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Pitavastatine

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https://www.readbyqxmd.com/read/28500776/analysis-of-national-pharmacovigilance-data-associated-with-statin-use-in-korea-adverse-drug-reactions-with-statins
#1
Hyunah Kim, Namhyo Kim, Da Hee Lee, Hun-Sung Kim
The aim of this study was to evaluate clinical manifestations, age distribution and risk factors of adverse drug reactions (ADRs) of statins. Korean Adverse Event Reporting System (KAERS) database records (July 2009 - June 2014) on statin-treated adults were used. ADRs classified as "certain," "probable" and "possible" based on the WHO-Uppsala Monitoring Centre criteria were analysed. The frequency of ADRs was compared between adults (18-64 years) and older people (age ≥ 65 years) groups. In total, 2161 ADRs from 1690 patients (579, 34...
May 13, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28468836/comparison-of-methods-for-estimating-unbound-intracellular-to-medium-concentration-ratios-in-rat-and-human-hepatocytes-using-statins
#2
Takashi Yoshikado, Kota Toshimoto, Tomohisa Nakada, Kazuaki Ikejiri, Hiroyuki Kusuhara, Kazuya Maeda, Yuichi Sugiyama
It is essential to estimate concentrations of unbound drugs inside the hepatocytes to predict hepatic clearance, efficacy, and toxicity of the drugs. The present study was undertaken to compare predictability of the unbound hepatocyte-to-medium concentration ratios (Kp,uu) by two methods based on the steady-state cell-to-medium total concentration ratios at 37°C and on ice (Kp,uu,ss) and based on their initial uptake rates (Kp,uu,V0). Poorly metabolized statins were used as test drugs because of their concentrative uptake via organic anion transporting polypeptides (OATPs)...
May 3, 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/28466409/effects-of-pitavastatin-on-walking-capacity-and-cd34-133-cell-number-in-patients-with-peripheral-artery-disease
#3
Kenshiro Arao, Takanori Yasu, Yasuhiro Endo, Toshikazu Funazaki, Yoshimi Ota, Kazunori Shimada, Eiichi Tokutake, Naoki Naito, Bonpei Takase, Minoru Wake, Nahoko Ikeda, Yasuto Horie, Hiroyuki Sugimura, Shin-Ichi Momomura, Masanobu Kawakami
This multi-center prospective non-randomized comparative study investigated the effects of pitavastatin in patients with peripheral artery disease (PAD) in terms of exercise tolerance capacities and peripheral CD34(+)/133(+) cell numbers. At baseline, a peripheral blood test was administered to 75 patients with PAD, along with a treadmill exercise test using the Skinner-Gardner protocol to measure asymptomatic walking distance (AWD) and maximum walking distance (MWD). Each patient was assigned to a 6-month pitavastatin treatment group (n = 53) or a control group (n = 22), according to the patient's preference...
May 2, 2017: Heart and Vessels
https://www.readbyqxmd.com/read/28456721/investigation-of-the-importance-of-multidrug-resistance-associated-protein-4-mrp4-abcc4-in-the-active-efflux-of-anionic-drugs-across-the-blood-brain-barrier
#4
Kayoko Kanamitsu, Hiroyuki Kusuhara, John D Schuetz, Kenji Takeuchi, Yuichi Sugiyama
The importance of multidrug resistance-associated protein 4 (Mrp4/Abcc4) in limiting the penetration of Mrp4 substrate compounds into the central nervous system across the blood-brain barrier (BBB) was investigated using Mrp4(-/-) mice. Significant ATP-dependent uptake by MRP4 was observed for ochratoxin A, pitavastatin, raltitrexed (Km 43.7 μM), pravastatin, cGMP, 2,4-dichlorophenoxyacetate, and urate. The defect in the Mrp4 gene did not affect the brain-to-plasma ratio (Kp,brain) of quinidine and dantrolene...
