Esmolol

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.

Esmolol
Clinical data
AHFS/Drugs.comMonograph
Pregnancy
category
  • AU: C
  • US: C (Risk not ruled out)
    Routes of
    administration    		iv
    ATC code
    Pharmacokinetic data
    Bioavailability-
    Protein binding60%
    MetabolismErythrocytic
    Elimination half-life9 minutes
    ExcretionRenal
    Identifiers
    CAS Number
    PubChem CID
    IUPHAR/BPS
    DrugBank
    ChemSpider
    UNII
    KEGG
    ChEBI
    ChEMBL
    CompTox Dashboard (EPA)
    Chemical and physical data
    FormulaC16H25NO4
    Molar mass295.379 g·mol−1
    3D model (JSmol)
     NY (what is this?)  (verify)

    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.[3]

    It was patented in 1980 and approved for medical use in 1987.[4]

    Medical uses

    To terminate supraventricular 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.[5]

    Dosing

    A loading dose of 0.5 mg/kg is given followed by 0.05–0.2 mg/kg/min infusion.

    Metabolism

    Esmolol is considered a soft drug,[6] 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 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. Esmolol has a rapid distribution half-life of about 2 minutes and an elimination half-life of about 9 minutes.

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    References
    1. 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.
    2. 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.
    3. Tripathi KD. "Antiadrenergic Drugs and Drugs for Glaucoma". Essentials of Medical Pharmacology (7th ed.). p. 149.
    4. Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 462. ISBN 978-3-527-60749-5.
    5. Sharma S, Suthar OP, Tak ML, Thanvi A, Paliwal N, Karnawat R (2018). "Comparison of Esmolol and Dexmedetomidine for Suppression of Hemodynamic Response to Laryngoscopy and Endotracheal Intubation in Adult Patients Undergoing Elective General Surgery: A Prospective, Randomized Controlled Double-blinded Study". Anesthesia: Essays and Researches. 12 (1): 262–266. doi:10.4103/aer.AER_226_17. PMC 5872877. PMID 29628593.
    6. Bodor N, Buchwald P (2000). "Soft drug design: General principles and recent applications". Medicinal Research Reviews. 20 (1): 58–101. doi:10.1002/(SICI)1098-1128(200001)20:1<58::AID-MED3>3.0.CO;2-X. PMID 10608921.
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