Peringatan Keamanan

No data are available regarding celiprolol overdose in humans. The most common symptoms to be expected following overdosage with beta-adrenoceptor blocking agents are bradycardia, hypotension, bronchospasm and acute cardiac insufficiency.

Celiprolol

DB04846

small molecule approved investigational

Deskripsi

Celiprolol is indicated for the management of mild to moderate hypertension and effort-induced angina pectoris. It is simultaneously a selective ?1 receptor antagonist, a ?2 receptor partial agonist and a weak ?2 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). Celiprolol is not approved for use by the FDA in the treatment of vascular Ehlers–Danlos syndrome.

Struktur Molekul 2D

Berat 379.501
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) 5 hours
Volume Distribusi The distribution volume is 4.5L/kg. Celiprolol is hydrophilic and does not cross the blood-brain barrier. The binding to plasma proteins is about 25-30%.
Klirens (Clearance) Cleared by both renal and non-renal excretory pathways. Celiprolol is not recommended for patients with creatinine clearance less than 15 mL per minute.

Absorpsi

Absorption of an oral dose is rapid and consistent but incomplete (55% for 200 mg dose and 74% for 400 mg dose) from the gastrointestinal tract. The bioavailability of celiprolol has been shown to be markedly affected by food and one should avoid administration of celiprolol with food. Coadministration of chlorthalidone, hydrochlorothiazide and theophylline also reduces the bioavailability of celiprolol. Following oral dosing, maximal blood concentrations are reached between 2 and 3 hours.

Metabolisme

A 14C labelled dose was completely recovered within 48 hours. The first-pass effect in the liver is insignificant. Celiprolol is metabolized to a minor extent (1-3%).

Rute Eliminasi

Data eliminasi belum tersedia.

Interaksi Makanan

3 Data
  • 1. Avoid fruit juice. Orange juice may reduce the absorption of celiprolol.
  • 2. Avoid grapefruit products. Grapefruit juice may reduce the absorption of celiprolol.
  • 3. Take with or without food. The bioavailability of celiprolol may be reduced when taken with food, however, it is unlikely that this reduction is clinically relevant.

