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佐美酸对健康成年人止血及体外血小板功能的影响。

Effects of zomepirac on hemostasis in healthy adults and on platelet function in vitro.

作者信息

Mielke C H, Kahn S B, Muschek L D, Tighe J J, Ng K T, Minn F L

出版信息

J Clin Pharmacol. 1980 May-Jun;20(5-6 Pt 2):409-17.

PMID:7400378
Abstract

Zomepirac, a new nonnarcotic analgesic, was studied in 25 healthy adults for possible effects on hemostasis. Given in a single 200-mg dose or for 15 days at 300 mg/day, zomepirac prolonged template bleeding time and caused transient decreases in platelet adhesiveness, in stimulated platelet aggregation, and in the release of platelet serotonin. The short duration of these effects contrasts with the known week-long duration of the effects of aspirin. Data from in vitro platelet function studies, correlated with plasma level determinations, indicate that these effects on platelet function in man are probably dependent only on the presence of intact zomepirac and not on any metabolites. The qualitative effects of zomepirac on platelets are assumed to be the consequence of reversible inhibition of prostaglandin synthetase in these cells. Platelet concentration and the humoral clotting mechanism were not affected by zomepirac. Although no unusual bleeding has been noted in patients given zomepirc postoperatively, it should be used with the same caution as aspirin in patients with known defects in platelet function or coagulation.

摘要

对乙酰氨基酚,一种新型非麻醉性镇痛药,在25名健康成年人中进行了研究,以观察其对止血的可能影响。以200毫克单剂量给药或连续15天每天300毫克给药时,对乙酰氨基酚会延长模板出血时间,并导致血小板黏附性、刺激的血小板聚集以及血小板血清素释放出现短暂下降。这些作用的持续时间较短,与已知的阿司匹林长达一周的作用时间形成对比。体外血小板功能研究的数据与血浆水平测定结果相关,表明对乙酰氨基酚对人体血小板功能的这些影响可能仅取决于完整的对乙酰氨基酚的存在,而不取决于任何代谢产物。对乙酰氨基酚对血小板的定性作用被认为是这些细胞中前列腺素合成酶受到可逆性抑制的结果。血小板浓度和体液凝血机制不受对乙酰氨基酚的影响。尽管在术后接受对乙酰氨基酚治疗的患者中未发现异常出血情况,但对于已知血小板功能或凝血功能有缺陷的患者,使用时应与阿司匹林一样谨慎。

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Eur J Clin Pharmacol. 1995;48(3-4):241-6. doi: 10.1007/BF00198305.
2
The clinical assessment of analgesic drugs.镇痛药的临床评估。
Br J Clin Pharmacol. 1981 Apr;11(4):319-32. doi: 10.1111/j.1365-2125.1981.tb01128.x.
3
Zomepirac: a review of its pharmacological properties and analgesic efficacy.佐美酸:其药理特性与镇痛效果综述
Drugs. 1982 Apr;23(4):250-75. doi: 10.2165/00003495-198223040-00002.