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

Active ingredient

Composition

Quantity, g

The active ingredient:

Dosage 25 mg

Dosage 50 mg

0.025

0.050

Excipients: Pregelatinized starch, lactose monohydrate, hypromellose, calcium stearate, colloidal silicon dioxide (aerosil A-380)-enough to obtain a tablet weighing 0.230 g (25 mg dosage), or weighing 0.350 g (50 mg dosage)

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

How to take, the dosage

The drug should be taken under a physician’s supervision.

Overly, after a meal, swallow the whole tablet with a small amount of water at room temperature.

The tablets must never be crushed, crushed or chewed.

The dose of Allaforte® is adjusted individually. Treatment should begin with a prescription of 25 mg tablets every 8 hours. In the absence or insufficiency of therapeutic effect the dose should be increased – tablets of 25 mg every 6 hours or tablets of 50 mg every 12 hours. To judge about the therapeutic effect of the drug at its first use or if the dose is increased, not earlier than after 2-3 days of regular use of the drug.

In order to prevent undesirable effects of the drug on the cardiac conduction system, its use and dose increase should be monitored with ECG. It is reasonable to record ECG 1-2 hours after taking another single dose of the drug.

If the PQ interval is prolonged to 300 ms or if a higher degree of atrial-ventricular block develops, the dose should be reduced and, if necessary, treatment should be temporarily stopped.

Lengthening of the QRS complex by up to 25% of the baseline is safe, but the QRS duration must not exceed 140 ms. It is unacceptable to lengthen the QRS complex beyond 50% of the baseline or more than 160 ms!

The maximum daily dose of the drug is 100 mg (25 mg 4 times daily or 50 mg 2 times daily). It is not recommended to take the drug in a dose greater than 100 mg per day due to lack of controlled clinical trials.

The conversion of patients taking Allapinin® to treatment with Allaforte® is done by simple substitution, starting with the next dose of one drug for another using the same doses and intervals between doses.

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

Interaction

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

Lappaconitine hydrobromide increases the effect of nondepolarizing myorelaxants.

In concomitant use of lappaconitine hydrobromide with other antiarrhythmic drugs, the risk of side effects associated with the effect on sinus node function and atrial-ventricular conduction increases. Individual dosing of each of these agents needs to be adjusted.

In clinical study when using lappaconitine hydrobromide against standard hypotensive therapy with angiotensin-converting enzyme inhibitors, angiotensin II receptor antagonists, slow calcium channel blockers of dihydropyridine derivatives, beta-adrenoblockers no enhancement or weakening of antihypertensive effect was observed.

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

Special Instructions

Contraindications

Side effects

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

Nervous system disorders

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

Skin and subcutaneous tissue disorders

often: allergic reactions, skin hyperemia.

Visual organ disorders

very often: diplopia.

Cardiac disorders

very common: intraventricular and AV conduction abnormalities; ECG changes: prolongation of the PQ interval, enlargement of the QRS complex;

often: sinus tachycardia (with long-term use), increased BP;

infrequent: arrhythmogenic effects.

Overdose

Similarities