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https://www.readbyqxmd.com/read/27923200/a-quantitative-lc-ms-ms-method-for-simultaneous-determination-of-cocaine-and-its-metabolites-in-whole-blood
#1
Xiabin Chen, Xirong Zheng, Kai Ding, Ziyuan Zhou, Chang-Guo Zhan, Fang Zheng
As new metabolic pathways of cocaine were recently identified, a high performance liquid chromatography tandem mass spectrometry (LC-MS/MS) method was developed to simultaneously determine cocaine and nine cocaine-related metabolites in whole blood samples. One-step solid phase extraction was used to extract all of the ten compounds and corresponding internal standards from blood samples. All compounds and internal standards extracted were separated on an Atlantis T3 (100Å, 3μm, 2.1mm×150mm I.D) column and detected in positive ion and high sensitivity mode with multiple reaction monitoring...
November 11, 2016: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/27923161/antinociceptive-tolerance-to-nsaids-in-the-rat-formalin-test-is-mediated-by-the-opioid-mechanism
#2
Nana Tsiklauri, Ivliane Nozadze, Gulnaz Gurtskaia, Merab G Tsagareli
BACKGROUND: In the past decade it has been shown that tolerance develops to the antinociceptive effect of repeated systemic administration of commonly used non-steroidal anti-inflammatory drugs (NSAIDs) in acute pain models using rats. This is similar to the tolerance observed with opioid-induced analgesia. In the present study, we investigated the development of tolerance to the analgesic effects of NSAIDs diclofenac, ketorolac and xefocam in a chronic inflammatory pain model, the formalin test...
October 6, 2016: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/27923160/adolescent-and-adult-mice-display-differential-sensitivity-to-the-effects-of-bupropion-on-the-acquisition-of-a-water-maze-task
#3
Carmen Gómez, Carmen Carrasco, Rosa Redolat
BACKGROUND: Adolescence is characterized by major neurobiological changes, and the effects of some psychoactive drugs seem to differ between adolescents and adults. Bupropion, an antidepressant that is also used to treat nicotine addiction, induces behavioral actions in both adolescent and adult rodents. However, the effects of this drug on spatial ability have not been compared in animals at different stages of their development. The present study was conducted to assess the effects of bupropion on spatial learning and memory in adolescent and adult mice...
October 12, 2016: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/27923158/effect-of-intensive-lipid-lowering-therapies-on-cholinesterase-activity-in-patients-with-coronary-artery-disease
#4
Edyta Pytel, Bożena Bukowska, Maria Koter-Michalak, Małgorzata Olszewska-Banaszczyk, Paulina Gorzelak-Pabiś, Marlena Broncel
BACKGROUND: Many disease entities, including coronary artery disease (CAD), demonstrate abnormalities in the activity of cholinesterases. As CAD is characterized by an increase in cholesterol level, patients with this disease are treated with lipid-lowering drugs. The present study attempts to determine how statin or combined statin and ezetimibe therapy influences cholinesterase activity. METHODS: Plasma and erythrocytes were isolated from the peripheral blood of CAD patients (n=61) and healthy subjects (n=63)...
September 21, 2016: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/27923157/adjuvant-neuronal-nitric-oxide-synthase-inhibition-for-combined-treatment-of-epilepsy-and-comorbid-depression
#5
Tanveer Singh, Rajesh Kumar Goel
BACKGROUND: Elevated nitric oxide (NO) levels in the brain have been apparently associated with depression in kindled animals. Owing to the major role of neuronal nitric oxide synthase (nNOS) in brain and ineffectiveness of antiepileptic drugs (AEDs) in restoring nitrosative stress, the present study was envisaged to evaluate the adjuvant nNOS inhibitor, 7-nitroindazole (7-NI) with valproic acid for combined treatment of epilepsy and associated depression. METHODS: Pentylenetetrazole kindled animals associated with depression were treated with vehicle, valproate (300mg/kg/day ip), valproate with 7-NI (10mg/kg; 20mg/kg; 40mg/kg)/day ip and 7-NI (40mg/kg/day ip) for 15days...
