults, one capsule (2.5 mg of pimobendan) twice daily after meals
Route of Administration:
Oral
composite platelet aggregation (area under the curve [AUC]) and maximal platelet aggregation (aggregation units [AUs]) at 10.0μM pimobendan were significantly decreased for collagen-induced aggregation (AUC, 349.7 ± 58.4 vs 285.1 ± 72.2; maximal platelet aggregation, 196.2 ± 25.8 AUs vs 161.5 ± 38.0 AUs), and the AUC and velocity of aggregation at 10.0μM pimobendan were significantly decreased for ADP-induced aggregation (AUC, 268.5 ± 35.1 vs 213.4 ± 77.2; velocity of aggregation, 15.7 ± 2.9 AUs/min vs 11.8 ± 3.5 AUs/min).
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613JXV89SU
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118428-38-9
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4823
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SUBSTANCE RECORD
