Lappaconitine hydrobromide
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Clinical Pharmacology
Allapinin - class I antiarrhythmic drug. Lappaconitin is an alkaloid obtained from the wild-growing perennial aconite plant of the white-tinted family of buttercups.
Allapinin (lappaconitine) has a membrane stabilizing effect, blocking the “fast” sodium channels of cardiomyocyte membranes.
Allapinin causes slowing of atrioventricular and intraventricular conduction, shortens the effective and functional refractory periods in the atria and ventricles. It has a moderate spasmolytic, coronary dilating, anticholinergic and sedative effects. Bioavailability is 39% - undergoes intensive presystemic biotransformation. With the on / in the introduction and ingestion of the half-life - 1-1,2h. Gets through the BBB. One of the three major metabolites lowers blood pressure. When ingested, the effect develops in 40-60 minutes, reaches a maximum in 4-5 hours and lasts 8 hours or more. Under the conditions of intravenous injection, the antiarrhythmic effect is manifested after 15-20 minutes and lasts 6-8 hours (with a maximum after 2 hours). Elongation of the half-life was observed with prolonged use, renal failure (2-3 times), liver cirrhosis (3-10 times).
Indications
Supraventricular and ventricular premature beats, paroxysms of atrial fibrillation and flutter, paroxysmal supraventricular tachycardia (including Wolff-Parkinson-White syndrome (WPW), paroxysmal ventricular tachycardia, arrhythmia against myocardial infarction
Composition
1 tablet contains lappaconitine hydrobromide 25 mg.
Lappaconitine hydrobromide is marketed under different brands and generic names, and comes in different dosage forms:
Brand name | Manufacturer | Country | Dosage form |
---|---|---|---|
Allapinin | Pharmacentre VILAR ZAO | Russia | pills |
pills |
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Dosage and Administration
Orally, drinking warm water (pills must be crushed), 30 minutes before meals. First, appoint 0,025 g every 8 hours; in the absence of effect - 0,025 g every 6 hours. It is possible to further increase the dose to 0.05 g per reception every 6-8 hours. The course depends on the condition of the patient and the nature of the rhythm disturbance and the treatment can last up to several months. The highest single dose - 0.15 g, daily - 0.3 g
Adverse reactions
Dizziness, headache, dizziness, facial flushing, diplopia, ataxia, electrocardiographic changes, allergic reactions. With prolonged use may cause sinus tachycardia.
Contraindications
Hypersensitivity, atrioventricular block (AV) II and higher degrees; severe hepatic and renal failure; pregnancy (prescribed for health reasons only)
Drug interactions
Enhances the effect of non-depolarizing muscle relaxants.
Special instructions
If you have a headache, dizziness, diplopia, reduce the dose. Repeated parenteral administration is allowed only after 6 hours. When sinus tachycardia appears on the background of long-term administration, beta-adrenergic blockers are shown (small doses). Appointment to patients with AV block I degree, sick sinus syndrome and severe heart failure is possible only in a hospital with medical observation and ECG monitoring. With care (mainly for health reasons) prescribed in the first 3 months of pregnancy.
Overdosage
Symptoms: the drug has a small breadth of therapeutic action, so severe intoxication can easily occur (especially with the simultaneous use of other antiarrhythmic drugs): prolongation of the PR and QT intervals, expansion of the QRS complex, increase in the amplitude of the T wave, bradycardia, sinoatrial blockade, AV blockade, asystolia , paroxysms of polymorphic ventricular tachycardia, reduction in myocardial contractility, pronounced decrease in blood pressure, dizziness, blurred vision, headache, gastrointestinal disorders.
Treatment: conduct symptomatic therapy. For the treatment of ventricular tachycardia, you should not use class I A and I C antiarrhythmic drugs. Sodium bicarbonate can eliminate the expansion of the QRS complex, bradycardia and arterial hypotension.
- Brand name: Allapinin
- Active ingredient: Lappaconitine hydrobromide
- Dosage form: Pills.
- Manufacturer: Pharmacentre VILAR ZAO
- Country of Origin: Russia
Studies and clinical trials of Lappaconitine hydrobromide (Click to expand)