Strofantin mechanism of action pharmacology. Application for violations of liver function

Instructions for medical use

medicinal product

STROFANTIN K

Tradename

Strofantin K

International non-proprietary name

Dosage form

Solution for injection, 0.25 mg/ml

Compound

1 ml of solution contains:

activesubstance: strophanthin K 0.25 mg;

Excipients: ethanol 96%, water for injections.

Description

transparent colorless or yellowish color liquid.

Pharmacotherapeutic group

Drugs for the treatment of heart disease. cardiac glycosides. Strophanthus glycosides. Strofantin.

ATX code C01AC01

Pharmacological properties

Pharmacokinetics.

The therapeutic effect is observed within 5-10 minutes after intravenous administration and reaches a maximum after 15-30 minutes. The half-life of Strofantin K from blood plasma is on average 23 hours. The cumulative effect is practically absent.

Pharmacodynamics.

Strophanthin K is a mixture of cardiac glycosides (K-strophanthin-β, K-strophanthoside, etc.) from the seeds of the tropical liana Strophathus Kombe Oliver and belongs to the group of so-called polar (hydrophilic) cardiac glycosides, which are poorly soluble in lipids and poorly absorbed from gastrointestinal tract. The mechanism of action is associated with the blockade of Na + -K + -ATPase, the effect on Na + -Ca 2+ metabolism, which improves contractility myocardium. The drug potentiates the strength and speed of heart contractions, lengthens diastole, improves blood flow to the ventricles of the heart, increases stroke volume, has little effect on the function of n. vagus.

Indications for use

Acute cardiovascular failure

Chronic heart failure II B - III stages (supraventricular arrhythmias, atrial fibrillation and flutter).

Dosage and administration

Strofantin K is used intravenously (sometimes intramuscularly). For intravenous administration, the drug is diluted in 10-20 ml of isotonic sodium chloride solution. The drug is administered slowly, over 5-6 minutes. In the first 2 days, you can enter 2 times a day.

A solution of Strophanthin K can also be administered intravenously (in 100 ml of isotonic sodium chloride solution), since with this form of administration less often develops toxic effect. If Strofantin K cannot be injected into a vein, then it is prescribed intramuscularly. In this way, the dose of the drug is increased by 1.5 times.

The maximum doses of Strofantin K for adults intravenously: single - 0.0005 g (0.5 mg), daily - 0.001 g (1 mg).

Daily doses, they are also saturation doses when using 0.25 mg / ml of Strofantin K solution: from birth to 2 years - 0.01 mg / kg / day (0.04 ml / kg); from 2 years old - 0.007 mg / kg / day (0.03 ml / kg).

The maintenance dose is ½ - ⅓ of the saturation dose.

Side effects

loss of appetite, nausea, vomiting, diarrhea.

From the side of cardio-vascular system: ventricular arrhythmias, bradycardia, atrioventricular block.

From the side nervous system: headache, dizziness, sleep disturbance, fatigue, rarely - a violation color vision, depression, psychosis.

Other: allergic reactions, urticaria, thrombocytopenia, thrombocytopenic purpura, epistaxis, petechiae, gynecomastia.

Contraindications

Organic lesions of the heart and blood vessels

Acute myocarditis, endocarditis

Severe cardiosclerosis

Acute myocardial infarction

Atrioventricular block II-III degree

Severe bradycardia

Hypertrophic obstructive cardiomyopathy

Constrictive pericarditis

Hypercalcemia

hypokalemia

carotid sinus syndrome

Aneurysm thoracic aorta

weakness syndrome sinus node

WPW syndrome

Glycoside intoxication

Pregnancy and lactation.

Drug Interactions

When Strofantin K is used together with barbiturates (phenobarbital, etaminal sodium, etc.), the cardiotonic effect of the glycoside decreases. Simultaneous use of Strophanthin K with sympathomimetics, methylxanthines, reserpine and tricyclic antidepressants increases the risk of arrhythmias. The concentration of Strophanthin K in plasma increases with the simultaneous administration of quinidine, amiodarone, captopril, calcium antagonists, erythromycin and tetracycline. Against the background of magnesium sulfate, the possibility of slowing down the conduction and the occurrence of atrioventricular heart block increases.

