Generic Name : Bumetanide.

Trade Name     : Burinex.

Drug Class       : Loop Diuretics.

Forms of The Drug

  1. Tablet: 0.5mg – 1mg – 2mg.
  2. Injectable Solution: 0.25mg/mL.

Mechanism of Action

The mechanism of action of bumetanide primarily involves its effects on the kidneys and their ability to regulate fluid and electrolyte balance in the body. Bumetanide acts on the thick ascending limb of the loop of Henle in the kidneys. This segment plays a crucial role in reabsorbing sodium, potassium, and chloride ions from the urine filtrate. By inhibiting the sodium-potassium-chloride co-transporter (NKCC2) located in this part of the nephron, bumetanide reduces the reabsorption of these ions. The inhibition of NKCC2 prevents the reabsorption of sodium, potassium, and chloride from the tubular fluid into the bloodstream. This results in increased excretion of these ions in the urine. As a consequence, water follows the excreted ions, leading to increased urine production and subsequent removal of excess fluid from the body. By promoting diuresis, bumetanide helps to reduce fluid overload, relieve edema, and lower blood pressure.

Bumetanide’s diuretic effect is more potent compared to other loop diuretics, such as furosemide. It has a rapid onset of action and a relatively short duration of activity. The drug is usually administered orally or intravenously, and its effects are typically seen within 30 minutes to an hour after administration. Apart from its diuretic properties, bumetanide has also been found to have additional actions. It has been shown to exert antiepileptic effects by blocking the activity of a specific transporter called NKCC1, which is responsible for regulating chloride ion movement in neurons. By inhibiting NKCC1, bumetanide helps to restore the balance of chloride ions and reduce neuronal excitability, thereby potentially providing therapeutic benefits in certain types of epilepsy.

Indications

  1. Edema associated with congestive heart failure.
  2. Edema associated with liver disease.
  3. Renal impairment.
  4. Hypertension.
  5. Ascites.
  6. Hypercalcemia.

Contraindications

  1. Hypersensitivity.
  2. Anuria.
  3. Severe electrolyte imbalance.
  4. Severe hepatic encephalopathy.
  5. Pre-coma or coma state.
  6. Dehydration.
  7. Pregnancy and breastfeeding.

Side Effects

  1. Hyperuricemia (18%)
  2. Hypochloremia (15%)
  3. Hypokalemia (15%)
  4. Azotemia (11%)
  5. Hyponatremia (9%)
  6. Hyperglycemia (7%)
  7. Increased serum creatinine (7%)
  8. Variations in phosphorus (5%)
  9. Variations in CO2 content (4%)
  10. Variations in bicarbonate (3%)
  11. Variations in calcium (2%)
  12. Dizziness (1%)
  13. Muscle cramps (1%)
  14. Ototoxicity (1%)

Drug Interaction

Other drugs that can interact with it.

  1. NSAIDs such as ibuprofen and naproxen.
  2. Aminoglycoside antibiotics such as gentamicin and tobramycin.
  3. Lithium.
  4. Digoxin.
  5. Antihypertensive medications such as beta-blockers or ACE inhibitors.
  6. Corticosteroids such as prednisone or dexamethasone.
  7. Diuretics such as thiazides.

Precautions

  1. Pregnancy: Category C.
  2. Lacation: Bumetanide is known to be excreted into breast milk, and its use during lactation should be approached with caution. The effects of bumetanide on nursing infants are not well-established, and there is limited information available regarding its safety during breastfeeding. Therefore, the use of bumetanide while breastfeeding should be carefully considered, weighing the potential benefits against the possible risks to the nursing infant.

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