Bumelex

Bumelex Uses, Dosage, Side Effects, Food Interaction and all others data.

Bumelex is a loop diuretic with a rapid onset and short duration of action. Pharmacological and clinical studies have shown that 1 mg Bumelex has a diuretic potency equivalent to approximately 40 mg furosemide. The major site of Bumelex action is the ascending limb of the loop of Henle.

Bumelex inhibits sodium reabsorption in the ascending limb of the loop of Henle. Reabsorption of chloride in the ascending limb is also blocked by Bumelex.

Bumelex may have an additional action in the proximal tubule. Since phosphate reabsorption takes place largely in the proximal tubule, phosphaturia during Bumelex induced diuresis is indicative of this additional action. This proximal tubular activity does not seem to be related to an inhibition of carbonic anhydrase. Bumelex does not appear to have a noticeable action on the distal tubule.

Bumelex 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. Bumelex has more predictable pharmacokinetic properties as well as clinical effect. In patients with normal renal function, bumetanide is 40 times more effective than furosemide.

Trade Name Bumelex
Availability Prescription only
Generic Bumetanide
Bumetanide Other Names Bumetanida, Bumetanide, Bumetanidum
Related Drugs furosemide, hydrochlorothiazide, spironolactone, Lasix, chlorthalidone, torsemide, triamterene, Bumex, amiloride, ethacrynic acid
Type
Formula C17H20N2O5S
Weight Average: 364.416
Monoisotopic: 364.10929245
Protein binding

97%

Groups Approved
Therapeutic Class Loop diuretics
Manufacturer
Available Country Venezuela
Last Updated: September 19, 2023 at 7:00 am
Bumelex
Bumelex

Uses

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

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

How Bumelex works

Bumelex interferes with renal cAMP and/or inhibits the sodium-potassium ATPase pump. Bumelex 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

Bumelex 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 Bumelex.

Indomethacin: Concurrent therapy with Bumelex is not recommended.

Antihypertensives: Bumelex 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 Bumelex to have no effect on warfarin metabolism.

Food Interaction

  • Take with food. Food reduces irritation.

Bumelex 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.

Elimination Route

Bumelex 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

You find simplified version here Bumelex

Bumelex contains Bumetanide see full prescribing information from innovator Bumelex Monograph, Bumelex MSDS, Bumelex FDA label

*** Taking medicines without doctor's advice can cause long-term problems.
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