bumetanide indications/contra

Stem definitionDrug idCAS RN
diuretics, piretanide derivatives 427 28395-03-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • bumetanide
  • bumethanide
  • bufenox
A sulfamyl diuretic.
  • Molecular weight: 364.42
  • Formula: C17H20N2O5S
  • CLOGP: 3.37
  • LIPINSKI: 0
  • HAC: 7
  • HDO: 3
  • TPSA: 118.72
  • ALOGS: -4.15
  • ROTB: 8

Drug dosage:

DoseUnitRoute
1 mg O
1 mg P
1 mg O

Approvals:

DateAgencyCompanyOrphan
Feb. 28, 1983 FDA

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
Acute kidney injury 651.48 45.87 158 356 49525 3335820
Dehydration 141.31 45.87 45 469 33604 3351741
Hypotension 124.26 45.87 45 469 49469 3335876
Hyperkalaemia 104.53 45.87 28 486 11266 3374079
Renal impairment 86.98 45.87 27 487 18234 3367111
Blood ketone body increased 78.65 45.87 11 503 131 3385214
Blood creatinine increased 78.21 45.87 26 488 21792 3363553
Bradycardia 72.44 45.87 23 491 16646 3368699
Circumstance or information capable of leading to medication error 71.30 45.87 15 499 2127 3383218
Hypokalaemia 59.72 45.87 19 495 13786 3371559
Medication error 58.27 45.87 18 496 11853 3373492
Dyspnoea 55.07 45.87 32 482 102902 3282443
Hypoglycaemia 50.93 45.87 17 497 14301 3371044
International normalised ratio increased 50.59 45.87 17 497 14598 3370747
Diarrhoea 49.40 45.87 30 484 104318 3281027
Syncope 48.22 45.87 19 495 25614 3359731
Fluid overload 47.65 45.87 12 502 3739 3381606

Pharmacologic Action:

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SourceCodeDescription
ATC C03CA02 CARDIOVASCULAR SYSTEM
DIURETICS
HIGH-CEILING DIURETICS
Sulfonamides, plain
ATC C03CB02 CARDIOVASCULAR SYSTEM
DIURETICS
HIGH-CEILING DIURETICS
Sulfonamides and potassium in combination
ATC C03EB02 CARDIOVASCULAR SYSTEM
DIURETICS
DIURETICS AND POTASSIUM-SPARING AGENTS IN COMBINATION
High-ceiling diuretics and potassium-sparing agents
FDA PE N0000175366 Increased Diuresis at Loop of Henle
FDA EPC N0000175590 Loop Diuretic
MeSH PA D004232 Diuretics
MeSH PA D049990 Membrane Transport Modulators
MeSH PA D045283 Natriuretic Agents
MeSH PA D049994 Sodium Potassium Chloride Symporter Inhibitors
CHEBI has role CHEBI:35498 diuretic

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
Edema indication 267038008
Pulmonary Edema due to Chronic Heart Failure indication
Peripheral Edema due to Chronic Heart Failure indication
Edema due to Hepatic Cirrhosis indication
Renal Disease with Edema indication
Anuria contraindication 2472002 DOID:2983
Hypocalcemia contraindication 5291005
Hypovolemia contraindication 28560003
Hyperuricemia contraindication 35885006 DOID:1920
Hypokalemia contraindication 43339004
Hepatic coma contraindication 72836002 DOID:12550
Diabetes mellitus contraindication 73211009 DOID:9351
Oliguria contraindication 83128009
Hearing disorder contraindication 128540005
Hypomagnesemia contraindication 190855004
Disease of liver contraindication 235856003 DOID:409
Thrombocytopenic disorder contraindication 302215000 DOID:1588
Hypertensive disorder off-label use 38341003 DOID:10763
Hypercalcemia off-label use 66931009 DOID:12678
Decompensated cardiac failure off-label use 195111005

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation levelDissociation constantType (acidic/basic)
pKa1 4.36 acidic
pKa2 9.88 acidic
pKa3 0.86 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
Solute carrier family 12 member 1 Transporter INHIBITOR Ki 7.60 WOMBAT-PK CHEMBL
Sodium/potassium-transporting ATPase subunit alpha-1 Transporter Kd 7.52 WOMBAT-PK
Solute carrier family 12 member 2 Transporter INHIBITOR IC50 5.60 IUPHAR
G-protein coupled receptor 35 GPCR AGONIST EC50 5.27 IUPHAR

External reference:

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IDSource
4837 IUPHAR_LIGAND_ID
4017794 VUID
N0000146155 NUI
C0006376 UMLSCUI
D00247 KEGG_DRUG
0Y2S3XUQ5H UNII
2943 INN_ID
DB00887 DRUGBANK_ID
4017794 VANDF
N0000146155 NDFRT
N0000007386 NDFRT
002312 NDDF
3606 MMSL
1808 RXNORM
387498005 SNOMEDCT_US
86647004 SNOMEDCT_US
4304 MMSL
d00179 MMSL
CHEMBL1072 ChEMBL_ID
2471 PUBCHEM_CID
D002034 MESH_DESCRIPTOR_UI
CHEBI:3213 CHEBI

