Celanidum

General characteristics. Structure:

Active agent: Celanidum – 0,25 mg.

Auxiliary veshchestva:laktoza, potato starch sucrose, calcium stearate.

Pharmacological properties:

Pharmacodynamics. The glycoside received from leaves of a foxglove woolly. Blocks transport sodium/potassium – an ATP phase therefore, the maintenance of ions of sodium increases in cardiomyocytes that leads to opening of calcium channels and entry of calcium into a cardiomyocyte. Excess of sodium promotes acceleration of release of calcium from a sarcoplasmic reticulum and to increase in its concentration in a cell that leads to inhibition of the troponinovy complex exerting the oppressing impact on interaction of actin and a myosin. Increases force and speed of reduction of a myocardium on the mechanism other than Frank-Starlinga mechanism (does not depend on degree of preliminary stretching of a myocardium); the systole becomes shorter and energetically economic. As a result of increase in contractility of a myocardium the stroke output of blood increases.
Reduces final systolic and final diastolic heart volumes that along with increase in a tone of a myocardium leads to reduction of the sizes of heart and, thus, to decrease in need of a myocardium for oxygen.
Has negative chronotropic effect, reduces excessive sympathetic activity by increase in sensitivity of cardiopulmonary baroreceptors.
Thanking increase in activity of a vagus nerve has the antiarrhytmic effect caused by reduction of speed of carrying out iipuls through an atrioventricular node and lengthening of the effective refractory period. This effect amplifies direct action on an atrioventricular uzeya and sympatholytic action.
Has direct vasopressor effect (if positive inotropic effect of cardiac glycosides at patients with normal contractility or with heart hyperdystension is not implemented); with chronic heart failure causes the mediated vazodilatirukshchy effect in patients, reduces venous pressure raises a diuresis, reduces hypostases, short wind.
Positive bathmotropic action is shown in subtoxic and toxic doses.
The initial effect of drug is shown in 1,5-2 hours, the maximum action – in 4-6 hours.

Pharmacokinetics. Vsasyvaniye:pri intake is well soaked up in the digestive tract (DT). The Biodostulnost of drug makes 15-45% and varies over a wide range depending on acidity of a gastric juice, motility of intestines and its blood supply, medicinal interaction (absorbent carbon, antiacid drugs, astringents reduce absorbability of Tselanida® in a GIT, метфклопрамид and a neostigmina methyl sulfate strengthen an intestines peristaltics, sharply reducing bioavailability of Tselanida®).
Distribution: at revenues in a system blood stream for 20-25% drug contacts proteins of a blood plasma. The elimination half-life makes 28-36 hours.
Removal: it biotransformirutsya in a liver and it is brought out of an organism in the form of inactive metabolites with urine and excrements. Slightly kumulirut.

Indications to use:

As a part of complex therapy of chronic heart failure of the II-IV functional class (in the presence of clinical manifestations), a takhisistolichesky form of blinking and an atrial flutter of a paroxysmal and chronic current (especially in combination with chronic heart failure).

Route of administration and doses:

Inside. Doses establish individually depending on a clinical picture and individual sensitivity.
The adult for performing necessary therapy appoint inside, since 0,25 mg-0,5 of mg (1-2 tabpetka) 3-4 times a day. At achievement of therapeutic effect (3-5 days) the daily dose is reduced to supporting – 0,0005-0,25 mg.
The highest doses for adults: one-time – 0,5 mg, daily – 1 mg.
At disturbance of secretory function of kidneys the dose is reduced at the clearance of creatinine (CC) 50-80 мл.мин an average maintenance dose makes 50% of an average maintenance dose for persons with normal function of kidneys; at KK less than 10 ml/min. – 25% of a usual dose.

Features of use:

As one of control methods of digitalization level at purpose of cardiac glycosides use control of their plasma concentration.
The probability of developing of intoxication increases at a hypopotassemia, a hypomagnesiemia, a hypercalcemia, a hypernatremia, a hypothyroidism, "pulmonary" heart, myocarditis.

Side effects:

- From the alimentary system: loss of appetite, nausea, vomiting, diarrhea.
- From cardiovascular system: arrhythmias, AV blockade.
- From the central nervous system: drowsiness, delirious psychosis, sleep disorders, headache, dizziness, confusion of consciousness.
- From bodies of a hemopoiesis: thrombocytopenia, Werlhof's disease.
- Allergic reactions: skin rash.
- Other: decrease in visual acuity, nasal bleedings, petechias, gynecomastia.

