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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...
July 14, 2016: 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...
May 19, 2016: Blood Pressure
Guido Grassi
Obesity-related hypertension represents a condition frequently observed in current clinical practice characterized by a complex pathophysiological background and a very high cardiovascular risk profile, particularly in severely obese individuals. This explains, on the one hand, the difficulty in reducing elevated blood pressure values in this pathological state and, on the other, the need to achieve this goal in a relatively short-time period to prevent the occurrence of fatal and nonfatal cardiovascular events...
2016: Integrated Blood Pressure Control
Giuseppe Derosa, Amedeo Mugellini, Rosa Maria Pesce, Angela D'Angelo, Pamela Maffioli
BACKGROUND: Essential hypertension has been extensively reported to cause endothelial dysfunction. The aim of this study was to evaluate the effects of barnidipine or lercanidipine, in addition to losartan, on some parameters indicative of endothelial damage and oxidative stress in hypertensive, type 2 diabetic patients. METHODS: One hundred and fifty one patients were randomised to barnidipine, 20 mg/day, or lercanidipine, 20 mg/day, both in addition to losartan, 100 mg/day, for 6 months...
2016: BMC Cardiovascular Disorders
Ankita D Chonkar, J Venkat Rao, Renuka S Managuli, Srinivas Mutalik, Swapnil Dengale, Prateek Jain, N Udupa
Lercanidipine is a vasoselective dihydropyridine calcium antagonist, mainly used for the treatment of hypertension and angina pectoris. However, it suffers from food dependent absorption, poor solubility, low permeability and considerable first pass metabolism, resulting in highly variable and low bioavailability of 10%. Nanoparticles of lercanidipine were incorporated in fast dissolving oral films (FDO) via preparation of nanosuspension by evaporative antisolvent precipitation method. Prepared nanosuspensions were incorporated in FDO without lyophilizing or spray drying...
June 2016: European Journal of Pharmaceutics and Biopharmaceutics
Basant A Habib, Mohamed H H AbouGhaly
OBJECTIVES: This study aims to illustrate the applicability of combined mixture-process variable (MPV) design and modeling for optimization of nanovesicular systems. METHODS: The D-optimal experimental plan studied the influence of three mixture components (MCs) and two process variables (PVs) on lercanidipine transfersomes. The MCs were phosphatidylcholine (A), sodium glycocholate (B) and lercanidipine hydrochloride (C), while the PVs were glycerol amount in the hydration mixture (D) and sonication time (E)...
June 2016: Expert Opinion on Drug Delivery
Gino Seravalle, Gianmaria Brambilla, Daniela Prata Pizzalla, Anna Casati, Marta Riva, Cesare Cuspidi, Michele Bombelli, Giuseppe Mancia, Guido Grassi
Scanty information is available on the effects of combination drug treatment based on an ACE inhibitor and a calcium channel blocker on the neurometabolic alterations characterizing obesity-related hypertension (OHT). After 2-week run-in with enalapril (20 mg), 36 OHTs were randomized according to a double-blind crossover design to a combination therapy with either lercanidipine 10 mg (L) or felodipine extended release 5 mg (F), each lasting 8 weeks. Measurements included clinic and ambulatory blood pressure (BP) and heart rate, homeostasis model assessment index, plasma norepinephrine, and muscle sympathetic nerve activity...
March 2016: Journal of the American Society of Hypertension: JASH
E Lambert Kuhn, D Levêque, B Lioure, B Gourieux, P Bilbault
WHAT IS KNOWN AND OBJECTIVE: Ibrutinib is a recently approved oral anticancer agent with pharmacokinetics that is very sensitive to metabolic inhibition. We report a serious side effect of ibrutinib potentially attributable to interaction with the moderate CYP3A4 inhibitor verapamil. CASE DESCRIPTION: A patient with mantle cell lymphoma was admitted to our emergency department with severe diarrhoea. During a prescription review, the clinical pharmacist identified a potential drug interaction between ibrutinib and verapamil present in a branded combination product also containing trandolapril...
February 2016: Journal of Clinical Pharmacy and Therapeutics
Ankita D Chonkar, Renuka S Managuli, Josyula Venkata Rao, Nayanabhirama Udupa
AIM: Quantitative estimation of lercanidipine HCl in bulk material as well as from nanosuspension formulations via a developed reverse phase HPLC method. MATERIALS AND METHODS: Optimized chromatographic condition was used to achieve separation on a Kromasil (100-5c18 250 × 4.6 mm) column using Shimadzu HPLC system. The mobile phase consisted of a mixture of acetate buffer (20 mM pH 4.5) and acetonitrile in the ratio of 10:90, v/v. It is pumped through the chromatographic system at a flow rate of 1 ml/min...
December 2015: Journal of Basic and Clinical Pharmacy
Nitya Selvaraj, Mangaiarkkarasi Adhimoolam, Deepa Kameswari Perumal, Meher Ali Rajamohammed
BACKGROUND: The available conventional antiepileptics do not afford cure or prophylactic treatment and henceforth there is always a quest to explore new targets for management of convulsions. In this perspective, dihydropyridine calcium channel blockers have been investigated in various animal models of epilepsy. Lercanidipine, a newer dihydropyridine calcium antagonist, is a potential candidate with its favourable lipid profile and longer duration of action. OBJECTIVE: (1) To evaluate the anticonvulsant effect of lercanidipine alone and in combination with standard drug in adult male Swiss albino mice...
