首页 > 最新文献

Blood pressure. Supplement最新文献

英文 中文
Achieving quality 24-h blood pressure control with candesartan cilexetil. 坎地沙坦西莱地酯实现高质量的24小时血压控制。
Pub Date : 2000-01-01
P Meredith

Epidemiological evidence suggests that optimal blood pressure control requires strategies that lower blood pressure consistently and fully throughout 24 h. In order to maximize compliance, antihypertensive agents also need to be well tolerated and effective when administered at a convenient once-daily dose. The new angiotensin II type 1 (AT1) receptor blocker candesartan binds tightly to, and dissociates slowly from, the AT1-receptor and thereby provides long-lasting suppression of the renin-angiotensin system. This is likely to explain its pronounced antihypertensive efficacy, which is maintained smoothly over 24 h. The trough-to-peak ratio is a useful measure of the persistence of antihypertensive efficacy at the end of the dosing interval. This ratio was found to be close to the ideal of 1.0 for candesartan cilexetil, 8 and 16 mg, whereas it was 0.7 for the prototype AT1-receptor blocker losartan, 50 mg. The antihypertensive effect of candesartan cilexetil, 16 mg, was also significantly greater than that of losartan, 100 mg, as demonstrated by ambulatory blood pressure measurements 0-36 h after dosing and by clinic measurements 48 h after dosing. By controlling blood pressure well beyond the normal dosing interval, candesartan cilexetil provides cardiovascular protection even in those patients who may occasionally miss doses.

流行病学证据表明,最佳的血压控制需要在24小时内持续和完全降低血压的策略。为了最大限度地提高依从性,抗高血压药物也需要具有良好的耐受性,并且在方便的每日一次剂量下有效。新型血管紧张素II型1 (AT1)受体阻滞剂坎地沙坦与AT1受体紧密结合并缓慢解离,从而对肾素-血管紧张素系统提供持久的抑制作用。这很可能解释了其明显的降压效果,在24小时内保持平稳。谷峰比是测量给药间隔结束时降压效果持久性的有用指标。该比率接近于坎地沙坦西列地酯8和16毫克的理想比率1.0,而原型at1受体阻滞剂氯沙坦50毫克的理想比率为0.7。通过给药后0-36小时的动态血压测量和48小时的临床测量,16毫克坎地沙坦西列地尔的降压作用也明显大于100毫克氯沙坦。坎地沙坦西列地尔通过控制血压远远超过正常给药间隔,即使对那些偶尔可能错过给药间隔的患者也能提供心血管保护。
{"title":"Achieving quality 24-h blood pressure control with candesartan cilexetil.","authors":"P Meredith","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Epidemiological evidence suggests that optimal blood pressure control requires strategies that lower blood pressure consistently and fully throughout 24 h. In order to maximize compliance, antihypertensive agents also need to be well tolerated and effective when administered at a convenient once-daily dose. The new angiotensin II type 1 (AT1) receptor blocker candesartan binds tightly to, and dissociates slowly from, the AT1-receptor and thereby provides long-lasting suppression of the renin-angiotensin system. This is likely to explain its pronounced antihypertensive efficacy, which is maintained smoothly over 24 h. The trough-to-peak ratio is a useful measure of the persistence of antihypertensive efficacy at the end of the dosing interval. This ratio was found to be close to the ideal of 1.0 for candesartan cilexetil, 8 and 16 mg, whereas it was 0.7 for the prototype AT1-receptor blocker losartan, 50 mg. The antihypertensive effect of candesartan cilexetil, 16 mg, was also significantly greater than that of losartan, 100 mg, as demonstrated by ambulatory blood pressure measurements 0-36 h after dosing and by clinic measurements 48 h after dosing. By controlling blood pressure well beyond the normal dosing interval, candesartan cilexetil provides cardiovascular protection even in those patients who may occasionally miss doses.</p>","PeriodicalId":8974,"journal":{"name":"Blood pressure. Supplement","volume":"1 ","pages":"23-6"},"PeriodicalIF":0.0,"publicationDate":"2000-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"21888401","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
The role of ambulatory blood pressure monitoring in elderly hypertensive patients. 动态血压监测在老年高血压患者中的作用。
Pub Date : 2000-01-01 DOI: 10.1080/713782692
G. Mancia, G. Parati
There is strong evidence that ambulatory blood pressure measurements show only limited agreement with blood pressures measured in the clinic ("office" blood pressures), and are more relevant to the prognosis of hypertension. Several markers of end-organ damage, for example, have been shown to correlate more strongly with 24-h blood pressure than with office blood pressure. In addition, end-organ damage has been shown to be correlated with 24-h blood pressure variability. Ambulatory blood pressure monitoring (ABPM) has revealed a number of differences between the blood pressure profiles of elderly and younger patients. Since 24-h blood pressure control is now widely accepted as an important goal of antihypertensive therapy, ABPM has a potentially useful role in monitoring treatment in clinical trials in elderly patients.
