Chemistry:Enoximone
Enoximone (INN, trade name Perfan) is an imidazolinone phosphodiesterase inhibitor.[1] It is used in the treatment of congestive heart failure and is selective for phosphodiesterase 3.
Medical uses
Enoximone produces haemodynamic improvement and a fall in pulmonary wedge pressure and vascular resistance. It is used as short-term treatment in acute decompensated heart failure and as a bridge to cardiac transplantation.[2]
However a systematic review of oral phosphodiesterase 3 inhibitors in chronic heart failure, found that longer-term use of enoximone was associated with an increased risk of arrhythmia and mortality, which has limited its role to short-term, intravenous therapy rather than chronic oral treatment.[3][4]
Pharmacology
Pharmacokinetics
Enoximone has an elimination half-life in the range of 4–10 hours with about 85% plasma protein binding.[5]
Pharmacodynamics
Enoximone is a imidazolone derivative that acts as a selective phosphodiesterase 3 (and, to a lesser extent, 4) inhibitor, raising intracellular cyclic AMP in cardiac and vascular smooth muscle to produce positive inotropic and vasodilator effects without significantly increasing cardiac oxygen demand.[4][2]
References
- ↑ "Enoximone". Drugs 42 (6): 997–1017. 1991. doi:10.2165/00003495-199142060-00008. PMID 1724645.
- ↑ 2.0 2.1 "The evolving role of the cardiac inotrope, enoximone, in heart failure.". The British Journal of Cardiology (Acute & Interventional Cardiology) 9 (1): 26–31. 2002. https://bjcardio.co.uk/files/pdf/aic/2002/Br-J-Cardiol-2002-9-aic26-aic31.pdf.
- ↑ "Phosphodiesterase III inhibitors for heart failure". The Cochrane Database of Systematic Reviews 2005 (1). January 2005. doi:10.1002/14651858.CD002230.pub2. PMID 15674893.
- ↑ 4.0 4.1 "Enoximone. A review of its pharmacological properties and therapeutic potential". Drugs 42 (6): 997–1017. December 1991. doi:10.2165/00003495-199142060-00008. PMID 1724645.
- ↑ "Enoximone". DrugBank. https://go.drugbank.com/drugs/DB04880.
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