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Pharmacokinetics of calcium antagonists
J L Reid1, P A Meredith, R Donnelly
1University Department of Materia Medica, Stobhill Hospital, Glasgow, Scotland.
Journal of Cardiovascular Pharmacology
|January 1, 1988
Summary
New calcium channel blocker amlodipine offers advantages for cardiovascular disease treatment. Its unique pharmacokinetic profile ensures a long-lasting effect, potentially improving patient management compared to existing drugs.
Area of Science:
- Pharmacology
- Cardiovascular Medicine
Background:
- Calcium antagonists are a diverse drug class blocking calcium entry into cardiac and smooth muscle cells.
- Existing agents like nifedipine, verapamil, and diltiazem are used for angina and hypertension but share pharmacokinetic limitations.
Purpose of the Study:
- To introduce amlodipine, a novel dihydropyridine calcium antagonist.
- To highlight amlodipine's distinct pharmacokinetic profile and its potential clinical advantages.
Main Methods:
- Review of amlodipine's pharmacokinetic properties.
- Comparison with established calcium antagonists.
Main Results:
- Amlodipine exhibits high bioavailability, slow absorption, and extensive liver metabolism.
- It possesses a long elimination half-life (35-50 hours) and prolonged pharmacodynamic action (>24 hours).
- These properties differ significantly from nifedipine, verapamil, and diltiazem.
Conclusions:
- Amlodipine's novel pharmacokinetics suggest practical benefits for long-term cardiovascular disease management.
- Its extended duration of action may enhance therapeutic efficacy and patient compliance.