Ibutilide Fumarate

A class III antiarrhythmic drug

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10mg

￥437.00

350.00

- +
100mg

￥1650.00

1320.00

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Background

Ibutilide fumarate is a Class III antiarrhythmic agent that is indicated for acute cardioconversion of atrial fibrillation and atrial flutter of a recent onset to sinus rhythm.Target: Calcium ChannelIbutilide fumarate is the first 'pure' class III antiarrhythmic drug to become available. Its predominant action is prolongation of the myocardial action potential duration. Intravenous ibutilide 0.01 to 0.025 mg/kg or 1 to 2 mg successfully converted atrial flutter or fibrillation to sinus rhythm in 33 to 49% of patients in 2 placebo-controlled trials involving 439 patients with sustained arrhythmia [1]. Ibutilide fumarate appears to be an effective alternative method for rapid conversion of recent-onset AF or AFl. The drug may be particularly useful in patients who have undergone recent cardiac surgery or those who are not ideal candidates for DCC [2].

参考文献:
[1]. Foster, R.H., M.I. Wilde, and A. Markham, Ibutilide. A review of its pharmacological properties and clinical potential in the acute management of atrial flutter and fibrillation. Drugs, 1997. 54(2): p. 312-30.
[2]. Howard, P.A., Ibutilide: an antiarrhythmic agent for the treatment of atrial fibrillation or flutter. Ann Pharmacother, 1999. 33(1): p. 38-47.

Protocol

Cell experiment [1]:
Cell lines	Neonatal rat cardiomyocytes
Preparation method	The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.
Reacting condition	10-8 to 10-3 mol/L for 4-12 h
Applications	Ibutilide protected against H2O2-induced cardiomyocytes injury through inhibiting endoplasmic reticulum and mitochondrial stress pathways.
Animal experiment [2]:
Animal models	Open-chest beagles model
Dosage form	10 μg/kg, intravenous administration, for 10 min; 0.1 mg/kg/h
Applications	Ibutilide significantly decreased defibrillation threshold through the reduction of activation pattern complexity during ventricular fibrillation in canine hearts.
Other notes	Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.
参考文献: 1. Wang, Y., Wang, Y. L., Huang, X., Yang, Y., Zhao, Y. J., Wei, C. X. and Zhao, M. (2016) Ibutilide protects against cardiomyocytes injury via inhibiting endoplasmic reticulum and mitochondrial stress pathways. Heart Vessels 2. Jin, Q., Zhou, J., Zhang, N., Lin, C. J., Pang, Y., Gu, G., Shen, W. F. and Wu, L. Q. (2012) Ibutilide decreases defibrillation threshold by the reduction of activation pattern complexity during ventricular fibrillation in canine hearts. Chin Med J (Engl). 125, 2701-2707