Half life of metoprolol er

Pro Research Analysisby

Searched over 200M research papers

Analyzed relevant papers

Half-Life of Metoprolol ER: A Comprehensive Overview

Introduction to Metoprolol ER

Metoprolol ER (extended-release) is a beta1-selective adrenergic receptor blocker commonly used to treat hypertension, angina, and heart rhythm disorders. Understanding its pharmacokinetics, particularly its half-life, is crucial for optimizing therapeutic regimens and ensuring effective patient management.

Pharmacokinetics and Half-Life of Metoprolol ER

Absorption and Distribution

Metoprolol is rapidly and completely absorbed after oral administration, with about 40% of the dose reaching systemic circulation due to first-pass metabolism . The drug is extensively distributed to extravascular tissues, with a distribution half-life of approximately 12 minutes .

Elimination Half-Life

The elimination half-life of metoprolol varies depending on the formulation and patient population. For the immediate-release form, the elimination half-life is typically around 3 to 4 hours 128. However, for the extended-release formulation, the half-life is extended to approximately 4 to 6 hours, allowing for once-daily dosing .

Variability in Half-Life

The half-life of metoprolol can vary significantly among different patient populations. For instance, in geriatric patients, the plasma half-life averages about 3.5 hours, which is consistent with findings in younger populations . In patients with hepatic cirrhosis, the half-life can be prolonged to around 7.2 hours due to impaired hepatic metabolism .

Impact of Formulation on Half-Life

The extended-release formulation of metoprolol (Metoprolol ER) is designed to provide a more consistent plasma concentration over a 24-hour period. Studies have shown that the controlled-release formulation maintains therapeutic levels more effectively than multiple daily doses of the immediate-release form . This formulation helps in reducing the frequency of dosing and improving patient compliance.

Conclusion

The half-life of metoprolol ER is generally between 4 to 6 hours, which supports its use in once-daily dosing regimens. This extended half-life, compared to the immediate-release form, offers better management of conditions like hypertension and angina by providing more stable plasma concentrations. Understanding these pharmacokinetic properties is essential for optimizing treatment and improving patient outcomes.

Sources and full results

Most relevant research papers on this topic

Pharmacokinetic studies on the selectiveβ1-receptor antagonist metoprolol in man

Metoprolol is rapidly absorbed and excreted in the urine within 72 hours after oral administration, with a 3-hour elimination half-life for the parent compound and metabolites.

Non-RCTHighly Cited

1974·

118citations

·C. Regårdh et al.

Plasma levels and effect on heart rate and blood pressure of metoprolol after acute oral administration in 12 geriatric patients.

Metoprolol's plasma levels in geriatric patients vary significantly, potentially due to body weight, absorption, and first-pass effects.

Non-RCT

2009·

22citations

·P. Lundborg et al.

Bioavailability and disposition of metoprolol and hydrochlorothiazide combined in one tablet and of separate doses of hydrochlorothiazide.

Metoprolol and hydrochlorothiazide combined in a tablet do not significantly influence each other's bioavailability or time-course, making repeated doses unlikely to cause significant clinical interactions.

Non-RCT

1979·

25citations

·L. Jordö et al.

The Pharmacokinetics of Metoprolol and its Metabolites in Dialysis Patients

Metoprolol's pharmacokinetics in dialysis patients is similar to healthy volunteers, with hepatic metabolism playing a role in its elimination, and its elimination depends on dialysis technique.

Observational Study

1980·

39citations

·K. Seiler et al.

Formulation Development and In-vitro Evaluation of Sustained Release Tablets of Metoprolol Succinate

Metoprolol succinate sustained release tablets formulated using polymers show acceptable physical characteristics and dissolution rates that meet USP specifications.

2021·

1citation

·Priyanka M. Salve et al.

Pharmacokinetic studies of metoprolol-(3-h) in the rat and the dog.

The dog is a better model for human experiments with metoprolol-(3-h) than the rat, as its pharmacokinetic characteristics are similar to those of human patients.

Non-RCTAnimal Study

2009·

25citations

·K. Borg et al.

A comparison of a short half-life marker (low-dose isoniazid), a long half-life pharmacological indicator (low-dose phenobarbitone) and measurements of a controlled release 'therapeutic drug' (metoprolol, Metoros) in reflecting incomplete compliance by volunteers.

Phobarbitone measurements are more effective than isoniazid or metoprolol measurements in reflecting partial compliance over the previous 1 to 4 weeks.

Observational Study

1990·

15citations

·E. Hardy et al.

Plasma levels and effects of metoprolol on blood pressure and heart rate in hypertensive patients after an acute dose and between two doses during long‐term treatment

Metoprolol effectively reduces systolic blood pressure and heart rate in patients with mild hypertension, with both doses showing a linear relationship to plasma concentrations.

Non-RCTHighly Cited

1975·

120citations

·C. Bengtsson et al.

Pharmacokinetics of Metoprolol in Patients with Hepatic Cirrhosis

Impaired liver function does not significantly affect the pharmacokinetics of metoprolol, with total body clearance and half-life related to galactose clearance and serum bilirubin.

Non-RCT

1981·

67citations

·C. Regårdh et al.

Comparison between metoprolol orally osmotic once daily and metoprolol two or three times daily in suppressing exercise-induced and daily myocardial ischemia.

The once daily OROS formulation of metoprolol effectively suppresses daily and exercise-induced ischemia, providing 24-hour coverage and improved patient compliance.

RCT

1996·

5citations

·D. Tzivoni et al.

Try another search

floride toothpaste

tooth decay self-care

what is bronchodilation

how to improve lung capacity

meaning of green house

virgin galactic spaceship 2