Saluretics, adrenocorticotropic hormones, glucocorticosteroids, insulin, calcium preparations, laxatives, carbenoxolone, amphotericin B, benzylpenicillin, salicylates increase the risk of glycoside intoxication. Antiarrhythmic drugs, including beta-adrenergic receptor blockers, potentiate the negative chrono- and dromotropic effect of the glycoside. Inducers of microsomal liver enzymes (phenytoin, rifampicin, phenobarbital, phenylbutazone, spironolactone), as well as neomycin and cytostatic agents reduce the concentration of Strofantin K in blood plasma. Calcium preparations increase sensitivity to cardiac glycosides.

special instructions

With caution, the drug should be prescribed for hypomagnesemia, hypernatremia, hypothyroidism, severe dilatation of the heart cavities, cor pulmonale, myocarditis, obesity and the elderly, since in these cases the likelihood of intoxication increases.

With rapid intravenous administration of the drug, bradyarrhythmia may develop, ventricular tachycardia, atrioventricular block and cardiac arrest. At the maximum of action, extrasystole may appear, sometimes in the form of bigeminia. To prevent the occurrence of this effect, the dose can be divided into 2-3 intravenous injections, or the first dose should be administered intramuscularly. In the case of previous treatment with other cardiac glycosides before intravenous administration Strofantina K take a break (otherwise there may be a toxic effect of the summation of the action of glycosides). The duration of the break is from 5 to 24 days, depending on the manifestations of the cumulative properties of the previous drug.

Due to the pronounced cardiotropic effect of the drug and the speed of its action, maximum accuracy in dosages and indications for use is required.

Treatment is carried out under constant ECG control.

Application in pediatrics

By strict indications used from birth.

Pregnancy and lactation

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

Features of the effect of the drug on the ability to drive vehicle or potentially dangerous mechanisms

Overdose

Symptoms of an overdose are varied.

From the side of the cardiovascular system: arrhythmias, including bradycardia, atrioventricular block, ventricular tachycardia or extrasystole, ventricular fibrillation.

From the gastrointestinal tract: anorexia, nausea, vomiting, diarrhea.

From the side of the central nervous system and sensory organs: headache, fatigue, very rarely - confusion, syncope.

Treatment: discontinuation of the drug or reduction of subsequent doses and an increase in the time intervals between injections of the drug, the introduction of antidotes (unithiol, EDTA), symptomatic therapy (antiarrhythmic drugs- lidocaine, phenytoin, amiodarone; potassium preparations; anticholinergics - atropine sulfate).

Release form

1 ml of the drug in a glass ampoule.

10 ampoules, together with instructions for medical use in the state and Russian languages ​​and an ampoule scarifier, are put into a box with a corrugated insert. The box is pasted over with a label-package. Or 10 ampoules are put into a blister pack.

1 contour pack, together with instructions for medical use in the state and Russian languages, and an ampoule scarifier are put into a pack.

When using ampoules with a breaking point or ring, scarifiers are not inserted.

Storage conditions

Store in a place protected from light at a temperature not exceeding 25 ° C.

Keep away from children!

Shelf life

Do not use after the expiration date.

Terms of dispensing from pharmacies

On prescription.

Manufacturer

JSC "Galicpharm"

Ukraine, 79024, Lviv, st. Opryshkovskaya, 6/8.

Registration certificate holder

JSC Galichpharm, Ukraine.

Address of the organization accepting claims from consumers on the quality of products (goods) on the territory of the Republic of Kazakhstan

Strofantin-G: instructions for use

Compound

active ingredient: ouabain;

1 ml of solution contains ouabain (strophanthin G) 0.25 mg;

excipients: citric acid, monohydrate: sodium hydroxide: water for injection.

Description

clear, colorless liquid.

pharmachologic effect

Strophant in-G (ouabain) - cardiac glycoside. which is obtained from the seeds of strophanthus gratu sa. Strofantin-1 exhibits high cardiotonus and clear activity (1 g of the drug contains 43000 - 54000 LHD. 5800 - 7100 COD), has a pronounced positive inotropic effect. exhibits negative chronotropic. dromotropic effect s, as a result of which it has a significant systolic effect (in the experiment it is slightly inferior to the effect of strophanthin K), slightly slows down the heart rate. The basis of the mechanism of the cardiotonic action of the glycoside is the effect on the potassium-sodium pump of cardiomyocytes. the exchange of calcium ions, the release of catecholamines from labile depots, the level of cyclic adenosine monophosphate. energy supply of myocardial contraction. In patients with acute heart failure Strofantin-G reduces venous pressure, increases diuresis, reduces swelling, shortness of breath.

