Peringatan Keamanan

LD50 information
Oral LD50 of bisoprolol in the mouse was 730 mg/kg.L7234

Overdose information

Signs of a ?-blocker overdose include cardiovascular symptoms such as hypotension, congestive heart failure, and bradycardia. Other symptoms such as bronchospasm, and hypoglycemia may occur. If an overdose occurs with bisoprolol, supportive treatment should be initiated. Glucagon has been shown to be beneficial in bradycardia and hypotension associated with beta-blocker overdosage.A180550 Hypoglycemia may be managed by administering IV glucose.L7219 Monitor the patient and administer atropine in cases of bradycardia, pressors and fluids in the case of hypotension, and conventional heart failure therapy if heart failure occurs. If heart block occurs, the patient must be closely monitored and isoproterenol infusion or transvenous cardiac pacemaker insertion should take place.L7219 For the management of overdose-related bronchospasm, administer bronchodilators with or without IV aminophylline. Limited research suggests that bisoprolol fumarate is not removed adequately by hemodialysis sessions.A180553,L7219

Bisoprolol

DB00612

small molecule approved

Deskripsi

Bisoprolol is a cardioselective ?1-adrenergic blocking agent used to treat high blood pressure.A180472,L7219 It is considered a potent drug with a long-half life that can be used once daily to reduce the need for multiple doses of antihypertensive drugs.A180472 Bisoprolol is generally well tolerated, likely due to its ?1-adrenergic receptor selectivity and is a useful alternative to non-selective ?-blocker drugs in the treatment of hypertension such as Carvedilol and Labetalol. It may be used alone or in combination with other drugs to manage hypertensionL7219 and can be useful in patients with chronic obstructive pulmonary disease (COPD) due to its receptor selectivity.A180562

Struktur Molekul 2D

Berat 325.443
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) A pharmacokinetic study in 12 healthy individuals determined the mean plasma half-life of bisoprolol to be 10-12 hours.[A180472] Another study comprised of healthy patients determined the elimination half-life to be approximately 10 hours.[A180475] Renal impairment increased the half-life to 18.5 hours.[A180475]
Volume Distribusi The volume of distribution of bisoprolol is 3.5 L/kg.[L7222] The mean volume of distribution was found to be 230 L/kg in heart failure patients, which was similar to the volume of distribution in healthy patients.[A180532] Bisoprolol is known to cross the placenta.[T643]
Klirens (Clearance) Total body clearance in healthy patients was determined to be 14.2 L/h. In patients with renal impairment, clearance was reduced to 7.8 L/h. Hepatic dysfunction also reduced the clearance of bisoprolol.[A180475]

Absorpsi

Bisoprolol is well absorbed in the gastrointestinal tract.L7222 The bioavailability of bisoprolol is about 90% due to the minimal first-pass effects.A180460 Absorption is unaffected by food intake.A180460 Peak plasma concentrations of bisoprolol are attained within 2-4 hours and steady-state concentrations are achieved within 5 days of administration.L7219 In a pharmacokinetic study, the mean peak concentration of bisoprolol was 52 micrograms/L.A180475 Cmax at steady state concentrations of bisoprolol is 64±21 ng/ml administered at 10 mg daily.L7222 The area under the curve (AUC) following oral administration of 10mg bisoprolol ranged from 597 to 661 ug/L x h. Following intravenous administration of the same dosage, the AUC was 672 ug/L x h.A180460

Metabolisme

Approximately 50% of the bisoprolol dose is eliminated by non-renal pathways. Bisoprolol is metabolized through oxidative metabolic pathways with no subsequent conjugation. Bisoprolol metabolites are polar and, therefore, really eliminated. Major metabolites found in plasma and urine are inactive. Bisoprolol is mainly metabolized by CYP3A4 (95%), whereas CYP2D6 plays a minor role. The CYP3A4-mediated metabolism of bisoprolol appears to be non-stereoselective.A259537,L7219,L46427

Rute Eliminasi

Bisoprolol is eliminated equally by both renal and hepatic pathways. About 50% of an oral dose is excreted unchanged in the urine with the remainder of the dose excreted as inactive bisoprolol metabolites. Under 2% of the ingested dose is found to be excreted in the feces.L7219,L7222

