Digoxin of Grindeks
Producer: AS Grindex (JSC Grindeks) Latvia
Code of automatic telephone exchange: C01AA05
Release form: Firm dosage forms. Tablets.
General characteristics. Structure:
Active ingredient: 250 mkg of digoxin.
Excipients: sucrose, potato starch, glucose monohydrate, talc, calcium stearate, liquid paraffin.
Pharmacological properties:
Pharmacodynamics. Digoxin is the cardiac glycoside received from a foxglove of woolly (Digitalis lanata). Has positive inotropic effect which is connected with an inhibiting effect on Na+/K+-ATF-azu of a membrane of cardiomyocytes that brings to the uvelicheniyuvnutrikletochny maintenance of ions of sodium and, respectively, to decrease in potassium ions. Thereof there is an increase in intracellular content of the calcium responsible for contractility of cardiomyocytes that leads to increase in force of reduction of a myocardium.
Medicine possesses also negative chronotropic effect.
The negative dromotropic effect of digoxin is shown in increase in a refrakternost of an atrioventricular (AV) node that allows to use it at paroxysms of supraventricular tachycardias and tachyarrhythmias.
At a ciliary tachyarrhythmia promotes delay of frequency of ventricular reductions, extends a diastole, improves an endocardiac and system hemodynamics.
Has direct vasopressor effect which is most accurately shown in the absence of congestive peripheral hypostases.
Pharmacokinetics. Absorption from the digestive tract (DT) after oral administration – is variable, makes 60-85% (generally of a small intestine). Food slows down the drug absorption speed, but not its degree. Action comes within 2 hours and reaches a maximum in 6 hours. Therapeutic concentration in a blood plasma is individual and makes 0,5-2 ng/ml. Digoxin contacts proteins of plasma кровив limits of 20-30%, the free fraction gets into fabrics, first of all into a cardiac muscle. Concentration of digoxin in a cardiac muscle is more, than in a blood plasma. As the most part of medicine is in fabrics, at a hemodialysis digoxin is badly dialyzed (3% within 5 hours). The relative volume of distribution – 5 l/kg. It is metabolized in a liver. An eliminative elimination half-life – 1,5-2 days. Digoxin is emitted through kidneys (by glomerular filtering and tubular secretion), generally in not changed look. Allocation depends on the speed of glomerular filtering. Digoxin is emitted with breast milk.
Indications to use:
- supraventricular disturbances of a rhythm (for example, atrial fibrillation).
Route of administration and doses:
For intake. The dose is established with care, individually for each patient.
In the course of treatment allocate two periods: period of an initial digitalization (saturation) and period of a maintenance therapy.
In the period of an initial digitalization there is a gradual saturation of an organism cardiac glycoside before achievement of optimum therapeutic effect. The Individual Sating Dose (ISD) leads to an adequate digitalization of the specific patient and fluctuates from 50% to 200% of the average full dose (AFD) causing full therapeutic effect of an ubolshinstvo of patients.
At moderately bystry digitalization appoint inside 0,25 mg 4 times a day or on 0,5 mg 2 times a day. Digitalization is reached on average in 2-3 days then the patient is transferred to a maintenance dose which usually makes 0,25-0,5 mg of a vsutka.
If the patient does not need such bystry digitalization, it is possible to accept 0,25 mg 1-2 разав days. Constant concentration in a blood plasma is usually reached within 7 days. A usual maintenance dose – 0,125-0,25 mg a day.
Patients of advanced age should apply small doses of drug, beginning treatment with a slow digitalization. At patients of advanced age it is necessary to control the content of digoxin in blood serum and to avoid a hypopotassemia.
At a renal failure the dose of drug should be reduced according to the speed of glomerular filtering (GFR).
If reception next a dozypreparata is missed, it needs to be accepted at once as soon as an opportunity appeared. To apply Preparatsleduyet strictly according to instructions of the doctor. The dose cannot be changed independently.
Features of use:
During treatment by Digoksinom Grindeks the patient has to be under observation of the doctor to avoid the side effects arising owing to overdose.
