Metoprolol drug classification

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Metoprolol Drug Classification: Beta-Blocker and Biopharmaceutics Classification System (BCS) Reference

Beta-Blocker Drug Class: Cardiovascular Use

Metoprolol is classified as a beta-adrenoceptor antagonist, commonly known as a beta-blocker. It is widely prescribed for the treatment of various cardiovascular conditions, including hypertension, coronary artery disease, and heart failure. Metoprolol works by blocking beta-adrenergic receptors, which helps to lower heart rate and blood pressure, making it effective in managing these conditions Anikin2013Koch-Weser1979.

Biopharmaceutics Classification System (BCS): High Permeability Reference

Metoprolol is also significant in pharmaceutical sciences as a reference compound for the Biopharmaceutics Classification System (BCS). The BCS categorizes drugs based on their aqueous solubility and intestinal permeability, which are important for predicting drug absorption and bioavailability. Metoprolol is used as the benchmark for the high/low permeability boundary in this system Kasim2004Dahan2013Takagi2006+2 MORE.

BCS Class 1: High Solubility and High Permeability

Metoprolol is considered a BCS Class 1 drug, meaning it has both high solubility and high permeability. This classification is supported by studies showing that metoprolol dissolves easily in water and is well absorbed through the intestinal wall. As a result, immediate-release oral products containing metoprolol are likely to be bioequivalent under various conditions, including when taken with food Kasim2004Dahan2013Takagi2006+1 MORE. This high solubility and permeability make metoprolol a model drug for evaluating the performance of other oral medications.

Pharmacokinetics and Metabolism

Metoprolol is predominantly metabolized by the liver enzyme CYP2D6. Genetic differences in this enzyme can affect how quickly or slowly metoprolol is broken down in the body, which can influence drug levels and effectiveness in different individuals . However, these genetic differences do not change its overall drug classification as a beta-blocker or its role as a BCS reference compound.

Conclusion

Metoprolol is classified as a beta-blocker used for cardiovascular diseases and is a key reference drug in the Biopharmaceutics Classification System due to its high solubility and high permeability. Its role as a BCS Class 1 drug and as a permeability benchmark makes it important for both clinical use and pharmaceutical development Kasim2004Dahan2013Takagi2006+4 MORE.

Sources and full results

Most relevant research papers on this topic

Molecular properties of WHO essential drugs and provisional biopharmaceutical classification.

High-solubility drugs on the WHO Essential Drug List can be reliably classified using in vitro dissolution tests, ensuring clinical performance of these products.

Highly Cited

2004·

847citations

·N. A. Kasim et al.

Molecular pharmaceutics·

DOI

Purely in silico BCS classification: science based quality standards for the world's drugs.

Simple in silico methods can accurately estimate permeability and solubility of top-selling oral drugs, with CLogP producing the best correlation to experimental values.

Highly Cited

2013·

75citations

·A. Dahan et al.

Molecular pharmaceutics·

DOI

A provisional biopharmaceutical classification of the top 200 oral drug products in the United States, Great Britain, Spain, and Japan.

More than 55% of oral drug products in the top 200 in the US, UK, Spain, and Japan are classified as high-solubility drugs, suggesting in vivo bioequivalence can be assured with a less expensive in vitro dissolution test.

Highly Cited

2006·

589citations

·T. Takagi et al.

Molecular pharmaceutics·

DOI

Clinico-pharmacological aspects of metoprolol use

Metoprolol is a common prescription drug for treating various cardiovascular conditions, including hypertension, coronary artery disease, and heart failure.

2013·

0citations

·G. Anikin et al.

DOI

IMPLICATIONS OF CYP2D6 POLYMORPHISMS FOR THERAPEUTIC DRUG MONITORING IN PATIENTS WITH HYPERTENSION

CYP2D6 genotype influences metoprolol serum concentrations, but does not affect the classification of non-adherence in hypertensive patients.

Observational StudyVery Rigorous Journal

2022·

0citations

·L. Halvorsen et al.

Journal of Hypertension·

DOI

Drug therapy: metoprolol.

Metoprolol is a beta-blocker approved for treating hypertension, the first systemic -blocker to be approved in the United States since propranolol in 1967.

Highly Cited

1979·

104citations

·J. Koch-Weser

The New England journal of medicine·

DOI

Intestinal permeability study of minoxidil: assessment of minoxidil as a high permeability reference drug for biopharmaceutics classification.

Minoxidil may be an acceptable reference drug for high permeability classification, but its higher jejunal permeability than metoprolol may raise the permeability criteria for BCS classification.

In Vitro Study

2015·

23citations

·Makoto Ozawa et al.

Molecular pharmaceutics·

DOI

The effect of food on the relative bioavailability of rapidly dissolving immediate-release solid oral products containing highly soluble drugs.

Rapidly dissolving immediate-release solid oral products containing BCS class I drugs are likely to be bioequivalent under fed conditions, and BCS class III drugs may have the potential to be bioequivalent under fed conditions.

Non-RCT

2004·

39citations

·Lawrence X. Yu et al.

Molecular pharmaceutics·

DOI

The low/high BCS permeability class boundary: physicochemical comparison of metoprolol and labetalol.

Both metoprolol and labetalol are not optimal low/high-permeability class boundary standards, as they both exhibit significant segmental-dependent permeability in the gastrointestinal tract.

In Vitro Study

2014·

68citations

·Moran Zur et al.

Molecular pharmaceutics·

DOI

Metoprolol Induced Psoriasis: A Case Report

Metoprolol, an antihypertensive drug, may cause chronic plaque psoriasis with a "probable" causal relationship and a "moderate" severity adverse reaction.

Case Report

2019·

1citation

·Syed Z. Inamdar et al.

Indian Journal of Pharmacy Practice·

DOI

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