UMLS:C0085580 - FACTA Search

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Query: UMLS:C0085580 (essential hypertension)
14,686 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Celiprolol is a beta 1-selective adrenoceptor antagonist (beta-blocker) which acts as a weak agonist at beta 2-adrenoceptors. The drug demonstrates vasodilator properties and does not depress heart rate to the same extent as propranolol, atenolol or metoprolol. Celiprolol has shown equivalent antihypertensive efficacy to other beta-blockers, notably propranolol, atenolol, metoprolol and pindolol, in patients aged 18 to 75 years with mild to moderate essential hypertension. The drug has also shown similar antihypertensive efficacy to the angiotensin converting enzyme inhibitor enalapril and to combination diuretic therapy with hydrochlorothiazide and amiloride. Celiprolol was equally effective in adult patients of all ages, although no data are available for patients aged over 75 years. Data from a small number of clinical trials indicate celiprolol to be as effective as both propranolol and atenolol in improving work capacity and reducing the frequency of anginal attacks in patients with stable effort angina. However, the drug has not yet been evaluated in postmyocardial infarction patients. Celiprolol offers advantages over other beta-blockers, including reduction of peripheral vascular resistance and maintenance of resting heart rate, cardiac output and renal perfusion. The drug is also associated with improvements in plasma lipid profiles and does not appear to adversely affect carbohydrate metabolism or lung function, although its use in patients with reversible obstructive pulmonary disease is not recommended. Celiprolol is therefore a highly cardioselective beta-blocker with ancillary characteristics which are potentially useful in patients with hypertension and angina complicated by other conditions commonly associated with advanced age. These include impaired glucose tolerance or diabetes mellitus, peripheral vascular disease and hyperlipidaemia. The drug may also be preferred to other beta-blockers in patients in whom a reduction in heart rate would be particularly undesirable. Further long term (> 12 months) clinical trials and pharmacoeconomic data are now required to confirm the clinical relevance of the pharmacodynamic advantages of celiprolol therapy.
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PMID:Celiprolol. An evaluation of its pharmacological properties and clinical efficacy in the management of hypertension and angina pectoris. 857 93

We assessed the effects of 6 months of treatment with an angiotensin-converting enzyme (ACE) inhibitor (cilazapril) or a beta 1-adrenergic blocker (atenolol) on aortic stiffness in essential hypertension. Forty patients (16 women) aged 47 +/- 9 years (mean +/- SD) with baseline systolic and diastolic blood pressures of 162 +/- 15 and 105 +/- 5 mm Hg, respectively, were entered into a double-blind, parallel-group study with cilazapril, 5 mg once daily, or atenolol, 100 mg once daily. The treatment period was preceded by a 4-week placebo washout phase. Aortic elastic modulus (Ep) was determined by cine magnetic resonance imaging (MRI) and indirect brachial artery blood pressure measurements prior to and after 3 weeks and 6 months of therapy. The reductions in systolic and diastolic blood pressures from baseline to 6 months averaged -17 +/- 13 and -10 +/- 6 mm Hg, respectively, with cilazapril and -23 +/- 16 and -14 +/- 6 mm Hg with atenolol. Concomitantly, Ep of the ascending aorta decreased with cilazapril from a median of 2,234 10(3)dyn/cm2 (interquartile range, 866-3,740) to 868 10(3)dyn/cm2 (515-1,486) and with atenolol from a median of 1,611 10(3)dyn/cm2 (895-2,790) to 1,054 10(3)dyn/cm2 (616-1,860). In repeated-measurements analysis of variance, the change in Ep with time was statistically significant (p < 0.001) but the group x time interaction was not. We conclude that 6 months of treatment with either cilazapril or atenolol reduces the stiffness of the ascending aorta in essential hypertension. No statistically significant differences between the effects of the two drugs were observed. The mechanisms and clinical significance of improved aortic distensibility with antihypertensive therapy deserve further study.
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PMID:Effects of angiotensin-converting enzyme inhibition versus beta-adrenergic blockade on aortic stiffness in essential hypertension. 865 66

