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Drug efficacy

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https://www.readbyqxmd.com/read/29793058/the-transcription-factor-skn-1-and-detoxification-gene-ugt-22-alter-albendazole-efficacy-in-caenorhabditis-elegans
#1
Pauline Fontaine, Keith Choe
Parasitic nematodes infect over 1/4 th of the human population and are a major burden on livestock and crop production. Benzimidazole class anthelmintics are widely used to treat infections, but resistance is a widespread problem. Mutation of genes encoding the benzimidazole target β-tubulin is a well-established mechanism of resistance, but recent evidence suggests that metabolism of the drugs may also occur. Our objective was to investigate contributions of the detoxification-response transcription factor SKN-1 to anthelmintic drug resistance using C...
April 25, 2018: International Journal for Parasitology, Drugs and Drug Resistance
https://www.readbyqxmd.com/read/29793051/promising-antileishmanial-activity-of-novel-imidazole-antifungal-drug-luliconazole-against-leishmania-major-in-vitro-and-in-silico-studies
#2
Azar Shokri, Mahdi Abastabar, Masoud Keighobadi, Saeed Emami, Mahdi Fakhar, Saeed Hosseini Teshnizi, Koichi Makimura, Ali Rezaei-Matehkolaei, Hassan Mirzaei
OBJECTIVES: Pentavalent antimonials have been used for the treatment of leishmaniasis for more than 70 years; however their toxicity limits their benefits. Unfortunately, the efficacy of the first line drugs has been decreased and resistance seems to be noticeable. Luliconazole is a new azole with unique effects on fungi which has not been tested on Leishmania parasites yet. METHODS: In the present study, we evaluated cytotoxicity and anti-leishmanial activities of Luliconazole on promastigotes and intracellular amastigotes of Leishmania major (L...
May 21, 2018: Journal of Global Antimicrobial Resistance
https://www.readbyqxmd.com/read/29793000/effect-of-a-bisphosphonate-and-selective-estrogen-receptor-modulator-on-bone-remodeling-in-streptozotocin-induced-diabetes-and-ovariectomized-rat-model
#3
Young-Seok Lee, Rishab Gupta, Jeong-Taik Kwon, Dae-Chul Cho, Ye Jin Seo, Sung Young Seu, Eui Kyun Park, Inbo Han, Chi-Heon Kim, Joo-Kyung Sung, Kyoung-Tae Kim
BACKGROUND CONTEXT: Diabetes and menopause can cause severe osteoporosis. In general, menopause and diabetes can lead to an imbalance in bone turnover, which results in secondary osteoporosis. However, the efficacy of antiresorptive drugs against this form of osteoporosis has not been extensively evaluated. OBJECTIVE: The aim of this study was to determine the changes in vertebral bone remodeling when postmenopausal osteoporosis is accompanied by diabetes and the efficacy of bisphosphonates and selective estrogen-receptor modulators (SERMs) against these outcomes...
May 21, 2018: Spine Journal: Official Journal of the North American Spine Society
https://www.readbyqxmd.com/read/29792888/oral-vitamin-a-coupled-valsartan-nanomedicine-high-hepatic-stellate-cell-receptors-accessibility-and-prolonged-enterohepatic-residence
#4
Nesrine S El-Mezayen, Wessam F El-Hadidy, Wessam M El-Refaie, Thanaa I Shalaby, Mahmoud M Khattab, Aiman S El-Khatib
So far, liver fibrosis still has no clinically-approved treatment. The loss of stored vitamin-A (VA ) in hepatic stellate cells (HSCs), the main regulators to hepatic fibrosis, can be applied as a mechanism for their targeting. Valsartan is a good candidate for this approach; it is a marketed oral-therapy with inverse- and partial-agonistic activity to the over-expressed angiotensin-II type1 receptor (AT1R) and depleted nuclear peroxisome proliferator-activated receptor-gamma (PPAR-γ), respectively, in activated HSCs...
May 21, 2018: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/29792544/synergistic-phytochemicals-fail-to-protect-against-ovariectomy-induced-bone-loss-in-rats
#5
Suresh Ambati, Colette N Miller, Erica F Bass, Natalie M Hohos, Diane L Hartzell, Emily W Kelso, Emily R Trunnell, Jeong-Yeh Yang, Mary Anne Della-Fera, Clifton A Baile, Srujana Rayalam
Menopause induces a loss of bone as a result of estrogen deficiency. Despite pharmaceutical options for the treatment of osteopenia and osteoporosis, many aging women use dietary supplements with estrogenic activity to prevent bone loss and other menopausal-related symptoms. Such supplements are yet to be tested for efficacy against a Food and Drug Administration (FDA) approved medication for menopausal bone loss such as zoledronic acid (ZA). The postmenopausal rat model was used to investigate the efficacy of various synergistic phytochemical blends mixed into the diet for 16 weeks...
