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Jia Yu, Jing Tang, Xiaowei Yuan, Xingjie Guo, Longshan Zhao
Separations of six dihydropyridine enantiomers on three commercially available cellulose-based chiral stationary phases (Chiralcel OD-RH, Chiralpak IB, and Chiralpak IC) were evaluated with high-performance liquid chromatography (HPLC). The best enantioseparation of the six chiral drugs was obtained with a Chiralpak IC (250 × 4.6 mm i.d., 5 μm) column. Then the influence of the mobile phase including an alcohol-modifying agent and alkaline additive on the enantioseparation were investigated and optimized...
March 28, 2017: Chirality
Kai-Hung Cheng, Kai-Chun Cheng, Kai-Yuan Cheng, Yi-Hsin Yang, Chung-Wei Lee, Wen-Ter Lai
OBJECTIVE: Calcium channel blockers (CCBs) have been proved to have beneficial effects on cardiovascular (CV) outcomes, especially in stroke. Lercanidipine, a highly lipophilic CCB, lacks data regarding long-term outcomes including: CV, stroke, renal and all-cause mortality. This retrospective cohort study aims to clarify this. PATIENTS AND METHODS: A total of 144,630 newly diagnosed hypertension (HTN) patients (age: 18-65 years) in 2005 from the Taiwan's National Health Insurance Research Database were enrolled in this observational study...
April 13, 2017: Current Medical Research and Opinion
Robert Lins, Yves Haerden, Caroline de Vries
INTRODUCTION: Hypertension is the leading cause of cardiovascular disease worldwide. Calcium channel blockers are an effective antihypertensive treatment, but frequently hypertension remains uncontrolled for many patients, partly due to tolerability issues. AIM: To assess the tolerability and effectiveness of barnidipine in mild to moderate hypertension patients switching treatment from other calcium channel blockers in daily practice. METHODS: BASIC-HT, a prospective real life study, enrolled 20,479 hypertensive patients initiating barnidipine treatment...
January 6, 2017: High Blood Pressure & Cardiovascular Prevention: the Official Journal of the Italian Society of Hypertension
Christina Antza, Stella Stabouli, Vasilios Kotsis
Hypertension is an important risk factor for premature death as it increases the probability of stroke, myocardial infarction, and heart failure. Antihypertensive drugs can decrease cardiovascular (CV) morbidity and mortality. The majority of hypertensive patients need more than one antihypertensive agent to attain blood pressure (BP) targets. Monotherapy can effectively reduce BP only in 20%-40% of patients. Multiple mechanisms including increased peripheral vascular resistance, increased cardiac work, and hypervolemia are involved in the pathogenesis of hypertension...
2016: Vascular Health and Risk Management
Sangeetha Gupta, Uma Sharma, Naranamangalam R Jagannathan, Yogendra Kumar Gupta
Oxidative stress, inflammation and apoptotic neuronal cell death are cardinal mechanisms involved in the cascade of acute ischemic stroke. Lercanidipine apart from calcium channel blocking activity possesses anti-oxidant, anti-inflammatory and anti-apoptotic properties. In the present study, we investigated neuroprotective efficacy and therapeutic time window of lercanidipine in a 2h middle cerebral artery occlusion (MCAo) model in male Wistar rats. The study design included: acute (pre-treatment and post-treatment) and sub-acute studies...
February 2017: Experimental Neurology
K Tsioufis, Costas Tsioufis, Kyriakos Dimitriadis, Emmanouil Mantzouranis, Ilianna Mani, Dimitrios Tousoulis
OBJECTIVE: The aim of the present study was to compare the effects of the combination of lercanidipine/enalapril versus amlodipine/enalapril and hydrochlorothiazide/enalapril on blood pressure, target organ damage and sympathetic activation in patients with grade 2 essential hypertension. RESEARCH DESIGN AND METHODS: This was a 3 month, randomized, blinded-endpoint study in essential hypertensive patients. MAIN OUTCOME MEASURES: Office and ambulatory blood pressure, arterial stiffness, urinary albumin to creatinine ratio, renal arterial resistive index, and muscle sympathetic nerve activity were evaluated at baseline, after a 2 week run-in placebo period, at 1 month and at 3 months...
