Digoxin pills 250mcg 30pcs

Composition

of 1 tab. digoxin 250 mcgm Auxiliary substances: colloidal silicon dioxide-0.5 mg, magnesium stearate-1 mg, gelatin-1.5 mg, talc-1.5 mg, corn starch-20 mg, lactose monohydrate-75.25 mg

Pharmacological action

Cardiac glycoside. It has a positive inotropic effect. This is due to the direct inhibitory effect on Na+ / K+ – ATPASES on the cardiomyocyte membrane, which leads to an increase in the intracellular content of sodium ions and, accordingly, a decrease in potassium ions. An increased content of sodium ions causes activation of sodium-calcium metabolism, an increase in the content of calcium ions, as a result of which the force of myocardial contraction increases.

As a result of an increase in the contractility of the myocardium, the stroke volume of blood increases. The final systolic and final diastolic volumes of the heart are reduced, which, along with an increase in myocardial tone, leads to a reduction in its size and thus to a decrease in the need for oxygen in the myocardium. It has a negative chronotropic effect, reduces excessive sympathetic activity by increasing the sensitivity of cardiopulmonary baroreceptors.

Due to an increase in the activity of the vagus nerve, it has an antiarrhythmic effect due to a decrease in the speed of conducting impulses through the atriventricular node and an extension of the effective refractory period. This effect is enhanced by direct action on the atrioventricular node and sympatholytic action.

The negative dromotropic effect is manifested in an increase in the refractoriness of the atrioventricular node, which allows it to be used for paroxysms of supraventricular tachycardia and tachyarrhythmias.

With atrial fibrillation, it helps to slow down the frequency of ventricular contractions, lengthens diastole, and improves intracardiac and systemic hemodynamics.

A positive bathotropic effect is shown when subtoxic and toxic doses are prescribed.

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

At the same time, the indirect vasodilating effect (in response to an increase in minute blood volume and a decrease in excessive sympathetic stimulation of vascular tone), as a rule, prevails over the direct vasoconstrictor effect, resulting in a decrease in total peripheral vascular resistance (OPSS).

Indications

• in the complex therapy of chronic heart failure II (in the presence of clinical manifestations) and III-IV functional class;
• tachysystolic form of atrial fibrillation and flutter of paroxysmal and chronic course (especially in combination with chronic heart failure).

Contraindications

• glycoside intoxication;
• Wolf-Parkinson-White syndrome;
• AV block II degree;
• intermittent complete block;
• hypersensitivity to the drug.

With caution (it is necessary to compare the intended benefit and potential risk): grade I AV block, sinus node weakness syndrome without a pacemaker, the likelihood of unstable AV node conduction, indications in the anamnesis of Morgagni-Adams-Stokes attacks; hypertrophic subaortic stenosis, isolated mitral stenosis with rare heart rate, cardiac asthma in patients with mitral stenosis (in the absence of tachysystolic atrial fibrillation), acute myocardial infarction, unstable angina, arteriovenous shunt, hypoxia, heart failure with impaired diastolic function (restrictive cardiomyopathy, amyloidosis of the heart, constrictive pericarditis, cardiac tamponade), extrasystole, severe dilatation of the heart cavities, “pulmonary” heart.

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

Side effects

The reported side effects are often the initial signs of overdose.

Symptoms of digitalis intoxication

From the cardiovascular system:  ventricular paroxysmal tachycardia, ventricular extrasystole (often bigeminia, polytopic ventricular extrasystole), nodal tachycardia, sinus bradycardia, sinoauricular block, atrial fibrillation and flutter, AV block, on the ECG-a decrease in the ST segment with the formation of a two-phase T wave.

From the digestive system:  anorexia, nausea, vomiting, diarrhea, abdominal pain, intestinal necrosis.

From the central nervous system:  sleep disorders, headache, dizziness, neuritis, sciatica, manic-depressive syndrome, paresthesia and syncope, rarely (mainly in elderly patients suffering from atherosclerosis) – disorientation, confusion, single-color visual hallucinations.

From the side of the visual organ:  coloring of visible objects in yellow-green color, flickering of “flies” in front of the eyes, decreased visual acuity, macro-and micropsia.

