High β1-Selectivity and Favourable Pharmacokinetics as the Outstanding Properties of Bisoprolol

Haeusler, G.; Hj, Schliep; Schelling, Pierre; Kh, Becker; Klockow, Michael; Ko, Minck; Hj, Enenkel; Schulze, Ernst Detlef; Bergmann, Reinhard; Cj, Schmitges

doi:10.1097/00005344-198511001-00002

Cited by 34 publications

(13 citation statements)

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“…6 As the purpose of this study was to compare the efficacy of different AR antagonists in suppressing LV remodeling secondary to hypertension, the prerequisite for a chosen drug is to lower blood pressure to a normal level. The drug doses were determined by referring to previous studies on animal models of LV remodeling [7][8][9][10] and by a preliminary study in which the drug doses were increased gradually from a low dose until the systolic blood pressure (SBP) in each drug-treated group reached the level of SBP as that of WKY rats. Our preliminary results showed that bisoprolol, propranolol and carvedilol at a dose of 2 mg kg À1 per day, 6 mg kg À1 per day and 6 mg/kg/day, respectively, were effective in normalizing SBP in SHR and thus, these doses were finally chosen for comparing the therapeutic effects of bisoprolol, propranolol and carvedilol in suppressing LV remodeling in SHR.…”

Section: Animal Model and Experimental Protocolmentioning

confidence: 99%

Is overall blockade superior to selective blockade of adrenergic receptor subtypes in suppressing left ventricular remodeling in spontaneously hypertensive rats?

et al. 2010

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To test the hypothesis that nonselective blockade of adrenergic receptor (AR) subtypes is superior to selective blockade of AR subtypes in suppressing left ventricular (LV) remodeling induced by hypertension. Sixty-four spontaneously hypertensive rats (SHR) were randomly divided into four groups: bisoprolol-treated, propranolol-treated, carvedilol-treated and no treatment groups (n¼16, each). Sixteen Wistar-Kyoto (WKY) rats served as a control group. Echocardiography and cardiac catheterization were carried out to record the mitral flow velocity ratio of E wave to A wave (E/A), LV mass index (LVMI), maximal rising (dp/dt max ) and falling (Àdp/dt max ) rate of the LV pressure and LV relaxation time constant (s). The mRNA and protein expression levels of AR, protein kinase(PK) and G-protein subtypes, intracellular free calcium (Ca 2+ ) concentration and cardiocyte apoptoisis rate were determined. Three drug-treated groups showed higher velocity ratio of E wave to A wave (E/A) and Àdp/dt max and lower systolic blood pressure (SBP), LVMI, s, apoptosis rate and intracellular free Ca 2+ concentration than the no treatment group. The mRNA expression levels of AR-a 1B in the carvedilol group were significantly lower than the other two drug-treated groups. The mRNA expression levels of AR-b 1 , AR-b 2 and Gsa were significantly higher in the three drug-treated groups than in the no treatment group, with the expression levels of AR-b 2 being the highest in the carvedilol-treated group. The protein expression levels of PKA and PKC subtype a and d were lower in the three drug-treated groups than in the no treatment group. Overall blockade of AR subtypes is not superior to selective blockade of AR subtypes in suppressing LV remodeling in SHR. Although carvedilol is the most effective in attenuating cardiocyte apoptosis, normalizing AR-a 1B and Gsa expression and increasing AR-b 2 expression.

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Section: Animal Model and Experimental Protocolmentioning

confidence: 99%

Is overall blockade superior to selective blockade of adrenergic receptor subtypes in suppressing left ventricular remodeling in spontaneously hypertensive rats?

et al. 2010

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“…With the plasma concentration achieved after 10 mg of bisoprolol only p,-adrenoceptors are occupied, while after 100 mg of atenolol-at least during the first hours after dosing-P,-adrenoceptors are also occupied, indicating superior P1 selectivity of bisoprolol vs. atenolol. The pronounced P,-selectivity of bisoprolol had already been observed in various animal pharmacology investigations (18,24). With respect to the extent of the P,-adrenoceptor selectivity in humans, the following selectivity ratios were demonstrated: bisoprolol, 751 1; atenolol, 351 1; betaxolol, 351 1; and metoprolol, 2011 (53).…”

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confidence: 52%

“…(c) To permit once-a-day treatment, longer-acting P-blockers are preferred in all indications for @-blocker treatment, i.e., particularly in the case of angina pectoris. (d) For pharmacokinetically rational @-blocker treatment of patients with specific pathophysiological conditions, such as impaired renal or hepatic function, a P-blocker that can be cleared both renally and metabolically (hepatically) is preferred.Bisoprolol is a @-blocker without ISA (18,24,30) with pronounced PI selectivity …”

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confidence: 99%

Bisoprolol in Angina Pectoris

Bethge¹,

Léopold²,

Wagner³

1991

Cardiovascular Drug Reviews

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The treatment of angina pectoris caused by coronary artery disease with @-blockers is generally accepted. P-Blockers competitively inhibit the effect of endogenous catecholamines at @-receptors. Reduction in the positive chronotropic and positive inotropic effect of the catecholamines on the myocardium results in a decrease in the myocardial oxygen demand in patients with coronary artery disease, in particular in situations where there is frequently increased catecholamine release. The reduction in the positive bathmotropic effect of the catecholamines can probably explain the antiarrhythmic effect of P-blockers and their protective effect against acute cardiac death.Numerous P-blockers have been introduced into therapy in the last 20 years. Their mode of action in angina pectoris does not differ fundamentally between substances. However, additional pharmacodynamic and pharmacokinetic properties of the individual P-blockers are often of importance in practical therapy: (a) For certain therapeutic aims, for instance reinfarction prophylaxis, P-blockers without intrinsic sympathomimetic activity (ISA) are preferred. (b) For as low-risk treatment as possible of patients with often nondefinitively identified concomitant diseases, such as chronic obstructive bronchitis, a P-blocker with pronounced PI selectivity is desirable. It does not impair the effect of the frequently prescribed P,-agonists, thus having an advantage over nonselective P-blockers where the bronchodilatory effect of the P,-agonist is impaired. (c) To permit once-a-day treatment, longer-acting P-blockers are preferred in all indications for @-blocker treatment, i.e., particularly in the case of angina pectoris. (d) For pharmacokinetically rational @-blocker treatment of patients with specific pathophysiological conditions, such as impaired renal or hepatic function, a P-blocker that can be cleared both renally and metabolically (hepatically) is preferred.Bisoprolol is a @-blocker without ISA (18,24,30) with pronounced PI selectivity

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“…Bisoprolol is considered to have a very satisfactory pharmacokinetic profile [94]; it is well absorbed with low "first pass" metabolism, there is low protein binding, high bioavailability, and balanced renal and hepatic clearance. Doses of bisoprolol and of cetamolol should be reduced in renal failure, because these drugs are eliminated mainly by the kidney (Table 1).…”

Section: Pharmacokineticsmentioning

confidence: 99%