Pimobendane

Revision as of 16:57, 20 August 2015 by WikiBot (talk | contribs) (Protected "Pimobendane": Bot: Protecting all pages from category Drug ([Edit=Allow only administrators] (indefinite) [Move=Allow only administrators] (indefinite)))
(diff) ← Older revision | Latest revision (diff) | Newer revision → (diff)
Jump to navigation Jump to search
Pimobendan
Clinical data
AHFS/Drugs.comInternational Drug Names
Routes of
administration
Oral
ATCvet code
Legal status
Legal status
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability60 to 65%
Elimination half-life0.4 hours
ExcretionIn feces
Identifiers
CAS Number
PubChem CID
ChemSpider
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
FormulaC19H18N4O2
Molar mass334.37 g/mol
3D model (JSmol)
 ☒N☑Y (what is this?)  (verify)

WikiDoc Resources for Pimobendane

Articles

Most recent articles on Pimobendane

Most cited articles on Pimobendane

Review articles on Pimobendane

Articles on Pimobendane in N Eng J Med, Lancet, BMJ

Media

Powerpoint slides on Pimobendane

Images of Pimobendane

Photos of Pimobendane

Podcasts & MP3s on Pimobendane

Videos on Pimobendane

Evidence Based Medicine

Cochrane Collaboration on Pimobendane

Bandolier on Pimobendane

TRIP on Pimobendane

Clinical Trials

Ongoing Trials on Pimobendane at Clinical Trials.gov

Trial results on Pimobendane

Clinical Trials on Pimobendane at Google

Guidelines / Policies / Govt

US National Guidelines Clearinghouse on Pimobendane

NICE Guidance on Pimobendane

NHS PRODIGY Guidance

FDA on Pimobendane

CDC on Pimobendane

Books

Books on Pimobendane

News

Pimobendane in the news

Be alerted to news on Pimobendane

News trends on Pimobendane

Commentary

Blogs on Pimobendane

Definitions

Definitions of Pimobendane

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

Symptoms of Pimobendane

Causes & Risk Factors for Pimobendane

Diagnostic studies for Pimobendane

Treatment of Pimobendane

Continuing Medical Education (CME)

CME Programs on Pimobendane

International

Pimobendane en Espanol

Pimobendane en Francais

Business

Pimobendane in the Marketplace

Patents on Pimobendane

Experimental / Informatics

List of terms related to Pimobendane

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]

Overview

Pimobendan (or pimobendane)(INN) is a veterinary medication manufactured by Boehringer Ingelheim under the trade names Vetmedin and Acardi (Japan). It is both a calcium sensitizer and a selective inhibitor of phosphodiesterase III (PDE3) with positive inotropic and vasodilator effects.

Pimobendan is used in the management of heart failure in dogs, most commonly caused by myxomatous mitral valve disease (also previously known as endocardiosis), or dilated cardiomyopathy.[1] Research has shown that pimobendan increases survival time and improves quality of life in canine 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 (increases myocardial contractility). It sensitizes and increases the binding efficiency of cardiac troponin in the myofibril to the calcium ions that are already present in systole. In normal hearts it increases the consumption of oxygen and energy to the same degree as dobutamine but in diseased hearts it may not.[4] [5] Pimobendan also causes peripheral vasodilation by inhibiting the function of phosphodiesterase III. This results in decreased resistance to blood flow through systemic arterioles, which decreases afterload (decreases the failing heart's workload) and reduces the amount of mitral regurgitation.[6][7]

Pharmacokinetics

Pimobendan is absorbed rapidly when given via the oral route and has a bioavailability of 60-65%.[8] Bioavailability is markedly decreased when ingested with food. It 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.[9] 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 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.

Combinations

Pimobendan is often used in combination with three other drugs to palliate dogs with heart failure (pulmonary edema, pleural effusion, ascites). These are:

Other drugs may also be used as required to manage certain arrhythmias that are often associated with heart disease.

Synthesis

Pimobendan can be synthesized beginning with anisoyl chloride.


See also

References

  1. 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.
  2. 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): 1124–35. doi:10.1111/j.1939-1676.2008.0150.x. PMID 18638016.
  3. "Kusuri-no-Shiori Drug Information Sheet". RAD-AR Council, Japan. April 2005. Retrieved 2008-08-06.
  4. Hata K1, Goto Y, Futaki S, Ohgoshi Y, Yaku H, Kawaguchi O, Takasago T, Saeki A, Taylor TW, Nishioka T, et al. Mechanoenergetic effects of pimobendan in canine left ventricles. Comparison with dobutamine. Circulation. 1992 Oct;86(4):1291-301.
  5. Goto Y1, Hata K. Mechanoenergetic effect of pimobendan in failing dog hearts. Heart Vessels. 1997;Suppl 12:103-5.
  6. Verdouw PD, Hartog JM, Duncker DJ, Roth W, Saxena PR. Cardiovascular profile of pimobendan, a benzimidazole-pyridazinone derivative with vasodilating and inotropic properties. Eur J Pharmacol. 1986 Jul 15;126(1-2):21-30.
  7. Kanno N, Kuse H, Kawasaki M, Hara A, Kano R, Sasaki Y. Effects of pimobendan for mitral valve regurgitation in dogs. J Vet Med Sci. 2007 Apr;69(4):373-7.
  8. http://www.vetmedin.com/Vetmedin%20Insert_6-07.pdf
  9. Hanzlicek AS1, Gehring R, Kukanich B, Kukanich KS, Borgarelli M, Smee N, Olson EE, Margiocco M. Pharmacokinetics of oral pimobendan in healthy cats. J Vet Cardiol. 2012 Dec;14(4):489-96.


Template:Phosphodiesterase inhibitors