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

The authors administered to 10 patients with mild hypertension a single dose of 10 mg bisoprolol (Concor-Merck) during bioimpedance control of changes of the cardiac index and peripheral vascular resistance after an interval of 3 and 24 hours following administration of the drug. In all patients administration of the drug led to a statistically significant drop of the blood pressure. In patients with a high cardiac output (group A, n = 6) the decline of blood pressure was due to a blocked increment of the cardiac output and a slight block of the peripheral vascular resistance. In the group with a low cardiac output and high peripheral vascular resistance (group B, n = 3) the drop of the blood pressure was caused by peripheral vascular dilatation, the cardiac output was influenced minimally. Bisoprolol did not affect the left ventricular systolic function.
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PMID:[The effect of a single dose of Bisoprolol on changes in blood pressure and hemodynamic indicators in patients with mild hypertension]. 148 78

The authors administered to 10 patients with mild hypertension a single dose of 10 mg bisoprolol (CONCOR-Merck) during bioimpedance control of changes of the cardiac index and peripheral vascular resistance during an isometric load after an interval of 3 and 24 hours following administration of the drug. In all patients administration of the drug led during the third hour to a statistically significant drop of the blood pressure after a load. Twenty-four hours after administration the drop was no longer statistically significant. In patients with a high cardiac index (group A, n = 6) the decline of blood pressure was due to a blocked increment of the cardiac output and a slight block of the peripheral vascular resistance. In the group with a low cardiac index and high peripheral vascular resistance (group B, n = 3) the drop of the blood pressure was less marked than in group A and it was due only to the blocked increment of the cardiac output. The increment of the peripheral vascular resistance was not influenced by the preparation. Bisoprolol did not affect the left ventricular systolic function.
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PMID:[The effect of a single dose of Bisoprolol on changes in blood pressure and hemodymic indicators in patients with mild hypertension during loading]. 148 79

In an initial double-blind randomized study with three parallel groups, 48 patients, mean age 49.6 years (32-65 years), with hypertension WHO I-II, were given bisoprolol in doses of 5, 10, and 20 mg. Bisoprolol is a new beta 1-selective beta-blocking agent with a plasma half-life of 10-12 h and without intrinsic sympathomimetic activity (ISA). After the initial 8 weeks, systolic (SBP) and diastolic blood pressure (DBP) and heart rate (HR) measured at rest and during exercise 24 h after last drug intake showed a significant decrease for all three parameters in all three treatment groups. There were no differences in efficacy between the 5 and 10 mg doses of bisoprolol, whereas 20 mg was significantly more effective than both 5 mg (p less than 0.01) and 10 mg (p less than 0.05). After 10 months of treatment with dose adjustments up or down, the reduction of SBP, DBP, and HR at rest and during exercise remained unchanged. One patient had an acute myocardial infarction (AMI) and died during the study; another patient had a car accident in which he got asphyxial cerebral lesions and could not complete the study. Twelve patients spontaneously expressed side effects of the kind normally seen in treatment with beta-blocking agents. Three of them complained of cold hands and feet, and one of them was unable to complete the study. The rest of the adverse effects were mild, and 45 patients completed the long-term study. Laboratory safety tests were normal, and there were no significant changes in the lipoprotein patterns (cholesterol, HDL cholesterol, and triglycerides).(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Dose-effect relationship and long-term effects of bisoprolol in mild to moderate hypertension. 243 80

Forty-two patients (28 men, 14 women, age range 27-65 years) with newly discovered mild to moderate hypertension were randomly allocated to treatment with either bisoprolol or atenolol for a double-blind comparison of these two beta 1-adrenoceptor blocking drugs. Two doses of each drug (10 and 20 mg/d for bisoprolol and 50 and 100 mg/d for atenolol) were given, each dose for a 3-month period, the dose to be given first being decided by random allocation of the patients. During the second 3-month period, the patient received the alternative dose. After treatment for 6 and 12 weeks with each dose, the blood pressure, heart rate, and lipoprotein concentrations were checked. Bisoprolol treatment (both 10 and 20 mg) resulted in a decrease in blood pressure in the supine position from 154/100 to 138/89 mm Hg; and atenolol treatment resulted in decreases from 161/102 to 145/90 mm Hg (50 mg/d) and 146/91 mm Hg (100 mg/d). The drugs and doses did not differ in their effect. The triglyceride content in very low density lipoproteins (VLDL) increased during treatment with bisoprolol (10 mg/d) from 1.04 to 1.31 mmol/l (p less than 0.05); during treatment with atenolol (100 mg/d) it increased from 0.90 to 1.14 mmol/l (p less than 0.05). The cholesterol content in low density lipoproteins did not change, but that in high density lipoproteins (HDL) decreased during treatment with both drugs (from 1.22 to 1.10 mmol/l with bisoprolol 20 mg/d, p less than 0.01: and from 1.21 to 1.13 mmol/l with atenolol 100 mg/d, p less than 0.05).(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:A comparison of the effects of bisoprolol and atenolol on lipoprotein concentrations and blood pressure. 243 83