April 26, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28430910/low-density-lipoprotein-cholesterol-targeting-with-pitavastatin-ezetimibe-for-patients-with-acute-coronary-syndrome-and-dyslipidaemia-the-hij-proper-study-a-prospective-open-label-randomized-trial
#5
Nobuhisa Hagiwara, Erisa Kawada-Watanabe, Ryo Koyanagi, Hiroyuki Arashi, Junichi Yamaguchi, Koichi Nakao, Tetsuya Tobaru, Hiroyuki Tanaka, Toshiaki Oka, Yasuhiro Endoh, Katsumi Saito, Tatsuro Uchida, Kunihiko Matsui, Hiroshi Ogawa
Aims: To elucidate the effects of intensive LDL-C lowering treatment with a standard dose of statin and ezetimibe in patients with dyslipidaemia and high risk of coronary events, targeting LDL-C less than 70 mg/dL (1.8 mmol/L), compared with standard LDL-C lowering lipid monotherapy targeting less than 100 mg/dL (2.6 mmol/L). Methods and Results: The HIJ-PROPER study is a prospective, randomized, open-label trial to assess whether intensive LDL-C lowering with standard-dose pitavastatin plus ezetimibe reduces cardiovascular events more than standard LDL-C lowering with pitavastatin monotherapy in patients with acute coronary syndrome (ACS) and dyslipidaemia...
April 18, 2017: European Heart Journal
https://www.readbyqxmd.com/read/28416195/pitavastatin-versus-pravastatin-in-adults-with-hiv-1-infection-and-dyslipidaemia-intrepid-12-week-and-52-week-results-of-a-phase-4-multicentre-randomised-double-blind-superiority-trial
#6
Judith A Aberg, Craig A Sponseller, Douglas J Ward, Vladimir A Kryzhanovski, Stuart E Campbell, Melanie A Thompson
BACKGROUND: People living with HIV-1 infection are at greater risk for cardiovascular disease than seronegative adults. Treatment of dyslipidaemia with statins has been challenging in people with HIV because of an increased potential for drug interactions due to competing cytochrome P450 metabolism between statins and commonly used antiretroviral agents. Neither pitavastatin nor pravastatin depend on cytochrome P450 for primary metabolism. We aimed to assess the safety and efficacy of pitavastatin versus pravastatin in adults with HIV and dyslipidaemia...
April 13, 2017: Lancet HIV
https://www.readbyqxmd.com/read/28410749/efficacy-and-safety-of-k-877-a-novel-selective-peroxisome-proliferator-activated-receptor-%C3%AE-modulator-spparm%C3%AE-in-combination-with-statin-treatment-two-randomised-double-blind-placebo-controlled-clinical-trials-in-patients-with-dyslipidaemia
#7
Hidenori Arai, Shizuya Yamashita, Koutaro Yokote, Eiichi Araki, Hideki Suganami, Shun Ishibashi
BACKGROUND AND AIMS: Substantial residual cardiovascular risks remain despite intensive statin treatment. Residual risks with high triglyceride and low high-density lipoprotein cholesterol are not the primary targets of statins. K-877 (pemafibrate) demonstrated robust efficacy on triglycerides and high-density lipoprotein cholesterol and a good safety profile as a monotherapy. The aim of these studies was to evaluate the efficacy and safety of K-877 add-on therapy to treat residual hypertriglyceridaemia during statin treatment...
