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Plasma concentration--effect relationships for felodipine: a meta analysis
E Blychert1, B Edgar, D Elmfeldt
1Department of Clinical Pharmacology, Sahlgrenska University Hospital, Göteborg, Sweden.
Clinical Pharmacology and Therapeutics
|July 1, 1992
Summary
This study shows that higher plasma concentrations of felodipine correlate with a greater antihypertensive effect in patients with hypertension. The Emax model effectively describes this relationship, aiding in personalized treatment strategies.
Area of Science:
- Pharmacology
- Cardiovascular Medicine
Background:
- Hypertension is a significant global health concern requiring effective antihypertensive therapies.
- Calcium channel blockers, such as felodipine, are commonly prescribed for managing high blood pressure.
Purpose of the Study:
- To investigate the relationship between plasma concentrations of felodipine and its antihypertensive effect.
- To evaluate the applicability of the Emax model in characterizing this relationship in hypertensive patients.
Main Methods:
- A study involving 67 patients with hypertension and 21 healthy subjects.
- Utilized the Emax model to analyze plasma drug concentration and blood pressure data over time.
- Monitored plasma felodipine concentrations and corresponding blood pressure changes.
Main Results:
- Felodipine demonstrated a clear concentration-effect relationship in hypertensive patients, with plasma levels mirroring blood pressure reduction.
- The Emax model effectively fitted diastolic blood pressure data for most hypertensive patients.
- Average Emax was 29 mm Hg, with 8 nmol/L of felodipine achieving 50% of maximal effect.
Conclusions:
- Felodipine's antihypertensive efficacy is closely linked to its plasma concentration in patients with hypertension.
- The Emax model provides a valuable tool for understanding and potentially optimizing felodipine dosing.
- Initial diastolic blood pressure influenced the maximal effect, but not the concentration required for half-maximal effect.