The antihypertensive effect and possible adverse effects of bisoprolol were assessed in 96 Japanese patients with mild to moderate hypertension. After a 2- to 4-week placebo period, bisoprolol was administered to 68 outpatients at a daily dose of 5 mg to 20 mg for 6 to 8 weeks, and to 28 inpatients with the same dose range up to a maximum of 4 weeks. For outpatients, blood pressure and heart rate were recorded every 2 weeks, while for inpatients, in addition to daily measurements, the effect of bisoprolol on diurnal variation of blood pressure was also studied. Bisoprolol lowered blood pressure and heart rate significantly in both groups of patients. The most common adverse effect was bradycardia. It is expected that bisoprolol will be a very effective and useful antihypertensive drug.
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PMID:Clinical evaluation of bisoprolol in patients with hypertension: interim report. 243 85

Bisoprolol, (+/-)1-(4-[(2-isopropoxyethoxy)-methyl]-phenoxy)-3-isopropyl-amino -2- propanol-hemifumarate, is a new, highly selective beta 1-adrenoceptor blocking agent without intrinsic sympathomimetic activity and low to moderate local anaesthetic activity. As demonstrated in binding experiments, and in classical pharmacological studies using rats, guinea pigs, cats, and dogs, bisoprolol markedly differentiated between beta 1-adrenoceptors of the heart, or the renal juxtaglomerular apparatus, and the beta 2-subtype in arterial blood vessels, bronchi, liver, or skeletal muscle. Up to concentrations nearly 100-fold higher than the therapeutic plasma levels in humans, bisoprolol did not affect the functional refractory period of the heart, and was devoid of a direct suppressive effect on myocardial contractility and of calcium antagonistic properties in heart and vascular muscle. The pattern of haemodynamic effects of bisoprolol was typical of beta-blockers and included decreases in blood pressure (BP), heart rate (HR), and cardiac output, concomitant with an increase in calculated total peripheral resistance. In contrast to other beta-blockers, bisoprolol increased renal blood flow in anaesthetized dogs. Bisoprolol lowered BP in hypertensive dogs and rats, attenuated the development of spontaneous hypertension in rats, decreased plasma renin activity and protected the heart from the sequelae of transient ischemia. It did not block presynaptic beta-adrenoceptors in blood vessels. Serum lipids and the serum lipoprotein profile remained unaltered after bisoprolol. Bisoprolol was devoid of affinity for autonomic receptors other than beta-adrenoceptors or for autacoid receptors. This is probably one of the reasons why bisoprolol did not affect the function of the central nervous, respiratory, and gastrointestinal systems in an obvious way. The high beta 1-selectivity of bisoprolol is linked with extremely favourable pharmacokinetic properties. These include nearly complete enteral absorption and virtual absence of liver first-pass metabolism, both resulting in high bioavailability, long plasma half-life, pharmacokinetics that are linear over a wide dose range and independent of age, food intake and hydroxylator status, low plasma protein binding, and a 1:1 ratio of hepatic metabolization to renal elimination of the unaltered substance. This sum of favourable pharmacological and pharmacokinetic properties characterize bisoprolol as an optimized beta-blocker.
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PMID:High beta 1-selectivity and favourable pharmacokinetics as the outstanding properties of bisoprolol. 243 93

The effects of single doses of 10, 20, and 40 mg of bisoprolol on left ventricular performance were assessed by left ventricular systolic time interval measurements, echocardiographic measurements, and exercise stress tests in patients with mild to moderate arterial hypertension. Bisoprolol caused a significant, dose-dependent fall in systolic and diastolic blood pressure and heart rate, at rest and under exercise stress test. Left ventricular systolic time intervals were prolonged at the higher doses, but pre-ejection period/left ventricular ejection time (PEP/LVET) ratio, as an indicator for left ventricular performance, remained unchanged. Left ventricular echocardiographic dimensions increased significantly, but shortening fraction was not altered. We conclude that 10-40 mg bisoprolol, apart from the blockade of beta 1-adrenoceptors, does not affect left ventricular cardiac function.
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PMID:Noninvasive assessment of left ventricular performance after administration of bisoprolol. 243 6

