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Celiprolol: A Unique Selective Adrenoceptor Modulator. | LitMetric

Celiprolol: A Unique Selective Adrenoceptor Modulator.

Cardiol Rev

From the *College of Pharmacy, University of New Mexico, Albuquerque, NM; †Department of Clinical Pharmacy, Albert Einstein College of Medicine/Montefiore Medical Center, Bronx, NY; and ‡Department of Medicine, New York Medical College/Westchester Medical Center, Valhalla, NY.

Published: January 2017

AI Article Synopsis

  • * It has antihypertensive and antianginal effects and is used for these purposes in various countries, but in the U.S., it's primarily indicated for vascular type Ehlers-Danlos syndrome.
  • * Studies showed celiprolol significantly reduces arterial events in patients with this rare connective tissue disorder, highlighting its distinct benefits compared to other β-blockers.

Article Abstract

Celiprolol is a β-blocker with a unique pharmacologic profile: it is a β1-andrenoceptor antagonist with partial β2 agonist activity. Given this combination of effects, celiprolol may be better described as a selective adrenoreceptor modulator. It has antihypertensive and antianginal properties and is indicated for those uses in various countries around the world. In the United States, however, the proposed indication for this drug will be for the treatment of vascular type Ehlers-Danlos syndrome, a rare connective tissue disorder characterized by fragile arterial structure and an increased risk of life-threatening vascular complications. By reducing heart rate and pulsatile pressure, celiprolol may reduce the mechanical stress on collagen fibers within the arterial wall and be of benefit in patients with vascular type Ehlers-Danlos syndrome. The largest investigation of celiprolol in vascular Ehlers-Danlos syndrome was prematurely terminated due to significant benefit with celiprolol in reducing arterial events in patients with this condition. Celiprolol, therefore, represents a β-blocker that is unique from others in its class in both its pharmacology and clinical applications.

Download full-text PDF

Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5549637PMC
http://dx.doi.org/10.1097/CRD.0000000000000159DOI Listing

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