Pharmacokinetics

After intravenous administration, the effect is observed after 2-10 minutes. reaches a maximum after 30 - 60 - 120 minutes and begins to decline after 2 - 3 hours. The duration of action of Strofantin-G is from 1 to 3 days. The drug is more powerful than strophanthin-K binds to plasma proteins (40%). not biotransformed, excreted mainly by the kidneys unchanged. The drug accumulates in insignificant degree. The elimination half-life from blood plasma averages 23 hours: with impaired renal function and in elderly patients, it increases.

Indications for use

Cardiovascular insufficiency II - 111 degrees (111 - IV degree according to the NYHA classification). especially with the ineffectiveness of digitoxin preparations. supraventricular tachycardia, atrial fibrillation and flutter.

Contraindications

Organic lesions of the heart and blood vessels, acute myocarditis, endocarditis, severe cardiosclerosis, acute infarction myocardium, atrioventricular blockade of 11 - 111 degrees, severe bradycardia. hypertrophic obstructive cardiomyopathy and constrictive pericardial t, hypercalcemia. hypokalemia. carotid sinus syndrome, thoracic aortic aneurysm, glycoside intoxication. WPW syndrome pulmonary hypertension. During pregnancy and breastfeeding. Childhood up to 15 years old.

Pregnancy and lactation

The drug is contraindicated in women during pregnancy and lactation.

Dosage and administration

Applied to adults and children over the age of 15 in the form of a slow intravenous injection. I dissolve a single dose of the drug! in 10 - 20 ml of 0.9% sodium chloride solution and injected over 5 - 6 minutes.

The dose is set individually. Maximum single dose is 0.25 mg. daily 1 mg. The drug is administered in low doses of 0.1 - 0.15 mg with an interval of 30 minutes to 2 hours. With an average rate of digitalization during the period of saturation, adults are usually administered 0.25 mg 2 times a day with an interval of 12 hours. The duration of the saturation period on average

1 day. The maintenance dose of Strofantin-1 "should not exceed 0.25 mg per day. The duration of the saturation period and the adequacy of the dose are assessed by clinical effects drug and the appearance of signs of icosidic intoxication.

Side effect

Strofantin-G has a narrow spectrum therapeutic action, causes a violation heart rate, due to the effect on automatism and conduction (supraventricular tachycardia, extrasystole, atrioventricular block, etc.). possible nausea, vomiting, diarrhea, weakness, insomnia, myocardial infarction, headache, depression, hallucinations, psychosis, color vision disorders, gynecomastia, allergic reactions; rarely - mesenteric infarction.

Overdose

Symptoms of an overdose are varied.

From arrhythmias, including bradycardia.

atrioventricular blockade, ventricular tachycardia or extrasystole. ventricular fibrillation.

From the side digestive tract: anorexia, nausea. vomiting, diarrhea.

On the part of the central itepeuoii system and sensory organs, headache, fatigue, rarely a violation of color vision, decreased visual acuity, scotoma, macro- and micropsia. very rarely confusion, syncope.

With the development of glycoside intoxication, the drug must be canceled, prescribe potassium preparations, parenterally introduce \ nitiol (the first 2 days 0.05 g per 10 kg of body weight 3-4 times a day, then 1-2 times until the cardiotoxic effect stops), conduct symptomatic therapy (lidocaine phenytoin).

Interaction with other drugs

Calcium antagonists (especially verapamil). quinidine. erythromycin, tetracycline, amiodarone slow down excretion and increase plasma concentration (if necessary joint application the dose of Strofantin-G is reduced by 2 times). Sympathomimetics. calcium salts, methylxanthine (theophylline, etc.). antiarrhythmic drugs increase the risk of rhythm disturbances. When using magnesium sl.tfata, the possibility of reducing conduction and atrioventricular blockade of the heart increases. Diuretics, glucocorticoids. inosine increase the risk of developing glycosepsis intoxication.

Application features

I use it with extreme caution! drug for patients with thyrotoxicosis and atrial extrasystole. the elderly and those with impaired renal function.

