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.
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.
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 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.
