Celiprolol

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Celiprolol
Celiprolol.svg
Clinical data
AHFS/Drugs.com International Drug Names
ATC code
Pharmacokinetic data
Bioavailability 30-70%
Biological half-life 5 hours
Identifiers
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
ECHA InfoCard 100.054.980
Chemical and physical data
Formula C20H33N3O4
Molar mass 379.49 g/mol
3D model (Jmol)
Chirality Racemic mixture

Celiprolol (brand names Cardem, Selectol, Celipres, Celipro, Celol, Cordiax, Dilanorm) is a medication in the class of beta blockers, used in the treatment of high blood pressure. It has a unique pharmacology: it is a selective β1 receptor antagonist, but a β2 receptor partial agonist. It is also a weak α2 receptor antagonist.

In 2010, a clinical trial has suggested a use for this medication in the prevention of vascular complications of a rare inherited disease called vascular Ehlers–Danlos syndrome. This study demonstrated decreased incidence of arterial rupture or dissection (a specific type of arterial rupture in which the layers of the vessel separate prior to complete failure of the artery wall).[1]

Celiprolol is believed to provide clinical benefit for people with vascular Ehlers–Danlos syndrome by promoting normal collagen synthesis in the blood vessels, and by shifting the pressure load away from the vessels most prone to dissection and rupture. [2] Acer Therapeutics is currently developing celiprolol as a potential treatment option specifically for people with vEDS. In 2015, the U.S. Food and Drug Administration (FDA) granted celiprolol orphan drug designation for the treatment of vascular Ehlers–Danlos syndrome.

References[edit]

  1. ^ Ong K-T; et al. (2010). "Effect of celiprolol on prevention of cardiovascular events in vascular Ehlers-Danlos syndrome: a prospective randomised, open, blinded-endpoints trial". Lancet. 376 (9751): 1476–1484. PMID 20825986. doi:10.1016/S0140-6736(10)60960-9. 
  2. ^ Beridze N, Frishman WH (2012). "Vascular Ehlers-Danlos syndrome: pathophysiology, diagnosis, and prevention and treatment of its complications". Cardiol Rev. 1: 4–7. PMID 22143279. doi:10.1097/CRD.0b013e3182342316. 

External links[edit]