Page last updated: 2024-12-04

celiprolol

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Description

Celiprolol is a beta blocker with vasodilating properties. It is a selective beta1-receptor antagonist, meaning it primarily blocks the effects of adrenaline and noradrenaline on the heart. This leads to a reduction in heart rate and blood pressure. Celiprolol also possesses vasodilating effects through its interaction with the potassium channels in vascular smooth muscle cells, leading to relaxation of blood vessels and further lowering blood pressure. Celiprolol has been studied extensively for its potential therapeutic benefits in treating hypertension, angina, and other cardiovascular conditions. Its unique combination of beta-blocking and vasodilating properties offers a promising approach to manage these conditions. However, it has been largely replaced by newer beta-blockers with better side-effect profiles.'

Celiprolol: A cardioselective beta-1 adrenergic antagonist that has intrinsic sympathomimetic activity. It is used in the management of ANGINA PECTORIS and HYPERTENSION. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID2663
CHEMBL ID27810
CHEBI ID94461
SCHEMBL ID49415
MeSH IDM0026215

Synonyms (53)

Synonym
celectol
st-1396
3-[3-acetyl-4-({3-[(1,1-dimethylethyl)amino]-2-hydroxypropyl}oxy)phenyl]-1,1-diethylurea
56980-93-9
rhc 5320 a
n'-(3-acetyl-4-(3-((1,1-dimethylethyl)amino)-2-hydroxypropoxy)phenyl)-n,n-diethylurea
rhc-5320a
urea, n'-(3-acetyl-4-(3-((1,1-dimethylethyl)amino)-2-hydroxypropoxy)phenyl)-n,n-diethyl-
ul/1677
celiprololum [inn-latin]
einecs 260-497-7
ccris 3400
brn 2776298
celiprolol [inn:ban]
D07660
celiprolol pch (tn)
celiprolol (inn)
celiprolol
L013433
celiprolol pch
CHEMBL27810
st1396
3-[3-acetyl-4-[3-(tert-butylamino)-2-hydroxypropoxy]phenyl]-1,1-diethylurea
AKOS015917778
celiprololum
drb57k47qc ,
edsivo
unii-drb57k47qc
BRD-A95602221-003-01-3
SCHEMBL49415
celiprolol [who-dd]
celiprolol [inn]
celiprolol hydrochloride impurity c [ep impurity]
acer-002 free base
acer002 free base
n-[3-acetyl-4-[(2rs)-3-(tert-butylamino)-2-hydroxypropoxy]phenyl]-n'-tert-butylurea
3-(3-acetyl-4-(3-(tert-butylamino)-2-hydroxypropoxy)phenyl)-1,1-diethylurea
celiprolol [vandf]
celiprolol [mi]
gtpl9064
rev 5320
DTXSID3020259
rs)-n'-{3-acetyl-4-[3-(tert-butylamino)-2-hydroxypropoxy]phenyl}-n,n-diethylurea
DB04846
CHEBI:94461
HY-119873
NCGC00344562-02
Q420586
bdbm50470842
celiprolol base
EN300-19765921
1-{3-acetyl-4-[3-(tert-butylamino)-2-hydroxypropoxy]phenyl}-3,3-diethylurea
CS-0078214

Research Excerpts

Overview

Celiprolol is a beta 1 selective adrenoreceptor blocker with partial beta 2 agonism and direct vasodilator activity. It causes renal vasodilation by increasing tissue nitric oxide (NO) levels.

