- 同
- Brevibloc
WordNet
- intravenous beta blocker (trade name Brevibloc) that acts for only a short time; used primarily for cardiac arrhythmias (同)Brevibloc
Wikipedia preview
出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2016/01/18 02:00:49」(JST)
[Wiki en表示]
Esmolol
|
| Systematic (IUPAC) name |
|
methyl (RS)-3-{4-[2-hydroxy-3-(propan-2-ylamino)propoxy]phenyl}propanoate
|
| Clinical data |
| AHFS/Drugs.com |
monograph |
Pregnancy
category |
- AU: C
- US: C (Risk not ruled out)
|
Routes of
administration |
iv |
| Pharmacokinetic data |
| Bioavailability |
- |
| Protein binding |
60% |
| Metabolism |
Erythrocytic |
| Biological half-life |
9 minutes |
| Excretion |
Renal |
| Identifiers |
| CAS Number |
103598-03-4 Y |
| ATC code |
C07AB09 |
| PubChem |
CID: 59768 |
| IUPHAR/BPS |
7178 |
| DrugBank |
DB00187 N |
| ChemSpider |
53916 Y |
| UNII |
MDY902UXSR N |
| KEGG |
D07916 Y |
| ChEBI |
CHEBI:4856 N |
| ChEMBL |
CHEMBL768 Y |
| Chemical data |
| Formula |
C16H25NO4 |
| Molecular mass |
295.374 g/mol |
SMILES
-
O=C(OC)CCc1ccc(OCC(O)CNC(C)C)cc1
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InChI
-
InChI=1S/C16H25NO4/c1-12(2)17-10-14(18)11-21-15-7-4-13(5-8-15)6-9-16(19)20-3/h4-5,7-8,12,14,17-18H,6,9-11H2,1-3H3 Y
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Key:AQNDDEOPVVGCPG-UHFFFAOYSA-N Y
|
| NY (what is this?) (verify) |
Esmolol (trade name Brevibloc) is a cardioselective beta1 receptor blocker with rapid onset,[1] a very short duration of action, and no significant intrinsic sympathomimetic or membrane stabilising activity at therapeutic dosages.
It is a class II antiarrhythmic.[2] Esmolol decreases the force and rate of heart contractions by blocking beta-adrenergic receptors of the sympathetic nervous system, which are found in the heart and other organs of the body. Esmolol prevents the action of two naturally occurring substances: epinephrine and norepinephrine.
Dosing
Esmolol is given by slow intravenous injection. It is commonly used in patients during surgery to prevent or treat tachycardia, and is also used in treatment of acute supraventricular tachycardia. Esmolol is also the drug of choice when aortic dissection is suspected.
Metabolism
Esmolol is rapidly hydrolyzed by plasma esterases and not by plasma cholinesterases. Esmolol's short duration of action is based on the ester-methyl side chain which allows for quick hydrolysis. Esmolol's structure is reflected in its name, es-molol as in ester-methyl. Plasma cholinesterases and red cell membrane acetylcholinesterase do not have any action. This metabolism results in the formation of a free acid and methanol. The amount of methanol produced is similar to endogenous methanol production. Its elimination half-life is about 9 minutes.
References
- ^ Deng CY; Lin SG; Zhang WC; et al. (December 2006). "Esmolol inhibits Na+ current in rat ventricular myocytes". Methods Find Exp Clin Pharmacol 28 (10): 697–702. doi:10.1358/mf.2006.28.10.1037498. PMID 17235414.
- ^ Jaillon P, Drici M (December 1989). "Recent antiarrhythmic drugs". Am. J. Cardiol. 64 (20): 65J–69J. doi:10.1016/0002-9149(89)91203-4. PMID 2688391.
