About: Bisoprolol     Goto   Sponge   NotDistinct   Permalink

An Entity of Type : http://linked.opendata.cz/ontology/drugbank/Drug, within Data Space : linked.opendata.cz associated with source document(s)

AttributesValues
rdf:type
http://linked.open...gbank/description
  • Bisoprolol is a cardioselective &beta;1-adrenergic blocking agent used for secondary prevention of myocardial infarction (MI), heart failure, angina pectoris and mild to moderate hypertension. Bisoprolol is structurally similar to metoprolol, acebutolol and atenolol in that it has two substituents in the <i>para</i> position of the benzene ring. The &beta;1-selectivity of these agents is thought to be due in part to the large substituents in the <i>para</i> position. At lower doses (less than 20 mg daily), bisoprolol selectively blocks cardiac &beta;1-adrenergic receptors with little activity against &beta;2-adrenergic receptors of the lungs and vascular smooth muscle. Receptor selectivity decreases with daily doses of 20 mg or greater. Unlike propranolol and pindolol, bisoprolol does not exhibit membrane-stabilizing or sympathomimetic activity. Bisoprolol possesses a single chiral centre and is administered as a racemic mixture. Only <i>l</i>-bisoprolol exhibits significant &beta;-blocking activity. (en)
http://linked.open...y/drugbank/dosage
http://linked.open...gy/drugbank/group
  • approved (en)
http://linked.open...drugbank/halfLife
  • 9-12 hours; prolonged in the elderly and those with decreased renal function (en)
http://linked.open...ugbank/indication
  • For management of heart failure, angina pectoris, and mild to moderate hypertension and for secondary prevention of myocardial infarction (MI). (en)
http://linked.open...bank/manufacturer
sameAs
Title
  • Bisoprolol (en)
adms:identifier
http://linked.open...mechanismOfAction
  • Bisoprolol selectively blocks catecholamine stimulation of &beta;1-adrenergic receptors in the heart and vascular smooth muscle. This results in a reduction of heart rate, cardiac output, systolic and diastolic blood pressure, and possibly reflex orthostatic hypotension. At higher doses (e.g. 20 mg and greater) bisoprolol may competitively block &beta;2-adrenergic receptors in bronchial and vascular smooth muscle causing bronchospasm and vasodilation. (en)
http://linked.open...drugbank/packager
http://linked.open...outeOfElimination
  • Eliminated equally by renal and non-renal pathways. Approximately 50% of the total orally administered dose is excreted unchanged in urine with the remainder appearing as inactive metabolites. Less than 2% of the dose is excreted in the feces. (en)
http://linked.open.../drugbank/synonym
  • Bisoprolol (en)
  • Bisoprololum (en)
  • (RS)-1-(4-(2-isopropoxyethoxymethyl)phenoxy)-3-(isopropylamino)-2-propanol (en)
  • (+-)-1-((alpha-(2-Isopropoxyethoxy)-P-tolyl)oxy)-3-(isopropylamino)-2-propanol (en)
http://linked.open...drugbank/toxicity
  • Oral, mouse: LD<sub>50</sub> = 100 mg/kg; Skin, rabbit: LD<sub>50</sub> = 200 mg/kg;&nbsp;Skin, rat: LD<sub>50</sub> = 500 mg/kg. Symptoms of overdose include congestive heart failure (marked by sudden weight gain, swelling of the legs, feet, and ankles, fatigue, and shortness of breath), difficult or labored breathing, low blood pressure, low blood sugar, and slow heartbeat. (en)
http://linked.open.../drug/hasAHFSCode
http://linked.open...k/foodInteraction
  • Take without regard to meals. (en)
http://linked.open.../drugbank/mixture
http://linked.open...nk/proteinBinding
  • Binding to serum proteins is approximately 30% (en)
http://linked.open...ogy/drugbank/salt
  • (en)
http://linked.open...ynthesisReference
  • Yoshihiro Iwao, Katsuyuki Ookubo, Katsuhiro Okada, Kunihiro Minami, Shuichiro Yuasa, "Adhesive Pharmaceutical Preparation Containing Bisoprolol." U.S. Patent US20090169604, issued July 02, 2009. (en)
http://linked.open...y/mesh/hasConcept
foaf:page
http://linked.open...ugbank/IUPAC-Name
http://linked.open...gy/drugbank/InChI
http://linked.open...Molecular-Formula
http://linked.open.../Molecular-Weight
http://linked.open...noisotopic-Weight
http://linked.open...y/drugbank/SMILES
http://linked.open.../Water-Solubility
http://linked.open...ogy/drugbank/logP
http://linked.open...ogy/drugbank/logS
http://linked.open...l/drug/hasATCCode
http://linked.open...nd-Acceptor-Count
http://linked.open...-Bond-Donor-Count
http://linked.open...drugbank/InChIKey
http://linked.open...urface-Area--PSA-
http://linked.open...nk/Polarizability
http://linked.open...bank/Refractivity
http://linked.open...atable-Bond-Count
http://linked.open...ugbank/absorption
  • Well absorbed. Bioavailability > 80%. Absorption is not affected by food. Peak plasma concentrations occur within 2-4 hours. (en)
http://linked.open.../affectedOrganism
  • Humans and other mammals (en)
http://linked.open...casRegistryNumber
  • 66722-44-9 (en)
http://linked.open...drugbank/category
  • (en)
http://linked.open...gbank/containedIn
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