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[莫苯丁酮的药理学、毒理学及药代动力学]

[Pharmacology, toxicology and pharmacokinetics of mofebutazone].

作者信息

Loew D, Schuster O, Knoell H E, Graul E H

出版信息

Z Rheumatol. 1985 Jul-Aug;44(4):186-92.

PMID:4050150
Abstract

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.

摘要

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。

相似文献

1
[Pharmacology, toxicology and pharmacokinetics of mofebutazone].[莫苯丁酮的药理学、毒理学及药代动力学]
Z Rheumatol. 1985 Jul-Aug;44(4):186-92.
2
[Kinetics of mofebutazone in plasma and synovial fluid].[莫比丁在血浆和滑液中的动力学]
Z Rheumatol. 1984 Jul-Aug;43(4):179-81.
3
[Distribution of 4-14C-mofebutazone in the rat].[4-¹⁴C-莫比布宗在大鼠体内的分布]
Z Rheumatol. 1986 Mar-Apr;45(2):83-6.
4
Pharmacokinetics of [4-14C] mofebutazone after oral administration in man.[4-14C]莫比布宗口服给药后在人体的药代动力学。
Eur J Drug Metab Pharmacokinet. 1984 Jul-Sep;9(3):223-7. doi: 10.1007/BF03189645.
5
Influence of phenylbutazone, mofebutazone and aspirin on the pharmacokinetics of dexamethasone in the rat.保泰松、莫比可保泰松和阿司匹林对大鼠体内地塞米松药代动力学的影响。
Eur J Drug Metab Pharmacokinet. 1981;6(1):11-20. doi: 10.1007/BF03189511.
6
Influence of mofebutazone in comparison to phenylbutazone on the adenosine triphosphate level of polymorphonuclear cells and their migration.
Arzneimittelforschung. 1992 Nov;42(11):1336-8.
7
Disposition of [4-14C]mofebutazone in the rat.[4-¹⁴C]莫比布宗在大鼠体内的处置情况。
Eur J Drug Metab Pharmacokinet. 1980;5(4):201-6. doi: 10.1007/BF03189465.
8
Determination of mofebutazone and its 4-hydroxy metabolite in plasma and urine by high-performance liquid chromatography.采用高效液相色谱法测定血浆和尿液中莫苯丁酮及其4-羟基代谢物。
J Chromatogr. 1986 Nov 21;369(2):440-4. doi: 10.1016/s0021-9673(00)90155-9.
9
The interaction of mofebutazone with furosemide.莫苯唑酮与呋塞米的相互作用。
Curr Med Res Opin. 1987;10(9):638-44. doi: 10.1185/03007998709112418.
10
Structure of phenylbutazone and mofebutazone in the crystalline state and in solution.
J Pharm Sci. 1987 Dec;76(12):920-9. doi: 10.1002/jps.2600761217.