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- celiprolol hydrochloride
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出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2016/07/22 02:45:38」(JST)
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Celiprolol
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Systematic (IUPAC) name |
(RS)-N'-{3-acetyl-4-[3-(tert-butylamino)-2-hydroxypropoxy]phenyl}-N,N-diethylurea
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Clinical data |
AHFS/Drugs.com |
International Drug Names |
Pharmacokinetic data |
Bioavailability |
30-70% |
Biological half-life |
5 hours |
Identifiers |
CAS Number |
56980-93-9 |
ATC code |
C07AB08 (WHO) |
PubChem |
CID 2663 |
DrugBank |
DB04846 Y |
ChemSpider |
2563 |
UNII |
DRB57K47QC Y |
KEGG |
D07660 |
ChEMBL |
CHEMBL27810 |
Chemical data |
Formula |
C20H33N3O4 |
Molar mass |
379.49 g/mol |
Chirality |
Racemic mixture |
SMILES
-
O=C(N(CC)CC)Nc1ccc(OCC(O)CNC(C)(C)C)c(c1)C(=O)C
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Celiprolol (brand names Cardem, Selectol, Celipres, Celipro, Celol, Cordiax, Dilanorm) 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.
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. This study demonstrated decreased incidence of arterial rupture or dissection (a specific type of arterial rupture in which the layers of the vessel separate prior to complete failure of the artery wall).[1]
References
- ^ Ong K-T; et al. (2010). "Effect of celiprolol on prevention of cardiovascular events in vascular Ehlers-Danlos syndrome: a prospective randomised, open, blinded-endpoints trial". Lancet 376 (9751): 1476–1484. doi:10.1016/S0140-6736(10)60960-9. PMID 20825986.
External links
- Selectol Summary of Product Characteristics (from the IPHA Medicines Compendium)
- Celiprolol data sheet for New Zealand
Beta blockers (C07)
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β, non-selective |
- Alprenolol
- Bopindolol
- Bupranolol
- Carteolol
- Cloranolol
- Mepindolol
- Nadolol
- Oxprenolol
- Penbutolol
- Pindolol/Iodopindolol
- Propranolol
- Sotalol
- Tertatolol
- Timolol
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β1-selective |
- Acebutolol
- Atenolol
- Betaxolol
- Bevantolol
- Bisoprolol
- Celiprolol
- Epanolol
- Esmolol
- Metoprolol
- Nebivolol
- Practolol
- S-Atenolol
- Talinolol
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β2-selective |
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α1- + β-selective |
- Arotinolol
- Carvedilol
- Labetalol
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- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III
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UpToDate Contents
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English Journal
- Chiral β-cyclodextrin functionalized polymer monolith for the direct enantioselective reversed phase nano liquid chromatographic separation of racemic pharmaceuticals.
- Ahmed M1, Ghanem A2.Author information 1Chirality Program, Biomedical Science, University of Canberra, Canberra, Australian Capital Territory (ACT) 2601, Australia.2Chirality Program, Biomedical Science, University of Canberra, Canberra, Australian Capital Territory (ACT) 2601, Australia. Electronic address: ashraf.ghanem@canberra.edu.au.Abstract2,3,6-Tris(phenylcarbamoyl)-β-cyclodextrin-6-methacrylate was prepared and used as a functional monomer for the preparation of new β-cyclodextrin (β-CD) functionalized polymer monoliths. The polymer monoliths were prepared via the copolymerization of β-CD methacrylate and ethylene glycol dimethacrylate in different ratios in situ in fused silica capillary (internal diameter 150μm). The effect of functional monomer/cross linker concentration on the chiral separation of different classes of pharmaceuticals namely; α- and β-blockers, antiinflammatory drugs, antifungal drugs, dopamine antagonists, norepinephrine-dopamine reuptake inhibitors, catecholamines, sedative hypnotics, diuretics, antihistaminics, anticancer drugs and antiarrhythmic drugs was investigated. Baseline separation was achieved for propranolol, ifosfamide, alprenolol, tertalol, 1-indanol, tebuconazole, o-methoxymandelic acid, celiprolol and cizolertine under reversed phase conditions with mobile phase composed of methanol and water, using nano liquid chromatography. The method provides more economical analysis under environmentally benign conditions. The prepared capillary columns showed good mechanical stability and good repeatability (run-to run and batch-to batch).
- Journal of chromatography. A.J Chromatogr A.2014 Apr 16. pii: S0021-9673(14)00575-5. doi: 10.1016/j.chroma.2014.04.023. [Epub ahead of print]
- 2,3,6-Tris(phenylcarbamoyl)-β-cyclodextrin-6-methacrylate was prepared and used as a functional monomer for the preparation of new β-cyclodextrin (β-CD) functionalized polymer monoliths. The polymer monoliths were prepared via the copolymerization of β-CD methacrylate and ethylene glycol dimetha
- PMID 24786651
- Adverse respiratory effect of acute beta-blocker exposure in asthma: a systematic review and meta-analysis of randomized controlled trials.
