Esmolol
- (±)- methyl-3- {4 - [ 2-hydroxy- 3 - ( isopropylamino ) propoxy] phenyl} propionate
- (RS)- methyl-3- {4 - [ 2-hydroxy- 3 - ( isopropylamino ) propoxy] phenyl} propionate
- DL- methyl-3- {4 - [ 2-hydroxy- 3 - ( isopropylamino ) propoxy] phenyl} propionate
- Rac- methylene -3- {4 - [ 2-hydroxy- 3 - ( isopropylamino ) propoxy] phenyl} propionate
- 81147-92-4 (free base)
- 81161-17-3 ( monohydrochloride )
C07AB09
β -adrenergic receptor blocker
- 295.37 g · mol -1 ( free base)
- 331.84 g.mol -1 ( monohydrochloride )
- 48-50 ° C ( free base)
- 85-86 ° C ( hydrochloride)
Hydrochloride
Attention
- 71 mg · kg -1 ( LD50, rat, i.v.)
- 93 mg · kg -1 ( LD50, mouse, i.v.)
- 32 mg · kg -1 ( LD50, dog, i.v.)
Template: Infobox chemical / molecular formula search available
Esmolol is a drug from the group of sympatholytic, which is used as the shortest effective β1 - blocker.
Pharmacology
Its half-life is about nine minutes, as esmolol, in contrast to other beta-blockers is not degraded organ bonded but occurs via the elimination of esterases, hydrolases. For this reason, esmolol must be continuously supplied intravenously as needed. The effects and side effects are similar to those of beta-blockers. In medicine, esmolol is used for diagnostic purposes and in emergency medicine mainly because of the short cast time. It finds application in paroxysmal supraventricular tachycardias, requiring treatment non- compensatory sinus tachycardia and the hyperkinetic heart syndrome. Cardiovascular Stable and chronically ill patients receive long-acting beta-blocker in tablet form.
Stereoisomerism
Esmolol is a drug with a chiral stereocenter. The active isomer ( eutomer ) is the (S)- esmolol. Esmolol is used as the racemate, that is a 1:1 mixture of the ( S) form and (R )-form.
Synthesis
The synthesis of racemic esmolol is from 3 - (4 -hydroxyphenyl ) propionate of which the first step is etherified in the presence of potassium carbonate with epichlorohydrin. In the second step is added to the epoxide intermediate of isopropylamine.