Composition, form of production and packaging
Tablets are white, round, biconvex.
Lappaconitin hydrobromide (alapinin В® ) 25 mg
Excipients: sucrose (sugar or sugar-raffirad, or granulated sugar) 65.5 mg, potato starch 7.5 mg, calcium stearate (calcium stearate) 1 mg, croscarmellose sodium 1 mg.
10 pieces. - packings of cellular contour (1) - packs cardboard.
10 pieces. - packings cellular planimetric (2) - packs cardboard.
10 pieces. - packings cellular planimetric (3) - packs cardboard.
10 pieces. - packings cellular planimetric (5) - packs cardboard.
30 pcs. - packings of cellular contour (1) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2011.
Antiarrhythmic drug of class I C. It blocks fast sodium channels of membranes of cardiomyocytes. It causes a slowing of AV and intraventricular conduction, shortens the effective and functional refractory periods of the atria, AV node, bundle of His and Purkinje fibers, does not affect the duration of the QT interval, AV conduction in the anterograde direction, heart rate, blood pressure, myocardial contractility initial absence of heart failure).
Do not depress the automatism of the sinus node. Does not cause negative inotropic and hypotensive effect.
Allapinin В® renders moderate spasmolytic, coronary dilatory, anticholinergic, local anesthetic and sedative action. When ingested, the effect develops in 40-60 minutes, reaches a maximum after 80 minutes and lasts 8 hours or more.
Bioavailability is 40%. The drug is exposed to the effect of "first passage" through the liver.
Distribution and Metabolism
When ingested, V d is 690 liters. Penetrates through the BBB.
T 1/2 is 1-1.2 hours. It is excreted by the kidneys.
Pharmacokinetics in special clinical cases
With prolonged use, an increase of T 1/2 is possible. In chronic renal failure T 1/2 increases 2-3 times, with cirrhosis - 3-10 times.
- supraventricular extrasystole;
- ventricular extrasystole;
- paroxysms of flicker and atrial flutter;
- Paroxysmal supraventricular tachycardia (including with WPW syndrome);
- paroxysmal ventricular tachycardia (in the absence of organic damage to the heart).
Assign inside 25 mg (1 tab.) Every 8 hours, with no therapeutic effect - every 6 hours.
It is possible to increase the single dose to 50 mg (2 tablets) every 6-8 hours. The maximum daily dose is 300 mg (12 tablets).
The duration of treatment and the change in the dosage regimen (increase in the dose) is determined by the doctor.
The drug is taken orally, after eating, squeezed with a small amount of water at room temperature, do not grind the tablets.
From the side of the central nervous system and peripheral nervous system: dizziness, headache, a sense of heaviness in the head, ataxia, diplopia.
From the side of the cardiovascular system: there may be violations of AV and intraventricular conduction, the appearance of sinus tachycardia (with prolonged use), arrhythmogenic action, changes in ECG (prolongation of the PQ interval, expansion of the QRS complex).
Other: possible flushing of the skin, allergic reactions.
- Sinoatrial blockade;
- AV blockade II and III degree (without artificial pacemaker);
- cardiogenic shock;
- blockade of the right leg of the bundle of Hisb, combined with a blockage of one of the branches of the left leg;
- severe arterial hypotension (systolic blood pressure less than 90 mm Hg);
- Moderate and severe chronic heart failure of III-IV functional class according to NYHA classification;
- marked hypertrophy of the myocardium of the left ventricle (1.4 cm);
- presence of postinfarction cardiosclerosis;
- Severe violations of the liver and / or kidney function;
- fructose intolerance, glucose / galactose absorption impairment syndrome, sugarase / isomaltase deficiency (the preparation contains sucrose);
- children and adolescents under 18 years of age (efficacy and safety not established);
- Hypersensitivity to the drug.
With caution should be used with AV blockade of I degree, violation of intraventricular conduction, SSSU, bradycardia, severe peripheral circulation disorders, angle-closure glaucoma, prostatic hypertrophy, impaired conduction along Purkinje fibers, blockage of one of the legs of the bundle of Guiss, disturbance of electrolyte metabolism (hypokalemia , giperkaliemia, hypomagnesemia), with simultaneous reception with other antiarrhythmic drugs.
PREGNANCY AND LACTATION
Application of the drug Allapinin В® in pregnancy is not recommended. It is possible to use the drug only for life indications, if the intended benefit for the mother exceeds the potential risk to the fetus or the child.
There is no data on the isolation of lappaconitin hydrobromide in breast milk. The use of the drug is not recommended during breastfeeding. If the use of the drug during lactation is necessary, breastfeeding should be discontinued.
APPLICATION FOR FUNCTIONS OF THE LIVER
Contraindicated in severe impairment of kidney function.
In chronic renal failure , a reduction in the dose of Allapinin is required.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Contraindicated in severe violations of liver function.
Before the application of the drug Allapinin В®, it is necessary to eliminate the disturbances of water-electrolyte metabolism, during the therapy it is necessary to control the water-electrolyte balance of water.
In patients who underwent acute myocardial infarction, or in patients with heart failure, as well as in patients with an established pacemaker, the threshold of its stimulation may increase.
With the development of headache, dizziness, diplopia should reduce the dose of the drug Allapinin В® .
When sinus tachycardia appears against the background of long-term use of the drug, beta-blockers in low doses are indicated.
1 tablet contains 74 mg of carbohydrates, which corresponds to 0.01 XE.
Impact on the ability to drive vehicles and manage mechanisms
When using the drug, care should be taken when carrying out potentially hazardous activities requiring special attention and quick reactions (transport management, work with moving mechanisms).
Symptoms: the drug has a small breadth of therapeutic effect, so heavy intoxication can easily occur (especially with the simultaneous use of other antiarrhythmics): prolongation of the PR and QT intervals, expansion of the QRS complex, increase in the amplitude of the T wave, bradycardia, sinoatrial block, AV blockade, asystole , paroxysms of polymorphic ventricular tachycardia, decreased myocardial contractility, marked decrease in blood pressure, dizziness, blurred vision, headache, gastrointestinal disorders.
Treatment: conduct symptomatic therapy. To treat ventricular tachycardia, antiarrhythmic drugs of Class I A and I C should not be used. Sodium bicarbonate can eliminate the expansion of the QRS complex, bradycardia and arterial hypotension.
With the simultaneous use of microsomal liver enzymes with inducers, the efficacy of lappaconitin hydrobromide decreases, and the risk of toxic effects increases.
Antiarrhythmic drugs of other classes increase the risk of arrhythmogenic action.
Lappakonitina hydrobromide enhances the action of nondepolarizing muscle relaxants.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored out of the reach of children, protected from light at a temperature of no higher than 25 В° C. Shelf life - 5 years.