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Also referred to as intrinsic sympathomimetic effect, this term is used particularly with beta blockers that can show both agonism and antagonism at a given beta receptor, depending on the concentration of the agent (beta blocker) and the concentration of the antagonized agent (usually an endogenous compound, such as norepinephrine).
Acebutolol is a cardioselective beta-1 blocker which also considered a partial agonist due to its intrinsic sympathomimetic activity (ISA). This means it provides low-grade beta stimulation at rest but acting as typical beta-blockers when sympathetic activity is high. [3]
Some β-blockers partially activate the receptor while preventing catecholamines from binding to the receptor, making them partial agonists. They provide a background of sympathetic activity, while preventing normal and enhanced sympathetic activity. These β-blockers possess intrinsic sympathomimetic activity (ISA).
Beta blockers Non-selective agents Alprenolol; Bucindolol; Carteolol; Carvedilol (has additional α-blocking activity) Labetalol (has additional α-blocking activity) Nadolol; Penbutolol (has intrinsic sympathomimetic activity) Pindolol (has intrinsic sympathomimetic activity) Propranolol; Sotalol; Timolol; β 1-selective agents
Pindolol is a first generation, [29] non-selective beta blocker in the class of β-adrenergic receptor antagonists. On the receptor level it is a competitive partial agonist . It possesses intrinsic sympathomimetic activity , meaning it has some degree of agonist effects in the absence of competing ligands.
Oxprenolol (brand names Trasacor, Trasicor, Coretal, Laracor, Slow-Pren, Captol, Corbeton, Slow-Trasicor, Tevacor, Trasitensin, Trasidex) is a non-selective beta blocker with some intrinsic sympathomimetic activity. It is used for the treatment of angina pectoris, abnormal heart rhythms and high blood pressure.
The mechanisms of sympathomimetic drugs can be direct-acting (direct interaction between drug and receptor), such as α-adrenergic agonists, β-adrenergic agonists, and dopaminergic agonists; or indirect-acting (interaction not between drug and receptor), such as MAOIs, COMT inhibitors, release stimulants, and reuptake inhibitors that increase the levels of endogenous catecholamines.
Labetalol is a beta blocker, or an antagonist of the β-adrenergic receptors. It is specifically a non-selective antagonist of the β 1-and β 2-adrenergic receptors. [17] Labetalol has intrinsic sympathomimetic activity. [17] It is also an antagonist of the α 1-adrenergic receptor, and hence is additionally an alpha blocker.