Pimobendane: Difference between revisions
No edit summary |
No edit summary |
||
Line 3: | Line 3: | ||
| verifiedrevid = 408556559 | | verifiedrevid = 408556559 | ||
| IUPAC_name = (''RS'')-6-[2-(4-methoxyphenyl)-1''H''-benzimidazol-5-yl]-5-methyl-4,5-dihydropyridazin-3(2''H'')-one | | IUPAC_name = (''RS'')-6-[2-(4-methoxyphenyl)-1''H''-benzimidazol-5-yl]-5-methyl-4,5-dihydropyridazin-3(2''H'')-one | ||
| image = Pimobendan | | image = Pimobendan.png | ||
| width = 200px | | width = 200px | ||
| imagename = 1 : 1 mixture (racemate) | | imagename = 1 : 1 mixture (racemate) | ||
Line 52: | Line 52: | ||
}} | }} | ||
__NOTOC__ | __NOTOC__ | ||
{{SI}} | |||
{{CMG}} | {{CMG}} | ||
==Overview== | ==Overview== | ||
Line 86: | Line 86: | ||
[[Category:Phosphodiesterase inhibitors]] | [[Category:Phosphodiesterase inhibitors]] | ||
[[Category:Cardiovascular Drugs]] | [[Category:Cardiovascular Drugs]] | ||
[[Category: | [[Category:Drug]] | ||
Revision as of 20:38, 24 July 2014
Clinical data | |
---|---|
AHFS/Drugs.com | International Drug Names |
Routes of administration | Oral |
ATCvet code | |
Legal status | |
Legal status |
|
Pharmacokinetic data | |
Bioavailability | 60 to 65% |
Elimination half-life | 0.4 hours |
Excretion | In feces |
Identifiers | |
| |
CAS Number | |
PubChem CID | |
UNII | |
KEGG | |
ChEMBL | |
E number | {{#property:P628}} |
ECHA InfoCard | {{#property:P2566}}Lua error in Module:EditAtWikidata at line 36: attempt to index field 'wikibase' (a nil value). |
Chemical and physical data | |
Formula | C19H18N4O2 |
Molar mass | 334.37 g/mol |
3D model (JSmol) | |
| |
(what is this?) (verify) |
WikiDoc Resources for Pimobendane |
Articles |
---|
Most recent articles on Pimobendane Most cited articles on Pimobendane |
Media |
Powerpoint slides on Pimobendane |
Evidence Based Medicine |
Clinical Trials |
Ongoing Trials on Pimobendane at Clinical Trials.gov Clinical Trials on Pimobendane at Google
|
Guidelines / Policies / Govt |
US National Guidelines Clearinghouse on Pimobendane
|
Books |
News |
Commentary |
Definitions |
Patient Resources / Community |
Patient resources on Pimobendane Discussion groups on Pimobendane Patient Handouts on Pimobendane Directions to Hospitals Treating Pimobendane Risk calculators and risk factors for Pimobendane
|
Healthcare Provider Resources |
Causes & Risk Factors for Pimobendane |
Continuing Medical Education (CME) |
International |
|
Business |
Experimental / Informatics |
Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]
Overview
Pimobendan (INN is a veterinary medication manufactured by Boehringer Ingelheim under the trade names Vetmedin and Acardi) or pimobendane. It is a calcium sensitizer with positive inotropic and vasodilator effects. It is also a selective inhibitor of phosphodiesterase III (PDE3).
Pimobendan is used in the management of heart failure in dogs, most commonly caused by myxomatous mitral valve disease (also known as endocardiosis), or dilated cardiomyopathy.[1] Research has shown that pimobendan increases survival time and improves quality of life in patients with congestive heart failure secondary to mitral valve disease when compared with benazepril, an angiotensin-converting-enzyme (ACE) inhibitor.[2] Under the trade name Acardi, it is available for human use in Japan.[3]
Mechanism of action
Pimobendan is a positive inotrope. It sensitizes and increases the binding efficiency of cardiac myofibril to the calcium ions that are already present without increasing the consumption of oxygen and energy. Pimobendan also causes peripheral vasodilation by inhibiting the function of phosphodiesterase III. This results in decreased pressure, translating into smaller cardiac preload and afterload (decreases the failing heart's workload).
Pharmacokinetics
Pimobendan is absorbed rapidly when given via the oral route and has a bioavailability of 60-65%. It is metabolized into its active form by the liver. The half-life of pimobendan in the blood is 0.4 hours and the half-life of its metabolite is 2 hours. Elimination is by excretion in the bile and then feces. Pimobendan is 90–95% bound to plasma proteins in circulation. This has implications in patients suffering from low blood protein levels (hypoproteinemia/hypoalbuminemia) and with patients that are on concurrent therapies that are also highly protein bound.
Combinations
Pimobendan is often used in combination with three other drugs to palliate dogs with heart disease and reduce clinical signs of disease. These are:
- Furosemide, a diuretic, to reduce pulmonary edema. This can be given intravenously if the animal is in respiratory distress (6–8 mg/kg), and then titrated down to the minimum dose required orally.
- Spironolactone, an aldosterone antagonist. This has two actions, firstly, as a potassium-sparing diuretic, although its diuretic properties are small compared with those of furosemide. Secondly, it reduces aldosterone-mediated myocardial remodelling and fibrosis, slowing the progression of heart disease.
- An ACE inhibitor, often enalapril (trade name Enacard) or benazepril (Fortekor). These drugs inhibit the action of angiotensin-converting enzyme, producing a balanced vasodilation, along with other favourable effects.
Other drugs may also be used as required to manage certain arrhythmias that are often associated with heart disease.
Chemistry
Pimobendan can be synthesized beginning with anisoyl chloride:[4]
References
- ↑ Gordon SG, Miller MW, Saunders AB (2006). "Pimobendan in heart failure therapy—a silver bullet?". J Am Anim Hosp Assoc. 42 (2): 90–3. PMID 16527909.
- ↑ Häggström J, Boswood A, O'Grady M; et al. (July 2008). "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". J. Vet. Intern. Med. 22 (5): 1124. doi:10.1111/j.1939-1676.2008.0150.x. PMID 18638016.
- ↑ "Kusuri-no-Shiori Drug Information Sheet". RAD-AR Council, Japan. April 2005. Retrieved 2008-08-06.
- ↑ Nicolas, C; Verny, M; Maurizis, J. C.; Payard, M.; Faurie, M (1986). "Synthesis of14C-bucromarone succinate and hydrochloride". J. Labeled Cmpd. Radiopharm. 23: 837. doi:10.1002/jlcr.2580230806.
Template:Phosphodiesterase inhibitors Template:Cardiac stimulants excluding cardiac glycosides
- Pages with script errors
- CS1 maint: Multiple names: authors list
- CS1 maint: Explicit use of et al.
- Template:drugs.com link with non-standard subpage
- Drugs with non-standard legal status
- Articles with changed EBI identifier
- E number from Wikidata
- ECHA InfoCard ID from Wikidata
- Chemical articles with unknown parameter in Infobox drug
- Infobox drug articles with non-default infobox title
- Chemical pages without ChemSpiderID
- Chemical pages without DrugBank identifier
- Articles without InChI source
- Drugboxes which contain changes to verified fields
- Phosphodiesterase inhibitors
- Cardiovascular Drugs
- Drug