Dose-related effects of metoprolol on heart rate and pharmacokinetics in heart failure

Andersson, Bert; Åberg, Jan; Lindelöw, Björn; Täng, Margareta Scharin; Wikstrand, John

doi:10.1054/jcaf.2001.28230

Cited by 21 publications

(14 citation statements)

References 18 publications

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“…The results from this study, which for the first time compared once daily metoprolol CR/XL 200 mg with multiple dosing of metoprolol IR 50 and 100 mg in patients with acute myocardial infarction, are in agreement with pharmacokinetic results from studies in healthy subjects [16] and in heart failure patients [17]. …”

Section: Discussionsupporting

confidence: 85%

A Pharmacokinetic and Pharmacodynamic Comparison of Immediate-Release Metoprolol and Extended-Release Metoprolol CR/XL in Patients with Suspected Acute Myocardial Infarction: A Randomized, Open-Label Study

Karlson

Dellborg²,

Gullestad³

et al. 2013

Cardiology

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Background: Previous metoprolol studies in myocardial infarction patients were performed with immediate-release (IR) metoprolol. This study aims to evaluate if extended-release metoprolol CR/XL once daily gives a similar β-blockade over 24 h compared to multiple dosing of metoprolol IR. Methods: After 2 days of routine metoprolol treatment, 27 patients with suspected acute myocardial infarction were randomized to open-label treatment with metoprolol IR (50 mg four times daily or 100 mg twice daily) or metoprolol CR/XL 200 mg once daily for 3 days. Results: Metoprolol CR/XL 200 mg once daily gave more pronounced suppression of peak heart rate, with lower peak and less variation in peak to trough plasma levels. There were no differences in AUC between the CR/XL and IR formulations, although the trough plasma metoprolol levels were comparable for metoprolol CR/XL 200 mg once daily and metoprolol IR 50 mg four times daily, but lower for metoprolol IR 100 mg twice daily. Both treatments were well tolerated. Conclusions: Metoprolol CR/XL 200 mg once daily showed lower peak and less variation in peak to trough plasma levels compared to multiple dosing of metoprolol IR with the same AUC. This was accompanied by a more uniform β-blockade over time, which was reflected by heart rate, and a more pronounced suppression of peak heart rate with similar tolerability. This suggests metoprolol CR/XL may be used as an alternative to metoprolol IR in patients with myocardial infarction.

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Section: Discussionsupporting

confidence: 85%

A Pharmacokinetic and Pharmacodynamic Comparison of Immediate-Release Metoprolol and Extended-Release Metoprolol CR/XL in Patients with Suspected Acute Myocardial Infarction: A Randomized, Open-Label Study

Karlson

Dellborg²,

Gullestad³

et al. 2013

Cardiology

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“…When compared to atenolol (50 mg once daily) over a 24-hour interval, metoprolol CR/XL (100 mg once daily) shows a more even plasma concentration, with lower fluctuation ratio and longer time period of concentration higher than 50% of maximum concentration [36]. In addition, the low peak plasma concentration produced by metoprolol CR/XL may lead to higher β 1 -selectivity than equivalent doses of atenolol [30], while cardioselectivity is maintained up to dosages of 200 mg of metoprolol CR/XL [37, 38]. …”

Section: Discussionmentioning

confidence: 99%

Atenolol Is Inferior to Metoprolol in Improving Left Ventricular Function and Preventing Ventricular Remodeling in Dogs with Heart Failure

Zacà¹,

Rastogi²,

Mishra³

et al. 2008

Cardiology

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Objectives: β-Blockers are standard therapy for patients with heart failure (HF). This study compared the effects of chronic monotherapy with 2 different β₁-selective adrenoceptor blockers, namely atenolol and metoprolol succinate, on left ventricular (LV) function and remodeling in dogs with coronary microembolization-induced HF [LV ejection fraction (EF) 30–40%]. Methods: Twenty HF dogs were randomized to 3 months of therapy with atenolol (50 mg once daily, n = 6), metoprolol succinate (100 mg, once daily, n = 7) or to no therapy (control, n = 7). LV EF and volumes were measured before initiating therapy and after 3 months of therapy. The change (Δ) in EF and volumes between measurements before and after therapy was calculated and compared among study groups. Results: In controls, EF decreased and end-systolic volume increased. Atenolol prevented the decrease in EF and the increase in ESV. In contrast, metoprolol succinate significantly increased EF and decreased end-systolic volume. ΔEF was significantly higher and Δend-systolic volume significantly lower in metoprolol succinate-treated dogs compared to atenolol-treated dogs (EF: 6.0 ± 0.86% vs. 0.8 ± 0.85%, p < 0.05; end-systolic volume: –4.3 ± 0.81 ml vs. –1 ± 0.52 ml, p <0.05). Conclusions: In HF dogs, chronic therapy with atenolol does not elicit the same LV function and remodeling benefits as those achieved with metoprolol succinate.

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“…Carvedilol blocks beta 1 ‐, beta 2 ‐, and alpha 1 ‐adrenergic receptors, whereas metoprolol selectively blocks beta 1 ‐adrenergic receptors. The carvedilol formulation should be taken every 12 hours, whereas a single dose of CR metoprolol antagonizes adrenergic activity for 24 hours 6 . Whether these or other pharmacological differences translate to differences in therapeutic outcomes in practice has not been established.…”

mentioning

confidence: 99%

Carvedilol Versus Controlled‐Release Metoprolol for Elderly Veterans with Heart Failure

Rector

Anand

Nelson

et al. 2008

J American Geriatrics Society

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Doses of beta-blockers being prescribed to predominantly elderly veterans with heart failure were much lower than proven doses. Whether efforts to increase doses can improve the effectiveness of beta-blocker therapy warrants further study. At the prescribed doses, CR metoprolol was associated with better survival than carvedilol, although unmeasured confounding variables might explain the observed difference in survival.

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Dose-related effects of metoprolol on heart rate and pharmacokinetics in heart failure

Cited by 21 publications

References 18 publications

A Pharmacokinetic and Pharmacodynamic Comparison of Immediate-Release Metoprolol and Extended-Release Metoprolol CR/XL in Patients with Suspected Acute Myocardial Infarction: A Randomized, Open-Label Study

A Pharmacokinetic and Pharmacodynamic Comparison of Immediate-Release Metoprolol and Extended-Release Metoprolol CR/XL in Patients with Suspected Acute Myocardial Infarction: A Randomized, Open-Label Study

Atenolol Is Inferior to Metoprolol in Improving Left Ventricular Function and Preventing Ventricular Remodeling in Dogs with Heart Failure

Carvedilol Versus Controlled‐Release Metoprolol for Elderly Veterans with Heart Failure

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