ExcerptReferenceRelevance
"Celiprolol is a selective beta(1)-adrenoceptor antagonist with antihypertensive actions, which causes renal vasodilation by increasing tissue nitric oxide (NO) levels. "( Celiprolol increases coronary blood flow and reduces severity of myocardial ischemia via nitric oxide release.
Asakura, M; Asanuma, H; Hori, M; Kim, J; Kitakaze, M; Minamino, T; Node, K; Ogita, H; Sakata, Y; Sanada, S; Tada, M; Takashima, S; Ueda, Y, 2003
)
3.2
"Celiprolol is a novel beta 1 selective adrenoreceptor blocker with partial beta 2 agonism and direct vasodilator activity. "( Cardiorespiratory and symptomatic variables during maximal and submaximal exercise in men with stable effort angina: a comparison of atenolol and celiprolol.
Christie, J; Dargie, HJ; Ford, I; Grant, S; Henderson, E; MacFarlane, N; McCann, G; Norrie, J; Ray, SG, 1994
)
1.93
"Celiprolol is a third-generation beta-adrenoceptor blocker with selective beta 1-antagonist, partial beta 2-agonist and mild alpha 2-antagonist actions. "( A risk-benefit assessment of celiprolol in the treatment of cardiovascular disease.
Kendall, MJ; Rajman, I, 1994
)
2.02
"Celiprolol is a beta 1-selective adrenoceptor antagonist (beta-blocker) which acts as a weak agonist at beta 2-adrenoceptors. "( Celiprolol. An evaluation of its pharmacological properties and clinical efficacy in the management of hypertension and angina pectoris.
Dunn, CJ; Spencer, CM, 1995
)
3.18
"Celiprolol is a cardioselective beta-blocker with a partial beta-2 agonist activity and an alpha-2 blocking activity, with a minimal depressant effect on heart rate."( [Combination of celiprolol and amiodarone in the treatment of recurrent ventricular tachycardia].
Coutte, R; Frank, R; Hidden, F; Himbert, C; Naditch, L; Tonet, J, 1996
)
1.36
"Celiprolol is a beta 1-selective adrenoceptor antagonist with partial agonist activity at the beta 2-receptor as well as vasodilator properties."( Acute effects of celiprolol on muscle blood flow and insulin sensitivity: studies using [15O]-water, [18F]-fluorodeoxyglucose and positron emission tomography.
Haaparanta, M; Knuuti, MJ; Laine, H; Malminiemi, K; Nuutila, P; Oikonen, V; Ruotsalainen, U, 1997
)
1.36
"Celiprolol is a beta-adrenoceptor antagonist which has desirable ancillary properties since it is relatively cardioselective and can exert direct vasodilator and bronchodilator effects. "( Celiprolol: agonist and antagonist effects at cardiac beta 1- and vascular beta 2-adrenoceptors determined under in vivo conditions in the rat.
Alda, O; Alvarez-Guerra, M; Garay, RP, 1997
)
3.18
"Celiprolol is a novel beta-adrenoceptor blocking drug that displays clinically favorable effects on glucose and lipid metabolism. "( Effects of chronic celiprolol treatment on brown fat, feeding, and drinking in fa/fa Zucker rats.
Huupponen, R; Koulu, M; Luukkaa, V; Malminiemi, K; Pesonen, U; Rouru, J; Savontaus, E, 2000
)
2.08
"Celiprolol is a beta 1 -receptor blocker with vasodilating properties, whereas esmolol is an ultra-short-acting beta 1 -blocker."( Acute hemodynamic effects of beta-blockers in patients with severe congestive heart failure: comparison of celiprolol and esmolol.
Baumann, G; Doerffel, W; Felix, SB; Kieback, A; Stangl, K; Stangl, V; Staudt, A; Wernecke, KD, 2001
)
1.25
"Celiprolol (C) is a new selective beta 1-blocker with partial beta 2-agonistic activity. "( Short-term effects of celiprolol on blood pressure and left ventricular performance in hypertensive cardiomyopathy.
Alay, D; Cuenca, P; Lorenzo, JG; Plaza, L; Rodríguez Rodrigo, FJ; Ruiz, I; Terol, I, 1992
)
2.04
"Celiprolol is a new antihypertensive agent that represents a new generation of beta-blockers. "( Preclinical pharmacology of celiprolol: a cardioselective beta-adrenergic antagonist and mild vasodilator.
Barrett, JA; Perrone, MH, 1991
)
2.02
"Celiprolol is a new-generation beta-blocker with ancillary properties that include partial beta 2-agonism and direct vasodilating activity. "( Submaximal, but not maximal, exercise testing detects differences in the effects of beta-blockers during treadmill exercise: a study of celiprolol and atenolol. II.
Dargie, HJ; Ford, I; Grant, S; Henderson, E; McLenachan, JM, 1991
)
1.93
"Celiprolol is a potent beta blocker on beta 1-adrenoceptors and exhibits cardioselectivity both in vitro and in vivo in the pithed rat, but shows no significant in vitro alpha 1-blocking action."( Pharmacology of celiprolol.
Drummer, OH; Louis, WJ; Tung, LH, 1991
)
1.35
"Celiprolol hydrochloride is a cardioselective beta 1-adrenergic antagonist with partial agonist activity. "( Evaluation of celiprolol, a new cardioselective beta 1-adrenergic blocker with vasodilating properties, in the treatment of mild to moderate hypertension in the elderly.
Lamon, KD, 1991
)
2.08
"Celiprolol is a 'third generation' beta-blocking agent which is claimed to avoid problems associated with simpler beta-blockers, such as vasoconstriction, bronchoconstriction and myocardial depression. "( Acute haemodynamic profile of celiprolol in patients with coronary heart disease and hypertension: a double-blind comparison with metoprolol.
Franz, N; Heublein, B; Modersohn, D; Panzner, B, 1991
)
2.01
"Celiprolol is a third generation beta blocking drug with intrinsic vasodilator effect. "( [Celiprolol in the treatment of chronic stable angina].
Cuevas, G; Martínez, D; Román, O; Vargas, W, 1991
)
2.63
"Celiprolol is a hydrophilic, beta 1-selective adrenoceptor antagonist with mild selective beta 2-agonist as well as weak vasodilator properties. "( Celiprolol. An updated review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in cardiovascular disease.
Buckley, MM; Milne, RJ, 1991
)
3.17
"Celiprolol hydrochloride is a new highly cardioselective vasodilating beta-adrenoceptor antagonist that has been proven effective and safe for the treatment of essential hypertension."( Clinical safety and efficacy of celiprolol.
Lamon, KD, 1991
)
1.29
"Celiprolol is a novel cardioselective beta-blocking agent with attributed cardio-stimulating properties."( Differential actions of atenolol and celiprolol on cardiac performance in ischemic heart disease.
Frais, MA; Reynolds, G; Silke, B; Taylor, SH; Verma, SP, 1986
)
1.27
"Celiprolol HC1 is a new cardioselective beta-blocker with properties which may make it the next advance in the evolution of this class of compounds. "( Celiprolol: a new beta adrenoceptor antagonist with novel ancillary properties.
Grebow, P; Khandwala, A; Pruss, TP; Wolf, PS; Wong, L, 1986
)
3.16
"Celiprolol is a new dimension in beta-blocking therapy in that it achieves these additional hemodynamic benefits by widespread modulation of sympathoadrenal activity."( Beta-blocking drugs and myocardial function.
Taylor, SH, 1986
)
0.99
"Celiprolol is a new cardioselective beta-adrenergic blocking agent. "( A pharmacokinetic evaluation of celiprolol in healthy elderly volunteers.
Lee, EH; Muirhead, D; Norris, RJ; Sanders, SW, 1986
)
2
"Celiprolol HCl is a new cardioselective beta adrenoceptor antagonist with both mild propranolol-sensitive partial agonist activity and propranolol-insensitive cardiostimulatory properties. "( Effects of celiprolol in anesthetized dogs with reduced myocardial function.
Barrett, JA; Pruss, TP; Smith, RD; Wolf, PS, 1986
)
2.1
"Celiprolol is reported to be a new cardioselective beta blocker with novel ancillary properties including vasodilator effects. "( No evidence for a direct vasodilatory effect of celiprolol on human vasculature in vivo or in vitro.
Goldberg, P; Hughes, A; Martin, G; Sever, P; Thom, S, 1987
)
1.97
"Celiprolol is a safe, effective and well tolerated once-daily antihypertensive drug and has no detrimental effects on plasma lipids."( Celiprolol in systemic hypertension.
Flamenbaum, W; Frishman, WH; Godfrey, JC; Greenberg, S; Lazar, E; Neri, GS; Schoenberger, J; Schwartz, GL; Stevenson, A; Vidt, DG, 1989
)
2.44
"Celiprolol is a new 'cardioselective' beta-adrenoceptor blocking drug with intrinsic sympathomimetic (partial agonist) activity and a weak vasodilating effect. "( Celiprolol. A preliminary review of its pharmacodynamic and pharmacokinetic properties and its therapeutic use in hypertension and angina pectoris.
Brogden, RN; Riddell, JG; Shanks, RG, 1987
)
3.16
"Celiprolol is a new generation beta blocker with a novel profile of activity that includes a high degree of cardioselectivity, partial beta 2-agonist activity, and possibly a degree of direct peripheral vasodilation. "( Antihypertensive therapy with celiprolol: a new cardioselective beta blocker.
Norris, RJ, 1988
)
2.01
"Celiprolol was found to be an effective antianginal agent compared with placebo."( Celiprolol in angina pectoris.
Frishman, WH; Soberman, JE, 1988
)
2.44
"Celiprolol is a third-generation, beta-adrenoceptor antagonist with ancillary pharmacologic properties that are potentially advantageous in the treatment of hypertension. "( Celiprolol in hypertension.
Taylor, SH, 1988
)
3.16
"Celiprolol hydrochloride is a highly cardioselective beta1-adrenergic antagonist with a unique pharmacologic profile. "( Safety profile of celiprolol.
Lamon, KD, 1988
)
2.05
"Celiprolol is a cardioselective beta-adrenoceptor antagonist, with interesting propranolol-insensitive cardiostimulatory, vasodilatory and bronchodilatory effects. "( Celiprolol, a potent cardioselective beta 1-adrenoceptor antagonist with mild alpha 2-adrenoceptor antagonist properties.
Mann, WS; Pruss, TP; Rand, MJ; Romano, DV; Smith, RD; Wolf, PS, 1985
)
3.15
"Celiprolol is a cardioselective beta-adrenoceptor antagonist with attributed cardiostimulant properties. "( Comparative effects of metoprolol and celiprolol on cardiac hemodynamics and left ventricular volume at rest and during exercise-induced angina.
Frais, MA; Reynolds, G; Silke, B; Taylor, SH; Verma, SP, 1986
)
1.98
"Celiprolol is a newly developed cardioselective beta-blocking agent with mild beta 2-agonist and weak alpha 2-antagonist properties. "( Effects of celiprolol on plasma renin, aldosterone, norepinephrine and epinephrine in primary hypertension.
DeQuattro, V; Hernandez, PH; Kimura, S; Lee, DD, 1988
)
2.11

