Amrinone
- 3-amino- 5-(4 -pyridinyl) -2 ( 1H) -pyridinone
- Inamrinon ( USAN )
C01CE01
PDE inhibitors
294-297 ° C
Risk
102 mg · kg -1 ( LD50, rat, oral)
Template: Infobox chemical / molecular formula search available
Amrinone is no longer available in German-speaking drug, the - one of the inhibitors of phosphodiesterase ( PDE) - as enoximone and milrinone. It causes a drop in blood pressure and increases the force of contraction of the heart.
Mechanism of action
Amrinone inhibits the isoenzyme III phosphodiesterase, which catalyzes the breakdown of cAMP. It will not work on membrane- bound receptors.
At the heart of the accumulation of cAMP causes activation of protein kinase A. This phosphorylates calcium channels and opens it, so that more calcium ions to enter (Ca2 ) in the heart muscle cells. Thus, the force of contraction of heart muscle cells is increased ( positive inotropic ).
In the smooth muscle cells of the peripheral blood vessels, the Ca2 concentration is increasing from the vessel wall and relaxes, so that the blood pressure decrease.
Thus, amrinone belongs to the group of Inodilatoren.
Application
Studies report little about the long-term benefits, however, but by frequent side effects. Amrinone was only for short-term treatment of patients with heart failure (NYHA IV), did not respond to digitalis, diuretics or ACE inhibitors, applied. Because of the reduction of pulmonary arterial blood pressure, it has also been used in primary or secondary pulmonary hypertension, and by a heart-lung transplants.
Unwanted side effects are:
- Ventricular arrhythmias,
- Supra-and ventricular tachycardia to ventricular fibrillation,
- Drop in blood pressure,
- Nausea, vomiting, abdominal pain, fever, myalgia, taste disturbance, Milzschwellungen.
Contraindications are:
- Volume depletion,
- Cardiac arrhythmia,
- Renal insufficiency,
- Pregnancy and lactation,
- Heart failure,
- Severe obstructive aortic or Pulmonalklappenerkrankungen.
Dobutamine enhances the effects of PDE inhibitors additively.
Commercial preparations
This was introduced in 1981 amrinone is not more than commercial product available in Germany, Austria, Belgium, Luxembourg and Switzerland. By 2005, it was sold under the trademark Wincoram ®. In the USA sold under the trademark amrinone Inocor ®.