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PMID: 413839 Published · ppublish English Journal Article Research Support, U.S. Gov't, P.H.S.

Inhibition of platelet prostaglandin synthetase by oral aspirin.

The Journal of clinical investigation ·Vol. 61 ·No. 2 ·1978-02-00 ·Pages 314-9

Burch JW, Stanford N, Majerus PW

Abstract

Aspirin inhibits platelet function by permanently acetylating the cyclooxygenase that forms prostaglandins. We determined the sensitivity of platelets to aspirin in normal subjects by measuring [3H-acetyl]aspirin-susceptible cyclooxygenase in washed platelets obtained at various times after aspirin ingestion. A single 325-mg aspirin dose inactivated 89% of platelet cyclooxygenase. The inhibition persisted for 2 days suggesting that oral aspirin also inactivated megakaryocyte cyclooxygenase. Thereafter, active enzyme returned with a time-course reflecting platelet turnover (life-span 8.2+/-2 days). Single doses of 20-650 mg aspirin resulted in 34- greater than 95% inhibition after 24 h. Daily doses of 20-325 mg aspirin for brief periods produced 61- greater than 95% inactivation when measured 24 h after cessation of the drug. Platelet cyclooxygenase is more sensitive to inactivation by aspirin than enzyme in sheep seminal vesicles.

MeSH Terms
Acetylation Adult Animals Aspirin/pharmacology Blood Platelets/enzymology Cyclooxygenase Inhibitors Humans Male Middle Aged Prostaglandin-Endoperoxide Synthases/blood Seminal Vesicles/enzymology Sheep
Chemicals
Cyclooxygenase Inhibitors Prostaglandin-Endoperoxide Synthases Aspirin
Authors & Affiliations
3 authors, click to expand affiliations / ORCID
Burch J W
Stanford N
Majerus P W
References (34)
34 references, click to expand
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Article Info
Journal
The Journal of clinical investigation
Abbr.
J Clin Invest
ISSN
0021-9738
DOI
10.1172/JCI108941
Published
1978-02-00
Pages
314-9
Language
English
Region
United States
NLM ID
7802877
PMCID
PMC372541
Subset
IM
External Links
PubMed source DOI: 10.1172/JCI108941 PMC Full Text View journal details
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