[药理抑制环氧酶2]。

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Beubler E

[药理抑制环氧酶2]。

维恩地中海Wochenschr。2003; 153 (5 - 6): 95 - 9。

PubMed ID

12705061 (在PubMed

]

文摘

前列腺素是疼痛和炎症的重要调节器。,疼痛和炎症可以抑制磷脂酶A2的糖皮质激素水平或水平的环氧合酶(COX)非甾体抗炎药(非甾体抗炎药)。正式“环氧酶”一般被认为是负责合成前列腺素参与疼痛、发炎、发烧以及cytoprotection在胃里,止血和肾脏的血流量。之后,两个同功酶,cyclooxygenase-1和cyclooxygenase-2被发现。这是假设cyclooxygenase-1存在既定的和负责cytoprotection止血而cyclooxygenase-2诱导和参与疼痛,发炎和发烧。同时也发现了本构cyclooxygenase-2各组织。Cyclooxygenase-inhibitors可能分为四组:非选择性的(布洛芬、双氯芬酸等),cyclooxygenase-1选择性抑制剂(sc - 560), cyclooxygenase-2优惠的(meloxicam)和cyclooxygenase-2选择性抑制剂(塞来昔布,万络,parecoxib)。选择性cyclooxygenase-2-inhibitors相反的经典的非甾体抗炎药在治疗剂量出血时间无影响。最重要的非甾体抗炎药的副作用是出血,溃疡和上消化道穿孔,损伤肾脏。选择性cyclooxygenase-2-inhibitors显示胃十二指肠溃疡的少。 Risk patients, however, still need gastroprotection during therapy with cyclooxygenase-2-inhibitors. In patients with low dose aspirin prophylaxis cyclooxygenase-2-inhibitors do not show any benefit compared to classic non steroidal anti-inflammatory drugs (CLASS-study). Less gastrointestinal side effects do not mean a higher overall safety benefit. Cardiovascular and thrombotic side effects of rofecoxib are higher than those of naproxen (VIGOR-study). Concerning valdecoxib, hypersensibilities are reported, probably due to its sulfonamidstructure. The same side effects are to be expected with its prodrug, parecoxib. Drug-drug interactions with cyclooxygenase-2-inhibitors and anticoagulant drugs are to be expected as well as other interactions with drugs, metabolised by the cytochrom P450 system.

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药物靶点

药物	目标	类	生物	药理作用	行动
双氯芬酸	前列腺素合成酶2 G / H	蛋白质	人类	是的	抑制剂	细节