有强有力的证据表明,动态血压测量与诊所测量的血压(“办公室”血压)只有有限的一致性,并且与高血压的预后更相关。例如,一些终末器官损伤的标志已被证明与24小时血压的相关性比与办公室血压的相关性更强。此外,终末器官损伤已被证明与24小时血压变异性相关。动态血压监测(ABPM)揭示了老年和年轻患者血压谱之间的许多差异。由于24小时血压控制现在被广泛接受为抗高血压治疗的一个重要目标,ABPM在老年患者的临床试验中具有潜在的有用作用。
{"title":"The role of ambulatory blood pressure monitoring in elderly hypertensive patients.","authors":"G. Mancia, G. Parati","doi":"10.1080/713782692","DOIUrl":"https://doi.org/10.1080/713782692","url":null,"abstract":"There is strong evidence that ambulatory blood pressure measurements show only limited agreement with blood pressures measured in the clinic (\"office\" blood pressures), and are more relevant to the prognosis of hypertension. Several markers of end-organ damage, for example, have been shown to correlate more strongly with 24-h blood pressure than with office blood pressure. In addition, end-organ damage has been shown to be correlated with 24-h blood pressure variability. Ambulatory blood pressure monitoring (ABPM) has revealed a number of differences between the blood pressure profiles of elderly and younger patients. Since 24-h blood pressure control is now widely accepted as an important goal of antihypertensive therapy, ABPM has a potentially useful role in monitoring treatment in clinical trials in elderly patients.","PeriodicalId":8974,"journal":{"name":"Blood pressure. Supplement","volume":"32 1","pages":"12-6"},"PeriodicalIF":0.0,"publicationDate":"2000-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86992649","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 6
The 1999 WHO-ISH Guidelines for the Management of Hypertension--new targets, new treatment and a comprehensive approach to total cardiovascular risk reduction. 1999年世卫组织- ish高血压管理指南——全面降低心血管风险的新目标、新治疗方法和综合方法。
Pub Date : 1999-01-01
L Hansson, T Hedner, A Himmelmann
{"title":"The 1999 WHO-ISH Guidelines for the Management of Hypertension--new targets, new treatment and a comprehensive approach to total cardiovascular risk reduction.","authors":"L Hansson,&nbsp;T Hedner,&nbsp;A Himmelmann","doi":"","DOIUrl":"","url":null,"abstract":"","PeriodicalId":8974,"journal":{"name":"Blood pressure. Supplement","volume":"1 ","pages":"3-5"},"PeriodicalIF":0.0,"publicationDate":"1999-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"21268821","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
1999 World Health Organization--International Society of Hypertension Guidelines for the Management of Hypertension. Guidelines Sub-Committee. 1999年世界卫生组织——国际高血压学会高血压管理指南。指南小组委员会。
Pub Date : 1999-01-01
{"title":"1999 World Health Organization--International Society of Hypertension Guidelines for the Management of Hypertension. Guidelines Sub-Committee.","authors":"","doi":"","DOIUrl":"","url":null,"abstract":"","PeriodicalId":8974,"journal":{"name":"Blood pressure. Supplement","volume":"1 ","pages":"9-43"},"PeriodicalIF":0.0,"publicationDate":"1999-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"21268822","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
The 1999 WHO-ISH Guidelines for the Management of Hypertension--new targets, new treatment and a comprehensive approach to total cardiovascular risk reduction. 1999年世卫组织- ish高血压管理指南——全面降低心血管风险的新目标、新治疗方法和综合方法。
Pub Date : 1999-01-01 DOI: 10.1080/080370599439733-1
L. Hansson, T. Hedner, A. Himmelmann
The 1999 WHO-ISH Guidelines for the Management of Hypertension--newtargets, new treatment and a comprehensive approach to totalcardiovascular risk reduction [editorial]
1999年世卫组织高血压管理指南——降低心血管总风险的新目标、新治疗和综合方法[社论]
{"title":"The 1999 WHO-ISH Guidelines for the Management of Hypertension--new targets, new treatment and a comprehensive approach to total cardiovascular risk reduction.","authors":"L. Hansson, T. Hedner, A. Himmelmann","doi":"10.1080/080370599439733-1","DOIUrl":"https://doi.org/10.1080/080370599439733-1","url":null,"abstract":"The 1999 WHO-ISH Guidelines for the Management of Hypertension--newtargets, new treatment and a comprehensive approach to totalcardiovascular risk reduction [editorial]","PeriodicalId":8974,"journal":{"name":"Blood pressure. Supplement","volume":"28 8","pages":"3-5"},"PeriodicalIF":0.0,"publicationDate":"1999-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"91502495","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 23
The pharmacological properties of lipophilic calcium antagonists. 亲脂性钙拮抗剂的药理学性质。
Pub Date : 1998-01-01
P A van Zwieten

