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Concentration-effect and time-effect relationships of carteolol
European Journal of Clinical Pharmacology
|January 1, 1983
Summary
Carteolol effectively reduces exercise heart rate and blood pressure, demonstrating a strong correlation between plasma concentration and its beta-blocking effect over 48 hours in healthy adults.
Area of Science:
- Pharmacology
- Cardiovascular Physiology
Background:
- Carteolol is a beta-blocker with partial agonist activity.
- Understanding its concentration-effect relationship is crucial for therapeutic use.
Purpose of the Study:
- To evaluate the concentration-beta blocking effect and time-effect relationships of carteolol.
- To assess hemodynamic responses to intravenous and oral carteolol in healthy adults.
Main Methods:
- Eight healthy adults received 15 mg i.v. and 20 mg orally carteolol on separate occasions.
- Resting and post-exercise blood pressure and heart rate were measured up to 48 hours.
- Plasma carteolol concentrations were correlated with beta-blocking effects.
Main Results:
- Carteolol caused a transient, insignificant heart rate increase but lowered diastolic blood pressure at rest.
- Post-exercise heart rate and double product were significantly reduced for 48 hours.
- A significant correlation was found between log plasma carteolol concentration and beta-blocking effect (r=0.508 i.v., r=0.626 p.o.).
Conclusions:
- Carteolol exhibits a dose-dependent beta-blocking effect.
- The drug effectively reduces exercise-induced cardiovascular responses.
- Individual variations in the concentration-effect relationship exist.