UMLS:C0020538 - FACTA Search

Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts: Target Concepts:

Query: UMLS:C0020538 (hypertension)
170,190 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Bisoprolol is a beta 1-adrenoceptor antagonist with no partial agonist (intrinsic sympathomimetic) activity or membrane stabilising (local anaesthetic) activity. The oral bioavailability of bisoprolol is high (90%) and the drug has a long elimination half-life which allows once-daily administration; in addition, it is hepatically and renally cleared in equal proportions. In non-comparative studies, and comparative trials, bisoprolol proved effective, and as efficacious as atenolol, low doses of metoprolol, diuretics and nifedipine SR in hypertension, and atenolol and verapamil in stable angina pectoris. Bisoprolol has been well tolerated in most patients. Thus, bisoprolol is an effective alternative to other beta-adrenoceptor antagonists in patients with mild to moderate essential hypertension or stable angina pectoris. Furthermore, its unique pharmacokinetic properties may offer advantages in selected patients. However, the results of further comparative studies with established agents in the treatment of hypertension and angina pectoris are still awaited so that a final assessment of the relative place in therapy of bisoprolol in these disease states may be made.
...
PMID:Bisoprolol. A preliminary review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in hypertension and angina pectoris. 290 20

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. Two hundred and ninety-two (175 men and 117 women) were eligible for statistical follow-up. Their mean age was 52.6 years (range 28-70). All patients had a supine diastolic blood pressure of 95-120 mmHg on two occasions during the four weeks of placebo treatment. Twenty-four patients ended the study prematurely and a further 19 had their regimes changed because of an insufficient effect. The reasons for drop-out were similar in the three treatment groups. Thus, 249 patients continued to receive the treatment they were allocated to, with 80, 83 and 86 patients in the three respective groups. The sex and age distributions and the number of previously treated hypertensives were similar in the three groups. At the end of placebo treatment the supine blood pressures in the three groups (bisoprolol 5 or 10 mg day-1 or atenolol 50 mg day-1, respectively) were 163.9/102.5, 157.4/101.8 and 160.0/102.2 mmHg, respectively. 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. After 26 weeks of treatment the supine blood pressures in the three groups were 150.6/90.8, 142.0/89.1 and 148.6/91.7 mmHg, respectively. The largest estimated difference in blood pressure reduction was 4.6/2.3 mmHg between the group receiving bisoprolol 10 mg day-1 and the group receiving atenolol 50 mg day-1. A reduction in mean blood pressure of greater than or equal to 10 mmHg was noted in 66% of the patients in the bisoprolol group (10 mg day-1), in the other groups 66 and 59%, n.s. Bisoprolol is effective, well-tolerated and safe in the treatment of hypertension. A daily dose of 5 mg seems recommendable for the majority of hypertensive patients and seems equipotent with 50 mg day-1 of atenolol in the present study.
...
PMID:Efficacy and safety of bisoprolol and atenolol in patients with mild to moderate hypertension: a double-blind, parallel group international multicentre study. 296 86

This 30-center, randomized, double-blind, placebo-controlled, parallel-group study was designed to (1) establish that 6.25 mg of hydrochlorothiazide (HCTZ) given once daily with 5 mg of bisoprolol fumarate can contribute to antihypertensive effectiveness in patients with stage I and stage II (mild to moderate) systemic hypertension; and (2) assess whether this formulation was more effective or possessed a safety advantage over standard monotherapy with bisoprolol or 25 mg of HCTZ. Results showed that HCTZ 6.25 mg contributed significantly to the antihypertensive effectiveness of bisoprolol 5 mg. Bisoprolol 5 mg/HCTZ 6.25 mg (B5/H6.25) produced significantly greater mean reductions from baseline in sitting systolic and diastolic blood pressure (-15.8 mm Hg/-12.6 mm Hg) than bisoprolol 5 mg alone (-10.0 mm Hg/-10.5 mm Hg) and HCTZ 25 mg alone (-10.2 mm Hg/-8.5 mm Hg). A 73% response rate was achieved with the low-dose formulation compared with 61% for the bisoprolol 5 mg (B5) group and 47% for the HCTZ 25 mg (H25) group. B5/H6.25 was found to be significantly more effective than B5 or H25 in all subgroups of patients, regardless of gender, race, age, or smoking history. Antihypertensive effects were maintained during the 24-hour dosing interval. The incremental effectiveness of B5/H6.25 was not accompanied by an increase in the frequency or severity of adverse experiences; the incidence of adverse experiences in the B5/H6.25 group was comparable to that in the placebo group. B5/H6.25 was shown to provide safety advantages over H25, as shown by less hypokalemia (< 1% with B5/H6.25 versus 6.5% with H25).(ABSTRACT TRUNCATED AT 250 WORDS)
...
PMID:First-line therapy option with low-dose bisoprolol fumarate and low-dose hydrochlorothiazide in patients with stage I and stage II systemic hypertension. 775 30

