CELIPROLOL

Possibly Marketed Outside US

Details

Stereochemistry	RACEMIC
Molecular Formula	C20H33N3O4
Molecular Weight	379.4937
Optical Activity	( + / - )
Defined Stereocenters	0 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CCN(CC)C(=O)NC1=CC=C(OCC(O)CNC(C)(C)C)C(=C1)C(C)=O

InChI

InChIKey=JOATXPAWOHTVSZ-UHFFFAOYSA-N

InChI=1S/C20H33N3O4/c1-7-23(8-2)19(26)22-15-9-10-18(17(11-15)14(3)24)27-13-16(25)12-21-20(4,5)6/h9-11,16,21,25H,7-8,12-13H2,1-6H3,(H,22,26)

HIDE SMILES / InChI

Description
Sources: http://www.medicines.ie/document.aspx?documentId=12378
Curator's Comment: description was created based on several sources, including https://www.drugs.com/international/celiprolol.html | https://www.ncbi.nlm.nih.gov/pubmed/20825986 | http://onlinelibrary.wiley.com/doi/10.1111/j.1527-3466.1984.tb00456.x/abstract

Celiprolol is beta blocker, used to treat high blood pressure. Celiprolol is a selective β1 receptor antagonist, β2 receptor partial agonist. Celiprolol is not approved by the FDA, but is available worldwide under brand names Cardem, Selectol, Celipres, Celipro, Celol, Cordiax, Dilanorm. It is used to treat mild to moderate hypertension and angina prectoris. In 2010 celiprolol has demonstrated positive results in the prevention of vascular complications of Ehlers-Danlos syndrome. Celiprolol has fewer CNS-related side effects than other beta blockers presumably because of limited penetration through blood-brain barrier because of its solubility.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Beta-1 adrenergic receptor 163 Target ID: CHEMBL213 Sources: http://www.medicines.ie/document.aspx?documentId=12378	Antagonist 2849		0.35 nM [Ki]
Beta-2 adrenergic receptor 209 Target ID: CHEMBL210 Sources: http://www.medicines.ie/document.aspx?documentId=12378	Partial Agonist 297		2.8 nM [Ki]

Conditions

Condition	Modality	Highest Phase	Product
Ehlers-Danlos syndrome 2 Sources: https://www.ncbi.nlm.nih.gov/pubmed/20825986	Palliative	Phase IV 63	Unknown Approved Use Unknown
Angina pectoris 110 Sources: http://www.medicines.ie/document.aspx?documentId=12378	Palliative	Approved 8583	SELECTOL Approved Use Celiprolol is a vasodilating beta-1 selective adrenoceptor antagonist with partial beta-2 agonist activity. The beta-2 agonist activity is thought to account for its mild vasodilating and positive inotropic properties. It lowers the blood pressure in hypertensive patients at rest and exercise. The effects on heart rate and cardiac output are dependent on the pre-existing background level of sympathetic tone.
Mild to moderate hypertension 2 Sources: http://www.medicines.ie/document.aspx?documentId=12378	Primary	Approved 8583	SELECTOL Approved Use Celiprolol is a vasodilating beta-1 selective adrenoceptor antagonist with partial beta-2 agonist activity. The beta-2 agonist activity is thought to account for its mild vasodilating and positive inotropic properties. It lowers the blood pressure in hypertensive patients at rest and exercise. The effects on heart rate and cardiac output are dependent on the pre-existing background level of sympathetic tone.
Chronic obstructive pulmonary disease 175 Sources: https://clinicaltrials.gov/ct2/show/NCT02380053	Palliative	Phase IV 63	Unknown Approved Use Unknown

C_max

Value	Dose	Analyte	Population
13.1 ng/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/530263_2149029F1020_1_14F_1F.pdf#page=19	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	CELIPROLOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
116 ng/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/530263_2149029F1020_1_14F_1F.pdf#page=19	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	CELIPROLOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
295 ng/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/530263_2149029F1020_1_14F_1F.pdf#page=19	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	CELIPROLOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
855 ng/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/530263_2149029F1020_1_14F_1F.pdf#page=19	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	CELIPROLOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
477 ng/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/530263_2149029F1020_1_14F_1F.pdf#page=20	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	CELIPROLOL plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
187 ng/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/530263_2149029F1020_1_14F_1F.pdf#page=20	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	CELIPROLOL plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
624 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/34585840/	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	CELIPROLOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
307 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/34585840/	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	CELIPROLOL, S- plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
317 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/34585840/	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	CELIPROLOL, R- plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
687 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2427859/	200 mg 1 times / day multiple, oral dose: 200 mg route of administration: Oral experiment type: MULTIPLE co-administered:	CELIPROLOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
597 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2427859/	200 mg 1 times / day multiple, oral dose: 200 mg route of administration: Oral experiment type: MULTIPLE co-administered:	CELIPROLOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
1583 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2427859/	400 mg 1 times / day multiple, oral dose: 400 mg route of administration: Oral experiment type: MULTIPLE co-administered:	CELIPROLOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
1676 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2427859/	400 mg 1 times / day multiple, oral dose: 400 mg route of administration: Oral experiment type: MULTIPLE co-administered:	CELIPROLOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
2478 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2427859/	600 mg 1 times / day multiple, oral dose: 600 mg route of administration: Oral experiment type: MULTIPLE co-administered:	CELIPROLOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
2597 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2427859/	600 mg 1 times / day multiple, oral dose: 600 mg route of administration: Oral experiment type: MULTIPLE co-administered:	CELIPROLOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

