bisoprolol indications/contra

Stem definitionDrug idCAS RN
beta-adrenoreceptor antagonists 380 66722-44-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • bisoprolol hemifumarate
  • bisoprolol
  • bisoprolol fumarate
A cardioselective beta-1 adrenergic blocker. It is effective in the management of HYPERTENSION and ANGINA PECTORIS.
  • Molecular weight: 325.45
  • Formula: C18H31NO4
  • CLOGP: 1.79
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 2
  • TPSA: 59.95
  • ALOGS: -3.66
  • ROTB: 12

Drug dosage:

DoseUnitRoute
10 mg O

Approvals:

DateAgencyCompanyOrphan
July 31, 1992 FDA TEVA WOMENS

FDA Adverse Event Reporting System

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MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Bradycardia 1676.10 37.67 413 3396 16256 3365794
Hypotension 1155.50 37.67 394 3415 49120 3332930
Acute kidney injury 902.83 37.67 329 3480 49354 3332696
Syncope 819.85 37.67 260 3549 25373 3356677
Drug interaction 634.62 37.67 251 3558 46561 3335489
Fall 536.38 37.67 238 3571 58645 3323405
Hyperkalaemia 506.28 37.67 149 3660 11145 3370905
Atrial fibrillation 463.22 37.67 167 3642 23774 3358276
Dizziness 435.52 37.67 224 3585 76288 3305762
Dyspnoea 402.36 37.67 235 3574 102699 3279351
Suicide attempt 392.41 37.67 133 3676 15714 3366336
Intentional overdose 365.98 37.67 125 3684 15100 3366950
Loss of consciousness 321.37 37.67 134 3675 28013 3354037
Circulatory collapse 262.55 37.67 78 3731 5971 3376079
Atrioventricular block complete 260.54 37.67 64 3745 2368 3379682
Malaise 259.11 37.67 151 3658 65026 3317024
Sinus bradycardia 253.96 37.67 67 3742 3312 3378738
Orthostatic hypotension 240.74 37.67 70 3739 4966 3377084
Asthenia 219.02 37.67 136 3673 65529 3316521
Cardiac failure 216.65 37.67 92 3717 20013 3362037
Fatigue 197.24 37.67 154 3655 107086 3274964
Dehydration 191.46 37.67 99 3710 33550 3348500
Toxicity to various agents 181.21 37.67 107 3702 46947 3335103
Vomiting 180.73 37.67 136 3673 89395 3292655
Vertigo 172.49 37.67 67 3742 11565 3370485
Confusional state 166.42 37.67 94 3715 37904 3344146
Agitation 166.33 37.67 76 3733 19630 3362420
Renal failure 159.29 37.67 87 3722 32853 3349197
Hypoglycaemia 159.01 37.67 67 3742 14251 3367799
Presyncope 157.44 37.67 51 3758 5180 3376870

Pharmacologic Action:

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SourceCodeDescription
ATC C07AB07 CARDIOVASCULAR SYSTEM
BETA BLOCKING AGENTS
BETA BLOCKING AGENTS
Beta blocking agents, selective
ATC C07BB07 CARDIOVASCULAR SYSTEM
BETA BLOCKING AGENTS
BETA BLOCKING AGENTS AND THIAZIDES
Beta blocking agents, selective, and thiazides
ATC C07FB07 CARDIOVASCULAR SYSTEM
BETA BLOCKING AGENTS
BETA BLOCKING AGENTS, OTHER COMBINATIONS
Beta blocking agents and calcium channel blockers
ATC C07FX04 CARDIOVASCULAR SYSTEM
BETA BLOCKING AGENTS
BETA BLOCKING AGENTS, OTHER COMBINATIONS
Beta blocking agents, other combinations
ATC C09BX02 CARDIOVASCULAR SYSTEM
AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
ACE INHIBITORS, COMBINATIONS
ACE inhibitors, other combinations
FDA EPC N0000175556 beta-Adrenergic Blocker
MeSH PA D018663 Adrenergic Agents
MeSH PA D018674 Adrenergic Antagonists
MeSH PA D058671 Adrenergic beta-1 Receptor Antagonists
MeSH PA D000319 Adrenergic beta-Antagonists
CHEBI has role CHEBI:35674 antihypertensive agent
CHEBI has role CHEBI:35530 beta-adrenergic antagonist
CHEBI has role CHEBI:38070 anti-arrhythmia drug
CHEBI has role CHEBI:66991 sympatholytic agent
MeSH PA D000959 Antihypertensive Agents
MeSH PA D001337 Autonomic Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018373 Peripheral Nervous System Agents
MeSH PA D013565 Sympatholytics