May 24, 2018: Journal of Medicinal Food
https://www.readbyqxmd.com/read/29792524/managing-comorbid-cardiovascular-disease-and-sleep-apnea-with-pharmacotherapy
#6
Jacek Wolf, Krzysztof Narkiewicz
Highly prevalent sleep disordered breathing (SDB) has been recognized as an independent cardiovascular disease (CVD) risk factor. Although these two entities often coexist, there is a shortage of sufficiently-powered studies testing the interplay between the course of sleep apnea and CVD pharmacotherapy. The mutual relationship between treated/untreated obstructive sleep apnea (OSA) with ongoing cardiovascular pharmacotherapies is an evident gap in clinical expertise. Areas covered: In this article, the authors review the available evidence and outline future research directions concerning the reciprocal relationship between the pharmacological treatment of CVD and SDB...
May 24, 2018: Expert Opinion on Pharmacotherapy
https://www.readbyqxmd.com/read/29792360/newer-human-inosine-5-monophosphate-dehydrogenase-2-himpdh2-inhibitors-as-potential-anticancer-agents
#7
Chetan P Shah, Prashant S Kharkar
Human inosine 5'-monophosphate dehydrogenase 2 (hIMPDH2), being an age-old target, has attracted attention recently for anticancer drug development. Mycophenolic acid (MPA), a well-known immunosuppressant drug, was used a lead structure to design and develop modestly potent and selective analogues. The steep structure-activity relationship (SAR) requirements of the lead molecule left little scope to synthesise newer analogues. Here, newer MPA amides were designed, synthesised and evaluated for hIMPDH2 inhibition and cellular efficacy in breast, prostate and glioblastoma cell lines...
December 2018: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/29792288/tralokinumab-for-severe-uncontrolled-asthma-stratos-1-and-stratos-2-two-randomised-double-blind-placebo-controlled-phase-3-clinical-trials
#8
Reynold A Panettieri, Ulf Sjöbring, AnnaMaria Péterffy, Peter Wessman, Karin Bowen, Edward Piper, Gene Colice, Christopher E Brightling
BACKGROUND: Tralokinumab is an anti-interleukin-13 human monoclonal antibody developed for the treatment of severe, uncontrolled asthma. These clinical trials aimed to assess the efficacy and safety of tralokinumab in this population. METHODS: STRATOS 1 and STRATOS 2 were randomised, double-blind, parallel-group, placebo-controlled, phase 3 clinical trials that enrolled participants aged 12-75 years with severe asthma that was inadequately controlled despite use of inhaled corticosteroids (≥500 μg per day fluticasone or equivalent) and a long-acting β2 agonist (but not oral corticosteroids)...
May 18, 2018: Lancet Respiratory Medicine
https://www.readbyqxmd.com/read/29792136/zinc-dependent-histone-deacetylase-inhibitors-in-cancer-therapeutics-recent-update
#9
Panagiotis I Georgianos, Maria Divani, Theodoros Eleftheriadis, Peter R Mertens, Vassilios Liakopoulos
BACKGROUND: Despite optimal management of diabetic kidney disease (DKD) with intensive glycemic control and administration of agents blocking the renin-angiotensin-aldosterone-system, the residual risk for nephropathy progression to end-stage-renal-disease (ESRD) remains high. Sodium-glucose co-transporter type 2 (SGLT-2)-inhibitors represent a newly-introduced anti-diabetic drug class with pleiotropic actions extending above their glucose-lowering efficacy. Herein, we provide an overview of preclinical and clinical-trial evidence supporting a protective effect of SGLT-2 inhibitors on DKD...
May 23, 2018: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/29792125/characteristics-of-apixaban-treated-patients-evaluation-of-the-dose-prescribed-and-the-persistence-of-treatment-a-cohort-study-in-catalonia
#10
Ainhoa Gomez-Lumbreras, Jordi Cortes, Maria Giner-Soriano, M Angeles Quijada-Manuitt, Rosa Morros
BACKGROUND: Apixaban is a direct oral anticoagulant, which inhibits factor Xa. It has demonstrated clinical efficacy in prevention of stroke and systemic embolism in adult patients with nonvalvular atrial fibrillation and a better safety profile compared to warfarin. OBJECTIVES: (1) To describe the characteristics of patients with nonvalvular atrial fibrillation beginning treatment with apixaban, (2) to analyze concomitant prescriptions of medications that could potentially interact with apixaban, (3) to evaluate the level of appropriate usage according to the recommended dosage, and (4) to estimate the level of apixaban persistence among naive and non-naive patients...
