Digoxin - instructions for use, reviews, analogs and forms of release (tablets of 0.1 mg and 0.25 mg, injections in ampoules for injection in solution) of a drug for the treatment of heart failure in adults, children and pregnancy. Composition
In this article, you can read the instructions for using the drug Digoxin. Comments of visitors of the site - consumers of this medication, as well as opinions of doctors of specialists on the use of Digoxin in their practice are presented. 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 Digoxin in the presence of existing structural analogues.Use for the treatment of heart failure and rhythm disorders in adults, children, as well as in pregnancy and lactation. Composition of the preparation.
Digoxin cardiac glycoside. It has a positive inotropic effect. This is due to the direct inhibitory effect on Na + / K + -ATPase on the membrane of cardiomyocytes, which leads to an increase in the intracellular content of sodium ions and, accordingly, a decrease in potassium ions. The 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 shock volume of the blood increases. The final systolic and terminal diastolic volumes of the heart decrease, which, along with an increase in myocardial tone, leads to a reduction in its size and thus to a decrease in myocardial oxygen demand. Has a negative chronotropic effect, reduces excessive sympathetic activity by increasing the sensitivity of cardiopulmonary baroreceptors. Due to the increase in the activity of the vagus nerve has antiarrhythmic effect,caused by a decrease in the rate of impulses through the atrioventricular node and an elongation of the effective refractory period. This effect is enhanced by direct action on the atrioventricular node and sympatholytic action.
Negative dromotropic effect is manifested in increased refractoriness of the atrioventricular node, which allows to use for paroxysms of supraventricular tachycardias and tachyarrhythmias.
Atrial tachyarrhythmia contributes to slowing the frequency of ventricular contractions, lengthens the diastole, improves intracardiac and systemic hemodynamics.
A positive batmotropic effect is manifested in the administration of toxic and toxic doses.
Has a direct vasoconstrictive 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 the minute volume of blood and the reduction of excessive sympathetic stimulation of the vascular tone) tends to prevail over direct vasoconstrictive action, resulting in a decrease in the total peripheral vascular resistance (OPSS).
Composition
Digoxin + excipients.
Pharmacokinetics
Absorption from the gastrointestinal tract can be different and is 70-80% of the dose. Absorption depends on the motility of the gastrointestinal tract, dosage form, concomitant intake of food, from interaction with other medicines. With a normal acidity of gastric juice, an insignificant amount of digoxin breaks down, while a greater amount of digoxin can degrade under hyperacid conditions. For complete absorption, sufficient exposure in the intestine is required: with a decrease in motility of the gastrointestinal tract, bioavailability is maximal, with minimal peristalsis. The ability to accumulate in tissues (cumulate) explains the lack of correlation at the beginning of the treatment between the severity of the pharmacodynamic effect and its concentration in the blood plasma. Metabolised in the liver. Digoxin is excreted mainly by the kidneys (60-80% unchanged). The intensity of renal excretion is determined by the value of glomerular filtration.
Indications
- in the complex therapy of chronic heart failure 2 (in the presence of clinical manifestations) and 3-4 functional class;
- tachysystolic form of flickerand atrial flutter of paroxysmal and chronic course (especially in combination with chronic heart failure).
Forms of release
Tablets 0.25 mg.
Tablets for children 0.1 mg.
Solution for intravenous administration (injections in ampoules for injection).
Instructions for use and dosage
Method of application - inside.
As with all cardiac glycosides, the dose should be selected with caution, individually for each patient.
If the patient before the appointment of digoxin took cardiac glycosides, in this case, the dose of the drug should be reduced.
Adults and children over 10 years of age
The dose of the drug Digoxin depends on the need to quickly achieve a therapeutic effect.
Moderately rapid digitalization (24-36 hours) is used in emergency cases
The daily dose is 0.75-1.25 mg divided into 2 doses, under ECG monitoring before each subsequent dose.
After reaching saturation, they switch to supportive treatment.
