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西德Grunenthal研制的曲马多(tramadol盐酸盐,CG315、Tvamal、简称T)。药理和镇痛机理以及临床应用介绍如下:曲马多分子量:299.8,熔点:182℃、易溶水、Pka值为8.3。给动物口服曲马多,从胃肠道吸收迅速而完全(90％以上)。绝对生物利用度约为65％,因具有高生物利用度,口服和注射的效果相差无几,为同类药物所仅见。口服曲马多100mg20～30min开始生效,2小时后血浓度达到峰值(280±49ng/ml,镇痛阈值为100ng/ml),维持作用时限约4～6小时t1/2约5小时,而吗啡约3小时。
Tramadol HCl (CG315, Tvamal, abbreviated as T) developed by Grunenthal in West Germany. Pharmacological and analgesic mechanisms and clinical applications are described below: Tramadol MW: 299.8, melting point: 182 ° C, water-soluble, Pka value of 8.3. To animals, oral tramadol, quickly and completely absorbed from the gastrointestinal tract (90%). The absolute bioavailability of about 65%, due to its high bioavailability, oral and injecting effect is almost the same for the same drugs only see. Oral tramadol 100mg20 ~ 30min to take effect, 2 hours after the peak blood concentration (280 ± 49ng / ml, analgesic threshold of 100ng / ml), the maintenance effect of about 4 ~ 6 hours t1 / 2 about 5 hours, and morphine About 3 hours.