Description
Celiprolol hydrochloride is a once-daily, cardioselective β-adrenergic blocker
useful in the management of hypertension, angina pectoris and hyperkinetic heart
syndrome. It is also being evaluated in glaucoma.
Chemical Properties
White Crystalline Solid
Originator
Chemie Linz (Austria)
Uses
antihypertensive
antianginal;beta blocker
Uses
Cardioselective 1-adrenergic blocker. Antihypertensive, antianginal
Uses
Cardioselective β1-adrenergic blocker. Antihypertensive, antianginal.
Definition
ChEBI: Celiprolol hydrochloride is an aromatic ketone.
Brand name
Selecor (Rhone-Poulenc
Rorer);SELECTOL.
in vitro
the ability of celiprolol to induce the regulation of beta adrenergic receptors was investigated in s49 lymphoma cells. results showed that celiprolol did not stimulate adenylate cyclase in membranes from wild-type (wt) s49 cells or induced the sequestration of beta adrenergic receptors on intact cells. moreover, exposure of wt s49 cells to celiprolol led to the loss of around half of the total cellular beta adrenergic receptors [1].
in vivo
in a previous study, japanese white rabbits underwent 30 min of ischemia and 48 h of reperfusion. celiprolol was administered 20 min before ischemia with or without pretreatment with n(omega)-nitro-l-arginine methylester (l-name) or 5-hydroxydecanoic acid sodium salt (5-hd). results showed that celiprolol could significantly reduce the infarct size dose-dependently. the infarct size-reducing effect of celiprolol was found to be completely blocked by l-name but not by 5-hd. in addition, celiprolol could increase the myocardial interstitial levels of nox and reduce the intensity of myocardium staining [2].
Drug interactions
Potentially hazardous interactions with other drugs
Anaesthetics: enhanced hypotensive effect.
Analgesics: NSAIDs antagonise hypotensive effect.
Anti-arrhythmics: increased risk of myocardial
depression and bradycardia; increased risk of
bradycardia, myocardial depression and AV block
with amiodarone; increased risk of myocardial
depression and bradycardia with flecainide
Antidepressants: enhanced hypotensive effect with
MAOIs.
Antihypertensives; enhanced hypotensive effect;
increased risk of withdrawal hypertension with
clonidine; increased risk of first dose hypotensive
effect with post-synaptic alpha-blockers such as
prazosin.
Antimalarials: increased risk of bradycardia with
mefloquine.
Antipsychotics enhanced hypotensive effect with
phenothiazines
.Calcium-channel blockers: increased risk of
bradycardia and AV block with diltiazem;
hypotension and heart failure possible with
nifedipine and nisoldipine; asystole, severe
hypotension and heart failure with verapamil.
Cytotoxics: possible increased risk of bradycardia
with crizotinib.
Diuretics: enhanced hypotensive effect.
Fingolimod: possibly increased risk of bradycardia.Moxisylyte: possible severe postural hypotension.
Sympathomimetics: severe hypertension with
adrenaline and noradrenaline and possibly with
dobutamine.
Metabolism
Metabolism of celiprolol is minimal and it is mainly
excreted unchanged in the urine (50%) and faeces (50%)
References
[1] reynolds ee, molinoff pb. down regulation of beta adrenergic receptors in s49 lymphoma cells induced by atypical agonists. j pharmacol exp ther. 1986 dec;239(3):654-60.
[2] chen, x. ,minatoguchi, s.,arai, m., et al. celiprolol, a selective β1-blocker, reduces the infarct size through production of nitric oxide in a rabbit model of myocardial infarction. circulation journal 71(4), 574-579 (2007).
[3] ong kt et al. effect of celiprolol on prevention of cardiovascular events in vascular ehlers-danlos syndrome: a prospective randomised, open, blinded-endpoints trial. lancet. 2010 oct 30;376(9751):1476-84.
