bumetanide 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
diuretics, piretanide derivatives	427	28395-03-1

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: bumetanide bumethanide bufenox	A sulfamyl diuretic. Molecular weight: 364.42 Formula: C17H20N2O5S CLOGP: 3.07 LIPINSKI: 0 HAC: 7 HDO: 3 TPSA: 118.72 ALOGS: -4.15 ROTB: 8 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

bumetanide
bumethanide
bufenox

A sulfamyl diuretic.

Molecular weight: 364.42
Formula: C17H20N2O5S
CLOGP: 3.07
LIPINSKI: 0
HAC: 7
HDO: 3
TPSA: 118.72
ALOGS: -4.15
ROTB: 8

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
1	mg	O
1	mg	P
1	mg	O

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	90 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
EoM (Fraction excreted unchanged in urine)	45 %	Benet LZ, Broccatelli F, Oprea TI
BDDCS (Biopharmaceutical Drug Disposition Classification System)	3	Benet LZ, Broccatelli F, Oprea TI
CL (Clearance)	2.50 mL/min/kg	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	1.20 hours	Lombardo F, Berellini G, Obach RS
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.46 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
Vd (Volume of distribution)	0.16 L/kg	Lombardo F, Berellini G, Obach RS
S (Water solubility)	0.10 mg/mL	Benet LZ, Broccatelli F, Oprea TI
fu (Fraction unbound in plasma)	0.03 %	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
Feb. 28, 1983	FDA

FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Acute kidney injury	247.13	13.45	429	27771	262986	63197836
Cardiac failure congestive	238.04	13.45	247	27953	92186	63368636
Hypervolaemia	200.21	13.45	136	28064	28277	63432545
Fluid retention	199.43	13.45	184	28016	59502	63401320
Dyspnoea	180.44	13.45	672	27528	660641	62800181
Pulmonary arterial hypertension	137.85	13.45	99	28101	22478	63438344
Right ventricular failure	134.88	13.45	88	28112	17100	63443722
Body tinea	131.19	13.45	44	28156	1841	63458981
Pulmonary hypertension	125.02	13.45	115	28085	37008	63423814
Inhibitory drug interaction	109.91	13.45	43	28157	2806	63458016

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Acute kidney injury	257.90	13.15	575	21052	304413	34630891
Cardiac failure congestive	172.43	13.15	234	21393	83036	34852268
Cardiac failure	121.56	13.15	209	21418	91039	34844265
Dyspnoea	121.03	13.15	506	21121	376276	34559028
Fluid retention	116.53	13.15	111	21516	26776	34908528
Hypervolaemia	88.50	13.15	83	21544	19626	34915678
Pulmonary hypertension	88.03	13.15	85	21542	20839	34914465
Oedema peripheral	73.01	13.15	200	21427	119612	34815692
Drug ineffective	60.42	13.15	120	21507	456631	34478673
Pulmonary arterial hypertension	55.80	13.15	45	21582	8694	34926610

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Acute kidney injury	492.27	12.51	955	42655	518449	79182329
Cardiac failure congestive	356.87	12.51	414	43196	141988	79558790
Fluid retention	258.50	12.51	250	43360	69559	79631219
Hypervolaemia	242.59	12.51	195	43415	42495	79658283
Dyspnoea	241.47	12.51	1015	42595	856010	78844768
Cardiac failure	184.11	12.51	315	43295	154527	79546251
Pulmonary hypertension	175.70	12.51	171	43439	47909	79652869
Pulmonary arterial hypertension	166.30	12.51	132	43478	28234	79672544
Right ventricular failure	161.08	12.51	120	43490	23377	79677401
Oedema peripheral	142.62	12.51	379	43231	251909	79448869

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
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
CHEBI has role	CHEBI:35498	diuretics
CHEBI has role	CHEBI:131770	CFTR inhibitors
FDA EPC	N0000175590	Loop Diuretic
FDA PE	N0000175366	Increased Diuresis at Loop of Henle
MeSH PA	D004232	Diuretics
MeSH PA	D049990	Membrane Transport Modulators
MeSH PA	D045283	Natriuretic Agents

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Drug Use | Suggest Off label Use Form| |View source of the data|

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Disease	Relation	SNOMED_ID	DOID
Edema	indication	267038008
Edema due to Hepatic Cirrhosis	indication
Peripheral Edema due to Chronic Heart Failure	indication
Renal Disease with Edema	indication
Pulmonary Edema due to Chronic Heart Failure	indication
Hypertensive disorder	off-label use	38341003	DOID:10763
Hypercalcemia	off-label use	66931009	DOID:12678
Decompensated cardiac failure	off-label use	195111005
Anuria	contraindication	2472002	DOID:2983
Hypocalcemia	contraindication	5291005

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (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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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Solute carrier family 12 member 1	Transporter	Q13621	S12A1_HUMAN	INHIBITOR	Ki	7.60	WOMBAT-PK	CHEMBL
Sodium/potassium-transporting ATPase subunit alpha-1	Transporter	P05023	AT1A1_HUMAN		Kd	7.52	WOMBAT-PK
Solute carrier family 12 member 2	Transporter	P55011	S12A2_HUMAN	INHIBITOR	IC50	5.60	IUPHAR
G-protein coupled receptor 35	GPCR	Q9HC97	GPR35_HUMAN	AGONIST	EC50	5.54	IUPHAR

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External reference:

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ID	Source
002312	NDDF
0Y2S3XUQ5H	UNII
1808	RXNORM
2471	PUBCHEM_CID
2943	INN_ID
3606	MMSL
387498005	SNOMEDCT_US
4017794	VUID
4017794	VANDF
4304	MMSL

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Bumetanide	HUMAN PRESCRIPTION DRUG LABEL	1	0185-0128	TABLET	0.50 mg	ORAL	ANDA	21 sections
Bumetanide	HUMAN PRESCRIPTION DRUG LABEL	1	0185-0128	TABLET	0.50 mg	ORAL	ANDA	21 sections
Bumetanide	HUMAN PRESCRIPTION DRUG LABEL	1	0185-0129	TABLET	1 mg	ORAL	ANDA	21 sections
Bumetanide	HUMAN PRESCRIPTION DRUG LABEL	1	0185-0129	TABLET	1 mg	ORAL	ANDA	21 sections
Bumetanide	HUMAN PRESCRIPTION DRUG LABEL	1	0185-0130	TABLET	2 mg	ORAL	ANDA	21 sections
Bumetanide	HUMAN PRESCRIPTION DRUG LABEL	1	0185-0130	TABLET	2 mg	ORAL	ANDA	21 sections
Bumetanide	HUMAN PRESCRIPTION DRUG LABEL	1	0409-1412	INJECTION, SOLUTION	0.25 mg	INTRAMUSCULAR	ANDA	20 sections
bumetanide	HUMAN PRESCRIPTION DRUG LABEL	1	0615-8361	TABLET	1 mg	ORAL	ANDA	20 sections
bumetanide	HUMAN PRESCRIPTION DRUG LABEL	1	0615-8362	TABLET	2 mg	ORAL	ANDA	20 sections
Bumetanide	HUMAN PRESCRIPTION DRUG LABEL	1	0615-8393	TABLET	1 mg	ORAL	ANDA	21 sections

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