Strofantin K - instructions for use, dose, side effects, contraindications

Active substanceStrophantine-KStrophantine-K

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Strofantin® K

solution w / m in / in

GALICHFARM, PAO Ukraine

Dosage form: & nbspSolution for intravenous and intramuscular injection.

Composition:

1 ml of the solution contains:

active substance: strophanthin K - 0.25 mg;

auxiliary substances: ethanol (ethyl alcohol) 96% - 0.02 ml, water for injection up to 1 ml.

Description:Transparent colorless or slightly yellowish liquid.

Pharmacotherapeutic group:Cardiotonic is a cardiac glycoside.

ATX: & nbsp

C.01.A Cardiac glycosides

Pharmacodynamics:

Strofantin® K is a short-acting cardiac glycoside, blocks the transport

Na + / K + -ATPase, as a result, the content of sodium ions in cardiomyocytes increases, which leads to the opening of calcium channels and the entry of calcium ions into cardiomyocytes. Excess sodium ions leads to an acceleration of the release of calcium ions from the sarcoplasmic reticulum, i.e. the intracellular concentration of calcium ions increases, which leads to blockade of the troponin complex, which exerts a depressing effect on the interaction of actin and myosin.

Increases the strength and rate of contraction of the myocardium, which occurs by a mechanism different from the Frank-Starling mechanism, and does not depend on the degree of preliminary stretching of the myocardium; The systole becomes shorter and energy-efficient.As a result of increased myocardial contractility, the shock and minute volume of blood increases.

Reduces the end-systolic volume and the end-diastolic volume of the heart, which, along with an increase in the tone of the myocardium, leads to a reduction in its size, and so on. to a decrease in myocardial oxygen demand.

The negative dromotropic effect is manifested in the increased refractoriness of the atrioventricular node, which allows the drug to be used in paroxysms of supraventricular tachycardias and tachyarrhythmias. With ciliary tachyarrhythmia slows heart rate (heart rate), lengthen diastole, improving intracardiac and systemic hemodynamics. Decrease in heart rate occurs as a result of direct and indirect effects on the regulation of the heart rhythm. Has a direct vasoconstrictive effect (in the event that the positive inotropic effect of cardiac glycosides is not realized - in patients with normal contractility or with excessive stretching of the heart); in patients with chronic heart failure causes mediated vasodilating effect, reduces venous pressure, increases diuresis: reduces edema, dyspnea.Positive batmotropic effect is manifested in sub-toxic and toxic doses. Has an insignificant degree of negative chronotropic action. With intravenous administration (IV), the effect begins 10 minutes and reaches a maximum after 15-30 minutes.

Pharmacokinetics:

There is practically no cumulative effect.

Distribution relatively uniform; a little more concentrated in the tissues of the adrenal glands, pancreas, liver, kidneys. In the myocardium, 1% of the drug is found. Connection with blood plasma proteins - 5%.

Excretion. It is not subjected to biotransformation, it is excreted by the kidneys unchanged. Within 24 hours 85-90% of the drug is excreted; the concentration in blood plasma is reduced by 50% after 8 hours; completely eliminated from the body after 1 -3 days.

Indications:In the complex therapy of acute and chronic heart failure of the second functional class (in the presence of clinical manifestations), III-IV functional class according to the NYHA classification; tahisystolic form of flicker and atrial flutter of paroxysmal and chronic course (especially in combination with chronic heart failure).

Contraindications:Increased sensitivity to the drug, glycoside intoxication, Wolff-Parkinson-White syndrome, atrioventricular block II degree atrioventricular intermittent or complete blockage sinoatrialnaya.

Carefully:

Atrioventricular block I degree, sick sinus syndrome without pacemaker, the probability of unstable conduct by the atrioventricular node, indications of a history of attacks of Morgagni-Adams-Stokes, hypertrophic obstructive cardiomyopathy, isolated mitral stenosis with a rare heart rate, cardiac asthma in patients with mitral stenosis (in the absence tachysystolic atrial fibrillation), acute myocardial infarction, unstable angina, arteriovenous shunt, w poxvirus, constrictive pericarditis, heart failure with diastolic dysfunction (restrictive cardiomyopathy, amyloidosis heart, constrictive pericarditis, cardiac tamponade), ventricular premature beats, marked dilatation of the cavities of the heart, "pulmonary" heart. Atrial extrasystole due to the possibility of its transition into a flicker of the atria.

Electrolyte disorders: hypokalemia, hypomagnesemia, hypercalcemia, hypernatremia. Hypothyroidism, alkalosis, myocarditis, advanced age, renal and hepatic insufficiency, thyrotoxicosis.

