Allaforte tablets 50mg, No. 10

Supraventricular and ventricular premature beats, paroxysmal atrial fibrillation and atrial flutter, paroxysmal supraventricular tachycardia, incl. and with WPW syndrome, paroxysmal ventricular tachycardia (in the absence of organic myocardial changes).

The method of application and dosage regimen of a particular drug depends on its form of release and other factors. The optimal dosage regimen is determined by the doctor. It is necessary to strictly observe the compliance of the used dosage form of a particular drug with the indications for use and the dosage regimen.

It is taken orally at 25 mg every 8 hours, in the absence of a therapeutic effect - every 6 hours. It is possible to increase a single dose to 50 mg every 6-8 hours.

Active ingredient : lappaconitine hydrobromide (allapininЃ) -50 mg

Excipients : pregelatinized starch, lactose monohydrate, hypromellose, calcium stearate, colloidal silicon dioxide (Aerosil A-380) - a sufficient amount to obtain a tablet weighing 350 mg.

Sinoatrial block, II and III degree AV block (without an artificial pacemaker), cardiogenic shock, right bundle branch block, combined with blockade of one of the branches of the left leg, severe hypotension (systolic blood pressure less than 90 mm Hg), moderate and severe chronic heart failure of FC III-IV according to NYHA classification, severe hypertrophy of the left ventricular myocardium (> 1.4 cm), postinfarction cardiosclerosis, Brugada syndrome, acute myocardial infarction, severe liver and / or kidney dysfunction, age up to 18 years, increased sensitivity to lappaconitine hydrobromide.

Sustained-release tablets, white or white with a grayish or yellowish tinge, round, biconvex.

Composition:

Active ingredient: lappaconitine hydrobromide (allapininЃ) - 25 mg

Excipients : pregelatinized starch, lactose monohydrate, hypromellose, calcium stearate, colloidal silicon dioxide (Aerosil A-380) - a sufficient amount to obtain a tablet weighing 230 mg.

Sustained-release tablets, white or white with a grayish or yellowish tinge, round, biconvex.

Composition:

Active ingredient : lappaconitine hydrobromide (allapininЃ) -50 mg

Excipients : pregelatinized starch, lactose monohydrate, hypromellose, calcium stearate, colloidal silicon dioxide (Aerosil A-380) - a sufficient amount to obtain a tablet weighing 350 mg.

Clinical and pharmacological group: Antiarrhythmic drug

Pharmaco-therapeutic group: Antiarrhythmic agent

pharmachologic effect

Class I C antiarrhythmic agent. Blocks fast sodium channels of cardiomyocyte membranes. It slows down AV and intraventricular conduction, shortens the effective and functional refractory periods of the atria, AV node, His bundle and Purkinje fibers, does not affect the duration of the QT interval, conduction along the AV node in the anterograde direction, heart rate, blood pressure, myocardial contractility (with the initial absence of symptoms of heart failure).

The automatism of the sinus node does not oppress. Does not cause a negative inotropic and hypotensive effect, does not have an m-anticholinergic effect.

It has a moderate antispasmodic, coronary dilating, anticholinergic, local anesthetic and sedative effect. When taken orally, the effect develops after 40-60 minutes, reaches a maximum after 80 minutes and lasts 8 hours or more.

Pharmacokinetics

When taken orally, lappaconitine hydrobromide is rapidly absorbed from the gastrointestinal tract; Cmax in blood plasma is reached on average after 80 minutes, after which it decreases rapidly. Penetrates the BBB. T1 / 2 is 1.17-2.4 hours. Only about 10% of lappaconitine hydrobromide is excreted by the kidneys per day. The bioavailability of lappaconitine hydrobromide is 40-56%, which is associated with a 'first pass' effect through the liver. Vd - 690 HP Among the resulting metabolites, the main pharmacologically active metabolite is deacetyllappaconitine. In chronic heart failure II-III FC according to the NYHA classification, the absorption of lappaconitine hydrobromide is slow (Cmax in blood plasma is reached after 2 hours), and the role of renal excretion increases (up to 28% of lappaconitine hydrobromide is excreted by the kidneys per day).

Indications

Supraventricular and ventricular premature beats, paroxysmal atrial fibrillation and atrial flutter, paroxysmal supraventricular tachycardia, incl. and with WPW syndrome, paroxysmal ventricular tachycardia (in the absence of organic myocardial changes).

