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Lappaconitine Hydrobromide

$43

  • Brand : BIOFRON

  • Catalogue Number : BF-L2004

  • Specification : 98%

  • CAS number : 97792-45-5

  • Formula : C32H44N2O8.HBr

  • Molecular Weight : 665.61

  • PUBCHEM ID : 51346120

  • Volume : 20mg

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Quantity
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Catalogue Number

BF-L2004

Analysis Method

HPLC,NMR,MS

Specification

98%

Storage

2-8°C

Molecular Weight

665.61

Appearance

White crystalline powder

Botanical Source

Aconitum

Structure Type

Alkaloids

Category

Standards;Natural Pytochemical;API

SMILES

CCN1CC2(CCC(C34C2CC(C31)C5(CC(C6CC4C5(C6OC)O)OC)O)OC)OC(=O)C7=CC=CC=C7NC(=O)C.Br

Synonyms

Benzoic acid, 2-(acetylamino)-, (1α,14α,16β)-20-ethyl-8,9-dihydroxy-1,14,16-trimethoxyaconitan-4-yl ester, hydrobromide (1:1)/(1α,14α,16β)-20-Ethyl-8,9-dihydroxy-1,14,16-trimethoxyaconitan-4-yl 2-acetamidobenzoate hydrobromide (1:1)/(1a,14a,16b)-20-Ethyl-1,14,16-trimethyoxyaconitane-4,8,9-triol 4-(2-(Acetylamino)benzoate) Monohydrobromide/lappaconitine hydrobromide/(1α,14α,16β)-20-ethyl-8,9-dihydroxy-1,14,16-trimethoxyaconitan-4-yl 2-(acetylamino)benzoate hydrobromide (1:1)

IUPAC Name

[(1S,2S,3S,4S,5R,6S,8S,9S,13S,16S,17S)-11-ethyl-3,8-dihydroxy-4,6,16-trimethoxy-11-azahexacyclo[7.7.2.12,5.01,10.03,8.013,17]nonadecan-13-yl] 2-acetamidobenzoate;hydrobromide

Density

Solubility

Flash Point

401.8ºC

Boiling Point

740.8ºC at 760 mmHg

Melting Point

223-226ºC

InChl

InChl Key

WGK Germany

RID/ADR

HS Code Reference

2939800000

Personal Projective Equipment

Correct Usage

For Reference Standard and R&D, Not for Human Use Directly.

Meta Tag

provides coniferyl ferulate(CAS#:97792-45-5) MSDS, density, melting point, boiling point, structure, formula, molecular weight etc. Articles of coniferyl ferulate are included as well.>> amp version: coniferyl ferulate

PMID

28294889

Abstract

Lappaconitine Hydrobromide (LH, allapinin) has been included by authors of National Guidelines on Diagnosis and Treatment of Atrial Fibrillation (AF), 2012 in the number of medications recommended for use in patients with AF for rhythm control. Moreover, LH is also included into the List of Vital and Essential Medicinal Drugs (VEMD) 2015. However, LH is not mentioned in corresponding guidelines of the European Society of Cardiology (ESC). Aim of the present review was to explore evidence base underlining use of LH in the context of AF and to understand reason for LH-related discrepancy between European and domestic guidelines.

RESULTS:
Literature search has indicated that efficacy of LH was assessed only in small open studies. None of prospective trials included more than 100 patients. For more than 25 years of presence on the market slightly more than 400 patients were administered LH in clinical studies. In the only trial, designated as randomized number of participants (only men younger than 60 years) was small and the comparator was quinidine that presently is not used for maintenance of sinus rhythm in AF. Another study referenced in domestic guidelines on management of AF was observational and not intended for comparison of antiarrhythmic activity of drugs.

CONCLUSION:
Design of studies reviewed as well as their results provide insufficient evidence supporting the use of LH for maintenance of sinus rhythm in routine management of AF. At present inclusion of LH in guidelines on AF management and in the List of VEMD appears unjustified

Title

[The Study of Evidence Base for the Use of Lappaconitine Hydrobromide in Patients With Atrial Fibrillation].