October 2016: Current Medical Research and Opinion
Nicolas Roberto Robles, Carlos Calvo, Javier Sobrino, Eugenia Espinel, Rafael Esteban, Lourdes Mateos, Juan F Macias
OBJECTIVE: The RED LEVEL study (REnal Disease: LErcanidipine Valuable Effect on urine protein Losses) directly compares, in an explorative fashion, the effects of lercanidipine + enalapril and amlodipine + enalapril combinations on renal parameters in hypertensive subjects. RESEARCH DESIGN AND METHODS: This was a 1 year, prospective, multi-center, randomized, open-label, blinded-endpoint (PROBE) study in hypertensive patients with albuminuria. MAIN OUTCOME MEASURES: Renal function (albuminuria, serum creatinine, creatinine clearance, estimated glomerular filtration rate and proteinuria); blood pressure...
October 2016: Current Medical Research and Opinion
Gianfranco Parati
Hypertension is associated with alterations in the vascular structure, which in turn enhance the risk of cardiovascular events. Notably, anti-hypertensive treatment may prevent or regress the changes of arterial wall structures. Lercanidipine is a third-generation CCB with peculiar pharmaceutical properties. Enalapril is an effective drug acting on the renin-angiotensin-aldosterone axis. This commentary discusses the vascular effects of the lercanidipine/enalapril combination, and comments on their potential clinical relevance...
October 2016: Current Medical Research and Opinion
Damiano Rizzoni
OBJECTIVE: The dose-effect relationship of fixed-dose combinations of anti-hypertensive drugs has been only poorly explored. This pooled analysis investigates the dose-response relationship of fixed-dose lercanidipine + enalapril in patients with mild-to-moderate hypertension. RESEARCH DESIGN AND METHODS: This was an individual patient data analysis of four randomized studies (n = 2340). MAIN OUTCOME MEASURES: The primary efficacy variable was the change from baseline in sitting diastolic blood pressure (SDBP)...
October 2016: Current Medical Research and Opinion
Damiano Rizzoni
OBJECTIVE: This meta-analysis evaluates the efficacy and safety of lercanidipine/enalapril fixed-dose combination in patients with mild to moderate essential hypertension. METHODS: Four observational studies on patients with sitting diastolic blood pressure (SDBP) between 95 and 109 mmHg, treated with lercanidipine/enalapril fixed-dose combination, were analyzed. The Random-Effect Model was used to limit heterogeneity across the studies. Weights were applied to determine the influence of each study on the combined results...
October 2016: Current Medical Research and Opinion
Shen Peixiao, Fang Ningyuan, Wang Haiya
OBJECTIVE: This randomized study evaluates the effects of lercanidipine - as well as its antihypertensive efficacy - on the number of circulating endothelial progenitor cells (EPCs) in elderly patients with hypertension. RESEARCH DESIGN AND METHODS: In total, 61 patients with hypertension were randomly assigned to lercanidipine 10 mg/day or to other antihypertensive treatments (control group). MAIN OUTCOME MEASURES: Cytometry analysis was conducted at baseline, at 12 weeks and at 24 weeks...
October 2016: Current Medical Research and Opinion
Mengdan Xu, Ying Wu, Hao Wang, Xin Xu, Shuiping Zhao, Mei Zhang, Huigen- Jin, Jinchuan Yan, Bangning Wang, Jianbin Gong, Xiang Lu, Jianqiang Peng, Qiuyan Dai
OBJECTIVE: The objective of this study was to compare the effectiveness of lercanidipine with felodipine in patients with mild-to-moderate hypertension on day-to-day home blood pressure variability. METHODS: This is a sub-study of a multicenter, randomized, open-label, parallel group and active controlled clinical trial. Hypertensive patients aged 18-75 (i.e. diastolic blood pressure ≥90 mmHg and <110 mmHg; systolic blood pressure ≥140 mmHg and <180 mmHg) and 24 h mean BP >130/80 mmHg) were eligible for this study...
October 2016: Current Medical Research and Opinion
Enrico Agabiti Rosei
No abstract text is available yet for this article.
October 2016: Current Medical Research and Opinion
Praful Balavant Deshpande, Aravind Kumar Gurram, Amruta Deshpande, Gopal Venkatesh Shavi, Prashant Musmade, Karthik Arumugam, Ranjith Kumar Averineni, Srinivas Mutalik, Meka Sreenivasa Reddy, Nayanabhirama Udupa
AIM: The aim of the present study was to develop nanoproliposomes of lercanidipine, in order to overcome its poor biopharmaceutical properties and to improve its therapeutic efficacy in treating hypertension. MAIN METHODS: The nanoproliposomes were prepared using a modified thin-film hydration method, and the formula was optimized by varying the ratio of lipids and the types of cryoprotectants. This optimized formulation was characterized in terms of its particle size, solid-state, drug release, in-situ absorption, in-vivo pharmacokinetics, and in-vivo anti-hypertensive activity in DOCA-salt induced hypertensive rats...
