Use of carvedilol in hypertension: an update

Abstract

β-blockers are effective antihypertensive agents and, together with diuretics, have been the cornerstone of pioneering studies showing their benefits on cardiovascular morbidity and mortality as a consequence of blood pressure reduction in patients with hypertension. However, evidence from recent meta-analyses have demonstrated no benefit afforded by atenolol compared with placebo in risk of mortality, myocardial infarction, or stroke, and a higher risk of mortality and stroke with atenolol/propranolol compared with other antihypertensive drug classes. Thus, the effect of these agents on cardiovascular morbidity and mortality in hypertensive patients, especially their use in uncomplicated hypertension, has remained largely controversial. However, it is recognized that the clinical studies used in these meta-analyses were mainly based on the older second-generation β-blockers, such as atenolol and metoprolol. Actually, considerable heterogeneity in, eg, pharmacokinetic, pharmacological, and physicochemical properties exists across the different classes of β-blockers, particularly between the second-generation and newer third-generation agents. Carvedilol is a vasodilating noncardioselective third-generation β-blocker, without the negative hemodynamic and metabolic effects of traditional β-blockers, which can be used as a cardioprotective agent. Compared with conventional β-blockers, carvedilol maintains cardiac output, has a reduced prolonged effect on heart rate, and reduces blood pressure by decreasing vascular resistance. Studies have also shown that carvedilol exhibits favorable effects on metabolic parameters, eg, glycemic control, insulin sensitivity, and lipid metabolism, suggesting that it could be considered in the treatment of patients with metabolic syndrome or diabetes. The present report provides an overview of the main clinical studies concerning carvedilol administered as either monotherapy or in combination with another antihypertensive or more frequently a diuretic agent, with particular focus on the additional benefits beyond blood pressure reduction.

Potential Role of Carvedilol in the Cardiac Immune Response Induced by Experimental Infection with Trypanosoma cruzi

“…The third generation of beta-blocker, the carvedilol, has acquired a prominent role in different types of treatments such as antihypertensive [ 21 ], heart failure [ 22 ], and thrombosis [ 23 ], in addition to its high antioxidant activity [ 24 ], and improvements were made in left ventricular ejection fractions [ 25 – 27 ]. Some studies have shown that carvedilol besides the previously described and widely discussed effects also displays an immunomodulatory activity [ 26 , 28 , 29 ].…”

Mechanism of testicular protection of carvedilol in streptozotocin-induced diabetic rats

“…[ 3 ] Carvedilol is α 1 /β-adrenoceptors blocker used in the treatment of hypertension and congestive heart failure. [ 4 ] Despite that β-blockers are prescribed cautiously to diabetics due to undesirable effects on glucose control and insulin sensitivity, carvedilol is not associated with such effects. [ 5 ] Contrarily, carvedilol treatment ameliorates signs of diabetes in hypertensive patients[ 6 ] and have beneficial effects compared with other β-blockers.…”

Retrospective evaluation of adverse drug reactions induced by antihypertensive treatment

“…[ 23 ] Carvedilol is a nonselective beta-blocker with vasodilatory effects that are thought to be due to its ability to concurrently block both alpha- and beta-receptors. [ 24 ] In our study, we have documented that carvedilol induced ADRs in nine patients, commonly bradycardia. The Naranjo score indicated a probable relationship between antihypertensive drugs and ADRs in 92% of the patients, although due to the Ethics Agreement, we were unable to perform a re-challenge.…”