The antihypertensive effect of daily doses of three beta-adrenoblockers (Bisoprolol, 10 mg once a day, propranolol, 80 mg twice a day, and methoprolol, 100 mg twice a day), and placebo was examined in 14 patients with persistent mild and moderate hypertension during a double blind cross-over study by using 24-hour monitoring of blood pressure and its routine measurements. The latter made by a mercury sphygmomanometer indicated that the antihypertensive and negative chronotropic effect of Bisoprolol in a dose of 10 mg remained 24 hours after its administration and it did not significantly differ from that of the two other agents given in the above doses. The application of 24-hour blood pressure monitoring allows a more pronounced antihypertensive effect of bisoprolol to be revealed during 24 hours than that displayed by the two agents. Bisoprolol is an effective and safe antihypertensive agent.
...
PMID:[The antihypertensive effect of the new cardioselective prolonged-action beta-adrenoblocker bisoprolol compared with propranolol, metoprolol and placebo]. 777 86

It was first reported by our group in 1975 that heart failure due to idiopathic dilated cardiomyopathy (IDC) could be improved by long term treatment with a beta-blocker, starting at a low dose and continuing with a stepwise up-titration. Since then, many studies have been performed in patients with heart failure of various aetiologies and the beneficial effects of long term beta-blockade have been confirmed. About 3000 patients have been included in randomised studies in which beta-blockade, given for more than 2 months, mostly elicited significant improvements in functional class, exercise capacity, cardiac function, quality of life and/or morbidity. When started at a very low dose (one-tenth to one-twentieth of the doses generally used in angina or hypertension), the treatment is well tolerated in most patients. In these studies, various types of beta-blockers were used, including beta1-selective blockers and nonselective blockers with additional properties (vasodilator and antioxidative) such as metoprolol, bisoprolol, bucindolol and carvedilol. Several large studies have also reported benefits on mortality and morbidity. In the Metoprolol in Dilated Cardiomyopathy (MDC) trial, metoprolol treatment in patients with IDC resulted in a 34% reduction of the primary combined endpoint, total number of deaths and need for cardiac transplantation. In the Cardiac Insufficiency Bisoprolol Study (CIBIS), in patients with idiopathic as well as ischaemic cardiomyopathy, there was a nonsignificant 20% reduction in mortality. In the US carvedilol studies (n = 1094), also in patients with ischaemic and idiopathic cardiomyopathy, carvedilol reduced mortality by 65%, which was highly significant. A nonsignificant reduction in mortality was observed in the Australia-New Zealand (ANZ) Heart Failure Study with carvedilol. In all these studies there was a reduction in hospitalisations, with all drugs being generally well tolerated. It can thus be concluded that the beneficial effects of beta-blockers on cardiac function and morbidity have been documented in a large number of studies in selected groups of patients. The treatment has been accepted in some countries by the regulatory authorities. Larger, placebo-controlled studies are needed to convincingly demonstrate a reduction in total mortality as observed in the pooling of the 4 US carvedilol studies. Such studies are in progress for various beta-blockers, which may lead to acceptance of their routine clinical use in patients with congestive heart failure.
...
PMID:The role of beta-blockers in left ventricular dysfunction and heart failure. 933 58

