Metoprolol extended release dosage
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Metoprolol Extended Release Dosage: Insights from Recent Research
Introduction to Metoprolol Extended Release (ER)
Metoprolol, a beta1-selective adrenergic blocker, is widely used in the management of hypertension, angina pectoris, and chronic heart failure. The extended-release (ER) formulation of metoprolol succinate is designed to provide a consistent therapeutic effect over a 24-hour period, improving patient compliance and maintaining stable plasma drug levels.
Dosage Efficacy in Hypertensive Children
A clinical trial evaluated the efficacy and safety of ER metoprolol in children aged 6 to 16 years with hypertension. The study randomized patients to receive either a placebo or ER metoprolol at doses of 0.2 mg/kg, 1.0 mg/kg, or 2.0 mg/kg. Results indicated significant reductions in systolic blood pressure (SBP) at the 1.0 and 2.0 mg/kg doses and in diastolic blood pressure (DBP) at the 2.0 mg/kg dose compared to placebo, demonstrating a dose-response relationship .
Pharmacokinetics and Pharmacodynamics in Adults
A randomized, cross-over trial compared the pharmacokinetics (PK) and pharmacodynamics (PD) of brand-name versus generic formulations of metoprolol ER in adults with hypertension. The study found that while the area under the concentration-time curve (AUC) and maximum concentration (Cmax) were similar across formulations, the time to maximum concentration (Tmax) varied significantly. Despite these differences, 24-hour blood pressure and heart rate measurements were consistent across all formulations, suggesting therapeutic equivalence .
Metoprolol ER in Chronic Heart Failure
The Metoprolol CR/XL Randomised Intervention Trial in Congestive Heart Failure (MERIT-HF) demonstrated that metoprolol ER significantly reduced all-cause mortality and sudden death in patients with chronic heart failure. The study involved titrating doses from 12.5 to 25 mg once daily up to a target of 200 mg once daily. The findings highlighted the drug's efficacy in improving survival and clinical status in patients with mild to moderate heart failure 34.
Pharmacokinetic Considerations
ER metoprolol succinate provides a near-constant release of the drug over 20 hours, independent of food intake and gastrointestinal pH. This results in stable plasma concentrations and consistent beta1-blockade over 24 hours, which is beneficial for maintaining therapeutic effects and reducing side effects associated with peak plasma levels .
Bioequivalence in Different Populations
A study on healthy Chinese subjects under fasting and fed conditions confirmed the bioequivalence of test and reference metoprolol ER tablets. Both formulations were well tolerated, and the pharmacokinetic parameters fell within the acceptable bioequivalence range, ensuring consistent therapeutic outcomes .
Comparison with Immediate-Release Formulations
In patients with suspected acute myocardial infarction, metoprolol ER 200 mg once daily provided more uniform beta-blockade and lower peak plasma levels compared to multiple doses of immediate-release (IR) metoprolol. This suggests that ER formulations may offer better control of heart rate and reduced variability in drug levels .
Conclusion
Metoprolol ER is an effective and well-tolerated option for managing hypertension, chronic heart failure, and other cardiovascular conditions. Its extended-release formulation ensures stable plasma concentrations, improving therapeutic outcomes and patient compliance. Dosage adjustments based on clinical response and patient characteristics are essential to maximize benefits and minimize adverse effects.
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