Levosimendan (Levosimendanum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
Read on
Clinical and pharmacological group: & nbsp

Cardiac glycosides and non-glycosidic cardiotonic agents

Included in the formulation
  • Levosimendan-J
    concentrate d / infusion 
    ESCO PHARMA, LLC    
  • Levosimendan-native
    concentrate d / infusion 
    NATIVA, LLC     Russia
  • Simdax
    concentrate d / infusion 
    Orion Corporation     Finland
    • Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):

    VED

    АТХ:

    C.01.C.X   Other cardiotonic drugs

    C.01.C.X.08   Levosimendan

    Pharmacodynamics:

    Cardiotonic. It binds to the troponin C of the myocardium in the calcium-dependent phase, increasing the sensitivity of contractile proteins to calcium ions. Increases the power of the heart, without affecting the relaxation of the ventricles. Has vasodilating effect on arteries (including coronary) and veins. Activates the ischemic myocardium after thrombolysis or coronary angioplasty.

    Has a positive vasodilating and inotropic effect, due to which it increases the force of heart contractions, reducing preload and afterload.

    Improves myocardial perfusion in patients with heart failure, increases coronary blood flow after heart surgery. Reduces the level of circulating endothelin-1 in chronic heart failure.

    It determines the dose-dependent decrease in pressure in the pulmonary capillary network,mean arterial blood pressure and total peripheral vascular resistance also provides a dose-dependent increase in stroke volume and cardiac output within 24 hours after the end of perfusion.

    During 3-4 days, the influence on blood pressure continues due to the formation of an active metabolite, whose action is similar to levosimedan, so that hemodynamic effects persist for 7-9 days after 24 hours perfusion.

    Pharmacokinetics:

    The maximum concentration in the plasma after the administration of the drug is achieved after 2 days. The association of the drug with plasma proteins is 97-98%, active metabolite - 40%.

    Primary metabolism is carried out by conjugation with cyclic or with N-acetylated cysteinyl glycine and cysteine ​​conjugates. Up to 5% of the administered dose of the drug is metabolized in the small intestine to aminophenylpyridazionone, which, with the participation N-Acetyltransferase is converted into an active metabolite.

    The half-life of levomisedate is 1 hour; active metabolite - about 75-80 h.

    Elimination of the drug in the form of metabolites by the kidneys is 54%, with feces - 44%, about 0.05% is excreted unchanged in the urine.

    Indications:

    It is used in severe chronic heart failure in the stage of decompensation in order to maintain contractile function of the myocardium.

    ICD-10

    IX.I30-I52.I50.0   Congestive heart failure

    Contraindications:

    Mechanical obstruction of the heart valves, severe violations of the liver and kidneys (creatinine clearance less than 30 ml / min), hypokalemia, individual intolerance.

    Carefully:

    Ischemic heart disease, severe hypotension (systolic pressure below 90 mm Hg), renal and hepatic insufficiency of mild and moderate degree. Patients with severe heart failure awaiting transplant surgery.

    Pregnancy and lactation:

    Recommendations for FDA - Category C. It is used for pregnant women according to vital indications. There is no evidence of ingestion into breast milk, it is recommended to stop breastfeeding for 14 days after the infusion of the drug.

    Dosing and Administration:

    It is administered intravenously only in a hospital! Loading dose: 6-12 mcg / kg for 10 minutes. Subsequently, they switch to continuous infusion of the drug at a rate of 0.1 μg / min for 24 hours.

    The highest daily dose: calculated individually and depends on the patient's body weight.

    The highest single dose: 12 mcg / kg.

    Side effects:

    Central nervous system: dizziness, headache.

    The cardiovascular system: decrease in blood pressure, myocardial ischemia.

    The system of hematopoiesis: anemia, decrease in hematocrit.

    Digestive system: nausea, vomiting.

    Allergic reactions.

    Overdose:

    Symptoms: increased adverse reactions, atrial fibrillation, atrial flutter, tachycardia.

    Treatment: reduction in the rate of drug administration or termination of infusion.

    Interaction:

    Fully compatible with digoxin, nitroglycerin, furosemide.

    With the simultaneous application of isosorbide mononitrate, the hypotensive effect may increase.

    Special instructions:Intravenous perfusion of the drug is carried out only in a specialized hospital with the necessary equipment for continuous monitoring of vital body functions.
    Instructions
    Up