Effects

Celiprolol has shown equivalent antihypertensive efficacy to other beta-blockers, notably propranolol, atenolol, metoprolol and pindolol. It has a slightly beneficial effect on serum lipid profiles, and does not appear to exert adverse effects on carbohydrate metabolism.

ExcerptReferenceRelevance
"Celiprolol has a slightly beneficial effect on serum lipid profiles, and does not appear to exert adverse effects on carbohydrate metabolism."( Celiprolol. An updated review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in cardiovascular disease.
Buckley, MM; Milne, RJ, 1991
)
2.45
"Celiprolol has been previously shown in vivo to be an effective beta-adrenergic antagonist with cardio-selectivity and weak intrinsic sympathomimetic activity but no membrane stabilizing or "quinidine-like" effects. "( Effects of celiprolol (REV 5320), a new cardioselective beta-adrenoceptor antagonist, on in vitro adenylate cyclase, alpha- and beta-adrenergic receptor binding and lipolysis.
Khandwala, A; Neiss, E; Pruss, TP; Sutherland, CA; Van Inwegen, RG; Weinryb, I, 1984
)
2.1
"Celiprolol has shown equivalent antihypertensive efficacy to other beta-blockers, notably propranolol, atenolol, metoprolol and pindolol, in patients aged 18 to 75 years with mild to moderate essential hypertension."( Celiprolol. An evaluation of its pharmacological properties and clinical efficacy in the management of hypertension and angina pectoris.
Dunn, CJ; Spencer, CM, 1995
)
2.46
"Celiprolol has a slightly beneficial effect on serum lipid profiles, and does not appear to exert adverse effects on carbohydrate metabolism."( Celiprolol. An updated review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in cardiovascular disease.
Buckley, MM; Milne, RJ, 1991
)
2.45
"Celiprolol has been demonstrated to have antianginal and anti-ischemic effects comparable with both propranolol and atenolol, with a decreased incidence of bradycardia noted in the celiprolol-treated cohorts."( Clinical performance and therapeutic potential of celiprolol in angina pectoris.
Frishman, WH; Soberman, JE, 1989
)
1.25
"Celiprolol has no influence on the adenylyl cyclase activity of the dog heart."( [Intrinsic sympathomimetic action and its special features as demonstrated by the beta-1-receptor blocker celiprolol].
Pittner, H, 1985
)
1.2
"Celiprolol has to be considered as a further favourable cardioselective beta-blocker with intrinsic sympathicomimetic activity, causing a reasonable reduction in blood pressure and heart rate and moreover a propranolol-like effect in the peripheral metabolism of thyroid hormones in euthyroid patients."( [Effect of celiprolol compared to propranolol on thyroid metabolism].
Eber, O; Langsteger, W; Lind, P, 1985
)
1.38
"Celiprolol has been shown in preclinical studies to be a beta 1-selective antagonist with bronchosparing and vasodilating properties, but without any cardiodepressant effect."( Acute hemodynamic effects of celiprolol.
Donaldson, RM; Lee, EH; Williams, LA, 1988
)
1.29

