Source of information: Drugbank (External Link). Last updated on: 3rd July 18
*Trade Name used in the content below may not be the same as the HSA-registered product.
Active Ingredient / Synonyms
3-(Aminosulfonyl)-5-(butylamino)-4-phenoxybenzoic acid | 3-Butylamino-4-(phenoxy)-5-sulfamoylbenzoic acid | 3-Butylamino-4-phenoxy-5-sulfamoyl-benzoic acid | 3-Butylamino-4-phenoxy-5-sulfamoylbenzoic acid | Bumetanida | Bumetanidum | Bumetanide |
A sulfamyl diuretic. [PubChem]
For the treatment of edema associated with congestive heart failure, hepatic and renal disease including the nephrotic syndrome.
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.
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, meaning that the predictable absorption is reflected in a more predictable effect. Bumetanide is 40 times more potent than furosemide (for patients with normal renal function).
Bumetanide is completely absorbed (80%), and the absorption is not altered when taken with food. Bioavailability is almost complete.
45% is secreted unchanged. Urinary and biliary metabolites are formed by oxidation of the N-butyl side chain.
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.
* 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]
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.
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