Interaksi Makanan

1 Data
  • 1. Take with or without food. The absorption is unaffected by food.

Interaksi Obat

1745 Data
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Bisoprolol is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Bisoprolol is combined with Levodopa.
Risperidone Bisoprolol may increase the hypotensive activities of Risperidone.
Ranolazine The serum concentration of Bisoprolol can be increased when it is combined with Ranolazine.
Ceritinib Bisoprolol may increase the bradycardic activities of Ceritinib.
Ivabradine Bisoprolol may increase the bradycardic activities of Ivabradine.
Ruxolitinib Ruxolitinib may increase the bradycardic activities of Bisoprolol.
Alfuzosin Alfuzosin may increase the hypotensive activities of Bisoprolol.
Amifostine Bisoprolol may increase the hypotensive activities of Amifostine.
Diazoxide Diazoxide may increase the hypotensive activities of Bisoprolol.
Methylphenidate Methylphenidate may decrease the antihypertensive activities of Bisoprolol.
Dexmethylphenidate Dexmethylphenidate may decrease the antihypertensive activities of Bisoprolol.
Obinutuzumab Bisoprolol may increase the hypotensive activities of Obinutuzumab.
Pentoxifylline Pentoxifylline may increase the hypotensive activities of Bisoprolol.
Rituximab Bisoprolol may increase the hypotensive activities of Rituximab.
Zolmitriptan Zolmitriptan may decrease the antihypertensive activities of Bisoprolol.
Doxapram Doxapram may decrease the antihypertensive activities of Bisoprolol.
Phenmetrazine Phenmetrazine may decrease the antihypertensive activities of Bisoprolol.
Naratriptan Naratriptan may decrease the antihypertensive activities of Bisoprolol.
Frovatriptan Frovatriptan may decrease the antihypertensive activities of Bisoprolol.
Epicaptopril Epicaptopril may decrease the antihypertensive activities of Bisoprolol.
1-benzylimidazole 1-benzylimidazole may decrease the antihypertensive activities of Bisoprolol.
Amineptine Amineptine may decrease the antihypertensive activities of Bisoprolol.
Naluzotan Naluzotan may decrease the antihypertensive activities of Bisoprolol.
Esmirtazapine Esmirtazapine may decrease the antihypertensive activities of Bisoprolol.
Nitrous oxide Nitrous oxide may decrease the antihypertensive activities of Bisoprolol.
Cinitapride Cinitapride may decrease the antihypertensive activities of Bisoprolol.
Tyramine Tyramine may decrease the antihypertensive activities of Bisoprolol.
Ifenprodil Ifenprodil may decrease the antihypertensive activities of Bisoprolol.
Butriptyline Butriptyline may decrease the antihypertensive activities of Bisoprolol.
Dosulepin Dosulepin may decrease the antihypertensive activities of Bisoprolol.
Oxaprotiline Oxaprotiline may decrease the antihypertensive activities of Bisoprolol.
Atipamezole Atipamezole may decrease the antihypertensive activities of Bisoprolol.
Tetrahydrocannabivarin Tetrahydrocannabivarin may decrease the antihypertensive activities of Bisoprolol.
Piclozotan Piclozotan may decrease the antihypertensive activities of Bisoprolol.
Idazoxan Idazoxan may decrease the antihypertensive activities of Bisoprolol.
Opipramol Opipramol may decrease the antihypertensive activities of Bisoprolol.
Tramazoline Tramazoline may decrease the antihypertensive activities of Bisoprolol.
Amitriptylinoxide Amitriptylinoxide may decrease the antihypertensive activities of Bisoprolol.
Dibenzepin Dibenzepin may decrease the antihypertensive activities of Bisoprolol.
Quinupramine Quinupramine may decrease the antihypertensive activities of Bisoprolol.
Trichloroethylene Trichloroethylene may decrease the antihypertensive activities of Bisoprolol.
Fenozolone Fenozolone may decrease the antihypertensive activities of Bisoprolol.
Melitracen Melitracen may decrease the antihypertensive activities of Bisoprolol.
Lofepramine Lofepramine may decrease the antihypertensive activities of Bisoprolol.
Xenon Xenon may decrease the antihypertensive activities of Bisoprolol.
Iprindole Iprindole may decrease the antihypertensive activities of Bisoprolol.
Buflomedil Buflomedil may decrease the antihypertensive activities of Bisoprolol.
Imipramine oxide Imipramine oxide may decrease the antihypertensive activities of Bisoprolol.
Mefenorex Mefenorex may decrease the antihypertensive activities of Bisoprolol.