Several types of calcium antagonists (CA) (verapamil, diltiazem, nifedipine and related drugs) may be used as antihypertensives. In practice, the dihydropyridines (nifedipine and related drugs) are the CA used most frequently as antihypertensives. Apart from the lowering of blood pressure CA may lead to other, theoretically beneficial, effects: regression of left ventricular and vascular hypertrophy, renal protection, weak natriuretic, weak antiplatelet, anti-ischaemic and antiatherogenic activity. Several new dihydropyridine CA have been introduced in recent years. The advantages of the newer compounds, such as amlodipine, felodipine, isradipine, lacidipine and lercanidipine, may include: vasoselectivity, hence little or no cardiodepressant activity; an improved kinetic profile, resulting in a slow onset and long duration of action, fewer side-effects such as reflex tachycardia and headache, owing to the slow onset of the antihypertensive action. For a few newer CA a predominant effect on specialized circulatory beds (renal, coronary and cerebral) has been claimed. The new CA, which are clearly lipophilic, deserve special attention. Owing to the lipophilic character of such compounds considerable concentration occurs in lipid-containing membrane depots. The CA thus concentrated are slowly released from these depots and, subsequently, reach their targets, the L-type calcium channels. This phenomenon explains both the slow onset and the long duration of action of these CA. Owing to the slow onset of action reflex tachycardia is virtually absent. The long duration of action allows satisfactory control of blood pressure in hypertensives by means of a single daily dose. A few lipophilic dihydropyridine CA are vasoselective. This property implies that at therapeutic, vasodilatory dosages no cardiodepressant activity occurs. Lercanidipine is a recently introduced example of a lipophilic and vasoselective dihydropyridine CA. It is an effective vasodilator/antihypertensive drug, with a slow onset and long duration of action, which is associated with neither reflex tachycardia nor cardiodepressant activity. Other examples of recently introduced lipophilic CA are lacidipine, barnidipine and manidipine.

几种类型的钙拮抗剂(CA)(维拉帕米,地尔硫卓,硝苯地平及相关药物)可用于降压药。在实践中,二氢吡啶类药物(硝苯地平及相关药物)是最常用的抗高血压药物。除了降低血压外,CA还可能导致其他理论上有益的作用:左心室消退和血管肥大、肾保护、弱利钠、弱抗血小板、抗缺血和抗动脉粥样硬化活性。近年来介绍了几种新的二氢吡啶类CA。较新的化合物,如氨氯地平、非洛地平、伊地平、拉西地平和莱卡尼地平的优点可能包括:血管选择性,因此很少或没有心脏抑制剂活性;改善的动力学特征,导致起效缓慢,作用持续时间长,较少的副作用,如反射性心动过速和头痛,由于起效缓慢的降压作用。一些较新的CA主要作用于专门的循环床(肾、冠状动脉和脑)。新的CA显然是亲脂性的,值得特别注意。由于这些化合物的亲脂性,在含脂膜库中会出现相当大的浓度。这样被浓缩的钙离子缓慢地从这些钙离子库中释放出来,随后到达它们的目标——l型钙离子通道。这一现象解释了这些CA发病缓慢和作用持续时间长的原因。由于动作发病缓慢,反射性心动过速几乎不存在。作用持续时间长,可以通过每日一次剂量的方法满意地控制高血压患者的血压。少数亲脂性二氢吡啶CA具有血管选择性。这一特性表明,在治疗性的血管扩张剂量下,没有发生心脏抑制活性。来卡尼地平是最近引进的一种亲脂性和血管选择性的二氢吡啶类CA。它是一种有效的血管扩张剂/降压药,起效慢,持续时间长,与反射性心动过速和心脏抑制活性无关。最近引入的亲脂性CA的其他例子是拉西地平,巴尼地平和曼尼地平。
{"title":"The pharmacological properties of lipophilic calcium antagonists.","authors":"P A van Zwieten","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Several types of calcium antagonists (CA) (verapamil, diltiazem, nifedipine and related drugs) may be used as antihypertensives. In practice, the dihydropyridines (nifedipine and related drugs) are the CA used most frequently as antihypertensives. Apart from the lowering of blood pressure CA may lead to other, theoretically beneficial, effects: regression of left ventricular and vascular hypertrophy, renal protection, weak natriuretic, weak antiplatelet, anti-ischaemic and antiatherogenic activity. Several new dihydropyridine CA have been introduced in recent years. The advantages of the newer compounds, such as amlodipine, felodipine, isradipine, lacidipine and lercanidipine, may include: vasoselectivity, hence little or no cardiodepressant activity; an improved kinetic profile, resulting in a slow onset and long duration of action, fewer side-effects such as reflex tachycardia and headache, owing to the slow onset of the antihypertensive action. For a few newer CA a predominant effect on specialized circulatory beds (renal, coronary and cerebral) has been claimed. The new CA, which are clearly lipophilic, deserve special attention. Owing to the lipophilic character of such compounds considerable concentration occurs in lipid-containing membrane depots. The CA thus concentrated are slowly released from these depots and, subsequently, reach their targets, the L-type calcium channels. This phenomenon explains both the slow onset and the long duration of action of these CA. Owing to the slow onset of action reflex tachycardia is virtually absent. The long duration of action allows satisfactory control of blood pressure in hypertensives by means of a single daily dose. A few lipophilic dihydropyridine CA are vasoselective. This property implies that at therapeutic, vasodilatory dosages no cardiodepressant activity occurs. Lercanidipine is a recently introduced example of a lipophilic and vasoselective dihydropyridine CA. It is an effective vasodilator/antihypertensive drug, with a slow onset and long duration of action, which is associated with neither reflex tachycardia nor cardiodepressant activity. Other examples of recently introduced lipophilic CA are lacidipine, barnidipine and manidipine.</p>","PeriodicalId":8974,"journal":{"name":"Blood pressure. Supplement","volume":"2 ","pages":"5-9"},"PeriodicalIF":0.0,"publicationDate":"1998-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"20759582","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Sympathetic control of circulation in hypertension and congestive heart failure. 高血压和充血性心力衰竭的交感神经循环控制。