March 24, 2017: Atherosclerosis
https://www.readbyqxmd.com/read/28396527/leveraging-of-rifampicin-dosed-cynomolgus-monkeys-to-identify-bile-acid-3-o-sulfate-conjugates-as-potential-novel-biomarkers-for-organic-anion-transporting-polypeptides
#8
Rhishikesh Thakare, Hongying Gao, Rachel E Kosa, Yi-An Bi, Manthena V S Varma, Matthew Cerny, Raman Sharma, Max Kuhn, Bingshou Huang, Yiping Liu, Aijia Yu, Gregory S Walker, Mark Niosi, Larry M Tremaine, Yazen Alnouti, A David Rodrigues
In the search for novel bile acid (BA) biomarkers of liver organic anion-transporting polypeptides (OATPs), cynomolgus monkeys received oral rifampicin (RIF) at four dose levels (1, 3, 10 and 30 mg/kg) that generated plasma free Cmax values (0.06, 0.66, 2.57 and 7.79 μM, respectively) that covered the reported in vitro IC50s for OATP1B1 and OATP1B3 (≤ 1.7 μM). As expected, the area under the plasma concentration-time curve (AUC) of an OATP probe drug (intravenous (2)H4-pitavastatin, 0.2 mg/kg) was increased 1...
April 10, 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/28387909/targeting-colon-cancer-stem-cells-with-novel-blood-cholesterol-drug-pitavastatin
#9
Z-Y Zhang, S-H Zheng, W-G Yang, C Yang, W-T Yuan
OBJECTIVE: Previous studies have demonstrated the importance of stem cells in human cancer, including colon cancer. Pitavastatin is approved for the treatment of hyperlipidemia and has also been shown to inhibit stem cell proliferation in preliminary in vitro studies. This study was done to investigate the effects of pitavastatin on human colon carcinoma stem cells (coCSCs) in vitro and in mouse tumor xenografts in vivo. MATERIALS AND METHODS: Human colon adenocarcinoma cell lines, SW480 and SW620, were cultured to the spheroid formation...
March 2017: European Review for Medical and Pharmacological Sciences
https://www.readbyqxmd.com/read/28373111/pretreatment-with-rifampicin-and-tyrosine-kinase-inhibitor-dasatinib-potentiates-the-inhibitory-effects-toward-oatp1b1-and-oatp1b3-mediated-transport-without-affecting-plasma-membrane-localization-of-the-transporters
#10
Sonia Pahwa, Khondoker Alam, Alexandra Crowe, Taleah Farasyn, Sibylle Neuhoff, Oliver Hatley, Kai Ding, Wei Yue
Current studies determined the effects of pretreatment with rifampicin, an organic anion-transporting polypeptide (OATP) inhibitor, and the tyrosine kinase inhibitor dasatinib on OATP1B1- and OATP1B3-mediated transport, and to evaluate the OATP-mediated drug-drug interaction (DDI) potential of dasatinib using the static R-value and dynamic physiologically-based pharmacokinetic models. Rifampicin and dasatinib pretreatment significantly decreased OATP1B1- and OATP1B3-mediated transport. Rifampicin pretreatment also significantly decreased [(3)H]-pitavastatin and [(3)H]-CCK-8 accumulation in human sandwich-cultured hepatocytes...
March 31, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28276528/variability-in-statin-induced-changes-in-gene-expression-profiles-of-pancreatic-cancer
#11
Helena Gbelcová, Silvie Rimpelová, Tomáš Ruml, Marie Fenclová, Vítek Kosek, Jana Hajšlová, Hynek Strnad, Michal Kolář, Libor Vítek
Statins, besides being powerful cholesterol-lowering drugs, also exert potent anti-proliferative activities. However, their anti-cancer efficacy differs among the individual statins. Thus, the aim of this study was to identify the biological pathways affected by individual statins in an in vitro model of human pancreatic cancer. The study was performed on a human pancreatic cancer cell line MiaPaCa-2, exposed to all commercially available statins (12 μM, 24 h exposure). DNA microarray analysis was used to determine changes in the gene expression of treated cells...
