Enoximone

Absorption

Bioavailabvility is 50% following oral administration.

Description

Enoximone is a phosphodiesterase inhibitor indicated for selective use as a cardiostimulant in heart transplant patient maintenance. It is currently being investigated for other indications including acute congestive heart failure.

Originator

Merrell Dow (USA)

The Uses of Enoximone

Enoximone is a phosphodiesterase inhibitor used in the treatment of congestive heart failure and is selective to phosphodiesterase 3. Potent PDE-3 inhibitor.

Indications

For the treatment of congestive heart failure.

What are the applications of Application

Enoximone is a selective phosphodiesterase III (PDE3) inhibitor

Background

Enoximone is a selective phosphodiesterase inhibitor with vasodilating and positive inotropic activity that does not cause changes in myocardial oxygen consumption. It is used in patients with congestive heart failure. Trials were halted in the U.S., but the drug is used in various countries.

Definition

ChEBI: Enoximone is an aromatic ketone.

brand name

Perfan IV

Biological Activity

Inhibitor of type III phosphodiesterase (PDE3). Increases intracellular cyclic AMP (cAMP) concentrations and enhances myocardial contractility. Also induces concentration-dependent vasodilation in vitro .

Biochem/physiol Actions

Selective phosphodiesterase III (PDE3) inhibitor. Prevents the degradation of cAMP by PDE. Increased cAMP results in enhanced contractility of the heart.

Pharmacokinetics

Enoximone is a phosphodiesterase inhibitor (type III) that increases the force of contraction of the heart and dilates blood vessels. In June 2005, Myogen announced that they were discontinuing development of enoximone due to negative results. The drug is approved for use in the UK.

Metabolism

Hepatic oxidation

storage

Store at +4°C