5-methoxy-N,N-dimethyltryptamine 5-methoxy-N,N-dimethyltryptamine may decrease the antihypertensive activities of Bisoprolol.
Quinoline Yellow WS Quinoline Yellow WS may decrease the antihypertensive activities of Bisoprolol.
Isoflurane Isoflurane may decrease the antihypertensive activities of Bisoprolol.
Remifentanil Remifentanil may decrease the antihypertensive activities of Bisoprolol.
Desflurane Desflurane may decrease the antihypertensive activities of Bisoprolol.
Dutasteride Dutasteride may decrease the antihypertensive activities of Bisoprolol.
Mirtazapine Mirtazapine may decrease the antihypertensive activities of Bisoprolol.
Sufentanil Sufentanil may decrease the antihypertensive activities of Bisoprolol.
Methoxyflurane Methoxyflurane may decrease the antihypertensive activities of Bisoprolol.
Halothane Halothane may decrease the antihypertensive activities of Bisoprolol.
Finasteride Finasteride may decrease the antihypertensive activities of Bisoprolol.
Sevoflurane Sevoflurane may decrease the antihypertensive activities of Bisoprolol.
Solifenacin Solifenacin may decrease the antihypertensive activities of Bisoprolol.
Rotigotine Rotigotine may decrease the antihypertensive activities of Bisoprolol.
Cariprazine Cariprazine may decrease the antihypertensive activities of Bisoprolol.
Mianserin Mianserin may decrease the antihypertensive activities of Bisoprolol.
Vilazodone Vilazodone may decrease the antihypertensive activities of Bisoprolol.
Lurasidone Lurasidone may decrease the antihypertensive activities of Bisoprolol.
Cannabidiol Cannabidiol may decrease the antihypertensive activities of Bisoprolol.
Tianeptine Tianeptine may decrease the antihypertensive activities of Bisoprolol.
Siponimod Siponimod may decrease the antihypertensive activities of Bisoprolol.
Eletriptan Eletriptan may decrease the antihypertensive activities of Bisoprolol.
Protriptyline Protriptyline may decrease the antihypertensive activities of Bisoprolol.
Alfentanil Alfentanil may decrease the antihypertensive activities of Bisoprolol.
Propofol Propofol may decrease the antihypertensive activities of Bisoprolol.
Yohimbine Yohimbine may decrease the antihypertensive activities of Bisoprolol.
Diethyl ether Diethyl ether may decrease the antihypertensive activities of Bisoprolol.
Fentanyl Fentanyl may decrease the antihypertensive activities of Bisoprolol.
Desipramine Desipramine may decrease the antihypertensive activities of Bisoprolol.
Clomipramine Clomipramine may decrease the antihypertensive activities of Bisoprolol.
Dimetacrine Dimetacrine may decrease the antihypertensive activities of Bisoprolol.
Selpercatinib Selpercatinib may decrease the antihypertensive activities of Bisoprolol.
Naxitamab Naxitamab may decrease the antihypertensive activities of Bisoprolol.
Amiodarone The therapeutic efficacy of Bisoprolol can be increased when used in combination with Amiodarone.
Bupivacaine The serum concentration of Bupivacaine can be increased when it is combined with Bisoprolol.
Dipyridamole Dipyridamole may increase the bradycardic activities of Bisoprolol.
Dronedarone Dronedarone may increase the bradycardic activities of Bisoprolol.
Fingolimod Bisoprolol may increase the bradycardic activities of Fingolimod.
Floctafenine The risk or severity of adverse effects can be increased when Bisoprolol is combined with Floctafenine.
Mepivacaine The serum concentration of Mepivacaine can be increased when it is combined with Bisoprolol.
Methacholine Bisoprolol may increase the bronchoconstrictory activities of Methacholine.
Midodrine The therapeutic efficacy of Midodrine can be decreased when used in combination with Bisoprolol.
Nifedipine The risk or severity of congestive heart failure and hypotension can be increased when Nifedipine is combined with Bisoprolol.
Regorafenib Regorafenib may increase the bradycardic activities of Bisoprolol.
Rivastigmine Bisoprolol may increase the bradycardic activities of Rivastigmine.
Molsidomine Molsidomine may increase the hypotensive activities of Bisoprolol.
Insulin argine Bisoprolol may increase the hypoglycemic activities of Insulin argine.
Dorzolamide Bisoprolol may increase the hypotensive activities of Dorzolamide.
Bimatoprost Bisoprolol may increase the hypotensive activities of Bimatoprost.
Unoprostone Bisoprolol may increase the hypotensive activities of Unoprostone.

