Laporitmin, tablets 25 mg 30 pcs

Pharmacotherapeutic group: antiarrhythmic drug.

ATX code: C01BG

Pharmacological properties

Laporitmin® is bromine hydrogenate salt of lappaconitin alkaloid with the accompanying alkaloids, obtained from the grass of white bearded wormwood – Aconitum leucostomum Worosch. and rhizomes with roots of northern wolfberry (wolfsbane) – Aconitum septentrionale Koelle (A. Excelsum Reichenb.), family Ranunculaceae.

Pharmacodynamics

Antiarrhythmic drug of IC class. Blocks “fast” sodium channels of cardiomyocyte membranes. It causes delay in atrioventricular (AV) and intraventricular conduction, shortens effective and functional refractory periods of atria, AV node, Gis bundle and Nourkinje fibers and does not influence QT interval duration, conduction through AV node in anterograde direction, heart rate, myocardial contractility (in initial absence of cardiac insufficiency). It does not inhibit sinus node automatism, has no negative inotropic effect, has no antihypertensive and M-cholinolytic effects. It has moderate antispasmodic, coronary dilator, local anesthetic and sedative effect.

When taken orally, the effect develops in 40-60 minutes, reaches its maximum in 4-5 hours and lasts for 8 hours or more.

Pharmacokinetics

On oral administration, lappaconitine hydrobromide is rapidly absorbed in the gastrointestinal tract; maximum plasma concentration is reached in 80 minutes on average, after which it rapidly decreases. It penetrates the blood-brain barrier.

The elimination half-life (T1/2) is 1.17-2.4 hours. Only about 10% of lappaconitine hydrobromide is excreted by the kidneys during 24 hours. Bioavailability of lappaconitine hydrobromide is from 40 to 56%, which is associated with the effect of “primary passage” through the liver. The volume of distribution is 690 l. Among the metabolites formed the main pharmacologically active metabolite is deacetylappaconitine. In chronic heart failure IIb-III functional class according to NYHA classification absorption of lappaconitine hydrobromide is delayed (maximum concentration in blood plasma is reached after 2 hours), and the role of renal excretion is increased (kidneys excrete up to 28% of lappaconitine hydrobromide per day).

Indications

Supraventricular and ventricular extrasystoles, paroxysmal atrial fibrillation and flutter, paroxysmal supraventricular tachycardia, including in Wolf-Parkinson-White syndrome (WPW), paroxysmal ventricular tachycardia (in the absence of organic myocardial changes).

Active ingredient

Lappaconitine hydrobromide

Composition

Active ingredient:

Lappaconitin hydrobromide (in terms of 100% substance) – 25.0 mg

Excipients:

lactose monohydrate 63.5 mg,

potato starch 10.0 mg,

calcium stearate 1.0 mg,

colloidal silica 0.5 mg.

How to take, the dosage

Orally, after the meal with plenty of water, do not crush.

Take 1 tablet (25 mg) every 8 hours, in the absence of therapeutic effect – every 6 hours.

The single dose may be increased up to 2 tablets (50 mg) every 6-8 hours.

The maximum daily dose is 300 mg (12 tablets).

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

Interaction

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

Concomitant use of lappaconitine hydrobromide with other antiarrhythmic drugs increases the risk of arrhythmogenic effects.

Lappaconitine hydrobromide increases the effect of nondepolarizing muscle relaxants.

Simultaneous use of lappaconitine hydrobromide with other antiarrhythmic agents increases the risk of side effects associated with the effect on sinus node function and atrial-ventricular conduction. Individual selection of doses of each of these drugs is required.

In clinical trial during use of lappaconitine hydrobromide during standard hypotensive therapy with angiotensin-converting enzyme inhibitors, angiotensin II receptor antagonists, “slow” calcium channel blockers of dihydropyridine derivatives, beta-adrenoblockers the increase or weakening of antihypertensive effect was not observed.

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

Special Instructions

The drug is used as prescribed by the physician.

Laporitmin® must be treated before initiating the use of the drug; the water-electrolyte balance of the blood must be monitored during therapy.

All patients taking Laporitmin® should undergo electrocardiographic and clinical monitoring before and during therapy to enable early detection of side effects, to evaluate the effectiveness of the drug and the need for continued therapy.

Patients with a pacemaker in place may have a higher threshold of stimulation. Pacemakers should be checked and reprogrammed if necessary.

In case of development of headache, dizziness, diplopia, the drug dose should be reduced.

If sinus tachycardia occurs with long-term use of the drug, beta-adrenoblockers should be used (in individually adjusted doses).