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Beta blockers (C07)
|
|
| β, non-selective |
- Alprenolol
- Bopindolol
- Bupranolol
- Carteolol
- Cloranolol
- Mepindolol
- Nadolol
- Oxprenolol
- Penbutolol
- Pindolol
- Propranolol
- Sotalol
- Tertatolol
- Timolol
|
|
| β1-selective |
- Acebutolol
- Atenolol
- Betaxolol
- Bevantolol
- Bisoprolol
- Celiprolol
- Epanolol
- Esmolol
- Metoprolol
- Nebivolol
- Practolol
- S-Atenolol
- Talinolol
|
|
| β2-selective |
|
|
| α1- + β-selective |
|
|
-
- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III
|
|
|
Index of the circulatory system
|
|
| Description |
- Anatomy
- Arteries
- head and neck
- arms
- chest
- abdomen
- legs
- Veins
- head and neck
- arms
- chest
- abdomen and pelvis
- legs
- Development
- Cells
- Physiology
|
|
| Disease |
- Congenital
- Neoplasms and cancer
- Lymphatic vessels
- Injury
- Vasculitis
- Other
- Symptoms and signs
|
|
| Treatment |
- Procedures
- Drugs
- beta blockers
- channel blockers
- diuretics
- nonsympatholytic vasodilatory antihypertensives
- peripheral vasodilators
- renin–angiotensin system
- sympatholytic antihypertensives
- vasoprotectives
|
|
|
|
Antiarrhythmic agents (C01B)
|
|
| Channel blockers |
|
class I
(Na+ channel blockers)
|
|
class Ia (Phase 0→ and Phase 3→)
|
- Ajmaline
- Disopyramide
- Lorajmine
- Prajmaline
- Procainamide#
- Quinidine#
- Sparteine
|
|
|
class Ib (Phase 3←)
|
- IV (Lidocaine#)
- enteral (Aprindine
- Mexiletine
- Tocainide)
|
|
|
class Ic (Phase 0→)
|
- Encainide‡
- Ethacizine
- Flecainide
- Indecainide‡
- Lorcainide
- Moracizine‡
- Propafenone
|
|
|
|
class III
(Phase 3→, K+ channel blockers)
|
- Amiodarone
- Bretylium
- Bunaftine
- Dofetilide
- Dronedarone
- E-4031†
- Ibutilide
- Nifekalant
- Sotalol
- Tedisamil
- Vernakalant
|
|
|
class IV
(Phase 4→, Ca2+ channel blockers)
|
|
|
|
Receptor agonists
and antagonists |
|
class II
(Phase 4→, β blockers)
|
- Nadolol
- Pindolol
- Propranolol
- cardioselective (Acebutolol
- Atenolol
- Esmolol
- Metoprolol)
|
|
|
A1 agonist
|
- Adenosine
- Benzodiazepines
- Barbiturates
|
|
|
M2
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- muscarinic antagonist: Atropine
- Disopyramide
- Quinidine
muscarinic agonist: Digoxin
|
|
|
α receptors
|
- Amiodarone
- Bretylium
- Quinidine
- Verapamil
|
|
|
| Ion transporters |
|
|
- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III
|
|
|
Index of the heart
|
|
| Description |
- Anatomy
- Physiology
- Development
|
|
| Disease |
- Injury
- Congenital
- Neoplasms and cancer
- Other
- Symptoms and signs
- Blood tests
|
|
| Treatment |
- Procedures
- Drugs
- glycosides
- other stimulants
- antiarrhythmics
- vasodilators
|
|
|
UpToDate Contents
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- 1. 心房粗動における心拍数コントロールcontrol of ventricular rate in atrial flutter [show details]
…non-pre-excited atrial flutter . Esmolol is preferred to other intravenous beta blockers in this setting due to its rapid onset of action and a greater clinical experience. Esmolol begins to act in one to two …
- 2. 急性大動脈解離とそれ以外の急性大動脈症候群の概要overview of acute aortic dissection and other acute aortic syndromes [show details]
…consists typically of an intravenous beta blocker to reduce the heart rate below 60 beats/minute. Esmolol is useful in the acute setting due to its short half-life and ability to titrate to effect (250 to …
- 3. 高血圧緊急症の治療に用いる薬物drugs used for the treatment of hypertensive emergencies [show details]
…by 20 to 80 mg every 10 minutes to a total dose of 300 mg. The infusion rate is 0.5 to 2 mg/min. Esmolol, a relatively cardioselective beta blocker, is rapidly metabolized by blood esterases. Its effects …
- 4. 心房細動における心拍数のコントロール：薬理療法control of ventricular rate in atrial fibrillation pharmacologic therapy [show details]
…is preferable. Esmolol is a rapidly acting intravenous beta blocker that is metabolized by red blood cell esterase, resulting in a short duration of action (10 to 20 minutes) . Esmolol may be particularly …
- 5. 麻酔中の成人の循環動態の管理hemodynamic management during anesthesia in adults [show details]
…comparing nicardipine with esmolol for control of post-craniotomy emergence hypertension noted similar efficacy, but a greater need for a second "rescue" agent in patients receiving esmolol . A study comparing …
English Journal
- Esmolol Administration to Control Tachycardia in an Ovine Model of Peritonitis.
