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 |
|
| 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 |
|
| Mechanism of action of Ca2+ sensitizers--update 2001. | 2001 Sep |
|
| Effect of pimobendan in patients with chronic heart failure. | 2001 Winter |
|
| 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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| Combined endpoints: can we use them? | 2002 Oct 15 |
|
| [Pharmacological treatment of heart failure]. | 2003 Apr |
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| [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 |
|
| Use of pimobendan in the management of heart failure. | 2004 Sep |
|
| Efficacy and safet of pimobendan in canine heart failure caused by myxomatous mitral valve disease. | 2005 Mar |
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| Pimobendan in heart failure therapy--a silver bullet? | 2006 Mar-Apr |
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| [Subarachnoid hemorrhage complicated with different manifestations of transient abnormal left ventricular wall motion: two case reports]. | 2006 May |
|
| Acute heart failure: inotropic agents and their clinical uses. | 2006 Nov |
|
| New insights in the treatment strategy for pulmonary arterial hypertension. | 2006 Oct |
|
| 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 |
|
| Treatment options in myocarditis: what we know from experimental data and how it translates to clinical trials. | 2007 Sep |
|
| Cardiac Ca2+ signaling and Ca2+ sensitizers. | 2008 Dec |
|
| The role of cardiac troponin T quantity and function in cardiac development and dilated cardiomyopathy. | 2008 Jul 9 |
|
| Anaesthesia for the geriatric dog and cat. | 2008 Jun 1 |
|
| Alterations in vasomotor control of coronary resistance vessels in remodelled myocardium of swine with a recent myocardial infarction. | 2008 May |
|
| 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 |
|
| Sarcomere control mechanisms and the dynamics of the cardiac cycle. | 2010 |
|
| Canine dilated cardiomyopathy: a retrospective study of prognostic findings in 367 clinical cases. | 2010 Aug |
|
| Canine degenerative myxomatous mitral valve disease: natural history, clinical presentation and therapy. | 2010 Jul |
|
| Current use of pimobendan in canine patients with heart disease. | 2010 Jul |
|
| Synthesis, vasorelaxant activity and antihypertensive effect of benzo[d]imidazole derivatives. | 2010 Jun 1 |
|
| 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 |