October 4, 2016: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/27922765/therapeutic-drug-monitoring-of-anti-tumour-necrosis-factor-%C3%AE-agents-in-inflammatory-bowel-disease
#6
Nikola Mitrev, Rupert W Leong
Anti-TNFα therapy has revolutionised treatment of inflammatory bowel disease, however primary non-response and secondary loss of response are a significant problem. Therapeutic drug monitoring (TDM) has recently emerged as a means of optimising use of anti-TNFα agents. Areas covered: TDM of anti-TNFα agents can guide clinical decisions during treatment failure events, prevent treatment failure events, and potentially result in significant healthcare cost saving. TDM for anti-TNFα agent involves measurement of drug levels and anti-drug antibodies, and can be performed reactively or proactively...
December 6, 2016: Expert Opinion on Drug Safety
https://www.readbyqxmd.com/read/27922762/nonchemotherapy-drug-induced-agranulocytosis-in-children-detected-by-a-prospective-pharmacovigilance-program
#7
Nicolás Medrano-Casique, Hoi Y Tong, Alberto M Borobia, Antonio J Carcas, Jesús Frías, Elena Ramírez
OBJECTIVES: A prospective evaluation of nonchemotherapy drug-induced agranulocytosis (DIA) cases, which are infrequent in the pediatric population. We characterize agranulocytosis cases and assess lab test differences between drug- and nondrug-induced agranulocytosis. METHODS: Through our Prospective Pharmacovigilance Program from Laboratory Signals at Hospital we detected pediatric agranulocytosis cases from July 2007 to December 2010. This program estimates the incidence, drug causality, clinical features, outcomes of DIA pediatric cases, and assesses laboratory differences with respect to non-DIA...
December 6, 2016: Pediatric Hematology and Oncology
https://www.readbyqxmd.com/read/27922627/blood-based-and-urinary-prostate-cancer-biomarkers-a-review-and-comparison-of-novel-biomarkers-for-detection-and-treatment-decisions
#8
REVIEW
R J Hendriks, I M van Oort, J A Schalken
BACKGROUND: The diagnosis of prostate cancer (PCa) is currently based on serum PSA testing and/or abnormal digital rectal examination and histopathologic evaluation of prostate biopsies. The main drawback of PSA testing is the lack of specificity for PCa. To improve early detection of PCa more specific biomarkers are needed. In the past few years, many new promising biomarkers have been identified; however, to date, only a few have reached clinical practice. METHODS: In this review, we discuss new blood-based and urinary biomarker models that are promising for usage in PCa detection, follow-up and treatment decision-making...
December 6, 2016: Prostate Cancer and Prostatic Diseases
https://www.readbyqxmd.com/read/27922542/generalization-of-serotonin-and-dopamine-ligands-to-the-discriminative-stimulus-effects-of-different-doses-of-%C3%A2-3-4-methylenedioxymethamphetamine
#9
Jeremy I Webster, David N Harper, Susan Schenk
Studies that have attributed the discriminative stimulus effects of ±3,4-methylenedioxymethamphetamine (MDMA) to serotonergic mechanisms typically use a relatively low training dose of 1.5 mg/kg. The role of serotonin in the discriminative stimulus effects of higher doses of MDMA is, however, unknown. Separate groups of rats were trained to discriminate MDMA (1.5 or 3.0 mg/kg) from saline using a two-lever, food-reinforced drug-discrimination procedure. Generalization tests were carried out with a range of serotonin and dopamine ligands...
December 2, 2016: Behavioural Pharmacology
https://www.readbyqxmd.com/read/27922541/effects-of-the-5-ht1a-receptor-agonists-buspirone-and-8-oh-dpat-on-pupil-size-in-common-marmosets
#10
Manato Kotani, Naoko Urushino, Itaru Natsutani, Yuji Ogi, Kazuhito Ikeda
As pupil size is affected by psychotropic drugs in all mammals, it has been used as a well-established clinical indicator for the preclinical and clinical development of novel drugs. It has been reported that activation of the serotonin (5-HT)1A receptor differently affects pupil response in rodents (mydriasis) and humans (miosis). Thus, it is important to establish a quantitative system for measuring pupil size using other species, such as nonhuman primates. Common marmosets have recently attracted a great deal of attention as suitable experimental animals in the psychoneurological field because of handling ease compared with other nonhuman primates and the requirement for small amounts of test drugs...