Allergic reactions:  possible skin rash, rarely-urticaria.

Hematopoietic and hemostatic disorders:  thrombocytopenic purpura, nosebleeds, petechiae.

Other services:  hypokalemia, gynecomastia.

Interaction

When Digoxin is co-administered with drugs that cause electrolyte imbalance, in particular hypokalemia (for example, diuretics, glucocorticosteroids, insulin, beta-adrenomimetics, amphotericin B), the risk of arrhythmias and other toxic effects of Digoxin increases. Hypercalcemia can also lead to the development of toxic effects of Digoxin, so intravenous use of calcium salts to patients taking digoxin should be avoided. In these cases, the Digoxin dose should be reduced. Some medications may increase serum Digoxin concentrations, such as quinidine, slow calcium channel blockers (especially verapamil), amiodarone, spironolactone, and triamterene.

Intestinal digoxin absorption may be reduced by colestyramine, colestipol, aluminum-containing antacids, neomycin, and tetracyclines. There is evidence that the concomitant use of spironolactone not only changes the concentration of Digoxin in the blood serum, but can also distort the results of determining the concentration of Digoxin, so special attention is required when evaluating the results obtained.

Reduced bioavailability of Digoxin is observed when administered concomitantly with activated carbon, astringent drugs, kaolin, sulfasalazine (binding in the gastrointestinal tract lumen), metoclopramide, prozerin (increased gastrointestinal motility).

An increase in the bioavailability of Digoxin is noted when administered simultaneously with broad-spectrum antibiotics that suppress intestinal microflora (reducing destruction in the gastrointestinal tract).

Beta-blockers and verapamil increase the severity of the negative chronotropic effect, reduce the strength of the inotropic effect.

Inducers of microsomal oxidation (barbiturates, phenylbutazone, phenytoin, rifampicin, antiepileptic drugs, oral contraceptives) can stimulate Digoxin metabolism (if they are discontinued, digitalis intoxication is possible).

When used concomitantly with digoxin, the following drugs may interact with each other, as a result of which the therapeutic effect is reduced or the side or toxic effect of Digoxin is manifested: mineralocorticoids, glucocorticoids with a significant mineralocorticoid effect, amphotericin B for injection, carbonic anhydrase inhibitors, adrenocorticotropic hormone (ACTH), diuretics that promote the release of water and potassium (bumetadine, etacric acid, furosemide, indapamide, mannitol and thiazide derivatives), sodium phosphate.

Hypokalemia caused by these drugs increases the risk of toxic effects of Digoxin, so when they are used simultaneously with Digoxin, constant monitoring of the concentration of potassium in the blood is required.

Concomitant use with St. John’s wort induces P-glycoprotein and cytochrome P450 and, consequently, reduces bioavailability, increases metabolism and significantly reduces the concentration of digoxin in plasma.

When administered concomitantly with amiodarone, the concentration of digoxin in the blood plasma increases to a toxic level. The interaction of amiodarone and digoxin inhibits the activity of the sinus and atrioventricular nodes of the heart, and also slows down the conduction of a nerve impulse through the heart’s conducting system. Therefore, when prescribing amiodarone, it is necessary to cancel Digoxin or reduce the dose by half.

Preparations of aluminum, magnesium salts and other antacids can reduce the absorption of digoxin and reduce its concentration in the blood.

Simultaneous use with digoxin of antiarrhythmic agents, calcium salts, pancuronium, rauvolfia alkaloids, succinylcholine and sympathomimetics can provoke the development of cardiac arrhythmias, so in these cases it is necessary to monitor the patient’s heart activity and ECG.

Kaolin, pectin and other adsorbents, colestyramine, colestipol, laxatives, neomycin and sulfasalazine reduce the absorption of Digoxin and thereby reduce its therapeutic effect.

Slow calcium channel blockers, captopril, increase the concentration of Digoxin in blood plasma, so when they are used together, it is necessary to reduce the dose of Digoxin in order to avoid the toxic effect of the latter.

Edrophonium (an anticholinesterase agent) increases the tone of the parasympathetic nervous system, so its interaction with digoxin can cause severe bradycardia.

Erythromycin improves the absorption of Digoxin in the intestine.

