Anca Dalea *, V. Ghemigian **
* Anca Dalea – Medic Chimimport-export-plurinex SRL
** V. Ghemigian – Chimimport-export-plurinex SRL
Abstract
Bisoprolol is a β1, – selective β-blocker showing a ratio of Ci/β1, to Ci/β2 of 1:75, bisoprolol has no intrinsec β1- s ympathomimetic activity and no membrane – stabilising activity in the dose range relevant for β-receptor blockade. Bisoprolol is removed from the plasma via two equally effective routes of clearance – half dose is metabolised to inactive metabolites in the liver and the other half is excreted as the unchanged substance via the kidneys. Bisoprolol is both a lipophilic adn hydrophilic drug with a degree of metabolisation of 50%. It has a plasma protein binding of 30%. The bioavailability of bisoprolol from film-coated tablets is about 90%, an absorbtion of 90% and an elimination half life of 10 – 12 hours, meaning that bisoprolol can be administered once daily. The daily dosage is 10 mg. Bisoprolol shows only a small negatively inotropic effect and no clinically relevant affinity to the bronchial β2 -receptors not even when plasma levels are at their peak. Bisoprolol generally induces no changes in cholesterol frac tions, triglycerides and it doesn’ t affect the carbohydrate metabolism. Bisoprolol had an antihypertensvie effect in all hyperten sion models investigated, is protecting the myocardium from ischaemia-related damage and is inhibiting the basal and stimulated renin secretion. The TIBBS and TIBBS-follow-up studies demonstrated that in patients with chronic stable angina, the number and duration of transient ischemic episodes as well as the ischemic burden were significantly more reduced than with nifedipine in a slow release formulation.The results of the CIBIS and CIBIS II studies confirm that β-blockers such as bisoprolol should have a firm place in the treatment regimen of CHF, reducing-on top of standard therapy-significantly the mortality in CHF patients.