December 2, 2016: Behavioural Pharmacology
https://www.readbyqxmd.com/read/27922344/predictors-of-mortality-in-a-paediatric-intensive-care-unit-in-kigali-rwanda
#11
Rosine Nyirasafari, Mark H Corden, Angélique Charlie Karambizi, Jean Claude Kabayiza, Jean Damascene Makuza, Rex Wong, Michael F Canarie
BACKGROUND: The enormous burden of critical illness in resource-limited settings has led to a growing interest in paediatric critical care in these regions. However, published data on the practice of critical care and patient outcomes in these settings are scant. OBJECTIVE: This study sought to identify risk factors associated with mortality in the newly established Paediatric Intensive Care Unit (PICU) at Kigali University Teaching Hospital (KUTH) in Rwanda and test the predictive ability of a newly devised mortality risk score, the modified PRISM (MP) score...
December 6, 2016: Paediatrics and International Child Health
https://www.readbyqxmd.com/read/27922065/detc-based-bacterial-cellulose-bio-curatives-for-topical-treatment-of-cutaneous-leishmaniasis
#12
Fabiana S Celes, Eliane Trovatti, Ricardo Khouri, Johan Van Weyenbergh, Sidney J L Ribeiro, Valeria M Borges, Hernane S Barud, Camila I de Oliveira
The treatment of leishmaniasis still relies on drugs with potentially serious adverse effects. Herein, we tested a topical formulation of bacterial cellulose (BC) membranes containing Diethyldithiocarbamate (DETC), a superoxide dismutase 1 inhibitor. Leishmania-infected macrophages exposed to BC-DETC resulted in parasite killing, without pronounced toxic effects to host cells. This outcome was associated with lower SOD1 activity and higher production of superoxide and cytokine mediators. Topical application of BC-DETC significantly decreased lesion size, parasite load and the inflammatory response at the infection site, as well as the production of both IFN-γ and TNF...
December 6, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27921279/biocompatibility-of-fluids-for-multiphase-drops-in-drops-microfluidics
#13
Aishah Prastowo, Alexander Feuerborn, Peter R Cook, Edmond J Walsh
This paper addresses the biocompatibility of fluids and surfactants in the context of microfluidics and more specifically in a drops-in-drops system for mammalian cell based drug screening. In the drops-in-drops approach, three immiscible fluids are used to manipulate the flow of aqueous microliter-sized drops; it enables merging of drops containing cells with drops containing drugs within a Teflon tube. Preliminary tests showed that a commonly-used fluid and surfactant combination resulted in significant variability in gene expression levels in Jurkat cells after exposure to a drug for four hours...
December 2016: Biomedical Microdevices
https://www.readbyqxmd.com/read/27921260/development-of-oral-flexible-tablet-oft-formulation-for-pediatric-and-geriatric-patients-a-novel-age-appropriate-formulation-platform
#14
Prabagaran Chandrasekaran, Ruckmani Kandasamy
Development of palatable formulations for pediatric and geriatric patients involves various challenges. However, an innovative development with beneficial characteristics of marketed formulations in a single formulation platform was attempted. The goal of this research was to develop solid oral flexible tablets (OFTs) as a platform for pediatrics and geriatrics as oral delivery is the most convenient and widely used mode of drug administration. For this purpose, a flexible tablet formulation using cetirizine hydrochloride as model stability labile class 1 and 3 drug as per the Biopharmaceutical Classification System was developed...
December 5, 2016: AAPS PharmSciTech
https://www.readbyqxmd.com/read/27921196/danshen-injection-as-adjuvant-treatment-for-unstable-angina-pectoris-a-systematic-review-and-meta-analysis
#15
Jia-Rui Wu, Shi Liu, Xiao-Meng Zhang, Bing Zhang
OBJECTIVE: To systematically evaluate the clinical effectiveness and safety of Danshen Injection (, DS) as one adjuvant treatment for conventional therapy with Western medicine (WM) for unstable angina pectoris (UAP). METHODS: Using literature databases, a thorough and systematic retrieval of randomized controlled trials (RCTs) comparing DS plus WM with WM was conducted from inception to April 2015. The extracted data from included studies was analyzed by Review Manager 5...
