Levosimendan

Levosimendan

Mechanism of action

  • sensitizes cardiac muscle to Ca2+ (calcium sensitizer)
  • produces vasodilation by opening ATP-sensitive K+ channels in vascular smooth muscle
    -> reduces preload, afterload, improves O2 supply to myocardium, increases coronary blood flow and renal blood flow
  • in contrast to dobutamine, can be used with beta-blockers
  • also has anti-inflammatory and anti-apoptotic effects

Indications and dose

Side-effects

Hypotension

Headache

Arrhythmias

Pharmacokinetics

Onset: Rapidly distributed.

Peak plasma concentration of active metabolite in 48–78 hours

Bioavailability: 85%

Metabolism: Hepatic

Half-life of elimination: 1 hour (levosimendan), 70 hours (metabolites)

Excretion: Urine and faeces

Directions for administration

Dilute with 500 ml of 5% glucose.

Full loading of levosimendan = 25 mg!!!

Medicinal forms

1 vial = 12.5 mg in 5 ml (1 ml=2.5 mg)

References

  1. https://litfl.com/levosimendan/ 
  2. https://www.uptodate.com/contents/levosimendan-international-drug-information-concise?search=levosimendan&source=panel_search_result&selectedTitle=1~10&usage_type=panel&kp_tab=drug_international&display_rank=1 
  3. https://en.wikipedia.org/wiki/Levosimendan