Controlled beta-receptor blockade with esmolol and flestolol.
Beta-receptor-blocking agents are commonly used in the management of various cardiovascular diseases. Recently, esmolol, a pharmacokinetically novel cardioselective beta-receptor-blocking agent, has been introduced for use in the treatment of critically ill patients. It is devoid of intrinsic sympathomimetic activity and in doses used clinically, it has no direct depressant effect on the heart. Esmolol is an ester and is metabolized by choline-esterase to ASL 8123, an inactive molecule. Esmolol has an elimination half-life of nine minutes which accounts for its ultrashort duration of action. This unique pharmacokinetic property provides two advantages over other longer-acting beta-receptor-blocking agents. First, the magnitude of beta-receptor blockade can be titrated to a desired level. Second, if adverse effects are experienced, reducing the dosage or terminating the infusion results in rapid reversal of its pharmacological effects. Another ultrashort-acting, non-cardioselective beta-receptor blocking agent, flestolol is undergoing clinical evaluation. Esmolol has been approved for the management of supraventricular tachycardia. The clinical safety of these novel drugs will expand the use of beta-receptor-blocking agents in the management of cardiovascular diseases in critically ill patients.
D000319:Adrenergic beta-Antagonists / Q000494:pharmacology*; D000818:Animals; D004347:Drug Interactions; D005464:Fluorobenzenes; D006439:Hemodynamics / Q000187:drug effects; D006801:Humans; D011412:Propanolamines / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use
D000319:Adrenergic beta-Antagonists; D005464:Fluorobenzenes; D011412:Propanolamines; C047847:flestolol; C036604:esmolol