Metoprolol succinate or tartrate
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Comparison of Metoprolol Succinate and Metoprolol Tartrate in Clinical Applications
Introduction to Metoprolol Variants
Metoprolol, a selective β1-adrenergic antagonist, is widely used in the treatment of various cardiovascular conditions, including hypertension, heart failure, and angina. It is available in two primary formulations: metoprolol tartrate (MT) and metoprolol succinate (MS). While both forms are effective, they differ in their pharmacokinetic properties and clinical applications.
Hemodynamic Effects in Heart Failure
Hemodynamic Benefits and Adverse Effects
Both metoprolol tartrate and succinate have been shown to produce significant hemodynamic benefits in patients with congestive heart failure. A study comparing the two formulations found that long-term therapy with either drug resulted in similar improvements in functional, exercise, and hemodynamic parameters1. However, upon readministration during chronic therapy, both formulations exhibited parallel adverse hemodynamic effects, such as decreased cardiac index and increased systemic vascular resistance1.
Cardiac Function in Chronic Heart Failure
Heart Rate and Cardiac Function
In patients with chronic congestive heart failure, metoprolol succinate sustained-release tablets were found to decrease the average heart rate more effectively than metoprolol tartrate tablets (64.0 ± 5.4 vs. 69.5 ± 7.6, p < 0.05)2. Despite this difference in heart rate reduction, both formulations showed no significant differences in other cardiac and renal function parameters, such as left ventricular end-diastolic diameter (LVDd), ejection fraction (EF), blood urea nitrogen (BUN), and creatinine (Crea)2.
Efficacy in COPD with Heart Failure
Therapeutic Efficacy and Safety
In patients with chronic obstructive pulmonary disease (COPD) complicating chronic heart failure, metoprolol succinate was found to be more effective in improving cardiac function compared to metoprolol tartrate4. Both formulations, however, showed similar safety profiles and no significant differences in lung function or quality of life scores4.
Acute Myocardial Infarction
Heart Rate Reduction
In the context of acute myocardial infarction, both metoprolol succinate and tartrate were effective in reducing heart rates. However, the degree and trend of heart rate reduction over the first 72 hours were not significantly different between the two formulations6.
Structural and Pharmacokinetic Differences
Solid-State Behavior and Drug Release
The solid-state structures of metoprolol tartrate and succinate exhibit notable differences. Metoprolol succinate shows a slightly greater cohesive energy and undergoes reversible anisotropic lattice expansion/contraction upon temperature changes, whereas metoprolol tartrate expands/contracts isotropically and forms an amorphous solid upon cooling from the melt5. These differences can influence the drug's release profile and stability.
Clinical and Economic Considerations
Antianginal Efficacy and Pharmacoeconomics
In patients with vasospastic angina, metoprolol succinate demonstrated a significant reduction in the incidence of clinically significant angina attacks compared to metoprolol tartrate10. However, there were no significant differences in the rates of adverse cardiovascular events, such as myocardial infarction or stroke, between the two groups. Metoprolol tartrate, on the other hand, offers pharmacoeconomic advantages due to its lower cost10.
Conclusion
Both metoprolol succinate and tartrate are effective in managing various cardiovascular conditions, with some differences in their hemodynamic effects, heart rate reduction, and structural properties. Metoprolol succinate may offer advantages in terms of heart rate control and antianginal efficacy, while metoprolol tartrate provides cost benefits. Clinicians should consider these factors when choosing the appropriate formulation for their patients.
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