PDE3 inhibitor

Phosphodiesterase -3 inhibitors are a sub- group of drugs from the group of phosphodiesterase inhibitors, which are approved for the treatment of acute heart failure in the absence of catecholamines response by down-regulation of receptors on the myocardium.

Actually approved drugs are amrinone, cilostazol, milrinone and enoximone. For use on dogs, the active ingredient pimobendan is approved.

Indication

Treatment of acute heart failure and cardiac shock.

Mechanism of action

By inhibiting phosphodiesterase -3 it comes to increasing the second messenger cAMP. Characterized protein kinases are phosphorylated and activated calcium channels, whereby the inward calcium increases during the plateau phase of the action potential and increasing the calcium released from the sarcoplasmic reticulum. The effect is positive inotropic, that is, the force of contraction ( inotropy ) of the heart muscle is increased. In addition, the re-uptake of calcium into intracellular store ( sarcoplasmic reticulum ) is accelerated. Thus the PDE -3 inhibitors also have a positive lusitropic effect, ie they increase the relaxation rate, facilitate muscle relaxation. Furthermore, they do not have a vasodilatory effect and thus belong to the group of Inodilatoren.

Side effects

Reversible thrombocytopenia, elevation of transaminases, arrhythmias

Duration of use

Since the effect gradually weakens and it also comes to an unexplained increase in mortality in patients with heart failure are PDE 3 inhibitors only for short-term application is allowed (no more than 14 days).

Swell

  • Forth, HENSCHLER, Rummel, General and special pharmacology and toxicology, Munich 2002, page 457
  • Thiel, Roewer, Anaesthesiological pharmacotherapy, Stuttgart 2009, page 285f.
  • DGAI / DGTHT: Intensive Medical care of cardiac surgery patients. - Hemodynamic monitoring and cardiovascular therapy. In: www.awmf.org. Association of the Scientific Medical Societies in Germany (AWMF ), April 1, 2010, accessed on February 12, 2011.
  • Phosphodiesterase inhibitors
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