During intravenous administration of Strofantin-G and within 1 hour after administration, it is necessary to carry out OCG control. If frequent, group or polytopic ventricular extrasystole occurs, the administration must be stopped, and the next dose must be reduced by 2 times. In case of impaired renal function and patients of the elderly and old age the drug is recommended to be administered in lower doses, starting from 0.125 - 0.15 - 0.2 mg. and in the future, do not exceed the dose of 0.25 mg per day (with the exception of urgent conditions). With rapid intravenous administration, the development of bradyarrhythmia is possible. ventricular tachycardia, atrioventricular blockade, cardiac arrest. To prevent this effect, the daily dose is divided into 2-3 injections, or one of the doses is administered intramuscularly. Gels to the patient were previously used other cardiac glycosides. it is necessary before intravenous administration of Strofantina-G is sustained, a break of 5 - 24 days. depending on the severity of cumulative properties. Treatment is carried out" with constant monitoring of the ECG.

Particular care and ECG monitoring are necessary for atrioventricular blockade of the 1st degree, severe dilatation of the heart cavities, cor pulmonale, alkalosis and elderly patients.

Precautionary measures

The ability to influence the reaction rate when driving vehicles or working with other mechanisms.

During treatment, you should "refrain from driving vehicles and engaging in other potentially dangerous species activities that require increased concentration of attention and speed of psychomotor reactions.

Release form

1 ml in ampoules, 10 ampoules in packs.

Storage conditions

To store in the place protected from light at a temperature from 15 °C to 25 °C.

Best before date

Self-medication can be harmful to your health.
It is necessary to consult a doctor, and also read the instructions before use.

• Name of the drug: Strofantin-K
• Title on Latin: Strophanthinum K (Genitive Strophanthini K)
• chemical name medicinal product: (3-β,5-β)-[(2-,6-Dideoxy-3-O-methyl-β-D-ribohexopyranosyl)oxy]-5-,14-dihydroxy-19-oxocard-20- (22-)-enolide
• Gross formula of the drug: C30 H44 O9
• Pharmacological group: cardiac glycosides
• Pharmacological effect - cardiotonic
• Physicochemical characteristics: white or slightly yellowish powder, small crystals. It is poorly soluble in ethanol and water, practically insoluble in chloroform and ether.
• Object of application: human, cattle, dogs, horses
• Where to buy: medical pharmacies
• >Release form strophanthin: solution for injection in 1 ml ampoules 0.025%

Pharmacology strophanthin

Pharmacological action of strophanthin- cardiotonic.

The drug has:

• positive inotropic effect
• positive bathmotropic action
• negative chronotropic action
• negative dromotropic effect

Strofantin inhibits the transport sodium-potassium-ATPase of cardiomyocytes. 5–10 minutes after intravenous injection, the first pharmacological effect. Maximum effect reached in 15-30 minutes. The drug has practically no effect on the conduction of the impulse along the bundle of His and the heart rate. In plasma, only a small part (about 5%) of the drug is conjugated to proteins. Strofantin-K is completely excreted by the kidneys during the day. Does not have a cumulative effect.

Indications for the use of strophanthin in humans, dogs and other animals

According to instructions for the use of strophanthin for humans, dogs the following therapeutic indications:

• chronic heart failure in the acute stage
• acute heart failure
• chronic heart failure (stage II-III, especially if the use of digitalis preparations was not effective)
• flutter and atrial fibrillation
• supraventricular tachycardia

Method of application of strophanthin in medicine and its dose to a person

use strophanthin intravenously by stream, intravenous drip and intramuscularly at a starting dose of 250 mcg (1 ml of a 0.025% solution) followed by repeated injections every hour, 100 mcg to a total daily dose 1000 mcg. With an intravenous infusion method of administration, the drug is preliminarily diluted in a dextrose solution or an isotonic sodium chloride solution. Intramuscular injections strophanthin is very painful, the drug is injected into the so-called "novocaine lake", while using a 2% solution of novocaine.