- Morales DR, Jackson C, Lipworth BJ, Donnan PT, Guthrie B.AbstractABSTRACT BACKGROUND Beta-blockers are avoided in asthma over concerns regarding acute bronchoconstriction. Risk is greatest following acute exposure, including the potential for antagonism of beta2-agonist rescue therapy. MATERIALS AND METHODS A systematic review of databases was performed to identify all randomised, blinded, placebo-controlled clinical trials evaluating acute beta-blocker exposure in asthma. Effect estimates for changes in respiratory function, symptoms and beta2-agonist response were pooled using random effects meta-analysis with heterogeneity investigated. RESULTS Acute selective beta-blockers in the doses given caused a mean change in FEV1 of -6.9% (95%CI -8.5 to -5.2); a fall in FEV1 of ≥20% in 1 in 8 patients (P=0.03); symptoms affecting 1 in 33 patients (P=0.18); and attenuation of concomitant beta2-agonist response of -10.2% (95%CI -14.0 to -6.4). Corresponding values for acute non-selective beta-blockers in the doses given were -10.2% (95%CI -14.7 to -5.6); 1 in 9 patients (P=0.02); 1 in 13 patients (P=0.14); and -20.0% (95%CI -29.4 to -10.7). Following investigation of heterogeneity clear differences were found for celiprolol and labetalol. A dose-response relationship was demonstrated for selective beta-blockers. CONCLUSIONS Selective beta-blockers are better tolerated but not completely risk free. Risk from acute exposure may be mitigated using the smallest dose possible and beta-blockers with greater beta1-selectivity. Beta-blocker induced bronchospasm responded partially to beta2-agonists in the doses given with response blunted more by non-selective beta-blockers than selective beta-blockers. Use of beta-blockers in asthma could possibly be based upon a risk assessment on an individual patient basis.
- Chest.Chest.2013 Nov 7. doi: 10.1378/chest.13-1235. [Epub ahead of print]
- ABSTRACT BACKGROUND Beta-blockers are avoided in asthma over concerns regarding acute bronchoconstriction. Risk is greatest following acute exposure, including the potential for antagonism of beta2-agonist rescue therapy. MATERIALS AND METHODS A systematic review of databases was performed to identi
- PMID 24202435
- Celiprolol reduces oxidative stress and attenuates left ventricular remodeling induced by hypoxic stress in mice.
- Nishioka S1, Yoshioka T, Nomura A, Kato R, Miyamura M, Okada Y, Ishizaka N, Matsumura Y, Hayashi T.Author information 1Laboratory of Pathological and Molecular Pharmacology, Osaka University of Pharmaceutical Sciences, Osaka, Japan.AbstractWe have previously reported that intermittent hypoxic stress, which is relevant to sleep apnea syndrome (SAS), increases oxidative stress and induces left ventricular (LV) remodeling. Celiprolol, a β1-selective adrenoreceptor blocker, is known to have not only an antihypertensive effect but also an antioxidant effect through releasing nitric oxide. The aim of this study was to examine the hypothesis that celiprolol might ameliorate the LV remodeling induced by intermittent hypoxia through its antioxidant effect. Male C57BL/6J mice (8 weeks old) were exposed to intermittent hypoxia (30 s of 5% oxygen followed by 30 s of 21% oxygen) for 8 h day(-1) during the daytime for 10 consecutive days or were maintained under normoxic conditions. Animals were treated with either celiprolol (100 mg kg(-1) day(-1) by gavage) or vehicle. Hypoxic stress caused fluctuations in blood pressure (BP), an increase in the mean cardiomyocyte diameter, perivascular fibrosis and a decrease in endothelial nitric oxide synthase (eNOS) expression. These changes were associated with increased levels of 4-hydroxy-2-nonenal protein, superoxide, tumor necrosis factor-α mRNA and brain natriuretic peptide mRNA in the LV myocardium. Celiprolol significantly suppressed BP fluctuation, restored eNOS expression and reduced oxidative stress and superoxide production, thus ameliorating hypoxia-induced LV remodeling in mice. These findings suggest that treatment with celiprolol might prevent cardiovascular events in borderline hypertensive patients with SAS.
- Hypertension research : official journal of the Japanese Society of Hypertension.Hypertens Res.2013 Nov;36(11):934-9. doi: 10.1038/hr.2013.60. Epub 2013 Jun 20.
- We have previously reported that intermittent hypoxic stress, which is relevant to sleep apnea syndrome (SAS), increases oxidative stress and induces left ventricular (LV) remodeling. Celiprolol, a β1-selective adrenoreceptor blocker, is known to have not only an antihypertensive effect but also an
- PMID 23784509
Japanese Journal
- Effects of Itraconazole, Dexamethasone and Naringin on the Pharmacokinetics of Nadolol in Rats
- Comparison of Inhibitory Duration of Grapefruit Juice on Organic Anion-Transporting Polypeptide and Cytochrome P450 3A4
- Involvement of influx and efflux transport systems in gastrointestinal absorption of celiprolol
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