Loew D, Schuster O, Knoell H E, Graul E H
Z Rheumatol. 1985 Jul-Aug;44(4):186-92.
The difference between mofebutazone and phenylbutazone is shown by means of toxicological, pharmacological and pharmacokinetic studies as well as by the protein binding. In spite of a certain chemical similarity both substances differ distinctly. Mofebutazone is approx. 5-6 times less toxic than phenylbutazone but its analgesic and antiphlogistic effects are weaker than those of phenylbutazone. The half life time of mofebutazone of 1.9 h is considerably shorter than that of phenylbutazone (54-99 h). Mofebutazone, in contrast to phenylbutazone, is mainly glucuronidised and to 94% eliminated within 24 h, phenylbutazone on the other hand to only 88% within 21 days. In spite of a high plasma protein binding quota of 99%, mofebutazone is classed among those substances with a medium binding potential. Conclusions may only be drawn with great reservation with regard to a category of substances from the effect and side effects of one substance on the basis of the present studies.
通过毒理学、药理学、药代动力学研究以及蛋白结合情况,展示了莫比布宗与保泰松之间的差异。尽管二者在化学结构上有一定相似性,但这两种物质明显不同。莫比布宗的毒性约比保泰松低5至6倍,但其镇痛和抗炎作用比保泰松弱。莫比布宗的半衰期为1.9小时,明显短于保泰松(54 - 99小时)。与保泰松不同,莫比布宗主要经葡萄糖醛酸化代谢,24小时内94%被清除,而保泰松在21天内仅88%被清除。尽管莫比布宗的血浆蛋白结合率高达99%,但它仍被归类为具有中等结合潜力的物质。基于目前的研究,仅能极为谨慎地根据一种物质的作用和副作用对一类物质下结论。