The method of application of strophanthin in veterinary medicine and its dose to dogs, horses and cattle

In veterinary medicine Strofantin is used intravenously in a stream, intravenously drip and intramuscularly in doses big cattle and horses - 0.005-0.015g; for dogs - 0.00005-0.0005 g. For dogs dwarf breeds strophanthin is prescribed at a dose of 50 mcg, small breeds- 100 mcg, medium breeds - 150 mg, large breeds- 250 mcg, giant breeds - 250-500 mcg. Enter with 10-20% sterile glucose solution. Intramuscular injections of strophanthin are very painful, the drug is injected into the so-called "novocaine pillow", while using a 2% solution of novocaine.

Contraindications to the use of strophanthin

According to the instructions for the use of strophanthin for humans, horses, cattle and dogs, the following contraindications:

• Allergy and hypersensitivity
• acute myocarditis
• endocarditis
• organic pathology heart and blood vessels
• myocardial infarction in acute stage
• atrial extrasystole (possible transformation into atrial fibrillation)
• progressive cardiosclerosis
• atrioventricular block II–III degree
• constrictive pericarditis
• obstructive form hypertrophic cardiomyopathy(GKMP)
• intoxication and saturation with cardiac glycosides
• carotid sinus syndrome
• thyrotoxicosis

Side effects

At the use of strophanthin established the following side effects:

• nausea
• arrhythmia
• diarrhea
• vomit
• mesenteric thromboembolism
• migraine
• asthenia
• insomnia
• hallucinations
• gynecomastia
• depression
• psychoses and neuroses
• visual impairment

Interaction of strophanthin with other drugs

Against the background of the combined use of strophanthin and magnesium sulfate (and other magnesium-containing medications) increases the risk of developing conduction disorders and atrioventricular heart block.

The use of strophanthin with calcium salts, antiarrhythmic drugs and sympathomimetics increase the likelihood of developing cardiac arrhythmias.

Amiodarone, as well as blockers calcium channels(in particular verapamil) slow down the excretion of strophanthin and increase its content in the blood plasma. If there is a need for their combined use, Strofantin-K is used at ½ of the standard dose.

Overdose

Symptoms:

• rhythm dissociation
• bigeminy
• extrasystole

• discontinuation of the drug, dose reduction and reduction in the frequency of administration
• with hypokalemia, treatment is carried out with potassium preparations
• for arrhythmias, novocainamide, lidocaine, phenytoin, propranolol, as well as chelating drugs (EDTA) are used

Precautions when using the drug strophanthin

At the peak therapeutic effect from the use of strophanthin on the electrocardiogram, single, frequent extrasystoles may appear, sometimes - bigeminia.

With rapid intravenous injection, bradycardia, bradyarrhythmia, atrioventricular block, ventricular tachycardia and asystole may develop.

Before intramuscular application first, a 2% solution of novocaine is injected at a dose of 5 ml, then, without removing the needle, a solution of strophanthin-K is injected. It should be noted that the effectiveness of the intramuscular route of administration of the drug is two times lower.

If other drugs from the group of cardiac glycosides have been used in anamnesis, it is required to take a break in their use for 5–25 days, depending on their pronounced cumulative properties). After that, you can apply strofantin-K intravenously.

Strofanthin therapy is carried out under the control of electrocardiographic parameters.

Release form strophanthin-K

A drug Strofantin has following form release- 1 ml ampoules containing 0.025% (250 mcg) solution for intravenous and intramuscular injections.

Gross formula

C 30 H 44 O 9

Pharmacological group of the substance Strofantin-K

Nosological classification (ICD-10)

CAS code

508-77-0

Characteristics of the substance Strofantin-K

White or white with a slightly yellowish tint crystalline powder. It is sparingly soluble in water and ethanol, practically insoluble in ether and chloroform.

Pharmacology

pharmachologic effect- cardiotonic.

It exhibits positive ino- and batmotropic, negative chrono- and dromotropic effects, inhibits Na + -K + -ATPase of myocardiocytes. After intravenous administration, the effect appears after 5-10 minutes, reaches a maximum after 15-30 minutes. It has little effect on heart rate and conduction in the bundle of His. In the blood, only a small part (5%) binds to proteins. Completely excreted in the urine within 24 hours. Does not accumulate.

Application of the substance Strofantin-K

Acute cardiovascular failure, chronic insufficiency blood circulation stage II-III, especially with the ineffectiveness of digitalis preparations, supraventricular tachycardia, atrial fibrillation and flutter.