January 1, 2018: Journal of Cardiovascular Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/29792124/hypersensitivity-to-alemtuzumab-a-safe-and-effective-desensitization-protocol-a-case-report
#11
Diego Gutiérrez-Fernández, Mónica Saldaña-Valderas, Raquel de la Varga-Martínez, Antonio Foncubierta-Fernández, María J Fernández-Anguita, Maria Del C Fernández-Valle, Fermín Medina-Varo
We describe a successful desensitization to alemtuzumab in one patient diagnosed with T-cell prolymphocytic leukaemia. Alemtuzumab treatment was initiated during infusion number 18, the patient showed cutaneous eruption with a miliary pattern, despite premedication with corticosteroids and antihistamines. The eruption returned with successive alemtuzumab infusions (infusions 19, 20 and 21), remained present for longer and was more severe with each infusion. The patient was referred to our Allergy Unit as it was necessary to maintain alemtuzumab treatment...
January 1, 2018: Journal of Oncology Pharmacy Practice
https://www.readbyqxmd.com/read/29792024/metabotropic-glutamate-receptors-in-alcohol-use-disorder-physiology-plasticity-and-promising-pharmacotherapies
#12
Max E Joffe, Samuel W Centanni, Anel A Jaramillo, Danny G Winder, P Jeffrey Conn
Developing efficacious treatments for alcohol use disorder (AUD) has proven difficult. The insidious nature of the disease necessitates a deep understanding of its underlying biology as well as innovative approaches to ameliorate ethanol-related pathophysiology. Excessive ethanol-seeking and relapse are generated by long-term changes to membrane properties, synaptic physiology, and plasticity throughout the limbic system and associated brain structures. Each of these factors can be modulated by metabotropic glutamate (mGlu) receptors, a diverse set of G protein-coupled receptors highly expressed throughout the central nervous system...
May 23, 2018: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/29791921/does-gastroplus-support-similarity-and-dissimilarity-factors-of-in-vitro-in-vivo-prediction-in-biowaiver-studies-a-lower-strength-amlodipine-as-a-model-drug
#13
Abdel Naser Zaid, Naser Shraim, Asmaa Radwan, Nidal Jaradat, Samah Hirzallah, Ibrahim Issa, Aya Khraim
BACKGROUND: Many generic pharmaceutical products are currently available on the market place worldwide. Recently, there is a growing concern on the quality and efficacy of generic products. However, health care professionals such as physicians and pharmacists are in difficult situations to choose among alternatives. PURPOSE: The aim of this study is to assess the effectiveness of the in silico technique (Gastro Plus® ) in the biowaiver study and whether similarity and dissimilarity factors ( f 2 and f 1 respectively) are effective in this regard...
May 23, 2018: Drug Research
https://www.readbyqxmd.com/read/29791608/hiv-1-genetic-diversity-and-resistance-to-antiretroviral-drugs-among-pregnant-women-in-ribeir%C3%A3-o-preto-sp-brazil-cross-sectional-study
#14
Ana Teresa Mancini Pimenta, Isadora Alonso Correa, Patricia Pereira Dos Santos Melli, Renata Abduch, Geraldo Duarte, José Carlos Couto-Fernandez, Silvana Maria Quintana
BACKGROUND: Increasing genetic diversity of HIV-1 and emergence of drug-resistant mutations may reduce the efficacy of antiretroviral therapy and prophylaxis that are used to prevent mother-to-child transmission. The aim of this study was to assess the genetic diversity and prevalence of drug-resistant mutations among HIV-infected pregnant women. DESIGN AND SETTING: Cross-sectional study at an outpatient clinic for infectious diseases within gynecology and obstetrics...
March 2018: São Paulo Medical Journal, Revista Paulista de Medicina
https://www.readbyqxmd.com/read/29791520/use-of-direct-oral-anticoagulants-for-chronic-thromboembolic-pulmonary-hypertension
#15
Francisca Alexandra Gavilanes-Oleas, Jose Leonidas Alves, Caio Julio Cesar Fernandes, Luis Felipe Lopes Prada, William Salibe Filho, Mario Terra Filho, Luciana Morinaga, Susana Hoette, Carlos Jardim, Rogerio Souza
OBJECTIVES: Chronic thromboembolic pulmonary hypertension is one of the most prevalent forms of pulmonary hypertension and is a major complication of acute pulmonary embolism. One mainstay of chronic thromboembolic pulmonary hypertension treatment is lifelong anticoagulation. The recent advent of direct oral anticoagulants for acute pulmonary embolism treatment has provided a viable and effective alternative for treating this condition. However, little is known about the efficacy of this new class of drugs for treating chronic thromboembolic pulmonary hypertension...