December 5, 2016: Chinese Journal of Integrative Medicine
https://www.readbyqxmd.com/read/27921039/clinical-manifestation-and-management-of-adpkd-in-western-countries
#16
REVIEW
Claudia Sommerer, Martin Zeier
BACKGROUND: Autosomal dominant polycystic kidney disease (ADPKD) is the most common hereditary kidney disease in Western countries. The prevalence is between 2.4/10,000 and 3.9/10,000. ADPKD represents a systemic disease resulting in deterioration in renal function. Until now, mutations in two genes (PKD1 and PKD2) have been identified. Recently, the European Medicines Agency (EMA) approved the use of the vasopressin V2 receptor antagonist tolvaptan to slow the progression of cyst development and renal insufficiency connected with ADPKD in adult patients with chronic kidney disease stages 1-3 at initiation of treatment with evidence of rapidly progressing disease...
October 2016: Kidney Diseases
https://www.readbyqxmd.com/read/27921038/the-clinical-manifestation-and-management-of-autosomal-dominant-polycystic-kidney-disease-in-china
#17
REVIEW
Cheng Xue, Chen-Chen Zhou, Ming Wu, Chang-Lin Mei
BACKGROUND: Autosomal dominant polycystic kidney disease (ADPKD) is the most common monogenic hereditary kidney disease characterized by progressive enlargement of renal cysts. The incidence is 1-2‰ worldwide. Mutations in two genes (PKD1 and PKD2) cause ADPKD. Currently, there is no pharmaceutical treatment available for ADPKD patients in China. Summary: This review focused on advances in clinical manifestation, gene diagnosis, risk factors, and management of ADPKD in China. There is an age-dependent increase in total kidney volume (TKV) and decrease in renal function in Chinese ADPKD patients...
October 2016: Kidney Diseases
https://www.readbyqxmd.com/read/27920890/mesoporous-silica-nanoparticles-equipped-with-surface-nanovalves-for-ph-controlled-liberation-of-doxorubicin
#18
N V Roik, L A Belyakova
Silica carriers equipped with molecular and supramolecular pH-sensitive nanovalves were designed by combination of sol-gel synthesis and selective postsynthetic modification. Mesoporous structure of synthesized materials was characterized by low-temperature nitrogen adsorption-desorption, small-angle X-ray diffraction and transmission electron microscopy. Chemical immobilization of N-[N'-(N'-phenyl)-2-aminophenyl]aminoalkyl groups was confirmed by IR spectral and chemical analyses of surface layer. Loading and release behaviour of synthesized drug carriers was studied in phosphate buffer solutions with pH 5...
December 6, 2016: Interface Focus
https://www.readbyqxmd.com/read/27920885/cloning-and-expression-of-soluble-recombinant-hiv-1-crf35-protease-hp-thioredoxin-fusion-protein
#19
Asaad Azarnezhad, Zohreh Sharifi, Rahmatollah Seyedabadi, Arshad Hosseini, Behrooz Johari, Mahsa Sobhani Fard
BACKGROUND: As a drug target and an antigenic agent, HIV-1 protease (HIV-1 PR) is at the center of attention for designing anti-AIDS inhibitors and diagnostic tests. In previous studies, the production of the recombinant protease has been faced with several difficulties; therefore, the aims of this study were the easy production, purification of the soluble form of protease in E. coli and investigation of its immunoreactivity. METHODS: Protease coding region was isolated from the serum of an infected individual, amplified by RT-PCR and cloned into PTZ57R using TA-cloning...
October 2016: Avicenna Journal of Medical Biotechnology
https://www.readbyqxmd.com/read/27920723/sex-dependent-anti-stress-effect-of-an-%C3%AE-5-subunit-containing-gabaa-receptor-positive-allosteric-modulator
#20
Sean C Piantadosi, Beverly J French, Michael M Poe, Tamara Timić, Bojan D Marković, Mohan Pabba, Marianne L Seney, Hyunjung Oh, Beverley A Orser, Miroslav M Savić, James M Cook, Etienne Sibille
Rationale: Current first-line treatments for stress-related disorders such as major depressive disorder (MDD) act on monoaminergic systems and take weeks to achieve a therapeutic effect with poor response and low remission rates. Recent research has implicated the GABAergic system in the pathophysiology of depression, including deficits in interneurons targeting the dendritic compartment of cortical pyramidal cells. Objectives: The present study evaluates whether SH-053-2'F-R-CH3 (denoted "α5-PAM"), a positive allosteric modulator selective for α5-subunit containing GABAA receptors found predominantly on cortical pyramidal cell dendrites, has anti-stress effects...
2016: Frontiers in Pharmacology
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