Contraindications

hypersensitivity, organic lesions heart and blood vessels, acute myocarditis, endocarditis, severe cardiosclerosis, acute myocardial infarction, AV blockade II-III degree, hypertrophic obstructive cardiomyopathy and constrictive pericarditis, carotid sinus syndrome, intoxication with cardiac glycosides, thyrotoxicosis, atrial extrasystole (transition to atrial fibrillation is possible).

Side effects of the substance Strofantin-K

Arrhythmia, nausea, vomiting, diarrhea, mesenteric infarction, headache, weakness, insomnia, depression, hallucinations, psychosis, visual disturbances, gynecomastia.

Interaction

Calcium antagonists (especially verapamil) and amiodarone slow down excretion and increase plasma concentrations (if necessary, co-administration dose of strophanthin-K should be halved). Sympathomimetics, calcium salts and antiarrhythmic drugs increase the risk of rhythm disturbances. Against the background of magnesium sulfate, the likelihood of decreased conduction and AV heart block increases.

Overdose

Symptoms: extrasystole, bigeminia, rhythm dissociation.

Treatment: reduction of regular doses and an increase in the time intervals between doses; with hypokalemia - potassium preparations; in case of development of rhythm disturbances - lidocaine, procainamide, propranolol, phenytoin, chelating agents (EDTA).

Routes of administration

In / in, in / m / in drip.

Precautions for substance Strofantin-K

With rapid intravenous administration, the development of bradyarrhythmia, ventricular tachycardia, AV blockade and cardiac arrest is possible. At the peak of the effect, extrasystoles may appear, sometimes in the form of bigeminy. To prevent this effect, the dose can be divided into 2-3 intravenous injections, or one of the doses is administered intramuscularly. Before the intramuscular injection, 5 ml of a 2% solution of novocaine is administered, then, without removing the needle, strofantin-K; the effectiveness of the / m application is 2 times lower. If the patient was previously prescribed other cardiac glycosides, it is necessary to take a break before the intravenous administration of strophanthin-K (5-24 days, depending on their pronounced cumulative properties). Treatment is carried out under constant ECG control.

Strofantin K - a short-acting cardiac glycoside that 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. An excess of sodium ions leads to an acceleration of the release of calcium ions from the sarcoplasmic reticulum, thus. the intracellular concentration of calcium ions increases, which leads to blockade of the troponin complex, which has a depressing effect on the interaction of actin and myosin.

Increases the strength and speed of myocardial contraction, which occurs according to a mechanism different from the Frank-Starling mechanism, and does not depend on the degree of preliminary myocardial stretching; systole becomes shorter and energy efficient. As a result of an increase in myocardial contractility, the stroke and minute volume of blood increases.

It reduces the end-systolic volume and end-diastolic volume of the heart, which, along with an increase in myocardial tone, leads to a reduction in its size, and thus. to reduce myocardial oxygen demand.

A negative dromotropic effect is manifested in an increase in the refractoriness of the atrioventricular node, which allows the drug to be used for paroxysms of supraventricular tachycardia and tachyarrhythmias. With atrial tachyarrhythmia, it slows down the heart rate, lengthens the diastole, improving intracardiac and systemic hemodynamics. Decrease in heart rate occurs as a result of direct and indirect effects on the regulation of heart rate. It has a direct vasoconstrictor 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 an indirect vasodilating effect, reduces venous pressure, increases diuresis: reduces swelling, shortness of breath. A positive bathmotropic effect is manifested in subtoxic and toxic doses. To a small extent, it has a negative chronotropic effect. When administered intravenously (in / in), the action begins after 10 minutes and reaches a maximum after 15-30 minutes.

Pharmacokinetics

The cumulative effect is practically absent.

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

breeding. Does not undergo biotransformation, excreted by the kidneys unchanged. For 24 hours, 85-90% of the drug is excreted; plasma concentration decreases by 50% after 8 hours; completely excreted from the body after 1-3 days.

Indications

- in the composition complex therapy acute and chronic heart failure of the II functional class (in the presence of clinical manifestations), III-IV functional class according to NYHA classification;

- tachysystolic form of atrial fibrillation and flutter of paroxysmal and chronic course(especially in combination with chronic heart failure).

