this study was a randomized, multicenter, double-blind, parallel group, Phase III, 8-week clinical trial to compare the superiority of the S-AM/TEL 2.5/40-mg and S-AM/TEL 5/40-mg combinations with TEL 80-mg mono-therapy. The primary end point was the change in the mean sitting diastolic blood pressure from baseline (week 0) after 8 weeks of therapy between treatment groups.
In a prospective double-blind study, patients with hypertension and coronary artery disease were treated with either 40 mg telmisartan (n = 21) or placebo (n = 21) for 12 weeks. General markers of inflammation, such as high-sensitivity C-reactive protein (hs-CRP) and interleukin-6 (IL-6), and cell adhesion molecules, such as soluble intercellular adhesion molecule (s-ICAM-1) and the leucocyte adhesion molecule soluble-L-selectin (sL-selectin), as well as the lymphocytic expression of the beta2 integrin MAC-1, were assessed before and after treatment. Telmisartan therapy significantly decreased the lymphocyte beta2 integrin MAC-1 expression, whereas hs-CRP, IL-6, s-ICAM and sL-selectin remained unaltered. In-vitro experiments were conducted to clarify the mode of action. Cultured human lymphocytes were stimulated with either angiotensin II or phorbol-12-myristate-13-acetate (PMA)/ionomycin, alone or after pretreatment with telmisartan. Whereas angiotensin II exerted no effect on beta2-integrin MAC-1 expression in lymphocytes, telmisartan dose-dependently inhibited beta2-integrin expression in lymphocytes in the absence or presence of angiotensin II.
A robust and sensitive high-performance liquid chromatographic-tandem mass spectrometric (HPLC-MS/MS) assay for the high-throughput quantification of the antihypertensive drug azelnidipine in human plasma was developed and validated following bioanalytical validation guidelines. Azelnidipine and internal standard (IS), telmisartan, were extracted from human plasma by precipitation protein and separated on a C18 column using acetonitrile-methanol-ammonium formate with 0.1% formic acid as mobile phase. Detection was performed on a turbo-spray ionization source (ESI) and mass spectrometric positive multiple reaction monitoring mode (+MRM) using the respective transitions m/z 583.3 → 167.2 for azelnidipine and m/z 515.3 → 497.2 for IS. The method has a wide analytical measuring range from 0.0125 to 25 ng/mL. For the lowest limit of quantitation, low, medium and high quality controls, intra- and interassay precisions (relative standard deviation) were 3.30-7.01% and 1.78-8.09%, respectively. The drug was sufficiently stable under all relevant analytical conditions. The main metabolite of azelnidipine, M-1 (aromatized form), was monitored semiquantitatively using the typical transition m/z 581.3 → 167.2. Finally, the method was successfully applied to a clinical pharmacokinetic study in human after a single oral administration of azelnidipine 8 mg. The assay meets criteria for the analysis of samples from large research trials.
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We examined the effects of telmisartan on cholesterol transport-related proteins (apolipoprotein E [ApoE]/low-density lipoprotein receptor [LDL-R]) and microtubule-associated protein 2 (MAP2) in the brain of spontaneously hypertensive stroke resistant (SHR-SR). SHR-SR received transient middle cerebral artery occlusion (tMCAO) for 90 minutes at 12 weeks of age and then was divided into 3 experiment groups including a vehicle, low-dose telmisartan (.3 mg/kg/day), and high-dose telmisartan (3 mg/kg/day).
