Amlodipine dosage forms
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Amlodipine Dosage Forms: An Overview
Introduction to Amlodipine
Amlodipine is a widely used dihydropyridine calcium channel blocker, primarily prescribed for the treatment of hypertension and angina. It is known for its long-acting effects, which make it suitable for once-daily dosing8. This article explores the various dosage forms of amlodipine, including tablets, fixed-dose combinations, and liquid formulations, highlighting their pharmacokinetics, stability, and clinical applications.
Tablet Dosage Forms
Standard Tablets
Amlodipine is commonly available in tablet form, with typical doses ranging from 5 mg to 10 mg. These tablets are effective in providing smooth 24-hour blood pressure control without causing orthostatic hypotension8. The pharmacokinetics of amlodipine tablets show a mean plasma half-life of approximately 36 hours, making them suitable for once-daily administration5.
Dispersible Tablets
A newly developed dispersible tablet formulation of amlodipine besylate has been evaluated for its bioavailability and bioequivalence compared to established branded formulations. Studies in healthy Chinese male volunteers have shown that the dispersible tablets meet the regulatory criteria for bioequivalence, with similar pharmacokinetic properties to the standard tablets3.
Fixed-Dose Combination Tablets
Amlodipine and Valsartan
Fixed-dose combination (FDC) tablets of amlodipine and valsartan are designed to improve medication compliance by combining two antihypertensive agents with different mechanisms of action. Studies have shown that the pharmacokinetics of a newly developed FDC tablet containing amlodipine orotate and valsartan are bioequivalent to the conventional FDC tablet containing amlodipine besylate and valsartan1. These combinations have been found to achieve greater reductions in blood pressure compared to monotherapy with either drug alone9.
Amlodipine and Olmesartan
Similarly, FDC tablets of amlodipine and olmesartan have been studied, showing that the pharmacokinetics of the combination are comparable whether the drugs are administered separately or together in a single tablet. This combination is well-suited for coadministration, providing effective blood pressure control4.
Liquid Dosage Forms
Extemporaneously Prepared Suspensions
For pediatric or elderly patients who have difficulty swallowing tablets, liquid dosage forms of amlodipine are available. Studies have demonstrated that amlodipine besylate is stable in two different liquid suspensions for up to 91 days when stored at 4°C and for 56 days at 25°C. These formulations allow for accurate dosing based on body weight, making them suitable for infants and young children2.
Pediatric Oral Solution
A pediatric oral solution of amlodipine has been developed to provide the necessary dosing flexibility for children. This formulation, containing amlodipine besylate, sucrose syrup, and methyl paraben, remains stable for 12 months under refrigerated conditions. It offers a reliable alternative to manipulated commercial dosage forms or non-standardized extemporaneously compounded formulations10.
Conclusion
Amlodipine is available in various dosage forms, each tailored to meet the needs of different patient populations. Standard and dispersible tablets provide effective and convenient options for adults, while fixed-dose combinations enhance treatment efficacy and compliance. Liquid formulations offer a practical solution for pediatric and elderly patients, ensuring accurate dosing and stability. These diverse dosage forms make amlodipine a versatile and valuable medication in the management of hypertension and angina.
Sources and full results
Most relevant research papers on this topic
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.
RCTStability of amlodipine besylate in two liquid dosage forms.
Amlodipine besylate is stable in two liquid dosage forms for 91 days at 4 degrees C or 56 days at 25 degrees C, making it suitable for pediatric or elderly patients unable to swallow tablets and for accurate dose administration based on body weight.
Pharmacokinetics and bioequivalence evaluation of two formulations of 10-mg amlodipine besylate: an open-label, single-dose, randomized, two-way crossover study in healthy Chinese male volunteers.
The newly developed dispersible tablet formulation of amlodipine besylate shows bioequivalence with an established branded formulation in healthy Chinese male volunteers.
RCTPharmacokinetics of Amlodipine and Olmesartan After Administration of Amlodipine Besylate and Olmesartan Medoxomil in Separate Dosage Forms and as a Fixed‐Dose Combination
The fixed-dose combination of amlodipine and olmesartan is bioequivalent to amlodipine 10 mg plus olmesartan medoxomil 40 mg, with dose-proportional total exposure.
RCTThe 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-RCT
Highly CitedIs 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.
RCTAmlodipine 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 StudyAmlodipine 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