Meta-analysis of Trials Comparing β-Blockers, Calcium Antagonists, and Nitrates for Stable Angina

Abstract

beta-Blockers provide similar clinical outcomes and are associated with fewer adverse events than calcium antagonists in randomized trials of patients who have stable angina.

Mutation of Important Amino Acid Residue of Asp104Lys in Human .BETA.1-Adrenergic Receptor Triggers Functional and Constitutive Inactivation

“…Those ligands are known as inverse agonist, given that they have the opposite effect of agonists. Therefore, b-antagonists are used clinically to reduce heart rate and force of contraction in hypertension, angina and acute myocardial infarction by direct blocking endogenous catecholamine activity, [11][12][13] implying that inverse agonists may have preferred therapeutic applications in the pathophysiology of several cardiovascular diseases.In all seven transmembrane helix (TMH) of GPCRs it appears that the general mechanism of activation involves disruption of intramolecular constraints, leading to TMH movement and formation of new interactions, which stabilize the active state of the receptor. [14][15][16][17][18][19][20][21][22][23][24][25][26][27] The aspartic acid at position 104 in TMH II of the human b 1 -AR is conserved in all b-adrenergic 28-31) , a-adrenergic receptor 32) and also muscarinic cholinergic receptors, [33][34][35] which may take part in an ionic interaction with amino group containing catecholamines, whose disruption of interaction makes the receptor active conformation state.…”

“…Those ligands are known as inverse agonist, given that they have the opposite effect of agonists. Therefore, b-antagonists are used clinically to reduce heart rate and force of contraction in hypertension, angina and acute myocardial infarction by direct blocking endogenous catecholamine activity, [11][12][13] implying that inverse agonists may have preferred therapeutic applications in the pathophysiology of several cardiovascular diseases.…”

Long term medical treatment of stable coronary disease

“…Even in the absence of perceived and absolute contraindications, the use of β-blockers in patients with established CAD remains low 3. In a large meta-analysis, β-blockers were found to have similar efficacy to calcium channel blockers for angina relief, but were associated with fewer adverse events 4. Potential side effects of β-blockers include impaired sexual function, reduced exercise capacity, bradycardia and generalised fatigue.…”

Drug efficacy in treating stable angina pectoris: a protocol for network meta-analysis of randomised controlled trials

“…Available meta-analysis of randomised and crossover trials comparing BBs, CCBs and nitrates suggested that BBs provide similar clinical outcomes and are associated with fewer adverse events (AEs) than CCBs for patients with stable angina pectoris 4. Meta-analysis of efficacy of monotherapy compared with combined antianginal drugs for treating stable angina pectoris suggested that the combined therapy with CCBs and BBs is more effective than monotherapy 5.…”