Phospholipid Corticosteroids……*○ Bradykinin Angiotensin Phospholipase a Arachidonic acid Cyclooxygenase(CoX) NSAIDS……* 5-lipoXygenase PGG? Prostacyclin(PGl2 hydroperoxidase PGE PGF2a PGH2 Leukotrienes Thromboxane A2 Dipyridamole
Arachidonic acid Phospholipase A2 Corticosteroids ⊕ Bradykinin Angiotensin Cyclooxygenase (COX) PGG2 Prostacyclin(PGI2 ) PGE2 PGF2α Thromboxane A2 Dipyridamole hydroperoxidase NSAIDs Leukotrienes 5-lipoxygenase Phospholipid PGH2
Characteristics comparison between coX-1 and coX-2 COX-1 COX-2 Synthesis intrinsic induced Functions physiological physiological gastrointestinal production of PG protection elevated during platelet aggregation pregnancy regulation pathological: vascular resistance producing proteinase, regulation PG, and other renal blood flow inflammatory regulation mediators
COX-1 COX-2 Synthesis intrinsic induced Functions physiological: gastrointestinal protection platelet aggregation regulation vascular resistance regulation renal blood flow regulation physiological: production of PG elevated during pregnancy pathological: producing proteinase, PG, and other inflammatory mediators Characteristics comparison between COX-1 and COX-2
Classification Of Nsaids Aspirin and other salicylates(阿司匹林及水杨酸类) Aniline derivatives(苯胺类衍生物) Indole derivatives(吲哚类衍生物) Propionic acid derivatives(丙酸类衍生物) Others(烯醇酸类,灭酸类,杂环芳基乙酸类,茚乙酸类, 吡唑酮类,以及选择性cOX-2抑制剂)
Aspirin and other salicylates（阿司匹林及水杨酸类） Aniline derivatives（苯胺类衍生物） Indole derivatives（吲哚类衍生物） Propionic acid derivatives（丙酸类衍生物） Others (烯醇酸类，灭酸类，杂环芳基乙酸类，茚乙酸类， 吡唑酮类，以及选择性COX-2抑制剂) Classification of NSAIDs :
Acetyl group that Is transferred to cyclooxygenase 1. Aspirin COOH O CCH The mechanism of Aspirin aspirin: acetylating (Acetylsalicylic acid) COX enzyme H2o Cyclooxygenase acute irreversibly Normal deacetylation y●aaea acetylated clooxygenase inactive COOH OH Salicylic acId ( salicylate
The mechanism of aspirin: acetylating COX enzyme irreversibly 1. Aspirin
1. Aspirin 1.1 Actions and therapeutic uses: A Antipyretic and analgesic actions resets the thermostat toward normal and lowers the body temperature by increasing heat dissipation; alleviates pain of low to moderate intensity arising from integument, especially with inflammation
1.1 Actions and therapeutic uses: A Antipyretic and analgesic actions: -- resets the thermostat toward normal and lowers the body temperature by increasing heat dissipation; -- alleviates pain of low to moderate intensity arising from integument, especially with inflammation. 1. Aspirin