Carvedilol

Frishman, William H.

doi:10.1056/nejm199812103392407

Cited by 222 publications

(155 citation statements)

References 67 publications

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“…On a quantitative basis, the a-adrenoceptor antagonistic activity of arotinolol is considerably weaker (15) . Moreover, these pharmacological properties are similar to those of carvedilol (32) in that the ratio of a1 to fl-adrenoceptor blockade for carvedilol is 1:10, and for arotinolol is 1:8. Unfortunately, compared to the cumulative evidence supporting the beneficial effects of carvedilol in patients with heart failure (33), and animals (34) with renal impairment, the clinical and experimental data on arotinolol are lacking.…”

Section: Discussionsupporting

confidence: 57%

Nifedipine and Arotinolol in Combination for Accelerated-Malignant Hypertension: Results of One Year Follow-Up.

et al. 1999

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The effects of a combined therapy with a calcium channel antagonist and a$-blocker in patients with accelerated-malignant hypertension on blood pressure and renal function were examined. Thirteen patients presented with the clinical features of malignant hypertension (diastolic blood pressure >130 mmHg, retinal damage and progressive renal failure) at our hospital, over the 3 yr period from 1995 to 1997. These patients were treated with both a calcium antagonist, 60-80 mg/d dose of long acting nifedipine, and an a/9-blocker, 20 mg/d dose of arotinolol, for over 12 mo. At admission, the average blood pressure of the patients was 233 ± 8/144 ± 3 mmHg. The level of serum creatinine in these patients was 6.2 ± 1.0 mg/dl. Intermittent hemodialysis therapy was introduced in 7 patients. Three days after treatment, blood pressure decreased to 162 ± 4/ 102 ± 4 mmHg. A month later, blood pressure decreased to 148 ± 3/89 ± 2 mmHg and serum creatinine levels were 3.6 ± 0.4 mg/dl. Renal function in these patients improved, and they completely recovered from renal dysfunction, allowing withdrawal of haemodialysis therapy. One year later, the blood pressure in all of these patients was well controlled and no further renal deterioration was observed, except in one patient. Despite the reduction in blood pressure, one patient was on hemodialysis three times a week after 8 mo of treatment. From these finding, it is concluded that combination therapy with a calcium antagonist and ai9-blocker is effective in both the reduction of highly elevated blood pressure and protection of the kidneys, resulting in amelioration of accelerated-malignant hypertension. (Hypertens Res 1999; 22: 75-'80)

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Section: Discussionsupporting

confidence: 57%

Nifedipine and Arotinolol in Combination for Accelerated-Malignant Hypertension: Results of One Year Follow-Up.

et al. 1999

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“…Milligram for milligram, carvedilol is 2-4 times more potent than propranolol as a beta-receptor antagonist. 18 Carvedilol further has antioxidant activity, which may be of interest in patients with cirrhosis, but this possible benefit has not been studied. Figure 1 summarizes the mechanism by which carvedilol decreases portal pressure in patients with cirrhosis.…”

