Graffner C, Conradson T B, Hofvendahl S, Rydén L
Clin Pharmacol Ther. 1980 Jan;27(1):64-71. doi: 10.1038/clpt.1980.10.
Tocainide is structurally related to lidocaine but may be used orally as well as intravenously. A therapeutic plasma concentration range of 25 to 45 mumole/l has been suggested. Tocainide kinetics were studied in 6 healthy subjects and 16 patients with acute myocardial infarction. There was good accordance in kinetics of healthy subjects and patients. After intravenous administration the mean t1/2 was about 14 hr, volume of distribution about 3.0 l/kg, and corrected renal clearance about 140 ml/min. An average of 35% of the dose was recovered unchanged in urine. After oral administration the absorption rate was rapid relative to the elimination rate, extent of bioavailability was complete, and the apparent volume of distribution was the same as that after intravenous injection. A dose regimen of 750 mg intravenously directly followed by 800 mg orally and subsequently 400 mg 3 times daily resulted in therapeutic plasma levels within 15 min. The plasma levels remained within the therapeutic range throughout a period of observation from 48 to 168 hr.
妥卡尼在结构上与利多卡因相关，但可口服及静脉给药。建议治疗性血浆浓度范围为25至45微摩尔/升。对6名健康受试者和16名急性心肌梗死患者的妥卡尼动力学进行了研究。健康受试者和患者的动力学情况吻合良好。静脉给药后，平均半衰期约为14小时，分布容积约为3.0升/千克，校正肾清除率约为140毫升/分钟。平均35%的剂量以原形从尿中回收。口服给药后，相对于消除速率吸收迅速，生物利用度完全，且表观分布容积与静脉注射后相同。静脉直接注射750毫克，随后口服800毫克，接着每日3次每次400毫克的给药方案可在15分钟内达到治疗性血浆水平。在48至168小时的观察期内，血浆水平一直维持在治疗范围内。
