Bisoprolol 10mg Tablets
SUMMARY OF PRODUCT CHARACTERISTICS
1 NAME OF THE MEDICINAL PRODUCT
Bisoprolol 10mg tablets
2 QUALITATIVE AND QUANTITATIVE COMPOSITION
Each tablet contains 10mg of bisoprolol fumarate
For excipients, see 6.1
3 PHARMACEUTICAL FORM
Film-coated tablet; Bisoprolol 10mg tablets are Round film-coated, light brown coloured tablets with a break-line on one side and ‘10’ on other side.
4 CLINICAL PARTICULARS
4.1 Therapeutic indications
Management of hypertension Management of angina pectoris
4.2 Posology and method of administration
Route of Administration Oral
Posology:
Adults:
The usual dose is 10mg once daily with a maximum recommended dose of 20mg per day. In some patients 5mg per day may be adequate. In patients with final stage impairment of renal (creatinine clearance < 20ml/min) or liver function, the dose should not exceed 10mg bisoprolol fumarate once daily. Experience of the use of bisoprolol fumarate in renal dialysis patients is limited, however, there is no evidence that the dosage regimen needs to be altered.
Elderly:
No adequate adjustment is normally required but 5mg per day may be adequate in some dysfunction.
Children:
Not recommended as there is no experience Method of Administration For oral use
4.3 Contraindications
As with other beta-adrenoceptor antagonists, bisoprolol fumarate should not be used in cases of:
• Hypersensitivity to bisoprolol or any other ingredients in the tablet.
• Untreated cardiac failure
• Cardiogenic shock
• Marked bradycardia (heart rate less than 50 beats per minute)
• Sinoatrial block, second or third degree AV block
• Severe asthma
4.4 Special warnings and precautions for use
Caution should be taken in prescribing bisoprolol fumarate in the following
situations:
• Patients with prolonged PR conduction interval, poor cardiac reserve and peripheral circulatory disturbances ( such as Raynaud’s phenomenon)
• In patients with ischaemic heart disease, treatment should not be abruptly withdrawn.
• Patients with chronic obstructive airways disease or a family history of asthma.
• Bisoprolol fumarate is highly selective ^-adrenoceptor blocking agent. However, in some asthmatic patients some increase in airways resistance may occur, if this does, then treatment should be discontinued. This bronchospasm can usually be reversed by commonly used bronchodilators such as salbutamol.
• Diabetic patients as bisoprolol may mask the symptoms of hypoglycaemia (especially tachycardia). However, it should be noted that due to the low affinity of bisoprolol fumarate for ^2-receptors the drug appears not to have a hypoglycaemic effect
4.5 Interaction with other medicinal products and other forms of interaction
Caution should be taken in prescribing bisoprolol with the following
drugs/groups of drugs.
• Antihypertensive drugs: Bisoprolol fumarate may potentiate the effect of other concurrently administered antihypertensive drugs. Concomitant treatment with reserpine, methyldopa and clonidine may cause an exaggerated decrease in heart rate. If clonidine, in particular, is to be discontinued it should not be done unless bisoprolol fumarate treatment has been discontinued for several days.
• Myocardial depressants, inhibitors of AV conduction, class I antiarrhythmic agents. Bisoprolol fumarate should be used with care when myocardial depressants, inhibitors of AV conduction (such as calcium antagonists of the verapamil and diltiazem type) are used concurrently.
• The intravenous administration of calcium antagonists and antiarrhythmic agents is not recommended during bisoprolol fumarate therapy.
• Rifampicin: The concurrent use of rifampicin can reduce the half-life of bisoprolol, although an increase in dose is generally not necessary.
• The effects of insulin or oral hypoglycaemic agents may be potentiated when used concurrently with bisoprolol.
• Anaesthetics (enhanced hypotensive effect). The anaesthetist should be informed if the patient is taking bisoprolol fumarate. Care should be taken when using either cyclopropane or trichloroethylene. Beta-blockers have been reported to enhance the neuromuscular blockade of succinyl choline in animals. If the patient has severe ischaemic heart disease the risk/benefit of continuing treatment should be evaluated.
