Metoprolol succinate er tablets
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Metoprolol Succinate ER Tablets: Pharmacokinetics, Efficacy, and Clinical Applications
Pharmacokinetics and Bioequivalence of Metoprolol Succinate ER Tablets
Pharmacokinetic Profiles and Bioequivalence
Metoprolol succinate extended-release (ER) tablets are designed to provide consistent beta-1 blockade over a 24-hour period. A study conducted on healthy Chinese subjects under both fasting and fed conditions demonstrated that the test metoprolol ER tablet was bioequivalent to the reference tablet, Betaloc ZOK. The 90% confidence intervals for key pharmacokinetic parameters such as AUC0-48h, AUC0-inf, and Cmax were within the acceptable bioequivalence range of 80-125%1. This indicates that both formulations deliver the drug at similar rates and extents, ensuring therapeutic equivalence.
Comparison of Brand and Generic Formulations
A randomized, cross-over trial compared the pharmacokinetics and pharmacodynamics of brand name versus two generic formulations of metoprolol ER tablets in adults with hypertension. The study found that while the primary pharmacokinetic endpoints (AUC and Cmax) were similar between products, there were significant differences in Tmax, which could affect the drug's impact on autonomic balance over the dosing interval2. This suggests that while generics are generally equivalent, slight variations in release profiles may exist.
Clinical Efficacy in Chronic Heart Failure and Hypertension
Chronic Heart Failure
Extended-release metoprolol succinate has been extensively studied for its efficacy in managing chronic heart failure. The MERIT-HF trial, a large randomized, double-blind, placebo-controlled study, demonstrated that ER metoprolol succinate significantly reduced the relative risk of all-cause mortality by 34% and sudden death by 41% compared to placebo. The drug was well tolerated, with a discontinuation rate due to adverse events similar to that of the placebo group3. This highlights the substantial benefits of ER metoprolol succinate in improving survival and reducing hospitalizations in heart failure patients.
Hypertension Management
Metoprolol succinate ER tablets are also effective in treating hypertension. A study involving 60 patients with mild to moderate essential hypertension showed that the drug significantly reduced blood pressure and heart rate over a 24-hour period, demonstrating its efficacy as a once-daily antihypertensive agent8. Additionally, a clinical trial in hypertensive children aged 6 to 16 years found that ER metoprolol significantly reduced both systolic and diastolic blood pressure at higher doses, with no serious adverse events reported10. This underscores the drug's utility in pediatric hypertension management.
Formulation and Drug Release Characteristics
Multiple-Unit Pellet System (MUPS) Tablets
Research on the development of metoprolol succinate ER multiple-unit pellet system (MUPS) tablets has shown that these formulations can extend drug release up to 20 hours. The optimized MUPS tablets were found to deliver metoprolol at a desired rate, ensuring prolonged therapeutic effects4. This formulation approach helps in maintaining consistent plasma drug levels, reducing the frequency of dosing.
Bilayer Tablets
Bilayer tablets combining immediate-release (IR) and extended-release (ER) layers have been developed to provide both rapid onset and sustained drug release. A study formulated metoprolol succinate bilayer tablets with 30 mg IR and 70 mg ER components, achieving satisfactory drug release profiles and desirable physical properties5. This dual-layer approach can enhance patient compliance by combining the benefits of immediate and sustained drug action in a single tablet.
Conclusion
Metoprolol succinate ER tablets are a versatile and effective option for managing chronic heart failure and hypertension. Their pharmacokinetic profiles ensure consistent drug delivery, and various formulations like MUPS and bilayer tablets offer tailored release characteristics to meet different therapeutic needs. Clinical studies affirm their efficacy and safety, making them a reliable choice in cardiovascular therapy.
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Most relevant research papers on this topic
Pharmacokinetics and bioequivalence of two metoprolol succinate extended release tablets in healthy Chinese subjects under fasting and fed conditions.
The test metoprolol ER tablet was bioequivalent to the reference metoprolol ER tablet (Betaloc ZOK) in healthy Chinese subjects under both fasting and fed conditions, with both formulations being well-tolerated by study participants.
RCTA randomized, cross‐over trial of metoprolol succinate formulations to evaluate PK and PD end points for therapeutic equivalence
Metoprolol extended-release tablets show similar pharmacokinetics and pharmacodynamics, but differences in Tmax between brand and generic products may impact drug effects on autonomic balance over time.
RCT
Rigorous JournalExtended-Release Metoprolol Succinate in Chronic Heart Failure
Extended-release metoprolol succinate significantly reduces mortality and morbidity in chronic heart failure patients, with benefits evident in various patient subgroups.
Systematic ReviewDevelopment and In Vitro-In Vivo Evaluation of Extended-release Multiple-unit Pellet System Tablets of Metoprolol Succinate
The developed metoprolol succinate extended-release multiple-unit pellet system tablets effectively extend metoprolol delivery at a desired rate for 20 hours.
In Vitro StudyFormulation and Evaluation of Bilayer tablets of Metoprolol Succinate
Batch BL-3 of bilayer metoprolol succinate tablets demonstrates desirable properties and optimized drug release, with HPMC K 4M in 20% concentration sustaining the release for 12 hours.
In Vitro StudyFormulation Development and In-vitro Evaluation of Sustained Release Tablets of Metoprolol Succinate
Metoprolol succinate sustained release tablets formulated using polymers show acceptable physical characteristics and dissolution rates that meet USP specifications.
Metoprolol succinate extended release/hydrochlorothiazide combination tablets
Metoprolol extended release hydrochlorothiazide combination tablets effectively lower blood pressure and are a low-dose alternative to high-dose monotherapy, minimizing side-effects.
Rigorous JournalThe analysis of 60 patients of essential hypertension treatment with metoprolol succinate sustained-release tablets
Metoprolol succinate sustained-release tablets effectively treat mild to moderate essential hypertension, providing stable blood pressure over 24 hours.
RCT
Very Rigorous JournalTablet splitting: Product quality assessment of metoprolol succinate extended release tablets.
NIR chemical imaging can help determine the need for content uniformity studies in split metoprolol succinate extended release tablets, assessing the non-homogeneous distribution of metoprolol succinate beads on the tablet surface.
Efficacy and safety of extended release metoprolol succinate in hypertensive children 6 to 16 years of age: a clinical trial experience.
Extended release metoprolol succinate is an effective and well-tolerated treatment for hypertension in children aged 6-16 years.
RCT
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