Details
| Stereochemistry | RACEMIC |
| Molecular Formula | C19H18N4O2 |
| Molecular Weight | 334.3725 |
| Optical Activity | ( + / - ) |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1CC(=NN=C1c2ccc3c(c2)nc(-c4ccc(cc4)OC)[nH]3)O
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 |
|
| Identification of cytochrome P-450 isoform(s) responsible for the metabolism of pimobendan in human liver microsomes. | 2000 Jan |
|
| The role of inflammatory mediators in the failing heart: immunomodulation of cytokines in experimental models of heart failure. | 2001 Mar |
|
| Beneficial effects of the Ca2+ sensitizer EMD 57033 in exercising pigs with infarction-induced chronic left ventricular dysfunction. | 2001 Oct |
|
| Mechanism of action of Ca2+ sensitizers--update 2001. | 2001 Sep |
|
| Effects of pimobendan on adverse cardiac events and physical activities in patients with mild to moderate chronic heart failure: the effects of pimobendan on chronic heart failure study (EPOCH study). | 2002 Feb |
|
| A double-blind, randomized, placebo-controlled study of pimobendan in dogs with dilated cardiomyopathy. | 2002 May-Jun |
|
| Combined endpoints: can we use them? | 2002 Oct 15 |
|
| Mechanisms of action of novel cardiotonic agents. | 2002 Sep |
|
| Low-dose systemic phosphodiesterase III inhibitor pimobendan combined with prostacyclin therapy in a patient with severe primary pulmonary hypertension. | 2003 Jul |
|
| Inhibition and facilitation by pimobendan, a calcium sensitizer, of catecholamine secretion from bovine adrenal chromaffin cells. | 2003 Mar |
|
| Plasma concentration profile of orally administered pimobendan and plasma brain natriuretic peptide level in patients with severe heart failure. | 2003 May |
|
| [Inotropic agents]. | 2003 May |
|
| The role of Ca++-sensitizers for the treatment of heart failure. | 2003 Oct |
|
| Ca2+-sensitisers--a promising option to treat heart failure? | 2005 Dec |
|
| Effect of pimobendan on cardiopulmonary baroreflex control of sympathetic nerve activity in healthy young men. | 2005 Oct 30 |
|
| Clinical efficacy of pimobendan versus benazepril for the treatment of acquired atrioventricular valvular disease in dogs. | 2006 Jul-Aug |
|
| Syncope secondary to transient atrioventricular block in a German shepherd dog with dilated cardiomyopathy and atrial fibrillation. | 2006 May |
|
| Preclinical dilated cardiomyopathy in the dobermann. | 2006 May 27 |
|
| Acute heart failure: inotropic agents and their clinical uses. | 2006 Nov |
|
| Beta-blockers use in patients with chronic obstructive pulmonary disease and concomitant cardiovascular conditions. | 2007 |
|
| Effects of pimobendan for mitral valve regurgitation in dogs. | 2007 Apr |
|
| [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 |
|
| Knock-in mouse model of dilated cardiomyopathy caused by troponin mutation. | 2007 Jul 20 |
|
| 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 |
|
| [Phosphodiesterase III inhibitor--characteristics, mechanisms of action, pharmacokinetics, indications, contraindications, clinical trials, and side effects]. | 2007 May 28 |
|
| Treatment options in myocarditis: what we know from experimental data and how it translates to clinical trials. | 2007 Sep |
|
| Effect of short-term treatment with meloxicam and pimobendan on the renal function in healthy beagle dogs. | 2008 Apr |
|
| Cardiac Ca2+ signaling and Ca2+ sensitizers. | 2008 Dec |
|
| Defining the binding site of levosimendan and its analogues in a regulatory cardiac troponin C-troponin I complex. | 2008 Jul 15 |
|
| Effect of pimobendan on case fatality rate in Doberman Pinschers with congestive heart failure caused by dilated cardiomyopathy. | 2008 Jul-Aug |
|
| Anaesthesia for the geriatric dog and cat. | 2008 Jun 1 |
|
| Validity, reliability, and responsiveness of the Kansas City Cardiomyopathy Questionnaire in anemic heart failure patients. | 2008 Mar |
|
| 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 |
|
| Canine heart disease: progress and promise. | 2008 Nov |
|
| Treatment of congestive heart failure in dogs. | 2008 Oct 25 |
|
| 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 |
|
| 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 |
|
| Readability estimates for commonly used health-related quality of life surveys. | 2009 Sep |
|
| 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 |
|
| 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 |
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).
