Land: Sør-Afrika
Språk: engelsk
Kilde: South African Health Products Regulatory Authority (SAHPRA)
Merckp
CONCOR® 5 and CONCOR® 10 film-coated tablets SCHEDULING STATUS: S3 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 beta 1 -selective beta-adrenoceptor antagonist with low beta 2 -receptor affinity. It has no intrinsic sympathomimetic activity nor membrane-stabilising properties. It reduces blood pressure, and by blockade of the cardiac beta 1 -receptors, it reduces cardiac action, and hence myocardial oxygen demand. The mechanism of action of beta 1 -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 beta 1 -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, bronchit Les hele dokumentet