Amlodipine dosage

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Amlodipine Dosage: Efficacy, Safety, and Pharmacokinetics

Introduction to Amlodipine Dosage

Amlodipine is a long-acting calcium channel blocker commonly used to treat hypertension and angina. The appropriate dosage of amlodipine is crucial for maximizing its therapeutic benefits while minimizing potential side effects. This article synthesizes research findings on the dosage, efficacy, safety, and pharmacokinetics of amlodipine.

Efficacy of Amlodipine in Hypertension

Dosage Range and Blood Pressure Reduction

Clinical studies have demonstrated that amlodipine is effective in reducing blood pressure in patients with mild to moderate hypertension. The typical dosage range is 2.5-10 mg once daily. In a study involving 30 patients, amlodipine significantly reduced blood pressure by 16/12 mm Hg in the supine position and 14/4 mm Hg in the standing position over an 8-week period . Another study confirmed that doses of 2.5-10 mg daily effectively reduced both supine and standing blood pressures, with the minimum effective dose being 2.5 mg .

Long-Term Efficacy

Amlodipine provides smooth 24-hour blood pressure control without causing orthostatic hypotension. It is effective as monotherapy and in combination with other antihypertensive drugs, such as beta-blockers, diuretics, or ACE inhibitors . The drug maintains its efficacy over long-term use without developing tolerance .

Safety Profile of Amlodipine

Common Side Effects

Amlodipine is generally well tolerated, with a low incidence of serious side effects. The most common side effect is ankle edema, which is dose-dependent and usually mild 14. In a large pooled analysis, the incidence of severe side effects was lower compared to beta-blockers, with edema being the most notable side effect .

Safety in Special Populations

Amlodipine is safe for use in elderly patients and does not require dosage adjustments in patients with renal impairment. However, the dosage regimen for patients with hepatic impairment is not yet established . In children, doses as low as 2.5 mg can cause hypotension, indicating the need for careful dose management in pediatric populations .

Pharmacokinetics of Amlodipine

Absorption and Half-Life

Amlodipine has a mean plasma half-life of approximately 34-36 hours after oral administration, allowing for once-daily dosing . The drug reaches steady-state plasma concentrations after about seven days of repeated dosing, with an accumulation factor of approximately threefold .

Bioavailability and Distribution

The systemic availability of amlodipine after oral administration is around 64%, with a mean clearance rate of 7 ml/min/kg and an apparent volume of distribution of 21 l/kg . These pharmacokinetic properties support its efficacy in providing consistent blood pressure control over a 24-hour period.

Conclusion

Amlodipine is an effective and well-tolerated antihypertensive agent with a recommended dosage range of 2.5-10 mg once daily. It provides smooth, long-term blood pressure control and is safe for use in various patient populations, including the elderly and those with renal impairment. Its pharmacokinetic profile supports its once-daily dosing regimen, making it a convenient option for patients. However, careful dose management is necessary in pediatric populations to avoid hypotension.

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Most relevant research papers on this topic

Once daily amlodipine in the treatment of mild to moderate hypertension.

Once-daily amlodipine effectively reduces blood pressure in patients with mild to moderate hypertension, with no significant effects on heart rate or heart rate variability.

RCT

1987·

44citations

·J. Webster et al.

The pharmacokinetics of amlodipine in healthy volunteers after single intravenous and oral doses and after 14 repeated oral doses given once daily.

Amlodipine has a 36-hour half-life after intravenous administration and a 45-hour half-life after repeated oral administration, with steady state plasma concentration achieved after seven doses.

Non-RCTHighly Cited

1986·

228citations

·J. Faulkner et al.

Amlodipine in hypertension: an overview of the clinical dossier.

Amlodipine is an effective and well-tolerated antihypertensive drug, providing smooth 24-hour blood pressure control without orthostatic hypotension and being well-tolerated as monotherapy or in combination with other drugs.

Systematic Review

1988·

58citations

·Stevo Julius

Amlodipine: a double-blind evaluation of the dose-response relationship in mild to moderate hypertension.

Amlodipine effectively reduces blood pressures with once-daily dosing, with 2.5 mg being the minimum effective dose, and is well-tolerated in patients with mild to moderate hypertension.

RCT

1988·

25citations

·Frick Mh et al.

Is initial dose titration of amlodipine worthwhile in patients with mild to moderate hypertension?

Early increase in amlodipine dosage does not provide an advantage in antihypertensive effect, and a dose increase should not be considered until after six weeks of treatment at 5 mg once daily.

RCT

1999·

8citations

·K. Hayduk et al.

Amlodipine toxicity in children less than 6 years of age: a dose-response analysis using national poison data system data.

Hypotension may occur in children with amlodipine doses as low as 2.5 mg, and the National Poison Data System may provide insights into dose-response relationships in this population.

Observational Study

2010·

23citations

·B. E. Benson et al.

Efficacy and safety of amlodipine in vasospastic angina: An interim report of a multicenter, placebo-controlled trial

Amlodipine is a well-tolerated and effective antiischemic and antianginal therapy for patients with chronic stable angina pectoris, reducing angina attacks and nitroglycerin consumption.

RCT

1989·

18citations

·R. Chahine et al.

Pharmacokinetic comparison of 2 fixed-dose combination tablets of amlodipine and valsartan in healthy male Korean volunteers: a randomized, open-label, 2-period, single-dose, crossover study.

The newly developed FDC tablet of amlodipine and valsartan did not significantly differ from the conventional FDC tablet in healthy Korean male subjects, with both formulations well-tolerated and no serious adverse events observed.

RCT

2013·

13citations

·Yukyung Kim et al.

Usefulness of amlodipine for angina pectoris.

Amlodipine effectively reduces exercise-induced angina attacks and improves symptoms in most patients with stable angina pectoris, with a side-effect profile similar to placebo.

RCT

1994·

42citations

·S. Taylor

The safety of amlodipine.

Amlodipine has a good safety profile, with once-daily dosage, smooth onset, and long duration of action, making it a suitable antihypertensive and antiischemic agent.

Meta-AnalysisHighly Cited

1989·

72citations

·Ian H Osterloh

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