The aim of this study was to compare the effects of long-term monotherapy with five different beta-blockers on plasma lipids in patients with essential hypertension. We studied 99 male patients, aged 35-55 years, with mild to moderate hypertension, who worked in the same community. After a 1-month placebo period, patients were assigned to receive propranolol (160 mg/day), atenolol (100 mg/day), bisoprolol (10 mg/day), mepindolol (10 mg/day), or celiprolol (400 mg/day). Therapy was continued for 2 years. Blood pressure (BP), heart rate, and blood samples for evaluation of total cholesterol (TC), LDL-cholesterol (LDL-C), triglycerides (TG) and HDL-cholesterol (HDL-C) were taken before and after the initial placebo period, and subsequently every 6 months from the beginning of active treatment. All beta-blockers caused similar reductions in BP that were maintained throughout the study. None of the beta-blockers significantly affected TC or LDL-C. Propranolol, a nonselective beta-blocker, caused the most pronounced changes in TG (+33 to 43%) and in HDL-C (-30 to -32%). Atenolol, a beta 1-selective agent, had the same quantitative effects, but to a lesser extent (TG + 23 to 30%; HDL-C -15 to -19%). Bisoprolol, more beta 1-selective than atenolol, and mepindolol, nonselective with ISA, increased TG (+20 to 28% and +14 to 25%, respectively) but did not significantly affect HDL-C. In contrast, celiprolol, a highly cardioselective beta-blocker with beta 2-partial agonism, improved lipid risk factors by significantly reducing TG (-14 to -21%) and increasing HDL-C (+8 to 14%).(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Plasma lipids during chronic antihypertensive therapy with different beta-blockers. 248 87

A randomized, placebo-controlled, double-blind crossover investigation in 12 patients with non-asthmatic chronic obstructive lung disease and co-existing stable angina pectoris was done to compare two beta 1-selective adrenoceptor blocking agents, atenolol 100 mg and bisoprolol 20 mg. Systolic and diastolic blood pressures (SBP, DBP), heart rate (HR) as well as airway resistance (AWR, and less frequently forced expiratory volume in 1 s (FEV1) and intrathoracic gas volume (ITGV) were measured in the sitting position before and at various times up to 24 h after drug intake. During the first 4 h both beta-blockers produced a significant reduction in HR in comparison to placebo (p less than 0.01). Atenolol 100 mg significantly increased AWR relative to placebo and bisoprolol (p less than 0.05). After 24 h, a significant reduction in HR (p less than 0.01) could only be demonstrated after bisoprolol, whereas atenolol alone led to a significant elevation in AWR relative to placebo and bisoprolol (p less than 0.05) at that time. It is concluded that bisoprolol appears to have a high degree of beta 1-selectivity, thus providing a wide split between beta 1- and beta 2-adrenoceptor blockade. Bisoprolol in its therapeutic dose range is expected to be relatively safe as regards bronchoconstriction in patients suffering both from hypertension and/or angina pectoris and chronic obstructive lung disease.
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PMID:Effects of single oral doses of bisoprolol and atenolol on airway function in nonasthmatic chronic obstructive lung disease and angina pectoris. 287 33

Bisoprolol is a new highly beta 1-selective beta-adrenoceptor blocking drug; it is devoid of intrinsic sympathomimetic effects. Its haemodynamic effects are those expected from beta 1-blockade, heart rate is reduced at rest and on exercise, cardiac output falls and peripherial resistance is increased. Consequent on the beta 1-selectivity there is much greater inhibition of exercise tachycardia compared to inhibition of isoprenaline-induced falls of diastolic blood pressure, in contrast to propranolol. Studies in asthmatics confirm the selectivity of bisoprolol. Bisoprolol has similar solubility in water and organic solvents and predictably therefore about half is excreted by the kidneys unchanged, half metabolized by the liver. Estimates of half-life average about 10-12 h, this is in accord with the therapeutic efficacy of once daily administration. Therapeutic studies have demonstrated the efficacy of bisoprolol in angina pectoris, arrhythmias and hypertension. Comparative studies against atenolol and verapamil in angina suggest similar efficacy. In hypertension a similar antihypertensive effect to nifedipine has been found, while a significantly greater lowering of blood pressure was seen than that obtained with a diuretic. Some studies have also suggested more consistent antihypertensive effect from bisoprolol than atenolol 24 h after administration. This may have been a dosage phenomenon or reflects the longer plasma elimination half-life of bisoprolol, and requires confirmation. Bisoprolol has a favourable side-effect profile.
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PMID:Bisoprolol: a new beta-adrenoceptor blocking drug. 289 95


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