In the present study, we studied angiotensin II type 1 (AT1) and type 2 (AT2) receptor messengers by quantitative reverse transcriptase-polymerase chain reaction. We examined peripheral blood mononuclear cells from 30 healthy subjects and 50 subjects with primary hypertension, in whom angiotensin I-converting enzyme genotype was determined, before and after 15 days of treatment with different antihypertensive drugs. The medication included a calcium channel antagonist, an angiotensin I-converting enzyme inhibitor, and a beta 1-blocker. We also studied the relationship between AT1 receptor gene expression and biochemical parameters of the renin-angiotensin system. AT1 receptor messenger levels were positively correlated with plasma renin activity in both normotensive and untreated hypertensive subjects. Increases of this messenger and plasma angiotensin II levels were correlated with the D allele in the same individuals. AT1 receptor messenger levels decreased significantly with angiotensin I-converting enzyme inhibitor treatment in subjects with the DD genotype, and a significant decrease was observed in subjects with the II and ID genotypes treated with a calcium antagonist. No changes were observed in mRNA with the beta 1-blocker. We conclude that the AT2 receptor is not expressed in peripheral leukocytes and that AT1 receptor messenger levels vary in relation to angiotensin I-converting enzyme genotype and pharmacological treatment. These results suggest that angiotensin I-converting enzyme genotype may be an important factor when deciding on antihypertensive therapy in individuals with primary hypertension.
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PMID:Angiotensin I-converting enzyme genotypes and angiotensin II receptors. Response to therapy. 867 71

Recent studies have shown an enhanced signaling capacity of receptors coupled to pertussis toxin (PTX)-sensitive guanine nucleotide-binding proteins (G proteins) in immortalized B lymphoblasts from patients with essential hypertension. In the present study, we analyzed (1) whether such alterations would also be expressed in nontransformed cells of these individuals and (2) whether other G protein-mediated signaling pathways were also altered. Therefore, we established primary cultures of skin fibroblasts from previously characterized normotensive and hypertensive individuals (NT and HT cells, respectively). [Ca2+]i rises induced by lyso-phosphatidic acid (LPA), thrombin, and sphingosine-1-phosphate as well as the formation of inositol 1,4,5-trisphosphate and [3H]thymidine incorporation evoked by LPA were PTX sensitive and enhanced twofold in HT fibroblasts. In contrast, cellular responses induced by bradykinin, endothelin-1, and angiotensin II (all PTX insensitive) were similar in NT and HT cells. Formation of cAMP induced by stimulation of Gs with isoproterenol was identical in NT and HT cells. Western blot analysis yielded no evidence for an overexpression of G alpha i2, G alpha i3, G beta 2, and G beta 4. Furthermore, sequencing of cDNAs encoding for the ubiquitously expressed PTX-sensitive G protein subunits G alpha i2, G alpha i3, G beta 1, and G beta 2 from NT and HT cell lines yielded no evidence for mutations in these genes. Although the molecular mechanisms remain to be defined, these data support the concept of a selective enhancement of signal transduction via PTX-sensitive G proteins in essential hypertension.
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PMID:Selectively enhanced cellular signaling by Gi proteins in essential hypertension. G alpha i2, G alpha i3, G beta 1, and G beta 2 are not mutated. 888 89

The submitted review draws attention to advantages and pitfalls of the use of betablockers in the treatment of arterial hypertension. Despite certain metabolically adverse effects which are reduced to a minimum in small doses and more recent betablockers, the latter are along with diuretics the only antihypertensive agents where unequivocally the the long-term favourable effect on the general and cardiovascular mortality was proved. In other hypertensive agents results are expected after completion of multicentric studies which are underway. Beta-blockers, as monotherapy or combined with other drugs, are the drug of choice in the treatment of essential hypertension in young hypertonic patients with hyperkinetic circulation, a tendency for tachycardia, in hypertonic patients with ischaemic heart disease after myocardial infarction or with angina pectoris. In these subjects they quite obviously reduce the general as well as cardiovascular mortality, sudden death and myocardial re-infarction. Betablockers are effective also in elderly hypertonic patients where preparations with ISA or beta 1-selective preparations are more useful. With a certain amount of care similar types of beta-blockers or beta-blockers with a dual effect can be used in hypertension associated with diabetes mellitus, hyperlipoproteinaemia or ischaemia of the lower extremities. Beta-blockers are irreplaceable among antihypertensives of first choice and are experiencing their revival being effective, safe, cheap and well tolerated antihypertensive drugs. Their other properties such as the degree of selectivity, the presence of internal sympathetic activity, combined dual effect, lipophilic or hydrophilic character, enable us to indicate different preparations "tailored" with regard to the severity of hypertension, organ complications and associated diseases.
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PMID:[Do beta-blockers have a role in the modern treatment of arterial hypertension?]. 892 15

