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Description
Celanide is a cardiac glycoside contained in a woolly foxglove. It has a positive inotropic effect. The drug reduces venous pressure, reduces swelling, shortness of breath and causes mediated vasodilating effect.
Active ingredients
Lanatozid Ts
Release form
Pills
Composition
Lanatozid Ts, lactose, sucrose, potato starch, calcium stearate.
Pharmacological effect
Lanatozid Ts blocks the sodium / potassium-ATP-azu transport, resulting in increased sodium ion content in the cardiomyocytes, which leads to the opening of calcium channels and the entry of calcium ions into the cardiomyocyte. An excess of sodium ions helps to accelerate the release of calcium ions from the sarcoplasmic reticulum and increase its concentration in the cell, which leads to inhibition of the troponin complex, which has a suppressive effect on the interaction of actin and myosin. Increases the strength and speed of myocardial contraction by a mechanism different from the Frank-Starling mechanism (independent of the degree of myocardial pre-stretching), the systole becomes shorter and more energy efficient. As a result of the increase in myocardial contractility, the stroke volume and the minute volume of blood increase. Reduces the end systolic and end diastolic volumes of the heart, which, along with an increase in myocardial tone, leads to a reduction in its size and, thus, to a decrease in myocardial oxygen demand. The negative dromotropic effect manifests itself in an increase in the refractoriness of the atrioventricular (AV) node. In atrial tachyarrhythmias, cardiac glycosides slow down the heart rate (HR), prolong diastole, improving intracardiac and systemic hemodynamics. A decrease in heart rate occurs as a result of a direct and indirect effect on the regulation of heart rhythm. 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 excessive stretching of the heart), in patients with chronic heart failure (CHF) it 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.The initial effect of the drug appears after 1.5-2 hours, the maximum effect - after 4-6 hours.
Pharmacokinetics
Absorption: by ingestion is well absorbed in the gastrointestinal tract (GIT). The bioavailability of the drug is 15 - 45% and varies widely depending on the acidity of gastric juice, intestinal motility and blood supply, drug interactions (activated carbon, antacids, astringents reduce the absorbability of the drug in the gastrointestinal tract, metoclopramide and neostigmine methyl sulfate increase intestinal motility, dramatically reducing the bioavailability of the drug). Distribution: when it enters the systemic circulation by 20–25%, the drug binds to plasma proteins. The elimination half-life makes 28 - 36 hours. Excretion: biotransformed in the liver and excreted in the form of inactive metabolites by the kidneys and through the intestines. Slightly cumulative.
Indications
In the complex treatment of chronic heart failure II (in the presence of clinical manifestations), III and IV functional class according to the NYHA classification, the tachysystolic form of atrial fibrillation and atrial flutter of the paroxysmal and chronic course (especially in combination with chronic heart failure).
Contraindications
Glycosid intoxication, hypersensitivity to the components of the drug, AV block II degree, Wolff-Parkinson-White syndrome (WPW syndrome), intermittent complete blockade, pregnancy and breastfeeding, fructose intolerance and / or sucrase / isomaltase deficiency, lactase deficiency, lactose intolerance , glucose-galactose malabsorption, as the drug contains lactose and sucrose. Age up to 18 years.
Precautionary measures
With caution (comparing benefit / risk): bradycardia, AV block I degree, sick sinus syndrome without an artificial pacemaker, paroxysmal ventricular tachycardia, hypertrophic obstructive cardiomyopathy, acute myocardial infarction, unstable stenocardia, the likelihood of an unstable stenocardial myocardial infarction, unstable stenocardia, the likelihood of unsustainable myocardial myocardial infarction, unstable stenocardia, the likelihood of unsustainable obstructive cardiomyopathy for Morgagni-Adams-Stokes seizures, isolated mitral stenosis with a rare heart rate (hypertrophic subaortic stenosis),cardiac asthma in patients with mitral stenosis (in the absence of a tachysystolic form of atrial fibrillation), CHF with impaired diastolic function (restrictive cardiomyopathy, amyloidosis, constrictive pericarditis, cardiac tamponade), extrasystole, marked dilatation of the heart cavities, "pulmonary" heart. Water-electrolyte disorders: hypokalemia, hypomagnesemia, hypercalcemia, hypernatremia. Hypothyroidism, alkalosis, myocarditis, arteriovenous shunt, hypoxia, old age, renal / hepatic failure, obesity.
Use during pregnancy and lactation
Contraindicated in pregnancy and lactation.
Dosage and administration
Inside Dose set individually depending on the clinical picture and individual sensitivity. Celanide is prescribed orally, starting from 0.25 mg (1 tablet) - 0.5 mg (2 pills) 3-4 times a day. When a therapeutic effect is achieved (for 3-5 days), the daily dose is reduced to supporting - 0.25 mg (1 tablet) - 0.5 mg (2 pills). Higher doses for adults: single - 0.5 mg (2 pills), daily - 1 mg (4 pills). In case of violation of the renal excretory function, the dose is reduced: when creatinine (CK) clearance is 50-80 ml / min, the average maintenance dose is 50% of the average maintenance dose for persons with normal kidney function, with CK less than 10 ml / min - 25% of the usual dose .
