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非甾体抗炎芬那酸类药物可能拮抗前列腺素内过氧化物在人子宫肌层中的作用。

Fenamates may antagonize the actions of prostaglandin endoperoxides in human myometrium.

作者信息

Sanger G J, Bennett A

出版信息

Br J Clin Pharmacol. 1979 Nov;8(5):479-82. doi: 10.1111/j.1365-2125.1979.tb01030.x.

Abstract

1 The prostaglandin endoperoxide analogue U-46619 potently contracted human isolated myometrium, suggesting that prostaglandin H2 (PGH2) may be a major stimulant of myometrial contractions. 2 Sodium mefenamate, flufenamate or meclofenamate 2 microgram/ml greatly reduced contractions of the myometrium induced by the PGH2 analogue. 3 Flufenamate, but not the other two drugs, also significantly inhibited contractions to acetylcholine. 4 Sodium meclofenamate 2 microgram/ml did not consistently antagonize contractions to PGF2alpha. 5 The relief of dysmenorrhoea by fenamates may be explained both by inhibition of PG synthesis, and by antagonism of contractions to PGH2 produced by incompletely blocked PG synthesis.

摘要
  1. 前列腺素内过氧化物类似物U - 46619能有效收缩人离体子宫肌层,提示前列腺素H2(PGH2)可能是子宫肌层收缩的主要刺激物。2. 甲灭酸、氟灭酸或甲氯灭酸2微克/毫升能显著降低PGH2类似物诱导的子宫肌层收缩。3. 氟灭酸,而非其他两种药物,也能显著抑制对乙酰胆碱的收缩反应。4. 甲氯灭酸2微克/毫升不能持续拮抗对PGF2α的收缩反应。5. 灭酸类药物缓解痛经可能是通过抑制前列腺素合成,以及拮抗不完全阻断前列腺素合成所产生的对PGH2的收缩反应来实现的。

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本文引用的文献

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Prostaglandins, indomethacin and dysmenorrhea.
Prostaglandins. 1976 May;11(5):893-907. doi: 10.1016/0090-6980(76)90196-9.
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Determination of menstrual prostaglandin levels in non-dysmenorrheic and dysmenorrheic subjects.
Prostaglandins. 1978 Feb;15(2):365-75. doi: 10.1016/0090-6980(78)90176-4.

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