In an open multicenter study, 2,012 patients with mild to moderate essential hypertension were treated for 8 weeks with the beta1-selective blocker bisoprolol. A total of 570 general practitioners participated in this study. A total of 1,597 patients whose resting diastolic blood pressure (DBP) ranged from 95 to 115 mm Hg were considered eligible for this study. Patients received one tablet of bisoprolol (5 mg) o.d. for the first 4 weeks. In patients not responding satisfactorily to treatment, the dose could be increased to 10 mg o.d. for the following 4 weeks. A total of 1,201 patients were evaluated for efficacy and all 2,012 patients were evaluated for tolerability. After 4 weeks of therapy, mean systolic blood pressure (SBP) was lowered significantly from 170+/-15 to 151+/-14 mm Hg, and mean DBP was lowered from 104+/-5 to 92+/-7 mm Hg. A further 4-week treatment lowered the blood pressure even more: mean SBP from 151+/-14 to 144+/-13 mm Hg and mean DBP from 92+/-7 to 88+/-7 mm Hg. The total extent of both SBP and DBP reduction was equal in all age groups and showed no dependency of the initial blood pressure value. At the end of the study. the responder rate was 94.9% in patients aged under 60 years, and 90.6% in patients aged over 60 years. The age group 31-40 years showed the highest responder rate (97.5%). After 8 weeks of treatment, 69.5% of the patients were still on 5 mg of bisoprolol and 27.6% on 10 mg of bisoprolol. Of all 2,012 patients, 11.6% reported side effects such as vertigo, fatigue. gastrointestinal disturbances, and headache. The incidence of adverse drug reactions was highest in the age group 31-40 years. Bisoprolol proved in this study to be an effective and safe antihypertensive agent when given to patients with mild to moderate hypertension for 8 weeks.
...
PMID:Age dependence of therapy result and risk in the treatment of arterial hypertension? 1152 25

There is a small increase in the functional beta2-adrenoceptor response on the spontaneously hypertensive rat (SHR) left atrium in the early stages of hypertension. In the present study, the functional beta1- and beta2-adrenoceptors of the left and right atrium in SHR pre-hypertension and age-matched (5-week-old) Wistar Kyoto (WKY) rats were characterized. Contractility methods with isoprenaline, T-0509 (a selective beta1-adrenoceptor agonist) and procaterol (a selective beta2-adrenoceptor agonist) were used. At 5 weeks, the SHRs were pre-hypertensive. Isoprenaline was more potent on the left atrium of 5-week-old SHRs than WKY rats. Bisoprolol, a selective beta1-adrenoceptor antagonist, was more potent against isoprenaline and T-0509 on the SHR than WKY rat left atrium. ICI 118,551, a selective beta(2)-adrenoceptor antagonist, was more potent against procaterol and T-0509 on the SHR than WKY rat left atrium. The results with bisoprolol and ICI 118,551 suggest that there are more functional beta(1)- and beta(2)-adrenoceptors on the left atrium of 5-week-old SHRs than WKY rats. Isoprenaline, T-0509 and procaterol were equipotent on the right atrium of 5-week-old WKY rats and SHRs. Bisoprolol was more potent against isoprenaline, T-0509 and procaterol on the SHR than WKY rat right atrium. ICI 118,551 was more potent against T-0509, but not isoprenaline and procaterol, on the SHR than WKY rat left atrium. This suggests there are more functional beta1-adrenoceptors, and probably more functional beta2-adrenoceptors, on the right atrium of 5-week-old SHRs than WKY rats. These functional differences in beta1- and beta2-adrenoceptor-mediated responses of the left and right atria of pre-hypertensive SHRs cannot be caused by hypertension, and may be associated with the onset of hypertension.
...
PMID:Functional beta1- and beta2-adrenoceptors in the left and right atrium of pre-hypertensive rats. 1239 4