Digoxin reduces the anticoagulant effect of heparin, so heparin doses should be increased when administered concomitantly with Digoxin.

Indometacin reduces the release of Digoxin, so the risk of toxic effects of the latter increases.

Magnesium sulfate solution for injection is used to reduce the toxic effects of cardiac glycosides.

Phenylbutazone reduces the concentration of digoxin in the blood serum.

Preparations of potassium salts should not be taken if under the influence of Digoxin there are conduction disturbances on the ECG. However, potassium salts are often prescribed together with digitalis preparations to prevent cardiac arrhythmias.

Quinidine and quinine can dramatically increase Digoxin concentrations.

Spironolactone reduces the rate of Digoxin elimination, so when they are used together, the dose of Digoxin should be adjusted.

In the study of myocardial perfusion with thalia (Thalia chloride) preparations in patients taking Digoxin, the degree of accumulation of talia in the sites of heart muscle damage decreases and the results of the study are distorted.

Thyroid hormones increase the metabolism, so the dose of Digoxin should be increased.

How to take, course of use and dosage

Apply inside.

As with all cardiac glycosides, the dose should be selected with caution, individually for each patient.

If the patient took cardiac glycosides before prescribing digoxin, then the dose of the drug should be reduced.

For adults

The dose of digoxin depends on the need to quickly achieve a therapeutic effect.

Moderately fast digitalization (24-36 hours) is used in emergency cases

The daily dose is 0.75-1.25 mg, divided into 2 doses, under the control of an ECG before each subsequent dose.

After reaching saturation, they switch to maintenance treatment.

Slow digitalization (5-7 days)

The daily dose is 125-500 mcg 1 time/day for 5-7 days (until saturation is achieved), after which they switch to maintenance treatment.

Chronic heart failure (CHF)

In patients with CHF, digoxin should be used in small doses: up to 250 mcg / day (for patients weighing more than 85 kg, up to 375 mcg/day). In elderly patients, the daily dose should be reduced to 62.5-125 mcg (1/4-1/2 tablets).

Maintenance therapy

The daily dose for maintenance therapy is set individually and is 125-750 mcg. Maintenance therapy is usually carried out for a long time.

Overdose

Symptoms: decreased appetite, nausea, vomiting, diarrhea, abdominal pain, intestinal necrosis, ventricular paroxysmal tachycardia, ventricular extrasystole (often polytopic or bigeminia), nodular tachycardia, sinoatrial block, atrial fibrillation and flutter, AV block, drowsiness, confusion, delirious psychosis, decreased visual acuity, yellow-green staining of visible objects, flickering of “flies” in front of the eyes, perception of objects in a reduced or enlarged form, neuritis, sciatica, manic-depressive syndrome, paresthesia.

Treatment: withdrawal of digoxin, use of activated charcoal (to reduce absorption), use of antidotes (unitiol, EDTA, digoxin antibodies), symptomatic therapy. Constant ECG monitoring is performed.

In cases of hypokalemia, potassium salts are widely used: 0.5-1 g of potassium chloride is dissolved in water and taken several times a day to a total dose of 3-6 g (40-80 mEq of potassium) for adults, provided adequate renal function. In emergency cases, intravenous drip use of 2% or 4% potassium chloride solution is indicated. The daily dose is 40-80 mEq of potassium (diluted to a concentration of 40 mEq of potassium per 500 ml). The recommended injection rate should not exceed 20 mEq / h (under ECG control). Magnesium salts are recommended for hypomagnesemia.

In cases of ventricular tachyarrhythmia, slow intravenous use of lidocaine is indicated. In patients with normal heart and kidney function, slow intravenous use (within 2-4 minutes) of lidocaine at an initial dose of 1-2 mg/kg of body weight is usually effective, followed by a transition to drip use at a rate of 1-2 mg / min. In patients with impaired renal and/or cardiac function, the dose should be reduced accordingly.

In the presence of grade II-III AV block, lidocaine and potassium salts should not be prescribed until an artificial pacemaker is installed.

During treatment, it is necessary to monitor the level of calcium and phosphorus in the blood and daily urine.