Actions

Celiprolol did not activate lipolysis in rat adipocytes in vitro or stimulate human beta(3)-adrenoceptors expressed in Chinese hamster ovary cells as measured with Cytosensor microphysiometer. It does not produce bronchoconstriction but has mild propranolol-resistant bronchodilatory properties in cats.

ExcerptReferenceRelevance
"Celiprolol did not activate lipolysis in rat adipocytes in vitro or stimulate human beta(3)-adrenoceptors expressed in Chinese hamster ovary cells as measured with Cytosensor microphysiometer."( Effects of chronic celiprolol treatment on brown fat, feeding, and drinking in fa/fa Zucker rats.
Huupponen, R; Koulu, M; Luukkaa, V; Malminiemi, K; Pesonen, U; Rouru, J; Savontaus, E, 2000
)
1.36
"Celiprolol does not produce bronchoconstriction but has mild propranolol-resistant bronchodilatory properties in cats."( Preclinical pharmacology of celiprolol: a cardioselective beta-adrenergic antagonist and mild vasodilator.
Barrett, JA; Perrone, MH, 1991
)
1.3

Treatment

Celiprolol treatment in patients with essential hypertension for 12 months significantly decreased interventricular septal thickness (IVST) and LV posterior wall thickness (PWT) There was no significant correlation between IVST+PWT or LVMI and blood pressure before and after treatment.

ExcerptReferenceRelevance
"Celiprolol treatment significantly increased myocardial eNOS and activated phosphorylation of eNOS."( Celiprolol, a vasodilatory beta-blocker, inhibits pressure overload-induced cardiac hypertrophy and prevents the transition to heart failure via nitric oxide-dependent mechanisms in mice.
Asakura, M; Asano, Y; Asanuma, H; Hori, M; Kim, J; Kitakaze, M; Kitamura, S; Liao, Y; Minamino, T; Ogai, A; Sanada, S; Shintani, Y; Takashima, S; Tomoike, H, 2004
)
2.49
"Celiprolol treatment in patients with essential hypertension for 12 months significantly decreased interventricular septal thickness (IVST)+LV posterior wall thickness (PWT) and LV mass index (LVMI), but there was no significant correlation between IVST+PWT or LVMI and blood pressure before and after treatment."( Effect of celiprolol on cardiac hypertrophy in hypertension.
Haneda, T; Honda, H; Kataoka, R; Kato, J; Kikuchi, K; Matsuhashi, H; Morimoto, H; Ogawa, Y; Takenaka, T; Tanazawa, S, 2000
)
1.43
"Treatment with celiprolol is tolerated in most patients with vEDS. "( Celiprolol Treatment in Patients with Vascular Ehlers-Danlos Syndrome.
Baderkhan, H; Björck, M; Stattin, EL; Stenborg, A; Wanhainen, A, 2021
)
2.42
"Treatment with celiprolol was not associated with considerable heart rate decrease or changes of stroke volume and cardiac output."( [Use of selective long-acting beta-blocker with vasodilating activity celiprolol in patients with essential hypertension].
Mozharova, LG; Podzolkov, VI, 2002
)
0.89

Toxicity

ExcerptReferenceRelevance
" Celiprolol hydrochloride is a new highly cardioselective vasodilating beta-adrenoceptor antagonist that has been proven effective and safe for the treatment of essential hypertension."( Clinical safety and efficacy of celiprolol.
Lamon, KD, 1991
)
1.48
" The adverse experience safety data derived from 18 double-blind trials (n = 2884) were evaluated."( Safety profile of celiprolol.
Lamon, KD, 1988
)
0.61
" Therefore, they should not have adverse bronchial effects and could even have a slight bronchodilator activity."( [Safety and efficacy of celiprolol in hypertensive patients with chronic obstructive lung disease].
Bravo, C; Chahuán, M; Corradi, L; Román, O, 2000
)
0.61
" No significant adverse effects occurred."( Bisoprolol versus celiprolol on dynamic hyperinflation, cardiopulmonary exercise and domiciliary safety in COPD: a single-centre, randomised, crossover study.
Anderson, W; Lipworth, BJ; Ross, R; Short, P, 2023
)
1.24

Pharmacokinetics

A rapid and sensitive high performance, thin-layer chromatographic (HPTLC) method has been developed for the measurement of celiprolol in human plasma. The authors evaluated the contribution of the SLCO2B1 polymorphism to the pharmacokinetics o.