AUC

Value	Dose	Analyte	Population
47.6 ng × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/530263_2149029F1020_1_14F_1F.pdf#page=19	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	CELIPROLOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
304 ng × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/530263_2149029F1020_1_14F_1F.pdf#page=19	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	CELIPROLOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
1830 ng × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/530263_2149029F1020_1_14F_1F.pdf#page=19	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	CELIPROLOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
6810 ng × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/530263_2149029F1020_1_14F_1F.pdf#page=19	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	CELIPROLOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
3063 ng × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/530263_2149029F1020_1_14F_1F.pdf#page=20	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	CELIPROLOL plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
1812 ng × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/530263_2149029F1020_1_14F_1F.pdf#page=20	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	CELIPROLOL plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
3262 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/34585840/	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	CELIPROLOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
1642 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/34585840/	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	CELIPROLOL, S- plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
1619 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/34585840/	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	CELIPROLOL, R- plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
3688 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2427859/	200 mg 1 times / day multiple, oral dose: 200 mg route of administration: Oral experiment type: MULTIPLE co-administered:	CELIPROLOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
3317 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2427859/	200 mg 1 times / day multiple, oral dose: 200 mg route of administration: Oral experiment type: MULTIPLE co-administered:	CELIPROLOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
9092 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2427859/	400 mg 1 times / day multiple, oral dose: 400 mg route of administration: Oral experiment type: MULTIPLE co-administered:	CELIPROLOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
9729 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2427859/	400 mg 1 times / day multiple, oral dose: 400 mg route of administration: Oral experiment type: MULTIPLE co-administered:	CELIPROLOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
15020 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2427859/	600 mg 1 times / day multiple, oral dose: 600 mg route of administration: Oral experiment type: MULTIPLE co-administered:	CELIPROLOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
16550 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2427859/	600 mg 1 times / day multiple, oral dose: 600 mg route of administration: Oral experiment type: MULTIPLE co-administered:	CELIPROLOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

T_1/2

Value	Dose	Analyte	Population
3.94 h OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/530263_2149029F1020_1_14F_1F.pdf#page=19	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	CELIPROLOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
1.45 h OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/530263_2149029F1020_1_14F_1F.pdf#page=19	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	CELIPROLOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
4.81 h OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/530263_2149029F1020_1_14F_1F.pdf#page=19	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	CELIPROLOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
5.89 h OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/530263_2149029F1020_1_14F_1F.pdf#page=19	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	CELIPROLOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
4.5 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/34585840/	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	CELIPROLOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
4.7 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/34585840/	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	CELIPROLOL, S- plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
4.3 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/34585840/	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	CELIPROLOL, R- plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
5.61 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2427859/	200 mg 1 times / day multiple, oral dose: 200 mg route of administration: Oral experiment type: MULTIPLE co-administered:	CELIPROLOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
7.91 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2427859/	200 mg 1 times / day multiple, oral dose: 200 mg route of administration: Oral experiment type: MULTIPLE co-administered:	CELIPROLOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
5 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2427859/	400 mg 1 times / day multiple, oral dose: 400 mg route of administration: Oral experiment type: MULTIPLE co-administered:	CELIPROLOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
7.49 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2427859/	400 mg 1 times / day multiple, oral dose: 400 mg route of administration: Oral experiment type: MULTIPLE co-administered:	CELIPROLOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
5.44 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2427859/	600 mg 1 times / day multiple, oral dose: 600 mg route of administration: Oral experiment type: MULTIPLE co-administered:	CELIPROLOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
7.33 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2427859/	600 mg 1 times / day multiple, oral dose: 600 mg route of administration: Oral experiment type: MULTIPLE co-administered:	CELIPROLOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

F_unbound

Value	Dose	Co-administered	Analyte	Population
73% OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/530263_2149029F1020_1_14F_1F.pdf#page=20			CELIPROLOL plasma	Homo sapiens
75% REVIEW https://pubmed.ncbi.nlm.nih.gov/28742547/			CELIPROLOL plasma	Homo sapiens

