Disease relevance of BISOPROLOL

• Thus, the primary study end point of death from cardiac causes or nonfatal myocardial infarction occurred in 2 patients in the bisoprolol group (3.4 percent) and 18 patients in the standard-care group (34 percent, P<0.001) [1].
• The combination of low dosages of bisoprolol and hydrochlorothiazide may be a rational alternative to conventional stepped-care therapy for the initial treatment of patients with mild to moderate hypertension [2].
• The Total Ischemic Burden Bisoprolol Study (TIBBS) was a randomized double-blind controlled study with two parallel groups; 330 patients from 30 centers in seven European countries with stable angina pectoris, a positive exercise test and more than two transient ischemic episodes during 48 h of Holter monitoring (central evaluation) were included [3].
• METHODS: Bisoprolol (60 mg/kg body weight per day) was given 30 min or 14 days after MI or sham operation [4].
• Recently, bisoprolol has been investigated regarding its effects on exercise tolerance and the duration of action in patients with coronary heart disease (CHD) following single oral administration [5].

Psychiatry related information on BISOPROLOL

• Bisoprolol-induced rapid eye movement sleep behavior disorder [6].
• Event history analysis revealed that among patients who died under treatment after having at least 1 nonlethal cardiovascular event, 20 patients were treated with placebo but only 7 patients were treated with bisoprolol (RR 0.41; 95% CI 0.17 to 0.98; P <.05) [7].
• Comparative effects of bisoprolol and nitrendipine on exercise capacity in hypertensive patients with regular physical activity [8].
• In conclusion, bisoprolol appeared to be as effective as diazepam in the treatment of cardiac neurosis, but with better effects on somatic symptoms and without affecting patients' psychomotor performance [9].
• Between bisoprolol and bendrofluazide neither in the intention-to-treat nor in the efficacy analysis any difference was found in quality of life variables, such as Health Status Index, somatic symptoms, anxiety, depression, total psychiatric morbidity, cognitive symptoms and hostility score [10].

High impact information on BISOPROLOL

• The effect of bisoprolol on perioperative mortality and myocardial infarction in high-risk patients undergoing vascular surgery. Dutch Echocardiographic Cardiac Risk Evaluation Applying Stress Echocardiography Study Group [1].
• This effect was blocked by both the specific beta 1 blocker bisoprolol and the peptide P0-beta [11].
• METHODS AND RESULTS: In 557 patients studied, bisoprolol significantly reduced heart rate (-16.3+/-15.3 versus -1.6+/-13.4 bpm, respectively; P<.001) compared with placebo at 2 months after inclusion in the study [12].
• CONCLUSIONS: Preservation of left ventricular function appears to play a key role in the bisoprolol-induced beneficial effects on prognosis in heart failure [12].
• The competition by (+/-)bisoprolol (beta 1-selective antagonist) and ICI 118,551 (beta 2-selective antagonist) for [125I](-)iodocyanopindolol binding sites in coronary artery resulted in nonlinear Hofstee plots (beta 1:beta 2 = 90%:10%) [13].

Chemical compound and disease context of BISOPROLOL

• We tested the hypothesis that long-term beta-blocker treatment with bisoprolol prevents creatine kinase (CK) and lactate dehydrogenase system changes that occur after chronic myocardial infarction [14].
• The decrease in total creatine levels after myocardial infarction (74.2 +/- 4.9 vs. 54.9 +/- 3.3 nmol/mg protein, p < 0.05, sham vs. myocardial infarction) was prevented by bisoprolol treatment [14].
• The efficacy and safety of the new cardioselective beta-blocker bisoprolol 5 mg and 10 mg once daily in the treatment of angina pectoris was compared with atenolol 100 mg once daily [15].
• In conclusion, bisoprolol 10-20 mg o.d. proved to be as equally effective as nifedipine SR 20-40 mg b.i.d. for the treatment of essential hypertension in the elderly [16].
• Maintenance of sinus rhythm after electrical cardioversion of persistent atrial fibrillation; sotalol vs bisoprolol [17].

