Allaforte® (Allaforte)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceLappakonitina hydrobromideLappakonitina hydrobromide
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  • Allapin® tablets 25 mg
    pills inwards 
    FARMTSENTR VILAR, ZAO     Russia
  • Allaforte®
    pills inwards 
    FARMTSENTR VILAR, ZAO     Russia
    • Dosage form: & nbspsustained-release tablets
    Composition:For one tablet:

    Amount, g

    Active substance:

    Dosage of 25 mg

    Dosage 50 mg

    Lappaconitin hydrobromide (Allapinin®) (in terms of 100% of the substance)

    0,025

    0,050

    Excipients: starch pregelatinized, lactose monohydrate, hypromellose, calcium stearate, silicon colloidal dioxide (aerosil A-380) -a sufficient amount to prepare a tablet weighing 0.230 g (dosage of 25 mg), or a mass of 0.350 g (dosage of 50 mg)
    Description:

    Tablets are round, biconvex, white or white with a grayish or yellowish hue.

    Pharmacotherapeutic group:Antiarrhythmic drug
    ATX: & nbsp

    C.01.B.G   Other antiarrhythmic drugs I class

    Pharmacodynamics:

    Pharmacological properties

    The active substance of the preparation is a hydrobromic acid salt of the alkaloid lappakonitina with concomitant alkaloids, obtained from the grass of a white wrestler or from the rhizomes and roots of a white- Aconitum leucostomum Worosch., or from the rhizomes with the roots of the fighter of the north (high wrestler) - Aconitum septentrionale Koelle (A. excelsum Reichenb.), family of buttercup - Ranunculaceae, or from the technical amount of alkaloids of the family of buttercups.

    Pharmacodynamics

    Antiarrhythmic drug IC class.

    It blocks "fast" sodium channels of cardiomyocyte membranes. Causes slowing of atrioventricular (AV) and intraventricular conduction, inhibits the conduct of additional pathways in the syndrome of Wolff-Parkinson-White, shortens the effective and functional refractory periods of the atria, AV node, the bundle of His and the fibers of Purkinje. Does not affect the duration of the interval QT, the conductivity along AV node of the vagal route, heart rate (heart rate) and blood pressure (BP), myocardial contractility (with the initial absence of heart failure). Does not inhibit the automaticity of the sinus node, does not have a negative inotropic effect, does not have antihypertensive and m-holinoliticheskim action.

    Has mild antispasmodic, coronary dilatation, local anesthetic and sedative action.

    When ingestion the effect develops in 40-60 minutes, remains at the reached level of 4-5 hours and gradually decreases. In general, the effect of the drug after a single oral intake is maintained for at least 12 hours.

    Pharmacokinetics:

    When taking Allaforte® inside lappaconitin hydrobromide is slowly absorbed in the gastrointestinal tract, reaching a maximum concentration in the blood plasma on average after 80 minutes, after that the concentration remains practically unchanged for 4-5 hours and gradually decreases thereafter within 24 hours with a half-life (T1/2) of the order of 7.2 hours.

    The bioavailability of lappaconitin hydrobromide is 56%, which is due to the effect of "primary transmission" through the liver. The volume distribution of 690 liters. Penetrates through the blood-brain barrier. The main pharmacologically active metabolite is deacetyl lapaconitin. With long-term use does not cumulate.

    In chronic renal failure T1/2 increases 2-3 times, with cirrhosis - 3-10 times.

    With chronic heart failure II-III functional class by classification NYHA absorption of lappaconitin hydrobromide is slowed (the maximum concentration in the blood plasma is reached after 2 hours). It is excreted by the kidneys in a modified form (up to 28%), the rest - through the intestine.

    Indications:

    Nadzheludochkovaya and ventricular extrasystole, paroxysmal form of atrial fibrillation and flutter, paroxysmal supraventricular tachycardia,including the syndrome Wolff-Parkinson-White syndrome, paroxysmal ventricular tachycardia (in the absence of organic changes infarction).