Previous studies have demonstrated that beta-blockade increases the levels of plasma atrial natriuretic peptide (ANP), but relationships between this effect and the antihypertensive action of beta-blockade remain unknown. In this study we investigated the amplitude and determinants of bisoprolol-induced ANP increase and the relationships between this increase and the antihypertensive effect of bisoprolol. Nineteen patients with mild to moderate hypertension were included in the study. In the first phase of the study (cross-over, placebo controlled, randomized phase), the effects of 10 mg bisoprolol on plasma ANP at rest and during exercise were compared to placebo. The antihypertensive action of bisoprolol was then evaluated after a 2-week period of treatment (10 mg/day) using ambulatory blood pressure monitoring. Bisoprolol significantly increased plasma ANP level at rest (from 30.6 +/- 20.5 to 42.8 +/- 35.6; P < 0.05) and also during exercise (from 54.7 +/- 44.3 to 119.1 +/- 159.9; pg/mL +/- SD; P < 0.05). Plasma ANP at rest was not significantly correlated with left ventricular mass. After the 15 days of treatment, the bisoprolol-induced daytime diastolic blood pressure reduction was significantly correlated to the initial bisoprolol-induced plasma ANP increase (r = 0.49, P = 0.035). These results suggest that the antihypertensive effect of beta-blocking agents could be partly mediated by an increase of ANP release.
...
PMID:Relationships between the antihypertensive effects of bisoprolol and levels of plasma atrial natriuretic peptide in hypertensive patients. 1260 61

Measurement of levels of hormones of the pituitary-gonadal system, dopplerography of penile arteries and questioning after Vasiltchenko were carried out in 30 men (age 35-55 years) with I-II degree arterial hypertension who received monotherapy with bisoprolol and nebivolol for 2 months. Treatment with both superselective beta-adrenoblockers was associated with significant lowering of systolic and diastolic blood pressure and heart rate. Antihypertensive effect of bisoprolol was significantly more pronounced than that of nebivolol. Bisoprolol and nebivolol significantly increased concentration of testosterone (by 82 and 85%, respectively) and prolactin (by 77 and 83%, respectively), lowered levels of estradiol and follicle-stimulating hormone, improved vascular blood flow in penile arteries, and did not worsen sexual function.
...
PMID:[Level of hormones of pituitary-gonadal axis, penile blood flow and sexual function in men with arterial hypertension during monotherapy with bisoprolol and nebivolol]. 1826 Aug 76

In patients with hypertension, beta blockade decreases muscle sympathetic nerve activity (MSNA; micrographic technique) expressed in burst frequency (burst/min) but does not affect MSNA expressed in burst incidence (burst/100 heart beats), because reductions in blood pressure (BP) upon each diastole continue to deactivate the arterial baroreceptors, but at a slower heart rate (HR). We studied the effects of oral beta blockade on MSNA and baroreflex sensitivity (BRS) in normal participants. Bisoprolol (5 mg, 1 week) was administered in 10 healthy young adults, using a double-blind, placebo-controlled, randomized cross-over study design. The beat-to-beat mean RR interval (RR) and systolic blood pressure (SBP) series were analyzed by power spectral analysis and power computation over the very low frequency (VLF), low frequency, and high frequency (HF) bands. Baroreflex sensitivity was computed from SBP and RR cross-analysis, using time and frequency domain methods. Bisoprolol increased RR (P < .0005), decreased mean SBP and diastolic blood pressure values (P < .01), did not change the SBP and RR powers, except for RR power in VLF (P < .02) and SBP power in HF (P < .03). The MSNA variability (P > .13) and respiratory pattern (P = .84) did not change from placebo to bisoprolol condition. The bisoprolol-induced bradycardia was associated with higher burst/100 heart beats (P < .05) and bisoprolol did not affect burst/min (P = .80). Time domain BRS estimates were increased after bisoprolol (P < .05), while frequency domain ones did not change (P > .1). Oral bisoprolol induces differential effects on sympathetic burst frequency and incidence in normal participants. Peripheral sympathetic outflow over time is preserved as a result of an increased burst incidence, in the presence of a slower HR. Unchanged BP and HR and MSNA variability suggests that the larger burst incidence is not due to sympathetic activation.
...
PMID:Differential effects of oral beta blockade on cardiovascular and sympathetic regulation. 1990 82

<< Previous 1 2 3 4 Next >>