Doses

Dose	Population	Adverse events
1200 mg single, oral Highest studied dose Dose: 1200 mg Route: oral Route: single Dose: 1200 mg Sources: https://pubmed.ncbi.nlm.nih.gov/8390369/	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M Food Status: FASTED Sources: https://pubmed.ncbi.nlm.nih.gov/8390369/	Sources: https://pubmed.ncbi.nlm.nih.gov/8390369/
200 mg 1 times / day multiple, oral Recommended Dose: 200 mg, 1 times / day Route: oral Route: multiple Dose: 200 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/8098286/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/8098286/	Disc. AE: Pneumonitis... AEs leading to discontinuation/dose reduction: Pneumonitis Sources: https://pubmed.ncbi.nlm.nih.gov/8098286/

AEs

AE	Significance	Dose	Population
Pneumonitis	Disc. AE	200 mg 1 times / day multiple, oral Recommended Dose: 200 mg, 1 times / day Route: oral Route: multiple Dose: 200 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/8098286/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/8098286/

PubMed

Title	Date	PubMed
Development of a list of potentially inappropriate drugs for the korean elderly using the delphi method.	2010-12	21818443
Human health risk assessment of pharmaceuticals in water: issues and challenges ahead.	2010-11	21139869
Fruit juice inhibition of uptake transport: a new type of food-drug interaction.	2010-11	21039758
Effect of celiprolol on prevention of cardiovascular events in vascular Ehlers-Danlos syndrome: a prospective randomised, open, blinded-endpoints trial.	2010-10-30	20825986
Celiprolol therapy for vascular Ehlers-Danlos syndrome.	2010-10-30	20825985
Positive influence of AT(1) receptor antagonism upon the impaired celiprolol-induced vasodilatation in aorta from spontaneously hypertensive rats.	2010-10-10	20637193
Highly sensitive transient isotachophoresis sample stacking coupling with capillary electrophoresis-amperometric detection for analysis of doping substances.	2010-06-15	20441897
[Endothelial dysfunction: role of vasodilating betablockers in hypertension and chronic heart failure].	2010-04	20399940
Fate of beta blockers in aquatic-sediment systems: sorption and biotransformation.	2010-02-01	20030338
Chiral separations of some beta-adrenergic agonists and antagonists on AmyCoat column by HPLC.	2010-01	19208401
Acute pulmonary edema due to stress cardiomyopathy in a patient with aortic stenosis: a case report.	2009-12-02	20062645
Modification of pharmacokinetics of norfloxacin following oral administration of curcumin in rabbits.	2009-12	19934593
Analysis of drug interactions involving fruit beverages and organic anion-transporting polypeptides.	2009-12	19789373
The role of transporters in the pharmacokinetics of orally administered drugs.	2009-09	19568696
Uptake/efflux transport of tramadol enantiomers and O-desmethyl-tramadol: focus on P-glycoprotein.	2009-09	19496778
Evaluation of left atrial volumes using multidetector computed tomography: comparison with echocardiography.	2009-08-20	20461182
Involvement of influx and efflux transport systems in gastrointestinal absorption of celiprolol.	2009-07	19067419
Chiral separation of beta-adrenergic blockers on CelluCoat column by HPLC.	2009-04-30	19203609
Immune defects in Alzheimer's disease: new medications development.	2008-12-03	19090986
Direct determination of celiprolol in human urine using on-line coupled ITP-CZE method with fiber-based DAD.	2008-11	18975302
American College of Endocrinology Pre-Diabetes Consensus Conference: part two.	2008-11	18955719
Progress in the development of early diagnosis and a drug with unique pharmacology to improve cancer therapy.	2008-10-13	18644768
Effects of the antioxidative beta-blocker celiprolol on endothelial progenitor cells in hypertensive rats.	2008-09	18636069
Ozonation of reverse osmosis concentrate: kinetics and efficiency of beta blocker oxidation.	2008-06	18472125
Simultaneous separation of eight beta-adrenergic drugs using titanium dioxide nanoparticles as additive in capillary electrophoresis.	2008-06	18435493
Effect of pluronic F68 block copolymer on P-glycoprotein transport and CYP3A4 metabolism.	2008-05-22	18242899
Hesperidin in orange juice reduces the absorption of celiprolol in rats.	2008-04	18344215
Natural and synthetic polymers as inhibitors of drug efflux pumps.	2008-03	17896100
Effects of the vasodilating beta-blocker nebivolol on smoking-induced endothelial dysfunction in young healthy volunteers.	2008	19066009
Carvedilol in hypertension treatment.	2008	18629377
[The inhibitory effect of pluronic on P-glycoprotein drug pump].	2007-09	18050744
Metabolic syndrome: treatment of hypertensive patients.	2007-08-02	17667215
Separation of beta-receptor blockers and analogs by capillary liquid chromatography (CLC) and pressurized capillary electrochromatography (pCEC) using a vancomycin chiral stationary phase column.	2007-08	17867552
Ehlers-Danlos syndrome type IV.	2007-07-19	17640391
Celiprolol reduces the intimal thickening of autogenous vein grafts via an enhancement of nitric oxide function through an inhibition of superoxide production.	2007-07	17606127
Celiprolol, a selective beta1-blocker, reduces the infarct size through production of nitric oxide in a rabbit model of myocardial infarction.	2007-04	17384462
beta1 antagonist and beta2 agonist, celiprolol, restores the impaired endothelial dependent and independent responses and decreased TNFalpha in rat with type II diabetes.	2007-01-16	17141277
Impact of curcumin-induced changes in P-glycoprotein and CYP3A expression on the pharmacokinetics of peroral celiprolol and midazolam in rats.	2007-01	17050652
Beneficial effect of combination therapy with antihypertensive drugs in patients with hypertension.	2007	18650977
Beta-blockers use in patients with chronic obstructive pulmonary disease and concomitant cardiovascular conditions.	2007	18268926
Celiprolol-induced lupus-like syndrome.	2006-12	17205925
[Vascular Ehlers-Danlos syndrome].	2006-12	17159712
Effects of celiprolol and simvastatin on the calculated risk of coronary heart disease (the Celisimva study).	2006-06	16798663
Concurrent dolichoectasia of basilar and coronary arteries.	2006-05-09	16682695
Non-neuroleptic catecholaminergic drugs for neuroleptic-induced tardive dyskinesia.	2006-01-25	16437424
Screening of domperidone in wastewater by high performance liquid chromatography and solid phase extraction methods.	2006-01-15	18970411
[Identification of blockers of adrenergic beta-receptors by thin layer chromatography].	2006-01	16506605
[Pharmacological studies of celiprolol: III. Effects of celiprolol on the cardiovascular system and renal function, and its antiarrhythmic effects].	1990-04	1973400
[Pharmacological studies of celiprolol: I. Beta-blocking effect, intrinsic sympathomimetic activity, vasodilating and hypotensive effects].	1990-04	1973398
Anti-ischemic effects of celiprolol in patients with exercise-induced angina pectoris.	1989-10	2571590

