Digoxin pills 0,25mg №56

Tablets of 0,25 mg

One pill contains

active substance - digoxin 0.25 mg,

Excipients: sucrose, potato starch, glucose monohydrate, talc, Calcium stearate, vaseline oil.

Cardiac glycosides. Digital glycosides.

Pharmacology

Absorption from the gastrointestinal tract (GIT) after oral administration is variable, 60-85% (mainly from the small intestine). Food slows down the rate of absorption of the drug, but not its degree. The action occurs within 2 hours and reaches a maximum after 6 hours. The therapeutic concentration in the blood plasma is individual and is 0.5 2 ng / ml. Digoxin binds to plasma proteins in the range of 20–30%, the free fraction penetrates into tissues, primarily into the heart muscle. The concentration of digoxin in the heart muscle is greater than in the blood plasma. Since most of the drug is in the tissues, digoxin does not dialyse poorly during hemodialysis (3% for 5 hours). Relative volume of distribution - 5 l / kg.

Metabolized in the liver. The elimination half-life is 1.5-2 days. Digoxin is secreted through the kidneys (by glomerular filtration and tubular secretion), mostly unchanged. Allocation depends on the speed of glomerular filtration. Digoxin is excreted in breast milk.

Digoxin is a cardiac glycoside derived from digitalis woolly (Digitalis lanata). It has a positive inotropic effect, which is associated with an inhibitory effect on the Na + / K + -ATP-azu of the cardiomyocyte membrane, which leads to an increase in the intracellular content of sodium ions and, accordingly, a decrease in potassium ions. As a result, an increase in the intracellular calcium content, responsible for the contractility of cardiomyocytes, occurs, which leads to an increase in the force of contraction of the myocardium.

The drug also has a negative chronotropic effect.

The negative dromotropic effect of digoxin is manifested in the increased refractoriness of the atrioventricular (AV) node, which makes it possible to use it in paroxysms of supraventricular tachycardias and tachyarrhythmias.

In atrial tachyarrhythmias, it slows down the frequency of ventricular contractions, lengthens diastole, improves intracardiac and systemic hemodynamics.

It has a direct vasoconstrictor effect, which is most clearly manifested in the absence of congestive peripheral edema.

Indications and usage

-heart failure

- supraventricular arrhythmias (for example, atrial fibrillation)

Dosage and administration

For oral administration. Dose set with caution, individually for each patient.

In the course of treatment, two periods are distinguished: the period of initial digitalization (saturation) and the period of maintenance therapy.

During the initial digitalization period, the body is gradually saturated with cardiac glycoside until the optimal therapeutic effect is achieved. Individual saturating dose (IND) leads to adequate digitalization of a particular patient and ranges from 50% to 200% of the average total dose (SPD), which causes the full therapeutic effect in the majority of patients.

With moderately rapid digitalization, oral administration of 0.25 mg 4 times a day or 0.5 mg 2 times a day is prescribed. Digitalization is achieved on average in 2-3 days, after which the patient is transferred to a maintenance dose, which is usually 0.25-0.5 mg per day.

If the patient does not need such rapid digitalization, you can take 0.25 mg 1-2 times a day. Permanent plasma concentrations are usually reached within 7 days. The usual maintenance dose is 0.125-0.25 mg per day.

Elderly patients

Elderly patients should use small doses of the drug, starting treatment with slow digitalization. In elderly patients, the content of digoxin in the serum should be monitored and hypokalemia should be avoided.

With renal failure dose should be reduced in accordance with the rate of glomerular filtration (GFR).

Glomerular rate

Filtration (GFR) Dose

20-50 ml / min 0,25 mg per day

10 20 ml / min 0.125-0.25 mg per day

<10 ml / min to 0.125 mg per day

If you miss the next dose of the drug, you must take it as soon as an opportunity. The drug should be used strictly as directed by the doctor. The dose can not be changed independently.

Adverse reactions

Often

drowsiness, dizziness

- visual impairment (blurred vision, staining of visible objects in yellow)

-arrhythmias and conduction disorders: atrial tachycardia, atrial fibrillation and flutter, nodular tachycardia, ventricular extrahystists of the type of bigeminy or trigeminy, ventricular paroxysmal tachycardia, ventricular fibrillation; sinus bradycardia, prolongation of the PR interval on the ECG (in the absence of other symptoms, does not indicate side effects of digoxin), sinoatrial block, atrioventricular block

- nausea, vomiting, diarrhea, abdominal pain

Seldom

-depression

-allergic reactions (pruritus, urticaria)

Very rarely

- thrombocytopenia, thrombocytopenic purpura, nasal bleeding

sprays, urticaria

-lack of appetite

-apathy, psychosis, confusion, anxiety, euphoria

-headache

superaventricular tachyarrhythmia, ventricular arrhythmia, ST segment depression on an ECG

- thrombosis of mesenteric vessels, intestinal ischemia, intestinal necrosis

- Gincomastia (in case of long treatment with digoxin)

weakness, fatigue, tiredness

Hypopotassemia

Contraindications

Absolute:

- glycoside intoxication

- hypersensitivity to digoxin or other cardiac glycosides

- heart rhythm disorders caused by digital intoxication

ventricular fibrillation

-hypertrophic obstructive cardiomyopathy (except for the case of severe heart failure)

-Wolf-Parkinson-White syndrome (especially with concomitant atrial fibrillation)

-periodic complete atrioventricular block or atrioventricular block II degree

-shock

- ventricular tachycardia

-lactation

- children's and teenage age up to 18 years

Relative:

pronounced bradycardia

- atrioventricular block I degree

- the isolated mitral stenosis

hypertrophic subaortic stenosis

Acute myocardial infarction

unstable angina

heart tamponade

- extrasystole

Drug Interactions

With simultaneous appointment of Digoxin Grindeks with drugs that cause electrolyte imbalance, in particular hypokalemia (thiazide and "loop" diuretics, glucocorticosteroids, insulin, beta-adrenomimetiki, amphotericin B), the risk of arrhythmias and the development of other toxic effects of digoxin increases. In this case, the dose of Digoxin Grindeks should be reduced.

