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CIBIS II - Cardiac Insufficiency Bisoprolol Study (12 Abbildungen)
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Zum ersten Bild Abb. 1: CIBIS II - Cardiac Insufficiency Bisoprolol Study Abb. 2: CIBIS II - Cardiac Insufficiency Bisoprolol Study - Objectives Abb. 3: CIBIS II - Cardiac Insufficiency Bisoprolol Study - Main inclusion criteria Aktuelles Bild - Abb. 4: CIBIS II - Cardiac Insufficiency Bisoprolol Study - Design Abb. 5: CIBIS II - Cardiac Insufficiency Bisoprolol Study - Characteristics (I) Abb. 6: CIBIS II - Cardiac Insufficiency Bisoprolol Study - Characteristics (II) Abb. 7: CIBIS II - Cardiac Insufficiency Bisoprolol Study -Survival Zum letzten Bild
Abbildung 4: CIBIS II - Cardiac Insufficiency Bisoprolol Study - Design
Receptor occupancy detected by an in vitro incubation of plasma samples with a ▀-adrenoceptor preparation allows for a prediction of the relative extent of ▀-adrenoceptor antagonistic effects in man. In this study the time course of plasma concentration after a single oral dose of 100 mg of bisoprolol - a dosage far beyond the therapeutic dose range - was compared with the ▀-adrenoceptor occupancy of the two adrenoceptor subtypes in an ex-vivo/in-vitro assay. 24 hours after the administration of 100 mg bisoprolol, there was no longer any ▀2-adrenoceptor occupancy detected in the plasma samples. Up to that time, plasma levels far exceeded the normal therapeutic range. Therefore an occupancy of the ▀2-receptors is practically not to be expected under therapeutic conditions. 36 to 60 hours after a single oral dose of 100 mg of bisoprolol, plasma concentrations similar to a steady state condition after once daily dosage of 10 mg were found. At an 80 % occupancy of ▀1-receptors, there was no occupancy of ▀2-receptors seen with bisoprolol, whilst under 200 mg of atenolol (slide 4) when there was a maximum occupancy of ▀1-receptors of 80%, 25% of ▀2-receptors were occupied as well. Occupancy of the ▀1-receptors with bisoprolol is in the range of approximately 80-30 % for the therapeutic dose range of 5-10 mg.
 
CIBIS II - Cardiac Insufficiency Bisoprolol Study - Design
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Abbildung 4: CIBIS II - Cardiac Insufficiency Bisoprolol Study - Design
Receptor occupancy detected by an in vitro incubation of plasma samples with a ▀-adrenoceptor preparation allows for a prediction of the relative extent of ▀-adrenoceptor antagonistic effects in man. In this study the time course of plasma concentration after a single oral dose of 100 mg of bisoprolol - a dosage far beyond the therapeutic dose range - was compared with the ▀-adrenoceptor occupancy of the two adrenoceptor subtypes in an ex-vivo/in-vitro assay. 24 hours after the administration of 100 mg bisoprolol, there was no longer any ▀2-adrenoceptor occupancy detected in the plasma samples. Up to that time, plasma levels far exceeded the normal therapeutic range. Therefore an occupancy of the ▀2-receptors is practically not to be expected under therapeutic conditions. 36 to 60 hours after a single oral dose of 100 mg of bisoprolol, plasma concentrations similar to a steady state condition after once daily dosage of 10 mg were found. At an 80 % occupancy of ▀1-receptors, there was no occupancy of ▀2-receptors seen with bisoprolol, whilst under 200 mg of atenolol (slide 4) when there was a maximum occupancy of ▀1-receptors of 80%, 25% of ▀2-receptors were occupied as well. Occupancy of the ▀1-receptors with bisoprolol is in the range of approximately 80-30 % for the therapeutic dose range of 5-10 mg.
 
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