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)
| Molecular Formula | C19H18N4O2 |
| Molecular Weight | 334.3718 |
| Charge | 0 |
| Count |
|
| Stereochemistry | RACEMIC |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Optical Activity | ( + / - ) |
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 |
|
| A case of severe hypoglycemia due to pimobendan. | 2001 Aug |
|
| New pharmacological strategies for the treatment of heart failure. | 2001 Jul |
|
| Disparate force-frequency effects of pimobendan and dobutamine in conscious dogs with tachycardia-induced cardiomyopathy. | 2002 Dec |
|
| Low-dose systemic phosphodiesterase III inhibitor pimobendan combined with prostacyclin therapy in a patient with severe primary pulmonary hypertension. | 2003 Jul |
|
| [Inotropic agents]. | 2003 May |
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| The role of Ca++-sensitizers for the treatment of heart failure. | 2003 Oct |
|
| Successful allogeneic bone marrow transplantation for acute myelogenous leukemia after drug-induced cardiomyopathy. | 2004 Sep |
|
| Increased mitral valve regurgitation and myocardial hypertrophy in two dogs with long-term pimobendan therapy. | 2005 |
|
| Selective blockade of nicotinic acetylcholine receptors by pimobendan, a drug for the treatment of heart failure: reduction of catecholamine secretion and synthesis in adrenal medullary cells. | 2005 Feb |
|
| [Cytokine antagonists and endothelin antagonists for therapy of heart failure]. | 2005 Feb 10 |
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| Pharmacokinetic characterization of transcellular transport and drug interaction of digoxin in Caco-2 cell monolayers. | 2005 Jan |
|
| Efficacy and safet of pimobendan in canine heart failure caused by myxomatous mitral valve disease. | 2005 Mar |
|
| Acute heart failure: inotropic agents and their clinical uses. | 2006 Nov |
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| Beta-blockers use in patients with chronic obstructive pulmonary disease and concomitant cardiovascular conditions. | 2007 |
|
| Translational medicine with a capital T, troponin T, that is. | 2007 Jul 20 |
|
| The value added by measuring myocardial contractility 'in vivo' in safety pharmacological profiling of drug candidates. | 2007 Sep-Oct |
|
| Effect of pimobendan on case fatality rate in Doberman Pinschers with congestive heart failure caused by dilated cardiomyopathy. | 2008 Jul-Aug |
|
| Concerns about "Comparative adverse cardiac effects of pimobendan and benazepril monotherapy in dogs with mild degenerative mitral valve disease". | 2008 Mar-Apr |
|
| Concerns about "Comparative adverse cardiac effects of pimobendan and benazepril monotherapy in dogs with mild degenerative mitral valve disease: a prospective, controlled, blinded and randomized study". | 2008 Mar-Apr |
|
| Alterations in vasomotor control of coronary resistance vessels in remodelled myocardium of swine with a recent myocardial infarction. | 2008 May |
|
| Cardiac sarcoidosis culminating in severe biventricular failure. | 2009 |
|
| Agents with inotropic properties for the management of acute heart failure syndromes. Traditional agents and beyond. | 2009 Dec |
|
| Readability estimates for commonly used health-related quality of life surveys. | 2009 Sep |
|
| Acute effect of pimobendan and furosemide on the circulating renin-angiotensin-aldosterone system in healthy dogs. | 2009 Sep-Oct |
|
| Current use of pimobendan in canine patients with heart disease. | 2010 Jul |
|
| Refining the human iPSC-cardiomyocyte arrhythmic risk assessment model. | 2013 Dec |
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).
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 11:20:45 GMT 2023
by
admin
on
Sat Dec 16 11:20:45 GMT 2023
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| Record UNII |
613JXV89SU
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| Record Status |
Validated (UNII)
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| Record Version |
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| Related Record | Type | Details | ||
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RACEMATE -> ENANTIOMER |
