Simdax - instructions for use, reviews, analogs and forms of release (injections in ampoules for injection in a solution of 2.5 mg in 1 ml) of a drug for the treatment of chronic heart failure in adults, children and pregnancy. Composition

In this article, you can read the instructions for using the drug Simdax. There are reviews of visitors to the site - consumers of this medication, as well as opinions of specialists on the use of the syndrome in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of the Syndax if there are existing structural analogues.Use for the treatment of chronic heart failure in adults, children, as well as during pregnancy and lactation. Composition of the preparation.

Simdax cardiotonic. Increases the sensitivity of contractile proteins to calcium by binding to troponin C of the myocardium in the calcium-dependent phase. Levosimendan (the active ingredient of the preparation Simdax) increases the strength of the heartbeat, but does not affect the relaxation of the ventricles. Has vasodilating effect on arteries (including coronary) and veins. Levosimendan is a selective inhibitor of the enzyme phosphodiesterase (PDE) 3 in vitro. Due to the presence of a positive inotropic and vasodilating effect, in heart failure increases the force of the heartbeats and reduces both preload and postload.

Levosimendan activates the ischemic myocardium in patients after coronary angioplasty or thrombolysis. It increases coronary blood flow in patients undergoing cardiac surgery and improves myocardial perfusion in patients with heart failure. These positive effects are achieved without a significant increase in myocardial oxygen consumption.Simdax significantly reduces the circulating level of endothelin-1 in chronic heart failure. The drug causes a dose-related increase in cardiac output and stroke volume, as well as a dose-dependent decrease in pressure in the pulmonary capillary network, a decrease in mean arterial pressure (BP) and total peripheral vascular resistance (OPS).

The positive effect on cardiac output and pressure in the pulmonary capillaries is maintained for at least 24 hours after discontinuation of the infusion. The effect on blood pressure, as a rule, lasts 3-4 days. When used in therapeutic doses, one pharmacologically active metabolite is formed which gives hemodynamic effects similar to levosimendan, persisting up to 7-9 days after discontinuation of the infusion.

Composition

Levosimendan + auxiliary substances.

Pharmacokinetics

The maximum concentration of levosimendan in the blood plasma is reached approximately 2 days after discontinuation of the drug administration. Binding to blood plasma proteins (mainly with albumin) is 97-98%. The binding with proteins of the active metabolite is 40%. Simdax is almost completely metabolized.About 5% of the administered dose is metabolized in the small intestine by reduction to aminophenylpyridazinone, which after reabsorption is metabolized with the participation of N-acetyltransferase to the active metabolite. The drug is produced almost completely in the form of metabolites: with urine - 54%, with feces - 44%. Less than 0.05% is excreted in the urine unchanged. With a mild degree of hepatic insufficiency associated with cirrhosis, the withdrawal of levosimendan is somewhat delayed.

Indications

• severe chronic (congestive) heart failure in the stage of acute decompensation (for short-term therapy with ineffective standard therapy and the need to maintain contractile function of the myocardium).

Forms of release

Concentrate for the preparation of a solution for infusions of 2.5 mg in 1 ml (injections in ampoules for injection).

Instructions for use and dosing regimen

Only for hospital use. Intravenously, with the help of infusion. Concentrate Syndaksa 2.5 mg / ml should be used only in diluted form.

To prepare an infusion solution with a concentration of 0.05 mg / ml, dilute 10 ml of levosimendan concentrate 2.5 mg / ml in 500 ml of a 5% solution of Dextrose (glucose).To prepare an infusion solution of 0.025 mg / ml, dilute 5 ml of levosimendan concentrate 2.5 mg / ml in 500 ml of a 5% solution of dextrose (glucose). Concentrate Symdaksa 2.5 mg / ml is intended for single use only.

Before infusion, diluted solution, like other preparations for parenteral use, should be checked for foreign particles and discoloration. When stored, the color of the concentrate may change to orange, which is not accompanied by a decrease in the activity of the preparation.

Infusion can be carried out through peripheral or central veins. The dose and duration of treatment are selected individually, taking into account the clinical state of the patient and the therapeutic effect.

Treatment begins with a loading dose of 6-12 mcg per 1 kg of body weight, which is injected for 10 minutes. Continuous infusion is then carried out at a rate of 0.1 μg per kg per minute. A lower dose (6 μg per kg) is recommended for patients receiving concomitant intravenous therapy with vasodilators and / or inotropic agents. The administration of a higher loading dose (12 μg per kg) will be accompanied by a stronger hemodynamic effect, but it is possible that the frequency of transient side effects will also increase.

The response of the patient to therapy is assessed by the administration of a loading dose or within 30-60 minutes after dose adjustment or depending on the clinical picture. With pronounced changes in the parameters of hemodynamics (arterial hypotension, tachycardia), the infusion rate should be reduced to 0.05 μg per kg per minute or infusion should be stopped. With good tolerability of the initial dose and the need for a more pronounced hemodynamic effect, the infusion rate can be increased to 0.2 μg per kg per minute.

The recommended duration of the infusion is 24 hours. After the termination of Symdax infusion, signs of development of tolerance or withdrawal syndrome were not revealed.

Hemodynamic effects are observed for at least 24 hours and can persist for 9 days after completion of the 24-hour infusion.

