Metoprolol tartrate half life
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Metoprolol Tartrate Half-Life: An Overview
Introduction to Metoprolol Tartrate
Metoprolol tartrate is a selective β1-adrenergic antagonist commonly used to treat cardiovascular conditions such as hypertension, angina, and heart failure. It is known for its rapid absorption and significant first-pass metabolism, which affects its pharmacokinetic properties1 4.
Pharmacokinetics and Half-Life
The elimination half-life of metoprolol tartrate varies slightly depending on the study and the method of administration. Generally, the half-life ranges from 3 to 5 hours. For instance, one study reported a half-life of 3 to 4 hours when administered orally1, while another found it to be approximately 4.0 ± 0.6 hours in healthy volunteers2. In patients with renal impairment, the half-life was observed to be around 4.6 ± 1.2 hours, indicating that renal function does not significantly alter the drug's elimination rate5.
Factors Influencing Half-Life
First-Pass Metabolism
Metoprolol tartrate undergoes extensive first-pass metabolism, which significantly reduces its bioavailability to about 12% when taken orally1. This extensive metabolism can influence the drug's half-life and overall effectiveness.
Renal Function
Studies have shown that renal impairment does not significantly affect the elimination half-life of metoprolol tartrate. Both healthy subjects and patients with renal failure exhibited similar half-lives, suggesting that the drug's clearance is not heavily dependent on renal function5 8.
Smoking and Gender
Research indicates that smoking can increase the steady-state volume of distribution of metoprolol, but it does not significantly affect the half-life, systemic clearance, or bioavailability. Similarly, no significant differences in pharmacokinetic parameters, including half-life, were observed between males and females9.
Modified Release Formulations
Various modified release formulations of metoprolol tartrate have been developed to extend its half-life and improve patient compliance. Slow-release (SR) tablets, for example, have been shown to reduce peak plasma levels and delay the time to reach peak concentration, although the overall area under the plasma concentration curve (AUC) remains similar to that of ordinary tablets2. These formulations aim to provide a more consistent therapeutic effect over a longer period.
Conclusion
The elimination half-life of metoprolol tartrate typically ranges from 3 to 5 hours, with minimal variation due to renal function, smoking, or gender. Modified release formulations can help extend the drug's duration of action, offering potential benefits for patient compliance and therapeutic effectiveness. Understanding these pharmacokinetic properties is crucial for optimizing the clinical use of metoprolol tartrate in treating cardiovascular conditions.
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Most relevant research papers on this topic
Design and Evaluation of Metoprolol Tartrate Containing Buccal Tablets
The formulation FA1 with sodium alginate, Carbopol 934p, and mannitol shows promising potential for buccal metoprolol tartrate administration, demonstrating stable drug content and in vitro dissolution characteristics.
In Vitro StudyComparative bioavailability and effect studies on metoprolol administered as ordinary and slow-release tablets in single and multiple doses.
Slow-release metoprolol tablets have similar bioavailability and pharmacological effects as ordinary tablets, with slower peak plasma levels and slightly higher effects at the end of the dosage interval.
Non-RCTEudragit FS based colonic microparticls of metoprolol tartrate.
Eudragit FS is a suitable polymer for designing pH-dependent microparticles using solvent evaporation technique for the release of metoprolol tartrate in colon, with T2 being an optimum formulation.
In Vitro StudyFORMULATION AND EVALUATION OF TRANSDERMAL PATCHES OF METOPROLOL TARTRATE USING PERMEATION ENHANCERS OF NATURAL AND SYNTHETIC ORIGIN
The developed transdermal patches using basil oil as a penetration enhancer are stable, non-irritating, and show increased efficacy of metoprolol tartrate for hypertension treatment.
In Vitro StudyPharmacokinetic and Pharmacodynamic Properties of Metoprolol in Patients with Impaired Renal Function
Metoprolol's bioavailability and elimination rate remain unchanged in patients with impaired renal function, and its -blocking properties remain unchanged.
Highly CitedDesign and characterization of mouth dissolving tablets of Metoprolol Tartrate
Mouth dissolving tablets of metoprolol tartrate with increased rate of dissolution show no drug interaction and show promising short-term stability.
In Vitro StudyPharmacokinetics and pharmacodynamics of oral and intravenous metoprolol tartrate in clinically healthy horses.
Intravenous and oral metoprolol tartrate in horses have similar pharmacokinetic properties and cardiovascular effects, with sweating as the most common side effect.
RCT
Animal StudyThe Effect of Impaired Renal Function on the Plasma Concentration and Urinary Excretion of Metoprolol Metabolites
Impaired renal function increases the elimination half-life of metoprolol metabolites, but its contribution to the -adrenoceptor blocking effect is negligible.
Non-RCTInfluence of smoking and gender on the disposition kinetics of metoprolol
Cigarette smoking and gender do not significantly affect the pharmacokinetics of metoprolol, with only a larger steady-state volume of distribution observed in smokers.
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