Pharmaceutical products:

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ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
Bumetanide HUMAN PRESCRIPTION DRUG LABEL 1 0093-4232 TABLET 0.50 mg ORAL ANDA 12 sections
Bumetanide HUMAN PRESCRIPTION DRUG LABEL 1 0093-4233 TABLET 1 mg ORAL ANDA 12 sections
Bumetanide HUMAN PRESCRIPTION DRUG LABEL 1 0093-4234 TABLET 2 mg ORAL ANDA 12 sections
Bumetanide HUMAN PRESCRIPTION DRUG LABEL 1 0185-0128 TABLET 0.50 mg ORAL ANDA 12 sections
Bumetanide HUMAN PRESCRIPTION DRUG LABEL 1 0185-0129 TABLET 1 mg ORAL ANDA 12 sections
Bumetanide HUMAN PRESCRIPTION DRUG LABEL 1 0185-0130 TABLET 2 mg ORAL ANDA 12 sections
Bumetanide HUMAN PRESCRIPTION DRUG LABEL 1 0409-1412 INJECTION, SOLUTION 0.25 mg INTRAMUSCULAR ANDA 13 sections
Bumetanide HUMAN PRESCRIPTION DRUG LABEL 1 0615-4536 TABLET 1 mg ORAL ANDA 12 sections
Bumetanide HUMAN PRESCRIPTION DRUG LABEL 1 0615-5534 TABLET 2 mg ORAL ANDA 12 sections
Bumetanide HUMAN PRESCRIPTION DRUG LABEL 1 0641-6007 INJECTION 0.25 mg INTRAMUSCULAR ANDA 12 sections
Bumetanide HUMAN PRESCRIPTION DRUG LABEL 1 0641-6008 INJECTION 0.25 mg INTRAMUSCULAR ANDA 12 sections
Bumetanide HUMAN PRESCRIPTION DRUG LABEL 1 0641-6161 INJECTION 0.25 mg INTRAMUSCULAR ANDA 12 sections
Bumetanide HUMAN PRESCRIPTION DRUG LABEL 1 0641-6162 INJECTION 0.25 mg INTRAMUSCULAR ANDA 12 sections
Bumetanide HUMAN PRESCRIPTION DRUG LABEL 1 0832-0540 TABLET 0.50 mg ORAL ANDA 13 sections
Bumetanide HUMAN PRESCRIPTION DRUG LABEL 1 0832-0541 TABLET 1 mg ORAL ANDA 13 sections
Bumetanide HUMAN PRESCRIPTION DRUG LABEL 1 0832-0542 TABLET 2 mg ORAL ANDA 13 sections
Bumetanide HUMAN PRESCRIPTION DRUG LABEL 1 33261-983 TABLET 1 mg ORAL ANDA 12 sections
Bumetanide HUMAN PRESCRIPTION DRUG LABEL 1 35356-902 TABLET 2 mg ORAL ANDA 12 sections
Bumetanide HUMAN PRESCRIPTION DRUG LABEL 1 35356-912 TABLET 1 mg ORAL ANDA 12 sections
Bumetanide HUMAN PRESCRIPTION DRUG LABEL 1 35356-988 TABLET 0.50 mg ORAL ANDA 12 sections
Bumetanide HUMAN PRESCRIPTION DRUG LABEL 1 42291-178 TABLET 0.50 mg ORAL ANDA 12 sections
Bumetanide HUMAN PRESCRIPTION DRUG LABEL 1 42291-179 TABLET 1 mg ORAL ANDA 12 sections
Bumetanide HUMAN PRESCRIPTION DRUG LABEL 1 42291-180 TABLET 2 mg ORAL ANDA 12 sections
Bumetanide HUMAN PRESCRIPTION DRUG LABEL 1 42799-119 TABLET 0.50 mg ORAL NDA AUTHORIZED GENERIC 13 sections
Bumetanide HUMAN PRESCRIPTION DRUG LABEL 1 42799-120 TABLET 1 mg ORAL NDA AUTHORIZED GENERIC 13 sections
Bumetanide HUMAN PRESCRIPTION DRUG LABEL 1 42799-121 TABLET 2 mg ORAL NDA AUTHORIZED GENERIC 13 sections
Bumetanide HUMAN PRESCRIPTION DRUG LABEL 1 43353-288 TABLET 1 mg ORAL ANDA 12 sections
Bumetanide HUMAN PRESCRIPTION DRUG LABEL 1 43353-292 TABLET 2 mg ORAL ANDA 12 sections
Bumetanide HUMAN PRESCRIPTION DRUG LABEL 1 50436-4233 TABLET 1 mg ORAL ANDA 12 sections
Bumetanide HUMAN PRESCRIPTION DRUG LABEL 1 50436-4234 TABLET 2 mg ORAL ANDA 12 sections