ExcerptReferenceRelevance
" If the apparent pharmacodynamic advantages of celiprolol translate into clinical benefits and are confirmed in well designed long term clinical trials, then celiprolol should represent a definite advance in beta-blocker therapy."( Celiprolol. An updated review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in cardiovascular disease.
Buckley, MM; Milne, RJ, 1991
)
1.98
" A pharmacokinetic study in young healthy volunteers showed a nonlinear increase in AUC with increasing dose."( A pharmacokinetic evaluation of celiprolol in healthy elderly volunteers.
Lee, EH; Muirhead, D; Norris, RJ; Sanders, SW, 1986
)
0.55
" If the apparent pharmacodynamic advantages of celiprolol are confirmed in well designed therapeutic trials then celiprolol should represent a definite advance in beta-adrenoceptor blocking therapy."( Celiprolol. A preliminary review of its pharmacodynamic and pharmacokinetic properties and its therapeutic use in hypertension and angina pectoris.
Brogden, RN; Riddell, JG; Shanks, RG, 1987
)
1.97
" Population pharmacokinetic modeling of the data with a two-compartment open model with two lag times incorporating the motility data confirmed the effect of time to gastric emptying on the variability of the oral pharmacokinetics of celiprolol."( Celiprolol double-peak occurrence and gastric motility: nonlinear mixed effects modeling of bioavailability data obtained in dogs.
Amidon, GL; Langguth, P; Lee, ID; Lipka, E; Mutschler, E; Spahn-Langguth, H, 1995
)
1.92
" The Finapres measures the peripheral pressure using the volume clamp principle; it has not been validated under altered physiological conditions and during pharmacodynamic interventions."( Reliability of blood pressure determination with the Finapres with altered physiological states or pharmacodynamic conditions.
Farrell, S; McAuley, D; Silke, B, 1997
)
0.3
"A rapid and sensitive high performance, thin-layer chromatographic (HPTLC) method has been developed for the measurement of celiprolol in human plasma and its use in pharmacokinetic studies has been evaluated."( Plasma analysis of celiprolol by HPTLC: a useful technique for pharmacokinetic studies.
Gandhi, TP; Modi, IA; Modi, RI; Pandya, KK; Satia, MC; Savale, HS,
)
0.67
"The aim of this study was to evaluate whether curcumin could modulate P-glycoprotein (P-gp) and CYP3A expression, and in turn modify the pharmacokinetic profiles of P-gp and CYP3A substrates in male Sprague-Dawley rats."( Impact of curcumin-induced changes in P-glycoprotein and CYP3A expression on the pharmacokinetics of peroral celiprolol and midazolam in rats.
Lim, LY; Tan, TM; Zhang, W, 2007
)
0.55
"The authors evaluated the contribution of the SLCO2B1 polymorphism to the pharmacokinetics of celiprolol at a microdose (MD) and therapeutic dose (TD) and compared pharmacokinetic proportionality between the 2 dose forms in 30 SLCO2B1 genotype-matched healthy volunteers."( Microdosing clinical study: pharmacokinetic, pharmacogenomic (SLCO2B1), and interaction (grapefruit juice) profiles of celiprolol following the oral microdose and therapeutic dose.
Chiyoda, T; Doi, Y; Hirota, T; Ieiri, I; Irie, S; Iwasaki, K; Kimura, M; Maeda, K; Miyagawa, M; Sasaki, T; Sugiyama, Y, 2012
)
0.81
"The aim of this study was to search for associations of genetic variants with celiprolol pharmacokinetics in a large set of pharmacokinetic genes, and, more specifically, in a set of previously identified candidate genes ABCB1, SLCO1A2, and SLCO2B1."( Pharmacogenomics of celiprolol - evidence for a role of P-glycoprotein and organic anion transporting polypeptide 1A2 in celiprolol pharmacokinetics.
Backman, JT; Hirvensalo, P; Neuvonen, M; Niemi, M; Paile-Hyvärinen, M; Tapaninen, T; Tornio, A, 2022
)
1.27

Compound-Compound Interactions

The data suggest improvements in cardiac function from the combination of celiprolol and nitrate therapy which were not achieved by either agent when used as monotherapy. The findings afford an interesting insight into the manner in which such widely utilised therapeutic modalities interact.

ExcerptReferenceRelevance
"The influence of a once daily dose of 200 mg celiprolol alone and in combination with 12."( [Uricosuric action of a new beta receptor blocker-diuretic drug combination].
Brandstetter, G; Eslaminejad, S; Hoffmann, H; Maderbacher, H, 1986
)
0.53
" These data suggest improvements in cardiac function from the combination of celiprolol and nitrate therapy which were not achieved by either agent when used as monotherapy; they afford an interesting insight into the manner in which such widely utilised therapeutic modalities interact in coronary artery disease."( A rest and exercise haemodynamic evaluation of a new cardio-selective beta-adrenoceptor blocker celiprolol alone and in combination with nitroglycerine in ischaemic heart disease.
Frais, MA; Reynolds, G; Silke, B; Taylor, SH; Verma, SP, 1986
)
0.72

Bioavailability

Orange juice substantially reduces the bioavailability of celiprolol. The mechanism of this interaction remains to be resolved.

