Celiprolol powder is indicated for the management of mild to moderate hypertension and effort-induced angina pectoris. 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. [wpforms id="3634"]
02 Celiprolol powder (56980-93-9) video
03 Celiprolol powder Base Information
|Molecular Weight||379.501 g/mol|
|Melting Point||198 to 200°C|
|Half Life||approximately 5-6 hours|
|Solubility||soluble in water|
|Storage Condition||0 – 4 C for short term (days to weeks), or -20 C for long term (months)|
|Application||Celiprolol is currently approved for the treatment of management of mild to moderate hypertension and effort-induced angina pectoris.
04 Celiprolol powder General Description
Celiprolol powder 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.
Celiprolol powder 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. In 2019, a new drug application (NDA) for celiprolol was denied by the Food an the U.S. Food and Drug Administration (FDA), instead calling for an “adequate and well-controlled” trial to determine whether celiprolol reduced the risk of clinical events in patients with vEDS.
It was patented in 1973 and approved for medical use in 1982.
05 Celiprolol powder (56980-93-9) History
Celiprolol side effects includes:
Feeling dizzy, sleepy, tired or light-headed, Headache, Feeling sick (nausea) or being sick (vomiting), stomach upset
06 Celiprolol (56980-93-9) Mechanism Of Action
Celiprolol is a vasoactive beta-1 selective adrenoceptor antagonist with partial beta-2 agonist activity. The beta-2 agonist activity is thought to account for its mild vasodilating properties. It lowers blood pressure in hypertensive patients at rest and on exercise. The effects on heart rate and cardiac output are dependent on the pre-existing background level of sympathetic tone. Under conditions of stress such as exercise, celiprolol attenuates chronotropic and inotropic responses to sympathetic stimulation. However, at rest minimal impairment of cardiac function is seen.
07 How to take Celiprolol (56980-93-9)?
Before you start the treatment, read the manufacturer’s printed information leaflet from inside the pack. It will give you more information about celiprolol and will provide you with a full list of the side-effects which you may experience from taking it.
Take celiprolol exactly as your doctor tells you to. There are two strengths of tablet – 200 mg and 400 mg. It is usual to start by taking one 200 mg tablet daily, although your doctor may later increase this to the 400 mg strength tablet. You should take the tablet first thing in the morning, preferably ‘on an empty stomach’. This means that you should take the tablet at least 30 minutes before you have breakfast, or wait until two hours after you have eaten. Swallow the tablet with a drink of water.
If you forget to take a dose, take it when you remember (without food if possible). If you do not remember until the following day, leave out the missed dose. Do not take two doses together to make up for a forgotten dose.
08 Celiprolol (56980-93-9) More research
Celiprolol: A Unique Selective Adrenoceptor Modulator.
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.
09 Celiprolol (56980-93-9) Document Download
10 Celiprolol (56980-93-9) Reference
- Chen X, Minatoguchi S, Arai M, Wang N, Lu C, Narentuoya B, Uno Y, Misao Y, Takemura G, Fujiwara T, Fujiwara H: Celiprolol, a selective beta1-blocker, reduces the infarct size through production of nitric oxide in a rabbit model of myocardial infarction. Circ J. 2007 Apr;71(4):574-9. [PubMed:17384462]
- Hayashi T, Juliet PA, Miyazaki-Akita A, Funami J, Matsui-Hirai H, Fukatsu A, Iguchi A: beta1 antagonist and beta2 agonist, celiprolol, restores the impaired endothelial dependent and independent responses and decreased TNFalpha in rat with type II diabetes. Life Sci. 2007 Jan 16;80(6):592-9. Epub 2006 Dec 1. [PubMed:17141277]
- Yao EH, Fukuda N, Matsumoto T, Katakawa M, Yamamoto C, Han Y, Ueno T, Kobayashi N, Matsumoto K: Effects of the antioxidative beta-blocker celiprolol on endothelial progenitor cells in hypertensive rats. Am J Hypertens. 2008 Sep;21(9):1062-8. doi: 10.1038/ajh.2008.233. Epub 2008 Jul 17. [PubMed:18636069]
- 01. Overview
- 02. Celiprolol powder (56980-93-9) video
- 03. Celiprolol powder Base Information
- 04. Celiprolol powder General Description
- 05. Celiprolol powder (56980-93-9) History
- 06. Celiprolol (56980-93-9) Mechanism Of Action
- 07. How to take Celiprolol (56980-93-9)?
- 08. Celiprolol (56980-93-9) More research
- 09. Celiprolol (56980-93-9) Document Download
- 10. Celiprolol (56980-93-9) Reference