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Use of Nifekalant

A technology of nifecaran, uses

Inactive Publication Date: 2009-04-22
SICHUAN BAILI PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, MS-551 can prolong the QT interval of the rat coronary artery ligation-reperfusion model, and reduce the incidence of persistent ventricular fibrillation after reperfusion, while the pure IKr antagonists Sematilide and Dofetilide have no such effect

Method used

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  • Use of Nifekalant
  • Use of Nifekalant

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] In this example, nifekalant is used to prepare the following freeze-dried powder injections for the treatment of supraventricular arrhythmias such as atrial fibrillation and atrial flutter: the freeze-dried powder contains 50% nifekalant and 50% manna alcohol.

Embodiment 2

[0022] This example studies the acute effects of intravenous nifekalant on the patient's threshold for persistent and paroxysmal atrial fibrillation:

[0023] A total of 45 patients with sudden persistent atrial fibrillation were selected, and the duration of the onset of atrial fibrillation was greater than 24 hours. After the onset of atrial fibrillation, other antiarrhythmic drugs and direct current cardioversion were ineffective. The average age of the patients was 61.9±10 years old (43-78 years old), and the average ejection fraction was 56.4±13.8%. Among them, 4 cases suffered from mitral valve stenosis and 3 cases suffered from coronary heart disease. All patients had a history of taking other antiarrhythmic drugs before. The average duration of AF episodes in patients was 46.8±8.2 hours (35.8-49.5 hours). All patients received intracardiac defibrillation via an intravenous lead, but it was ineffective (failure to convert to sinus rhythm or immediate recurrence). The...

Embodiment 3

[0030]This example studies the enhancing effect of class III antiarrhythmic drugs (nifekalant) on the electrical defibrillation of hemodynamically deteriorated atrial fibrillation and the effect of preventing recurrence.

[0031] From the 1896 patients who entered the ICU ward due to cardiovascular disease, 201 patients with new onset atrial fibrillation were screened out, and 24 patients who met the following conditions were further screened out (the average age of the patients was 70±12 years old, and the systolic blood pressure was less than 90mmhg, resistant to general electrical defibrillation, 21 patients had congestive heart failure, 11 patients were mechanically ventilated, 19 were male, 5 were female) entered the clinical study: all patients were in the ICU Sinus rhythm, atrial fibrillation with recent hemodynamic deterioration, systolic blood pressure less than 90mmHg, QT interval less than or equal to 0.46 seconds, QRS wave group time greater than or equal to 0.14 se...

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PUM

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Abstract

The invention discloses novel application of nifekalant to preparation of medicine for treating supraentricular arrhythmias. An intravenous medicated medicine is prepared from the medicine containing the nifekalant with clinical effective dose as the unique activating agent. At least one new application of the nifekalant is developed through preparing the nifekalant into medicines for treating atrial fibrillation, atrial flutter and other supraentricular arrhythmias, and the medicinal application range of the nifekalant is increased and more patients with atrial fibrillation, atrial flutter and other supraentricular arrhythmias can received better treatment. The medicine can reduce the recurernce rate of the supraentricular arrhythmias, and improve all vital signs, and surviving rate of the patients.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations and applications, and in particular relates to a new medical application of nifekalant. Background technique [0002] Nifekalant is a newly developed class III antiarrhythmic drug, its chemical name is: 6-[2-[N-(2-hydroxyethyl)-3-(4-nitrophenyl) Propylamino]ethylamino]-1,3-dimethyl-2,4(1H,3H)pyrimidinedione hydrochloride, the molecular formula is: C 19 h 27 N 5 o 5 HCl; the structural formula is as follows: [0003] [0004] Nifekalant is a simple potassium channel I kr Blocker, used to treat the symptoms of the following arrhythmias: ventricular tachycardia, ventricular fibrillation; it has a high inhibitory effect on severe ventricular arrhythmias. [0005] A normal heart rhythm originates from the sinoatrial node, with a frequency of 60 to 100 beats / min (adult), which is relatively regular. The sinoatrial node impulse excites the atrium and ventricle sequentially t...

Claims

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Application Information

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IPC IPC(8): A61K31/513A61P9/06
Inventor 朱义
Owner SICHUAN BAILI PHARM CO LTD
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