Pharmacokinetics of enteric-coated aspirin and inhibition of platelet thromboxane A2 and vascular prostacyclin generation in humans.
We evaluated whether an enteric-coated aspirin formulation showed a "presystemic" component in its antiplatelet effect and if so would spare vascular cyclooxygenase. In six healthy volunteers, 30 to 45 minutes after ingestion of 325 mg enteric-coated aspirin, platelet thromboxane A2 generation was inhibited by about 20% before any drug could be detected in the peripheral venous blood. A further decline in thromboxane A2 generation occurred with appearance of aspirin in blood between 60 and 240 minutes. No presystemic component could be detected after 325 mg aspirin tablets. Ten patients undergoing saphenectomy received 325 mg of either aspirin tablet or enteric-coated aspirin; 12 hours later platelet thromboxane A2 and peripheral vascular prostacyclin generation were significantly reduced by 98% and 58%, respectively. The effects of the two aspirin formulations were not different. Aspirin formulations with "presystemic" component in their antiplatelet effect may not necessarily result in sparing of peripheral vascular cyclooxygenase.
Cerletti
C
C
Marchi
S
S
Lauri
D
D
Domanin
M
M
Lorenzi
G
G
Urso
R
R
Dejana
E
E
Latini
R
R
de Gaetano
G
G
D000328:Adult; D001241:Aspirin / Q000008:administration & dosage / Q000097:blood / Q000378:metabolism*; D001792:Blood Platelets / Q000187:drug effects*; D011464:Epoprostenol / Q000037:antagonists & inhibitors*; D005260:Female; D006801:Humans; D007700:Kinetics; D012459:Salicylates / Q000097:blood; D020156:Salicylic Acid; D012501:Saphenous Vein / Q000601:surgery; D013608:Tablets, Enteric-Coated; D013928:Thromboxane A2 / Q000037:antagonists & inhibitors*; D013929:Thromboxane B2 / Q000037:antagonists & inhibitors / Q000097:blood
D012459:Salicylates; D013608:Tablets, Enteric-Coated; D013929:Thromboxane B2; D013928:Thromboxane A2; D011464:Epoprostenol; D020156:Salicylic Acid; D001241:Aspirin