Pharmacokinetics of enteric-coated aspirin and inhibition of platelet thromboxane A2 and vascular prostacyclin generation in humans

Chiara Cerletti, Stefano Marchi, Davide Lauri, Maurizio Domanin, Giovanni Lorenzi, Renato Urso, Elisabetta Dejana, Roberto Latini, Giovanni de Gaetano

Research output: Contribution to journalArticle

Abstract

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 AZ 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.

Original languageEnglish
Pages (from-to)175-180
Number of pages6
JournalClinical Pharmacology and Therapeutics
Volume42
Issue number2
Publication statusPublished - Aug 1987

Fingerprint

Thromboxane A2
Epoprostenol
Aspirin
Blood Vessels
Blood Platelets
Pharmacokinetics
Prostaglandin-Endoperoxide Synthases
Enteric-Coated Tablets
Thromboxanes
Tablets
Healthy Volunteers
Eating

ASJC Scopus subject areas

  • Pharmacology

Cite this

Pharmacokinetics of enteric-coated aspirin and inhibition of platelet thromboxane A2 and vascular prostacyclin generation in humans. / Cerletti, Chiara; Marchi, Stefano; Lauri, Davide; Domanin, Maurizio; Lorenzi, Giovanni; Urso, Renato; Dejana, Elisabetta; Latini, Roberto; de Gaetano, Giovanni.

In: Clinical Pharmacology and Therapeutics, Vol. 42, No. 2, 08.1987, p. 175-180.

Research output: Contribution to journalArticle

Cerletti, Chiara ; Marchi, Stefano ; Lauri, Davide ; Domanin, Maurizio ; Lorenzi, Giovanni ; Urso, Renato ; Dejana, Elisabetta ; Latini, Roberto ; de Gaetano, Giovanni. / Pharmacokinetics of enteric-coated aspirin and inhibition of platelet thromboxane A2 and vascular prostacyclin generation in humans. In: Clinical Pharmacology and Therapeutics. 1987 ; Vol. 42, No. 2. pp. 175-180.
@article{a0dfff201a404fcb9a31ce2b06ab6679,
title = "Pharmacokinetics of enteric-coated aspirin and inhibition of platelet thromboxane A2 and vascular prostacyclin generation in humans",
abstract = "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 AZ 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.",
author = "Chiara Cerletti and Stefano Marchi and Davide Lauri and Maurizio Domanin and Giovanni Lorenzi and Renato Urso and Elisabetta Dejana and Roberto Latini and {de Gaetano}, Giovanni",
year = "1987",
month = "8",
language = "English",
volume = "42",
pages = "175--180",
journal = "Clinical Pharmacology and Therapeutics",
issn = "0009-9236",
publisher = "Nature Publishing Group",
number = "2",

}

TY - JOUR

T1 - Pharmacokinetics of enteric-coated aspirin and inhibition of platelet thromboxane A2 and vascular prostacyclin generation in humans

AU - Cerletti, Chiara

AU - Marchi, Stefano

AU - Lauri, Davide

AU - Domanin, Maurizio

AU - Lorenzi, Giovanni

AU - Urso, Renato

AU - Dejana, Elisabetta

AU - Latini, Roberto

AU - de Gaetano, Giovanni

PY - 1987/8

Y1 - 1987/8

N2 - 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 AZ 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.

AB - 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 AZ 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.

UR - http://www.scopus.com/inward/record.url?scp=0023259345&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0023259345&partnerID=8YFLogxK

M3 - Article

C2 - 3301151

AN - SCOPUS:0023259345

VL - 42

SP - 175

EP - 180

JO - Clinical Pharmacology and Therapeutics

JF - Clinical Pharmacology and Therapeutics

SN - 0009-9236

IS - 2

ER -