Slow digitalization (5-7 days)
The daily dose of 0.125-0.5 mg is prescribed once a day for 5-7 days (until reaching saturation), after which they switch to maintenance treatment.
Chronic heart failure
In patients with chronic heart failure, the drug Digoxin should be used in small doses: up to 0.25 mg per day (for patients with a body weight of more than 85 kg to 0.375 mg per day). In elderly patients, the daily dose of digoxin should be reduced to 0.0625-0.0125 mg (1/4; 1/2 tablets).
Supportive therapy
The daily dose for maintenance therapy is set individually and amounts to 0.125-0.75 mg. Supportive therapy, as a rule, is carried out for a long time.
Children between the ages of 3 and 10
The saturation dose for children is 0.05-0.08 mg / kg per day; this dose is prescribed within 3-5 days with moderately rapid digitalization or for 6-7 days with slow digitalization. The maintenance dose for children is 0.01-0.025 mg / kg per day.
Side effect
- ventricular paroxysmal tachycardia;
- ventricular extrasystole (often bigemini, polytopic ventricular extrasystole);
- nodal tachycardia;
- sinus bradycardia;
- sinoauric blockade;
- flicker and flutter of the atria;
- AV blockade;
- on the ECG - reduction of the ST segment with the formation of a two-phase T wave;
- anorexia;
- nausea, vomiting;
- diarrhea;
- stomach ache;
- necrosis of the intestine;
- sleep disorders;
- headache;
- dizziness;
- neuritis;
- radiculitis;
- manic-depressive syndrome;
- paresthesia and fainting;
- rarely (mainly in elderly patients suffering from atherosclerosis) - disorientation, confusion, single-color visual hallucinations;
- staining of visible objects in yellow-green color;
- flickering flies before your eyes;
- decreased visual acuity;
- macro and microposs;
- skin rash;
- hives;
- thrombocytopenic purpura;
- nasal bleeding;
- petechiae;
- hypokalemia;
- gynecomastia.
Contraindications
- hypersensitivity to the drug;
- glycoside intoxication;
- Wolff-Parkinson-White syndrome;
- atrioventricular block of degree 2;
- intermittent blockade;
- children up to 3 years;
- patients with rare hereditary diseases: fructose intolerance and glucose / galactose absorption impairment syndrome or insufficiency of sucrose / isomaltase; deficiency of lactase, lactose intolerance, glucose-galactose malabsorption.
Application in pregnancy and lactation
Drugs digitalis penetrate the placental barrier.During delivery, the concentration of digoxin in the blood serum of the newborn and the mother is the same. Digoxin on the safety of its use in pregnancy refers to the category "C": the risk in the application is not excluded. Studies of pregnant women are inadequate, the administration of the drug is possible only if the intended benefit to the mother exceeds the potential risk to the fetus.
Digoxin penetrates into breast milk. However, data on the effect of the drug on the newborn are not provided.
Application in elderly patients
Caution is prescribed to elderly patients. In elderly patients, the daily dose should be reduced to 62.5-125 μg (1 / 4-1 / 2 tablets).
Use in children
Contraindicated in children under 3 years.
special instructions
To avoid side effects resulting from an overdose, the patient should be monitored throughout the treatment period with Digoxin. Patients receiving digitalis preparations should not prescribe calcium preparations for parenteral administration.
It is necessary to reduce the dose of Digoxin to patients with chronic pulmonary heart disease, coronary insufficiency, violations of water-electrolyte balance, renal or hepatic insufficiency.Elderly patients also require careful selection of the dose, especially if they have one or more of the above states. It should be borne in mind that in these patients, even with impaired renal function, the values of creatinine clearance (CC) may be within normal limits, which is associated with a decrease in muscle mass and a decrease in the synthesis of creatinine. Since in renal failure pharmacokinetic processes are violated, the dose selection should be carried out under the control of Digoxin concentration in blood serum. If this is not feasible, then the following recommendations can be used. The dose should be reduced by approximately the same percentage, by how much the QC is reduced. If QC is not determined, then it can be approximately calculated based on the serum creatinine concentration (CCS). For men according to the formula (140-aged) / KKS. For women, the result should be multiplied by 0.85.