Biological context of BISOPROLOL

• Stroke volume index was unchanged in sham rats and in rats with a small to moderate infarct with early or late bisoprolol treatment and increased in rats with a large infarct in the late bisoprolol group [4].
• The systolic blood pressure was higher (P less than 0.05) in the group receiving bisoprolol 5 mg day-1 than in the 10 mg day-1 group [18].
• The single dose pharmacokinetics of bisoprolol were studied in patients with varying degrees of renal impairment and in healthy controls [19].
• Effects of bisoprolol on local vascular resistance [20].
• Comparison of the effects of two doses of bisoprolol on exercise tolerance in exercise-induced stable angina pectoris [5].

Anatomical context of BISOPROLOL

• Furthermore, catecholamine-induced increases in lymphocyte subsets could be inhibited by pretreatment with the nonselective beta-adrenoceptor antagonist propranolol, but not by the beta1-selective antagonist bisoprolol [21].
• Blood samples were collected for the determination of thyroid hormones and TSH concentration during L-T4 therapy and after 3 and 6 months of associated L-T4 plus bisoprolol therapy [22].
• Bisoprolol prolongs significantly sinus cycle length, corrected sinus node recovery time, AH interval, cycle length inducing AV-node block, effective and functional refractory periods of the AV-node [23].
• The different action on local vascular resistance in the brachial artery territory could be interpreted as the expression of the high beta 1 selectivity of bisoprolol leaving the vascular beta 2 receptors unopposed, whereas non-selective propranolol acts on both beta-adrenoceptor subtypes [20].
• The study examines intrinsic activity, beta-adrenoceptor-G-protein coupling and beta(1)-selectivity of nebivolol and bisoprolol in human ventricular myocardium [24].

Associations of BISOPROLOL with other chemical compounds

• Carvedilol, and recently, bisoprolol have been shown to reduce mortality in ischemic and nonischemic HF, whereas metoprolol has, to date, improved prognosis only in dilated cardiomyopathy [25].
• METHODS: Twenty patients with coronary artery disease underwent 24-h Holter monitoring for heart rate variability and blood sampling (6 hourly for 24 hours) after three consecutive treatment phases, (firstly with placebo, then bisoprolol, and finally quinapril) [26].
• Three hundred and fifteen patients were randomly allocated to treatment for six months with bisoprolol 5 or 10 mg day-1 or atenolol, 50 mg day-1, in a double-blind, double-dummy parallel group, international multicentre study [18].
• DBP was normalized in 22/28 (79%) patients on bisoprolol and in 24/28 (86%) patients on nifedipine (bisoprolol vs nifedipine: NS) [16].
• Bisoprolol was about 2 times more effective in suppressing isoprenaline-induced increases in LVdP/dtmax than those in heart rate [27].

Gene context of BISOPROLOL

• CYP2D6 metabolized bisoprolol stereoselectively (R > S), whereas the metabolism of bisoprolol by CYP3A4 was not stereoselective [28].
• In contrast, CYP2D6 genotype did not affect plasma concentrations of bisoprolol and the extent of its beta-adrenergic inhibition [29].
• Therefore, the species difference in the R/S ratio of metabolic clearance for the oxidation of bisoprolol enantiomers (dog > human) is mainly due to the species difference in the stereoselectivity of one of the cytochrome P450 subfamilies (CYP3A) [30].
• The relation between CLcr and the CL/F of bisoprolol was not altered by the CYP2D6 and CYP2C19 genotypes, gender, or age [31].
• They also decreased the in vivo heart beating frequency of mice pretreated with bisoprolol (a beta1-adrenergic receptor antagonist) for 4 min after injection [32].

Analytical, diagnostic and therapeutic context of BISOPROLOL

• Eligible patients were randomly assigned to receive standard perioperative care or standard care plus perioperative beta-blockade with bisoprolol [1].
• CONCLUSIONS: Treatments starting early (30 min) or late (14 days) after coronary artery ligation with bisoprolol increased left ventricular volume in sham rats and in rats with a small infarct but not in rats with a large infarct [4].
• Patients were given 5 or 10 mg bisoprolol once daily for 2 weeks according to a double-blind, randomized cross-over design [5].
• Eighteen patients were prescribed bisoprolol 10 mg once a day for 6 weeks and an exercise test was performed at the end of this period [33].
• Heart rate variability and ischaemia in patients with coronary heart disease and stable angina pectoris; influence of drug therapy and prognostic value. TIBBS Investigators Group. Total Ischemic Burden Bisoprolol Study [34].

References