Pregnancy and lactation:The drug is contraindicated during pregnancy and lactation due to the lack of data on safety of use.

Dosing and Administration:Strofantin® K is used intravenously, intramuscularly, only in urgent situations when it is impossible to apply cardiac glycosides inside. For intravenous administration, a 0.025% solution of the drug is used. It is diluted in 10 - 20 ml of a 5% solution of dextrose (glucose) or 0.9% sodium chloride solution. Introduction is carried out slowly, for 5-6 minutes (because a rapid injection can cause shock). Solution Strofantina ® K can be administered and drip (in 100 ml of a 5% solution of dextrose (glucose) or 0.9% solution of sodium chloride), because with this form of administration less toxic effect develops.

Higher doses of Strophantine® K for adults are intravenous: single dose - 2 ml (2 ampoules), daily - 4 ml (4 ampoules).

If intravenous injection is not possible, the drug is administered intramuscularly.To reduce the sharp painfulness with intramuscular injection, 5 ml of a 2% solution of procaine are preliminarily injected, and then through the same needle - the required dose of Strophantine® K diluted in 1 ml of a 2% solution of procaine. When administered intramuscularly, the doses increase 1.5 times.

Children: daily doses, they are the same dose of saturation with the application of 0.025% solution of Strofantin® K: to newborns - 0.06-0.07 ml / kg; up to 3 years - 0.04-0.05 ml / kg; from 4 to 6 years - 0,4 - 0,5 ml / kg; from 7 to 14 years - 0.5 - 1 ml. The maintenance dose is 1 / 2-1 / 3 of the saturation dose.

Side effects:

From the gastrointestinal tract: decreased appetite, nausea, vomiting, diarrhea.

From the cardiovascular system: bradycardia, extrasystole, atrioventricular block, ventricular paroxysmal tachycardia, ventricular fibrillation.

From the central nervous system: headache, dizziness, sleep disorders, fatigue, impaired color perception, depression, drowsiness, psychosis, confusion.

Other: allergic reactions, urticaria, petechiae, thrombocytopenia, thrombocytopenic purpura, nosebleeds, gynecomastia. With intramuscular route of administration, soreness at the site of administration.

Overdose:

Symptoms:

From the cardiovascular system: arrhythmias, including bradycardia, atrioventricular block, ventricular paroxysmal tachycardia, ventricular fibrillation, ventricular extrasystole (bigemia, polytopic), nodular tachycardia, sinoatrial blockade, flicker and atrial flutter. From the gastrointestinal tract: anorexia, nausea, vomiting, diarrhea. From the side of the central nervous system and sensory organs: headache, fatigue, dizziness, rarely - coloring of surrounding objects in green and yellow colors, sensation of flies flashing before the eyes, reduced visual acuity, scotoma, macro and microposs; very rarely, confusion, syncopal states.

Treatment: withdrawal of the drug or reduction of subsequent doses and increasing the time intervals between drug administration, administration of antidotes (sodium dimercaptopropanesulfonate), symptomatic therapy (antiarrhythmic drugs - lidocaine, phenytoin, amiodarone; preparations of potassium; m-holinoblokatory - atropine sulfate). As antiarrhythmic drugs - preparations of I class (lidocaine, phenytoin).With hypokalemia - IV injection of potassium chloride (6-8 g / day at the rate of 1-1.5 g per 0.5 L of a 5% solution of dextrose (glucose) and 6-8 units of insulin, injected drip, for 3 hours). With severe bradycardia, atrioventricular blockade - m-holinoblokatory. Beta-adrenomimetics is dangerous because of the possible increase in the arrhythmogenic effect of cardiac glycosides. With a full transverse blockade with attacks of Morgagni-Adams-Stokes, a temporary pacing.

Interaction:

