Celiprolol: A Unique Selective Adrenoceptor Modulator.
Article Details
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Nawarskas JJ, Cheng-Lai A, Frishman WH
Celiprolol: A Unique Selective Adrenoceptor Modulator.
Cardiol Rev. 2017 Sep/Oct;25(5):247-253. doi: 10.1097/CRD.0000000000000159.
- PubMed ID
- 28742547 [ View in PubMed]
- Abstract
Celiprolol is a beta-blocker with a unique pharmacologic profile: it is a beta1-andrenoceptor antagonist with partial beta2 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 beta-blocker that is unique from others in its class in both its pharmacology and clinical applications.
DrugBank Data that Cites this Article
- Drug Targets
Drug Target Kind Organism Pharmacological Action Actions Celiprolol Alpha-2A adrenergic receptor Protein Humans UnknownAntagonistDetails Celiprolol Alpha-2B adrenergic receptor Protein Humans UnknownAntagonistDetails Celiprolol Alpha-2C adrenergic receptor Protein Humans UnknownAntagonistDetails Celiprolol Beta-3 adrenergic receptor Protein Humans UnknownAgonistDetails