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Esmolol
BREVIBLOC^® FDA Package Insert
Indications and Usage
Dosage and Administration
Dosage Forms and Strengths
Contraindications
Warnings and Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Overdosage
Description
Clinical Pharmacology
Nonclinical Toxicology
Clinical Studies
How Supplied/Storage and Handling
Patient Counseling Information
Labels and Packages

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Ahmed Zaghw, M.D. [2]; Abdurahman Khalil, M.D. [3]

Synonyms / Brand Names: BREVIBLOC^®

Overview

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.

FDA Package Insert

BREVIBLOC (esmolol hydrochloride) injection

Mechanism of Action

REVIBLOC (Esmolol Hydrochloride) is a beta1-selective (cardioselective) adrenergic receptor blocking agent with rapid onset, a very short duration of action, and no significant intrinsic sympathomimetic or membrane stabilizing activity at therapeutic dosages. Its elimination half-life after intravenous infusion is approximately 9 minutes. BREVIBLOC inhibits the beta1 receptors located chiefly in cardiac muscle, but this preferential effect is not absolute and at higher doses it begins to inhibit beta2 receptors located chiefly in the bronchial and vascular musculature.

Esmolol and Alcohol

Esmolol hydrochloride is a relatively hydrophilic compound which is very soluble in water and freely soluble in alcohol. Its partition coefficient (octanol/water) at pH 7.0 is 0.42 compared to 17.0 for propranolol.

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. Unknown parameter |author-separator= ignored (help)
↑ 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.

[pmid17235414-1] 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. Unknown parameter |author-separator= ignored (help)

[pmid2688391-2] 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.

[1]

[2]

