What is the half life of metoprolol
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Half-Life of Metoprolol: Key Insights from Research
Introduction to Metoprolol Half-Life
Metoprolol is a selective beta1-adrenoceptor antagonist commonly used to treat conditions such as hypertension, angina, and arrhythmias. Understanding its half-life is crucial for optimizing dosing regimens and ensuring effective therapeutic outcomes.
General Half-Life Range of Metoprolol
The half-life of metoprolol varies depending on several factors, including the formulation and patient-specific variables. Generally, the elimination half-life of metoprolol in healthy individuals ranges from approximately 3 to 6 hours2 3 4 6 9. This range is consistent across different studies, indicating a relatively short duration of action for the drug.
Influence of Formulation on Half-Life
The formulation of metoprolol can significantly impact its pharmacokinetics. For instance, controlled-release formulations are designed to extend the drug's duration of action. In one study, the half-life of metoprolol in a controlled-release formulation was found to be around 4 to 6 hours, which aligns with the typical range observed for immediate-release formulations1 7.
Impact of Co-Administered Drugs
The half-life of metoprolol can be influenced by the co-administration of other drugs. For example, when metoprolol was combined with ranitidine, its elimination half-life was prolonged from 3-9 hours to approximately 6 hours2. This suggests that drug interactions can alter the pharmacokinetic profile of metoprolol, necessitating careful consideration in polypharmacy scenarios.
Variability in Special Populations
The half-life of metoprolol can vary in special populations, such as patients with hepatic cirrhosis or those undergoing dialysis. In patients with hepatic cirrhosis, the elimination half-life was observed to be longer, averaging around 7.2 hours compared to 4.2 hours in healthy controls5. Similarly, in dialysis patients, the half-life of metoprolol's metabolites was prolonged, indicating altered drug clearance in these individuals8.
Conclusion
In summary, the half-life of metoprolol typically ranges from 3 to 6 hours in healthy individuals, but this can be extended in certain formulations and special populations. Understanding these variations is essential for tailoring treatment plans to achieve optimal therapeutic outcomes.
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Most relevant research papers on this topic
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 StudySulphasalazine induced selective IgA deficiency in rheumatoid arthritis.
Combining metoprolol and atenolol with ranitidine prolongs the elimination half life and increases the peak plasma metoprolol concentration by 33%, but does not significantly affect beta-blockade inhibition.
Non-RCTPharmacokinetic 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-RCT
Highly CitedBioavailability 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-RCTPharmacokinetics 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-RCTPlasma 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 CitedFormulation 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.
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 StudyPlasma 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-RCTPharmacokinetic 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-RCT
Animal Study