March 9, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28252528/effects-of-pitavastatin-and-pravastatin-on-markers-of-immune-activation-and-arterial-inflammation-in-hiv
#12
Mabel Toribio, Kathleen V Fitch, Laura Sanchez, Tricia H Burdo, Kenneth C Williams, Craig A Sponseller, Mary McCurdy Pate, Judith A Aberg, Markella V Zanni, Steven K Grinspoon
OBJECTIVE: Persistent immune activation is thought to contribute to increased cardiovascular disease risk in HIV and statins may help modulate systemic immune activation. We aimed to compare the effects of two key statins on markers of systemic immune activation and arterial inflammation in the HIV population. DESIGN: Double-blind, active-controlled, parallel-group comparative trial performed in 45 sites. METHODS: Two hundred and fifty-two antiretroviral therapy-treated HIV-infected participants with dyslipidemia were randomized (1 : 1) to pitavastatin 4 mg daily vs...
March 27, 2017: AIDS
https://www.readbyqxmd.com/read/28251662/analysis-and-comparison-of-the-cost-effectiveness-of-statins-according-to-the-baseline-low-density-lipoprotein-cholesterol-level-in-korea
#13
Y J Jeong, H Kim, S J Baik, T M Kim, S J Yang, S-H Lee, J-H Cho, H Lee, H W Yim, I Y Choi, K-H Yoon, H-S Kim
WHAT IS KNOWN AND OBJECTIVE: There are a few Korean studies on the economics of statins based on reduction in low-density lipoprotein cholesterol (LDL-C) data from other countries. This study aimed to analyse and compare the cost-effectiveness of statins according to the baseline LDL-C level in Korea. METHODS: Between January 2009 and December 2015, the data of patients who were prescribed statins for the first time were extracted from electronic medical records...
March 1, 2017: Journal of Clinical Pharmacy and Therapeutics
https://www.readbyqxmd.com/read/28244896/adjunctive-therapy-with-statins-reduces-residual-albuminuria-proteinuria-and-provides-further-renoprotection-by-downregulating-the-angiotensin-ii-at1-pathway-in-hypertensive-nephropathy
#14
Zhi Zhang, Ziqiang Li, Kaijin Cao, Dailong Fang, Fazhan Wang, Gang Bi, Jian Yang, Yingju He, Jinhui Wu, Yuquan Wei, Xiangrong Song
OBJECTIVES: Blockade of the renin-angiotensin II (Ang II) system by AT1 blockers (ARBs) and angiotensin-converting enzyme inhibitors retards the progression of chronic kidney disease (CKD) by reducing albuminuria/proteinuria. However, many patients with CKD suffer from residual albuminuria/proteinuria, which is an independent risk factor for CKD progression. The aim of the current study is to investigate the effect of pitavastatin, one of the adjunctive agents to ARBs, on the reduction of albuminuria/proteinuria and further renoprotection mediated by telmisartan in spontaneously hypertensive rats...
February 27, 2017: Journal of Hypertension
https://www.readbyqxmd.com/read/28237671/erratum-to-pitavastatin-vs-pravastatin-in-reduction-of-remnant-lipoprotein-cholesterol-in-patients-with-dyslipidemias-clin-ther-2016-39-1250-1251
#15
Leonardo Roever
No abstract text is available yet for this article.
February 22, 2017: Clinical Therapeutics
https://www.readbyqxmd.com/read/28185713/effects-of-pitavastatin-on-lipid-rich-carotid-plaques-studied-using-high-resolution-magnetic-resonance-imaging
#16
Tao Feng, Xiaoxing Huang, Qundi Liang, Yun Liang, Yong Yuan, Li Feng, Wenjun Wu, Xuehong Xiao, Ying Han
PURPOSE: This study evaluates the effectiveness of pitavastatin in patients with atherosclerosis. METHODS: Sixty patients with atherosclerosis with lipid-rich carotid plaques were included and allocated into low-dose (2 mg/d) and high-dose (4 mg/d) pitavastatin groups with 48 weeks of treatment. Total cholesterol, LDL-C, HDL-C, triglycerides, apolipoprotein A1, apolipoprotein B, lipoprotein (a), and the inflammation-related factors interleukin 6, high-sensitivity C-reactive protein, and homocysteine were determined...