ExcerptReferenceRelevance
" Pharmacokinetic results indicate good dose-related bioavailability in the elderly, no accumulation on multiple dosing, and pharmacokinetics equivalent to those in a younger age group."( Evaluation of celiprolol, a new cardioselective beta 1-adrenergic blocker with vasodilating properties, in the treatment of mild to moderate hypertension in the elderly.
Lamon, KD, 1991
)
0.64
" The substance was equally well absorbed both by healthy volunteers and patients with renal disease."( [Comparative pharmacokinetics of the beta-1 receptor blookader celiprolol after a single oral administration in subjects with health kidneys and in patients with impaired renal function].
Balcke, P; Deutsch, E; Minar, E; Pittner, H; Schmidt, P; Takacs, F; Zazgornik, J, 1985
)
0.51
" These results are consistent with saturable active secretion and provide an explanation for the dose-dependent bioavailability of celiprolol."( Transport of celiprolol across human intestinal epithelial (Caco-2) cells: mediation of secretion by multiple transporters including P-glycoprotein.
Artursson, P; Karlsson, J; Kuo, SM; Ziemniak, J, 1993
)
0.86
" Intravenous doses were also given to obtain disposition and bioavailability parameters."( Celiprolol double-peak occurrence and gastric motility: nonlinear mixed effects modeling of bioavailability data obtained in dogs.
Amidon, GL; Langguth, P; Lee, ID; Lipka, E; Mutschler, E; Spahn-Langguth, H, 1995
)
1.73
"Orange juice substantially reduces the bioavailability of celiprolol, but the mechanism of this interaction remains to be resolved."( Orange juice substantially reduces the bioavailability of the beta-adrenergic-blocking agent celiprolol.
Juntti-Patinen, L; Lilja, JJ; Neuvonen, PJ, 2004
)
0.79
" Drug concentration was measured by HPLC and the apparent permeability coefficient (P(app)), absorption rate constant (k(a)) and the effective permeability coefficient (P(eff)) were calculated."( [The inhibitory effect of pluronic on P-glycoprotein drug pump].
Huang, JG; Li, G; Qiu, J; Si, LQ; Wu, XG; Zuo, KY, 2007
)
0.34
"Recently, a new type of interaction has been reported in which fruit juices diminish oral drug bioavailability through inhibition of organic anion-transporting polypeptide (OATP)."( Comparison of inhibitory duration of grapefruit juice on organic anion-transporting polypeptide and cytochrome P450 3A4.
Inui, N; Miyakawa, S; Namiki, N; Takeuchi, K; Tanaka, S; Uchida, S; Watanabe, H, 2013
)
0.39
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

The effect of celiprolol at a daily dosage of 300 mg (19 patients) on peripheral blood flow of the calf and foot was compared with that of propranolol. Dose-response effects on HR were evident in the presence of atenolol.