Dosing regimen

Strofantin K used intravenously, intramuscularly, only in emergency situations when it is impossible to use cardiac glycosides inside. For intravenous administration, a 0.025% solution of the drug is used. It is diluted in 10-20 ml of 5% dextrose (glucose) solution or 0.9% sodium chloride solution. The introduction is carried out slowly, for 5 to 6 minutes (because a quick introduction can cause shock). A solution of Strofantin K can also be administered drip (in 100 ml of a 5% dextrose (glucose) solution or 0.9% sodium chloride solution), since this form of administration rarely develops a toxic effect.

The highest doses of Strofantin K for adults intravenously: single - 2 ml (2 ampoules), daily - 4 ml (4 ampoules).

If intravenous administration is not possible, the drug is used intramuscularly. To reduce acute pain in intramuscular injection 5 ml of a 2% solution of procaine is first injected, and then through the same needle - the desired dose of Strofantin K, diluted in 1 ml of a 2% solution of procaine. With intramuscular injection, the dose is increased by 1.5 times.

Children: daily doses, they are also saturation doses when using a 0.025% solution of Strophanthin K; newborns- 0.06-0.07 ml/kg; up to 3 years- 0.04-0.05 ml/kg; 4 to 6 years old- 0.4-0.5 ml/kg; 7 to 14 years old- 0.5-1 ml. The maintenance dose is 1/2-1/3 of the saturation dose.

Side effect

From the gastrointestinal tract: loss of appetite, nausea, vomiting, diarrhea.

bradycardia, extrasystole, atrioventricular block, ventricular paroxysmal tachycardia, ventricular fibrillation.

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

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

Contraindications

- glycosidic intoxication;

- Wolff-Parkinson-White syndrome;

- atrioventricular block II degree;

- intermittent atrioventricular or sinoatrial complete blockade;

— hypersensitivity to the drug.

Carefully:(comparing benefit/risk): first-degree atrioventricular block, sick sinus syndrome without artificial pacemaker, chance of unstable conduction through the atrioventricular node, history of Morgagni-Adams-Stokes attacks, hypertrophic obstructive cardiomyopathy, isolated mitral stenosis with rare heart rate contractions, cardiac asthma in patients with mitral stenosis(in the absence of tachysystolic form atrial fibrillation), acute myocardial infarction, unstable angina, arteriovenous shunt, hypoxia, constrictive pericarditis, heart failure with impaired diastolic function ( restrictive cardiomyopathy cardiac amyloidosis, constrictive pericarditis, cardiac tamponade), ventricular extrasystole, pronounced dilatation of the cavities of the heart, "pulmonary" heart. Atrial extrasystole due to the possibility of its transition to atrial fibrillation.

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

Use during pregnancy and lactation

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

Application for violations of liver function

Use with caution in hepatic impairment.

Application for violations of kidney function

Use with caution in renal failure.

Use in elderly patients

Use with caution in the elderly.

Use in children under 12 years of age

No age restrictions reception.

special instructions

Use with extreme caution in patients with thyrotoxicosis and atrial extrasystole.

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

In case of violation excretory function kidneys, the dose should be reduced (prevention of glycoside intoxication).

The likelihood of overdose increases with hypokalemia, hypomagnesemia, hypercalcemia, hypernatremia, severe dilatation of the heart cavities, cor pulmonale, alkalosis, in elderly patients. Special care and electrocardiographic monitoring are required in violation of atrioventricular conduction.

With severe mitral stenosis and normo- or bradycardia, chronic heart failure develops due to a decrease in diastolic filling of the left ventricle. Strofantin K , increasing the contractility of the myocardium of the right ventricle, causes a further increase in pressure in the system pulmonary artery, which can cause pulmonary edema or aggravate left ventricular failure. Patients with mitral stenosis are prescribed cardiac glycosides when right ventricular failure is attached or in the presence of atrial tachyarrhythmia. Strofantin K in Wolff-Parkinson-White syndrome, by reducing atrioventricular conduction, it contributes to the conduction of impulses through additional pathways - bypassing the atrioventricular node, provoking the development of paroxysmal tachycardia. As one of the methods for controlling digitalization, monitoring of the plasma concentration of cardiac glycosides is used.

With rapid intravenous administration, the development of bradyarrhythmia, ventricular tachycardia, atrioventricular blockade and cardiac arrest is possible. At the maximum of action, extrasystole may appear, sometimes in the form of bigeminia. 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 prescribed other cardiac glycosides, it is necessary to take a break before intravenous administration of Strofantin K (5-24 days, depending on the severity of the cumulative properties of the previous drug).

