Bisoprolol
- Atc Codes:C07AB07
- CAS Codes:104344-23-2
- PHARMGKB ID:104344-23-2
Table of contents
- Brand Names
- Drug Combinations
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Unlabeled Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Substrate of
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Concor; Belgium: Bisoprolol, Bisosandoz, Docbisopro, Emconcor, Isoten; Bulgaria: Bisogamma, Bisohexal, Bisostad, Concor, Coronal; Czech Republic: Bisobela, Bisocard, Bisogamma, Bisoprolol, Bisprotin, Bivaxol, Byol, Concor, Rivocor; Denmark: Bisocor, Bisoprolol, Cardicor, Emconcor; Estonia: Bisprotin; Finland: Bisoprolol, Bisostad, Bisprotin, Emconcor, Orloc; France: Bisoce, Bisoprolol, Cardensiel, Cardiocor, Detensiel; Germany: Biselect, Biso, Bisobeta, Bisogamma, Bisohexal, BisoLich, Bisoprolol, Concor, Jutabis; Greece: Abitrol, Bisoprolol, Pactens, Speridol; Hungary: Bisoblock, Bisocard, Bisogamma, Bisoprolol, Bisotens, Bisprotin, Concor, Corviogal; Ireland: Bellimcor, Bisocor, Bisop, Bisopine, Bisoprolol, Cardicor, Emcolol, Emcor, Soprol; Italy: Bisoprololo, Cardicor, Concor, Congescor, Pluscor, Sequacor; Luxembourg: Concor; Lithuania: Bisprotin; Netherlands: Bioglan Bisoprololfumaraat, Bisoblock, Bisoprolol, Emcor; Poland: Bisocard, Bisohexal, Bisoprolol, Bisopromerck, Bisoratio, Concor; Portugal: Bisoprolol, Concor; Romania: Bisoblock, Bisogamma, Bisomerck, Bisoprolol, Bisostad, Bisotens, Byol, Concor, Coronal; Slovakia: Bisobela, Bisocard, Bisogamma, Bisomerck, Bisoprolol, Bisprotin, Bivaxol, Concor, Coronal, Rivocor; Spain: Bisoprolol, Emconcor, Euradal, Godal, Libracor, Vasico; Sweden: Bisoprolol, Bisprotin, Cardicor, Emconcor, Libracor, Speridol; UK: Cardicor, Emcor.
North America
Canada: Bisoprolol, Monocor, Zebeta; USA: Zebeta.
Latin America
Argentina: Concor, Corbis, Lostaprolol; Brazil: Concor; Mexico: Concor.
Asia
Japan: Azopsin, Bisoprolol, Bisotate, Luke, Mainheart, Mainries, Mainrol, Maintate, Maintowa, Meitat, Metolomain, Pramatate, Seafuri, Well-bi.
Drug combinations
Bisoprolol and Hydrochlorothiazide
Chemistry
Bisoprolol Fumarate: (C~18~H~31~NO~4~)~2~ C~4~H~4~O~4~. Mw: 766.96. (1) 2-Propanol, 1-[4-[[2-(1-methylethoxy)ethoxy]methyl]phenoxy]-3-[(1-methylethyl)amino]-, (±)-, (E)-2-butenedioate (2:1); (2)(±)-1-[[α-(2-Isopropoxyethoxy)-p-tolyl]oxy]-3-(isopropylamino)-2-propanol fumarate (2:1). CAS-104344-23-2 (1987).
Pharmacologic Category
β-Adrenergic Blocking Agents; β~1~-Selective β-Blocker. (ATC-Code: C07AB07).
Mechanism of action
Selective inhibitor of β~1~-adrenergic receptors (competitively blocks β~1~-receptors in myocardium), with little or no effect on β~2~-receptors at doses ≤20 mg (at high doses may block β~2~-adrenergic receptors within the bronchial and vascular smooth muscle). Decreases resting and exercise-stimulated heart rate and cardiac output, decreases isoproterenol-induced tachycardia, prolongs sinus node recovery time, refractory period of the AV node, and AV nodal conduction (with rapid atrial stimulation). No intrinsic sympathomimetic activity or membrane-stabilizing effect on the heart. Reduces blood pressure by decreasing cardiac output, decreasing sympathetic outflow from the CNS, and/or suppressing renin release.
Therapeutic use
Treatment of hypertension, alone or in combination with other agents. Management of mild to moderately severe heart failure of ischemic or cardiomyopathic origin in conjunction with other agents (do not use in patients with acutely decompensated heart failure requiring I.V. inotropic therapy, those with substantial fluid retention requiring intensive diuresis, and those who require hospitalization for heart failure).
Pregnancy and lactiation implications
No data available on whether bisoprolol crosses the placenta. Available evidence suggests β-blockers are generally safe during pregnancy (although neonatal persistent bradycardia, hypotension, and intrauterine growth retardation were described). Enters breast milk (neonatal hypoglycemia reported following use at parturition or during breast-feeding).
Unlabeled use
Chronic stable angina, supraventricular arrhythmias, premature ventricular contractions, heart failure.
Contraindications
Cardiogenic shock, overt cardiac failure, marked sinus bradycardia, heart block greater than first-degree (except in patients with a functioning artificial pacemaker).
Warnings and precautions
Possible increased reactivity to repeated, accidental, diagnostic, or therapeutic challenges with a variety of allergens while taking β-blockers. In general, patients with bronchospastic disease should not receive β-blockers. Avoid use in overt congestive heart failure (may precipitate heart failure). Caution in compensated heart failure (patients should be stabilized on heart failure prior to initiation of β-blocker). Consider pre-existing sick sinus syndrome before initiating. Caution in diabetes mellitus (may potentiate hypoglycemia and/or mask signs and symptoms). Caution in hepatic and renal impairment. Caution in myasthenia gravis. Can precipitate or aggravate symptoms of arterial insufficiency in peripheral vascular disease and Raynaud’s disease. In pheochromocytoma adequate α-blockade is required prior to use of any β-blocker. Caution in history of psychiatric illness (may cause or exacerbate CNS depression). May mask signs of hyperthyroidism (e.g. tachycardia). Abrupt discontinuation of β-blockade may exacerbate symptoms of hyperthyroidism and may also induce thyroid storm. Caution in patients receiving anesthetic agents which decrease myocardial function (e.g. ether, cyclopropane, and trichloroethylene). Caution in patients on concurrent calcium channel blockers (verapamil or diltiazem)(risk of bradycardia or heart block). Local anesthetic with vasoconstrictor can be safely used in patients medicated with bisoprolol. Nonsteroidal anti-inflammatory drugs (ibuprofen and indomethacin) can reduce the hypotensive effect of β-blockers after 3 or more weeks of therapy. Dose-related fatigue is common. Barbiturates may decrease the effects of β-blockers. β-Blocker therapy should not be withdrawn abruptly (risk of acute tachycardia, hypertension, and/or ischemia).