October 1, 2016: Life Sciences
C Tsioufis, A Kasiakogias, K Dimitriadis, T Kalos, I Liatakis, D Konstantinidis, E Andrikou, L Nikolopoulou, E Vlachos, K Kyriazopoulos, D Tousoulis
OBJECTIVE: The aim of the study is to compare in essential hypertensives the effects of lercanidipine/enalapril versus amlodipine/enalapril and enalapril/hydrochlorothiazide on various target organ damage end-points as well as on sympathetic nervous system activation during a follow-up period of 3 months. DESIGN AND METHOD: We studied 56 untreated patients with essential hypertension stage II [age: 56 ± 10 years, 30 males, office blood pressure (BP): 148/92 ± 14/11 mmHg] who were randomized to lercanidipine 10 mg/enalapril 20 mg (once daily) or amlodipine 5 mg/enalapril 20 mg (once daily) or enalapril 20 mg/hydrochlorothiazide 12...
September 2016: Journal of Hypertension
Nicolás R Robles, Francesco Fici, Guido Grassi
Although blood pressure control is considered the main mechanism for preventing the progression of chronic kidney disease (CKD), angiotensin-converting enzyme inhibitors and angiotensin receptors blockers have an additional organ-protective role. The effects of calcium channel blockers (CCBs) in renal disease are not so clearly defined. CCBs have pleiotropic effects that might contribute to protection of the kidney, such as attenuating the mesangial entrapment of macromolecules, countervailing the mitogenic effect of platelet-derived growth factors and platelet-activating factors and suppressing mesangial cell proliferation...
January 2017: Hypertension Research: Official Journal of the Japanese Society of Hypertension
Eboka Majolene B Sabi-Mouka, Janvier Engelbert Agbokponto, Run Zhang, Qian Li, Li Ding
A simple, sensitive and reproducible liquid chromatography-electrospray ionization-tandem mass spectrometry (LC-MS-MS) method was developed and validated for the first time for simultaneous quantification of lercanidipine and valsartan in human plasma. The analytes were extracted by simple protein precipitation with acetonitrile and separated on a Hanbon Hedera ODS-2 C18 (150 mm× 2.1 mm, 5 μm) column. The mobile phase was composed of a mixture (53:47, v/v) of acetonitrile and 10 mmol/L ammonium acetate containing 0...
July 12, 2016: Journal of Chromatographic Science
Leonid Feldman, Shlomo Vinker, Shai Efrati, Ilia Beberashvili, Oleg Gorelik, Walter Wasser, Michal Shani
Hypertension has been shown to be a risk factor for development of dementia. However, medical treatment of hypertension failed to reduce consistently the risk of dementia. Experimental study pointed to the possibility of difference between different calcium channel blockers (CCB) in their neuro-protective effect. The aim of our study was to evaluate the risk of dementia during treatment of hypertension with different CCBs. This is a retrospective cohort study based on electronic database of a large public health care organization...
2016: Clinical and Experimental Hypertension: CHE
Xiaobing Li, Fuguo Shi, Xiaojing He, Lingyan Jian, Li Ding
A rapid and highly sensitive liquid chromatography-tandem mass spectrometry (LC-MS/MS) method has been developed and validated for the determination of lercanidipine (LER) in human plasma. The plasma sample was deproteinized with methanol after addition of diazepam (internal standard, IS) and separated on a 38°C Hedera ODS-2 analytical column with a mobile phase of methanol and 5mM ammonium acetate buffer solution containing 0.1% formic acid at an isocratic flow rate of 400μL/min. The detection was performed on an API 4000 tandem mass spectrometer coupled with electrospray ionization (ESI) source in positive ESI mode...
September 5, 2016: Journal of Pharmaceutical and Biomedical Analysis
Carolina De Ciuceis, Claudia Rossini, Angela Tincani, Paolo Airò, Mirco Scarsi, Claudia Agabiti-Rosei, Giuseppina Ruggeri, Luigi Caimi, Doris Ricotta, Enrico Agabiti-Rosei, Damiano Rizzoni
BACKGROUND: It has been demonstrated that circulating endothelial progenitor cells (EPCs) number reflects the endogenous vascular repair ability, with the EPCs pool declining in presence of cardiovascular risk factors. Several drugs, including dihydropyridine calcium channel blockers, have been reported to elicit antioxidant and anti-inflammatory properties, as well as to improve vascular remodeling and dysfunction. However, no data are available about the effects of lercanidipine on EPCs...
2016: Blood Pressure
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