There is experience with the use of the following drugs with a possible positive effect: beta-blockers, procainamide, bretilium and phenytoin. Cardioversion can cause ventricular fibrillation. Atropine is indicated for the treatment of bradyarrhythmias and AV block. In case of grade II-III AV block, asystole, and suppression of sinus node activity, a pacemaker is indicated.

Special instructions

In order to avoid side effects resulting from overdose, the patient should be monitored during the entire period of treatment with Digoxin. Patients receiving digitalis preparations should not be prescribed calcium supplements for parenteral use.

The dose of Digoxin should be reduced in patients with chronic pulmonary heart disease, coronary insufficiency, impaired water-electrolyte balance, renal or hepatic insufficiency. In elderly patients, careful dose selection is also required, especially if they have one or more of the above conditions. It should be borne in mind that in these patients, even with impaired renal function, creatinine clearance (CC) values may be within the normal range, which is associated with a decrease in muscle mass and a decrease in creatinine synthesis. Since pharmacokinetic processes are disrupted in renal failure, the dose selection should be carried out under the control of the concentration of Digoxin in the blood serum. If this is not feasible, then you can use the following recommendations. The dose should be reduced by approximately the same percentage as the reduced creatinine clearance. If creatinine clearance is not determined, then it can be approximately calculated based on the serum creatinine concentration index (CCC). For men according to the formula (140 – age)/KKS. For women, the result obtained should be multiplied by 0.85.

In severe renal insufficiency, the serum digoxin concentration should be determined every 2 weeks, at least during the initial treatment period.

In idiopathic subaortic stenosis (obstruction of the left ventricular exit tract by an asymmetrically hypertrophied interventricular septum), the use of Digoxin leads to an increase in the severity of obstruction. With severe mitral stenosis and normo-or bradycardia, heart failure develops due to a decrease in the diastolic filling of the left ventricle. Digoxin increases the contractility of the right ventricular myocardium and causes a further increase in pressure in the pulmonary artery system, which can provoke pulmonary edema and worsen left ventricular failure. In patients with mitral stenosis, cardiac glycosides are prescribed with the addition of right ventricular failure, or in the presence of atrial fibrillation.

In patients with grade II AV block, the use of cardiac glycosides may worsen it and lead to the development of a Morgagni-Adams-Stokes attack. The use of cardiac glycosides in patients with grade I AV block requires caution, frequent ECG monitoring, and in some cases, pharmacological prophylaxis with means that improve AV conduction.

Digoxin in Wolf-Parkinson-White syndrome, slowing down AV conduction, promotes the conduction of impulses through additional pathways bypassing the AV node and, thereby, provokes the development of paroxysmal tachycardia. The likelihood of glycoside intoxication increases with hypokalemia, hypomagnesemia, hypercalcemia, hypernatremia, hypothyroidism, severe dilatation of the heart cavities, “pulmonary” heart, myocarditis and in the elderly.

Monitoring of their plasma concentration is used as one of the methods of monitoring the content of digitalization when prescribing cardiac glycosides.

Cross-sensitivity

Allergic reactions to digoxin and other digitalis preparations are rare. If there is an increased sensitivity to any one drug of digitalis, other representatives of this group can be used, since cross-sensitivity to digitalis preparations is not characteristic.

The patient must follow the following instructions exactly:

1. Use the drug only as prescribed by the doctor, do not change the dose yourself;

2. Use the drug every day only at the appointed time;

3. If your heart rate is below 60 beats / min, you should consult your doctor immediately.

4. If the next dose of the drug is missed, it should be taken immediately, when possible;

5. Do not increase or double the dose.

6. If the patient has not taken the drug for more than 2 days, inform the doctor about this.

Before stopping the use of the drug, it is necessary to inform the doctor about this.

If you experience vomiting, nausea, diarrhea, rapid pulse, you should immediately consult a doctor.

Before surgical operations or during emergency care, it is necessary to warn about the use of Digoxin.

Without a doctor’s permission, the use of other medications is undesirable.

Storage conditions

The drug should be stored out of the reach of children at a temperature not exceeding 30°C.

Shelf life

3 years

Active ingredient

Digoxin

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as prescribed by a doctor, for children as prescribed by a doctor

Indications

Heart Failure, Arrhythmia