BISOPROLOL FUMARATE

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 function (creatinine clearance <20ml/min) or liver function, the dose should not exceed 10mg bisoprolol once daily.

Experience of the use of bisoprolol in renal dialysis patients is limited, however, there is no evidence that the dosage regimen needs to be altered.

Elderly:

No dosage adjustment is normally required but 5mg per day may be adequate in some patients; as for other adults, dosage may have to be reduced in cases of severe renal or hepatic dysfunction.

Children:

There is no paediatric experience with bisoprolol, therefore its use cannot be recommended for children.

Method of administration:

For oral administration.

Blood and Lymphatic Disorders:

Thrombocytopenia, purpura.

Psychiatric Disorders:

Depression, hallucinations, psychoses, confusion, sleep disturbances, nightmares.

Nervous System Disorders:

Fatigue, headaches, impotence, dizziness, paraesthesia of the extremities.

Eye Disorders:

Visual disturbances, dry eyes, keratoconjunctivitis.

Cardiac disorders:

Bradycardia, slowed AV-conduction or increased existing AV- block, heart failure.

Vascular Disorders:

Hypotension, postural hypotension (with syncope), cold and cyanotic extremities, increased existing intermittent claudication, Raynaud’s phenomenon.

Respiratory, Thoracic and Mediastinal Disorders:

Dyspnoea, bronchospasm.

Gastrointestinal Disorders:

Nausea, vomiting, anorexia, diarrhoea, pancreatitis, abdominal pain/discomfort.

Skin and Subcutaneous Tissue Disorders:

Allergic rash, urticaria, exacerbation of psoriasis, photosensitivity. Hypersensitivity reactions (such as itching, flush, rash and angioedema) Reproductive System and Breast Disorders: impotence.

Other:

An increase in ANA (antinuclear antibodies) has been seen; its clinical relevance is not clear.

In patients with ischaemic heart disease, sudden withdrawal of beta-adrenoceptor blocking drugs may result in anginal attacks of increased frequency or severity. Therefore, withdrawal of bisoprolol in patients with ischaemic heart disease should be gradual.

If necessary at the same time replacement therapy should be initiated to prevent exacerbation of angina. Particular care is required with patients whose cardiac reserve is poor. Beta- adrenoceptor blocking drugs should be avoided in overt heart failure, although they may be used when cardiac failure has been controlled.

A reduction in heart rate is a pharmacological effect of bisoprolol. In rare cases where symptoms may be attributable to the slow heart rate, the dose should be reduced. Due to negative effects on conduction time, beta-blockers should only be given with caution to patients with first degree heart block.

Cardiac failure due to thyrotoxicosis may respond to bisoprolol alone, but if other adverse factors are also present it is important to control signs of failure with cardiac glycosides and diuretics. The symptoms of thyrotoxicosis may be masked in patients taking bisoprolol.

Bisoprolol modifies the tachycardia of hypoglycaemia and it may prolong the hypoglycaemic response to insulin. Care should be exercised during concomitant use of bisoprolol and hypoglycaemic therapy in patients with diabetes mellitus.

Hepatic function will deteriorate in patients with portal hypertension and hepatic encephalopathy may develop. It has been suggested that treatment with bisoprolol may increase the risk of developing hepatic encephalopathy. Beta-blockers should be used with great caution in patients with peripheral circulatory disorders (Raynaud’s disease/syndrome, intermittent claudication) as they may aggravate such disorders.

Care should be taken in prescribing beta-blockers to patients with a known risk of recurrence of psoriasis. Care is required when transferring patients from clonidine to a beta-adrenoceptor blocking drug. If the two drugs are given concurrently, clonidine should not be discontinued until several days after the withdrawal of the beta-adrenoceptor blocking drug.

Patients with: • uncontrolled cardiac failure. • cardiogenic shock. • sinoatrial block. • second or third degree AV block. • marked bradycardia (heart rate less than 50 beats/min). • extreme hypotension. • Sick sinus syndrome • Prinzmetal’s (variant) angina.

• severe peripheral vascular disease (Raynaud’s disease or syndrome, intermittent claudication). g. cyclopropane and trichlorethylene). • untreated phaeochromocytoma. • a history of bronchospasm, bronchial asthma or chronic obstructive airways disease.

• metabolic acidosis (eg in some diabetics). • after prolonged fasting. 1).