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| Clinical data | |
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| Trade names | Brevibloc |
| AHFS/Drugs.com | Monograph |
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| Routes of administration | Intravenous |
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| Pharmacokinetic data | |
| Protein binding | 60% |
| Metabolism | Red blood cell (erythrocytic) |
| Eliminationhalf-life | 9 minutes |
| Excretion | Kidney |
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| Chemical and physical data | |
| Formula | C16H25NO4 |
| Molar mass | 295.379 g·mol−1 |
| 3D model (JSmol) | |
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Esmolol, sold under the brand nameBrevibloc, is a cardio selectivebeta1 receptor blocker with rapidonset,[3] a very shortduration of action, and no significant intrinsicsympathomimetic ormembrane stabilising activity at therapeutic dosages.
It is a class IIantiarrhythmic.[4] Esmolol decreases the force and rate of heart contractions by blocking beta-adrenergic receptors of thesympathetic nervous system, which are found in theheart and other organs of the body. Esmolol prevents the action of two naturally occurring substances:epinephrine andnorepinephrine.[5]
It was patented in 1980 and approved for medical use in 1987.[6]
To terminatesupraventricular tachycardia,
Episodic atrial fibrillation or flutter,
Arrhythmia during anaesthesia,
To reduce HR and BP during and after cardiac surgery, and
In early treatment of myocardial infarction.
Esmolol is also used in blunting the hemodynamic response to laryngoscopy and intubation.[7]
Esmolol is abeta blocker, or anantagonist of theβ-adrenergic receptors.[8] It isselective for theβ1-adrenergic receptor and has nointrinsic sympathomimetic activity.[8]
Esmolol is considered asoft drug,[9] one that is rapidly metabolized to an inactive form. Esmolol is rapidly metabolized by hydrolysis of the ester linkage, chiefly by the esterases in the cytosol of red blood cells and not by plasma cholinesterases or red cell membrane acetylcholinesterase. Total body clearance in man was found to be about 20 L/kg/hr, which is greater than cardiac output; thus the metabolism of esmolol is not limited by the rate of blood flow to metabolizing tissues such as the liver or affected by hepatic or renal blood flow. Esmolol's short duration of action is based on theester-methyl side chain which allows for quick hydrolysis. Esmolol's structure is reflected in its name,es-molol as inester-methyl. Plasma cholinesterases and red cell membrane acetylcholinesterase do not have any action. This metabolism results in the formation of a free acid andmethanol. The amount of methanol produced is similar to endogenous methanol production. Esmolol has a rapid distribution half-life of about two minutes and an elimination half-life of about nine minutes.[citation needed]
Esmolol is classified as a beta blocker with moderatelipophilicity and hence moderate potential for crossing theblood–brain barrier.[10][8] As such, esmolol may produce effects in thecentral nervous system and have a risk ofneuropsychiatric side effects.[10][8]
The experimentallog P is 1.7 and its predicted log P ranges from 1.82 to 2.02.[11][12][13] It is a moderatelylipophilic beta blocker.[10][14]
