Levosimendan ( TIN ) / ˌ l iː v oʊ s aɪ ˈ m ɛ n d ən / is a calcium sensitizer used in the treatment of acute decompensated heart failure . It is sold under the trademark of Simdax ( Orion Corporation ).
Content
Mechanism of Action
Levosimendan is a calcium sensitizer - increases the sensitivity of the heart to calcium, thereby increasing cardiac compressibility without increasing intracellular calcium. Levosimendan has a positive inotropic effect due to an increase in calcium, the sensitivity of myocytes by binding to cardiac troponin C in a calcium-dependent manner. It also has a vasodilating effect, opening adenosine triphosphate (ATP) -sensitive potassium channels in the vascular smooth muscles , causing relaxation of smooth muscles. The combination of inotropic and vasodilator action leads to an increase in contraction force, a decrease in preload and a decrease in cardiac afterload. In addition, the drug has a cardioprotective effect. [one]
Clinical application
Indications
Levosimendan is used in connection with acute decompensated severe chronic heart failure .
[2]
[3]
Licensing Status
At Orion Corporation, which initially developed levosimendan and applied for a new drug in 1998 in the United States, the FDA requested further testing and Orion withdrew the application in November 1999. Orion initially obtained permission to sell the drug in Sweden in 2000. [4] Since then, 60 countries around the world have approved the drug, but it is still not licensed in the United States, where it is currently under development to reduce the incidence and mortality of cardiac patients due to low cardiac output syndrome. [five]
Contraindications
The use of levosimendan is contraindicated in patients with: moderate to severe renal failure , severe liver failure, severe ventricular filling or outflows, severe hypotension and tachycardia . [6]
Side Effects
headache, arterial hypotension, arrhythmias ( atrial fibrillation , extrasystole , atrial tachycardia , ventricular tachycardia), myocardial ischemia , hypokalemia and / or nausea (Rossi, 2006).
Compositions
Levosimendan is positioned as a 2.5 mg / ml concentrated solution for infusion. The concentrate is diluted with glucose 5% solution before infusion.
Links
- ↑ Levosimendan: Molecular Mechanisms and Clinical Implications: Consensus of Experts on the Mechanisms of Action of Levosimendan (English) // International Journal of Cardiology : journal. - 2012 .-- 23 August ( vol. 159 , no. 2 ). - P. 82-7 . - DOI : 10.1016 / j.ijcard.2011.07.022 . - PMID 21784540 .
- ↑ Levosimendan: Current Data, Clinical Use and Future Development (Neopr.) // Heart, Lung and Vessels. - 2013. - T. 5 , No. 4 . - S. 227-245 . - PMID 24364017 .
- ↑ Levosimendan vs Dobutamine for Patients with Acute Decompensated Heart Failure: the SURVIVE Randomized Trial (English) // JAMA: journal. - 2007 .-- 2 May ( vol. 297 , no. 17 ). - P. 1883-1891 . - DOI : 10.1001 / jama.297.17.1883 . - PMID 17473298 .
- ↑ Orion Simdax (levosimendan) Fact Sheet . Orion. Date of treatment February 16, 2013. Archived on May 28, 2012.
- ↑ Oxygen Biotherapeutics Product Pipeline - Levosimendan development . Oxygen Biotherapeutics. Date of treatment February 13, 2013.
- ↑ Rossi S, editor.