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QuickView for Bumetanide (compound)

Name: Bumetanide
PubChem Compound ID: 2471
Description: A sulfamyl diuretic.
Molecular formula: C17H20N2O5S
Molecular weight: 364.417 g/mol
NINDS_000034; Diurama; EINECS 249-004-6; Aquazone; Burinex; Bio2_000228; KBio2_006933; NCGC00015149-02; NCGC00015149-01; KBio1_000034.
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Name: Bumetanide
Name (isomeric): DB00887
Drug Type: small molecule
Description: A sulfamyl diuretic.
Bumetanidum [INN-Latin]; Bumetanida [INN-Spanish]
Brand: Fontego, Burine, Fordiuran, Burinex, Segurex, Lunetoron, Lixil, Bumex
Category: Diuretics, Sulfamyl, Diuretics, Sodium Potassium Chloride Symporter Inhibitors
CAS number: 28395-03-1
Indication: For the treatment of edema associated with congestive heart failure, hepatic and renal disease including the nephrotic syndrome.
Bumetanide is a loop diuretic of the sulfamyl category to treat heart failure. It is often used in patients in whom high doses of furosemide are ineffective. There is however no reason not to use bumetanide as a first choice drug. The main difference between the two substances is in bioavailability. It is said to be a more predictable diuretic, mea...
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Mechanism of Action: Bumetanide interferes with renal cAMP and/or inhibits the sodium-potassium ATPase pump. Bumetanide appears to block the active reabsorption of chloride and possibly sodium in the ascending loop of Henle, altering electrolyte transfer in the proximal tubule. This results in excretion of sodium, chloride, and water and, hence, diuresis.
Absorption: Bumetanide is completely absorbed (80%), and the absorption is not altered when taken with food. Bioavailability is almost complete.
Protein binding: 97%
Biotransformation: 45% is secreted unchanged. Urinary and biliary metabolites are formed by oxidation of the N-butyl side chain.
Route of elimination: Oral administration of carbon-14 labeled Bumex to human volunteers revealed that 81% of the administered radioactivity was excreted in the urine, 45% of it as unchanged drug. Biliary excretion of Bumex amounted to only 2% of the administered dose.
Half Life: 60-90 minutes
Clearance: 0.2 - 1.1 mL/min/kg [preterm and full-term neonates with respiratory disorders] 2.17 mL/min/kg [neonates receiving bumetanide for volume overload] 1.8 +/- 0.3 mL/min/kg [geriatric subjects] 2.9 +/- 0.2 mL/min/kg [younger subjects]
Toxicity: Overdosage can lead to acute profound water loss, volume and electrolyte depletion, dehydration, reduction of blood volume and circulatory collapse with a possibility of vascular thrombosis and embolism. Electrolyte depletion may be manifested by weakness, dizziness, mental confusion, anorexia, lethargy, vomiting and cramps. Treatment consists of replacement of fluid and electrolyte losses by careful monitoring of the urine and electrolyte output and serum electrolyte levels.
Affected organisms: Humans and other mammals
Food interaction:
Take with food to reduce irritation.
Drug interaction:
DigitoxinPossible electrolyte variations and arrhythmias
IbuprofenThe NSAID, ibuprofen, may antagonize the diuretic and antihypertensive effects of the loop diuretic, bumetanide.
KanamycinIncreased ototoxicity
SulindacThe NSAID, sulindac, decreases the diuretic and antihypertensive effects of the loop diuretic, bumetanide.
DigoxinPossible electrolyte variations and arrhythmias
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