It is necessary to apply with care Digoksin Grindeks to patients with acute injury of a myocardium (myocarditis), when strengthening heart failure or a serious pulmonary illness. It is necessary to avoid use of high single doses.
It is also necessary to be careful at an atrioventricular block of varying severity and at a sick sinus syndrome if at the patient atrial fibrillation attacks are observed.
Under the influence of digoxin at an exercise stress on an ECG there can be changes of a segment of ST which are not symptoms of poisoning but only the taking place natural changes caused by the mechanism of effect of medicine. Therefore at the Digoksina Grindeks use it is regularly necessary to carry out control of an ECG, to define concentration of electrolytes in blood serum.
At renal failures it is necessary to reduce doses and to watch concentration of digoxin in a blood plasma.
Treatment by Digoksinom Grindeks is recommended to be stopped in 24-48 hours prior to carrying out planned cardioversion as the risk of emergence of life-threatening disturbances of a heart rhythm appears.
Effect of digoxin can amplify prigipokaliyemiya, hypomagnesiemia, hypercalcemias, a hypoxia and a hypothyroidism. In these cases it is necessary to reduce the Digoksina Grindeks doses.
At a hyperthyroidism there can be a relative resistance to Digoksin Grindeks.
Tablets of the drug Digoxin of Grindeks contain sucrose and glucose monohydrate. To patients with glucose galactose malabsorption, and also to patients with rare inborn intolerance of fructose or insufficiency of invertase-isomaltase it is impossible to appoint this medicine.
The Digoksina Grindeks use during pregnancy perhaps only in case the advantage for mother exceeds risk for a fruit.
In the period of a lactation use of drug is contraindicated.
Features of influence of medicine on ability to manage the vehicle or potentially dangerous mechanisms
If Digoksin Grindeks causes drowsiness, dizziness, deterioration in sight or other side effects, it is necessary to refuse driving or work with potentially dangerous mechanisms.
Side effects:
Often:
- drowsiness, dizziness;
- vision disorders (a sight illegibility, coloring of visible objects in yellow color);
- conductivity disturbance arrhythmias: atrial tachycardia, blinking and an atrial flutter, nodal tachycardia, ventrikulyarny extrasystoles like bigeminals pulse or trigeminies, a ventricular Bouveret's disease, fibrillation of ventricles; a sinus bradycardia, lengthening of an interval of PR on an ECG (in the absence of others to the simptomoyena confirms side effect of digoxin), sinuatrial blockade, an atrioventricular block;
- nausea, vomiting, diarrhea, abdominal pain;
Seldom:
- depression;
- allergic reactions (skin itch, small tortoiseshell);
Very seldom:
- thrombocytopenia, Werlhof's disease, nasal bleedings;
- petechias, urtikarny rash;
- lack of appetite;
- apathy, psychosis, confusion of consciousness, concern, euphoria;
- headache;
- a supraventricular tachyarrhythmia, ventricular arrhythmia, ST segment depression on an ECG;
- thrombosis of mezenterialny vessels, intestines ischemia, intestines necrosis;
- a gynecomastia (in case of prolonged treatment by digoxin);
- weakness, fatigue, fatigue;
Interaction with other medicines:
At co-administration of Digoksina Grindeks with the drugs causing disturbances of electrolytic balance, in particular a hypopotassemia (thiazide and "loopback" diuretics, glucocorticosteroids, insulin, beta-adrenergic agonists, Amphotericinum In), the risk of developing of arrhythmias and development of other toxic effects of digoxin increases. In this case the dose of Digoxin of Grindeks needs to be reduced.
Salts of calcium can cause toxic effects of digoxin therefore it is necessary to avoid intravenous administration of salts of calcium by the patient accepting cardiac glycosides.
Spironolactonum increases concentration of digoxin in a blood plasma.
Quinidine, пропафенон and Amiodaronum prisovmestny use with Digoksinom Grindeks increase concentration of digoxin in a blood plasma.
Antiarrhytmic drugs increase the frequency of emergence of side effects of digoxin.
