Allaforte, 25 mg 20 pcs.

Pharmacotherapeutic group:

Antiarrhythmic medicine

ATC:

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

Pharmacodynamics:

Pharmacological properties

The active ingredient of the drug is a bromine-hydrogen salt of the lappaconitin alkaloid with associated alkaloids, obtained from the grass of whitebeard or from the rhizomes and roots of whitebeard – Aconitum leucostomum Worosch., or from rhizomes with roots of northern hogweed (wolfsbane) – Aconitum septentrionale Koelle (A. excelsum Reichenb.), family Buttercups – Ranunculaceae, or from technical sum of alkaloids of the buttercup family.

Pharmacodynamics

The IC class antiarrhythmic drug.

Blocks “fast” sodium channels of cardiomyocyte membranes. It causes delay in atrioventricular (AV) and intraventricular conduction, inhibits conduction through additional pathways in Wolff-Parkinson-White syndrome, shortens effective and functional refractory periods of atria, AV node, Gis bundle and Purkinje fibers. It does not affect the QT interval duration, AV node conduction in vanterograde direction, heart rate (HR) and blood pressure (BP), myocardial contractility (in the initial absence of heart failure phenomena). It does not inhibit sinus node automatism, has no negative inotropic effect, has no antihypertensive and m-cholinolytic action.

It has moderate antispasmodic, coronary dilator, local anesthetic and sedative effects.

When taken orally, the effect develops after 40-60 minutes, stays at the achieved level for 4-5 hours and then gradually decreases. In general, the effect of the drug after a single oral administration lasts for at least 12 hours.

Pharmacokinetics:

On oral administration of Allaforte®, lappaconitine hydrobromide is slowly absorbed in the gastrointestinal tract, reaching maximum plasma concentration after an average of 80 minutes, after which the concentration remains virtually unchanged for 4-5 hours and gradually decreases further over 24 hours with a half-life (T1/2) of approximately 7.2 hours.

The bioavailability of lappaconitine hydrobromide is 56%, which is associated with the effect of “primary passage” through the liver. Distribution volume is 690 l. It penetrates through the blood-brain barrier. The main pharmacologically active metabolite is deacetylappaconitin. It does not cumulate with prolonged use.

In chronic renal insufficiency the T1/2 is increased by 2-3 times, in liver cirrhosis – by 3-10 times.

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

Indications

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

Pharmacological effect

Pharmacotherapeutic group:

Antiarrhythmic drug

ATX:

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

Pharmacodynamics:

Pharmacological properties

The active substance of the drug is the hydrobromide salt of the alkaloid lappaconitine with accompanying alkaloids, obtained from the grass of the white-mouthed wrestler or from the rhizomes and roots of the white-mouthed wrestler – Aconitum leucostomum Worosch., or from the rhizomes with roots of the northern wrestler (high wrestler) – Aconitum septentrionale Koelle (A. excelsum Reichenb.), family Ranunculaceae – Ranunculaceae, or from the technical sum of alkaloids of the Ranunculaceae family.

Pharmacodynamics

Class IC antiarrhythmic drug.

Blocks “fast” sodium channels of cardiomyocyte membranes. Causes a slowdown in atrioventricular (AV) and intraventricular conduction, inhibits conduction along additional pathways in Wolff-Parkinson-White syndrome, 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 through the AV node in the venterograde direction, heart rate (HR) and blood pressure (BP), myocardial contractility (in the initial absence of heart failure). It does not inhibit the automatism of the sinus node, does not have a negative inotropic effect, and does not have an antihypertensive or m-cholinolytic effect.

It has a moderate antispasmodic, coronary dilation, local anesthetic and sedative effect.

When taken orally, the effect develops after 40-60 minutes, remains at the achieved level for 4-5 hours and gradually decreases. In general, the effect of the drug after a single oral dose lasts for at least 12 hours.

Pharmacokinetics:

When Allaforte® is taken orally, lappaconitine hydrobromide is slowly absorbed in the gastrointestinal tract, reaching a maximum concentration in the blood plasma after an average of 80 minutes, after which the concentration remains virtually unchanged for 4-5 hours and gradually decreases further over 24 hours with a half-life (T1/2) of about 7.2 hours.

The bioavailability of lappaconitine hydrobromide is 56%, which is associated with the effect of “first pass” through the liver. Distribution volume 690 l. Penetrates the blood-brain barrier. The main pharmacologically active metabolite is desacetyllappaconitine. With long-term use it does not accumulate.

