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十余年前合成的妥卡胺(室安卡因),是一种口服有效的抗心律失常药,作用时间长,治疗/中毒比值大。可治疗症状性室性心律失常。药理学妥卡胺系改变利多卡因侧链而成,能避免首次通过肝脏时发生的降解,故口服有效。口服后吸收良好,生物利用度接近100％。口服0.5～2h后达峰浓度。蛋白结合率约10％。治疗血浆浓度为4～10μg/ml。每日1200mg,分2～3次口服。约45％以原形由尿排泄,25％在肝内转化成葡萄糖醛酸化物。
More than ten years ago synthesis of metoclopramide (room Ankaine), is an orally available anti-arrhythmic drugs, the role of a long time, treatment / poisoning ratio. Symptomatic ventricular arrhythmias can be treated. Pharmacology Dowmannin changes the side chain of lidocaine, which can avoid the first degradation through the liver, so orally effective. After oral absorption, bioavailability close to 100%. Oral 0.5 ~ 2h after the peak concentration. Protein binding rate of about 10%. Treatment plasma concentration of 4 ~ 10μg / ml. Daily 1200mg, 2 to 3 times orally. About 45% is excreted in urine by the prototype, and 25% is converted to glucuronide in the liver.