In severe renal failure, the serum concentration of Digoxin should be determined every 2 weeks, at least during the initial treatment period.
With idiopathic subaortic stenosis (obstruction of the left ventricular outflow tract by asymmetrically hypertrophicinterventricular septum) the appointment of Digoxin leads to an increase in the severity of obstruction. With severe mitral stenosis and normo- or bradycardia, heart failure develops as a result of a decrease in the diastolic filling of the left ventricle. Digoxin, increasing myocardial contractility of the right ventricle, causes a further increase in pressure in the pulmonary artery system, which can provoke pulmonary edema and aggravate left ventricular failure. Patients with mitral stenosis are assigned cardiac glycosides when right-ventricular failure is attached, or in the presence of atrial fibrillation.
In patients with AV blockade of grade 2, the appointment of cardiac glycosides can aggravate it and lead to the development of the attack of Morgagni-Adams-Stokes. The appointment of cardiac glycosides with AV blockade 1 degree requires caution, frequent ECG monitoring, and in some cases - pharmacological prophylaxis with agents that improve AV conduction.
Digoxin in Wolff-Parkinson-White syndrome, slowing AV conduction, facilitates impulses through additional ways of bypassing the AV node and, thereby, provokes the development of paroxysmal tachycardia.The probability of occurrence of glycosidic intoxication increases with hypokalemia, hypomagnesemia, hypercalcemia, hypernatremia, hypothyroidism, marked 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 controlling the content of digitalization in the appointment of cardiac glycosides.
Cross-sensitivity
Allergic reactions to digoxin and other medicines of digitalis develop rarely. If there is an increased sensitivity to any one medicine of digitalis, other representatives of this group can be used, since the cross-sensitivity to the medicines of digitalis is not peculiar.
The patient is obliged to follow the following instructions:
- Use the drug only as prescribed by the doctor, do not change the dose alone;
- Every day, use the drug only at the appointed time;
- If the heart rate is below 60 beats / min, you should immediately consult a doctor;
- If the next dose of the drug is missed, it should be taken immediately, when possible;
- Do not increase or double the dose;
- If the patient did not take the drug for more than 2 days, it is necessary to inform the doctor about it.
Before discontinuing the use of the drug, it is necessary to inform the doctor about it.
If there is vomiting, nausea, diarrhea, rapid pulse, you should immediately consult a doctor.
Before surgical operations or when providing emergency care, it is necessary to warn about the use of Digoxin.
Without the permission of the doctor, the use of other medicinal products is undesirable.
Drug Interactions
With the simultaneous administration of Digoxin with drugs that cause electrolyte imbalance, in particular hypokalemia (eg, diuretics, glucocorticosteroids, insulin, beta-adrenomimetics, amphotericin B), the risk of arrhythmias and the development of other toxic effects of Digoxin is increased. Hypercalcemia can also lead to the development of toxic effects of digoxin, so I / O administration of calcium salts should be avoided for patients taking digoxin. In these cases, the dose of Digoxin should be reduced. Some drugs can increase the concentration of digoxin in the blood serum, for example, quinidine, slow calcium channel blockers (especially verapamil), amiodarone, spironolactone and triamterene.
Digoxin absorption in the intestine can be reduced by the action of colestyramine, colestipol, aluminum-containing antacids, neomycin, and tetracyclines. There is evidence that the simultaneous use of spironolactone not only changes the concentration of digoxin in the blood serum, but it can also distort the results of the determination of digoxin concentration, therefore special attention is required when evaluating the results.
Decrease in bioavailability Digoxin is noted with simultaneous administration with activated charcoal, astringent drugs, kaolin, Sulfasalazine (binding in the lumen of the gastrointestinal tract), metoclopramide, proserin (increased motility of the gastrointestinal tract).
