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Esmolol is a cardioselective beta-adrenergic blocker used for the short-term control of ventricular rate and heart rate in various types of tachycardia, including perioperative tachycardia and hypertension. Esmolol, commonly marketed under the trade name Brevibloc, is a cardioselective beta-1 receptor blocker.
- Mechanism
- Curator reviewed
Similar to other beta-blockers, esmolol blocks the agonistic effect of the sympathetic neurotransmitters by competing for receptor binding sites. Because it predominantly blocks the beta-1 receptors in cardiac tissue, it is said to be cardioselective. In general, so-called cardioselective beta-blockers are relatively cardioselective; at lower doses they block beta-1 receptors only but begin to block beta-2 receptors as the dose increases. At therapeutic dosages, esmolol does not have intrinsic sympathomimetic activity (ISA) or membrane-stabilizing (quinidine-like) activity. Antiarrhythmic activity is due to blockade of adrenergic stimulation of cardiac pacemaker potentials. In the Vaughan Williams classification of antiarrhythmics, beta-blockers are considered to be class II agents.
- Primary indication
- For the rapid control of ventricular rate in patients with atrial fibrillation or atrial flutter in perioperative, postoperative, or other emergent circumstances where short term control of ventricular rate with a short-acting agent is desirable.Curator reviewed · 6 structured indications
- Formula / weight
- C16H25NO4 · 295.374 g/mol (avg)
- First approval
- Canada, 2000 · United States, 1986
- Brand names
- Brevibloc
Resolves to
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Which drugs share a target with Esmolol, and which of those have an active Phase 3 trial?