Calcium salts can cause the toxic effects of digoxin, so intravenous calcium salts should be avoided in patients taking cardiac glycosides.

Spironolactone increases the concentration of digoxin in the blood plasma.

Quinidine, propafenone and Amiodarone, when used together with Digoxin Grindeks, increase the concentration of digoxin in the blood plasma.

Antiarrhythmic drugs increase the frequency of side effects of digoxin.

Beta-blockers may increase the risk of bradycardia and atrioventricular block caused by Digoxin Grindeks.

Blockers of “slow” calcium channels increase the concentration of digoxin in the blood plasma, therefore, when used together, the dose of Digoxin Grindeks should be reduced so that the toxic effects of the drug are not manifested. At simultaneous use of Digoxin Grindeks with Verapamil the possibility of an atrioventricular block increases. Nifedipine may increase the concentration of digoxin in the blood plasma.

Angiotensin II-receptor blockers (for example, telmisartan) increase the content of digoxin in the blood plasma.

Erythromycin, Azithromycin, Clarithromycin, roxithromycin, Tetracycline, Gentamicin, trimethoprim may increase the content of digoxin in the blood plasma.

Neomycin, kanamycin, paromomycin reduce digoxin absorption and reduce its therapeutic effect.

Rifampicin reduces the content of digoxin in the blood plasma.

Magnesium-containing laxatives and aluminum-containing antacids reduce digoxin absorption and reduce its therapeutic effect.

Hypolipidemic agents (cholestyramine, cholestipol) reduce the absorption of digoxin and thereby reduce its therapeutic effect.

Metoclopramide reduces the therapeutic effect of digoxin.

Sulfasalazine reduces the therapeutic effect of digoxin.

Proton pump blockers (for example, omeprazole) increase the concentration of digoxin in the blood plasma.

Non-steroidal anti-inflammatory drugs can increase the content of digoxin in the blood plasma.

Sucralfat reduces the absorption and therapeutic effect of digoxin.

Cyclosporine increases the concentration of digoxin in the blood plasma.

Preparations of Hypericum perforatum reduce the bioavailability of digoxin, increasing the rate of hepatic metabolism and significantly reducing its concentration in the blood plasma.

During treatment with Digoxin Grindeks patient should be under the supervision of a physician in order to avoid side effects resulting from overdose.

Digoxin Grindeks should be used with caution in patients with acute myocardial damage (myocarditis), with increased heart failure or severe lung disease. The use of large single doses should be avoided.

It is also necessary to be careful in case of atrioventricular block of varying severity and in sick sinus syndrome, if the patient has atrial fibrillation.

Under the action of digoxin during exercise on an ECG, there may be changes in the ST segment, which are not signs of poisoning, but only passing natural changes caused by the mechanism of action of the drug.Therefore, when using Digoxin Grindeks, it is necessary to regularly monitor the ECG, to determine the concentration of electrolytes in the serum.

In case of impaired renal function, reduce the dose and monitor the concentration of digoxin in the blood plasma.

Treatment with Digoxin Grindeks is recommended to be stopped 24-48 hours before planned cardioversion, as there is a risk of life-threatening heart rhythm disturbances.

The effect of digoxin may be enhanced by hypokalemia, hypomagnesaemia, hypercalcemia, hypoxia and hypothyroidism. In these cases, the doses of Digoxin Grindeks should be reduced.

In hyperthyroidism, relative resistance to Digoxin Grindeks may occur.

Tablets of the drug Digoxin Grindeks contain sucrose and glucose monohydrate. Patients with glucose-galactose malabsorption, as well as patients with rare congenital fructose intolerance or sucrase-isomaltase deficiency should not be prescribed this drug.

Pregnancy and lactation period

The use of Digoxin Grindeks during pregnancy is possible only when the benefit to the mother exceeds the risk to the fetus.

During lactation, the use of the drug is contraindicated.

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

If Digoxin Grindeks causes drowsiness, dizziness, blurred vision or other side effects, it is necessary to abandon driving a vehicle or working with potentially dangerous machinery.

The breadth of the therapeutic effect of the drug is small. Reception of 10-15 mg of Digoxin Grindeks can cause death due to overdose in 50% of adults.

Symptoms of poisoning develop gradually. There may be: decreased appetite, nausea, vomiting, diarrhea, abdominal pain, drowsiness, confusion, muscle weakness, delirious psychosis, reduced visual acuity, flickering "flies" before your eyes. Heart rhythm and conduction disturbances can cause death due to ventricular fibrillation or asystole caused by blockage.

Treatment: if Digoxin Grindeks is taken in a very large dose, gastric lavage can be done immediately after an overdose. Activated carbon, binding digoxin, prevents its absorption from the digestive tract. Bradyarrhythmia associated with poisoning can be treated by using atropine or by connecting a temporary pacemaker. Ventricular arrhythmias are treated with Lidocaine or phenytoin. In bradyarrhythmias and ventricular arrhythmias, it is possible to use antibodies specific for digoxin - F (ab) fragments (Wellcome).

Dialysis is not effective in life-threatening digoxin poisoning.

On 25 tablets in a blister strip packaging from a film of polyvinyl chloride and aluminum foil.

On 2 blister strip packagings together with the instruction for medical application in the state and Russian languages ​​place in a pack from a cardboard.

Store in a dark place at a temperature not exceeding 25 ° C.

Keep out of the reach of children!