November 2015: Journal of Clinical and Diagnostic Research: JCDR
Giuseppe Mancia, Stefano Omboni, Irina Chazova, Antonio Coca, Xavier Girerd, Hermann Haller, Gianfranco Parati, Paolo Pauletto, Danuta Pupek-Musialik, Yevgeniya Svyshchenko
OBJECTIVE: To compare a combination of a dihydropyridine calcium-channel blocker with an angiotensin converting enzyme inhibitor vs. monotherapy with one or the other drug and placebo for their effects on home blood pressure (HBP). METHODS: After a 2-week placebo wash-out, patients with an elevated office blood pressure (BP) (diastolic 100-109 and systolic <180 mmHg) and HBP (diastolic ≥85 mmHg) were randomized double-blind to a 10-week treatment with placebo, lercanidipine, 10 or 20 mg daily, enalapril, 10 or 20 mg daily, or the four possible combinations...
January 2016: Journal of Hypertension
Daniel Duda-Seiman, Corina Duda-Seiman, Florin Borcan, Livia-Cristina Borcan, Silvia Mancas, Speranta Avram
Calcium channel blockers (CCB) are widely used in cardiovascular medicine expressing high hopes upon decreasing cardiovascular risk, morbidity and mortality. Here, the potency of CCBs on 58 Romanian asymptomatic hypertensive patients, with no atherothrombotic cardiovascular disease, was studied by clinical and in silico methods. In our study, arterial elasticity/stiffness was assessed; anthropometric, metabolic (lipidic) parameters were quantified. We concluded that lercanidipine 10 mg once daily, during three weeks, is able to dramatically improve central aortic systolic blood pressure, aortic pulse wave velocity...
2015: Cardiovascular & Hematological Agents in Medicinal Chemistry
Giuseppe Derosa, Amedeo Mugellini, Fabrizio Querci, Ivano Franzetti, Rosa Maria Pesce, Angela D'Angelo, Pamela Maffioli
The aim of this study was to evaluate the effects of lercanidipine or barnidipine on echocardiographic parameters, in hypertensive, type 2 diabetics with left ventricular hypertrophy. One hundred and forty-four patients were randomized to lercanidipine, 20 mg/day, or barnidipine, 20 mg/day, in addition to losartan, 100 mg/day, for 6 months. We evaluated: blood pressure, fasting plasma glucose (FPG), glycated hemoglobin (HbA(1c)), lipid profile, creatinine, estimated glomerular filtration rate (eGFR), sodium, potassium, and acid uric...
2015: Scientific Reports
E V Gosteva, L V Vasil'eva
We studied effect of therapy with fixed combination of lercanidipine and enalapril on 24-hour blood pressure (BP) profile in 34 elderly patients (mean age 76.4±5.2 years, 14 men, 20 women) with degree I hypertension. After clinical examination patients were given lercanidipine/ enalapril combination (10/10 mg/day). The dose was increased to 10+20 mg/day when necessary. Assessment of efficacy was conducted on Rate of achievement of target BP [systolic (S) BP <150 mm HG, diastolic (D) BP<90 mmHg] and dynamics of parameters of 24-hour BP profile...
2015: Kardiologiia
Sang-Hoon Na, Hae-Young Lee, Sang Hong Baek, Hui-Kyung Jeon, Jin-Ho Kang, Yoon-Nyun Kim, Chang-Gyu Park, Jae-Kean Ryu, Moo-Yong Rhee, Moo-Hyun Kim, Taek-Jong Hong, Dong-Ju Choi, Seong-Wook Cho, Dong-Hun Cha, Eun-Seok Jeon, Jae-Joong Kim, Joon-Han Shin, Sung-Ha Park, Seung-Hwan Lee, Sung-Hee John, Eun-Seok Shin, Nam-Ho Kim, Sung-Yun Lee, Jun Kwan, Myung-Ho Jeong, Sang-Wook Kim, Jin-Ok Jeong, Dong-Woon Kim, Nam-Ho Lee, Woo-Jung Park, Jeong-Cheon Ahn, Kyung-Heon Won, Seung Uk Lee, Jang-Hyun Cho, Soon-Kil Kim, Taehoon Ahn, Sukkeun Hong, Sang-Yong Yoo, Song-Yi Kim, Byung-Soo Kim, Jae-Hyeon Juhn, Sun-Young Kim, Yu-Jeong Lee, Byung-Hee Oh
PURPOSE: The objective of this study was to evaluate the efficacy and safety of the lercanidipine/valsartan combination compared with lercanidipine monotherapy in patients with hypertension. METHODS: Part 1 of this study was the randomized, multicenter, double-blind, parallel group, Phase III, 8-week clinical trial to compare superiority of lercanidipine 10 mg/valsartan 80 mg (L10/V80) and lercanidipine 10 mg/valsartan 160 mg (L10/V160) combinations with lercanidipine 10 mg (L10) monotherapy...
August 2015: Clinical Therapeutics
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