DIUREXAN TABLETS 20MG
Active substance: XIPAMIDE
View full screen / Print PDF » Download PDF ⇩
Transcript
SUMMARY OF PRODUCT CHARACTERISTICS
1
NAME OF THE MEDICINAL PRODUCT
Diurexan Tablets
2
QUALITATIVE AND QUANTITATIVE COMPOSITION
Xipamide 20 mg
3
PHARMACEUTICAL FORM
The tablets are white, round and biplanar with bisecting score on one side and debossed A on the other. They have a diameter of approximately 6mm.
4
4.1
CLINICAL PARTICULARS
Therapeutic indications
For the treatment of hypertension, either alone or as an adjunct to treatment with anti-hypertensive drugs. For use as a diuretic.
4.2
Posology and method of administration
1.
Trearment of Hypertension
Dosage:
Adults: 1 tablet (20 mg) daily, as a single early morning dose. When using Diurexan in combination with other antihypertensive therapy, the same dose of 20 mg as a single early morning dose should be maintained. Children: No dose recommended. Elderly: See Precautions.
2.
Use as diuretic
Dosage: Adults: In the initial phase of treatment the usual dose is 2 tablets (40 mg) daily in a single early morning dose. Depending on the patients response, the dose may be lowered to 1 tablet daily when sufficient control of oedema has been achieved. Higher doses, up to 4 tablets daily (80 mg), may be employed in resistant cases. Children: No dose recommended. Elderly: See Precautions.
4.3
Contraindications Diurexan is contra-indicated in severe electrolyte deficiency, precomatose states associated with liver cirrhosis, severe renal insufficiency, hypersensitivity to xipamide and untreated Addisons disease.
4.4
Special warnings and precautions for use
Like other diuretics, Diurexan may induce hypokalaemia in long-term therapy. Potassium supplements may be necessary, particularly in the elderly where dietary potassium intake may be inadequate, in digitalised patients and in conditions where additional potassium loss occurs such as vomiting, diarrhoea, malnutrition, nephrosis, hepatic cirrhosis and hyperaldosteronism.
Diurexan may exacerbate gout or induce hyperuricaemia or impaired glucose metabolism in patients predisposed to these conditions. In such patients serum urate or glucose levels should be monitored. Hyperuricaemia may require concomitant use of a uricosuric agent while diabetic patients will probably require an adjustment of insulin dosage, or other hypoglycaemic agent therapy. As with all antihypertensive agents, care should be taken in patients with severe coronary or cerebral arteriosclerosis. An increased risk of developing urinary retention may arise in patients with prostatic hypertrophy.
4.5
Interaction with other medicinal products and other forms of interaction
The dosage of other hypotensive drugs and cardiac glycosides may require adjustment when used in conjunction with Diurexan. Diabetic patients may require an increase in their dose of insulin or oral hypoglycaemic drug. Corticosteroids, ACTH, carbenoxolone, amphotericin and laxatives may provoke hypokalaemia. Increased serum lithium levels may occur due to diminished urinary excretion.
4.6
Pregnancy and lactation
Use in pregnancy: Animal experiments have indicated that Diurexan is devoid of teratogenic properties or effects on fertility and reproduction. However, care should be taken when treating hypertension or oedema in pregnancy as excessive use may result in hypovolaemia and reduced placental perfusion. As with all drugs, treatment should be avoided in the first trimester of pregnancy. No information is available on the excretion of xipamide in breast milk. Treatment should be avoided in breast feeding mothers.
4.7
Effects on ability to drive and use machines
None known.
4.8
Undesirable effects
Diurexan is generally well-tolerated. Slight gastro-intestinal disturbances have been reported in a few cases as have episodes of mild dizziness. Hypokalaemia and, more rarely, other electrolyte disturbances such as hyponatraemia have been reported.
4.9
Overdose
Little information is available on the effects of acute overdosage with xipamide, however hypotension with metabolic disturbances and electrolyte imbalances are likely. Chronic overdose may lead to a temporary increase in blood viscosity due to haemoconcentration although thromboembolic complications have not been reported. There is no specific antidote to xipamide. Gastric lavage or induced emesis may prevent further absorption. General measures should be aimed at the maintenance of blood pressure, restoration of blood volume and correction of electrolyte imbalance with appropriate intravenous infusion as required.
