LAPPACONITINE HYDROBROMIDE
Lappaconitine hydrobromide is an alkaloid, obtained from a wild-growing perennial plant Aconitum leucostomum belonging to the family of Ranunculaceae.
Structural formula
Gross formula: C32H44N2O8·HBr
Purity: > = 95%
Chemical name: 4- (N-Acetylanthranoyloxy) -8,9-dihydroxy-1alpha, 14alpha, 16β-trimethoxy-N-ethyl-18-noracone hydrobromide
Molecular weight: 665.61 g / mol
Latin name: Lappaconitini hydrobromidum
CAS code:97792-45-5
Pharmacological group of substance
Pharmacological group of substance Lappaconitine hydrobromide: Antiarrhythmic agents.
Indications for use
• Supraventricular tachycardia
• Ventricular tachycardia
• Atrial fibrillation and flutter
• Premature depolarization of atria
• Premature depolarization of ventricles
Pharmacological properties:
Pharmacological action - antiarrhythmic. It has a membrane-stabilizing effect, it affects sodium channels, belongs to the class of IC antiarrhythmic drugs. It causes retardation of atrioventricular and intraventricular conduction, shortens the effective and functional refractory periods in the atria and ventricles, does not affect the duration of the QT interval, conduction in AV node in anterograde direction, heart rate and blood pressure, myocardial contractility (in the absence of heart insufficiency). It has mild antispasmodic, coronary-expanding, cholinolytic and sedative effects.
Bioavailability is 39% - is subjected to intensive pre-system biotransformation. With intravenous administration and ingestion of T1 / 2 - 1-1.2 hours, the volume of distribution - 42 and 690 liters, respectively. It penetrates through the BBB. One of the three major metabolites lowers blood pressure. When ingested, the effect develops in 40-60 minutes, reaches a maximum after 4-5 hours and lasts for 8 hours or more. In conditions of intravenous administration, the antiarrhythmic effect is manifested after 15-20 minutes and lasts for 6-8 hours (with a maximum after 2 hours). Elongation of T1 / 2 is observed with prolonged use, renal failure (2-3 times), cirrhosis (3-10 times).