Bumetanide

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[edit] BRAND NAMES

[edit] STRUCTURE

Bumetanide.jpg

[edit] MECHANISM OF ACTION

Bumetanide is a loop diuretic with a rapid onset and short duration of action.

Pharmacological and clinical studies have shown that Bumetanide is 40X more potent than furosemide (1mg bumetanide has a diuretic efficacy equivalent to approximately 40mg furosemide.

Bumetanide inhibits Na+/K+/2 Cl- co-transport in thick ascending limb, thus preventing the transport of sodium from the lumen of the loop of Henle into the basolateral interstitium. This co-transporter is responsible for 25% of the active sodium reabsorption.

Reabsorption of chloride in the ascending loop is also blocked by bumetanide. The excretion of chloride is greater than that of sodium and bumetanide also increases potassium excretion in a dose-related fashion.

Bumetanide decreases uric acid excretion and increases serum uric acid.

The diuretic effect of bumetanide is dose-related so that patients who fail to respond to a low initial dose usually respond as the dose is increased.

[edit] INDICATIONS

Bumetanide is indicated for the treatment of edema, particularly that associated with congestive heart failure, hepatic and renal diseases including the nephrotic syndrome and acute pulmonary edema.

Bumetanide is often used in people allergic to furosemide and in whom high doses of furosemide are ineffective

[edit] DOSAGE

The usual total oral daily dosage of bumetanide is 0.5 to 2.0 mg and in most patients may be given as a single dose.

If the diuretic response to an initial 1 mg dose is not adequate, a second or third dose may be given at 4 to 5 hour intervals. The maximum recommended daily dose is 10 mg.

An intermittent dose schedule, whereby Bumetanide is given on alternate days or for 3 to 4 days with rest periods of 1 to 2 days in between is recommended as the safest and most effective method for the continued control of edema.

In patients with hepatic failure the dosage should be kept to a minimum, and if necessary, dosage increased very carefully. A maintenance dose as low as 0.5 mg daily should be considered and the daily dose should not exceed 5 mg.


Paediatrics: Safety and efficacy in children below the age of 18 years has not been established

[edit] CONTRAINDICATIONS

  • Hypersensitivity to bumetanide
  • Anuria or in increasing azotemia: Although Bumetanide can be used to induce diuresis in renal insufficiency, any marked increase in blood urea nitrogen or creatinine or the development of oliguria during therapy of patients with progressive renal disease is an indication for discontinuation of treatment with bumetanide

[edit] PRECAUTIONS

Volume and electrolyte depletion:
Excessive doses or too-frequent administration can lead to profound water loss, electrolyte depletion, dehydration, reduction in blood volume and circulatory collapse with the possibility of vascular thrombosis and embolism, particularly in elderly patients.

Serum potassium should be measured periodically and potassium supplements or potassium-sparing diuretics added if necessary. Prevention of hypokalaemia is of particular importance in patients receiving digitalis and diuretics for congestive heart failure, hepatic cirrhosis or ascites; states of aldosterone excess with normal renal function; potassium-losing nephropathy, certain diarrhoeal states, or other states where hypokalemia is thought to represent particular added risks to the patient, i.e., history of ventricular arrhythmias.

Periodic determinations of other electrolytes (in particular, sodium, potassium, chloride, calcium and bicarbonate) are advised in patients treated with high doses or for prolonged periods, particularly in those on low salt diets.

Symptoms of electrolyte depletion are weakness, dizziness, lethargy, leg cramps, anorexia, vomiting or mental confusion.

Asymptomatic hyperuricaemia may occur. Reversible elevations of blood urea nitrogen (BUN) and creatinine may also occur, especially in association with dehydration and in patients with renal failure.


Hepatic cirrhosis and ascites:
Special caution should be used in these conditions since sudden changes in electrolyte balance may precipitate hepatic encephalopathy and coma.


Allergy to sulphonamides:
Patients allergic to sulphonamides may also exhibit hypersensitivity to bumetanide.

[edit] INTERACTIONS

  • Lithium: Bumetanide should not be administered concurrently with lithium salts since diuretics can reduce lithium clearance, resulting in high serum levels of lithium.
  • Probenecid: The diuretic and natriuretic effects of bumetanide are inhibited by probenecid.
  • Antihypertensives: Bumetanide may potentiate the effect of various antihypertensive drugs, necessitating a reduction in the dosage of the antihypertensive.
  • Digitalis: Low serum potassium levels may increase the sensitivity of the myocardium to the toxic effects of digitalis preparations, however studies have shown no direct effect of bumetanide on digoxin blood levels.
  • Drugs with ototoxic potential: Animal studies have shown bumetanide may produce ototoxicity.The possibility of ototoxic potentiation in humans cannot be excluded and concomitant administration of bumetanide and ototoxic drugs such as aminoglycosides should be avoided. This is of particular importance when renal function is impaired. It has been suggested that bumetanide may cause significantly less ototoxicity than furosemide.
  • Drugs with Nephrotoxic Potential: There has been no experience on the concurrent use of Bumetanide with drugs known to have a nephrotoxic potential. Therefore the simultaneous administration of these drugs should be avoided.
  • Indomethacin: Indomethacin may decrease the effect of bumetanide.

