Amlodipine peak
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Amlodipine Peak: Pharmacokinetics and Therapeutic Efficacy
Pharmacokinetics of Amlodipine
Absorption and Bioavailability
Amlodipine, a dihydropyridine calcium antagonist, exhibits unique pharmacokinetic properties. After oral administration, amlodipine is well absorbed with a bioavailability of 60-65%. Plasma concentrations peak gradually, typically 6 to 8 hours post-administration, indicating a slow absorption rate 38. This gradual rise in plasma levels contributes to its suitability for once-daily dosing.
Metabolism and Elimination
Amlodipine undergoes extensive hepatic metabolism, but it does not experience significant presystemic or first-pass metabolism. The drug is slowly cleared from the body, with a terminal elimination half-life ranging from 40 to 50 hours . This prolonged half-life supports its sustained therapeutic effect over a 24-hour period.
Volume of Distribution and Protein Binding
The volume of distribution for amlodipine is large (21 L/kg), and it exhibits a high degree of protein binding (98%) . These characteristics ensure that the drug remains in the systemic circulation for an extended period, contributing to its long-lasting effects.
Therapeutic Efficacy and Trough: Peak Ratios
Blood Pressure Control
Amlodipine is effective in managing hypertension, providing consistent blood pressure control over a 24-hour period. In a comparative study with perindopril, amlodipine demonstrated a global diastolic blood pressure trough: peak ratio of 0.80 and a systolic blood pressure trough: peak ratio of 0.83 . These ratios indicate a stable and sustained antihypertensive effect throughout the dosing interval.
Impact on Exercise Performance
In patients with angina pectoris, amlodipine significantly improved exercise tolerance. Studies showed that amlodipine increased peak oxygen consumption and endurance time during submaximal exercise tests, highlighting its efficacy in enhancing physical performance and reducing angina frequency 679.
Safety and Tolerability
Amlodipine is generally well tolerated. Common adverse effects include leg edema, which was reported in 19.1% of patients in one study . Despite this, the overall safety profile of amlodipine is favorable, with no significant pharmacokinetic drug interactions reported .
Conclusion
Amlodipine's pharmacokinetic profile, characterized by gradual absorption, extensive metabolism, and prolonged elimination, underpins its effectiveness in providing sustained blood pressure control and improving exercise performance in patients with angina. Its high bioavailability and long half-life make it suitable for once-daily dosing, ensuring consistent therapeutic coverage. While generally well tolerated, monitoring for common side effects such as leg edema is advisable. Overall, amlodipine remains a reliable option for managing hypertension and angina pectoris.
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