May 17, 2018: Clinics
https://www.readbyqxmd.com/read/29791175/-dyslipidemia-and-hypertension-what-to-worry-about-more
#16
Jan Václavík
Dyslipidemia is present in every other patient with arterial hypertension. With increasing blood pressure and cholesterol levels, the risk of cardiovascular events increases proportionally. Treatment of dyslipidemia appears to lower cardiovascular mortality to a greater extent than treatment of hypertension. A significant proportion of patients with dyslipidemia indicated for drug therapy are not treated at all or treated insufficiently and do not reach the target values. Concurrent treatment of hypertension and dyslipidemia reduces the incidence of cardiovascular events significantly more than treating only one of these diseases...
2018: Vnitr̆ní Lékar̆ství
https://www.readbyqxmd.com/read/29791172/-current-treatment-options-in-maturity-onset-diabetes-of-the-young
#17
Ludmila Brunerová, Jana Urbanová, Jan Brož
The discovery of MODY (Maturity-Onset Diabetes of the Young) and the elucidation of its heritability enabled more precise clinical characteristics of different MODY subtypes and led to understanding that glucokinase MODY (GCK-MODY) is not associated with vascular complications in long term follow-up, whereas MODY of transcription factors (e.g. HNF1A-MODY) is in case of bad metabolic control connected with the acceleration of particularly microvascular complications. There is a strong evidence of the needlessness of any specific antidiabetic treatment in prognosticaly favourable GCK-MODY (except for the pregnancy)...
2018: Vnitr̆ní Lékar̆ství
https://www.readbyqxmd.com/read/29791170/effectiveness-and-safety-of-lixisenatide-for-treatment-of-diabetes-in-the-real-world-data-from-the-monitoring-registry-in-a-real-life-cohort-in-the-czech-and-slovak-republic
#18
Martin Haluzík, Alena Adamíková, Milan Běhunčík, Marek Macko, Radka Štěpánová
INTRODUCTION: GLP1 receptor agonist lixisenatide has demonstrated its efficacy in numerous clinical trials, nevertheless its real-life effectiveness data is limited. AIM: To describe effectiveness and safety of lixisenatide in routine clinical practice in the Czech Republic and the Slovak Republic, as recorded by the Registry-Based Observational Study. METHODS: Multinational, multicenter, observational, non-interventional, 6-month prospective product registry of patients with type 2 diabetes mellitus aged > 18 years who were initiating therapy with lixisenatide...
2018: Vnitr̆ní Lékar̆ství
https://www.readbyqxmd.com/read/29791030/antiepileptic-drugs-as-prophylaxis-for-postcraniotomy-seizures
#19
REVIEW
Janette Greenhalgh, Jennifer Weston, Yenal Dundar, Sarah J Nevitt, Anthony G Marson
BACKGROUND: This is an updated version of the Cochrane Review previously published in Issue 3, 2015.The incidence of seizures following supratentorial craniotomy for non-traumatic pathology has been estimated to be between 15% to 20%; however, the risk of experiencing a seizure appears to vary from 3% to 92% over a five-year period. Postoperative seizures can precipitate the development of epilepsy; seizures are most likely to occur within the first month of cranial surgery. The use of antiepileptic drugs (AEDs) administered pre- or postoperatively to prevent seizures following cranial surgery has been investigated in a number of randomised controlled trials (RCTs)...
May 23, 2018: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/29791008/the-pharmacology-pharmacokinetics-efficacy-and-adverse-events-associated-with-kava
#20
REVIEW
C Michael White
Kava is a plant with numerous kavapyrones that can induce pharmacologic effects and drug interactions through the cytochrome P450 and P-glycoprotein systems. Kava is used recreationally and for the treatment of anxiety. Clinical trials verify anxiolytic effects in excess of placebo, but the effects are not seen immediately and the optimal dose and dosing schedule needs to be determined. Clinical trials usually lasting for 4 weeks found generally good tolerability and safety; however, dermatologic, hepatologic, and cognitive adverse effects may occur...
May 23, 2018: Journal of Clinical Pharmacology
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