Insulin resistance predicts development of type 2 diabetes mellitus (DM). Adipocytes release tumor Necrosis factor-alpha (TNF-α), and adiponectin. They modulate whole-body insulin sensitivity . The disturbance in the relationship between good and bad adipokines may cause insulin resistance. The renin-angiotensin aldosteron system (RAAS) plays a role in DM and the consequence of cardiovascular complications development. It is considered as a target for therapy. The present objective examined the relationship between renin angiotensin system and DM. There were, Group (1): Normal non obese rats, Group (2): Obese diabetic rats, Group (3): Obese diabetic rats with telmisartan, Group (4): Obese diabetic rats with enalapril, Group (5): Obese diabetic rats with aliskiren. There was a significant increase in serum glucose, lipid profile [triglycerides (TGs), low-density lipoprotein cholesterol (LDL), total serum cholesterol (TC)], tumor Necrosis factor-alpha (TNF-α), malondialdehyde (MDA) and a significant decrease in adiponectin associated with minor changes in superoxide dismutase (SOD) activity in the obese diabetic rats. Administration of telmisartan, enalapril and or aliskiren caused a significant improvement in serum lipid profile and adiponectin, a minor improvement in SOD activity, a decrease in TNF-α and or MDA. Renin angiotensin blockers significantly improve the metabolism and oxidative dysfunctions in Type 2 DM and aliskiren may show a promising powerful therapy.
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Many hypertensive subjects travel to high altitudes, but little is known on ambulatory blood pressure (ABP) changes and antihypertensive drugs' efficacy under acute and prolonged exposure to hypobaric hypoxia. In particular, the efficacy of angiotensin receptor blockers in this condition is unknown. This may be clinically relevant considering that renin-angiotensin system activity changes at altitude. The HIGHCARE-HIMALAYA study assessed changes in 24 h ABP under acute and prolonged exposure to increasing altitude and blood pressure-lowering efficacy and safety of an angiotensin receptor blockade in this setting.
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The aim of the study was to evaluate an antihypertensive effect of AT1-receptor blocker telmisartan on the rest and exercise blood pressure (BP) in patients suffering from mild and moderate arterial hypertension. Twenty males (mean age 50.9 +/- 6.9) following a 3-week placebo run-in phase were treated by telmisartan 80 mg q.d. Bicycle exercise test and echocardiography was performed at the end of placebo run-in phase and following 12 weeks of treatment. The workload on the bicycle exercise test has been increased by 25 watts every 2 min and stopped at systolic BP (SDP) 240 or diastolic BP (DBP) 130 mmHg. The maximal workload was the same, prior and after 12 weeks of the treatment. Antihypertensive therapy with telmisartan had a favorable effect, i.e. significantly decreased the rest BP--both SBP (152.5 +/- 11.4 mmHg vs. 139.2 +/- 12.3 mmHg, p < 0.001) and DBP (100.0 +/- 4.6 mmHg vs. 88.7 +/- 6.2 mmHg, p < 0.001). There were no significant changes in the heart rate (HR) at rest prior and after telmisartan treatment (71.4 +/- 9.1 b/min vs. 72.2 +/- 10.4 b/min). When repeating the exercise test after 12 weeks of telmisartan treatment we detected the significant decrease of BP at maximal workload, i.e. SBP decreased from 230.9 +/- 11.4 mmHg to 211.3 +/- 12.7 mmHg, p < 0.05 and DBP decreased from 124.6 +/- 7.5 mmHg to 109.7 +/- 9.7 mmHg, p < 0.05. There was a significant decrease in HR (140.6 +/- 13.2 b/min vs. 130.1 +/- 14.2 b/min, p < 0.05) and significant increase in JT interval at maximal workload after telmisartan treatment (0.193 +/- 0.014 sec vs. 0.201 +/- 0.014 sec, p < 0.05). Telmisartan decreased the double product at rest and maximal workload (diff. of 16 x 10(2) mmHg x b/min and 48 mmHg x 10(2) b/min, respectively, p < 0.05).