Pub Date : 1998-01-01
A Lanfranchi, D Spaziani, G Seravalle, C Turri, R Dell'Oro, G Grassi, G Mancia

Adrenergic overactivity is a common hallmark of both essential hypertension and congestive heart failure. Indirect and direct measures of sympathetic function have clearly shown that sympathetic activation characterizes essential hypertension. This adrenergic overactivity appears to be related to the severity of the hypertensive state, being detectable in its early stages and showing a progressive increase with the severity of the disease. Essential hypertension is also associated with an impaired baroreflex control of vagal activity, whereas baroreceptor modulation of sympathetic nerve traffic remains unaltered, although undergoing a resetting phenomenon. In contrast, secondary hypertension is not associated with an increased adrenergic activity, thus suggesting that an enhancement in efferent sympathetic outflow is a peculiar feature of essential hypertension. Congestive heart failure is a condition also characterized by sympathetic activation, whose degree is proportional to the clinical severity of the disease. This is paralleled by an impairment in arterial baroreceptor modulation of both vagal and sympathetic activity, thus suggesting that the adrenergic overactivity in congestive heart failure is triggered by a reduced afferent restraint on the vasomotor centre. Chronic angiotensin-converting enzyme inhibition reduces the degree of both sympathetic activation and baroreflex dysfunction occurring in heart failure patients, a finding which documents that the neurohumoral abnormalities can be at least partially reversed by pharmacologic treatment.

肾上腺素能亢进是原发性高血压和充血性心力衰竭的共同标志。交感神经功能的间接和直接测量清楚地表明,交感神经激活是原发性高血压的特征。这种肾上腺素能过度活动似乎与高血压状态的严重程度有关,在其早期阶段可检测到,并随着疾病的严重程度而逐渐增加。原发性高血压也与迷走神经活动的压力反射控制受损有关,而交感神经交通的压力感受器调节虽然经历了重置现象,但仍未改变。相反,继发性高血压与肾上腺素能活性增加无关,因此表明传出交感神经流出增强是原发性高血压的特有特征。充血性心力衰竭也是一种以交感神经激活为特征的疾病,其程度与疾病的临床严重程度成正比。这与迷走神经和交感神经活动的动脉压力感受器调节的损伤是平行的,因此表明充血性心力衰竭的肾上腺素能过度活动是由血管舒缩中枢传入抑制减少引起的。慢性血管紧张素转换酶抑制降低了心力衰竭患者交感神经激活和压力反射功能障碍的程度,这一发现证明神经体液异常至少可以通过药物治疗部分逆转。
{"title":"Sympathetic control of circulation in hypertension and congestive heart failure.","authors":"A Lanfranchi,&nbsp;D Spaziani,&nbsp;G Seravalle,&nbsp;C Turri,&nbsp;R Dell'Oro,&nbsp;G Grassi,&nbsp;G Mancia","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Adrenergic overactivity is a common hallmark of both essential hypertension and congestive heart failure. Indirect and direct measures of sympathetic function have clearly shown that sympathetic activation characterizes essential hypertension. This adrenergic overactivity appears to be related to the severity of the hypertensive state, being detectable in its early stages and showing a progressive increase with the severity of the disease. Essential hypertension is also associated with an impaired baroreflex control of vagal activity, whereas baroreceptor modulation of sympathetic nerve traffic remains unaltered, although undergoing a resetting phenomenon. In contrast, secondary hypertension is not associated with an increased adrenergic activity, thus suggesting that an enhancement in efferent sympathetic outflow is a peculiar feature of essential hypertension. Congestive heart failure is a condition also characterized by sympathetic activation, whose degree is proportional to the clinical severity of the disease. This is paralleled by an impairment in arterial baroreceptor modulation of both vagal and sympathetic activity, thus suggesting that the adrenergic overactivity in congestive heart failure is triggered by a reduced afferent restraint on the vasomotor centre. Chronic angiotensin-converting enzyme inhibition reduces the degree of both sympathetic activation and baroreflex dysfunction occurring in heart failure patients, a finding which documents that the neurohumoral abnormalities can be at least partially reversed by pharmacologic treatment.</p>","PeriodicalId":8974,"journal":{"name":"Blood pressure. Supplement","volume":"3 ","pages":"40-5"},"PeriodicalIF":0.0,"publicationDate":"1998-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"21190886","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
The new calcium antagonist lercanidipine and its enantiomers affect major processes of atherogenesis in vitro: is calcium entry involved? 新型钙拮抗剂莱卡尼地平及其对映异构体在体外影响动脉粥样硬化的主要过程:是否涉及钙的进入?
