Esmolol

Esmolol
Clinical data
Trade names	Brevibloc
AHFS/Drugs.com	Monograph
Pregnancy; category	AU: C; ;
Routes of; administration	Intravenous
ATC code	C07AB09 (WHO) ;
Legal status
Legal status	AU: S4 (Prescription only);
Pharmacokinetic data
Protein binding	60%
Metabolism	Red blood cell (erythrocytic)
Elimination half-life	9 minutes
Excretion	Kidney
Identifiers
	IUPAC name methyl (RS)-3-{4-[2-hydroxy-3-(propan-2-ylamino)propoxy]phenyl}propanoate;
CAS Number	81147-92-4 ;
PubChem CID	59768;
IUPHAR/BPS	7178;
DrugBank	DB00187 ;
ChemSpider	53916 ;
UNII	MDY902UXSR;
KEGG	D07916 ;
ChEBI	CHEBI:4856 ;
ChEMBL	ChEMBL768 ;
CompTox Dashboard (EPA)	DTXSID4022995 ;
Chemical and physical data
Formula	C16H25NO4
Molar mass	295.379 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES O=C(OC)CCc1ccc(OCC(O)CNC(C)C)cc1;
	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 ; Key:AQNDDEOPVVGCPG-UHFFFAOYSA-N ;
	(what is this?) (verify)

Esmolol, sold under the brand name Brevibloc, is a cardio selective beta₁ receptor blocker with rapid onset,^[3] a very short duration of action, and no significant intrinsic sympathomimetic or membrane stabilising activity at therapeutic dosages.

It is a class II antiarrhythmic.^[4] 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.^[5]

It was patented in 1980 and approved for medical use in 1987.^[6]

^ "Brevibloc esmolol hydrochloride 2.5 g powder for injection for infusion vial (310943)". Therapeutic Goods Administration (TGA). 26 May 2022. Retrieved 29 April 2023.
^ "Esmolol Juno (Juno Pharmaceuticals Pty Ltd)". Therapeutic Goods Administration (TGA). 13 January 2023. Archived from the original on 18 March 2023. Retrieved 29 April 2023.
^ Deng CY, Lin SG, Zhang WC, Kuang SJ, Qian WM, Wu SL, et al. (December 2006). "Esmolol inhibits Na+ current in rat ventricular myocytes". Methods and Findings in Experimental and Clinical Pharmacology. 28 (10): 697–702. doi:10.1358/mf.2006.28.10.1037498. PMID 17235414. Archived from the original on 2019-12-10. Retrieved 2008-07-27.
^ Jaillon P, Drici M (December 1989). "Recent antiarrhythmic drugs". The American Journal of Cardiology. 64 (20): 65J–69J. doi:10.1016/0002-9149(89)91203-4. PMID 2688391.
^ Tripathi KD. "Antiadrenergic Drugs and Drugs for Glaucoma". Essentials of Medical Pharmacology (7th ed.). p. 149.
^ Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 462. ISBN 978-3-527-60749-5.

[1] "Brevibloc esmolol hydrochloride 2.5 g powder for injection for infusion vial (310943)". Therapeutic Goods Administration (TGA). 26 May 2022. Retrieved 29 April 2023.

[2] "Esmolol Juno (Juno Pharmaceuticals Pty Ltd)". Therapeutic Goods Administration (TGA). 13 January 2023. Archived from the original on 18 March 2023. Retrieved 29 April 2023.

[pmid17235414-3] Deng CY, Lin SG, Zhang WC, Kuang SJ, Qian WM, Wu SL, et al. (December 2006). "Esmolol inhibits Na+ current in rat ventricular myocytes". Methods and Findings in Experimental and Clinical Pharmacology. 28 (10): 697–702. doi:10.1358/mf.2006.28.10.1037498. PMID 17235414. Archived from the original on 2019-12-10. Retrieved 2008-07-27.

[pmid2688391-4] Jaillon P, Drici M (December 1989). "Recent antiarrhythmic drugs". The American Journal of Cardiology. 64 (20): 65J–69J. doi:10.1016/0002-9149(89)91203-4. PMID 2688391.

[5] Tripathi KD. "Antiadrenergic Drugs and Drugs for Glaucoma". Essentials of Medical Pharmacology (7th ed.). p. 149.

[6] Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 462. ISBN 978-3-527-60749-5.

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