When using IC class antiarrhythmic agents in patients with severe organic myocardial changes, serious adverse reactions may occur. The use of Laporitmin® in such patients is possible only after careful evaluation of the expected benefits and possible risks to patients, and should be carried out under the supervision of a cardiologist experienced in the treatment of the corresponding cardiac rhythm disturbances. Laporitmin® should be used with particular caution in patients with coronary heart disease and stable angina pectoris, because one of the predisposing factors of proarrhythmic effect of IC class antiarrhythmic drugs is transient myocardial ischemia and high HR. Laporitmin® should be used with caution together with other antiarrhythmic drugs due to the increased risk of proarrhythmogenic action. Adverse effects of other IC class antiarrhythmic drugs on electrophysiological parameters and clinical manifestations in Brugada syndrome have been found. Lappaconitine hydrobromide has no experience with Brugada syndrome, and therefore Laporitmin® is contraindicated in patients with Brugada syndrome.

Laporitmin® is intended for long-term prophylactic antiarrhythmic therapy. The limited clinical experience available does not allow recommending the use of Laporitmin® orally to relieve paroxysms of supraventricular and ventricular tachycardia.

One tablet of Laporitmin® contains approximately 0.007 BE (bread units).

Influence on driving and operating machinery

When using the drug, caution should be exercised while driving vehicles and engaging in other potentially dangerous activities requiring increased concentration and quick psychomotor reactions due to the risk of dizziness.

Contraindications

Hypersensitivity to lappaconitine hydrobromide or any other drug component, sinoatrial block, atrioventricular block of II and III degree (without pacemaker), cardiogenic shock, right bundle branch block combined with a left bundle branch block, severe arterial hypotension (systolic blood pressure less than 90 mm Hg).), moderate and severe chronic heart failure III-IV functional class according to NYHA classification, significant left ventricular myocardial hypertrophy (≥1.4 cm), postinfarction cardiosclerosis, severe liver function and/or renal impairment, age under 18 years (effectiveness and safety are not established), lactase deficiency, lactose intolerance, glucose-galactose malabsorption (the drug contains lactose), Brugada syndrome.

. Use with caution in degree I atrioventricular block, intraventricular conduction disorders, sinus node weakness syndrome (SSNS), bradycardia, marked disorders of peripheral circulation, closed-angle glaucoma, Benign prostatic hypertrophy, Purkinje fibers conduction disorders, blockade of one of the pedicles of Gis bundle, electrolyte and water metabolism disorders (hypokalemia, hyperkalemia, hypomagnesemia), concomitant use of other antiarrhythmic drugs.

Side effects

According to the World Health Organization adverse effects are classified according to their frequency of development as follows: very frequently (≥10% of appointments); frequently (≥1% and <10%); infrequently (≥0.1% and <1%); rarely (≥0.01% and <0.1%); very rarely (<0.01%); frequency is unknown (there are not enough 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, skin itching).

Visual disorders: Very common: diplopia.

Cardiac disorders:

• very frequently: disorders of intraventricular and AV conduction.
• Frequent: sinus tachycardia (with prolonged use), increased blood pressure (BP).
• Infrequent: arrhythmogenic effects.

Laboratory and instrumental data: Very common: ECG changes: prolongation of PQ interval, dilation of QRS complex.

If you have side effects mentioned in the instructions or they are aggravated, or if you notice any other side effects not specified in the instructions, tell your doctor.

Overdose

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

Symptoms: prolongation of PR and QT intervals, QRS complex expansion, increased amplitude of T waves, bradycardia, sinoatrial and AV blocks, asystole, paroxysms of polymorphic ventricular tachycardia, decreased myocardial contractility, marked decrease of blood pressure, dizziness, blurred vision, headache, gastrointestinal disturbances.

Treatment: symptomatic; gastric lavage, defibrillation, administration of dobutamine, diazepam; if necessary – artificial lung ventilation and indirect heart massage; for the treatment of ventricular tachycardia do not use antiarrhythmic drugs IA and IC class; sodium hydrogen carbonate (IV drip) can eliminate QRS complex dilation, bradycardia and hypotension.

Pregnancy use

The use of the drug in pregnancy is not recommended due to the lack of controlled studies.

Animal studies have shown that lappaconitine hydrobromide at doses of 1-5 mg/kg has no teratogenic and embryotoxic effects. The effect on fertility has not been studied.

The drug may be used only for vital indications, if the estimated benefit to the mother exceeds the potential risk of side effects in the fetus/fetus.

No data on excretion of lappaconitine hydrobromide into the breast milk. Administration of the drug is not recommended during breastfeeding.

If the use of the drug Laporitmin® during lactation is necessary, breastfeeding should be stopped.

Similarities

Allapinin, Allaforte