Pub Date : 1998-01-01 DOI: 10.1080/080370598438997
A Corsini, M R Accomazzo, M Canavesi, A Sartani, R Testa, A L Catapano, R Fumagalli, R Paoletti, F Bernini

Atherosclerosis results from multiple factors and involves several mechanisms, including endothelial monocyte and smooth muscle cell (SMC) changes, cholesterol accumulation, plaque rupture and thromboembolism. Calcium ions play a role in the initial and chronic development of atherosclerotic lesions. Several studies in experimental animal models have demonstrated the potential direct antiatherosclerotic effects of calcium antagonists. In this study the antiatherogenic activity of lercanidipine, a new lipophilic, second-generation calcium antagonist, was investigated. Lercanidipine and its enantiomers inhibited the replication and migration of arterial myocytes in concentrations ranging from 10 to 50 microM. The antiproliferative effect of lercanidipine was dose dependent, with a potency similar to that of lacidipine and nifedipine, and was unrelated to the stereoselectivity of enantiomers to bind L-type calcium channels. Lercanidipine and its enantiomers (25 microM) decreased the serum-induced elevation of [Ca2+]i in SMC, with the (S)-enantiomer (69% inhibition) being 2.4-fold more active than the (R)-counterpart (29% inhibition). The studies performed with enantiomers of lercanidipine suggest that the observed effects are not related to the blockade of voltage-dependent Ca2+ channels and confirm, at least in vitro, the pharmacological potential of the compound to influence negatively the process of atherogenesis.

动脉粥样硬化是由多种因素引起的,涉及多种机制,包括内皮单核细胞和平滑肌细胞(SMC)的改变、胆固醇积累、斑块破裂和血栓栓塞。钙离子在动脉粥样硬化病变的初始和慢性发展中起作用。在实验动物模型中进行的几项研究表明,钙拮抗剂具有潜在的直接抗动脉粥样硬化作用。在这项研究中,研究了雷卡尼地平的抗动脉粥样硬化活性,一种新的亲脂性,第二代钙拮抗剂。利卡尼地平及其对映体在10 ~ 50 μ m浓度范围内抑制动脉肌细胞的复制和迁移。雷卡尼地平的抗增殖作用具有剂量依赖性,其效价与拉西地平和硝苯地平相似,与对映体结合l型钙通道的立体选择性无关。莱卡尼地平及其对映体(25微米)降低了SMC中血清诱导的[Ca2+]i升高,(S)-对映体(69%的抑制)比(R)-对映体(29%的抑制)活性高2.4倍。对莱卡尼地平的对构异体进行的研究表明,观察到的效果与电压依赖性Ca2+通道的阻断无关,并证实,至少在体外,该化合物的药理学潜力对动脉粥样硬化过程产生负面影响。
{"title":"The new calcium antagonist lercanidipine and its enantiomers affect major processes of atherogenesis in vitro: is calcium entry involved?","authors":"A Corsini,&nbsp;M R Accomazzo,&nbsp;M Canavesi,&nbsp;A Sartani,&nbsp;R Testa,&nbsp;A L Catapano,&nbsp;R Fumagalli,&nbsp;R Paoletti,&nbsp;F Bernini","doi":"10.1080/080370598438997","DOIUrl":"https://doi.org/10.1080/080370598438997","url":null,"abstract":"<p><p>Atherosclerosis results from multiple factors and involves several mechanisms, including endothelial monocyte and smooth muscle cell (SMC) changes, cholesterol accumulation, plaque rupture and thromboembolism. Calcium ions play a role in the initial and chronic development of atherosclerotic lesions. Several studies in experimental animal models have demonstrated the potential direct antiatherosclerotic effects of calcium antagonists. In this study the antiatherogenic activity of lercanidipine, a new lipophilic, second-generation calcium antagonist, was investigated. Lercanidipine and its enantiomers inhibited the replication and migration of arterial myocytes in concentrations ranging from 10 to 50 microM. The antiproliferative effect of lercanidipine was dose dependent, with a potency similar to that of lacidipine and nifedipine, and was unrelated to the stereoselectivity of enantiomers to bind L-type calcium channels. Lercanidipine and its enantiomers (25 microM) decreased the serum-induced elevation of [Ca2+]i in SMC, with the (S)-enantiomer (69% inhibition) being 2.4-fold more active than the (R)-counterpart (29% inhibition). The studies performed with enantiomers of lercanidipine suggest that the observed effects are not related to the blockade of voltage-dependent Ca2+ channels and confirm, at least in vitro, the pharmacological potential of the compound to influence negatively the process of atherogenesis.</p>","PeriodicalId":8974,"journal":{"name":"Blood pressure. Supplement","volume":"2 ","pages":"18-22"},"PeriodicalIF":0.0,"publicationDate":"1998-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1080/080370598438997","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"20759584","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 12
