Bumetanide (Bumethanidum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

Diuretics

Included in the formulation
АТХ:

C.03.C.A.02   Bumetanide

Pharmacodynamics:Interaction with the Cl binding site- and blocking Na+-TO+-2Cl-cotransporter (simport - BSC1) located on the apical surface of the epithelium of the thick segment of the ascending part of the Henle loop of the nephron leads to suppression of the reabsorption of sodium and chlorine ions, as well as of potassium and calcium ions, which in turn increases the excretion of sodium, potassium, magnesium, chlorine ions (and other halogens) and calcium. Weak inhibition of carbonic anhydrase results in increased excretion of HCO3 and phosphate. Promotes the excretion of sodium, potassium, calcium, magnesium.
Pharmacokinetics:

The diuretic effect with ingestion comes in 30-60 minutes, the maximum effect is achieved in 1-2 hours; duration of action 4 hours (at a dose of 1-2 mg), in higher doses - 4-6 hours. With intravenous administration, the onset of action after a few minutes, the maximum effect is achieved after 15-30 minutes, the duration of action is 3.5-4 hours.

Absorption is about 80%, bioavailability is 80-95%, the connection with plasma proteins is 94-96%. Biotransformation in the liver (incomplete) with the formation of inactive metabolites. Half-life - 1-1.5 hours. Elimination by the kidneys - 81% (45% unchanged), intestine - 2%.

Indications:
  • Pulmonary edema
  • Edema of the brain
  • Congestive heart failure
  • Chronic Renal Failure
  • Cirrhosis of the liver
  • Gestosis
ICD-10

VI.G90-G99.G93.6   Edema of the brain

IX.I30-I52.I50.0   Congestive heart failure

X.J80-J84.J81   Pulmonary edema

XI.K70-K77.K74   Fibrosis and cirrhosis of the liver

XIV.N17-N19.N18   Chronic Renal Failure

XIV.N17-N19.N17   Acute kidney failure

XV.O10-O16.O14   Pregnancy-induced hypertension with significant proteinuria

XVIII.R50-R69.R60   Edema, not elsewhere classified

Contraindications:
  • Hypersensitivity(including other sulphonyls)
  • Acute renal failure with anuria
  • Chronic Renal Failure
  • Acute hepatitis, hepatic coma
  • Decompensatedth diabetes mellitus
  • Gout
  • Hypokalemia
  • I trimester of pregnancy, breast-feeding.
Carefully:
  • Elderly age
  • Diabetes
  • Myocardial infarction
  • Pancreatitis (including anamnesis)
  • Joint use of other drugs, the toxicity of which increases with hypokalemia.
Pregnancy and lactation:

Recommendations by FDA - category C. Studies on humans have not been conducted. The use of bumetanide in the second half of pregnancy is possible only if the expected therapeutic effect for the mother exceeds the potential risk to the fetus.

Information about penetration into breast milk is not present.It is recommended to prescribe the drug only in those cases when the expected benefit for the mother exceeds the potential risk for the child.

Dosing and Administration:

Inside, usually in the morning before eating, 0.001 1 time a day, for 3-5 days, then 0.001-0.002 g once every 2-3 days. Single dose increase to 0.002 g in the absence of the desired effect. The highest daily dose is 0.006 g.

Intramuscular injection of 2-4 ml of 0.25%.

Intravenously injected slowly for 2-3 minutes, the drug diluted with 20 ml of isotonic sodium chloride solution or 5% glucose solution.

The highest daily dose for parenteral administration is 0.005 g.

In chronic renal failure, intravenously administered drip for 30-60 minutes at a dose of 0.002-0.005 g (dissolved in 500 ml of 0.9% sodium chloride solution). If necessary, repeat the infusion in the same dose after 6-8 hours.

Side effects:

From the side of water-electrolyte metabolism: hyponatremia, hypokalemia, hypochloraemic alkalosis.

From the cardiovascular system: arterial hypotension up to orthostatic collapse, arrhythmia.

On the part of the digestive system: dry mouth, thirst, abdominal pain, nausea, vomiting, anorexia, diarrhea, impaired liver function (icterus sclera, skin), pancreatitis.

From the side of metabolism: hyperuricemia, hyperglycemia, azotemia, increased concentration of creatinine.

From the central and peripheral nervous system: dizziness, headache.

From the musculoskeletal system: muscle spasms, myalgia, convulsions, pain in the joints (with exacerbation of gout).

On the part of the hematopoiesis system: leukopenia or agranulocytosis, thrombocytopenia.

From the sense organs: hearing impairment, visual impairment.

Dermatological reactions: itchy skin.

Allergic reactions: urticaria.

Overdose:

Symptoms: lowering blood pressure, dry mouth, thirst, convulsions.

Treatment: symptomatic.

Interaction:

The combined use of bumetanide with aminoglycosides and lithium preparations increases probability development of nephrotoxic effects.

The use of potassium-sparing diuretics during treatment reduces the risk of hypokalemia.

Diuretic (saluretic) properties of bumetanide decrease with simultaneous application probenecid and indomethacin.

Special instructions:During treatment it is recommended to eat foods rich in potassium salts.
Instructions
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