Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0948265 (metabolic syndrome)
 24,271 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Rilmenidine is an antihypertensive agent with selectivity for I1 imidazoline receptors that acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine provides antihypertensive efficacy comparable with that of diuretics, beta-blockers, calcium channel blockers, and angiotensin-converting enzyme (ACE) inhibitors. Experience from trials and clinical practice highlights rilmenidine's clinical and metabolic acceptability in hypertensive populations, including those at special risk because of old age, renal impairment, diabetes mellitus, or dyslipidemia. In the at-risk hypertensive, rilmenidine reduces left ventricular hypertrophy to a similar degree to other reference agents. New studies show a significant improvement in glucose metabolism in metabolic syndrome patients treated with rilmenidine, and a significant reduction in microalbuminuria during rilmenidine treatment of hypertensive type 2 diabetics. Thus the efficacy/tolerance ratio of rilmenidine supports its role as a first-line antihypertensive option for all groups of hypertensive patient, with specific advantages in some at-risk populations.
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PMID:Rilmenidine: a clinical overview. 1092 29

Centrally acting imidazoline I(1)-receptor agonists such as moxonidine and rilmenidine induce peripheral sympathoinhibition via the stimulation of hypothetical I(1)-receptors in the rostral ventrolateral medulla. Because of a rather weak affinity for alpha(2)-adrenoceptors, the use of these agents is associated with a lower incidence of adverse reactions, such as sedation and dry mouth, compared with classic centrally acting alpha(2)-adrenoceptor agonists (clonidine, guanfacine, methyldopa). The antihypertensive efficacy of moxonidine and rilmenidine is well documented, and they display a favorable hemodynamic profile. Their tolerability is better than that of the aforementioned centrally acting antihypertensive agents. However, long-term outcome data for moxonidine and rilmenidine are not available, and neither is a quantitative evaluation of their adverse effects. There exists some uncertainty with respect to the identity of the imidazoline I(1)-receptor, which has so far not been cloned. Furthermore, it would be desirable to develop highly selective I(1)-receptor agonists as successor drugs to moxonidine and rilmenidine. Although available data indicate that I(1)-receptor agonists are effective in patients with hypertension, comparative data versus agents such as beta-blockers, diuretics, calcium channel antagonists and ACE inhibitors are required to establish their position in the treatment of hypertension. Finally, I(1)-receptor agonists have potential in the treatment of patients with CHF and those with the metabolic syndrome; syndrome X.
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PMID:Centrally acting imidazoline I1-receptor agonists: do they have a place in the management of hypertension? 1472 14

Insulin resistance plays an important role in the pathogenesis of metabolic syndrome and hence an improvement of insulin resistance is important in the treatment of metabolic syndrome. Oral hypoglycemic agents such as thiazolidinediones and biguanides improve glycemic control by reducing insulin resistance. Furthermore, it has been clarified that they also have anti-dyslipidemic, anti-hypertensive and anti-atherosclerotic actions. In addition, such an insulin sensitizing effect has been demonstrated when alpha-glucosidase inhibitors, statins, fibrates and hypotensive agents such as ACE inhibitors, calcium channel blockers and ARBs have been given to patients with insulin resistance. These drugs should be used for each patient on the basis of the underlying diseases, in addition to a lifestyle modification.
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PMID:[Total care for patients with metabolic syndrome]. 1520 58

Diuretic antihypertensive therapy is recommended as first choice by many guidelines, often in combination with beta-blockers. However, such recommendations are based on relatively short-term trials, whereas treatment for hypertension is often a lifetime process. A meta-analysis of seven studies in 58,010 individuals, showed that the 'new' therapies, namely angiotensin-converting enzyme (ACE) inhibitors, angiotensin II type 1 receptor blockers (ARBs) and calcium channel blockers (CCBs) provoke less new diabetes than the conventional 'old' therapies (diuretics and beta-blockers). ACE inhibitors/ARBs decreased new diabetes by 20% (P < 0.001), whereas CCBs decreased new diabetes by 16% (P < 0.001). The number needed to treat for approximately 4 years by new rather than old conventional therapy to avoid one case of new diabetes is about 60-70. Other factors contributing to increased coronary risk are increased metabolic syndrome, blood lipid changes and hypokalaemia. It is not certain whether it is the new therapy that provides protection against new diabetes or the conventional therapy that precipitates new diabetes. However, when compared with placebo, ACE inhibition by ramipril or by the ARB, candesartan, both decrease the incidence of new diabetes, raising the hypothesis that these agents actually prevent the changes leading to insulin resistance, possibly by lessening the adverse effects of angiotensin II on the endothelium. Conversely, lipid abnormalities with conventional treatment could exert adverse effects on the endothelium. Therefore endothelial changes could help to explain the benefits of 'modern' treatment compared with the defects of conventional therapy.
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PMID:Old antihypertensives and new diabetes. 1536 50