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The availability of selective, potent, orally active and long acting nonpeptide angiotensin II type 1 (AT1) receptor antagonists has provided the opportunity to obtain the benefits of selectively blocking the renin-angiotensin-aldosterone system at the level of the AT1 receptor that mediates most, if not all, of the important actions of angiotensin II, and avoid the nonspecificity of the angiotensin I converting enzyme inhibitors. Losartan was the first, but by no means remained the only, AT1 receptor antagonist. Numerous other 'sartans' have emerged in the past several years and successfully completed clinical development. With the exception of eprosartan, all others, ie, candesartan, irbesartan, saprisartan, tasosartan, telmisartan, valsartan and zolasartan, are based on medications of losartan's prototypical chemical structure. Among the current AT1 receptor antagonists, the rank order of the relative binding affinities (highest affinity = 1) is: candesartan 1, telmisartan 10, E3174 (the active metabolite of losartan) 10, tasosartan 20, losartan 50, eprosartan 100 and the prodrug candesartan cilexetil 280. The mode of (functional) AT1 receptor antagonism has been characterized as surmountable/noncompetitive (losartan, tasosartan, eprosartan) or insurmountable/noncompetitive (candesartan, saprisartan, zolasartan, irbesartan, valsartan, telmisartan, E3174). It is very likely that slow dissociation kinetics from the AT1 receptor underlie insurmountable antagonism. However, competitive or noncompetitive antagonism does not determine the antihypertensive efficacy, but the slow off-rate may extend the occupancy of the AT1 receptor and thereby lengthen the duration of the antihypertensive effect.
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The present study document that, telmisartan and atorvastatin combination have better renoprotective effects but not with individual drug when compared to the diabetic group. The combination also attenuated the progression of diabetic nephropathy by slowing the proteinuria and microalbuminuria and these effects were confirmed by histopathological analysis.
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Studies have suggested that angiotensin receptor blockers may exert a protective role towards doxorubicin-induced cardiotoxicity, but they have not been extensively investigated in this area. We therefore investigated whether the co-treatment of telmisartan, an angiotensin (Ang II) type-1 receptor blocker, might offer protection against daunorubicin cardiotoxic properties in rats.
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The results did not show an effect of ARBs as a class on increasing cancer incidence in patients with diabetes. However, there was a negative association of losartan but a positive one of candesartan and telmisartan with the overall occurrence of cancer. The underlying mechanism certainly requires further investigation.
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Data for this retrospective cohort study were obtained from Caremark's data warehouse. Patients were included in the analysis if they filled prescriptions for ARBs only, did not receive ARB therapy within the 6 months before the filling of the first ARB prescription (index date), were continuously eligible for benefits for 6 months before the index date, were eligible for prescription benefits for the 12 months following the index date, and were age 20-80 years.
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All patients received medical treatment with telmisartan once daily and were randomized to either electronic compliance monitoring with a reminder and monitoring device or standard therapy for 6 months. Both groups were crossed over after 6 months. Intervention effectiveness was assessed using self-reported compliance and BP.
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This new analysis supports the results of the earlier investigation, in that indapamide SR 1.5 mg/day appeared to be the most effective drug for producing significant reductions in SBP within 8-12 weeks, which is an essential element in optimising cardiovascular prevention among hypertensive patients. The clinical application of these results should take into consideration all the limitations discussed in this analysis.
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Metabolic syndrome is common in patients with hypertension and increases the risk of developing diabetes mellitus. The objective of this study (the MARCADOR study) was to compare the effects of manidipine 20 mg with the extemporary combination of manidipine 10 mg/lisinopril 10 mg, amlodipine 10 mg and telmisartan 80 mg on insulin sensitivity, as well as metabolic, inflammatory and prothrombotic markers, in hypertensive non-diabetic patients with metabolic syndrome.
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Baseline characteristics of each group were similar. During the observation period, the blood pressures of each group decreased at similar rates. In the telmisartan group, 17 patients (47.2%) were introduced to renal replacement therapy, as compared with 31 patients (86.1%) in the control group (relative risk 0.55, 95% confidence interval 0.19 - 0.92, p < 0.05). Telmisartan significantly reduced proteinuria levels (from 3.47 +/- 3.00 to 2.41 +/- 2.46 g/g . creatinine, p < 0.05) and was associated with a reduction of 49.6% in the decline rate of eGFR. The incidence of major adverse events in both groups was similar.