Target Protein

Beta-1 adrenergic receptor ADRB1
Beta-2 adrenergic receptor ADRB2

Referensi & Sumber

Synthesis reference: Yoshihiro Iwao, Katsuyuki Ookubo, Katsuhiro Okada, Kunihiro Minami, Shuichiro Yuasa, "Adhesive Pharmaceutical Preparation Containing Bisoprolol." U.S. Patent US20090169604, issued July 02, 2009.
Artikel (PubMed)
  • PMID: 2903820
    Lancaster SG, Sorkin EM: Bisoprolol. A preliminary review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in hypertension and angina pectoris. Drugs. 1988 Sep;36(3):256-85. doi: 10.2165/00003495-198836030-00002.
  • PMID: 18612186
    Ishiguro H, Ikeda T, Abe A, Tsukada T, Mera H, Nakamura K, Yusu S, Yoshino H: Antiarrhythmic effect of bisoprolol, a highly selective beta1-blocker, in patients with paroxysmal atrial fibrillation. Int Heart J. 2008 May;49(3):281-93.
  • PMID: 18472978
    Metra M, Nodari S, Bordonali T, Milani P, Lombardi C, Bugatti S, Fontanella B, Verzura G, Danesi R, Dei Cas L: Bisoprolol in the treatment of chronic heart failure: from pathophysiology to clinical pharmacology and trial results. Ther Clin Risk Manag. 2007 Aug;3(4):569-78.
  • PMID: 2876722
    Leopold G, Ungethum W, Pabst J, Simane Z, Buhring KU, Wiemann H: Pharmacodynamic profile of bisoprolol, a new beta 1-selective adrenoceptor antagonist. Br J Clin Pharmacol. 1986 Sep;22(3):293-300. doi: 10.1111/j.1365-2125.1986.tb02890.x.
  • PMID: 12795776
    Nuttall SL, Routledge HC, Kendall MJ: A comparison of the beta1-selectivity of three beta1-selective beta-blockers. J Clin Pharm Ther. 2003 Jun;28(3):179-86.
  • PMID: 2887325
    Kirch W, Rose I, Demers HG, Leopold G, Pabst J, Ohnhaus EE: Pharmacokinetics of bisoprolol during repeated oral administration to healthy volunteers and patients with kidney or liver disease. Clin Pharmacokinet. 1987 Aug;13(2):110-7. doi: 10.2165/00003088-198713020-00003.
  • PMID: 2439803
    Chatterjee SS: The cardioselective and hypotensive effects of bisoprolol in hypertensive asthmatics. J Cardiovasc Pharmacol. 1986;8 Suppl 11:S74-7.
  • PMID: 28357786
    Dezsi CA, Szentes V: The Real Role of beta-Blockers in Daily Cardiovascular Therapy. Am J Cardiovasc Drugs. 2017 Oct;17(5):361-373. doi: 10.1007/s40256-017-0221-8.
Menampilkan 8 dari 14 artikel.
Textbook
  • William D. Tucker; Pramod Theetha Kariyanna (2019). Selective B1 blockers. Stat Pearls Publishing.
  • National Collaborating Centre for Women's and Children's Health (UK) (2010). NICE Guidelines for hypertension in pregnancy. RCOG Press.

Contoh Produk & Brand

Produk: 195 • International brands: 11
Produk
  • Ag-bisoprolol
    Tablet • 5 mg • Oral • Canada • Generic • Approved
  • Ag-bisoprolol
    Tablet • 10 mg • Oral • Canada • Generic • Approved
  • Apo-bisoprolol
    Tablet • 5 mg • Oral • Canada • Generic • Approved
  • Apo-bisoprolol
    Tablet • 10 mg • Oral • Canada • Generic • Approved
  • Ava-bisoprolol
    Tablet • 5 mg • Oral • Canada • Generic • Approved
  • Ava-bisoprolol
    Tablet • 10 mg • Oral • Canada • Generic • Approved
  • Bisoprolol
    Tablet, film coated • 5 mg/1 • Oral • US • Generic • Approved
  • Bisoprolol
    Tablet, film coated • 10 mg/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 195 produk.
International Brands
  • Bisocor
  • Cardicor — Bayer
  • Concor — Merck
  • Concore — Merck
  • Detensiel — Merck Santé
  • Emconcor — Merck
  • Emcor — Merck
  • Euradal — Lacer
  • Isoten — Meda
  • Monocor — Biovail Pharmaceuticals

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
© 2025 Digital Pharmacy Research - Universitas Esa Unggul