When using Strofantin® K together with barbiturates (phenobarbital and others), the cardiotonic effect of glycoside decreases. Simultaneous use of Strofantin® K with sympathomimetics, methylxanthines, reserpine and tricyclic antidepressants increases the risk of arrhythmias. The concentration of Strofantin® K in the blood plasma increases with the simultaneous use of quinidine, methyldopa, amiodarone, captopril, calcium antagonists, erythromycin and tetracycline. Against the background of magnesium sulfate, the possibility of slowing the conduction and occurrence of atrioventricular blockade of the heart increases. Diuretics (mostly thiazide and inhibitors of carbonic anhydrase), corticotropin (adrenocorticotropic hormone) preparation, glucocorticosteroids, insulin, calcium preparations, laxatives, carbenoxolone, amphotericin B, benzylpenicillin, salicylates increase the risk of developing glycosidic intoxication. Beta-adrenoblockers, antiarrhythmics, verapamil can not only increase the severity of the decrease in atrioventricular conduction (negative dromotropic action), but also potentiate the negative chronotropic effect of the drug Strofantin® K (decreasing heart rate). Inductors of microsomal liver enzymes (phenytoin, rifampicin, phenobarbital, phenylbutazone), and neomycin and cytostatic agents reduce the concentration of Strofantin® K in the blood plasma. Glycoside intoxication can cause, due to the development of hypokalemia, the inhibitor of carbonic anhydrase, mineralocorticoids, so when used simultaneously with cardiac glycosides, it is required to regularly determine the potassium content in the blood plasma. Drugs of potassium salts can not be used if under the influence of cardiac glycosides there are conduction disorders on the electrocardiogram, however, potassium salts are often prescribed together with digitalis preparations to prevent cardiac rhythm disturbances.

Anticholinesterase drugs increase bradycardia with simultaneous use with cardiac glycosides; edetic acid reduces the efficacy and toxicity of cardiac glycosides; should not be used in conjunction with cardiac glycosides trifosadenine; hypervitaminosis, caused by vitamin D, increases the action of cardiac glycosides due to the development of hypercalcemia; there is evidence of a decrease in kidney secretion of cardiac glycosides under the influence of paracetamol. Glucocorticosteroids and diuretics increase the risk of hypokalemia and hypomagnesemia, angiotensin converting enzyme inhibitors and angiotensin II receptor blockers - reduce.

Special instructions:

With special care apply in patients with thyrotoxicosis and atrial extrasystole.

Given the small therapeutic index during treatment, careful medical supervision and individual dose selection are necessary.

If the impaired excretory function of the kidneys should reduce the dose (prevention of glycosidic intoxication).

The likelihood of an overdose increases with hypokalemia, hypomagnesemia, hypercalcemia, hypernatremia, marked dilatation of the heart cavities, "pulmonary" heart, alkalosis, in elderly patients.Particular caution and electrocardiographic control are required if atrioventricular conduction is impaired.

With severe mitral stenosis and normo- or bradycardia, chronic heart failure develops as a result of a decrease in diastolic filling of the left ventricle. Strofantin® K, increasing myocardial contractility of the right ventricle, causes a further increase in pressure in the pulmonary artery system, which can provoke pulmonary edema or aggravate left ventricular failure. Patients with mitral stenosis are assigned cardiac glycosides upon adherence to right ventricular failure or in the presence of atrial tachyarrhythmia. Strofantin® K in Wolff-Parkinson-White syndrome, reducing atrioventricular conduction, promotes impulses through additional pathways - bypassing the atrioventricular node, provoking the development of paroxysmal tachycardia. As one of the methods of digitalization control, monitoring of the plasma concentration of cardiac glycosides is used.

With rapid intravenous administration, it is possible to develop bradyarrhythmia, ventricular tachycardia, atrioventricular blockade, and cardiac arrest.At the maximum of the action may appear extrasystole, sometimes in the form of bigeminy. To prevent this effect, the dose can be divided into 2-3 intravenous injections or the first of the doses is administered intramuscularly. If the patient was previously assigned other cardiac glycosides, it is necessary to take an intravenous injection of Strophantine ® K (5-24 days - depending on the degree of cumulative properties of the previous drug).

Effect on the ability to drive transp. cf. and fur:During the treatment period it is necessary to refrain from driving motor vehicles and practicing potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions (driving a car, etc.).

Form release / dosage:

Solution for intravenous and intramuscular injection 0.25 mg / ml.

Packaging:

1 ml per ampoule of clear, colorless glass.

For 10 ampoules, together with instructions for medical use and scarifier ampullum is put in a box with a corrugated liner.

Or 10 ampoules per contour cell pack. One out-of-the-box cell pack, together with a medical instruction and a scarifier, is put into a pack.

When using ampoules with a dot or a ring of fracture, the insertion of scarifiers is not provided.

Storage conditions:Store at a temperature not exceeding 25 ° C. Keep out of the reach of children.

Shelf life:3 years. Do not use the product after the expiration date printed on the package!

Terms of leave from pharmacies:On prescription

Registration number:010675

Date of registration:20.09.2011

The owner of the registration certificate:GALICHFARM, PAO GALICHFARM, PAO Ukraine

Manufacturer: & nbsp

GALICHFARM, PAO Ukraine

Representation: & nbspARTERIUM Corporation ARTERIUM Corporation Ukraine

Information update date: & nbsp25.08.2015

Illustrated instructions

Instructions

Strofantin® K (Strophanthin® K)