    Contraindications:

    Hypersensitivity to the components of the drug, sinoatrial blockade, AV blockade of II and III degree (without artificial pacemaker), cardiogenic shock, blockade of the right bundle of the bundle, combined with blockage of one of the branches of the left leg, severe arterial hypotension (systolic blood pressure less than 90 mm Hg), chronic heart failure III-IV functional class by classification NYHA, expressed left ventricular myocardial hypertrophy (≥ 1.4 cm), presence of postinfarction cardiosclerosis, acute coronary syndrome, Brugada syndrome, right ventricular arrhythmogenic cardiomyopathy (dysplasia), severe liver and / or kidney dysplasia, age under 18, lactose intolerance, deficiency of lactase or glucose-galactose malabsorption, syndrome of an elongated or shortened interval QT, heart disease, arrhythmogenic effect of any antiarrhythmic drug in history, pregnancy, the period of breastfeeding, alcohol abuse, AV blockade of the 1st degree with the lengthening of the interval PQ more than 200 ms, dilated cardiomyopathy, restrictive cardiomyopathy, myocarditis, no antiarrhythmic effect in the treatment of drug Allapinin® history.

    Carefully:

    FROM caution used in violation of intraventricular conduction blockade one bundle branch block, sick sinus syndrome, bradycardia, severe disturbances of peripheral circulation, angle-closure glaucoma, benign prostatic hypertrophy, disorders of water and electrolyte balance (hypokalemia, hyperkalemia, hypomagnesaemia), while the use of other antiarrhythmic agents, coronary heart disease.

    Pregnancy and lactation:

    Studies in animals have shown that lappaconitin hydrobromide at doses of 1-5 mg / kg does not possess teratogenic and embryotoxic effect. The use of the drug in pregnancy is not recommended because of the lack of controlled studies.

    It is possible to use the drug only for life indications, if the expected benefit to the mother outweighs the potential risk of side effects in the fetus / baby.

    Data on the isolation of lappaconitin hydrobromide in breast milk are absent. The use of the drug is not recommended during breastfeeding.

    If the use of Allaforte® during lactation is necessary, breastfeeding should be discontinued.

    Dosing and Administration:

    The drug should be taken under medical supervision.

    Inside, after eating, swallowing the tablet whole and washing down with a small amount of water at room temperature.

    Tablets are categorically forbidden to break, crush or chew!

    The dose of Allaforte® is selected individually. Treatment should begin with the appointment of tablets of 25 mg every 8 hours. In the absence or inadequacy of the therapeutic effect, the dose should be increased - tablets of 25 mg every 6 hours or tablets of 50 mg every 12 hours. To judge the therapeutic effect of the drug with its first use or with an increase in its dose should be no earlier than 2-3 days of regular use of the drug.

    To prevent undesirable effects of the drug on the conduction system of the heart, its use and dose increase should be monitored by ECG.It is advisable to register the ECG 1-2 hours after taking a regular single dose of the drug.

    If the PQ interval is extended to 300 ms or the development of atrioventricular blockades of a higher degree, the dose should be reduced, temporarily stopping treatment if necessary.

    It is safe to extend the QRS complex by up to 25% of the original QRS, but the QRS duration should not exceed 140 ms. It is inadmissible to extend the QRS complex beyond 50% of the original or more than 160 ms!

    The maximum daily dose of the drug is 100 mg (25 mg 4 times a day or 50 mg 2 times a day). In a dose of more than 100 mg per day, the drug is not recommended because of the lack of controlled clinical trials.

    The transfer of patients taking the drug Allapinin ®, for treatment with Allaforte ® is carried out by simple replacement, from the moment of the next intake of one drug to another with the use of the same doses and the interval between doses.

    The duration of treatment and correction of the dosing regimen (increase in dose) is determined by the doctor.

    Side effects:

    According to the World Health Organization, the undesirable effects are classified according to their frequency of development as follows: Often (≥10% of prescriptions); often (≥1% and <10%); infrequently (≥0.1% and <1%); rarely (≥0.01% and <0.1%); rarely (<0,01%); frequency unknown (insufficient data to estimate the frequency of development).

    Disturbances from the nervous system

    Often: dizziness, headache, a feeling of heaviness in the head, ataxia.

    Disturbances from the skin and subcutaneous tissues

    often: allergic reactions, hyperemia of the skin.

    Disturbances on the part of the organ of sight

    Often: diplopia.

    Heart Disease

    Often: violations of intraventricular and AV conductivity; ECG changes: lengthening of the interval PQ, expansion of the complex QRS;

    often: sinus tachycardia (with prolonged use), increased blood pressure;

    infrequently: arrhythmogenic action.

    Overdose:

    The drug has a small therapeutic latitude, so heavy intoxication can easily occur (especially with the simultaneous use of other antiarrhythmics).

