Allapinin^® (Tablets) Instructions for Use

Marketing Authorization Holder

Pharmtsentr Vilar JSC (Russia)

Contact Information

PHARMCENTR VILAR JSC (Russia)

ATC Code

C01BC (Class Ic antiarrhythmic agents)

Active Substance

Lappaconitine hydrobromide (Grouping name)

Dosage Form

Allapinin®

Tablets 25 mg: 10, 20, 30, or 50 pcs.

Dosage Form, Packaging, and Composition

Tablets are white, round, biconvex in shape.

* Lappaconitine hydrobromide with accompanying alkaloids (Allapinin^®) (calculated as 100% substance).

Excipients: sucrose (white sugar), potato starch, calcium stearate, croscarmellose sodium.

10 pcs. – contour cell packs (1) – cardboard packs.
10 pcs. – contour cell packs (2) – cardboard packs.
10 pcs. – contour cell packs (3) – cardboard packs.
10 pcs. – contour cell packs (5) – cardboard packs.

Clinical-Pharmacological Group

Antiarrhythmic drug

Pharmacotherapeutic Group

Means for the treatment of heart diseases; antiarrhythmic agents, classes I and III; antiarrhythmic agents, class IC

Pharmacological Action

An antiarrhythmic drug of class I C. It blocks the fast sodium channels of cardiomyocyte membranes. It causes a slowdown 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, conduction through the AV node in the anterograde direction, heart rate, blood pressure, myocardial contractility (in the initial absence of heart failure).

It does not depress sinus node automaticity. It does not cause a negative inotropic or hypotensive effect.

Allapinin^® has a moderate antispasmodic, coronary vasodilating, cholinoblocking, local anesthetic and sedative effect. When taken orally, the effect develops after 40-60 minutes, reaches a maximum after 80 minutes and lasts for 8 hours or more.

Pharmacokinetics

Absorption

Bioavailability is 40%. The drug undergoes the first-pass effect through the liver.

Distribution and Metabolism

When taken orally, V_d is 690 L. It penetrates the blood-brain barrier.

Elimination

T_1/2 is 1-1.2 hours. It is excreted by the kidneys.

Pharmacokinetics in Special Clinical Cases

With long-term use, an increase in T_1/2 is possible. In chronic renal failure, T_1/2 increases by 2-3 times, in liver cirrhosis – by 3-10 times.

Indications

• Supraventricular extrasystole;
• Ventricular extrasystole;
• Paroxysms of atrial fibrillation and flutter;
• Paroxysmal supraventricular tachycardia (including in WPW syndrome);
• Paroxysmal ventricular tachycardia (in the absence of organic heart lesions).

ICD codes

Dosage Regimen

It is prescribed orally, 25 mg (1 tab.) every 8 hours; if there is no therapeutic effect – every 6 hours.

An increase in the single dose to 50 mg (2 tab.) every 6-8 hours is possible. The maximum daily dose is 300 mg (12 tab.).

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

The drug is taken orally, after meals, with a small amount of water at room temperature; do not crush the tablets.

Adverse Reactions

From the central and peripheral nervous system: dizziness, headache, feeling of heaviness in the head, ataxia, diplopia are possible.

From the cardiovascular system: disturbances of AV and intraventricular conduction, occurrence of sinus tachycardia (with long-term use), arrhythmogenic action, changes on the ECG (prolongation of the PQ interval, widening of the QRS complex) are possible.

Other: skin hyperemia, allergic reactions are possible.

Contraindications

• Sinoatrial block;
• AV block of II and III degree (without an artificial pacemaker);
• Cardiogenic shock;
• Right bundle branch block combined with block of one of the branches of the left bundle branch;
• Severe arterial hypotension (systolic BP less than 90 mm Hg);
• Moderate and severe chronic heart failure of functional class III-IV according to the NYHA classification;
• Severe hypertrophy of the left ventricular myocardium (≥1.4 cm);
• Presence of post-infarction cardiosclerosis;
• Severe impairment of liver and/or kidney function;
• Fructose intolerance, glucose/galactose malabsorption syndrome, sucrase/isomaltase deficiency (the drug contains sucrose);
• Children and adolescents under 18 years of age (efficacy and safety have not been established);
• Hypersensitivity to the drug.

With caution, the drug should be used for AV block of I degree, impaired intraventricular conduction, sick sinus syndrome, bradycardia, severe peripheral circulatory disorders, closed-angle glaucoma, prostatic hyperplasia, impaired conduction through the Purkinje fibers, block of one of the bundle branches, electrolyte imbalance (hypokalemia, hyperkalemia, hypomagnesemia), with simultaneous use with other antiarrhythmic drugs.

Use in Pregnancy and Lactation

The use of Allapinin^® during pregnancy is not recommended. The drug can be used only for vital indications, if the intended benefit to the mother outweighs the potential risk to the fetus or child.

There are no data on the excretion of lappaconitine hydrobromide into 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.

Use in Hepatic Impairment

Contraindicated in severe liver function impairment.

Use in Renal Impairment

Contraindicated in severe renal function impairment.

In chronic renal failure, a dose reduction of Allapinin^® is required.

Special Precautions

Before starting the use of Allapinin^®, it is necessary to correct water-electrolyte imbalance; during therapy, control of water-electrolyte balance is required.

In patients who have had an acute myocardial infarction, or in patients with heart failure, as well as in patients with an established artificial pacemaker, the stimulation threshold may increase.

If headache, dizziness, or diplopia develops, the dose of Allapinin^® should be reduced.

If sinus tachycardia appears during long-term use of the drug, the use of beta-blockers in low doses is indicated.

1 tablet contains 74 mg of carbohydrates, which corresponds to 0.01 XE.

Effect on the ability to drive vehicles and mechanisms

Caution should be exercised when using the drug when engaging in potentially hazardous activities that require increased attention and rapid reactions (driving vehicles, working with moving mechanisms).

Overdose

Symptoms: the drug has a narrow therapeutic window, so severe intoxication can easily occur (especially with simultaneous use of other antiarrhythmic drugs): prolongation of PR and QT intervals, widening of the QRS complex, increase in T wave amplitude, bradycardia, sinoatrial block, AV block, asystole, paroxysms of polymorphic ventricular tachycardia, decreased myocardial contractility, pronounced decrease in BP, dizziness, blurred vision, headache, gastrointestinal disorders.

Treatment: symptomatic therapy is performed. Antiarrhythmic drugs of class I A and I C should not be used to treat ventricular tachycardia. Sodium bicarbonate can eliminate the widening of the QRS complex, bradycardia and arterial hypotension.

Drug Interactions

With simultaneous use with inducers of liver microsomal enzymes, the effectiveness of lappaconitine hydrobromide decreases, and the risk of toxic effects increases.

Antiarrhythmic agents of other classes increase the risk of arrhythmogenic action.

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

Storage Conditions

The drug should be stored out of the reach of children, protected from light, at a temperature not exceeding 25°C (77°F).

Shelf Life

The shelf life is 5 years.

Dispensing Status

The drug is dispensed by prescription.

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.