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Angiotensin-converting enzyme (ACE) inhibitors and angiotensin II (ATII)-receptor antagonists suppress the effects of ATII and are effective antihypertensive agents. However, the use of ACE inhibitors is sometimes associated with intolerable side effects (eg, cough, angioedema), and patients may develop a compensatory rise in ATII levels. ATII-receptor antagonists have tolerability profiles similar to that of placebo and inhibit the effects of ATII more completely by blocking the AT1 receptor.
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We report a drug metabolism based analysis of genetic polymorphisms in a Caucasian patient receiving fluvastatin and telmisartan experiencing myotoxicity (myalgia and moderate creatine kinase elevation).
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Telmisartan/amlodipine administered either on the morning or at bedtime can effectively reduce blood pressure. The efficacy of BP lowering is independent of the drug taking time. There is a trend both in better BP lowering and less BP variability when two medications are administered at bedtime.
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Prolongation of P-wave times and increase of P-wave dispersion (PWD) were shown to be independent predictors of atrial fibrillation (AF). Angiotensin II receptor blockers (AARBs) and angiotensin-converting enzyme inhibitors (ACEIs) have beneficial effects on atrial conduction times. However, there are not enough data about the comparative effects of those drugs on PWD.
The model of acute myocardial infarction (AMI) was established by ligating left anterior descending coronary artery. The surviving rats were divided into AMI (AMI) and telmisartan treatment (telmisartan) groups. And another sham operation group (sham) was designated (n = 8). At the end of study, total heart weight (THW), left ventricular weight (LVW) and weight index were measured; myocardial infarction and inflammatory reactions detected by hematoxylin and eosin and Masson staining; the serum levels of C-reactive protein (CRP), tumor necrosis factor-alpha (TNFα), monocyte chemotactic protein-1 (MCP-1), interleukin-6 (IL-6) and interleukin-1 beta (IL-1β) by enzyme-linked immunosorbent assay (ELISA); the levels of transforming growth factor 1 (TGFβ1), collagen I, collagen III and MMP9 mRNA in myocardial tissue by reverse transcription-polymerase chain reaction (RT-PCR); the expressions of TGFβ1, collagen I, collagen III, matrix metallopeptidase 9 (MMP9) and nuclear factor-kappa B (NF-κB) by Western blot.
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In the hepatic uptake of organic anions, organic anion transporting polypeptide (OATP) 1B1 is believed to be mainly involved. We have constructed a set of double-transfected cells coexpressing OATP1B1 and hepatic efflux transporters and characterized the transcellular transport of several anions. Recent reports have also suggested the importance of OATP1B3 in the hepatic uptake of some compounds. However, there is little information about OATP1B3-selective substrate and no good tool for the evaluation of efflux transporters of OATP1B3 substrates. In the present study, we found an OATP1B3-selective substrate and established a novel set of double transfectants expressing OATP1B3. Telmisartan acylglucuronide (tel-glu) is a main metabolite of telmisartan, an angiotensin II receptor antagonist. Tel-glu is recognized by hepatobiliary transport systems and efficiently distributed to liver. Several studies using rat and human hepatocytes and transporter-expressing cells revealed that OATP1B3 was responsible for the hepatic uptake of tel-glu in humans. By using double transfectants expressing OATP1B3, we investigated the transcellular transport of tel-glu as well as estradiol 17beta-d-glucuronide (E(2)17betaG) and cholecystokinin octapeptide (CCK-8) to identify the responsible efflux transporters in their biliary excretion. Vectorial basal-to-apical transport of tel-glu was observed in all kinds of double transfectants expressing OATP1B3. In contrast, basal-to-apical transport of E(2)17betaG and CCK-8 was seen only in the OATP1B3/MRP2 double transfectant compared with OATP1B3-expressing cells. Therefore, the newly established set of double transfectants expressing OATP1B3 combined with OATP1B1-expressing double transfectants can be used as a powerful tool for the rapid identification of hepatic uptake and efflux transporters of organic anions.