[edit] PREGNANCY AND LACTATION

  • Pregnancy Category C (US). It should be given to a pregnant woman only if the potential benefit justifies the potential risk to the fetus.
  • Use in Lactation: It is not known whether bumetanide is excreted in breast milk, therefore the drug is not recommended for use during lactation unless the expected benefits outweigh the potential risks.

[edit] SIDE EFFECTS

The most frequent clinical adverse reactions observed with bumetanide are muscle cramps (1.1%), dizziness (1.1%), hypotension (0.8%), headache (0.6%), nausea (0.6%), and encephalopathy (in patients with preexisting liver disease) (0.6%).

[edit] RELATED LINKS

[edit] BIBLIOGRAPHY

http://www.csl.com.au/docs/426/920/Burinex%20PI%20-%20approved%20Oct2011,0.pdf

[edit] REFERENCES

Antihypertensives
ACE inhibitors Benazepril (Lotensin)   Captopril (Capoten)   Cilazapril   Delapril   Enalapril (Renitec, Vasotec)   Fosinopril (Monopril)  Lisinopril (Prinivil, Zestril)   Moexipril (Univasc)  Perindopril (Aceon)  Quinapril (Accupril)  Ramipril (Altace, Triatec)   Trandolapril (Mavik)  Zofenopril (Bifril, Zopranol)
Angiotensin II receptor antagonist Azilsartan (Edarbi)   Candesartan (Atacand)   Eprosartan (Teveten)   Irbesartan (Aprovel, Avapro, Karvea)   Losartan (Cozaar)   Olmesartan (Benicar, Olmetec)   Telmisartan (Micadis)   Valsartan (Diovan, Tareg)
Renin inhibitors Aliskiren (Rasilez, Tekturna)
Alpha-1 blockers Doxazosin (Cardura)   Prazosin (Minipress)   Terazosin (Hytrin)
Alpha-2 agonists (centrally acting) Clonidine (Oral route)   Clonidine (Transdermal) (Catapresan)   Guanfacine (Tenex)   Methyldopa (Aldomet)
Calcium channel blockers Dihydropyridines‎ Amlodipine (Norvasc)   Barnidipine (Vasexten)   Felodipine (Plendil)   Isradipine (Dynacirc)   Lacidipine (Lacipil, Motens)   Lercanidipine (Zanidip)   Manidipine   Nicardipine   Nifedipine (Adalat)   Nisoldipine   Nitrendipine
Benzothiazepine‎ Diltiazem (Cardizem, Taztia XT, Tiazac, Tildiem)
Phenylalkylamine‎ Gallopamil   Verapamil (Calan)
Beta blockers Beta1 selective (cardioselective) Acebutolol (Sectral)   Atenolol (Tenormin)   Betaxolol (Kerlon)   Bisoprolol (Concor)   Celiprolol (Cordiax)   Metoprolol (Betaloc, Lopressor, Toprol-XL)   Nebivolol (Bystolic, Lobivon, Nebilox)
Nonselective (Beta1 and Beta2 blockers) Oxprenolol (Trasitensin)   Propranolol (Inderal)   Timolol (Blocadren)
Nonselective (Beta1, Beta2 and Alpha1 blockers) Carvedilol (Dilatrend)   Labetalol (Trandate)
Beta blocker with intrinsic sympathomimetic activity (ISA) Acebutolol (Sectral)   Celiprolol (Cordiax)
Lipophilic Beta blockers Propranolol (Inderal)   Metoprolol (Betaloc, Lopressor, Toprol-XL)   Oxprenolol (Trasitensin)
Diuretics Carbonic anhydrase inhibitors Acetazolamide (Diamox)
Loop diuretics Bumetanide   Etacrynic acid   Furosemide (Lasix)   Piretanide   Torasemide (Demadex)
Thiazide diuretics Chlorothiazide (Diuril)   Hydrochlorothiazide (Esidrex)
Thiazide-like diuretics Chlortalidone (Hygroton)   Indapamide (Lozol, Lozide)   Metolazone
Potassium-sparing diuretics Epithelial sodium channel blockers: Amiloride (Midamor)   Triamterene (Dyrenium)
Aldosterone receptor antagonists: Potassium canrenoate   Eplerenone (Inspra)   Spironolactone (Aldactone)
Osmotic diuretics Mannitol
Combination therapy Amiloride/Hydrochlorothiazide (Moduretic)   Spironolactone/Hydrochlorothiazide (Aldactazide)