Bumetanide

Uses

Bumetanide is used for the treatment of edema associated with congestive heart failure, hepatic and renal disease, including the nephrotic syndrome.

Bumetanide is also used to associated treatment for these conditions: Edema

How Bumetanide works

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.

Dosage

Bumetanide dosage

Oral1 mg in the morning , repeated after 6-8 hours if necessary, In severe cases , 5 mg daily increased by 5 mg every 12-24 hours according to response. Elderly , 500 micrograms daily may be sufficient.

ParenteralBy IV Injection : 1-2 mg, repeated after 20 minutes if necessary. Elderly, 500 micrograms (1 ml of Bumecard) daily may be sufficient.

By IV Infusion : 2-5 mg over 30-60 minutes.Elderly, 500 micrograms (1 ml of Bumecard) daily may be sufficient.

By IM Injection : 1 mg initially then adjusted according to response , Elderly 500 micrograms (1 ml of Bumecard) daily may be sufficient.

Paediatric use: Safety and effectiveness in paediatric patients below the age of 18 have not been established.

Side Effects

Muscle cramps (1.1%), dizziness (1.1%), hypotension (0.8%), headache (0.6%), nausea (0.6%)Others (ECG changes (0.4 %), musculoskeletal pain (0.2 %), Abdominal pain (0.2 %), renal failure (0.1%), thrombocytopenia (0.2%) etc.

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.

Precaution

Serum potassium should be measured periodically and potassium supplements or potassium sparing diuretics added if necessary.

Interaction

Lithium: Lithium should generally not be given with diuretics because they reduce its renal clearance and add a high risk of lithium toxicity.

Probenecid: should not be administered concurrently with Bumetanide.

Indomethacin: Concurrent therapy with Bumetanide is not recommended.

Antihypertensives: Bumetanide may potentiate the effect of various antihypertensive drugs, necessitating a reduction in the dosage of these drugs.

Digoxin: Interaction studies in humans have shown no effect on digoxin blood levels.

Anticoagulants: Interaction studies in humans have shown Bumetanide to have no effect on warfarin metabolism.

Food Interaction

• Take with food. Food reduces irritation.

Bumetanide Alcohol interaction

[Moderate]

Many psychotherapeutic and CNS-active agents (e.g., anxiolytics, sedatives, hypnotics, antidepressants, antipsychotics, opioids, alcohol, muscle relaxants) exhibit hypotensive effects, especially during initiation of therapy and dose escalation.

Coadministration with antihypertensives and other hypotensive agents, in particular vasodilators and alpha-blockers, may result in additive effects on blood pressure and orthostasis.

Caution and close monitoring for development of hypotension is advised during coadministration of these agents.

Some authorities recommend avoiding alcohol in patients receiving vasodilating antihypertensive drugs.

Patients should be advised to avoid rising abruptly from a sitting or recumbent position and to notify their physician if they experience dizziness, lightheadedness, syncope, orthostasis, or tachycardia.

Bumetanide Drug Interaction

Moderate: insulin glargine, insulin glargine, metoprolol, metoprolol, metoprolol, metoprololMinor: aspirin, aspirin, aspirin, aspirinUnknown: apixaban, apixaban, clopidogrel, clopidogrel, cyanocobalamin, cyanocobalamin, ascorbic acid, ascorbic acid, cholecalciferol, cholecalciferol

Bumetanide Disease Interaction

Major: anuria, cirrhosis, electrolyte losses, ototoxicity, renal dysfunctionModerate: diabetes, hyperuricemia

Elimination Route

Bumetanide is completely absorbed (80%), and the absorption is not altered when taken with food. Bioavailability is almost complete.

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]

Elimination Route

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.

Pregnancy & Breastfeeding use

Pregnancy: Pregnancy Category C : There are no adequate and well controlled studies in pregnant woman .Lactation: It is not known wheather this drug is excreted in human milk.

Contraindication

Loop diuretics should be avoided in severe hypokalaemia, severe hyponatraemia, anuria, comatose and precomatose states associated with liver cirrhosis and in renal failure.

Special Warning

Paediatric use: Safety and effectiveness in paediatric patients below the age of 18 have not been established.

Acute Overdose

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. Treatment consists of replacement of fluid and electrolyte losses by careful monitoring of the urine and electrolyte output and serum electrolyte levels.

Storage Condition

Store in a cool & dry place. Protect from light.

Innovators Monograph

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