Diabetes and hypertension frequently coexist, and their combination provides additive increases in the risk of life-threatening cardiovascular events. Recent guidelines agree on the need for early, aggressive reduction of blood pressure, with a goal of <130/80 mmHg, in patients with diabetes. The mechanism that underpins the increased sensitivity of diabetic subjects to hypertension is not known, but may involve impaired autoregulation or attenuated nocturnal decrease of blood pressure. All classes of antihypertensive agents are effective in reducing blood pressure in diabetic subjects, and all show evidence of a concomitant reduction in cardiovascular risk. Although there is some evidence that agents that interrupt the renin-angiotensin system (RAS) provide greater protective effects, the data are not conclusive. However, most diabetic subjects will require combination therapy to reach goal blood pressure. Antihypertensive drugs can also significantly influence the probability that otherwise healthy individuals will develop metabolic syndrome or type 2 diabetes. While diuretics and betablockers have a prodiabetic effect, angiotensin-converting enzyme inhibitors and angiotensin II receptor blockers may prevent diabetes more effectively than the metabolically neutral calcium channel blockers. Given that diabetes is an important cardiovascular risk factor, there is the potential for reductions in risk due to reduced blood pressure to be offset by an increased risk due to the development of diabetes. Such concerns should be considered in the selection of antihypertensive therapy.
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PMID:The association of hypertension and diabetes: prevalence, cardiovascular risk and protection by blood pressure reduction. 1586 15

Insulin resistance and central obesity are often associated with hypertension. The metabolic syndrome is a cluster of these common clinical disorders, and is related with an increased risk for cardiovascular diseases. A number of pro-inflammatory cytokines derived from adipose tissues have been thought to contribute to the development of insulin resistance and accelerated atherosclerosis. Among them, TNF-alpha has been most widely studied; it not only suppresses the insulin signaling, but also elicits vascular inflammation. Indeed, inhibition of TNF-alpha was found to improve insulin resistance in obese rats and reduce the progression of atherosclerosis in apolipoprotein E knockout mice, respectively. These observations demonstrate that TNF-alpha could play a central role in the pathogenesis of insulin resistance and accelerated atherosclerosis in the metabolic syndrome. Considering that the primary goals of treatment for hypertensive patients with the metabolic syndrome are prevention of the development of diabetes and cardiovascular events, anti-hypertensive drugs that have abilities to block the TNF-alpha signaling would be desirable as a first-line therapy for these patients. In the process of the search for such a unique anti-hypertensive drug, we have recently found that azelnidipine, a newly developed and commercially used long-acting dihydropyridine-based calcium antagonist (DHP), inhibited TNF-alpha-induced activator protein-1 activation and interleukin-8 expression in human umbilical vein endothelial cells by suppressing NADPH oxidase-mediated reactive oxygen species generation. The concentration of azelnidipine that was found effective in these in vitro-experiments is well within the therapeutic range. Since endothelial cells do not possess voltage-operated L-type calcium channels, these observations suggest that the beneficial effects of azelnidipine are not likely due to calcium channel blocking property, but due to its unique anti-oxidative ability. Furthermore, we have very recently found that serum levels of monocyte chemoattractant protein-1, a biomarker for subclinical atherosclerosis, were significantly decreased by the treatment of azelnidipine in patients with essential hypertension. In this paper, we would like to hypothesize that due to its unique TNF-alpha signal modulatory, anti-oxidative property, azelnidipine may be a promising DHP that targets diabetes and cardiovascular diseases in hypertensive patients with the metabolic syndrome.
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PMID:Unique atheroprotective property of azelnidipine, a dihydropyridine-based calcium antagonist. 1589 34

