1. Name Of The Medicinal Product
Burinex® 1 mg Tablets.
2. Qualitative And Quantitative Composition
Bumetanide Ph Eur 1 mg.
3. Pharmaceutical Form
Tablet.
4. Clinical Particulars
4.1 Therapeutic Indications
Burinex is indicated whenever diuretic therapy is required in the treatment of oedema, e.g. that associated with congestive heart failure, cirrhosis of the liver and renal disease including the nephrotic syndrome.
In oedema of cardiac or renal origin where high doses of a potent short acting diuretic are required, Burinex 5 mg tablets may be used.
4.2 Posology And Method Of Administration
For oral administration.
Most patients require a daily dose of 1 mg which can be given as a single morning or early evening dose. Depending on the patient's response, a second dose can be given six to eight hours later. In refractory cases, the dose can be increased until a satisfactory diuretic response is obtained, or infusions of Burinex can be given.
Children: not recommended for children under 12 years of age.
Dosage in the elderly: adjust dosage according to response. A dose of 0.5 mg bumetanide per day may be sufficient in some elderly patients.
4.3 Contraindications
Although Burinex can be used to induce diuresis in renal insufficiency, any marked increase in blood urea or the development of oliguria or anuria during treatment of severe progressing renal disease are indications for stopping treatment with Burinex.
Hypersensitivity to Burinex. Burinex is contra-indicated in hepatic coma and care should be taken in states of severe electrolyte depletion.
As with other diuretics, Burinex should not be administered concurrently with lithium salts. Diuretics can reduce lithium clearance resulting in high serum levels of lithium.
4.4 Special Warnings And Precautions For Use
Excessively rapid mobilisation of oedema, particularly in elderly patients, may give rise to sudden changes in cardiovascular pressure-flow relationships with circulatory collapse. This should be borne in mind when Burinex is given in high doses intravenously or orally. Electrolyte disturbances may occur, particularly in those patients taking a low salt diet. Regular checks of serum electrolytes, in particular sodium, potassium, chloride and bicarbonate, should be performed and replacement therapy instituted where indicated.
Encephalopathy may be precipitated in patients with pre-existing hepatic impairment.
Burinex should be used with caution in patients already receiving nephrotoxic or ototoxic drugs.
4.5 Interaction With Other Medicinal Products And Other Forms Of Interaction
Like other diuretics, Burinex shows a tendency to increase the excretion of potassium which can lead to an increase in the sensitivity of the myocardium to the toxic effects of digitalis. Thus the dose may need adjustment when given in conjunction with cardiac glycosides.
Burinex may potentiate the effects of antihypertensive drugs. Therefore, the dose of the latter may need adjustment when Burinex is used to treat oedema in hypertensive patients.
As with other diuretics, Burinex may cause an increase in blood uric acid. Periodic checks on urine and blood glucose should be made in diabetics and patients suspected of latent diabetes.
Patients with chronic renal failure on high doses of Burinex should remain under constant hospital supervision.
Certain non-steroidal anti-inflammatory drugs have been shown to antagonise the action of diuretics.
4.6 Pregnancy And Lactation
Although tests in four animal species have shown no teratogenic effects, the ordinary precaution of avoiding use of Burinex in the first trimester of pregnancy should at present be observed. Since it is not known whether bumetanide is distributed into breast milk, a nursing mother should either stop breast feeding or observe the infant for any adverse effects if the drug is absolutely necessary for the mother.
4.7 Effects On Ability To Drive And Use Machines
None known.
4.8 Undesirable Effects
Reported reactions include abdominal pain, vomiting, dyspepsia, diarrhoea, stomach and muscle cramps, arthralgia, dizziness, fatigue, hypotension, headache, nausea, encephalopathy (in patients with pre-existing hepatic disease), fluid and electrolyte depletion, dehydration, hyperuricaemia, raised blood urea and serum creatinine, hyperglycaemia, abnormalities of serum levels of hepatic enzymes, skin rashes, pruritus, urticaria, thrombocytopenia, gynaecomastia and painful breasts. Bone marrow depression associated with the use of Burinex has been reported rarely but it has not been proven definitely to be attributed to the drug. Hearing disturbance after administration of Burinex is rare and reversible.
High dose therapy:
In patients with severe chronic renal failure given high doses of Burinex, there have been reports of severe, generalised musculoskeletal pain sometimes associated with muscle spasm, occurring one to two hours after administration and lasting up to 12 hours. The lowest reported dose causing this type of adverse reaction was 5 mg by intravenous injection and the highest was 75 mg orally in a single dose. All patients recovered fully and there was no deterioration in their renal function. The cause of this pain is uncertain but it may be a result of varying electrolyte gradients at the cell membrane level.
Experience suggests that the incidence of such reactions is reduced by initiating treatment at 5-10 mg daily and titrating upwards using a twice daily dosage regimen at doses of 20 mg per day or more.
4.9 Overdose
Symptoms would be those caused by excessive diuresis. Empty stomach by gastric lavage or emesis. General measures should be taken to restore blood volume, maintain blood pressure and correct electrolyte disturbance.
5. Pharmacological Properties
5.1 Pharmacodynamic Properties
Burinex is a potent, high ceiling loop diuretic with a rapid onset and a short duration of action. The primary site of action is the ascending limb of the Loop of Henlé where it exerts inhibiting effects on electrolyte reabsorption causing the diuretic and natriuretic action observed.
After oral administration of 1 mg Burinex, diuresis begins within 30 minutes with a peak effect between one and two hours. The diuretic effect is virtually complete in three hours after a 1 mg dose.
5.2 Pharmacokinetic Properties
Burinex is well absorbed after oral administration with the bioavailability reaching between 80 and 95%. The elimination half life ranges from between 0.75 to 2.6 hours. No active metabolites are known. Renal excretion accounts for approximately half the clearance with hepatic excretion responsible for the other half. There is an increase in half-life and a reduced plasma clearance in the presence of renal or hepatic disease. In patients with chronic renal failure the liver takes more importance as an excretory pathway although the duration of action is not markedly prolonged.
5.3 Preclinical Safety Data
There are no pre-clinical data of relevance to the prescriber which are additional to that already included in other sections of the SPC.
6. Pharmaceutical Particulars
6.1 List Of Excipients
Maize starch, lactose, colloidal anhydrous silica, povidone, polysorbate 80, agar powder, talc and magnesium stearate.
6.2 Incompatibilities
None known
6.3 Shelf Life
5 years.
6.4 Special Precautions For Storage
None.
6.5 Nature And Contents Of Container
Blister packs of 28 tablets (OP).
6.6 Special Precautions For Disposal And Other Handling
None.
7. Marketing Authorisation Holder
LEO Laboratories Limited
Longwick Road
Princes Risborough
Bucks HP27 9RR
UK
8. Marketing Authorisation Number(S)
PL 0043/0021R
9. Date Of First Authorisation/Renewal Of The Authorisation
27 June 1996.
10. Date Of Revision Of The Text
December 2005
LEGAL CATEGORY
POM
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