NON-ADRENERGIC

Ca sensitizer and PDE-III inhibitor
selectively

short term management of severe acute heart failure

in IV form only - clear yellow solution 2.5mg/mL in 5 and 10ml vials

Increases Myofilament Ca sensitivity, vasodilation

i) ↑myofilament Ca sensitivity by binding to Cardiac trop C in Ca-dependent manner.
ii) Vasodilation through opening of ATP-sensitive K channels
iii) selective PDE-III inhibition at higher conc - inotropy

CVS:
- Increased cardiac output without increasing MVO2
- Causes coronary and peripheral vasodilation → anti-ischaemia and anti-stunning effects

GU:
Increased GFR and UO secondary to increased CO

Interference with potassium channels causes an increase in the QTc- theoretical ↑risk of arrhythmias. May cause hypotension. Caution should be exercised in
patients with renal or hepatic impairment.

IV only

small vd

98% protein binding.
Peak concentration after 48 hrs

0.2 L/kg

Intestinal bacteria OR1896 active metabolite

Hepatic conjugation

excretion renal and fecal. Cardiac Effects 2-7 days

1 hour (70hr for active metabolite)

IV, loading dose of 6 to 24 mcg/kg over 10 minutes
then continuous infusion of 0.05-0.2 mcg/kg/min

Level 3

Level 1