In chronic renal failure, T1/2 increases by 2-3 times, in liver cirrhosis – by 3-10 times.

In chronic heart failure of functional class II-III according to the NYHA classification, the absorption of lappaconitine hydrobromide is slowed down (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 intestines.

Special instructions

When canceling previous ineffective antiarrhythmic therapy, treatment with Allaforte® should be started within a period exceeding 2-5 half-lives of these drugs (depending on their dose) in order to avoid mutually reinforcing the adverse effects on the function of the cardiac conduction system. In the case of amiodarone, which has a very long half-life, the use of Allaforte® is possible immediately after discontinuation of the previous drug, but additional precautions are required, as when carrying out combination therapy.

Active ingredient

Lappaconitine hydrobromide

Composition

For one tablet:

Quantity, g

Active ingredient:

Dosage 25 mg

Dosage 50 mg

Lappaconitine hydrobromide (Allapinin®) (calculated as 100% substance)

0.025

0.050

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

Description:

The tablets are round, biconvex, white or white with a grayish or yellowish tint.

Contraindications

Hypersensitivity to the components of the drug, sinoatrial block, AV block II and III degrees (without an artificial pacemaker), cardiogenic shock, right bundle branch block combined with blockade 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 according to the NYHA classification, severe myocardial hypertrophy left ventricle (≥1.4 cm), the presence of post-infarction cardiosclerosis, acute coronary syndrome, Brugada syndrome, arrhythmogenic cardiomyopathy (dysplasia) of the right ventricle, severe liver and/or kidney dysfunction, age under 18 years, lactose intolerance, lactase deficiency or glucose-galactose malabsorption, long or short QT interval syndrome, heart defects, history of arrhythmogenic effects of any antiarrhythmic drug, pregnancy, breastfeeding, alcohol abuse, first degree AV block with prolongation of the PQ interval by more than 200 ms, dilated cardiomyopathy, restrictive cardiomyopathy, myocarditis, lack of antiarrhythmic effect during treatment with Allapinin® in history.

With caution:
Use with caution in case of intraventricular conduction disorders, blockade of one of the His bundle branches, sick sinus syndrome, bradycardia, severe peripheral circulatory disorders, angle-closure glaucoma, benign prostatic hypertrophy, water-electrolyte balance disorders (hypokalemia, hyperkalemia, hypomagnesemia), with simultaneous use of other antiarrhythmic drugs, with coronary heart disease.

Side Effects

According to the World Health Organization, adverse effects are classified according to their frequency as follows: very common (≥10% of prescriptions); often (≥1% and <10%); uncommon (≥0.1% and <1%); rare (≥0.01% and <0.1%); very rare (<0.01%); frequency unknown (insufficient data to estimate the frequency of development).

Nervous system disorders

very often: dizziness, headache, feeling of heaviness in the head, ataxia.

Skin and subcutaneous tissue disorders

often: allergic reactions, hyperemia of the skin.

Visual disorders

very common: diplopia.

Heart disorders

very often: intraventricular and AV conduction disorders; ECG changes: prolongation of the PQ interval, expansion of the QRS complex;

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

uncommon: arrhythmogenic effect.

Interaction

Inducers of microsomal liver enzymes do not affect the effectiveness of lappaconitine hydrobromide.

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

With simultaneous use of lappaconitine hydrobromide with other antiarrhythmic drugs, the risk of side effects associated with the effect on the function of the sinus node and atrioventricular conduction increases. Individual selection of doses of each of these drugs is required.

In a clinical study, when lappaconitine hydrobromide was used against the background of standard antihypertensive therapy with angiotensin-converting enzyme inhibitors, angiotensin II receptor antagonists, blockers of “slow” calcium channels, dihydropyridine derivatives, and beta-blockers, no increase or decrease in the antihypertensive effect was observed.

There is no data on the adverse effects of lappaconitine hydrobromide on the effectiveness and safety of indirect anticoagulants.

Overdose

The drug has a small therapeutic breadth, so severe intoxication can easily occur (especially with simultaneous use of other antiarrhythmic drugs).

Storage conditions

In a place protected from light, at a temperature not exceeding 25 ° C.

Keep out of the reach of children.

Shelf life

3 years.

Do not use after expiration date.

Manufacturer

Pharmcenter VILAR JSC, Russia