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磺吡酮的作用机制。

Mechanisms of action of sulphinpyrazone.

作者信息

Wallis R B

出版信息

Thromb Res Suppl. 1983;4:31-8. doi: 10.1016/0049-3848(83)90355-9.

DOI:10.1016/0049-3848(83)90355-9
PMID:6415857
Abstract

Sulphinpyrazone normalises the shortened platelet survival associated with gout or artificial heart valves and has shown benefit in secondary prevention of myocardial infarction. The compound is metabolised in all species but in variable amounts to a sulphide metabolite which is a potent cyclo-oxygenase inhibitor. At the plasma concentration found in man, the metabolic inhibits prostaglandin synthesis-dependent platelet behaviour and this is therefore the likely mechanism of action of sulphinpyrazone. The compound has some additional effects which may be important.

摘要

磺吡酮可使与痛风或人工心脏瓣膜相关的缩短的血小板生存期恢复正常,并已显示出对心肌梗死二级预防有益。该化合物在所有物种中均会代谢,但代谢量各不相同,会生成一种硫化物代谢产物,它是一种强效环氧化酶抑制剂。在人体中发现的血浆浓度下,这种代谢产物会抑制依赖前列腺素合成的血小板行为,因此这可能是磺吡酮的作用机制。该化合物还有一些其他可能很重要的作用。

相似文献

1
Mechanisms of action of sulphinpyrazone.磺吡酮的作用机制。
Thromb Res Suppl. 1983;4:31-8. doi: 10.1016/0049-3848(83)90355-9.
2
Inhibition of human platelet cyclo-oxygenase activity by sulfinpyrazone and three of its metabolites.磺吡酮及其三种代谢产物对人血小板环氧化酶活性的抑制作用。
Eur J Pharmacol. 1984 Jun 1;101(3-4):209-14. doi: 10.1016/0014-2999(84)90158-4.
3
Differential inhibition of platelet thromboxane and lung prostacyclin production by sulphinpyrazone, acetylsalicylic acid and indomethacin by human tissues in vitro.在体外人组织中,磺吡酮、乙酰水杨酸和吲哚美辛对血小板血栓素和肺前列环素生成的差异抑制作用。
Thromb Res. 1985 Feb 15;37(4):493-502. doi: 10.1016/0049-3848(85)90095-7.
4
The effect of prolonged treatment with sulphinpyrazone on thromboxane A2 and prostacyclin in man.磺吡酮长期治疗对人体血栓素A2和前列环素的影响。
Br J Clin Pharmacol. 1982 Sep;14(3):456-8. doi: 10.1111/j.1365-2125.1982.tb02009.x.
5
The effect of sulphinpyrazone and its metabolites on platelet function in vitro and ex vivo.磺吡酮及其代谢产物对体外和体内血小板功能的影响。
Haemostasis. 1981;10(3):165-75. doi: 10.1159/000214400.
6
Sulphinpyrazone prevents in vivo the inhibitory effect of aspirin on rat platelet cyclo-oxygenase activity.
Biochem Pharmacol. 1981 Oct;30(20):2773-6. doi: 10.1016/0006-2952(81)90414-7.
7
Cyclooxygenase inhibition, platelet function, and metabolite formation during chronic sulfinpyrazone dosing.慢性服用苯磺唑酮期间的环氧化酶抑制、血小板功能及代谢物形成
Clin Pharmacol Ther. 1985 Jan;37(1):36-42. doi: 10.1038/clpt.1985.8.
8
Prostaglandin endoperoxides and thromboxane A2 in thrombus formation in the hamster cheek pouch in vivo.前列腺素内过氧化物和血栓素A2在仓鼠颊囊体内血栓形成中的作用
Prostaglandins. 1984 Jul;28(1):29-41. doi: 10.1016/0090-6980(84)90111-4.
9
Inhibition by sulphinpyrazone of the platelet-dependent bronchoconstriction due to platelet-activating factor (PAF-acether) in the guinea pig.在豚鼠中,磺吡酮对血小板活化因子(PAF-乙酰醚)所致的血小板依赖性支气管收缩的抑制作用。
Eur J Pharmacol. 1982 Feb 19;78(1):71-9. doi: 10.1016/0014-2999(82)90373-9.
10
Effects of platelet-modifying drugs on arterial thromboembolism in baboons. Aspirin potentiates the antithrombotic actions of dipyridamole and sulfinpyrazone by mechanism(s) independent of platelet cyclooxygenase inhibition.血小板修饰药物对狒狒动脉血栓栓塞的影响。阿司匹林通过独立于血小板环氧化酶抑制作用的机制增强双嘧达莫和磺吡酮的抗血栓形成作用。
J Clin Invest. 1985 May;75(5):1591-9. doi: 10.1172/JCI111865.

引用本文的文献

1
A benefit-risk assessment of benzbromarone in the treatment of gout. Was its withdrawal from the market in the best interest of patients?苯溴马隆治疗痛风的获益-风险评估。其退市符合患者的最大利益吗?
Drug Saf. 2008;31(8):643-65. doi: 10.2165/00002018-200831080-00002.
2
Determination of sulfinpyrazone and four metabolites in plasma and urine by high pressure liquid chromatography.
Pharm Weekbl Sci. 1985 Dec 13;7(6):252-9. doi: 10.1007/BF01959198.
3
Renal clearance of sulphinpyrazone in man.磺胺吡唑酮在人体中的肾脏清除率。
Eur J Clin Pharmacol. 1986;31(4):473-8. doi: 10.1007/BF00613527.
4
A serial study of platelet reactivity throughout the first six months after myocardial infarction: its modification by sulphinpyrazone.心肌梗死后前六个月血小板反应性的系列研究:磺吡酮对其的影响
Postgrad Med J. 1987 May;63(739):351-6. doi: 10.1136/pgmj.63.739.351.