| Name | Type | Language | ||
|---|---|---|---|---|
|
Official Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Brand Name | English | ||
|
Common Name | English | ||
|
Systematic Name | English | ||
|
Brand Name | English | ||
|
Common Name | English | ||
|
Code | English | ||
|
Common Name | English | ||
|
Systematic Name | English | ||
|
Common Name | English | ||
|
Code | English | ||
|
Common Name | English | ||
|
Brand Name | English | ||
|
Code | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English |
| Classification Tree | Code System | Code | ||
|---|---|---|---|---|
|
CFR |
21 CFR 520.1780
Created by
admin on Sat Jun 26 12:40:44 UTC 2021 , Edited by admin on Sat Jun 26 12:40:44 UTC 2021
|
||
|
EMA VETERINARY ASSESSMENT REPORTS |
FORTEKOR PLUS (AUTHORISED)
Created by
admin on Sat Jun 26 12:40:44 UTC 2021 , Edited by admin on Sat Jun 26 12:40:44 UTC 2021
|
||
|
NCI_THESAURUS |
C744
Created by
admin on Sat Jun 26 12:40:44 UTC 2021 , Edited by admin on Sat Jun 26 12:40:44 UTC 2021
|
| Code System | Code | Type | Description | ||
|---|---|---|---|---|---|
|
1569315
Created by
admin on Sat Jun 26 12:40:44 UTC 2021 , Edited by admin on Sat Jun 26 12:40:44 UTC 2021
|
PRIMARY | USP-RS | ||
|
34AP3BBP9T
Created by
admin on Sat Jun 26 12:40:44 UTC 2021 , Edited by admin on Sat Jun 26 12:40:44 UTC 2021
|
PRIMARY | |||
|
PIMOBENDAN
Created by
admin on Sat Jun 26 12:40:44 UTC 2021 , Edited by admin on Sat Jun 26 12:40:44 UTC 2021
|
PRIMARY | |||
|
SUB09845MIG
Created by
admin on Sat Jun 26 12:40:44 UTC 2021 , Edited by admin on Sat Jun 26 12:40:44 UTC 2021
|
PRIMARY | |||
|
118428-36-7
Created by
admin on Sat Jun 26 12:40:44 UTC 2021 , Edited by admin on Sat Jun 26 12:40:44 UTC 2021
|
SUPERSEDED | |||
|
CHEMBL24646
Created by
admin on Sat Jun 26 12:40:44 UTC 2021 , Edited by admin on Sat Jun 26 12:40:44 UTC 2021
|
PRIMARY | |||
|
2171
Created by
admin on Sat Jun 26 12:40:44 UTC 2021 , Edited by admin on Sat Jun 26 12:40:44 UTC 2021
|
PRIMARY | |||
|
C041648
Created by
admin on Sat Jun 26 12:40:44 UTC 2021 , Edited by admin on Sat Jun 26 12:40:44 UTC 2021
|
PRIMARY | |||
|
M8815
Created by
admin on Sat Jun 26 12:40:44 UTC 2021 , Edited by admin on Sat Jun 26 12:40:44 UTC 2021
|
PRIMARY | Merck Index | ||
|
DB11450
Created by
admin on Sat Jun 26 12:40:44 UTC 2021 , Edited by admin on Sat Jun 26 12:40:44 UTC 2021
|
PRIMARY | |||
|
C82305
Created by
admin on Sat Jun 26 12:40:44 UTC 2021 , Edited by admin on Sat Jun 26 12:40:44 UTC 2021
|
PRIMARY | |||
|
74150-27-9
Created by
admin on Sat Jun 26 12:40:44 UTC 2021 , Edited by admin on Sat Jun 26 12:40:44 UTC 2021
|
PRIMARY | |||
|
5090
Created by
admin on Sat Jun 26 12:40:44 UTC 2021 , Edited by admin on Sat Jun 26 12:40:44 UTC 2021
|
PRIMARY | |||
|
1110783
Created by
admin on Sat Jun 26 12:40:44 UTC 2021 , Edited by admin on Sat Jun 26 12:40:44 UTC 2021
|
PRIMARY | RxNorm | ||
|
4823
Created by
admin on Sat Jun 26 12:40:44 UTC 2021 , Edited by admin on Sat Jun 26 12:40:44 UTC 2021
|
PRIMARY |
ACTIVE MOIETY
METABOLITE ACTIVE (PARENT)
SALT/SOLVATE (PARENT)