Interaksi Obat

1548 Data
Ceritinib Celiprolol may increase the bradycardic activities of Ceritinib.
Ivabradine Celiprolol may increase the bradycardic activities of Ivabradine.
Ruxolitinib Ruxolitinib may increase the bradycardic activities of Celiprolol.
Alfuzosin Alfuzosin may increase the hypotensive activities of Celiprolol.
Amifostine Celiprolol may increase the hypotensive activities of Amifostine.
Diazoxide Diazoxide may increase the hypotensive activities of Celiprolol.
Methylphenidate Methylphenidate may decrease the antihypertensive activities of Celiprolol.
Dexmethylphenidate Dexmethylphenidate may decrease the antihypertensive activities of Celiprolol.
Obinutuzumab Celiprolol may increase the hypotensive activities of Obinutuzumab.
Pentoxifylline Pentoxifylline may increase the hypotensive activities of Celiprolol.
Rituximab Celiprolol may increase the hypotensive activities of Rituximab.
Desmopressin Desmopressin may decrease the antihypertensive activities of Celiprolol.
Zolmitriptan Zolmitriptan may decrease the antihypertensive activities of Celiprolol.
Doxapram Doxapram may decrease the antihypertensive activities of Celiprolol.
Naratriptan Naratriptan may decrease the antihypertensive activities of Celiprolol.
Rizatriptan Rizatriptan may decrease the antihypertensive activities of Celiprolol.
Frovatriptan Frovatriptan may decrease the antihypertensive activities of Celiprolol.
Dutasteride Dutasteride may decrease the antihypertensive activities of Celiprolol.
Finasteride Finasteride may decrease the antihypertensive activities of Celiprolol.
Epicaptopril Epicaptopril may decrease the antihypertensive activities of Celiprolol.
1-benzylimidazole 1-benzylimidazole may decrease the antihypertensive activities of Celiprolol.
Naluzotan Naluzotan may decrease the antihypertensive activities of Celiprolol.
Nitrous oxide Nitrous oxide may decrease the antihypertensive activities of Celiprolol.
Cinitapride Cinitapride may decrease the antihypertensive activities of Celiprolol.
Ifenprodil Ifenprodil may decrease the antihypertensive activities of Celiprolol.
Moxisylyte Moxisylyte may decrease the antihypertensive activities of Celiprolol.
Atipamezole Atipamezole may decrease the antihypertensive activities of Celiprolol.
Tetrahydrocannabivarin Tetrahydrocannabivarin may decrease the antihypertensive activities of Celiprolol.
Piclozotan Piclozotan may decrease the antihypertensive activities of Celiprolol.
Siponimod Siponimod may decrease the antihypertensive activities of Celiprolol.
Idazoxan Idazoxan may decrease the antihypertensive activities of Celiprolol.
Trichloroethylene Trichloroethylene may decrease the antihypertensive activities of Celiprolol.
Xenon Xenon may decrease the antihypertensive activities of Celiprolol.
Buflomedil Buflomedil may decrease the antihypertensive activities of Celiprolol.
5-methoxy-N,N-dimethyltryptamine 5-methoxy-N,N-dimethyltryptamine may decrease the antihypertensive activities of Celiprolol.
Quinoline Yellow WS Quinoline Yellow WS may decrease the antihypertensive activities of Celiprolol.
Solriamfetol Solriamfetol may decrease the antihypertensive activities of Celiprolol.
Sufentanil Sufentanil may decrease the antihypertensive activities of Celiprolol.
Remifentanil Remifentanil may decrease the antihypertensive activities of Celiprolol.
Halothane Halothane may decrease the antihypertensive activities of Celiprolol.
Sumatriptan Sumatriptan may decrease the antihypertensive activities of Celiprolol.
Alfentanil Alfentanil may decrease the antihypertensive activities of Celiprolol.
Fentanyl Fentanyl may decrease the antihypertensive activities of Celiprolol.
Flibanserin Flibanserin may decrease the antihypertensive activities of Celiprolol.
Diethyl ether Diethyl ether may decrease the antihypertensive activities of Celiprolol.
Selpercatinib Selpercatinib may decrease the antihypertensive activities of Celiprolol.
Naxitamab Naxitamab may decrease the antihypertensive activities of Celiprolol.
Linezolid The risk or severity of hypertension can be increased when Linezolid is combined with Celiprolol.
Amiodarone The therapeutic efficacy of Celiprolol can be increased when used in combination with Amiodarone.
Bupivacaine The serum concentration of Bupivacaine can be increased when it is combined with Celiprolol.
Dipyridamole Dipyridamole may increase the bradycardic activities of Celiprolol.
Disopyramide Disopyramide may increase the bradycardic activities of Celiprolol.
Dronedarone Dronedarone may increase the bradycardic activities of Celiprolol.
Fingolimod Celiprolol may increase the bradycardic activities of Fingolimod.
Floctafenine The risk or severity of adverse effects can be increased when Celiprolol is combined with Floctafenine.
Mepivacaine The serum concentration of Mepivacaine can be increased when it is combined with Celiprolol.
Methacholine Celiprolol may increase the bronchoconstrictory activities of Methacholine.
Midodrine The therapeutic efficacy of Midodrine can be decreased when used in combination with Celiprolol.
Nifedipine The risk or severity of congestive heart failure and hypotension can be increased when Nifedipine is combined with Celiprolol.
Propafenone The risk or severity of adverse effects can be increased when Propafenone is combined with Celiprolol.
Regorafenib Regorafenib may increase the bradycardic activities of Celiprolol.
