Amlodipine onset peak duration

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Amlodipine: Onset, Peak, and Duration of Action

Introduction to Amlodipine

Amlodipine is a long-acting dihydropyridine calcium channel blocker commonly used in the treatment of hypertension and angina pectoris. Its unique pharmacokinetic and pharmacodynamic properties make it suitable for once-daily dosing, providing sustained therapeutic effects with minimal side effects.

Onset of Action

The onset of action for amlodipine is gradual. After oral administration, the drug is absorbed slowly, with peak plasma concentrations occurring approximately 6 to 8 hours post-dose 357. This slow absorption rate contributes to a gradual decrease in blood pressure, reducing the likelihood of reflex tachycardia and other vasodilator side effects 57.

Peak Effect

Amlodipine reaches its peak effect around 6 to 8 hours after administration, coinciding with the peak plasma concentrations 357. This timing is consistent across different doses, as demonstrated in studies involving healthy volunteers and patients with stable angina pectoris 49. The peak effect is characterized by a significant reduction in blood pressure and an increase in exercise tolerance, with improvements in time to onset of angina and total exercise duration 246.

Duration of Action

The duration of action for amlodipine is notably long, attributed to its slow elimination half-life of 40 to 60 hours 367. This extended half-life allows for once-daily dosing, maintaining stable plasma concentrations and therapeutic effects over a 24-hour period 357. Clinical studies have shown that the antihypertensive and antianginal effects of amlodipine persist throughout the dosing interval, with minimal fluctuations in efficacy 246.

Conclusion

Amlodipine's pharmacokinetic profile, characterized by a gradual onset, peak effect at 6 to 8 hours, and prolonged duration of action, makes it an effective and well-tolerated option for managing hypertension and angina pectoris. Its once-daily dosing regimen ensures consistent therapeutic benefits, enhancing patient compliance and overall treatment outcomes.

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Most relevant research papers on this topic

Amlodipine, a long-acting calcium antagonist drug reduces ischemia-induced ventricular conduction delay in pig hearts.

Amlodipine reduces ischemia-induced ventricular conduction delay in pig hearts, potentially reducing the likelihood of lethal ventricular arrhythmias in early stages of myocardial ischemia.

RCTAnimal Study

1989·

5citations

·M. Rämö et al.

A four-week double-blind, placebo-controlled, parallel dose-response study of amlodipine in patients with stable exertional angina pectoris.

Amlodipine is an effective and well-tolerated once-daily treatment for chronic stable angina, with no severe adverse reactions compared to placebo.

RCT

1989·

20citations

·Stanley H. Taylor et al.

Clinical Pharmacokinetics of Amlodipine

Amlodipine has distinct pharmacokinetic characteristics, making it suitable for single daily administration with minimal drug interactions.

Highly Cited

1992·

235citations

·P. Meredith et al.

Amlodipine in patients with stable angina pectoris treated with nitrates and beta-blockers. The influence on exercise tolerance, systolic and diastolic functions of the left ventricle.

Amlodipine significantly improves exercise tolerance and left ventricle function in patients with stable angina pectoris, with 10 mg dose being most effective and well-tolerated.

RCT

1992·

7citations

·J. Meluzin et al.

Amlodipine: an overview of its pharmacodynamic and pharmacokinetic properties.

Amlodipine has a unique pharmacokinetic profile, with a slow onset of action and long duration of effect, potentially benefiting patients with slower reflex tachycardia and lower incidence of vasodilator side effects.

1994·

50citations

·van Zwieten Pa

Antianginal Efficacy and Safety of Ivabradine Compared with Amlodipine in Patients with Stable Effort Angina Pectoris

Ivabradine has comparable efficacy to amlodipine in improving exercise tolerance and reducing rate-pressure product in patients with stable angina, with similar safety.

RCTLarge Human TrialHighly Cited

2012·

152citations

·W. Rużyłło et al.

Pharmacokinetics and pharmacodynamics of amlodipine.

Amlodipine effectively treats hypertension and angina pectoris with once-daily dosing, offering a low-clearance, dihydropyridine calcium antagonist with high oral bioavailability.

Highly Cited

1992·

83citations

·Darrell R. Abernethy

Comparison of controlled-onset, extended-release verapamil with amlodipine and amlodipine plus atenolol on exercise performance and ambulatory ischemia in patients with chronic stable angina pectoris.

COER-24 verapamil and amlodipine plus atenolol improve exercise capacity and decrease ambulatory myocardial ischemia in patients with chronic stable angina pectoris.

RCTLarge Human TrialHighly Cited

1999·

85citations

·W. Frishman et al.

Amlodipine Pharmacokinetics in Healthy Volunteers

Amlodipine effectively lowers blood pressure when given once daily, with headache being the most common side effect, and its long half-life and gradual absorption minimize side effects.

RCT

1988·

61citations

·Dennis M. Williams et al.

Pharmacologic profile of amlodipine.

Amlodipine is a potent calcium antagonist and effective oral antihypertensive agent with natriuretic properties, making it a potential first-line treatment for hypertension.

Non-RCTAnimal StudyHighly Cited

1989·

95citations

·R. Burges et al.

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