February 6, 2017: Clinical Therapeutics
https://www.readbyqxmd.com/read/28165667/use-of-moderate-intensity-statins-for-low-density-lipoprotein-cholesterol-level-above-190-mg-dl-at-baseline-in-koreans
#17
Hun-Sung Kim, Hyeseon Lee, Sue Hyun Lee, Yoo Jin Jeong, Tong Min Kim, So Jung Yang, Sun Jung Baik, Hyunah Kim, Seung-Hwan Lee, Jae Hyoung Cho, In-Young Choi, Kun-Ho Yoon, Ju Han Kim
The ACC/AHA 2013 guideline recommends high-intensity statin therapy for a decrease in low-density lipoprotein cholesterol (LDL-C) level by >50% among patients with baseline values of ≥190 mg/dL (approximately 4.872 mmol/L); however, this value should be modified before applying it to Korean populations. We investigated the statin-specific LDL-C-lowering effects in Korean patients with baseline LDL-C value ≥ 4.872 mmol/L. Data of patients prescribed a statin for the first time from January 2009 to December 2013 were assessed...
February 6, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28159531/a-validated-lc-ms-ms-method-for-the-estimation-of-glimepiride-and-pitavastatin-in-rat-plasma-application-to-drug-interaction-studies
#18
Shruti Surendran, David Paul, Ratna Sushmita, Lavanya Krishna, Nirbhay Kumar Tiwari, Sanjeev Giri, Nanjappan Satheeshkumar
Glimepiride (GLI) is prescribed for the management of type-2 diabetes where as pitavastatin (PIT) for the treatment of diabetes associated dyslipidemia. Both the drugs are metabolized by CYP2C9 and have the potential of altering the enzyme through either inhibition or induction. In this respect, we present a simple, fast and validated bioanalytical LC-MS/MS method for the simultaneous estimation of GLI and PIT from rat plasma. Waters XTerra RP HPLC column (4.6×100mm, 5μm) with mobile phase consisting of acetonitrile and 10mM ammonium acetate (pH-6...
January 9, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/28130659/pitavastatin-a-review-in-hypercholesterolemia
#19
REVIEW
Sheridan M Hoy
Oral pitavastatin (Livalo(®); Livazo(®)) is a competitive HMG-CoA reductase inhibitor that is available in the EU for the reduction of elevated total cholesterol and low-density lipoprotein cholesterol (LDL-C) levels in adults with primary hypercholesterolemia and combined (mixed) dyslipidemia. In short-term, phase III or IV studies in this patient population, pitavastatin 1-4 mg once daily was generally no less effective than presumed equipotent dosages of atorvastatin and simvastatin (including in patients with type 2 diabetes or ≥2 cardiovascular risk factors) and was superior to pravastatin (including in patients aged ≥65 years) in lowering LDL-C levels...
April 2017: American Journal of Cardiovascular Drugs: Drugs, Devices, and Other Interventions
https://www.readbyqxmd.com/read/28121706/greater-remnant-lipoprotein-cholesterol-reduction-with-pitavastatin-compared-with-pravastatin-in-hiv-infected-patients
#20
Parag H Joshi, P Elliott Miller, Seth S Martin, Steven R Jones, Joseph M Massaro, Ralph B D'Agostino, Krishnaji R Kulkarni, Craig Sponseller, Peter P Toth
OBJECTIVE: Cardiovascular disease (CVD) is a leading cause of morbidity and mortality in those with HIV. An emerging CVD risk factor is triglyceride-rich remnant lipoprotein cholesterol (RLP-C: the sum of intermediate-density lipoprotein and very low-density lipoprotein cholesterol). The effects of statin therapy on lipoprotein subfractions, including RLP-C, in HIV dyslipidemia are unknown. METHODS: This is a post hoc analysis of the randomized INTREPID trial (NCT 01301066) comparing pitavastatin 4 mg daily vs...
April 24, 2017: AIDS
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