@@ Line 1: / Line 1: @@
-{{Simvastatin}}
+{{Esmolol}}
-{{CMG}}; {{AE}} {{SS}}
-'''''For patient information about Simvastatin, click [[Simvastatin (patient information)|here]].'''''
+{{CMG}}; {{AE}} {{AZ}}; {{AK}}
-{{SB}} ZOCOR<sup>®</sup>,generic
+{{SB}} BREVIBLOC<sup>®</sup>
 ==Overview==
+'''Esmolol''' (trade name '''Brevibloc''') is a cardioselective [[beta-blocker|beta<sub>1</sub> receptor blocker]] with rapid onset,<ref name="pmid17235414">{{cite journal |author=Deng CY |title=Esmolol inhibits Na+ current in rat ventricular myocytes |journal=Methods Find Exp Clin Pharmacol |volume=28 |issue=10 |pages=697–702 |date=December 2006 |pmid=17235414 |doi=10.1358/mf.2006.28.10.1037498 |url=http://journals.prous.com/journals/servlet/xmlxsl/pk_journals.xml_summaryn_pr?p_JournalId=6&p_RefId=1037498 |author-separator=, |author2=Lin SG |author3=Zhang WC |display-authors=3 |last4=Kuang |first4=S.J. |last5=Qian |first5=W.M. |last6=Wu |first6=S.L. |last7=Shan |first7=Z.X. |last8=Yang |first8=M. |last9=Yu |first9=X.Y.}}</ref> a very short duration of action, and no significant [[Intrinsic sympathomimetic activity|intrinsic sympathomimetic]] or membrane stabilising activity at therapeutic dosages.
-'''Simvastatin''' ([[International Nonproprietary Name|INN]]) ({{pronEng|ˈsɪmvəstætɨn}})  is a [[hypolipidemic agent|hypolipidemic drug]] belonging to the class of pharmaceuticals called "[[statin]]s". It is used to control [[hypercholesterolemia]] (elevated [[cholesterol]] levels) and to prevent[[cardiovascular disease]].  Simvastatin is a synthetic derivate of a fermentation product of ''[[Aspergillus terreus]]''.
+It is a [[Antiarrhythmic#Class II agents|class II antiarrhythmic]].<ref name="pmid2688391">{{cite journal |author=Jaillon P, Drici M |title=Recent antiarrhythmic drugs |journal=Am. J. Cardiol. |volume=64 |issue=20 |pages=65J–69J |date=December 1989 |pmid=2688391 |doi= 10.1016/0002-9149(89)91203-4|url=}}</ref>
-==History==
+Esmolol decreases the force and rate of heart contractions by blocking [[beta-adrenergic receptor]]s 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]].
-The development of simvastatin was closely linked with the research and development of [[lovastatin]]. Biochemist Jesse Huff and his colleagues at[[Merck & Co.|Merck]] began researching the biosynthesis of cholesterol in the early 1950s. In 1956, [[mevalonic acid]] was isolated from a yeast extract by [[Karl Folkers]], Carl Hoffman, and others at Merck; while Huff and his associates confirmed that mevalonic acid was an intermediate in cholesterol biosynthesis. In 1959, the [[HMG-CoA reductase]] enzyme (a major contributor of internal cholesterol production) was discovered by researchers at the [[Max Planck Institute]]. This discovery encouraged scientists worldwide to find an effective inhibitor of this enzyme.
+==Category==
-By 1976, [[Akira Endo (biochemist)|Akira Endo]] had isolated the first inhibitor (compactin ML-236B) from the [[fungus]], ''[[Penicillium|Penicillium citrinium]]'' in Sankyo, Japan.<ref>Liao and Laufs. Pleiotropic Effects of Statins.(2005) Annu. Rev. Pharmacol. Toxicol:45:89-118</ref> In 1979, Hoffman and colleagues isolated lovastatin from a strain of the fungus ''[[Aspergillus|Aspergillus terreus]]''. While developing and researching lovastatin, Merck scientists synthetically derived a more potent HMG-CoA reductase inhibitor from a fermentation product of ''Aspergillus terreus'', which was designated MK-733 (later to be named simvastatin).<!--
+[[Beta-blockers]].
-  --><ref name = "preview">{{cite book | title=Innovation Management - Strategies, Implementation, and Profits | url=http://www-personal.umich.edu/~afuah/ | editor=Ed. Allan Afuah | year=1998 | publisher=Oxford University Press | author= Olivia Williams, Anne-Marie Jacks, Jim Davis, Sabrina Martinez |chapter=Case 10: Merck(A): Mevacor* | chapterurl=http://www-personal.umich.edu/~afuah/cases/case10.html}}</ref>
-==Category==
+==FDA Package Insert==
-Alcohols,Carboxylate esters,Lactones,Merck,Statins,Tetrahydropyrans,World Health Organization essential medicines,Neuroprotective agents,Cardiovascular Drugs
+====BREVIBLOC (esmolol hydrochloride) injection====
-==FDA Package Insert==
+'''  [[Esmolol indications and usage|Indications and Usage]]'''
+'''| [[Esmolol dosage and administration|Dosage and Administration]]'''
+'''| [[Esmolol dosage forms and strengths|Dosage Forms and Strengths]]'''
+'''| [[Esmolol contraindications|Contraindications]]'''
+'''| [[Esmolol warnings and precautions|Warnings and Precautions]]'''
+'''| [[Esmolol adverse reactions|Adverse Reactions]]'''
+'''| [[Esmolol drug interactions|Drug Interactions]]'''
+'''| [[Esmolol use in specific populations|Use in Specific Populations]]'''
+'''| [[Esmolol overdosage|Overdosage]]'''
+'''| [[Esmolol description|Description]]'''
+'''| [[Esmolol clinical pharmacology|Clinical Pharmacology]]'''
+'''| [[Esmolol nonclinical toxicology|Nonclinical Toxicology]]'''
+'''| [[Esmolol clinical studies|Clinical Studies]]'''
+'''| [[Esmolol how supplied storage and handling|How Supplied/Storage and Handling]]'''
+'''| [[Esmolol patient counseling information|Patient Counseling Information]]'''
+'''| [[Esmolol labels and packages|Labels and Packages]]'''
-'''  [[Simvastatin indications and usage|Indications and Usage]]'''
-'''| [[Simvastatin dosage and administration|Dosage and Administration]]'''
-'''| [[Simvastatin dosage forms and strengths|Dosage Forms and Strengths]]'''
-'''| [[Simvastatin contraindications|Contraindications]]'''
-'''| [[Simvastatin warnings and precautions|Warnings and Precautions]]'''
-'''| [[Simvastatin adverse reactions|Adverse Reactions]]'''
-'''| [[Simvastatin drug interactions|Drug Interactions]]'''
-'''| [[Simvastatin use in specific populations|Use in Specific Populations]]'''
-'''| [[Simvastatin overdosage|Overdosage]]'''
-'''| [[Simvastatin description|Description]]'''
-'''| [[Simvastatin clinical pharmacology|Clinical Pharmacology]]'''
-'''| [[Simvastatin nonclinical toxicology|Nonclinical Toxicology]]'''
-'''| [[Simvastatin clinical studies|Clinical Studies]]'''
-'''| [[Simvastatin how supplied storage and handling|How Supplied/Storage and Handling]]'''
-'''| [[Simvastatin patient counseling information|Patient Counseling Information]]'''
-'''| [[Simvastatin labels and packages|Labels and Packages]]'''
 ==Mechanism of Action==
-Simvastatin is a prodrug and is hydrolyzed to its active β-hydroxyacid form, simvastatin acid, after administration. Simvastatin is a specific inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, the enzyme that catalyzes the conversion of HMG-CoA to mevalonate, an early and rate limiting step in the biosynthetic pathway for cholesterol. In addition, simvastatin reduces VLDL and TG and increases HDL-C.
+REVIBLOC (Esmolol Hydrochloride) is a [[beta1]]-selective (cardioselective) adrenergic receptor blocking agent with rapid onset, a very short duration of action, and no significant [[Intrinsic sympathomimetic activity|intrinsic sympathomimetic]] or membrane stabilizing activity at therapeutic dosages. Its elimination half-life after intravenous infusion is approximately 9 minutes. BREVIBLOC inhibits the [[beta1]] receptors located chiefly in cardiac muscle, but this preferential effect is not absolute and at higher doses it begins to inhibit [[beta2]] receptors located chiefly in the bronchial and vascular musculature.
+==Esmolol and Alcohol==
+Esmolol hydrochloride is a relatively hydrophilic compound which is very soluble in water and freely soluble in alcohol. Its partition coefficient (octanol/water) at pH 7.0 is 0.42 compared to 17.0 for [[propranolol]].
-==Interaction with Alcohol==
-The drug should be used with caution in patients who consume substantial quantities of alcohol and/or have a past history of liver disease.
 ==References==
 {{Reflist|2}}
-{{Statins}}
-{{Merck&Co}}
-[[Category:Alcohols]]
-[[Category:Carboxylate esters]]
-[[Category:Lactones]]
-[[Category:Merck]]
-[[Category:Statins]]
 [[Category:Cardiovascular Drugs]]
 [[Category:Drugs]]