Section: Carvedilolmentioning

confidence: 99%

Carvedilol for Portal Hypertension in Patients With Cirrhosis

Bosch

2010

Hepatology

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A 48-year-old male with hepatitis C-related cirrhosis is found on endoscopy to have large esophageal varices with red signs. He has never previously had variceal bleeding, and there is no evidence of hepatic encephalopathy. He does have mild ascites. Comorbidity includes diabetes which has been present for many years and is well-controlled on a stable dose of insulin. He has no cardiopulmonary disease. The hemoglobin is 12.4 g/dL, white blood cell count is 6800/mm 3 , and platelets are 112 Â 10 9 /L. Serum bilirubin is 1.8 mg/ dL, creatinine is 1.2 mg/dL, international normalized ratio is 1.3, and the serum albumin is 3.5 g/dL. The electrocardiogram and chest x-ray are normal. The ultrasound examination does not show portal vein thrombosis or hepatocellular carcinoma.What is the role of carvedilol in the prevention of variceal bleeding in this patient? How will the dose of carvedilol be adjusted and how is the patient to be monitored for adverse drug events? When would carvedilol be preferred over nadolol or propranolol? Would the approach be different if the patient was of Child-Pugh class C cirrhosis? The ProblemPortal hypertension is an almost unavoidable complication of cirrhosis, and provides the driving force for most of its complications, such as esophageal and gastric varices, variceal bleeding, portal hypertensive gastropathy, ascites, spontaneous bacterial peritonitis, hepatorenal syndrome, thrombopenia, leukopenia and anemia, and portal-systemic encephalopathy.1 Recent studies have shown that for these complications to develop, the portacaval pressure gradient-evaluated clinically by the hepatic venous pressure gradient (HVPG)-should increase above 10 mm Hg and should be above 12 mm Hg for variceal bleeding. 2,3The prevalence of varices is about 40% in asymptomatic compensated patients.2 Development of varices follows an incidence of approximately 6% per year. The incidence is nearly double in patients with a baseline HVPG >10 mm Hg, who therefore represent a high-risk group.2 These patients are also at higher risk of developing decompensation (ascites, bleeding, jaundice, encephalopathy) and hepatocellular carcinoma. 4,5 Because of this, there is a great interest in strategies to revert portal hypertension, since these would prevent portal hypertension-related complications, clinical decompensation, and death. The benefit of reduction of HVPG has actually been proven for patients exhibiting a ''good hemodynamic response'' to nonselective beta-adrenergic blockers; i.e., those who exhibit a decrease in HVPG > 20% of baseline or to values below 12 mm Hg during continued therapy, 6,7 or who show a decrease in HVPG >10% of baseline 20 minutes after an intravenous infusion of propranolol. 8,9 Besides the increased intravascular pressure, the risk of bleeding from varices is further influenced by other factors, such as the diameter of the varices and the thickness of the variceal wall.10 These factors are interrelated by Laplace's law in the concept of wall tension (t), according to which: t ¼ variceal tran...

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“…At high doses, it blocks the entry of calcium. Milligram per milligram, it is two to four times more potent than propranolol as ß antagonist [16,17]. In the U.S. Carvedilol Heart Failure Program [18], it is used in the treatment of heart failure, and it is also indicated for high blood pressure and myocardial ischemia.…”

Section: Most Frequently Used Beta-blockersmentioning

confidence: 99%

Nebivolol: Does the key lie in β3 agonism?

Arazi¹,

Gonzalez²

2017

Vascul Dis Ther

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Beta-blockers are drugs indicated in the treatment of multiple cardiovascular pathologies. The review highlights the mechanisms of action of Nebivolol and its particular potential effect on β3 receptors that increases nitric oxide that may mark very significant differences, which are traduced to benefits in clinical results.Nebivolol has an special place in the treatment of adrenergic hypertension associated with tachycardia and emotional stress, more frequently in young individuals, and may be considered adequate even in patients with glucose and lipid metabolism disorders due to its pleiotropic effect.In patients with heart failure, Nebivolol showed effectiveness and safety in patients over 75 years old.Nebivolol showed a reduction of cardiomyocyte apoptosis and improvement of contractile function through a mechanism related to β3 receptor agonism after an acute coronary syndrome.Because of all these actions Nebivolol should be considered not only a third-generation Beta-blocker.

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Carvedilol

Cited by 222 publications

References 67 publications

Nifedipine and Arotinolol in Combination for Accelerated-Malignant Hypertension: Results of One Year Follow-Up.

Nifedipine and Arotinolol in Combination for Accelerated-Malignant Hypertension: Results of One Year Follow-Up.

Carvedilol for Portal Hypertension in Patients With Cirrhosis

Nebivolol: Does the key lie in β3 agonism?

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