Patents

Sample Use Guides

In Vivo Use Guide

The route of administration is oral. The usual dose in adults is 200 mg once daily in the morning. In the case of an inadequate response the dose may be increased to 400 mg daily. It is important to take Selectol one hour before or two hours after food with a glass of water. If the treatment is to be discontinued, reduce the dosage gradually over a period of 1-2 weeks. In hypertensive patients, additional treatment with other anti-hypertensive agents according to clinical guidelines is possible, in particular with diuretics. When a combination is initiated an increased monitoring of the blood pressure is recommended.

Route of Administration: Oral

In Vitro Use Guide

In order to quantify the affinity constants and potential partial agonist properties of beta-adrenoceptor antagonists at beta1-and beta2-adrenoceptors, competitive experiments for binding of [125I]-iodocyanopindolol (specific activity 2000 Cimmol-1) to beta-adrenoceptors were performed. Specific binding was defined as the difference in binding in the absence and in the presence of propranolol (3 umol^-1). Celiprolol at increasing concentrations (0.0001-100 umol-1) was used for binding experiments with lung, and with myocardial tissue. The experiments were performed in the presence and absence of Gpp(NH)p to evaluate agonist properties of the beta-adrenoceptor antagonists by changing the agonist affinity state of the binding site in the presence of the metabolically stable guanine nucleotide.

Name

Type

Language

CELIPROLOL

Official Name

English

CELIPROLOL PCH

Preferred Name

English

Celiprolol [WHO-DD]

Common Name

English

celiprolol [INN]

Common Name

English

ACER-002 FREE BASE

Code

English

N-[3-acetyl-4-[(2RS)-3-(tert-butylamino)-2-hydroxypropoxy]phenyl]-N?-tert-butylurea

Systematic Name

English

UREA, N'-(3-ACETYL-4-(3-((1,1-DIMETHYLETHYL)AMINO)-2-HYDROXYPROPOXY)PHENYL)-N,N-DIETHYL-

Systematic Name

English

CELIPROLOL [MI]

Common Name

English

ACER002 FREE BASE

Code

English

CELIPROLOL [VANDF]

Common Name

English

3-(3-ACETYL-4-(3-(TERT-BUTYLAMINO)-2-HYDROXYPROPOXY)PHENYL)-1,1-DIETHYLUREA

Systematic Name

English

CELIPROLOL HYDROCHLORIDE IMPURITY C [EP IMPURITY]

Common Name

English

Classification Tree Code System Code

WHO-VATC

QC07AB08