Increase in bioavailability Digoxin is noted with simultaneous appointment with antibiotics of a wide spectrum of action, suppressing intestinal microflora (reduction of destruction in the digestive tract).
Beta-adrenoblockers and Verapamil increase the severity of the negative chronotropic effect, reduce the strength of the inotropic effect.
Inductors of microsomal oxidation (barbiturates, phenylbutazone, phenytoin, rifampicin, antiepileptic, oral contraceptives) can stimulate digoxin metabolism (when they are canceled, digitalis intoxication is possible).
With simultaneous use with digoxin below these drugs, they may interact, due to which the therapeutic effect or the side effect or toxic effect of digoxin is manifested: mineralocorticoids, glucocorticosteroids with a significant mineralocorticoid effect, amphotericin B for injections, carbonic anhydrase inhibitors, adrenocorticotropic hormone (ACTH), diuretic drugs that promote the release of water and potassium (buometadine, ethacrynic acid, furosemide, indapamide, mannitol and derivatives of thiazide), sodium phosphate.
Hypokalemia caused by these drugs increases the risk of toxic effects of Digoxin, so when used simultaneously with Digoxin requires constant monitoring of the concentration of potassium in the blood.
With the simultaneous administration of St. John's wort, P-glycoprotein and cytochrome P450 are induced and, consequently, the bioavailability decreases, metabolism increases and the digoxin concentration in the plasma decreases markedly.
With simultaneous administration 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 the conduction of the nerve impulse through the conduction system of the heart. Therefore, in the appointment of amiodarone, it is necessary to cancel Digoxin or reduce the dose by half.
Drugs of salts of aluminum, magnesium and other antacid agents can reduce absorption of digoxin and reduce its concentration in the blood.
The simultaneous use of antiarrhythmic agents, calcium salts, pancuronium, rauwolfia alkaloids, succinylcholine and sympathomimetics with digoxin can provoke the development of cardiac rhythm disturbances, therefore in these cases it is necessary to monitor the cardiac activity and the patient's ECG.
Kaolin, pectin and other adsorbents, colestyramine, colestipol, laxative, neomycin and sulfasalazine reduce digoxin absorption and thereby reduce its therapeutic effect.
The blockers of the "slow" calcium channels, Captopril - increase the concentration of Digoxin in the blood plasma, so when they are used together it is necessary to reduce the dose of Digoxin in order to avoid toxic effects of the latter.
Edrophonia (anticholinesterase agent) increases the tone of the parasympathetic nervous system, so its interaction with digoxin can cause a pronounced bradycardia.
Erythromycin improves digoxin absorption in the intestine.
Digoxin reduces the anticoagulant effect of heparin, so doses of Heparin should be increased with a simultaneous appointment with digoxin.
Indomethacin reduces the secretion of digoxin, so the risk of toxic effects of the latter increases.
A solution of magnesium sulfate for injection is used to reduce the toxic effects of cardiac glycosides.
Phenylbutazone reduces the concentration of digoxin in the blood serum.
Drugs of potassium salts can not be taken if, under the influence of Digoxin, there are conduction abnormalities on the ECG. However, potassium salts are often prescribed together with digitalis preparations to prevent cardiac rhythm disturbances.
Quinidine and quinine can dramatically increase the concentration of Digoxin.
Spironolactone reduces the rate of excretion of Digoxin, therefore, when combined, the dose of Digoxin should be adjusted.
In the study of myocardial perfusion with waist (Thalia chloride) preparations in patients taking Digoxin, the degree of waist accumulation decreases at the sites of the heart muscle lesion and the results of the study are distorted.
Thyroid hormones increase metabolism, so the dose of Digoxin should be increased.
Analogues of medicinal product Digoxin
Structural analogs for the active substance:
- Digoxin Grindex;
- Digoxin TFT;
- Novodigal.
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