5
5.1
PHARMACOLOGICAL PROPERTIES
Pharmacodynamic properties
Xipamide is an anti-hypertensive diuretic which can be characterised pharmacologically neither as a thiazide nor as a specific loop diuretic. Although structurally similar to chlorthalidone, it has a markedly different pharmacological profile with its main diuretic effect exerted at the distal section of the nephron. As a diuretic, xipamide has been shown to be as effective as frusemide in terms of daily urine output, but has a more gradual and prolonged action.
5.2
Pharmacokinetic properties
Following single oral administration of 20 mg xipamide, peak plasma concentrations of up to 3 g/ml occur within 1 hour. Absolute bioavailability after oral administration is about 73%.
Xipamide is highly bound to plasma protein and has a volume of distributions of about 10 litres. After oral or i.v. administration, the apparent elimination t1/2 is of the order of 5-8 h. About 90% of an oral or i.v. dose is excreted in the urine with 50% of the dose eliminated in urine unchanged and a further 30% as the 0-0 glucuronide
5.3
Preclinical safety data
Not relevant.
6
6.1
PHARMACEUTICAL PARTICULARS
List of excipients
Maize Starch Mannitol Cellulose Powder Colloidol Silicon Dioxide Magnesium Stearate Purified Water
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
Aluminium - PVC Blister strip holds 14 tablets presented as either 10 blister strips or 2 blister strips in folded cardboard box. Aluminium - PVC Blister strip holds 4 tablets.
6.6
Special precautions for disposal
Not relevant
7
MARKETING AUTHORISATION HOLDER
Meda Pharmaceuticals Ltd 249 West George Street Glasgow G2 4RB Trading as: Meda Pharmaceuticals Ltd Skyway House Parsonage Road Takeley Bishops Stortford CM22 6PU UK
8
MARKETING AUTHORISATION NUMBER(S)
PL 15142/0132
9
DATE OF FIRST AUTHORISATION/RENEWAL OF THE AUTHORISATION
03/04/2009
10
DATE OF REVISION OF THE TEXT
24/06/2009
1
NAME OF THE MEDICINAL PRODUCT
Diurexan Tablets
2
QUALITATIVE AND QUANTITATIVE COMPOSITION
Xipamide 20 mg
3
PHARMACEUTICAL FORM
The tablets are white, round and biplanar with bisecting score on one side and debossed A on the other. They have a diameter of approximately 6mm.
4
4.1
CLINICAL PARTICULARS
Therapeutic indications
For the treatment of hypertension, either alone or as an adjunct to treatment with anti-hypertensive drugs. For use as a diuretic.
4.2
Posology and method of administration
1.
Trearment of Hypertension
Dosage:
Adults: 1 tablet (20 mg) daily, as a single early morning dose. When using Diurexan in combination with other antihypertensive therapy, the same dose of 20 mg as a single early morning dose should be maintained. Children: No dose recommended. Elderly: See Precautions.
2.
Use as diuretic
Dosage: Adults: In the initial phase of treatment the usual dose is 2 tablets (40 mg) daily in a single early morning dose. Depending on the patients response, the dose may be lowered to 1 tablet daily when sufficient control of oedema has been achieved. Higher doses, up to 4 tablets daily (80 mg), may be employed in resistant cases. Children: No dose recommended. Elderly: See Precautions.
4.3
Contraindications Diurexan is contra-indicated in severe electrolyte deficiency, precomatose states associated with liver cirrhosis, severe renal insufficiency, hypersensitivity to xipamide and untreated Addisons disease.
4.4
Special warnings and precautions for use
Like other diuretics, Diurexan may induce hypokalaemia in long-term therapy. Potassium supplements may be necessary, particularly in the elderly where dietary potassium intake may be inadequate, in digitalised patients and in conditions where additional potassium loss occurs such as vomiting, diarrhoea, malnutrition, nephrosis, hepatic cirrhosis and hyperaldosteronism.
Diurexan may exacerbate gout or induce hyperuricaemia or impaired glucose metabolism in patients predisposed to these conditions. In such patients serum urate or glucose levels should be monitored. Hyperuricaemia may require concomitant use of a uricosuric agent while diabetic patients will probably require an adjustment of insulin dosage, or other hypoglycaemic agent therapy. As with all antihypertensive agents, care should be taken in patients with severe coronary or cerebral arteriosclerosis. An increased risk of developing urinary retention may arise in patients with prostatic hypertrophy.