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Thirty-five subjects enrolled and completed the protocol. At entry (median or %): age 49 years, 43% female, 77% non-white, 91% non-smokers, CD4+ T cell count 590 cells/mm(3), BMI 31 kg/m(2). AT responses were heterogeneous, with statistically significant losses of median (IQR) total (TAT, 2.9% (-9.8, 0.7), p = 0.03) and subcutaneous (SAT, -2.7% (-9.8, 1.1), p = 0.03) AT, but not VAT (-2.7% (-20.5, 14.2), p = 0.53). Significant decreases in waist circumference and waist:hip ratio occurred (both p<0.001) without BMI or weight changes. In an exploratory analysis, significant increases in TNF-α occurred among female subjects without changes in other inflammatory or metabolic markers. No related adverse events occurred.
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In this double-blind, placebo-controlled trial, we randomly assigned 558 hypertensive participants with ADPKD (15 to 49 years of age, with an estimated glomerular filtration rate [GFR] >60 ml per minute per 1.73 m(2) of body-surface area) to either a standard blood-pressure target (120/70 to 130/80 mm Hg) or a low blood-pressure target (95/60 to 110/75 mm Hg) and to either an angiotensin-converting-enzyme inhibitor (lisinopril) plus an angiotensin-receptor blocker (telmisartan) or lisinopril plus placebo. The primary outcome was the annual percentage change in the total kidney volume.
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Twenty-four-hour, day and night average systolic blood pressure (SBP) and 24-hour, day and night SBP load in the two groups were lowered as compared with before treatment (P < 0.05). The effects of Western medicine combined with SXC on blood pressure depression were better than those of Western medicine (P < 0.05). Western medicine combined with SXC had a significant influence on diastolic blood pressure (DBP) as compared with Western medicine (P < 0.05). The heart rate in the SXC group was reduced as compared with before treatment and the routine group (P < 0.05). Trough to peak ratio in SXC group was higher than that in the routine group, while there was no significant difference in smoothness index between the two groups. Morning surge in blood pressure in the two groups was improved as compared with before treatment (P < 0.05), and there was a significant difference in morning surge in blood pressure between the two groups (P < 0.05).
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Although protection of the kidneys by renin-angiotensin system (RAS) inhibitors is well known, differences in renal protection and the characteristics of RAS inhibitors have not been fully investigated. We randomly allocated 80 patients with hypertension complicated by type 2 diabetes and accompanied by microalbuminuria to 4 groups for treatment with the angiotensin receptor blockers (ARBs) telmisartan, losartan, candesartan and valsartan. Strict anti-hypertensive therapy was performed for 12 months (target blood pressure: lower than 130/80 mmHg), and renal function was compared. At study completion, all groups achieved the hypotensive target and no difference was noted in blood pressure levels. However, influences on renal function differed. In the telmisartan group in particular, the serum creatinine level was unchanged while the urinary albumin level and protein excretion were significantly decreased, displaying a strong renoprotective effect. These findings suggest that, although renal protection is a class effect of ARBs, the effect of telmisartan is particularly strong.
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Telmisartan attenuates liver fibrosis in bile duct-ligated rats via increasing ACE2 expression level.
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There were 20 patients in each group (n=40), with a mean age of 32.65 years in the treatment group. Plasma creatinine did not show any significant change in the different time lapse in which blood samples were taken, but creatinine clearance at the end of surgery (196.415±56.507 vs. 150.1995±75.081; p=0.034), and at 2 h postoperative period (162.105±44.756 vs. 113.235±31.228; p≤0.001) was statistically significant, which supports an increase in renal function in the telmisartan group.
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DPP-4 inhibition on top of ARB treatment significantly reduced urinary albumin excretion and oxidative stress in diabetic eNOS knockout mice. Linagliptin on top of an angiotensin II receptor blocker may offer a new therapeutic approach for patients with diabetic nephropathy.