ExcerptRelevanceReference
" Dosage reduction in patients with renal impairment does not seem to be necessary."( Comparative enantioselective pharmacokinetic studies of celiprolol in healthy volunteers and patients with impaired renal function.
Frölich, M; Hartmann, C; Knauf, H; Krauss, D; Mutschler, E; Spahn-Langguth, H, 1990
)
0.53
" Prophylactic medication for asthma was given in constant dosage for a month before the study and throughout the study."( A comparison of celiprolol and chlorthalidone in hypertensive patients with reversible bronchial obstruction.
Capone, P; Clauzel, AM; Dorow, P; Mathieu, M; Mayol, R, 1986
)
0.62
" Following titration patients were maintained at constant dosage for 12 weeks."( A randomized double-blind study of atenolol and celiprolol in mild to moderate hypertension.
Rosenthal, F; Silke, B; Taylor, S, 1986
)
0.53
" Its hemodynamic profile was compared with that of atenolol (cardioselective; no ISA) in a comparative dose-response study of 24 patients with angiographically documented coronary artery disease."( Differential actions of atenolol and celiprolol on cardiac performance in ischemic heart disease.
Frais, MA; Reynolds, G; Silke, B; Taylor, SH; Verma, SP, 1986
)
0.54
"The effects of once-daily dosing with celiprolol 200 mg, celiprolol 400 mg, and atenolol 100 mg have been studied in 19 male patients with chronic stable angina pectoris."( A single-blind randomized comparison of the 24-h antianginal efficacy of celiprolol versus atenolol.
Jackson, NC; Lee, PS; Taylor, SH, 1986
)
0.77
"In series of 20 patients suffering from atrial arrhythmias, hypertension or hyperkinetic heart syndrome in euthyroid subjects the effect of the new cardioselective beta-blocker celiprolol was examined when orally administered in doses of 300 mg per day against propranolol in a dosage of 160 mg per day."( [Effect of celiprolol compared to propranolol on thyroid metabolism].
Eber, O; Langsteger, W; Lind, P, 1985
)
0.85
" According to the method of Dettli a reduction in dosage of the beta 1-blocker, celiprolol is not necessary in patients with more or less impaired kidney function."( [Comparative pharmacokinetics of the beta-1 receptor blookader celiprolol after a single oral administration in subjects with health kidneys and in patients with impaired renal function].
Balcke, P; Deutsch, E; Minar, E; Pittner, H; Schmidt, P; Takacs, F; Zazgornik, J, 1985
)
0.74
" Computer-assisted analysis of dose-response curves resulting from the inhibition of the binding of [125I]iodopindolol by the beta-1 and beta-2 selective compounds ICI 89,406 and ICI 118,551 revealed that approximately one-third of the beta adrenergic receptors on these cells were beta-1 receptors."( Selective regulation of beta-1 and beta-2 adrenergic receptors by atypical agonists.
Barrett, DA; Molinoff, PB; Neve, KA, 1985
)
0.27
" In general Celiprolol was well accepted by the patients, the dosage being 200 mg every morning."( [Treatment of coronary heart disease with the beta-1-receptor blocker celiprolol in a long-term study over a 12-month period].
Klinger, D, 1987
)
0.89
" The results demonstrated a wide margin of safety for celiprolol over the recommended dosage range of 200 to 600 mg once daily."( Safety profile of celiprolol.
Lamon, KD, 1988
)
0.86
" Its hemodynamic profile was compared in a dose-response study with that of metoprolol, which is also cardioselective but lacks cardiostimulatory activity."( Comparative effects of metoprolol and celiprolol on cardiac hemodynamics and left ventricular volume at rest and during exercise-induced angina.
Frais, MA; Reynolds, G; Silke, B; Taylor, SH; Verma, SP, 1986
)
0.54
"The effect of celiprolol at a daily dosage of 300 mg (19 patients) was compared with that of propranolol at a daily dosage of 120 mg (14 patients) on peripheral blood flow of the calf and foot in a randomized double-blind trial."( [Comparative studies of the effect of a cardioselective and a noncardioselective beta-blocker on peripheral circulation in patients with arterial occlusive disease].
Klieber, M; Resch, F, 1986
)
0.63
" Prophylactic medication for asthma was given at a constant dosage for 1 month before the study and throughout the study."( Celiprolol--review of airways studies.
Dorow, P, 1988
)
1.72
" This dosing schedule can therefore be regarded as appropriate for antihypertensive therapy."( Evaluation of the antihypertensive effect of celiprolol by ambulatory blood pressure monitoring.
Casadei, R; Mancia, G; Parati, G; Pomidossi, G; Ravogli, A; Trazzi, S; Zanchetti, A, 1988
)
0.53
" The decrease in diastolic blood pressure at the end of the second week was significantly correlated with the reciprocal of the plasma celiprolol concentration at steady-state at the end of the dosage interval."( Comparison of the antihypertensive effects of celiprolol and acebutolol.
Belovezhdov, N; Gerova, Z; Terziivanov, D; Vlahov, V, 1988
)
0.74
" On a dosage basis, the order of antifibrillatory potency of these compounds is: carazolol-FD > propranolol-FD > carazolol > propranolol > celiprolol-FD > celiprolol."( Synthesis and pharmacological evaluation of the antifibrillatory effect of fluorinated derivatives of carazolol and celiprolol: comparison with propranolol.
Aboul-Enein, HY; Almotrefi, AA; Dzimiri, N; Premkumar, LS, 1993
)
0.7
" Before dosing and after placebo, the aortic flow velocity, acceleration and velocity integral increased progressively during exercise, as did heart rate, blood pressure and cardiac output."( A placebo controlled comparison of the effects of metoprolol and celiprolol on echo-Doppler measurements of cardiovascular function in normal volunteers.
Leitch, A; Riddell, JG; Silke, B; Thompson, A, 1995
)
0.53
" In four dogs racemic celiprolol was dosed perorally in a crossover design during four different phases of the fasted-state gastric cycle and gastric motility was recorded simultaneously using a manometric measurement system."( Celiprolol double-peak occurrence and gastric motility: nonlinear mixed effects modeling of bioavailability data obtained in dogs.
Amidon, GL; Langguth, P; Lee, ID; Lipka, E; Mutschler, E; Spahn-Langguth, H, 1995
)
2.05
"), the heart rate dose-response curves to isoprenaline were shifted to the right of those determined in matched groups of vehicle-pretreated animals."( Celiprolol: agonist and antagonist effects at cardiac beta 1- and vascular beta 2-adrenoceptors determined under in vivo conditions in the rat.
Alda, O; Alvarez-Guerra, M; Garay, RP, 1997
)
1.74
" Dose-response effects on HR with celiprolol were evident in the presence of atenolol, unlike those with propranolol that abolished the HR increase between celiprolol, 200 mg and 800 mg."( Effects of beta-adrenoceptor agonists and antagonists on heart-rate variability in normal subjects assessed using summary statistics and nonlinear procedures.
Guy, S; Riddell, JG; Silke, B, 1997
)
0.58
" The beta-blockers were administered in four dose tiers, with an increase in dosage every 15 min."( Acute hemodynamic effects of beta-blockers in patients with severe congestive heart failure: comparison of celiprolol and esmolol.
Baumann, G; Doerffel, W; Felix, SB; Kieback, A; Stangl, K; Stangl, V; Staudt, A; Wernecke, KD, 2001
)
0.52
" Three drugs (celiprolol, fexofenadine, and atenolol) were orally administered as a cassette dosing following the MD (totally 97."( Microdosing clinical study: pharmacokinetic, pharmacogenomic (SLCO2B1), and interaction (grapefruit juice) profiles of celiprolol following the oral microdose and therapeutic dose.
Chiyoda, T; Doi, Y; Hirota, T; Ieiri, I; Irie, S; Iwasaki, K; Kimura, M; Maeda, K; Miyagawa, M; Sasaki, T; Sugiyama, Y, 2012
)
0.95
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
aromatic ketoneA ketone in which the carbonyl group is attached to an aromatic ring.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (2)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
ATP-dependent translocase ABCB1Homo sapiens (human)Ki313.00000.02002.35948.5900AID681383
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Ki8.91250.00010.739610.0000AID4411
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (17)

