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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.
Some beta blockers (e.g. oxprenolol, pindolol, penbutolol, labetalol and acebutolol) exhibit intrinsic sympathomimetic activity (ISA). These agents are capable of exerting low-level agonist activity at the β-adrenergic receptor while simultaneously acting as a receptor site antagonist.
Penbutolol (has intrinsic sympathomimetic activity) Pindolol (has intrinsic sympathomimetic activity) Propranolol; Sotalol; Timolol; β 1-selective agents Acebutolol (has intrinsic sympathomimetic activity) Atenolol; Betaxolol; Bisoprolol; Celiprolol; Esmolol; Metoprolol; Nebivolol; β 2-selective agents Butaxamine (weak α-adrenergic agonist ...
They provide a background of sympathetic activity, while preventing normal and enhanced sympathetic activity. These β-blockers possess intrinsic sympathomimetic activity (ISA). Some of them also possess what is called membrane-stabilizing activity (MSA) on myocardial muscle fibers. [12]
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]
Labetalol possesses significant intrinsic sympathomimetic activity (ISA). [2] [22] In particular, it is a partial agonist at β 2-adrenergic receptors located in the vascular smooth muscle. Labetalol relaxes vascular smooth muscle by a combination of this partial β 2-adrenergic receptor agonism and through α 1-adrenergic receptor blockade.
Beta-blockers with intrinsic sympathomimetic activity: acebutolol, pindolol; Some common side effects include increased airway resistance for non-selective beta-blockers, exacerbation of peripheral vascular diseases, and hypotension [15] Beta-blockers are contraindicated in patients with second- or third-degree atrioventricular block.
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.