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
Hypertensive disorder indication 38341003 DOID:10763
Anuria contraindication 2472002 DOID:2983
Psoriasis contraindication 9014002 DOID:8893
Hypercholesterolemia contraindication 13644009
Secondary angle-closure glaucoma contraindication 21571006
Complete atrioventricular block contraindication 27885002
Hypovolemia contraindication 28560003
Dehydration contraindication 34095006
Depressive disorder contraindication 35489007 DOID:2848
Hyperuricemia contraindication 35885006 DOID:1920
Sick sinus syndrome contraindication 36083008 DOID:13884
Anaphylaxis contraindication 39579001
Hypokalemia contraindication 43339004
Sinus bradycardia contraindication 49710005
Systemic lupus erythematosus contraindication 55464009 DOID:9074
Sympathectomy contraindication 57071006
Hypercalcemia contraindication 66931009 DOID:12678
Hyperparathyroidism contraindication 66999008 DOID:13543
Hypochloremic alkalosis contraindication 70134007
Hepatic coma contraindication 72836002 DOID:12550
Diabetes mellitus contraindication 73211009 DOID:9351
Pulmonary emphysema contraindication 87433001
Cardiogenic shock contraindication 89138009
Hyponatremia contraindication 89627008
Gout contraindication 90560007 DOID:13189
Kidney disease contraindication 90708001 DOID:2527
Myasthenia gravis contraindication 91637004 DOID:437
Hypomagnesemia contraindication 190855004
Partial atrioventricular block contraindication 195039008
Decompensated cardiac failure contraindication 195111005
Asthma contraindication 195967001 DOID:2841
Acute pancreatitis contraindication 197456007 DOID:2913
Disease of liver contraindication 235856003 DOID:409
Raynaud's phenomenon contraindication 266261006
Neonatal hyperbilirubinemia contraindication 281610001
Pregnancy, function contraindication 289908002
Pheochromocytoma contraindication 302835009
Severe chronic obstructive pulmonary disease contraindication 313299006
Peripheral arterial occlusive disease contraindication 399957001
Peripheral vascular disease contraindication 400047006
Azotemia contraindication 445009001
Acute exacerbation of asthma contraindication 708038006
Chronic heart failure off-label use 48447003
Atrial fibrillation off-label use 49436004 DOID:0060224
Angina pectoris off-label use 194828000
Diastolic heart failure off-label use 418304008 DOID:9775
Prevention of Post Cardio-Thoracic Surgery Atrial Fibrillation off-label use

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.19 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Beta-1 adrenergic receptor GPCR ANTAGONIST Ki 7.65 WOMBAT-PK CHEMBL
Beta-3 adrenergic receptor GPCR Ki 5.04 WOMBAT-PK
Beta-2 adrenergic receptor GPCR Ki 5.94 WOMBAT-PK

External reference:

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IDSource
4023923 VUID
N0000021928 NUI
C0053799 UMLSCUI
7129 IUPHAR_LIGAND_ID
D00634 KEGG_DRUG
CHEMBL645 ChEMBL_ID
DB00612 DRUGBANK_ID
4023923 VANDF
N0000007329 NDFRT
N0000021928 NDFRT
003703 NDDF
19484 RXNORM
108547003 SNOMEDCT_US
386868003 SNOMEDCT_US
d00709 MMSL
2405 PUBCHEM_CID
CHEMBL1200708 ChEMBL_ID
UR59KN573L UNII
104344-23-2 SECONDARY_CAS_RN
D017298 MESH_DESCRIPTOR_UI
5225 INN_ID
CHEBI:3127 CHEBI

Pharmaceutical products:

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ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
Bisoprolol Fumarate HUMAN PRESCRIPTION DRUG LABEL 1 0093-5270 TABLET, FILM COATED 5 mg ORAL ANDA 12 sections
Bisoprolol Fumarate HUMAN PRESCRIPTION DRUG LABEL 1 0093-5271 TABLET, FILM COATED 10 mg ORAL ANDA 12 sections
Bisoprolol Fumarate and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 0185-0701 TABLET, COATED 2.50 mg ORAL ANDA 13 sections
Bisoprolol Fumarate and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 0185-0704 TABLET, COATED 5 mg ORAL ANDA 13 sections
Bisoprolol Fumarate and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 0185-0707 TABLET, COATED 10 mg ORAL ANDA 13 sections
bisoprolol fumarate HUMAN PRESCRIPTION DRUG LABEL 1 0185-0771 TABLET, COATED 5 mg ORAL ANDA 12 sections
bisoprolol fumarate HUMAN PRESCRIPTION DRUG LABEL 1 0185-0774 TABLET, COATED 10 mg ORAL ANDA 12 sections
Bisoprolol Fumarate and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 0378-0501 TABLET, FILM COATED 2.50 mg ORAL ANDA 13 sections
Bisoprolol Fumarate and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 0378-0503 TABLET, FILM COATED 5 mg ORAL ANDA 13 sections
Bisoprolol Fumarate and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 0378-0505 TABLET, FILM COATED 10 mg ORAL ANDA 13 sections
Bisoprolol Fumarate HUMAN PRESCRIPTION DRUG LABEL 1 0378-0523 TABLET, FILM COATED 5 mg ORAL ANDA 13 sections
Bisoprolol Fumarate HUMAN PRESCRIPTION DRUG LABEL 1 0378-0524 TABLET, FILM COATED 10 mg ORAL ANDA 13 sections
bisoprolol fumarate and hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 10544-173 TABLET 2.50 mg ORAL ANDA 13 sections
bisoprolol fumarate and hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 10544-174 TABLET 10 mg ORAL ANDA 13 sections
bisoprolol fumarate and hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 10544-563 TABLET 5 mg ORAL ANDA 13 sections
Bisoprolol Fumarate HUMAN PRESCRIPTION DRUG LABEL 1 21695-667 TABLET 5 mg ORAL ANDA 13 sections
Bisoprolol Fumarate HUMAN PRESCRIPTION DRUG LABEL 1 21695-670 TABLET 10 mg ORAL ANDA 13 sections
Bisoprolol Fumarate and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 21695-808 TABLET, COATED 5 mg ORAL ANDA 12 sections
Bisoprolol Fumarate and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 21695-809 TABLET, COATED 10 mg ORAL ANDA 12 sections
Bisoprolol Fumarate HUMAN PRESCRIPTION DRUG LABEL 1 29300-127 TABLET 10 mg ORAL ANDA 13 sections
bisoprolol fumarate and hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 29300-189 TABLET 10 mg ORAL ANDA 13 sections
bisoprolol fumarate and hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 33261-918 TABLET 5 mg ORAL ANDA 13 sections
Bisoprolol Fumarate and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 43063-134 TABLET, FILM COATED 10 mg ORAL ANDA 13 sections
bisoprolol fumarate and hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 50090-0789 TABLET 5 mg ORAL ANDA 13 sections
bisoprolol fumarate and hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 50090-0796 TABLET 2.50 mg ORAL ANDA 13 sections
bisoprolol fumarate and hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 50090-0799 TABLET 10 mg ORAL ANDA 13 sections
Ziac HUMAN PRESCRIPTION DRUG LABEL 2 51285-040 TABLET, FILM COATED 10 mg ORAL NDA 14 sections
Ziac HUMAN PRESCRIPTION DRUG LABEL 2 51285-047 TABLET, FILM COATED 2.50 mg ORAL NDA 14 sections
Ziac HUMAN PRESCRIPTION DRUG LABEL 2 51285-050 TABLET, FILM COATED 5 mg ORAL NDA 14 sections
Bisoprolol Fumarate and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 54868-4576 TABLET, COATED 5 mg ORAL ANDA 12 sections