Side effects
On the part of the digestive system are possible: loss of appetite, nausea, vomiting, diarrhea. Since the cardiovascular system: arrhythmias, AV blockade. On the part of the central nervous system: drowsiness, delirious psychosis, sleep disturbances, headache, dizziness, confusion. From the side of blood-forming organs: thrombocytopenia, thrombocytopenic purpura. Allergic reactions: skin rash. Others: decreased visual acuity, nosebleeds, petechiae, gynecomastia.
Overdose
The likelihood of intoxication increases with hypokalemia, hyponatremia, hypercalcemia, hypernatremia, hypothyroidism, "pulmonary" heart, myocarditis. On the part of the cardiovascular system: ventricular paroxysmal tachycardia, ventricular premature beats (often polytopic or bigeminia), nodular tachycardia, sinoatrial (SA) blockade, atrial fibrillation and flutter, AV blockade.On the part of the digestive tract: loss of appetite, abdominal pain, nausea, vomiting, diarrhea, intestinal necrosis. From the central nervous system and sensory organs: drowsiness, confusion, delirious psychosis, neuritis, sciatica, manic-depressive syndrome, paresthesias, reduced visual acuity, changes in visual perception (staining of visible objects in yellow-green color, perception of objects in diminished or enlarged view), flashing "flies" before my eyes. In the event of signs of overdose, it is necessary to reduce the dose or temporarily stop taking the drug. To reduce side effects, gastric lavage with a suspension of activated carbon is recommended, the use of saline laxatives, colestyramine, unithiol, potassium preparations, oxygen therapy, with rhythm disturbances that do not correct potassium preparations, antiarrhythmic drugs are recommended (difenin, lidocaine).
Interaction with other drugs
Antacids, sulfasalazine, colestiramine - reduce the absorption of the drug from the gastrointestinal tract, so the dose of the drug should be increased, after discontinuation of the antacid should be appointed initially lower dose of the drug. In combination with potassium permanganate, ammonia-anisic drops, hydrogen peroxide, silver nitrate, raspberry syrup, alkaloids salts, sulfonamides, tannin lanatoside C forms a precipitate, and inactive products with acids and bases. When combined with barbiturates (especially phenobarbital) due to the induction of liver enzymes and acceleration of metabolism, the effectiveness of the drug decreases. Glucocorticosteroids, diuretics increase the risk of hypokalemia and hypomagnesemia, thiazides, calcium preparations (especially when administered intravenously) - hypercalcemia, amiodarone, mercazole - hypothyroidism. Catecholamines, calcium preparations, diuretics increase the risk of glycoside intoxication. Synergism with lanatoside C has calcium supplements. The combination of lanatozid Ts with Aminazine helps to increase blood clotting. With the joint appointment of lanatoside C with heparin, the effect of heparin may be weakened due to an increase in blood clotting under the influence of the drug. When taking the drug along with lincomycin, pseudomembranous colitis develops.Lanatoside C excretion decreases and increases its toxicity when combined with diuretics (except potassium-sparing), insulin, amphotericinin, with prolonged use, dextrose, glucocorticosteroids, antibiotics, as a result of hypokalemia and hypomagnemia. With simultaneous use with quinidine, verapamil, nifedipine, spironolactone (to a lesser extent), the concentration of lanatoside C in the blood plasma increases (competitive reduction of secretion by the proximal tubules of the kidneys). At the same time, it is recommended to use Celanid (lanatozide C) with certain medications. With the introduction of lanatozida C with anabolic steroids, thiamine chloride, riboflavin, pyridoxine, folic acids, orotic, methyluracil, methionine, phosphadenes, inosine increases its inotropic effect.
special instructions
As one of the methods of monitoring the level of digitalization in the appointment of cardiac glycosides, control of their plasma concentration is used. In hypertrophic obstructive cardiomyopathy, the use of lanatoside C leads to increased obstruction. In severe mitral stenosis, normo-or bradycardia, heart failure develops due to a decrease in the diastolic filling of the left ventricle (LV). Lanatozide C, increasing the contractility of the myocardium of the right ventricle, causes a further increase in pressure in the pulmonary artery system, which can provoke pulmonary edema or exacerbate LV failure. Patients with mitral stenosis cardiac glycosides prescribed for accession of right ventricular failure or in the presence of atrial tachyarrhythmia. In patients with AV block II, the appointment of cardiac glycosides may aggravate it and lead to the development of a Morgagni-Adams-Stokes attack. The purpose of cardiac glycosides in AV block I degree requires caution, frequent ECG monitoring, and in some cases prophylactic use of drugs that improve AV conductivity. Lanatoside C in WPW syndrome, reducing AV conduction, contributes to the conduction of impulses through additional conduction paths bypassing the AV node and thereby provokes the development of paroxysmal tachycardia. Use the drug only as prescribed, without changing the dose yourself.If the heart rate is less than 60 beats per minute, you should immediately consult with your doctor. If the patient has not taken the drug for more than 2 days, you must inform the doctor about this. Before discontinuing the drug, inform your doctor. If you experience side effects, you should immediately consult a doctor. Before surgery or in the case of emergency care, it is necessary to warn the doctor about the use of the drug. One tablet of the drug contains 0,09875 g of carbohydrates, which corresponds to 0,008 XE (bread units).