4.6 Fertility, Pregnancy and lactation
No teratogenic effects have been demonstrated in animal studies, but the safety of bisoprolol fumarate during human pregnancy has not been established. Like other beta-blockers, the benefits of use during pregnancy should be weighed against the possible hazard to mother and foetus. Beta-blockers administered in late pregnancy may cause bradycardia or hypotension in the foetus/neonate. Studies in animals suggest that no clinically relevant levels of bisoprolol fumarate reach the milk. However, as in pregnancy, caution should be exercised for use during lactation.
4.7 Effects on ability to drive and use machines
Bisoprolol fumarate may cause dizziness. Patients should be warned of this effect and advised to make sure they are not affected before driving or operating machinery.
4.8 Undesirable effects
Bisoprolol fumarate is generally well tolerated. The reported side effects are generally attributable to the pharmacological actions. The following side effects have been reported.
Effects on CNS: lassitude, fatigue, dizziness, mild headache and rarely sleep disturbances including vivid dreams
Effects on the gastrointestinal system:
Nausea, vomiting, diarrhoea
Effects on the CVS:
Aggravation of intermittent claudication or Raynaud’s disease and paraesthesia or coldness of extremities, oedema. Occasionally a marked decrease in blood pressure and pulse rate or a disturbance of AV conduction has been reported.
Effects on musculoskeletal system:
Muscle and joint pains Other effects:
Skin rashes, perspiration, dry eyes, bronchospasm
In the case of overdosage or a precipitous drop in pulse rate and/or blood pressure, treatment with bisoprolol fumarate must be discontinued. If necessary, the following antidotes should be administered alone or consecutively: intravenous atropine 0.5-2.0mg, intravenous orciprenaline 0.5mg by slow intravenous injection; also glucagon may be given at a low level of 1-5 mg.
5 PHARMACOLOGICAL PROPERTIES
5.1 Pharmacodynamic properties
Bisoprolol is a potent, highly P-selective-adrenoceptor blocking agent devoid of intrinsic sympathomimetic activity and without relevant membrane stabilising activity.
As with other P1-blocking agents, the mode of action in hypertension is unclear. However, it is known that bisoprolol markedly depresses plasma renin levels. In patients with angina, the blockade of P1-receptors reduces heart action and thus reduces oxygen demand. Hence bisoprolol is effective in eliminating or reducing the symptoms.
5.2 Pharmacokinetic properties
Bisoprolol is absorbed almost completely from the gastro-intestinal tract. Together with the very small first pass effect in the liver, this results in a high bioavailability of approximately 90%. The drug is cleared equally by the liver and kidney.
The plasma elimination half-life (10-12 hours) provides 24 hours efficacy following a once daily dosage. About 95% of the drug substance is excreted through the kidney, half of this is as unchanged bisoprolol. There are no active metabolites in man.
Preclinical safety data
5.3
There are no preclinical 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
Core
Maize Starch
Microcrystalline Cellulose Crospovidone
Anhydrous Calcium Hydrogen Phosphate Colloidal Anhydrous Silica Magnesium Stearate Purified Water
Film-coating Hypromellose Titanium dioxide (E171)
Macrogol 6000
Dimeticone 350
Iron Oxide Yellow (E 172)
Iron Oxide Red (E 172)
Purified Water
6.2 Incompatibilities
Not applicable
2 Years
6.4 Special precautions for storage
Do not store above 25 °C. Store in the original package.
6.5 Nature and contents of container
Blister PVC/PVdC /Aluminium foil, 28 tablets in a carton.
6.6 Special precautions for disposal
Not applicable
7 MARKETING AUTHORISATION HOLDER
Crescent Pharma Limited
3&4 Quidhampton Business Units
Polhampton Lane
Overton
Hampshire
RG25 3ED
UK
8 MARKETING AUTHORISATION NUMBER(S)
PL 20416/0299
9 DATE OF FIRST AUTHORISATION/RENEWAL OF THE AUTHORISATION
04/03/2009
10 DATE OF REVISION OF THE TEXT
04/12/2014