Influence on the ability to drive vehicles and control mechanisms

During the period of treatment, it is necessary to refrain from driving vehicles and engaging in potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions (driving a car, etc.).

Overdose

Symptoms:

From the side of the cardiovascular system: arrhythmias, including bradycardia, atrioventricular block, ventricular paroxysmal tachycardia, ventricular fibrillation, ventricular extrasystole (bigeminia, polytopic), nodal tachycardia, sinoatrial block, atrial fibrillation and flutter.

From the gastrointestinal tract: anorexia, nausea, vomiting, diarrhea.

From the side of the central nervous system and sensory organs: headache, fatigue, dizziness, rarely - staining of surrounding objects in green and yellow colors, sensation of flies flickering before the eyes, decreased visual acuity, scotoma, macro- and micropsia; very rarely - confusion, syncope.

Treatment: withdrawal of the drug or reduction of subsequent doses and an increase in the time intervals between injections of the drug, the introduction of antidotes (sodium dimercaptopropanesulfonate), symptomatic therapy (antiarrhythmic drugs - lidocaine, phenytoin, amiodarone; potassium preparations; m-anticholinergics - atropine sulfate). As antiarrhythmic drugs - class I drugs (lidocaine, phenytoin). With hypokalemia - in / in the introduction of potassium chloride (6-8 g / at the rate of 1-1.5 g per 0.5 l of 5% dextrose (glucose) solution and 6-8 IU of insulin; injected drip for 3 hours). With severe bradycardia, atrioventricular blockade - m-anticholinergics. It is dangerous to administer beta-agonists, due to the possible increase in the arrhythmogenic effect of cardiac glycosides. With a complete transverse blockade with attacks of Morgagni-Adams-Stokes - temporary pacing.

drug interaction

When using Strophanthin K together with barbiturates (phenobarbital, etc.), the cardiotonic effect of the 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 blood plasma increases with simultaneous application quinidine, methyldopa, amiodarone, captopril, calcium antagonists,
erythromycin and tetracycline. Against the background of magnesium sulfate, the possibility of slowing down the conduction and the occurrence of atrioventricular heart block increases. Diuretics (mostly thiazide and carbonic anhydrase inhibitors), corticotropin preparation (adrenocorticotropic hormone), glucocorticosteroids, insulin, calcium preparations, laxatives, carbenoxolone, amphotericin B, benzylpenicillin, salicylates increase the risk of glycoside intoxication. Beta-blockers, antiarrhythmic drugs, verapamil can not only increase the severity of the decrease in atrioventricular conduction (negative dromotropic effect), but also potentiate the negative chronotropic effect of the drug Strofantin K (decreased heart rate). Inducers of microsomal liver enzymes (phenytoin, rifampicin, phenobarbital, phenylbutazone), as well as neomycin and cytostatic agents reduce the concentration of Strophanthin K in blood plasma. Glycosidic intoxication can be caused, due to the development of hypokalemia, by a carbonic anhydrase inhibitor, mineralocorticoids, therefore, when they are used simultaneously with cardiac glycosides, it is necessary to regularly determine the content of potassium in the blood plasma. Preparations of potassium salts should not be used if, under the influence of cardiac glycosides, conduction disturbances appeared on the electrocardiogram, however, potassium salts are often prescribed together with digitalis preparations to prevent heart rhythm disturbances.

Anticholinesterase drugs increase bradycardia when used simultaneously with cardiac glycosides; edetic acid reduces the effectiveness and toxicity of cardiac glycosides; should not be used in conjunction with cardiac glycosides triposadenine; hypervitaminosis caused by vitamin D enhances the action of cardiac glycosides due to the development of hypercalcemia; there is evidence of a decrease in the excretion of cardiac glycosides by the kidneys under the influence of paracetamol. Glucocorticosteroids and diuretics increase the risk of developing hypokalemia and hypomagnesemia, angiotensin-converting enzyme inhibitors and angiotensin II receptor blockers - reduce.

Terms of dispensing from pharmacies

On prescription.

Terms and conditions of storage

Store at a temperature not exceeding 25°C. Keep out of the reach of children. Shelf life - 3 years.