Reserpine Reserpine may increase the hypotensive activities of Celiprolol.
Deserpidine Deserpidine may increase the hypotensive activities of Celiprolol.
Guanethidine Guanethidine may increase the hypotensive activities of Celiprolol.
Rivastigmine Celiprolol may increase the bradycardic activities of Rivastigmine.
Benzylpenicilloyl polylysine Celiprolol may decrease effectiveness of Benzylpenicilloyl polylysine as a diagnostic agent.
Spironolactone The risk or severity of hyperkalemia can be increased when Celiprolol is combined with Spironolactone.
Flunisolide The risk or severity of hypokalemia can be increased when Flunisolide is combined with Celiprolol.
Beclomethasone dipropionate The risk or severity of hypokalemia can be increased when Beclomethasone dipropionate is combined with Celiprolol.
Betamethasone The risk or severity of hypokalemia can be increased when Betamethasone is combined with Celiprolol.
Fluticasone propionate The risk or severity of hypokalemia can be increased when Fluticasone propionate is combined with Celiprolol.
Fluocinolone acetonide The risk or severity of hypokalemia can be increased when Fluocinolone acetonide is combined with Celiprolol.
Triamcinolone The risk or severity of hypokalemia can be increased when Triamcinolone is combined with Celiprolol.
Prednisone The risk or severity of hypokalemia can be increased when Prednisone is combined with Celiprolol.
Fludrocortisone The risk or severity of hypokalemia can be increased when Fludrocortisone is combined with Celiprolol.
Hydrocortisone The risk or severity of hypokalemia can be increased when Hydrocortisone is combined with Celiprolol.
Prednisolone The risk or severity of hypokalemia can be increased when Prednisolone is combined with Celiprolol.
Methylprednisolone The risk or severity of hypokalemia can be increased when Methylprednisolone is combined with Celiprolol.
Trilostane The risk or severity of hypokalemia can be increased when Trilostane is combined with Celiprolol.
Budesonide The risk or severity of hypokalemia can be increased when Budesonide is combined with Celiprolol.
Dexamethasone The risk or severity of hypokalemia can be increased when Dexamethasone is combined with Celiprolol.
Corticotropin The risk or severity of hypokalemia can be increased when Corticotropin is combined with Celiprolol.
Cortisone acetate The risk or severity of hypokalemia can be increased when Cortisone acetate is combined with Celiprolol.
Paramethasone The risk or severity of hypokalemia can be increased when Paramethasone is combined with Celiprolol.
Ciclesonide The risk or severity of hypokalemia can be increased when Ciclesonide is combined with Celiprolol.
Aldosterone The risk or severity of hypokalemia can be increased when Aldosterone is combined with Celiprolol.
Fluticasone furoate The risk or severity of hypokalemia can be increased when Fluticasone furoate is combined with Celiprolol.
Fluprednidene The risk or severity of hypokalemia can be increased when Fluprednidene is combined with Celiprolol.
Tixocortol The risk or severity of hypokalemia can be increased when Tixocortol is combined with Celiprolol.
Fluprednisolone The risk or severity of hypokalemia can be increased when Fluprednisolone is combined with Celiprolol.
Meprednisone The risk or severity of hypokalemia can be increased when Meprednisone is combined with Celiprolol.
Dexamethasone isonicotinate The risk or severity of hypokalemia can be increased when Dexamethasone isonicotinate is combined with Celiprolol.
Melengestrol The risk or severity of hypokalemia can be increased when Melengestrol is combined with Celiprolol.
Deflazacort The risk or severity of hypokalemia can be increased when Deflazacort is combined with Celiprolol.
Cortivazol The risk or severity of hypokalemia can be increased when Cortivazol is combined with Celiprolol.
Prednylidene The risk or severity of hypokalemia can be increased when Prednylidene is combined with Celiprolol.
Fluocortin The risk or severity of hypokalemia can be increased when Fluocortin is combined with Celiprolol.
Fluperolone The risk or severity of hypokalemia can be increased when Fluperolone is combined with Celiprolol.
Cloprednol The risk or severity of hypokalemia can be increased when Cloprednol is combined with Celiprolol.
Fluclorolone The risk or severity of hypokalemia can be increased when Fluclorolone is combined with Celiprolol.

Target Protein

Beta-1 adrenergic receptor ADRB1
Beta-2 adrenergic receptor ADRB2
Beta-3 adrenergic receptor ADRB3
Alpha-2A adrenergic receptor ADRA2A
Alpha-2B adrenergic receptor ADRA2B
Alpha-2C adrenergic receptor ADRA2C

Referensi & Sumber

Synthesis reference: Zolss, G., Pittner, H., Stormann-Menninger-Lerchenthal, H. and Lindner, I.; US. Patent 3,983,169; September 28,1976; assigned to Chemie Linz AG (Austria).
Artikel (PubMed)
  • PMID: 20825986
    Ong KT, Perdu J, De Backer J, Bozec E, Collignon P, Emmerich J, Fauret AL, Fiessinger JN, Germain DP, Georgesco G, Hulot JS, De Paepe A, Plauchu H, Jeunemaitre X, Laurent S, Boutouyrie P: 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. doi: 10.1016/S0140-6736(10)60960-9. Epub 2010 Sep 7.

Contoh Produk & Brand

Produk: 0 • International brands: 1
International Brands
  • Selectol — Sanofi

Sekuens Gen/Protein (FASTA)

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