Consequences of the increased autonomic nervous drive in hypertension, heart failure and diabetes. 高血压、心力衰竭和糖尿病患者自主神经驱动增强的后果。
Pub Date : 1998-01-01 DOI: 10.1080/080370598438410-1
S Julius, M Valentini

It is estimated that 40 million people in the USA have hypertension, 14 million are diabetic and 4 million suffer congestive heart failure. Since all three conditions are age-related, as the longevity in industrialized societies continues to improve, the overall burden of congestive heart failure, hypertension and diabetes will increase. These major diseases of civilization are characteristically associated with an increased autonomic cardiovascular drive. In our terminology the output that emanates from the central nervous system via sympathetic and parasympathetic efferents is referred to as "tone". The overall "drive" depends on the balance between inhibitory (parasympathetic) and excitatory (sympathetic) tone and the organ's responsiveness to that tone. The responsiveness, in turn, depends on the receptors' properties as well as on the intrinsic functional or anatomic properties of the responding organs. These components can change independently. For example, in the course of hypertension the alpha-adrenergic responsiveness increases whereas the beta-adrenergic responses are down-regulated. Another example is: plasma noradrenaline and sympathetic tone are increased in elderly subjects but their circulation does not show any tell-tale response of increased sympathetic tone, presumably because the responses to sympathetic tone decrease with aging. These complex interactions between the autonomic tone and organ responsiveness determine to a great extent the overall clinical impact of the autonomic abnormality in hypertension, non-insulin-dependent diabetes mellitus and in congestive heart failure. The major thesis of this review is that, whether primary or secondary, whether easily discerned or hidden, an enhanced autonomic drive, independent of the underlying condition, greatly increases the risk of poor cardiovascular outcomes. It follows that targeting the underlying autonomic imbalance in congestive heart failure, hypertension and diabetes may not only be pathophysiologically sound but such an approach may also lead to better outcomes.

据估计,美国有4000万人患有高血压,1400万人患有糖尿病,400万人患有充血性心力衰竭。由于这三种疾病都与年龄有关,随着工业化社会的寿命不断提高,充血性心力衰竭、高血压和糖尿病的总体负担将会增加。这些文明的主要疾病都与自主心血管驱动的增加有关。在我们的术语中,由中枢神经系统通过交感神经和副交感神经传出信号发出的输出被称为“音调”。整个“驱动”取决于抑制性(副交感神经)和兴奋性(交感神经)张力之间的平衡以及器官对这种张力的反应。反过来,反应性取决于受体的特性以及反应器官的内在功能或解剖特性。这些组件可以独立更改。例如,在高血压过程中,α -肾上腺素能反应增加,而β -肾上腺素能反应下调。另一个例子是:血浆去甲肾上腺素和交感神经张力在老年受试者中增加,但他们的循环没有显示出交感神经张力增加的任何明显反应,可能是因为交感神经张力的反应随着年龄的增长而减少。自主神经张力和器官反应性之间的复杂相互作用在很大程度上决定了高血压、非胰岛素依赖型糖尿病和充血性心力衰竭患者自主神经异常的总体临床影响。这篇综述的主要论点是,无论是原发性的还是继发性的,无论是容易识别的还是隐藏的,自主驱动的增强,独立于潜在的条件,大大增加了不良心血管结局的风险。因此,针对充血性心力衰竭、高血压和糖尿病的潜在自主神经失衡,不仅在病理生理学上是合理的,而且这种方法也可能导致更好的结果。
{"title":"Consequences of the increased autonomic nervous drive in hypertension, heart failure and diabetes.","authors":"S Julius,&nbsp;M Valentini","doi":"10.1080/080370598438410-1","DOIUrl":"https://doi.org/10.1080/080370598438410-1","url":null,"abstract":"<p><p>It is estimated that 40 million people in the USA have hypertension, 14 million are diabetic and 4 million suffer congestive heart failure. Since all three conditions are age-related, as the longevity in industrialized societies continues to improve, the overall burden of congestive heart failure, hypertension and diabetes will increase. These