Side effect

• significant reduction in blood pressure;
• extrasystole (violation of the heart rhythm);
• Atrial fibrillation, atrial flutter (cardiac rhythm disturbance);
• tachycardia, ventricular tachycardia (rapid heart rate);
• Myocardial ischemia (coronary blood flow, when the volume of blood flowing to the heart muscle is not sufficient to ensure normal operation of the heart with the available load);
• dizziness, headache;
• nausea, vomiting;
• reduction of hemoglobin, hematocrit, hypokalemia.

Contraindications

• mechanical obstruction (blockage), preventing the filling of the ventricles or the release of blood from the ventricles;
• severe renal impairment with creatinine clearance (CK) of less than 30 mL per minute;
• severe violations of liver function;
• arterial hypotension (low blood pressure);
• tachycardia;
• trembling-fibrillation of ventricles in the anamnesis;
• uncontrolled hypokalemia;
• children and adolescents under 18;
• hypersensitivity to levosimendan.

Application in pregnancy and lactation

Clinical experience with the use of Symdax during pregnancy is absent. The application is only possible in cases where the expected benefit of therapy for the mother exceeds the potential risk to the fetus.

In experimental studies, a toxic effect on reproduction was noted.

It is not known whether levosimendan is excreted in breast milk. The patient should refuse breastfeeding for a period of 14 days after the infusion.

Use in children

Contraindicated in children and adolescents under 18 years.

Application in elderly patients

Correction of dose in elderly patients is not required.

special instructions

With extreme caution apply in acute heart failure due to extracardiac causes; with severe decompensated heart failure after surgery; severe heart failure in patients awaiting transplantation.

Caution should be used in patients with mild to moderate renal insufficiency, mild to moderate hepatic impairment, concomitant anemia, atrial fibrillation, in patients with existing myocardial ischemia, prolongation of the QT interval of different genesis, or concomitant administration of QT prolonging drugs (only under the careful control of the electrocardiogram (ECG)).

Data on the safety and efficacy of the use of Symdax are absent in the following diseases: hypertrophic obstructive cardiomyopathy, severe mitral valve insufficiency, rupture, myocardial perforation, cardiac gemotamponade, right ventricular infarction and potentially life-threatening arrhythmia of 3 months or more.

During treatment, ECG, blood pressure, heart rate (heart rate) and diuresis should be constantly monitored.In addition, it is necessary to monitor the dynamics of heart failure symptoms, invasive methods for monitoring hemodynamics are recommended for this.

Non-invasive monitoring is recommended after the end of infusion for at least 3 days or until hemodynamics stabilize. In patients with mild to moderate renal or hepatic impairment, monitoring should be performed for at least 5 days.

In patients with impaired liver and kidney function, the concentration of metabolites may increase, resulting in a more intense and prolonged effect on heart rate.

Before using levosimendan, hypokalemia, hypovolemia should be corrected. During the treatment should be monitored the potassium content in the serum.

If there are abrupt fluctuations in blood pressure or heart rate, you should reduce the rate of administration or cancel the infusion.

In patients with severe cardiac dysfunction, levosimendan should be used under constant monitoring of cardiac output and filling pressure.

Before using Symdaksa, it is necessary to stop arrhythmia and stabilize the clinical state of patients with a constant form of ventricular tachycardia,paroxysmal tachycardia, not associated with reperfusion or life-threatening forms of arrhythmia.

After discontinuation of treatment, withdrawal syndrome is not observed.

Drug Interactions

Derivation of levosimendan metabolite from the body has not been studied enough, so the drug interaction associated with this process is difficult to predict; it is believed that there is a risk of a more pronounced and prolonged effect on the heart rate.

With the simultaneous use of isosorbide mononitrate, there is a risk of increasing the hypotensive effect.

Analogues of the medicinal product

Structural analogs for the active substance:

• Levosimendan.

Analogues of the preparation of Simdaks on the pharmacological group (cardiac glycosides and non-glycosidic cardiotonic agents):

• Adonid concentrated;
• Aurocard;
• Hawthorn tincture;
• Hawthorn fruit extract is dry;
• Hawthorn fruits;
• Hawthorn flowers;
• Hawthorn flowers and leaves extract dry;
• Hawthorn extract is liquid;
• Goricolvet extract is thick;
• Digoxin;
• Digofton;
• Dobutamine;
• Extracted;
• Dobutrex;
• Dopamine;
• Dopmin;
• Doppelherz;
• Dopamine;
• An icteric spreading extract is liquid;
• Cardioval;
• Cardiotron;
• Cardiaplant;
• Korglikard;
• Korglikon;
• Cratched;
• Kratagus;
• Kregium;
• Lanatoside C;
• Lily of the valley tincture;
• Lily-Valerian drops;
• Lydyshev-Leonurus drops;
• Levosimendan;
• Novodigal;
• Strofantin;
• Taukrat;
• Ubidecarenone;
• Celanide.

Response of a cardiologist

Simdax is an expensive medication, which limits its use in practice in the treatment of decompensated congestive heart failure. A rare patient can afford to buy this medicine. Patients tolerate therapy well, but there are side effects. Most often it is dizziness, marked decrease in blood pressure, vomiting, disturbances of the heart rhythm. But in our department there is all the necessary equipment for monitoring the patient's condition during the introduction of Simex. Therefore, we almost always manage to cope with these undesirable reactions on time.

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