Processvia Protein(s)Taxonomy
G2/M transition of mitotic cell cycleATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic metabolic processATP-dependent translocase ABCB1Homo sapiens (human)
response to xenobiotic stimulusATP-dependent translocase ABCB1Homo sapiens (human)
phospholipid translocationATP-dependent translocase ABCB1Homo sapiens (human)
terpenoid transportATP-dependent translocase ABCB1Homo sapiens (human)
regulation of response to osmotic stressATP-dependent translocase ABCB1Homo sapiens (human)
transmembrane transportATP-dependent translocase ABCB1Homo sapiens (human)
transepithelial transportATP-dependent translocase ABCB1Homo sapiens (human)
stem cell proliferationATP-dependent translocase ABCB1Homo sapiens (human)
ceramide translocationATP-dependent translocase ABCB1Homo sapiens (human)
export across plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
transport across blood-brain barrierATP-dependent translocase ABCB1Homo sapiens (human)
positive regulation of anion channel activityATP-dependent translocase ABCB1Homo sapiens (human)
carboxylic acid transmembrane transportATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic detoxification by transmembrane export across the plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic transport across blood-brain barrierATP-dependent translocase ABCB1Homo sapiens (human)
regulation of chloride transportATP-dependent translocase ABCB1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (14)

Processvia Protein(s)Taxonomy
protein bindingATP-dependent translocase ABCB1Homo sapiens (human)
ATP bindingATP-dependent translocase ABCB1Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
efflux transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
ATP hydrolysis activityATP-dependent translocase ABCB1Homo sapiens (human)
transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
ubiquitin protein ligase bindingATP-dependent translocase ABCB1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
carboxylic acid transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
phosphatidylcholine floppase activityATP-dependent translocase ABCB1Homo sapiens (human)
phosphatidylethanolamine flippase activityATP-dependent translocase ABCB1Homo sapiens (human)
ceramide floppase activityATP-dependent translocase ABCB1Homo sapiens (human)
floppase activityATP-dependent translocase ABCB1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (7)

Processvia Protein(s)Taxonomy
cytoplasmATP-dependent translocase ABCB1Homo sapiens (human)
plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
cell surfaceATP-dependent translocase ABCB1Homo sapiens (human)
membraneATP-dependent translocase ABCB1Homo sapiens (human)
apical plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
extracellular exosomeATP-dependent translocase ABCB1Homo sapiens (human)
external side of apical plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (13)

Assay IDTitleYearJournalArticle
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID40539Selectivity for beta-1 receptor1988Journal of medicinal chemistry, Nov, Volume: 31, Issue:11
Modeling of beta-adrenoceptors based on molecular electrostatic potential studies of agonists and antagonists.
AID41891Tested for intrinsic sympathomimetic activity (ISA); antagonist with partial agonistic properties1988Journal of medicinal chemistry, Nov, Volume: 31, Issue:11
Modeling of beta-adrenoceptors based on molecular electrostatic potential studies of agonists and antagonists.
AID681383TP_TRANSPORTER: inhibition of Taxol transepithelial transport (basal to apical) in Caco-2 cells2001Pharmaceutical research, Feb, Volume: 18, Issue:2
A functional assay for quantitation of the apparent affinities of ligands of P-glycoprotein in Caco-2 cells.
AID781326pKa (acid-base dissociation constant) as determined by Avdeef ref: DOI: 10.1002/047145026X2014Pharmaceutical research, Apr, Volume: 31, Issue:4
Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds.
AID4411Binding affinity of a compound to rat brain 5-hydroxytryptamine 1A (serotonin) receptor assayed by radiolabeled [3H]-8-OH-DPAT ligand displacement1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
Binding of arylpiperazines, (aryloxy)propanolamines, and tetrahydropyridylindoles to the 5-HT1A receptor: contribution of the molecular lipophilicity potential to three-dimensional quantitative structure-affinity relationship models.
AID409950Inhibition of human brain MAOA2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
AID679124TP_TRANSPORTER: uptake in K562 and K562/ADR cell1996The Journal of pharmacy and pharmacology, Oct, Volume: 48, Issue:10
Active secretion of drugs from the small intestinal epithelium in rats by P-glycoprotein functioning as an absorption barrier.
AID41489Selectivity towards beta-2 adrenergic receptor;Not selective towards beta-2 adrenergic receptor1988Journal of medicinal chemistry, Nov, Volume: 31, Issue:11
Modeling of beta-adrenoceptors based on molecular electrostatic potential studies of agonists and antagonists.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (395)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990150 (37.97)18.7374
1990's153 (38.73)18.2507
2000's53 (13.42)29.6817
2010's26 (6.58)24.3611
2020's13 (3.29)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 57.22

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index57.22 (24.57)
Research Supply Index6.35 (2.92)
Research Growth Index4.39 (4.65)
Search Engine Demand Index96.50 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (57.22)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials164 (40.00%)5.53%
Reviews41 (10.00%)6.00%
Case Studies6 (1.46%)4.05%
Observational1 (0.24%)0.25%
Other198 (48.29%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (4)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Phase 3 Randomized, Double-Blind, Decentralized Clinical Trial to Compare the Efficacy of Celiprolol to Placebo in the Treatment of Patients With COL3A1-Positive Vascular Ehlers-Danlos Syndrome [NCT05432466]Phase 3150 participants (Anticipated)Interventional2022-11-07Recruiting
Prevention of Postoperative Cardiac Arrythmias in Thoracic Surgery : Celiprolol Versus Diltiazem [NCT03752931]Phase 230 participants (Anticipated)Interventional2018-12-31Not yet recruiting
Proof of Concept Study to Assess the Differential Effects of Chronic Beta-blockade (Celiprolol Versus Bisoprolol) on Cardiopulmonary Outcomes at Rest and During Exercise in Chronic Obstructive Pulmonary Disease [NCT02380053]Phase 410 participants (Anticipated)Interventional2016-06-07Completed
Prevention of Vascular Complications by BetaBlocker Treatment in Vascular Ehlers-Danlos Syndrome [NCT00190411]Phase 454 participants (Actual)Interventional2003-10-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]