- Hosokawa K1, Su F, Taccone FS, Post EH, Pereira AJ, Herpain A, Creteur J, Vincent JL.
- Anesthesia and analgesia.Anesth Analg.2017 Jul 13. doi: 10.1213/ANE.0000000000002196. [Epub ahead of print]
- PMID 28708664
- Clevidipine versus sodium nitroprusside in acute aortic dissection: A retrospective chart review.
- Ulici A1, Jancik J2, Lam TS3, Reidt S4, Calcaterra D5, Cole JB6.
- The American journal of emergency medicine.Am J Emerg Med.2017 Jun 16. pii: S0735-6757(17)30474-6. doi: 10.1016/j.ajem.2017.06.030. [Epub ahead of print]
- PMID 28669696
- Continuous synthesis and anti-myocardial injury of tanshinone IIA derivatives.
- Qin YL1, Chen L2, He W3, Su M2, Jin Q2, Fang Z1, Ouyang PK1, Guo K1.
- Journal of Asian natural products research.J Asian Nat Prod Res.2017 Jun 8:1-9. doi: 10.1080/10286020.2017.1337751. [Epub ahead of print]
- PMID 28595458
Japanese Journal
- Landiolol, an Ultra-Short-Acting β_1-Blocker, More Effectively Terminates Atrial Fibrillation Than Diltiazem After Open Heart Surgery : Prospective, Multicenter, Randomized, Open-Label Study (JL-KNIGHT Study)
- SAKAMOTO Atsuhiro,KITAKAZE Masafumi,TAKAMOTO Shinichi,NAMIKI Akiyoshi,KASANUKI Hiroshi,HOSODA Saichi
- Circulation journal : official journal of the Japanese Circulation Society 76(5), 1097-1101, 2012-04-25
- … Recent studies have suggested that esmolol is the first choice for rate control in patients with postoperative atrial fibrillation (AF) after coronary artery bypass surgery, but side-effects of esmolol such as hypotension are problematic. … To overcome this problem, landiolol, an ultra-short-acting β<sub>1</sub>-blocker with a less negative inotropic effect than esmolol, has been developed. …
- NAID 10030132260
- Direct Effects of Esmolol and Landiolol on Cardiac Function, Coronary Vasoactivity, and Ventricular Electrophysiology in Guinea-Pig Hearts
- Shibata Shigehiro,Okamoto Yosuke,Endo Shigeatsu [他],ONO Kyoichi
- Journal of pharmacological sciences 118(2), 255-265, 2012-02-20
- … The ultra-short acting, selective <I>β</I><SUB>1</SUB>-adrenergic antagonists landiolol and esmolol are widely used perioperatively; … Direct application of esmolol significantly decreased systolic left ventricular pressure and heart rate at concentrations > … Esmolol also shortened the action potential duration (APD) in a concentration-dependent manner, an action maintained even when the delayed rectifier K<SUP>+</SUP> …
- NAID 10030455076
Related Pictures
★リンクテーブル★
[★]
- 英
- esmolol
- 化
- 塩酸エスモロール esmolol hydrochloride
- 商
- ブレビブロック
[★]
- 関
- esmolol