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Application of tamoxifen in preparation of medicine for preventing and treating cardiac toxic and side effects caused by bupivacaine

A technology of tamoxifen, toxic and side effects, applied in the application field of medicine

Inactive Publication Date: 2016-07-06
诺莱生物医学研究院(北京)有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] 3) Recent studies suggest that the myocardial toxicity of bupivacaine may also be related to its inhibition of potassium and calcium channels
[0009] At present, there is no report showing that tamoxifen can prevent and treat cardiotoxic side effects caused by bupivacaine

Method used

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  • Application of tamoxifen in preparation of medicine for preventing and treating cardiac toxic and side effects caused by bupivacaine
  • Application of tamoxifen in preparation of medicine for preventing and treating cardiac toxic and side effects caused by bupivacaine
  • Application of tamoxifen in preparation of medicine for preventing and treating cardiac toxic and side effects caused by bupivacaine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Example 1 Tamoxifen can inhibit the prolongation of the action potential cycle of rat cardiomyocytes caused by bupivacaine

[0034] 1. Isolation of rat cardiomyocytes

[0035] SD rats were anesthetized by intraperitoneal injection of 25% urethane (1.0g / kg), and an appropriate amount of myocardial tissue to be tested was taken (the following operations were all carried out in an ultra-clean workbench except for water bath and centrifugation) and immediately placed in a pre-cooled D- Hank's solution, rinse 3 times. Cut the ventricular muscle to 1mm with ophthalmic scissors 3 Then add 10mL of 0.1% trypsin solution, bathe in water at 37°C for 8min, absorb the upper suspension and discard it. Then add 15 mL of 0.1% collagenase solution, stir in a 37°C water bath with a magnetic stirrer for 30-40 min, absorb the upper suspension, and place it in pre-cooled 10% DMEM to terminate the reaction. Add 15mL of 0.1% collagenase solution to the remaining precipitate, stir in a 37°C...

Embodiment 2

[0039]Example 2 Tamoxifen can inhibit the bradycardia in rats caused by bupivacaine

[0040] Preliminary experiment: After repeated tests, it was found that the first injection of 0.6-1.5mg / kg of bupivacaine could easily lead to slow heart rate, and some people died directly, so the first injection of bupivacaine at 1 mg / kg, and then another injection of 0.5mg / kg bupivacaine, observe the changes of heart rate and respiration of rats in each group. If most rats did not die on the spot, with the metabolism of bupivacaine, some rats recovered ECG. But if the heart rate is below 150 beats, it is generally difficult for the rat to recover by itself, and it is difficult to rescue, and it will die soon. After thoracotomy, it is found that the atrioventricular is generally separated, and the heart beat is weak and mostly localized.

[0041] After the pre-experiment, 60 Spague-Dawlay (SD) rats were taken, half male and half male, weighing 180±20 g. Immediately divided into 6 groups,...

Embodiment 3

[0046] Example 3 Tamoxifen can prevent and reverse arrhythmia and ventricular fibrillation caused by bupivacaine

[0047] Ten 5-year-old adult rhesus male monkeys were randomly divided into two groups, one as the control group and the other as the experimental group, under general anesthesia with 1.5 mL of ketamine.

[0048] Control group: rhesus monkeys supine ECG limb lead II lead to measure P0 heart rate ( Figure 4 ). The monkey's right internal jugular vein was dissected, and a 22G intravenous catheter (BD) was inserted into ( Figure 5 ). Slowly retreat into the bupivacaine to observe the heart rate changes. When the heart rate changes significantly, the drug is stopped. At 172 beats / min, the whole body of the monkey convulses. After the rescue, the monkey is given epinephrine and 2 mg of dexamethasone, and the symptoms are relieved. According to the electrocardiogram variation trend, the heart rate variation ( Figure 6 ).

[0049] Experimental group: Rhesus monkey...

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Abstract

The invention relates to the technical field of medicine, in particular to the application of tamoxifen in the preparation of medicines for preventing and treating cardiotoxic side effects caused by bupivacaine. The drug can effectively prevent and treat cardiac toxic side effects such as bradycardia, atrioventricular or intraventricular conduction block, and ventricular arrhythmia caused by bupivacaine.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to the application of tamoxifen in the preparation of medicines for preventing and treating cardiotoxic side effects caused by bupivacaine. Background technique [0002] Local anesthetics are a class of drugs that can reversibly block the generation and conduction of nerve impulses, and cause temporary and reversible sensory loss in the parts innervated by the nerves under conscious conditions. Bupivacaine, an amide local anesthetic, is widely used in clinical anesthesia and analgesia because of its strong anesthesia performance, long duration, separation of sensory and motor block, and low price. It mainly acts on the nerve cell membrane, by inhibiting Na + channel, reduce the excitability of the cell membrane, inhibit the conduction of excitation, and produce local anesthetic effect. Although with the improvement of regional anesthesia techniques, the reports of severe poisonin...

Claims

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Application Information

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IPC IPC(8): A61K31/138A61K31/445A61P9/04A61P9/06A61P9/00
CPCA61K31/138A61K31/445
Inventor 顾宇春
Owner 诺莱生物医学研究院(北京)有限公司
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