Amlodipine dose
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Amlodipine Dose: Efficacy, Safety, and Pharmacokinetics
Introduction to Amlodipine Dosage
Amlodipine, a calcium channel blocker, is widely used for the treatment of hypertension and angina. The appropriate dosage of amlodipine is crucial for achieving optimal therapeutic outcomes while minimizing side effects. This article synthesizes research findings on the efficacy, safety, and pharmacokinetics of various doses of amlodipine.
Efficacy of Amlodipine in Hypertension
Dose-Response Relationship
Multiple studies have demonstrated that amlodipine effectively reduces blood pressure in a dose-dependent manner. In a multicenter, placebo-controlled trial, doses ranging from 1.25 mg to 10 mg were evaluated. Significant reductions in blood pressure were observed in the medium (2.5-5.0 mg) and high-dose (5.0-10.0 mg) groups compared to placebo, with the minimum effective dose being 2.5 mg. Another study confirmed that target blood pressure was achieved in 41% of patients with 2.5 mg, 56% with 5 mg, and 73% with 10 mg of amlodipine once daily.
Long-Term Efficacy
Amlodipine provides smooth 24-hour blood pressure control without orthostatic hypotension, making it suitable for once-daily dosing. The drug maintains its efficacy over long-term administration without developing tolerance. This sustained effect is beneficial for chronic management of hypertension.
Safety and Tolerability
Common Side Effects
Amlodipine is generally well tolerated, with a low incidence of side effects. Common adverse effects include headache, dizziness, and slight ankle edema, particularly at higher doses . In pediatric patients, side effects such as fatigue, headache, and facial flushing were reported, but the drug was still considered safe and effective.
Toxicity in Overdose
In cases of overdose, particularly in children, amlodipine can cause significant hypotension and other cardiovascular issues. A study analyzing poison data found that doses as low as 2.5 mg could induce clinically important responses, with higher doses (>10 mg) significantly increasing the risk of adverse effects.
Pharmacokinetics of Amlodipine
Absorption and Half-Life
Amlodipine has a long half-life, ranging from 31.2 to 36.8 hours depending on the dose, which supports its once-daily dosing regimen. The drug is gradually absorbed, with peak plasma levels occurring 5.6 to 6.4 hours post-dose. This gradual absorption helps minimize side effects related to rapid drug uptake.
Steady-State Concentrations
Repeated oral administration of amlodipine results in steady-state plasma concentrations being reached after approximately seven doses, with an accumulation factor of about threefold. This steady-state pharmacokinetic profile ensures consistent therapeutic effects with daily dosing.
Conclusion
Amlodipine is an effective and well-tolerated antihypertensive agent with a clear dose-response relationship. The minimum effective dose for blood pressure reduction is 2.5 mg, with higher doses providing greater efficacy. The drug's long half-life and gradual absorption make it suitable for once-daily administration, ensuring smooth and sustained blood pressure control. While generally safe, caution is advised in cases of overdose, especially in pediatric patients. Overall, amlodipine remains a valuable option in the management of hypertension and angina.
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