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磺吡酮:其药理特性与治疗用途综述

Sulfinpyrazone: a review of its pharmacological properties and therapeutic use.

作者信息

Margulies E H, White A M, Sherry S

出版信息

Drugs. 1980 Sep;20(3):179-97. doi: 10.2165/00003495-198020030-00002.

DOI:10.2165/00003495-198020030-00002
PMID:7000488
Abstract

Sulfinpyrazone1 has long been recognised as a potent uricosuric agent, but has more recently been studied extensively as a platelet inhibitor and antithrombotic agent. It is active in man following oral administration and has been reported to be effective in reducing the incidence of transient ischaemic attacks, thromboembolism associated with vascular and cardiac prostheses, recurrent venous thrombosis, arteriovenous shunt thrombosis and sudden cardiac death following myocardial infarcton. Sulfinpyrazone has not been demonstrated to be effective in preventing or reducing the risk of stroke or death in patients with cerebrovascular disease with a recent history of cerebral or retinal ischaemioc attacks. The normal total dose of sulfinpyrazone as an antithrombotic agent is 800mg daily. The drug has been used continuously for up to 4 years with no serious adverse reactions or laboratory abnormalities. There has been no apparent diminution of effect with time. Sulfinpyrazone is not a substitute for conventional anticoagulant agents (e.g. the coumarin derivatives) in the treatment of venous thrombosis, but is an important drug for the treatment of conditions associated with arterial thrombosis and possibly for the prophylaxis of recurrent venous thrombosis.

摘要

磺吡酮长期以来一直被认为是一种有效的促尿酸尿剂,但最近作为血小板抑制剂和抗血栓形成剂得到了广泛研究。口服给药后在人体中具有活性,据报道可有效降低短暂性脑缺血发作、与血管和心脏假体相关的血栓栓塞、复发性静脉血栓形成、动静脉分流血栓形成以及心肌梗死后心源性猝死的发生率。尚未证明磺吡酮对近期有脑或视网膜缺血性发作病史的脑血管疾病患者预防或降低中风或死亡风险有效。作为抗血栓形成剂,磺吡酮的正常总剂量为每日800毫克。该药物已连续使用长达4年,未出现严重不良反应或实验室异常。随着时间的推移,效果没有明显减弱。在治疗静脉血栓形成方面,磺吡酮不是传统抗凝剂(如香豆素衍生物)的替代品,但它是治疗与动脉血栓形成相关病症以及可能预防复发性静脉血栓形成的重要药物。

相似文献

1
Sulfinpyrazone: a review of its pharmacological properties and therapeutic use.磺吡酮:其药理特性与治疗用途综述
Drugs. 1980 Sep;20(3):179-97. doi: 10.2165/00003495-198020030-00002.
2
Platelet inhibition in the management of thrombosis.血小板抑制在血栓形成管理中的应用
Thromb Diath Haemorrh. 1974 Sep 30;32(1):21-34.
3
Antithrombotic effects of drugs which suppress platelet function: their potential in prevention growth of tumour cells.
Prog Clin Biol Res. 1982;89:31-62.
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Antiplatelet drugs or dicoumarol: what is the most effective prophylaxis in occlusive arterial disease?抗血小板药物还是双香豆素:哪种是闭塞性动脉疾病最有效的预防措施?
Int Angiol. 1986 Jul-Sep;5(3):169-80.
5
[Action mechanism and clinical indications for thrombocyte aggregation inhibitors].[血小板聚集抑制剂的作用机制及临床适应证]
Schweiz Med Wochenschr. 1979 Mar 10;109(10):348-53.
6
Antiplatelet drugs in thromboembolism.
Postgrad Med. 1979 Sep;66(3):119-23, 126-7. doi: 10.1080/00325481.1979.11715250.
7
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.
8
Aspirin and other platelet-aggregation inhibiting drugs.阿司匹林及其他血小板聚集抑制药物。
Med J Aust. 1985 Jan 7;142(1):41-7.
9
Platelet function inhibitors: their clinical use.
Adv Intern Med. 1978;23:251-64.
10
[Antiplatelet drugs (author's transl)].
Anesth Analg (Paris). 1979;36(7-8):283-7.