Dosage regimen

The method of application and dosage regimen of a particular drug depends on its form of release and other factors. The optimal dosage regimen is determined by the doctor. It is necessary to strictly observe the compliance of the used dosage form of a particular drug with the indications for use and the dosage regimen.

It is taken orally at 25 mg every 8 hours, in the absence of a therapeutic effect - every 6 hours. It is possible to increase a single dose to 50 mg every 6-8 hours.

Side effect

From the nervous system: very often - dizziness, headache, a feeling of heaviness in the head, ataxia.

On the part of the skin and subcutaneous tissues: often - allergic reactions (hyperemia of the skin, itching).

From the side of the organ of vision: very often - diplopia.

From the side of the cardiovascular system: very often - disturbances of intraventricular and AV conduction, changes in the ECG (lengthening of the PQ interval, expansion of the QRS complex); often - sinus tachycardia (with prolonged use), increased blood pressure; infrequently - arrhythmogenic effect.

Contraindications for use

Sinoatrial block, II and III degree AV block (without an artificial pacemaker), cardiogenic shock, right bundle branch block, combined with blockade of one of the branches of the left leg, severe hypotension (systolic blood pressure less than 90 mm Hg), moderate and severe chronic heart failure of FC III-IV according to NYHA classification, severe hypertrophy of the left ventricular myocardium (> 1.4 cm), postinfarction cardiosclerosis, Brugada syndrome, acute myocardial infarction, severe liver and / or kidney dysfunction, age up to 18 years, increased sensitivity to lappaconitine hydrobromide.

Application during pregnancy and lactation

Use during pregnancy and breastfeeding is contraindicated.

Application for violations of liver function

Contraindication: severe liver dysfunction.

Application for impaired renal function

Contraindication: severe renal dysfunction.

Application in children

The drug is contraindicated for use in children and adolescents under the age of 18 years.

special instructions

Use with caution in patients with an artificial heart rate driver, with AV block I degree, chronic heart failure I-II FC according to NYHA classification, impaired intraventricular conduction, CVS, bradycardia, severe peripheral circulatory disorders, angle-closure glaucoma, benign prostatic hypertrophy, violation of conduction along Purkinje fibers, blockade of one of the legs of the bundle of His, violation of water-electrolyte metabolism (hypokalemia, hyperkalemia, hypomagnesemia).

With extreme caution, lappaconitine hydrobromide should be used in patients with coronary artery disease and stable exertional angina, since one of the predisposing factors of the proarrhythmic effect of class 1C antiarrhythmic drugs is transient myocardial ischemia and high heart rate. Use with caution in conjunction with other antiarrhythmic drugs due to the increased risk of proarrhythmogenic effects.

Lappaconitine hydrobromide is intended for long-term prophylactic antiarrhythmic therapy. The available limited clinical experience does not allow to recommend the use of oral lappaconitine hydrobromide for the relief of paroxysms of supraventricular and ventricular tachycardia.

Before starting use, it is necessary to eliminate violations of water-electrolyte metabolism, during the period of treatment, it is necessary to control the water-electrolyte balance of the blood.

Before starting use and during the period of treatment, an ECG and a clinical examination should be performed for early detection of side effects, assessing the effectiveness of the drug and determining the need to continue therapy.

In patients with an installed artificial pacemaker, the threshold for cardiac pacemaker may increase. Pacemakers should be tested and reprogrammed if necessary.

With the development of headache, dizziness, diplopia, the dose should be reduced.

With the appearance of sinus tachycardia against the background of prolonged use of the drug, the use of beta-blockers (in individually selected doses) is indicated.

When using class 1C antiarrhythmics in patients with severe organic changes in the myocardium, serious adverse reactions may occur. The use of lappaconitine hydrobromide in such patients is possible only after a careful assessment of the expected benefits and possible risks to patients, and should be carried out under the supervision of a cardiologist with experience in the treatment of the corresponding cardiac arrhythmias.

Influence on the ability to drive vehicles and mechanisms

During the period of treatment, care should be taken when performing potentially hazardous activities that require special attention and quick reactions (driving and working with moving mechanisms).

Drug interactions

With the simultaneous use of lappaconitine hydrobromide with other antiarrhythmic agents, the risk of developing an arrhythmogenic effect increases.

Lappaconitine hydrobromide enhances the effect of non-depolarizing muscle relaxants.

With the simultaneous use of lappaconitine hydrobromide with other antiarrhythmic agents, the risk of side effects associated with the influence on the function of the sinus node and AV conduction increases. An individual selection of doses of each of these drugs is required.