CONCOR® 5 and CONCOR® 10 film-coated tablets
SCHEDULING STATUS:
PROPRIETARY NAME
(and dosage form):
CONCOR® 5 and CONCOR® 10 film-coated tablets
COMPOSITION:
Each tablet contains 5 mg or 10 mg bisoprolol fumarate (2:1).
Bisoprolol is (±)-1-[[alpha-(2-isopropoxyethoxy)-p-tolyl]oxy]-3-(isopropylamino)-2-propanol fumarate (2:1).
PHARMACOLOGICAL CLASSIFICATION:
A 5.2 Adrenolytics (sympathicolytics).
PHARMACOLOGICAL ACTION:
Bisoprolol is a highly beta1-selective beta-adrenoceptor antagonist w
ith low beta2-receptor affinity. It has no intrinsic sympathomimetic activity nor membrane-stabilising properties. It reduces blood pressure, and by blockade of the cardiac beta1-receptors, it reduces cardiac action, and hence myocardial oxygen demand.
The mechanism of action of beta1-adrenergic blocking agents in hypertension is not clear, but it is known that bisoprolol reduces the heart rate and depresses plasma renin levels.
Bisoprolol is rapidly absorbed after oral administration in man and excreted predominantly via the urine as unaltered substance and metabolites. In man 50% of a dose is metabolised in the liver while the other 50% is eliminated unchanged via the kidneys. None of the metabolites found in man has beta1-receptor blocking action.
In man, the plasma elimination half-life is 10-12 hours, resulting in a duration of action of 24 hours. Because of its moderate hepatic metabolism, it is subject only to a very small hepatic first pass metabolism. Therefore, bisoprolol displays a high bioavailability of 90% after an oral dose.
INDICATIONS:
Concor* is indicated in the management of mild to moderate hypertension and angina pectoris.
CONTRA-INDICATIONS:
Hypersensitivity to bisoprolol.
Particular caution should be exercised with patients suffering from the following: Asthma, bronchitis, chronic respiratory diseases (See Special Precautions), second and third degree heart block, bradycardia less than 50 beats per minute, peripheral vascular disease and Raynaud’s phenomenon.
Uncontrolled cardiac failure excluding that due to hypertrophic obstructive cardiomyopathy.
Not to be used during pregnancy or lactation.
The normal dose should be reduced in elderly patients, or in patients suffering from renal dysfunction.
Patients with metabolic acidosis and sinus bradycardia.
Safety and efficacy in children have not been established.
WARNINGS:
If bisoprolol is to be withdrawn prior to surgery, at least 48 hours should be allowed to elapse between the last dose and anaesthesia. If bisoprolol treatment is to be continued during surgery, care should be taken when using anaesthetic agents such as ether, cyclopropane and trichloroethylene. Vagal dominance, if it occurs, may be corrected with atropine (1-2 mg i.v.).
In the perioperative period it is generally unwise to reduce the dosage to which the patient is accustomed, as there may be danger of aggravation of angina pectoris or of hypertension.
A patient’s normal tachycardiac response to hypovolaemia or blood loss may be obscured during or after surgery. Particular caution should be taken in this regard.
In patients suffering from ischaemic heart disease, treatment should not be discontinued abruptly.
Caution should be taken in prescribing bisoprolol with Class 1 antidysrhythmic agents such as disopyramide, myocardial depressants, and inhibitors of AV conduction such as calcium antagonists.
Use with caution in combination with verapamil in patients with impaired ventricular function. This combination should not be given to patients with conduction abnormalities. Neither drug should be administered intravenously within 48 hours of discontinuing the other.
The intravenous administration of calcium antagonists and antiarrhythmic agents is not recommended during bisoprolol therapy.
Caution should be exercised when transferring a patient from clonidine. The withdrawal of clonidine may result in the release of large amounts of catecholamines, which may give rise to a hypertensive crisis. If beta-blockers are administered in these circumstances, the unopposed alpha receptor stimulation may potentiate this effect. If a beta-blocker and clonidine are given concurrently, the clonidine should not be discontinued until several days after the withdrawal of the beta-blocker, as severe rebound hypertension may occur.
Bisoprolol modifies the tachycardia of hypoglycaemia. The dosage of bisoprolol should be adjusted in cases of severe renal function impairment.
Pregnancy: Administration to pregnant mothers shortly before giving birth or during labour result in the newborn infant being born hypotonic, collapsed or hypoglycaemic.