Calcium channel blockers have been widely used in clinical practice because of their antihypertensive capacity. Prevention of renal damage is a very important aim of antihypertensive therapy. This is particularly so taking into account the high prevalence of chronic kidney disease (CKD) in the general population. Recent data have shown that CKD is related to the absence of adequate BP control and also to the clustering of other cardiovascular risk factors seen in the metabolic syndrome. The knowledge of the capacities of the different antihypertensive drugs or their combinations to simultaneously control BP while protecting the kidney and avoiding the facilitation of metabolic alterations is warranted. Recent data from the Intervention as a Goal in Hypertension Treatment trial, Antihypertensive and Lipid-Lowering Treatment to Prevent Heart Attack Trial, and African American Study of Kidney Disease and Hypertension (AASK) allow the conclusion that in hypertensive patients with preserved renal function or with CKD, calcium channel blockers are effective antihypertensive drugs to be considered alone or in combination with an angiotensin-converting enzyme inhibitor or an angiotensin receptor blocker.
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PMID:Calcium channel blockers and renal protection: insights from the latest clinical trials. 1593 37

The number of an elderly patient who has hypertension with diabetes mellitus has been increasing year by year since the life style of people has become Americanized in our country. Metabolic syndrome is characterized by hypertension, dyslipidemia, central adiposity and insulin resistance. It is recently recognized as the high risk for the macrovascular disease such as cerebral infarction and acute myocardial infarction. In diabetic patients, to prevent the life-threatening event or slow complications intensive blood pressure control is as efficacious as good glycemic control. The optimal blood pressure level to reduce hypertension-related morbidity and mortality in diabetic elderly has been proposed 130/80 mmHg in JSH 2004. The blood pressure level in the elderly should be lowered very slowly with careful monitoring of systemic ischemia. Early use of antihypertensive drug combinations is gaining favor. As the first step therapy would be recommended angiotensin receptor blocker, angiotensin-converting enzyme inhibitor and sustained release calcium channel blocker. Especially in the elderly, good control of life-style related diseases would be achieved through a team effort comprising the clinician, psychologist, nurse, pharmacologist, dietitian, other professionals and the patient's family. Comprehensive geriatric assessment can facilitate the maintenance of drug compliance for well control of blood pressure level.
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PMID:[Management of hypertension with diabetes mellitus in the elderly]. 1594 90

The metabolic syndrome is a constellation of interrelated abnormalities that increase the risk for cardiovascular disease and progression to type 2 diabetes. The prevalence of this syndrome is increasing because of the 'obesity epidemic'. The National Cholesterol Education Program Adult Treatment Panel III defined practical criteria for the diagnosis of the metabolic syndrome and established the basic principles for its management. Also, the International Diabetes Federation recently proposed another definition. The metabolic syndrome is a secondary target for cardiovascular risk reduction. Clinicians should identify individuals with this condition, assess their cardiovascular risk and treat them by an aggressive and multifaceted approach. The most effective therapeutic intervention in patients with the metabolic syndrome should focus on modest weight reduction and regular physical activity. Adoption of a healthier diet and smoking cessation are necessary. Drug therapy may be needed to achieve recommended goals if therapeutic lifestyle changes are not sufficient. Low-density lipoprotein cholesterol is the primary target of therapy (new aggressive goals should be achieved). Statins are probably the drugs of choice. Fibrates and nicotinic acid are also useful options. Hypertension should be managed aggressively probably starting with an inhibitor of the renin-angiotensin system or a calcium channel blocker and adding a low dose of a thiazide diuretic if necessary. Aspirin should be administered if the cardiovascular risk is high. In the future acarbose, metformin, meglitinides and thiazolidinediones may be used in patients with the metabolic syndrome to delay the onset of type 2 diabetes and reduce cardiovascular risk. Such an intense and multifactorial approach is likely to reverse the bad prognosis associated with the metabolic syndrome.
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PMID:Diagnosis and management of the metabolic syndrome in obesity. 1624 14

The metabolic syndrome can be found in approximately one third of patients who do not have diabetes but have primary hypertension. Its presence has been associated with a wide range of traditional and nontraditional cardiovascular risk factors and early signs of cardiovascular and renal damage. Moreover, it was emphasized recently that the metabolic syndrome predicts an increased probability of sustaining a cardiovascular event or dying. In the clinical setting of insulin resistance, attention should be paid to the metabolic side effects of antihypertensive drugs; therefore, preference should be given to renin-angiotensin system inhibitors and calcium channel blockers rather than to beta blockers and diuretics.
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PMID:Metabolic syndrome and cardiovascular risk in primary hypertension. 1656 34


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