Carvedilol competitively blocks beta 1, beta 2 and alpha 1 receptors. The drug lacks sympathomimetic activity and has vasodilating properties that are exerted primarily through alpha 1-blockade. Animal models indicate that carvedilol confers protection against myocardial necrosis, arrhythmia and cell damage caused by oxidising free radicals, and the drug has no adverse effects on plasma lipid profiles. Recent data have confirmed the antihypertensive efficacy of carvedilol in patients with mild to moderate essential hypertension. Carvedilol has similar efficacy to other beta-blocking agents, calcium antagonists, ACE inhibitors and hydrochlorothiazide. Carvedilol also improves exercise tolerance and ischaemic symptoms in patients with stable angina pectoris. Significant reductions in serious cardiac events after acute myocardial infarction and in frequency and severity of ischaemic events in patients with unstable angina have also been demonstrated. Interest in the use of carvedilol in patients with congestive heart failure (CHF) has culminated in the publication of a cumulative analysis of data from 1094 patients with mild to severe CHF who participated in the US Carvedilol Heart Failure Study Program (4 trials). After a median follow-up of 6.5 months, a significant overall reduction in mortality relative to placebo (3.2 vs 7.8%) was revealed in patients who had received carvedilol 6.25 to 50 mg twice daily (plus diuretics and ACE inhibitors). All-cause mortality, risk of hospitalisation for cardiovascular reasons and hospitalisation costs were also reduced significantly (by 65, 28% and 62%, respectively) in these trials. In addition, the Australia and New Zealand Heart Failure Research Collaborative Group showed a 26% reduction in the combined risk of death or hospitalisation with carvedilol 12.5 to 50 mg/day relative to placebo after a mean 19-month follow-up period in 415 patients with CHF (relative risk 0.74). Adverse events with carvedilol appear to be less frequent than with other beta-blocking agents, are dosage-related and are usually seen early in therapy. Events most commonly reported are related to the vasodilating (postural hypotension, dizziness and headaches) and the beta-blocking (dyspnoea, bronchospasm, bradycardia, malaise and asthenia) properties of the drug. Carvedilol appears to date to have little effect on the incidence of worsening heart failure. Concomitant administration of carvedilol with some medications requires monitoring. Carvedilol is therefore likely to have a beneficial role in the management of controlled CHF, but further clinical studies are required to show the place of beta-adrenoceptor blocking therapy in general in this indication, and the position of carvedilol relative to other similar agents. Carvedilol is also confirmed as effective in the management of mild to moderate hypertension and ischaemic heart disease.
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PMID:Carvedilol. A reappraisal of its pharmacological properties and therapeutic use in cardiovascular disorders. 921 Oct 87

In this study we examined the effects of long-term treatment of 19 patients with primary hypertension with the beta 1-adrenoceptor antagonist atenolol on norepinephrine and epinephrine kinetics, at rest and during sympathoadrenal stimulation by lower body negative pressure. Norepinephrine and epinephrine kinetics were measured by using the radioisotope-dilution technique by steady-state infusion of tritiated norepinephrine and epinephrine. The patients were studied before and at the end of 3 months of treatment with atenolol (50 or 100 mg daily). A control group of four normotensive subjects was studied before and after 3 months without any drug treatment. In this group, only arterial blood samples were collected without infusion of the tritiated catecholamines. Atenolol decreased blood pressure and heart rate, but forearm vascular resistance was not affected by atenolol. During atenolol, baseline arterial plasma epinephrine decreased from 0.23 +/- 0.02 to 0.17 +/- 0.01 nM (p < 0.05), and this was accompanied by a decrease in total body epinephrine spillover from 0.50 +/- 0.05 to 0.35 +/- 0.04 nmol/min (p < 0.05). In the control group, arterial plasma epinephrine had not decreased after 3 months. In addition, the increment of arterial plasma epinephrine during lower body negative pressure at -40 mm Hg was attenuated during atenolol. Atenolol had no effect on total body and forearm norepinephrine spillover rates, either at rest or during lower body negative pressure. Clearance rates of epinephrine and norepinephrine were not significantly affected by atenolol. These results suggest that treatment of patients with primary hypertension with the beta 1-adrenoceptor blocker atenolol inhibits the adrenomedullary secretion of epinephrine, but it does not affect the biochemical indices of sympathoneural activity. It remains speculative whether this selective effect of atenolol on epinephrine secretion contributes to its hypotensive action and to its cardioprotective effects in the long term.
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PMID:Long-term beta 1-adrenergic blockade restores adrenomedullary activity in primary hypertension. 930 Mar 18