Beta adrenoblockers can increase risk of development of the bradycardia and an atrioventricular block caused by Digoksinom Grindeks.
Blockers of "slow" calcium channels increase concentration of digoxin in a blood plasma therefore at their combined use it is necessary to reduce the Digoksina Grindeks dose that toxic influence of drug was not shown. At simultaneous use of Digoxin of Grindeks with verapamil the possibility of an atrioventricular block increases.
Nifedipine can increase concentration of digoxin in a blood plasma.
Blockers angiotensin of II receptors (for example, телмисартан) increase the content of digoxin in a blood plasma.
Erythromycin, azithromycin, кларитромицин, рокситромицин, tetracycline, gentamycin, Trimethoprimum can increase the content of digoxin in a blood plasma.
Neomycinum, Kanamycinum, паромомицин reduce absorption of digoxin and reduce its medical action.
Rifampicin reduces the content of digoxin in a blood plasma.
The laxatives containing magnesium and aluminum-bearing antacids reduce absorption of digoxin and reduce its therapeutic action.
Hypolipidemic means (холестирамин, холестипол) reduce digoxin absorption and by that reduce its medical action.
Metoclopramidum reduces therapeutic effect of digoxin.
Sulfasalazinum reduces therapeutic effect of digoxin.
Blockers of the proton pump (for example, омепразол) increase concentration of digoxin in a blood plasma.
Non-steroidal anti-inflammatory drugs can increase the content of digoxin in a blood plasma.
Sukralfat reduces absorption and therapeutic effect of digoxin.
Cyclosporine increases concentration дигоксинав to a blood plasma.
Drugs of the St. John's Wort which is made a hole reduce bioavailability of digoxin, increasing speed hepatic metabolizma significantly reducing its concentration in a blood plasma.
Contraindications:
Absolute:
- glikozidny intoxication;
- hypersensitivity to digoxin or other cardiac glycosides;
- the disturbances of a cordial rhythm caused by digital intoxication;
- fibrillyatsiyazheludochok;
- a hypertrophic subaortic stenosis (except for a case of heavy heart failure);
- a WPW-syndrome (especially at the accompanying fibrillation of auricles);
- periodicheskayapolny atrioventricular block or atrioventricular block 3 degrees;
- shock;
- ventricular tachycardia;
- lactation;
- detskiy teenage age up to 18 years;
Relative:
- the expressed bradycardia;
- atrioventricular block of the I degree;
- the isolated mitral stenosis;
- hypertrophic subaortal stenosis;
- acute myocardial infarction;
- premature ventricular contraction.
Overdose:
Width of therapeutic effect of drug small. Reception of 10-15 mg of Digoksina Grindeks can cause death owing to overdose in 50% of adults.
Symptoms of poisoning develop gradually. Can be observed: a loss of appetite, nausea, vomiting, diarrhea, an abdominal pain, drowsiness, confusion of consciousness, muscular weakness, delirious psychosis, decrease in visual acuity, flashing of "front sights" before eyes. Disturbances of a cordial rhythm and conductivity can cause death owing to ventricular fibrillation or the asystolia caused by blockade.
Treatment: if Digoksin Grindeks is accepted in very high dose, it is possible to make a gastric lavage directly after overdose. Absorbent carbon, connecting digoxin, interferes with its absorption from a digestive tract. The bradyarrhythmia accompanying poisoning it is possible to treat, applying atropine or connecting a temporary pacemaker. Ventrikulyarny arrhythmias are treated by lidocaine or Phenytoinum. At a bradyarrhythmia and ventrikulyarny arrhythmia it is possible to apply antibodies, specific to digoxin, – fragments of F(ab) (Wellcome).
Dialysis is not effektivnympr life-threatening poisoning with digoxin.
Storage conditions:
To store in the places protected from children, dry, at a temperature not above 25 degrees Celsius.
Issue conditions:
According to the recipe
Packaging:
On 25 tablets in a blister strip packaging from a film of polyvinyl chloride and aluminum foil.
On the 2nd blister strip packagings together with the instruction on a medical use in the state and Russian languages помещаютв a pack from a cardboard.
