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Controlled-release carvedilol in the management of systemic hypertension and myocardial dysfunction.

Frishman WH, Henderson LS, Lukas MA - Vasc Health Risk Manag (2008)

Bottom Line: However, vasodilatory beta-blockers such as carvedilol have a different hemodynamic action that provides the benefits of beta-blockade with the addition of vasodilation resulting from alpha 1-adrenergic receptor blockade.Vasodilation reduces total peripheral resistance, which may produce an overall positive effect on tolerability.Recently, a new, controlled-release carvedilol formulation has been developed that provides the clinical efficacy of carvedilol but is indicated for once-daily dosing.

View Article: PubMed Central - PubMed

Affiliation: Departments of Medicine and Pharmacology, New York Medical College/Westchester Medical Center, Valhalla, NY 10595, USA. william_frishman@nymc.edu

ABSTRACT
Cardiovascular disease is the leading cause of death worldwide. Within the treatment armamentarium, beta-blockers have demonstrated efficacy across the spectrum of cardiovascular disease--from modification of a risk factor (ie, hypertension) to treatment after an acute event (ie, myocardial infarction). Recently, the use of beta-blockers as a first-line therapy in hypertension has been called into question. Moreover, beta-blockers as a class are saddled with a misperception of having poor tolerability. However, vasodilatory beta-blockers such as carvedilol have a different hemodynamic action that provides the benefits of beta-blockade with the addition of vasodilation resulting from alpha 1-adrenergic receptor blockade. Vasodilation reduces total peripheral resistance, which may produce an overall positive effect on tolerability. Recently, a new, controlled-release carvedilol formulation has been developed that provides the clinical efficacy of carvedilol but is indicated for once-daily dosing. This review presents an overview of the clinical and pharmacologic carvedilol controlled-release data.

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Related in: MedlinePlus

Glycosylated hemoglobin (HbA1c) at baseline and each maintenance month by treatment in GEMINI. Reproduced with permission from Bakris GL, Fonseca V, Katholi RE, et al 2004. Metabolic effects of carvedilol vs metoprolol in patients with type 2 diabetes mellitus and hypertension: a randomized controlled trial. JAMA, 292:2227–36. Copyright © 2004, American Medical Association. All Rights Reserved.Note: Data are means ± standard deviations.
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f2-vhrm-4-1387: Glycosylated hemoglobin (HbA1c) at baseline and each maintenance month by treatment in GEMINI. Reproduced with permission from Bakris GL, Fonseca V, Katholi RE, et al 2004. Metabolic effects of carvedilol vs metoprolol in patients with type 2 diabetes mellitus and hypertension: a randomized controlled trial. JAMA, 292:2227–36. Copyright © 2004, American Medical Association. All Rights Reserved.Note: Data are means ± standard deviations.

Mentions: The Glycemic Effects in Diabetes Mellitus: Carvedilol-Metoprolol Comparison in Hypertensives (GEMINI) trial compared the effects of carvedilol IR (6.25 mg to 25 mg twice daily) with metoprolol (50 mg to 200 mg twice daily) on glycemic control and lipid profile in 1235 patients with diabetes and hypertension (Bakris et al 2004). After 5 months of treatment in this randomized, double-blind, parallel-group trial, carvedilol IR did not increase HbA1c (0.02%; p = 0.65), whereas metoprolol significantly increased HbA1c levels from baseline (0.15%; p < 0.001) (Figure 2). Moreover, a greater number of patients withdrew because of worsening glycemic control in the metoprolol group (2.2%) compared with the carvedilol group (0.6%; p = 0.04). These data support the results of an earlier comparison study of metoprolol and carvedilol, which found that insulin sensitivity increased with carvedilol and decreased with metoprolol treatment (Jacob et al 1996).


Controlled-release carvedilol in the management of systemic hypertension and myocardial dysfunction.

Frishman WH, Henderson LS, Lukas MA - Vasc Health Risk Manag (2008)

Glycosylated hemoglobin (HbA1c) at baseline and each maintenance month by treatment in GEMINI. Reproduced with permission from Bakris GL, Fonseca V, Katholi RE, et al 2004. Metabolic effects of carvedilol vs metoprolol in patients with type 2 diabetes mellitus and hypertension: a randomized controlled trial. JAMA, 292:2227–36. Copyright © 2004, American Medical Association. All Rights Reserved.Note: Data are means ± standard deviations.
© Copyright Policy
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC2663448&req=5

f2-vhrm-4-1387: Glycosylated hemoglobin (HbA1c) at baseline and each maintenance month by treatment in GEMINI. Reproduced with permission from Bakris GL, Fonseca V, Katholi RE, et al 2004. Metabolic effects of carvedilol vs metoprolol in patients with type 2 diabetes mellitus and hypertension: a randomized controlled trial. JAMA, 292:2227–36. Copyright © 2004, American Medical Association. All Rights Reserved.Note: Data are means ± standard deviations.
Mentions: The Glycemic Effects in Diabetes Mellitus: Carvedilol-Metoprolol Comparison in Hypertensives (GEMINI) trial compared the effects of carvedilol IR (6.25 mg to 25 mg twice daily) with metoprolol (50 mg to 200 mg twice daily) on glycemic control and lipid profile in 1235 patients with diabetes and hypertension (Bakris et al 2004). After 5 months of treatment in this randomized, double-blind, parallel-group trial, carvedilol IR did not increase HbA1c (0.02%; p = 0.65), whereas metoprolol significantly increased HbA1c levels from baseline (0.15%; p < 0.001) (Figure 2). Moreover, a greater number of patients withdrew because of worsening glycemic control in the metoprolol group (2.2%) compared with the carvedilol group (0.6%; p = 0.04). These data support the results of an earlier comparison study of metoprolol and carvedilol, which found that insulin sensitivity increased with carvedilol and decreased with metoprolol treatment (Jacob et al 1996).

Bottom Line: However, vasodilatory beta-blockers such as carvedilol have a different hemodynamic action that provides the benefits of beta-blockade with the addition of vasodilation resulting from alpha 1-adrenergic receptor blockade.Vasodilation reduces total peripheral resistance, which may produce an overall positive effect on tolerability.Recently, a new, controlled-release carvedilol formulation has been developed that provides the clinical efficacy of carvedilol but is indicated for once-daily dosing.

View Article: PubMed Central - PubMed

Affiliation: Departments of Medicine and Pharmacology, New York Medical College/Westchester Medical Center, Valhalla, NY 10595, USA. william_frishman@nymc.edu

ABSTRACT
Cardiovascular disease is the leading cause of death worldwide. Within the treatment armamentarium, beta-blockers have demonstrated efficacy across the spectrum of cardiovascular disease--from modification of a risk factor (ie, hypertension) to treatment after an acute event (ie, myocardial infarction). Recently, the use of beta-blockers as a first-line therapy in hypertension has been called into question. Moreover, beta-blockers as a class are saddled with a misperception of having poor tolerability. However, vasodilatory beta-blockers such as carvedilol have a different hemodynamic action that provides the benefits of beta-blockade with the addition of vasodilation resulting from alpha 1-adrenergic receptor blockade. Vasodilation reduces total peripheral resistance, which may produce an overall positive effect on tolerability. Recently, a new, controlled-release carvedilol formulation has been developed that provides the clinical efficacy of carvedilol but is indicated for once-daily dosing. This review presents an overview of the clinical and pharmacologic carvedilol controlled-release data.

Show MeSH
Related in: MedlinePlus