Thiessen J J
Thromb Res Suppl. 1983;4:105-11. doi: 10.1016/0049-3848(83)90365-1.
The antithrombotic effect of acetylsalicylic acid is intimately linked to its reactivity. The labile acetyl moiety irreversibly acetylates not only cyclo-oxygenase, but other biological components. The presence off ubiquitous esterases leads to the rapid disappearance of ASA from the body. The pharmacokinetics of ASA is affected by the dosage form used and the presence of food. Despite the absence of a definable relationship between plasma ASA levels and response, recent data would suggest a dose of about 0.5 mg/kg/day adequately suppresses platelet aggregation without affecting prostacyclin formation.
乙酰水杨酸的抗血栓形成作用与其反应活性密切相关。不稳定的乙酰基部分不仅能不可逆地乙酰化环氧化酶,还能乙酰化其他生物成分。普遍存在的酯酶会导致乙酰水杨酸在体内迅速消失。乙酰水杨酸的药代动力学受所用剂型和食物的影响。尽管血浆乙酰水杨酸水平与反应之间不存在明确的关系,但近期数据表明,约0.5毫克/千克/天的剂量能充分抑制血小板聚集,且不影响前列环素的形成。