Author

Erlikh AD1.

Publish date

2016 Mar

PMID

25702400

Abstract

OBJECTIVE:
To assess and compare the safety and efficacy of allapinine and quinidine bisulphate in the treatment of patients with persistent atrial fibrillation after cardioversion. Design–Prospective, randomised, open study. Patients–73 consecutive patients (men only, mean age 44 ± 11 years) with persisnent atrial fibrillation and flutter. Interventions–37 patients were randomised to allapinine (ALP) (1.5 mg/kg/d), 36 to quinidine bisulphate (QUIN) (15 mg/kg/d) with subsequent successful pharmacological or electrical cardioversion. Main outcome measures–Recurrence of atrial fibrillation or side effects.

RESULTS:
In the ALP group 15 of the 37 patients developed atrial fibrillation up to 12 month of follow-up, while in the QUIN group 20 patients developed atrial fibrillation and 5 experienced significant side effects. Relative risk (RR) (ALP vs QUIN) 0.58 (95% CI 0.37-0.91, p < 0.02). The number needed to treat (NNT) was (-3.48) (14.2-1.97 harm). When 5 patients with significant side effects were excluded from the analysis RR was 0.62 (95% CI 0.39-1.0, p = 0.052) and NNT–(-4.1) (122.7-2.1 harm) but power of the study was too low–67%.

CONCLUSION:
Allapinine is as effective as quinidine bisulphate in the long term treatment of patients with persistent atrial fibrillation after successful cardioversion but causes significantly less side effects.

Title

[Efficacy and safety of allapinine and quinidine bisulphate in the treatment of patients with persistent atrial fibrillation after cardioversion].

Author

Rakhmanova MM, Sokolov SF.

Publish date

2014

PMID

24881307

Abstract

Allapinin, class 1C antiarrhythmic drug, is highly effective in treatment of patients with ventricular premature beats (VPB). The purpose of work was retrospective assessment of efficacy and safety of allapinin in patients with benign ventricular arrhythmias. 73 patients with VPB and no structural heart disease were selected from a database. In short course allapininin in dose of 75-150 mg per os daily decreased the number of VPB for more than 90% in 46,6% of patients. In 34,4% cases tolerable drug side effects were observed. Among patients with VPB burden of 10% and higher allapinin reduced this quantity below the indicated value in 76% of cases with tolerable drug side effects in 38,6% of cases. In long treatment study antiarrhythmic effect of allapinin persisted and no other side effects of the drug were documented.

CONCLUSION:
Allapinin is highly effective in treatment of patients with VPB without structural heart disease

Title

[Efficiency and safety of allapinin in short- and long-term treatment of patients with normal heart and ventricular premature beats].

Author

Sokolov SF, Bakalov SA, Mironova NA, Rogova MM, Malkina TA, Golitsyn SP.

Publish date

2014


Description :

Lappaconitine hydrobromide, a diterpene alkaloid, is a drug for the treatment of cardiac arrhythmias.IC50 value:Target: A natural product for anti-cardiac arrhythmiasIn vitro: Lappaconitine hydrobromide was found to exert an inhibitory effect on inward tetrodotoxin-sensitive sodium currents without changing their voltage dependence [1]. In vivo: The effect of Lappaconitine hydrobromide on aconitine--induced arrhythmias is due to modulation of genes encoding Na(+)-, K(+)-, Ca(2+)-channels, conducting ionic currents (I(Na), I(to), I(Ks), I(K1), I(CaT)), which are involved in the formation of different phases of the action potential [2]. Lappaconitine hydrobromide was found to be beneficial both in ventricular and supraventricular premature beats. Oral allapinine usually showed its effect 40-60 minutes following its administration, its maximum action being 4-5 hours later, its duration was some 8 hours. The optimal dose of the drug amounted to 75 mg/day [3].