Interaction with other medicines:

Antacids, Sulfasalazinum, Colestyraminum – reduce absorption.
In combination with potassium permanganate, nashatyrno-anisic drops, hydrogen peroxide, silver nitrate, crimson syrup, alkaloid salts, streptocides, a tannin the glycoside forms a deposit, with acids and the bases — inactive products.
At a combination to barbiturates (especially phenobarbital) owing to induction of enzymes of a liver and an urkoreniye of metabolism efficiency of Tselanida® decreases. A synergism with Tselanidom® calcium drugs possess.
The combination of Tselanida® to aminazine promotes increase in coagulability of blood. At joint purpose of Tselanida® with heparin easing of effect of heparin in connection with increase in coagulability of blood under influence of Tselanida® is possible.
At introduction of Tselanida® with lincomycin pseudomembranous colitis develops. Excretion of Tselanida® decreases and its toxicity at its combination to diuretics amplifies (except kaliysberegayushchy), insulin, Amphotericinum, at prolonged use of a dextrose, glucocorticosteroids, antibiotics, as a result of a hypopotassemia and a hypomagnesiemia. At simultaneous use with quinidine, verapamil, nifedipine, Spironolactonum concentration of Tselanida® in a blood plasma (to a lesser extent) increases. Antacids reduce absorption of drug from a GIT therefore the dose of Tselanida® has to be increased, after cancellation of reception of an antacid it is necessary to appoint originally smaller dose of drug.
At the same time it is recommended to apply Tselanid® with some medicines. At introduction of Tselanida® with anabolic steroids, Thiamini chloridum, Riboflavinum, a pyridoxine, acids folic, orotovy, methyluracil, methionine, fosfadeny, inosine its inotropic effect amplifies.

Contraindications:

Glikozidny intoxication, hypersensitivity to drug, atrioventricular (AV) || degrees, a WPW-syndrome, the alternating total block, pregnancy and the period of a lactation.
With care (comparing advantage/risk): atrioventricular block of the I degree, sick sinus syndrome without artificial pacemaker, probability of unstable carrying out on an atrioventricular node, instructions in the anamnesis on attacks of Morganyi-Edams-Stoksa, a hypertrophic subaortal stenosis, the isolated mitral stenosis with rare heart rate, cardiac asthma at patients with a mitral stenosis (in the absence of a takhisistolichesky form of a ciliary arrhythmia), an acute myocardial infarction, unstable stenocardia, the arteriovenous shunt, a hypoxia, heart failure with disturbance of diastolic function (a restrictive cardiomyopathy, a heart amyloidosis, chronic cardial compression, a cardiac tamponade), premature ventricular contraction, the expressed dilatation of cardial cavities, "pulmonary" heart, electrolytic disturbances: hypopotassemia, hypomagnesiemia, hypercalcemia, hyponatremia; hypothyroidism, alkalosis, myocarditis, advanced age, renal liver failure, obesity.

Overdose:

Symptoms:
From cardiovascular system: ventricular Bouveret's disease, ventricular premature ventricular contraction (often bigeminal pulse, polytopic ventricular premature ventricular contraction), nodal tachycardia, blinking and atrial flutter, AV blockade.
From a digestive tract: loss of appetite, vomiting, diarrhea, intestines necrosis.
From the central nervous system and sense bodys: neuritis, a maniac-depressive syndrome, change of visual perception (coloring of visible objects in flavovirent color, perception of objects in the reduced or increased look), flashing of "front sights" before eyes, decrease in visual acuity.
Treatment:
in case of signs of overdose it is necessary to lower a dose or to temporarily stop reception of a glycoside. For reduction of the arisen by-effects recommend a gastric lavage a suspension of absorbent carbon, use of salt laxatives, Colestyraminum, Unithiolum, potassium drugs; oxygenotherapy; at disturbances of a rhythm which do not korrigirut potassium drugs, recommend antiarrhytmic means (dipheninum, lidocaine).

Storage conditions:

List A. In protected from light and the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Tablets on 0,25 mg.
On 10 or 30 tablets in blister strip packagings. On the 3rd blister strip packagings No. 10 or 1 the blister strip packaging No. 30 together with the application instruction is placed in a pack from a cardboard.