major diseases of civilization are characteristically associated with an increased autonomic cardiovascular drive. In our terminology the output that emanates from the central nervous system via sympathetic and parasympathetic efferents is referred to as \"tone\". The overall \"drive\" depends on the balance between inhibitory (parasympathetic) and excitatory (sympathetic) tone and the organ's responsiveness to that tone. The responsiveness, in turn, depends on the receptors' properties as well as on the intrinsic functional or anatomic properties of the responding organs. These components can change independently. For example, in the course of hypertension the alpha-adrenergic responsiveness increases whereas the beta-adrenergic responses are down-regulated. Another example is: plasma noradrenaline and sympathetic tone are increased in elderly subjects but their circulation does not show any tell-tale response of increased sympathetic tone, presumably because the responses to sympathetic tone decrease with aging. These complex interactions between the autonomic tone and organ responsiveness determine to a great extent the overall clinical impact of the autonomic abnormality in hypertension, non-insulin-dependent diabetes mellitus and in congestive heart failure. The major thesis of this review is that, whether primary or secondary, whether easily discerned or hidden, an enhanced autonomic drive, independent of the underlying condition, greatly increases the risk of poor cardiovascular outcomes. It follows that targeting the underlying autonomic imbalance in congestive heart failure, hypertension and diabetes may not only be pathophysiologically sound but such an approach may also lead to better outcomes.</p>","PeriodicalId":8974,"journal":{"name":"Blood pressure. Supplement","volume":"3 ","pages":"5-13"},"PeriodicalIF":0.0,"publicationDate":"1998-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1080/080370598438410-1","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"21190294","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 55
Therapy of hypertension and metabolic syndrome: today's standard and tomorrow's perspectives. 高血压和代谢综合征的治疗:今天的标准和明天的观点。
Pub Date : 1998-01-01 DOI: 10.1080/080370598438438
L Hansson

Treatment of arterial hypertension is known to reduce cardiovascular morbidity and mortality and has a positive effect against stroke, where benefit is strongly linked to reduction in blood pressure per se. The protective effects against coronary heart disease (CHD) have also been significant but numerically less impressive than the effect against stroke. It is conceivable that this due to the fact that not just blood pressure, but also a number of metabolic variables need to be considered in this context. The insight that hypertension is often just one of the components of the so-called metabolic syndrome suggests that a modern antihypertensive drug should not only lower blood pressure; to exert optimal cardioprotective properties it should also have a neutral or even positive metabolic profile as regards its effects on lipids, glucose and insulin in order to achieve a better protection against CHD. Against this background the centrally acting selective imidazoline receptor (I1) agonist moxonidine is of considerable interest. Moxonidine has been shown to improve glucose tolerance in man, probably by two different mechanisms, i.e. by augmenting insulin sensitivity in peripheral tissues and by enhancing glucose-stimulated insulin release from the pancreas. By employing a therapeutic intervention against hypertension that not only lowers elevated arterial pressure but also positively affects some of the frequently occurring concomitant metabolic disturbances, it appears that today's standard of antihypertensive therapy may be surpassed in tomorrow's perspective.

