Celiprolol

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Structural formula
Celiprolol Structural Formulas V.1.svg
( R ) -Celiprolol (top) and ( S ) -Celiprolol (bottom), 1: 1 mixture of stereoisomers
General
Non-proprietary name Celiprolol
other names
  • ( RS ) - N '- (3-Acetyl-4- (3 - ((1,1-dimethylethyl) amino) -2-hydroxypropoxy) phenyl) - N , N -diethylurea
  • (±) - N '- (3-Acetyl-4- (3 - ((1,1-dimethylethyl) amino) -2-hydroxypropoxy) phenyl) - N , N -diethylurea
  • rac - N '- (3-acetyl-4- (3 - ((1,1-dimethylethyl) amino) -2-hydroxypropoxy) phenyl) - N , N -diethylurea
  • DL - N '- (3-Acetyl-4- (3 - ((1,1-dimethylethyl) amino) -2-hydroxypropoxy) phenyl) - N , N -diethylurea
  • Celiprololum
Molecular formula
  • C 20 H 33 N 3 O 4 (Celiprolol)
  • C 20 H 33 N 3 O 4 HCl (Celiprolol hydrochloride)
External identifiers / databases
CAS number
  • 56980-93-9
  • 57470-78-7 (Celiprolol hydrochloride)
EC number 260-497-7
ECHA InfoCard 100.054.980
PubChem 2663
ChemSpider 2563
DrugBank DB04846
Wikidata Q420586
Drug information
ATC code

C07 AB08

Drug class

Beta blockers

Mechanism of action

selective blockade of β1 receptors

properties
Molar mass
Melting point
  • 110-112 ° C (Celiprolol)
  • 197–200 ° C (decomposition) (Celiprolol hydrochloride)
safety instructions
Please note the exemption from the labeling requirement for drugs, medical devices, cosmetics, food and animal feed
GHS hazard labeling
no classification available
Toxicological data

2157 mg kg −1 ( LD 50 ,  rat ,  oral )

As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions .

Celiprolol , a drug from the group of β-receptor blockers , is used to treat high blood pressure and coronary artery disease .

Clinical information

Celiprolol is a moderately effective antagonist of β 1 -adrenoceptors and a partial agonist of β 2 -adrenoceptors , with a half-life of four to twelve hours and a duration of action of up to one day. The bioavailability of Celiprolol is 50%. As a β 2 -adrenoceptor agonist, celiprolol actively leads to vasodilation of peripheral vessels. Elimination occurs mainly through the kidneys. Use in the presence of severe renal insufficiency is contraindicated .

Other Information

The peculiarity of celiprolol and some other beta blockers ( acebutolol , oxprenolol and pindolol ) is their intrinsic sympathomimetic activity ( ISA , see intrinsic activity ).

Trade names

Monopreparations

Selectol (D, A, CH)

Combination preparations

with chlorthalidon : Selecturon (A)

Individual evidence

  1. ^ A b The Merck Index: An Encyclopedia of Chemicals, Drugs, and Biologicals , 14th Edition (Merck & Co., Inc.), Whitehouse Station, NJ, USA, 2006; P. 324, ISBN 978-0-911910-00-1 .
  2. ↑ This substance has either not yet been classified with regard to its hazardousness or a reliable and citable source has not yet been found.
  3. ↑ Data sheet CELIPROLOL HYDROCHLORIDE CRS (PDF) at EDQM , accessed on July 19, 2008.

literature

  • T. Karow, R. Lang-Roth: General and special pharmacology and toxicology . 2003, pp. 62-66.
  • G. Herold: Internal Medicine . 2004.
  • E. Mutschler, drug effects, 7th edition 1996, WVG Stuttgart, ISBN 3-8047-1377-7 .