4.5
Interaction with other medicinal products and other forms of interaction
The dosage of other hypotensive drugs and cardiac glycosides may require adjustment when used in conjunction with Diurexan. Diabetic patients may require an increase in their dose of insulin or oral hypoglycaemic drug. Corticosteroids, ACTH, carbenoxolone, amphotericin and laxatives may provoke hypokalaemia. Increased serum lithium levels may occur due to diminished urinary excretion.
4.6
Pregnancy and lactation
Use in pregnancy: Animal experiments have indicated that Diurexan is devoid of teratogenic properties or effects on fertility and reproduction. However, care should be taken when treating hypertension or oedema in pregnancy as excessive use may result in hypovolaemia and reduced placental perfusion. As with all drugs, treatment should be avoided in the first trimester of pregnancy. No information is available on the excretion of xipamide in breast milk. Treatment should be avoided in breast feeding mothers.
4.7
Effects on ability to drive and use machines
None known.
4.8
Undesirable effects
Diurexan is generally well-tolerated. Slight gastro-intestinal disturbances have been reported in a few cases as have episodes of mild dizziness. Hypokalaemia and, more rarely, other electrolyte disturbances such as hyponatraemia have been reported.
4.9
Overdose
Little information is available on the effects of acute overdosage with xipamide, however hypotension with metabolic disturbances and electrolyte imbalances are likely. Chronic overdose may lead to a temporary increase in blood viscosity due to haemoconcentration although thromboembolic complications have not been reported. There is no specific antidote to xipamide. Gastric lavage or induced emesis may prevent further absorption. General measures should be aimed at the maintenance of blood pressure, restoration of blood volume and correction of electrolyte imbalance with appropriate intravenous infusion as required.
5
5.1
PHARMACOLOGICAL PROPERTIES
Pharmacodynamic properties
Xipamide is an anti-hypertensive diuretic which can be characterised pharmacologically neither as a thiazide nor as a specific loop diuretic. Although structurally similar to chlorthalidone, it has a markedly different pharmacological profile with its main diuretic effect exerted at the distal section of the nephron. As a diuretic, xipamide has been shown to be as effective as frusemide in terms of daily urine output, but has a more gradual and prolonged action.
5.2
Pharmacokinetic properties
Following single oral administration of 20 mg xipamide, peak plasma concentrations of up to 3 g/ml occur within 1 hour. Absolute bioavailability after oral administration is about 73%.
Xipamide is highly bound to plasma protein and has a volume of distributions of about 10 litres. After oral or i.v. administration, the apparent elimination t1/2 is of the order of 5-8 h. About 90% of an oral or i.v. dose is excreted in the urine with 50% of the dose eliminated in urine unchanged and a further 30% as the 0-0 glucuronide
5.3
Preclinical safety data
Not relevant.
6
6.1
PHARMACEUTICAL PARTICULARS
List of excipients
Maize Starch Mannitol Cellulose Powder Colloidol Silicon Dioxide Magnesium Stearate Purified Water
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
Aluminium - PVC Blister strip holds 14 tablets presented as either 10 blister strips or 2 blister strips in folded cardboard box. Aluminium - PVC Blister strip holds 4 tablets.
6.6
Special precautions for disposal
Not relevant
7
MARKETING AUTHORISATION HOLDER
Meda Pharmaceuticals Ltd 249 West George Street Glasgow G2 4RB Trading as: Meda Pharmaceuticals Ltd Skyway House Parsonage Road Takeley Bishops Stortford CM22 6PU UK
8
MARKETING AUTHORISATION NUMBER(S)
PL 15142/0132
9
DATE OF FIRST AUTHORISATION/RENEWAL OF THE AUTHORISATION
03/04/2009
10
DATE OF REVISION OF THE TEXT
24/06/2009
Source: Medicines and Healthcare Products Regulatory Agency
Disclaimer: Every effort has been made to ensure that the information provided here is accurate, up-to-date, and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. This information has been compiled for use by healthcare practitioners and consumers in the United States. The absence of a warning for a given drug or drug combination in no way should be construed to indicate that the drug or drug combination is safe, effective or appropriate for any given patient. If you have questions about the drugs you are taking, check with your doctor, nurse or pharmacist.