众所周知,治疗动脉高血压可降低心血管疾病发病率和死亡率,并对中风有积极作用,其益处与血压本身的降低密切相关。对冠心病(CHD)的保护作用也很显著,但在数字上不如对中风的保护作用令人印象深刻。可以想象,这是因为在这种情况下,不仅需要考虑血压,还需要考虑许多代谢变量。高血压通常只是所谓代谢综合征的一个组成部分,这一见解表明,现代降压药不仅应该降低血压;为了发挥最佳的心脏保护作用,它还应该具有中性甚至是正的代谢特征,就其对脂质,葡萄糖和胰岛素的影响而言,以达到更好的预防冠心病的效果。在这种背景下,中枢作用的选择性咪唑啉受体(I1)激动剂莫昔定引起了相当大的兴趣。莫onidine已被证明可以改善人的葡萄糖耐量,可能是通过两种不同的机制,即通过增加外周组织的胰岛素敏感性和通过增强葡萄糖刺激的胰岛素从胰腺释放。通过对高血压的治疗干预,不仅可以降低升高的动脉压,还可以积极地影响一些经常发生的伴随代谢紊乱,看来今天的降压治疗标准可能在明天被超越。
{"title":"Therapy of hypertension and metabolic syndrome: today's standard and tomorrow's perspectives.","authors":"L Hansson","doi":"10.1080/080370598438438","DOIUrl":"https://doi.org/10.1080/080370598438438","url":null,"abstract":"<p><p>Treatment of arterial hypertension is known to reduce cardiovascular morbidity and mortality and has a positive effect against stroke, where benefit is strongly linked to reduction in blood pressure per se. The protective effects against coronary heart disease (CHD) have also been significant but numerically less impressive than the effect against stroke. It is conceivable that this due to the fact that not just blood pressure, but also a number of metabolic variables need to be considered in this context. The insight that hypertension is often just one of the components of the so-called metabolic syndrome suggests that a modern antihypertensive drug should not only lower blood pressure; to exert optimal cardioprotective properties it should also have a neutral or even positive metabolic profile as regards its effects on lipids, glucose and insulin in order to achieve a better protection against CHD. Against this background the centrally acting selective imidazoline receptor (I1) agonist moxonidine is of considerable interest. Moxonidine has been shown to improve glucose tolerance in man, probably by two different mechanisms, i.e. by augmenting insulin sensitivity in peripheral tissues and by enhancing glucose-stimulated insulin release from the pancreas. By employing a therapeutic intervention against hypertension that not only lowers elevated arterial pressure but also positively affects some of the frequently occurring concomitant metabolic disturbances, it appears that today's standard of antihypertensive therapy may be surpassed in tomorrow's perspective.</p>","PeriodicalId":8974,"journal":{"name":"Blood pressure. Supplement","volume":"3 ","pages":"20-2"},"PeriodicalIF":0.0,"publicationDate":"1998-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1080/080370598438438","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"21190882","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 11
期刊
Blood pressure. Supplement
全部 Acc. Chem. Res. ACS Applied Bio Materials ACS Appl. Electron. Mater. ACS Appl. Energy Mater. ACS Appl. Mater. Interfaces ACS Appl. Nano Mater. ACS Appl. Polym. Mater. ACS BIOMATER-SCI ENG ACS Catal. ACS Cent. Sci. ACS Chem. Biol. ACS Chemical Health & Safety ACS Chem. Neurosci. ACS Comb. Sci. ACS Earth Space Chem. ACS Energy Lett. ACS Infect. Dis. ACS Macro Lett. ACS Mater. Lett. ACS Med. Chem. Lett. ACS Nano ACS Omega ACS Photonics ACS Sens. ACS Sustainable Chem. Eng. ACS Synth. Biol. Anal. Chem. BIOCHEMISTRY-US Bioconjugate Chem. BIOMACROMOLECULES Chem. Res. Toxicol. Chem. Rev. Chem. Mater. CRYST GROWTH DES ENERG FUEL Environ. Sci. Technol. Environ. Sci. Technol. Lett. Eur. J. Inorg. Chem. IND ENG CHEM RES Inorg. Chem. J. Agric. Food. Chem. J. Chem. Eng. Data J. Chem. Educ. J. Chem. Inf. Model. J. Chem. Theory Comput. J. Med. Chem. J. Nat. Prod. J PROTEOME RES J. Am. Chem. Soc. LANGMUIR MACROMOLECULES Mol. Pharmaceutics Nano Lett. Org. Lett. ORG PROCESS RES DEV ORGANOMETALLICS J. Org. Chem. J. Phys. Chem. J. Phys. Chem. A J. Phys. Chem. B J. Phys. Chem. C J. Phys. Chem. Lett. Analyst Anal. Methods Biomater. Sci. Catal. Sci. Technol. Chem. Commun. Chem. Soc. Rev. CHEM EDUC RES PRACT CRYSTENGCOMM Dalton Trans. Energy Environ. Sci. ENVIRON SCI-NANO ENVIRON SCI-PROC IMP ENVIRON SCI-WAT RES Faraday Discuss. Food Funct. Green Chem. Inorg. Chem. Front. Integr. Biol. J. Anal. At. Spectrom. J. Mater. Chem. A J. Mater. Chem. B J. Mater. Chem. C Lab Chip Mater. Chem. Front. Mater. Horiz. MEDCHEMCOMM Metallomics Mol. Biosyst. Mol. Syst. Des. Eng. Nanoscale Nanoscale Horiz. Nat. Prod. Rep. New J. Chem. Org. Biomol. Chem. Org. Chem. Front. PHOTOCH PHOTOBIO SCI PCCP Polym. Chem.
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
0
微信
客服QQ
Book学术公众号 扫码关注我们
反馈
×
意见反馈
请填写您的意见或建议
请填写您的手机或邮箱
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
现在去查看 取消
×
提示
确定
Book学术官方微信
Book学术文献互助
Book学术文献互助群
群 号:481959085
Book学术
文献互助 智能选刊 最新文献 互助须知 联系我们:info@booksci.cn
Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。
Copyright © 2023 Book学术 All rights reserved.
ghs 京公网安备 11010802042870号 京ICP备2023020795号-1