Metoprolol pharmacological classification
Pro Research Analysisby 
Searched over 200M research papers
Metoprolol Pharmacological Classification: Beta-Blocker Drug Class
Metoprolol is classified as a beta-blocker, specifically a selective beta-1 adrenergic receptor antagonist. This means it primarily blocks the beta-1 receptors found in the heart, reducing the effects of adrenaline and noradrenaline on cardiac tissue. This action leads to a decrease in heart rate, cardiac output, and blood pressure, making metoprolol effective in treating various cardiovascular conditions such as hypertension, angina, and heart failure 12.
Beta-1 Selectivity and Mechanism of Action
Metoprolol is known for its high selectivity for beta-1 adrenergic receptors compared to beta-2 receptors. This selectivity allows it to inhibit the cardiac stimulant effects of catecholamines like noradrenaline and isoprenaline, while having minimal impact on the vasodilator and bronchodilator effects mediated by beta-2 receptors. As a result, metoprolol is less likely to cause bronchoconstriction, making it safer for patients with respiratory issues compared to non-selective beta-blockers .
Clinical Uses in Cardiovascular Disease
Metoprolol is widely prescribed for the management of hypertension, coronary artery disease, and heart failure. Its ability to lower blood pressure and reduce cardiac workload makes it a cornerstone therapy in these conditions. The drug is available in different formulations, such as metoprolol tartrate and metoprolol succinate, which are used based on the clinical scenario and desired duration of action .
Pharmacokinetics and Metabolism
Metoprolol is completely absorbed after oral administration and undergoes significant first-pass metabolism in the liver, primarily by the CYP2D6 enzyme. The drug’s elimination half-life is typically 3–4 hours. Genetic differences in CYP2D6 can significantly affect metoprolol metabolism, leading to variations in drug levels and response among individuals. Some people with certain CYP2D6 genotypes may metabolize metoprolol more slowly, resulting in higher drug exposure and potentially greater effects or side effects 35.
Conclusion
In summary, metoprolol is a cardioselective beta-blocker, classified pharmacologically as a beta-1 adrenergic receptor antagonist. Its selectivity, clinical effectiveness in cardiovascular diseases, and metabolism via CYP2D6 are key features that define its pharmacological profile 1235.
Sources and full results
Most relevant research papers on this topic