Metoprolol absorption and food interactions

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Metoprolol Absorption and Food Interactions: Key Findings

Food Effects on Metoprolol Bioavailability

Research shows that food can influence the absorption and bioavailability of metoprolol, but the effect depends on the formulation and the specific conditions of administration. In studies with healthy volunteers, taking metoprolol with food generally increased its bioavailability compared to taking it on an empty stomach, although there is significant variation between individuals . This suggests that food can enhance the amount of metoprolol that enters the bloodstream.

Influence of Food on Different Metoprolol Formulations

For metoprolol administered as an Oros (osmotic-controlled release oral delivery system) formulation, food intake did not significantly affect the drug’s absorption. Plasma concentration profiles, peak concentrations, and the time to reach peak levels were nearly identical whether the drug was taken with or without food. About 80-90% of the absorbed dose reached the systemic circulation within 10 hours, regardless of food intake . This indicates that the Oros system provides consistent absorption independent of meals.

Mechanisms Behind Food’s Impact on Absorption

Studies using isolated segments of the human jejunum found that the presence of nutrients in the intestine significantly increased metoprolol absorption—up to four times higher compared to saline solutions without nutrients 56. However, the presence of bile salts did not further enhance absorption. The relationship between the amount of drug absorbed and plasma concentration remained linear, and food did not affect the metabolism of metoprolol 56.

Comparison with Other Drugs and Formulations

Metoprolol, being highly soluble and permeable, is less affected by the increased viscosity of the stomach contents after eating, unlike drugs with limited permeability and absorption restricted to the upper intestine. For metoprolol, changes in the physical properties of the digestive environment due to food do not significantly alter its pharmacokinetic profile .

Clinical Implications

Overall, while food can enhance the absorption of metoprolol in some cases, especially with immediate-release formulations, extended-release systems like the Oros formulation are largely unaffected by food intake. The presence of nutrients in the gut can increase absorption, but this does not appear to saturate the body’s ability to process the drug, nor does it alter its metabolism 1256.

Conclusion

Metoprolol absorption can be increased by food, particularly with immediate-release formulations, but extended-release systems like Oros are not significantly affected by meals. The presence of nutrients in the intestine enhances absorption, but food does not impact the drug’s metabolism. These findings suggest that, depending on the formulation, metoprolol can be taken with or without food, but individual responses may vary.

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Most relevant research papers on this topic

Influence of food on the absorption of metoprolol administered as an Oros drug delivery system to man.

Food intake does not significantly affect the absorption of metoprolol administered as an Oros system to healthy volunteers.

Non-RCT

1985·

11citations

·J. Lecaillon et al.

Enhancement of the bioavailability of propranolol and metoprolol by food

Food intake enhances the bioavailability of propranolol and metoprolol, with significant interindividual variation in their bioavailability.

Non-RCTHighly Cited

1977·

222citations

·A. Melander et al.

Viscosity-mediated negative food effect on oral absorption of poorly-permeable drugs with an absorption window in the proximal intestine: In vitro experimental simulation and computational verification.

Food intake can negatively impact oral absorption of poorly-permeable drugs with limited permeability and a restricted absorption window in the upper intestine.

In Vitro Study

2014·

67citations

·S. Cvijić et al.

Metoprolol‐pridopidine drug–drug interaction and food effect assessments of pridopidine, a new drug for treatment of Huntington's disease

Pridopidine, a metabolism-dependent inhibitor of CYP2D6, may increase systemic levels of drugs metabolized by CYP2D6 when coadministered with metoprolol, but its exposure is unaffected by food conditions.

Non-RCTRigorous Journal

2017·

2citations

·L. Rabinovich‐Guilatt et al.

Investigation of drug absorption from the gastrointestinal tract of man. IV. Influence of food and digestive secretions on metoprolol jejunal absorption.

Nutrients significantly enhance metoprolol jejunal absorption, but bile salts do not enhance drug absorption.

Non-RCT

1985·

9citations

·D. Evard et al.

Investigation of drug absorption from the gastrointestinal tract of man: IV. Influence of food and digestive secretions on the jejunal absorption of metoprolol

Nutrients and digestive secretions significantly enhance the intestinal absorption of metoprolol, but bile salts do not enhance drug absorption.

Non-RCT

1985·

0citations

·D. Evard et al.

A Review of Food–Drug Interactions on Oral Drug Absorption

Food-drug interactions can significantly impact oral drug absorption rates and should be considered when recommending whether a specific drug should be taken with or without food.

Literature ReviewHighly Cited

2017·

163citations

·Jianyuan Deng et al.

The influence of viscosity-enhancing agents on oral absorption of drugs.

Oral absorption of metoprolol and bisoprolol is lowest in PVA solutions, influenced by decreased diffusion and interaction with PVA molecules.

In Vitro Study

2019·

2citations

·Y. Tanaka et al.

Design of a new multiple-unit controlled-release formulation of metoprolol — Metoprolol CR

The new controlled-release formulation of metoprolol CR provides continuous, smooth, and independent drug delivery throughout the day, independent of pH and physiological variables.

2004·

68citations

·A. Sandberg et al.

Minimal Physiologically-Based Pharmacokinetic Modeling of Atenolol and Metoprolol Absorption in Malnourished Rats

Malnutrition significantly alters the absorption of atenolol and metoprolol in rats, leading to increased bioavailability and higher absorption rates in both absorption phases.

Non-RCTAnimal Study

2025·

0citations

·Fatma Kir et al.

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