BUMETANIDE
Clinical safety rating: safe
Animal studies have demonstrated safety
Inhibits the Na-K-2Cl symporter (NKCC2) in the thick ascending limb of the loop of Henle, reducing reabsorption of sodium, chloride, and potassium, leading to increased urine output.
| Metabolism | Primarily metabolized by the liver via cytochrome P450 (CYP) enzymes, with approximately 50% excreted unchanged in urine. |
| Excretion | Primarily renal (approximately 80% as unchanged drug), with minimal biliary/fecal excretion (about 10-20%). |
| Half-life | Terminal elimination half-life is approximately 1-1.5 hours in healthy adults; prolonged to 1.5-3 hours in renal impairment. |
| Protein binding | Approximately 95% bound, primarily to albumin. |
| Volume of Distribution | 0.15-0.25 L/kg; indicates limited extravascular distribution, consistent with high protein binding. |
| Bioavailability | Oral: approximately 80-100% (mean ~90%), with a first-pass effect of about 10-20%. |
| Onset of Action | Intravenous: within 5 minutes; Oral: within 30-60 minutes. |
| Duration of Action | Intravenous: 2-3 hours; Oral: 4-6 hours; diuresis is dose-dependent and may be shorter in patients with renal impairment. |
0.5-2 mg IV/IM/PO once daily; may repeat every 6-8 hours; max 10 mg/day. Continuous IV infusion: 1 mg loading dose, then 0.5-2 mg/hour.
| Dosage form | INJECTABLE |
| Renal impairment | No specific dose adjustment for GFR >20 mL/min. For GFR 10-20 mL/min: use with caution, dose every 12-24 hours. For GFR <10 mL/min: not recommended due to lack of efficacy. |
| Liver impairment | Child-Pugh A: no adjustment. Child-Pugh B: reduce dose by 50%. Child-Pugh C: avoid use. |
| Pediatric use | IV/IM/PO: 0.015-0.1 mg/kg/dose every 6-24 hours; max 10 mg/day. For neonates: 0.01-0.05 mg/kg/dose every 12-24 hours. |
| Geriatric use | Start at 0.5 mg once daily; titrate cautiously due to increased sensitivity and risk of electrolyte imbalance and volume depletion. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Other ototoxic drugs may increase risk of hearing loss Indomethacin may reduce the diuretic effect Profound diuresis and electrolyte depletion can occur.
| Breastfeeding | Bumetanide is excreted into human milk in small amounts (M/P ratio not determined). Due to potential for diuresis in the infant, use with caution, especially in neonates. Consider alternative agents with more safety data. |
| Teratogenic Risk | Bumetanide crosses the placenta. First trimester: No adequate human studies; animal studies show no teratogenicity at clinically relevant doses. Second and third trimesters: Risk of electrolyte imbalances and hypovolemia in the fetus; possible oligohydramnios. Avoid use during pregnancy unless benefits outweigh risks. |
■ FDA Black Box Warning
Bumetanide is a potent diuretic that can lead to profound diuresis with water and electrolyte depletion. Close medical supervision and dose titration are required. Excessive doses can lead to hypovolemia, dehydration, and circulatory collapse.
| Common Effects | hepatic |
| Serious Effects |
["Anuria","Severe electrolyte depletion","Hepatic coma or pre-coma","Hypersensitivity to bumetanide or sulfonamides"]
| Precautions | ["Monitor fluid and electrolyte balance closely","Risk of ototoxicity, especially at high doses or with rapid infusion","May cause hyperuricemia and precipitate gout attacks","Can increase risk of digitalis toxicity due to hypokalemia"] |
| Food/Dietary | No specific food restrictions, but limit salt intake to help control edema and hypertension. Avoid excessive intake of black licorice (can worsen hypokalemia). Grapefruit juice may not significantly interact, but caution with any electrolyte-altering foods. Maintain adequate fluid intake unless fluid restriction is advised by your doctor. Foods high in potassium (bananas, oranges, spinach) may be recommended if hypokalemia occurs; consult provider for individual needs. |
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| Fetal Monitoring | Monitor maternal electrolytes, renal function, blood pressure, and fluid status. Fetal monitoring includes ultrasound for amniotic fluid volume (risk of oligohydramnios) and fetal growth. |
| Fertility Effects | No adverse effects on fertility reported in animal studies. Human data insufficient to determine impact. |
| Clinical Pearls | Bumetanide is a potent loop diuretic with rapid onset and short duration. Oral bioavailability is ~80% with minimal first-pass metabolism. Onset of diuresis within 30-60 minutes, peak at 1-2 hours, duration 4-6 hours. For acute pulmonary edema, intravenous bumetanide can be given 0.5-1 mg; onset within minutes. Monitor electrolytes especially potassium, magnesium, and calcium due to increased excretion. May cause ototoxicity, especially with rapid IV administration or concurrent aminoglycosides. Use with caution in sulfonamide allergy (cross-sensitivity). In renal impairment, bumetanide may be less effective due to reduced tubular secretion; higher doses may be needed. Combine with thiazides for sequential nephron blockade in resistant edema. |
| Patient Advice | Take bumetanide exactly as prescribed, usually once daily in the morning to avoid nighttime urination. · Do not skip doses or double up on missed doses; if you miss a dose, take it as soon as you remember unless it is almost time for the next dose. · This medication can cause dehydration and electrolyte imbalances; notify your doctor if you experience excessive thirst, dry mouth, weakness, muscle cramps, or irregular heartbeat. · Avoid alcohol and over-the-counter medications, especially NSAIDs (ibuprofen, naproxen) unless approved by your doctor, as they may reduce bumetanide's effectiveness and increase kidney risk. · Stand up slowly from sitting or lying to prevent dizziness from low blood pressure. · Monitor your weight daily and report rapid weight gain or loss to your healthcare provider. |