    Symptoms: interval lengthening PQ and QT, expansion of the complex QRS, increased amplitude of the T wave, bradycardia, sinoatrial and atrioventricular blockade, asystole, paroxysms of polymorphic ventricular tachycardia, decreased myocardial contractility, marked decrease in blood pressure, dizziness, blurred vision, headache, gastrointestinal disorders.

    Treatment: symptomatic, gastric lavage, defibrillation, administration of dobutamine, diazepam; if necessary - artificial ventilation and indirect heart massage.

    To treat ventricular tachycardia, do not use antiarrhythmic drugs IA and IC class.

    Interaction:

    Inducers of microsomal liver enzymes do not affect the efficacy of lappaconitin hydrobromide.

    Lappakonitina hydrobromide enhances the effect of nondepolarizing muscle relaxants.

    With the simultaneous use of lappaconitin hydrobromide with other antiarrhythmics, the risk of side effects associated with sinus node function and atrial-ventricular conduction increases. Individual dosage of each of these drugs is required.

    In a clinical study using lappaconitin hydrobromide against a background of standard antihypertensive therapy with angiotensin-converting enzyme inhibitors, angiotensin II receptor antagonists, dihydropyridine derivative blockers of the "slow" calcium channels, beta-adrenoblockers, no strengthening or weakening of antihypertensive action was observed.

    There is no evidence of adverse effects of lappaconitin hydrobromide on the efficacy and safety of indirect anticoagulants.

    Special instructions:

    With the cancellation of previous ineffective antiarrhythmic therapy, Allaforte® should be started at a time longer than 2 to 5 half-lives of these drugs (depending on their dose) in order to avoid the mutual enhancement of adverse effects on the function of the conduction system of the heart. In the case of amiodarone, which has a very long half-life, the use of Allaforte® is possible immediately after the discontinuation of the previous drug, but additional precautions are required, as in combination therapy.

    Compared with the non-protracted form of lappaconitin hydrobromide, Allaforte® provides a slower absorption and a uniform distribution of the concentration of the active substance in the blood between the doses, which leads to a reduction in the incidence and severity of side effects.

    Before starting the use of the drug, it is necessary to eliminate disturbances in the water-electrolyte balance, during the period of therapy, it is necessary to monitor the content of electrolytes in the blood.

    Each patient who takes Allaforte® should undergo an electrocardiographic and clinical examination before and during therapy for the early detection of side effects, evaluation of the effectiveness of the drug and the need for continued therapy.

    In patients with an established artificial heart rhythm driver, the threshold of its stimulation may increase.

    Pacemakers should be checked and, if necessary, reprogrammed.

    With the development of headache, dizziness, diplopia should reduce the dose of the drug.

    When sinus tachycardia appears against the background of long-term use of the drug, beta-blockers are indicated.

    As with other antiarrhythmic drugs IC class, in patients with significant organic changes in the myocardium, severe undesirable effects may occur when the drug is used. Special control with the use of a sample with physical activity requires the use of Allaforte® in patients with coronary heart disease and stable angina, as one of the predisposing factors of arrhythmogenic actions of drugs of the class IC is transient myocardial ischemia and high heart rate.

    When using antiarrhythmic drugs IC class patients with severe organic myocardial changes are predisposed to the development of serious side effects. The use of Allaforte® in such patients is possible only in exceptional cases, by the decision of a doctor's consultation.

    Effect on the ability to drive transp. cf. and fur:

    When using the drug, care must be taken when driving vehicles and engaging in other potentially hazardous activities requiring increased concentration and speed of psychomotor reactions due to the risk of dizziness.

    Form release / dosage:Tablets of prolonged action, 25 mg and 50 mg.
    Packaging:

    For 10 or 15 tablets in a planar cell packaging made of polyvinylchloride film and aluminum foil with thermo-lacquer coating.

    One, two or three contour packs of 10 or 15 tablets together with instructions for medical use are placed in a pack of cardboard for consumer containers.

    Storage conditions:

    In the dark place at a temperature of no higher than 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    3 years.

    Do not use after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:LP-004040
    Date of registration:22.12.2016
    Expiration Date:22.12.2021
    The owner of the registration certificate:FARMTSENTR VILAR, ZAO FARMTSENTR VILAR, ZAO Russia
    Manufacturer: & nbsp
    Representation: & nbspFARMCENTER VILAR CJSC FARMCENTER VILAR CJSC Russia
    Information update date: & nbsp08.07.2017
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