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The effect of sulphinpyrazone on oxidative drug metabolism in man: inhibition of tolbutamide elimination.磺吡酮对人体氧化药物代谢的影响:对甲苯磺丁脲消除的抑制作用。
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本文引用的文献

1
THE EFFECT OF SULFINPYRAZONE (ANTURAN) ON PLATELET ECONOMY AND BLOOD COAGULATION IN MAN.磺吡酮(安妥明)对人体血小板代谢及血液凝固的影响
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2
A STUDY OF STRUCTURE--ACTIVITY RELATIONSHIPS IN REGARD TO SPECIES DIFFERENCE IN THE PHENYLBUTAZONE SERIES.关于保泰松系列物种差异的结构-活性关系研究。
Biochem Pharmacol. 1964 Sep;13:1305-17. doi: 10.1016/0006-2952(64)90231-x.
3
Experimental platelet embolism.实验性血小板栓塞
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Clinical pharmacokinetics and potentially important drug interactions of sulphinpyrazone.磺吡酮的临床药代动力学及潜在的重要药物相互作用
Clin Pharmacokinet. 1982 Jan-Feb;7(1):42-56. doi: 10.2165/00003088-198207010-00003.
5
Plasma levels of sulfinpyrazone and of two of its metabolites after a single dose and during the steady state.单次给药后及稳态期间苯磺唑酮及其两种代谢物的血浆水平。
Eur J Clin Pharmacol. 1983;24(2):231-5. doi: 10.1007/BF00613823.
6
Effects of chronic metoprolol and sulphinpyrazone on human lymphocyte beta-adrenoceptors.慢性服用美托洛尔和磺吡酮对人淋巴细胞β-肾上腺素能受体的影响。
Br J Clin Pharmacol. 1984 Jul;18(1):45-50. doi: 10.1111/j.1365-2125.1984.tb05020.x.
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Sulphinpyrazone increases lymphocyte beta-adrenoceptors in man.磺吡酮可增加人体淋巴细胞的β-肾上腺素能受体。
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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.
9
Current issues in thrombosis prevention with antiplatelet drugs.抗血小板药物预防血栓形成的当前问题。
Drugs. 1986 Jun;31(6):517-49. doi: 10.2165/00003495-198631060-00004.
Br J Exp Pathol. 1962 Aug;43(4):350-62.
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An evaluation of factors which influence the incidence and extent of venous thrombosis.对影响静脉血栓形成发生率及范围的因素的评估。
Surgery. 1962 Mar;51:347-50.
5
A study of the inverse relationship between pKa and rate of renal excretion of phenylbutazone analogs in man and dog.关于人及犬体内苯丁唑酮类似物的pKa与肾排泄速率之间反比关系的研究。
Am J Med. 1960 Dec;29:1017-33. doi: 10.1016/0002-9343(60)90082-6.
6
A potent new uricosuric agent, the sulfoxide metabolite of the phenylbutazone analogue, G-25671.一种强效的新型促尿酸排泄剂,即保泰松类似物G-25671的亚砜代谢产物。
J Pharmacol Exp Ther. 1957 Mar;119(3):418-26.
7
White thrombo-embolism and vascular fragility in the hamster cheek pouch after anticoagulants.抗凝剂作用后仓鼠颊囊内的白色血栓栓塞与血管脆性
Blood. 1953 Feb;8(2):140-52.
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The effects of two different dosage regimens of sulphinpyrazone on platelet function ex vivo and blood chemistry in man.
Haemostasis. 1981;10(3):153-64. doi: 10.1159/000214399.
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A randomized, controlled trial of aspirin in persons recovered from myocardial infarction.一项针对心肌梗死康复者使用阿司匹林的随机对照试验。
JAMA. 1980 Feb 15;243(7):661-9.
10
Sulfinpyrazone in the prevention of sudden death after myocardial infarction.
N Engl J Med. 1980 Jan 31;302(5):250-6. doi: 10.1056/NEJM198001313020502.