药品详细
Tocainide(卡尼)
化学结构式图
中文名
卡尼
英文名
Tocainide
分子式
C11H16N2O
化学名
2-amino-N-(2,6-dimethylphenyl)propanamide
分子量
Average: 192.2575
Monoisotopic: 192.126263144
Monoisotopic: 192.126263144
CAS号
41708-72-9
ATC分类
C01B 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍
An antiarrhythmic agent which exerts a potential- and frequency-dependent block of sodium channels. [PubChem]
生产厂家
- Astrazeneca pharmaceuticals lp
封装厂家
参考
| Synthesis Reference | Not Available |
| General Reference | Not Available |
剂型
规格
化合物类型
| Type | small molecule |
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适应症
药理
| Indication | For the treatment of documented ventricular arrhythmias, such as sustained ventricular tachycardia, that, in the judgment of the physician, are life-threatening. | ||||||
| Pharmacodynamics | Tocainide is a primary amine analog of lidocaine with antiarrhythmic properties useful in the treatment of ventricular arrhythmias. Tocainide, like lidocaine, produces dose dependent decreases in sodium and potassium conductance, thereby decreasing the excitability of myocardial cells. In experimental animal models, the dose-related depression of sodium current is more pronounced in ischemic tissue than in normal tissue. Tocainide is a Class I antiarrhythmic compound with electrophysiologic properties in man similar to those of lidocaine, but dissimilar from quinidine, procainamide, and disopyramide. | ||||||
| Mechanism of action | Tocainide acts on sodium channels on the neuronal cell membrane, limiting the spread of seizure activity and reducing seizure propagation. Tocainide binds preferentially to the inactive state of the sodium channels.The antiarrhythmic actions are mediated through effects on sodium channels in Purkinje fibers. | ||||||
| Absorption | Following oral administration, the bioavailability approaches 100 percent, and is unaffected by food. | ||||||
| Volume of distribution | Not Available | ||||||
| Protein binding | Approximately 10 percent bound to plasma protein. | ||||||
| Metabolism |
Negligible first pass hepatic degradation. No active metabolites have been found.
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| Route of elimination | Not Available | ||||||
| Half life | The average plasma half-life in patients is approximately 15 hours. May be prolonged up to 35 hours in patients with severe renal function impairment (creatinine clearance less than 30 mL per min per 1.73 square meters of body surface area. | ||||||
| Clearance | Not Available | ||||||
| Toxicity | The oral LD50 of tocainide was calculated to be about 800 mg/kg in mice, 1000 mg/kg in rats, and 230 mg/kg in guinea pigs; deaths were usually preceded by convulsions. | ||||||
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理化性质
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| State | solid | ||||||||||||||||||||||||||||||||||||||||||
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药物相互作用
| Drug | Interaction |
|---|---|
| Rifampin | Rifampin lowers tocainide levels/effects |
| Terfenadine | Increased risk of cardiotoxicity and arrhythmias |
食物相互作用
Not Available
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