The dose dependence of the antihypertensive effect of the beta 1 selective blocker talinolol (CAS 57460-41-0, Cordanum) was investigated in 97 essential hypertensive patients (mild to moderate) using the ambulatory blood pressure monitoring (ABPM) in a single-centre, double-blind, randomized parallel-group study. After 4 weeks of treatment a comparison was made between the once daily administered doses of 50, 100 and 200 mg as well as with placebo. The primary parameter was the mean diastolic blood pressure between 8.00 and 22.00 (dTMW). Furthermore, the duration of action of the once daily administration of 200 mg talinolol was compared with the twice daily application of 100 mg each. With regard to dTMW an increasing antihypertensive effect was determined for the dosage step from 50 mg to 100 mg talinolol/d. No further increase in the blood pressure lowering effect was observed with 200 mg talinolol/d. The highest frequency of therapy responders was found in the 100 mg group with 72.2%. Moreover it could be demonstrated, that within the dosage range of 1 x 100-200 mg Talinolol/d a significant and 24 h lasting reduction of blood pressure and pulse rate was achieved, including the early morning period. There were no differences between the blood pressure profile of the 200 mg group and the 2 x 100 mg group at the end of the 4 weeks treatment. All talinolol dosages investigated in this study were proved to be safe and well tolerated. The observed complaints classified as adverse drug reactions represented typical side effects of beta-blockers of mild to moderate intensity. It can be concluded from the results that the once daily intake of talinolol in the dosage range of 100-200 mg/d shows a reliable efficacy in the treatment of essential hypertension accompanied by a noncritical safety profile.
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PMID:[Antihypertensive action of various talinolol dosages after four week's treatment in comparison with placebo]. 955 80

The present study investigated the effect of bisoprolol, a beta 1-selective beta-blocker without intrinsic sympathomimetic activity (ISA), on lipid and glucose metabolism and quality of life (QOL) in elderly patients with essential hypertention. Bisoprolol at doses of 5-10 mg was administered once daily for 12 weeks to 60 non-elderly and 21 elderly outpatients with mild to moderate essential hypertension. In both groups bisoprolol significantly decreased both systolic and diastolic blood pressures and significantly reduced pulse rates to the same extent. The levels of serum cholesterol, HDL-cholesterol and triglyceride, and the response of plasma glucose and insulin to 75 g oral glucose load, were not changed in either group by the bisoprolol treatment. Bisoprolol significantly improved QOL in both groups. Bradycardia, a side effect attributable to bisoprolol, was noted in only one patient in the elderly group. These results suggest that bisoprolol is a safe and useful antihypertensive drug in elderly and non-elderly patients with essential hypertension.
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PMID:[Effect of bisoprolol, a beta 1-selective beta-blocker, on lipid and glucose metabolism and quality of life in elderly patients with essential hypertension]. 956 39

The present study investigated the effect of the new ACE-inhibitor moexipril versus the beta 1-adrenergic blocker atenolol on metabolic parameters, adverse events (AEs) and sitting systolic (SSBP) and sitting diastolic blood pressure (SDBP) in obese postmenopausal women with hypertension (stage I and II). After a 4-week placebo run-in phase, 116 obese, postmenopausal women with primary hypertension were randomised into two treatment groups receiving once daily dosages of either moexipril 7.5 mg or atenolol 25 mg initially (mean age: 57 +/- 7 years in both groups; mean weight: 94 kg in the moexipril group and 89 kg in the atenolol group, corresponding to a body mass index (BMI) of 35.2 kg/m2 and 34.1 kg/m2 in both groups, respectively). After 4 and 8 weeks, the dosages were uptitrated to moexipril 15 mg, or if necessary to moexipril 15 mg/hydrochlorothiazide (HCTZ) 25 mg, or to atenolol 50 mg and atenolol 50 mg/HCTZ 25 mg, in patients whose blood pressure was not sufficiently controlled. At endpoint, metabolic parameters (total cholesterol, triglycerides, LDL, HDL, glucose, insulin) were not significantly altered in either treatment group. Most frequent adverse events under monotherapy (moexipril/atenolol) were asthenia (5.3/13.0%), headache (13.2/21.7%), cough (7.9/6.5%), pharyngitis (21.1/8.7%) and peripheral oedema (5.3/13.0%). Overall at least one AE was reported in 66% of the patients treated with moexipril and in 78% of those treated with atenolol. Reduction of SSBP/SDBP at endpoint was 14.7 +/- 1.9/10.0 +/- 1.1 and 8.7 +/- 1.9/8.4 +/- 1.1 mmHg after treatment with moexipril and atenolol, respectively. The results showed that moexipril and atenolol are equally effective in reducing blood pressure without adversely affecting blood lipids and carbohydrate metabolism.
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PMID:Comparison between moexipril and atenolol in obese postmenopausal women with hypertension. 981 86

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