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Modulation of vasoconstriction by clopidogrel and ticlopidine
L H Yang1, D Hoppensteadt, J Fareed
1Department of Pathology, Loyola University Medical Center, Maywood, Illinois 60153, USA.
Thrombosis Research
|October 29, 1998
Summary
Clopidogrel and ticlopidine, antiplatelet drugs, exhibit vasomodulatory effects in canines after intravenous administration. Their endogenous transformation is crucial for these vascular actions, impacting stroke management.
Area of Science:
- Pharmacology
- Cardiovascular Science
Background:
- Clopidogrel and ticlopidine are ADP receptor inhibitors used clinically for stroke prevention.
- Their antiplatelet mechanisms are well-established, but potential vascular effects require further investigation.
Purpose of the Study:
- To investigate the vasomodulatory actions of clopidogrel and ticlopidine.
- To determine if endogenous transformation is necessary for these vascular effects.
Main Methods:
- Canines received intravenous clopidogrel or ticlopidine (10 mg/kg).
- Femoral and pulmonary artery rings were isolated for ex vivo tissue bath studies.
- Vascular responses to serotonin, endothelin-1, and other agonists were measured.
Main Results:
- Intravenous administration led to significant desensitization to various vasoconstrictors in isolated artery preparations.
- Direct addition of drugs to organ baths did not elicit similar vasomodulatory effects.
- These findings highlight the importance of in vivo metabolism for drug efficacy.
Conclusions:
- Endogenous transformation of clopidogrel and ticlopidine is essential for their observed vasomodulatory actions.
- Both drugs modulate vascular sites, potentially contributing to their clinical benefits in arterial disorders.