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https://www.readbyqxmd.com/read/29745335/experimental-drugs-for-neuropathic-pain
#1
Kinga Salat, Beata Gryzlo, Katarzyna Kulig
Background Neuropathic pain (NP) is an important public health problem and despite recent progress in the understanding, diagnosis, pathophysiological mechanisms and the treatment of NP, many patients remain refractory to pharmacotherapy. OBJECTIVE: Currently used drugs have limited efficacy and dose-limiting adverse effects, and thus there is a substantial need for further development of novel medications for its treatment. Alternatively, drugs approved for the use in diseases other than NP can be applied as experimental for NP conditions...
May 10, 2018: Current Neuropharmacology
https://www.readbyqxmd.com/read/29735266/neuraminidase-1-activates-insulin-receptor-and-reverses-insulin-resistance-in-obese-mice
#2
Anne Fougerat, Xuefang Pan, Victoria Smutova, Nikolaus Heveker, Christopher W Cairo, Tarik Issad, Bruno Larrivée, Jeffrey A Medin, Alexey V Pshezhetsky
OBJECTIVES: Neuraminidase 1 (NEU1) cleaves terminal sialic acids of glycoconjugates during lysosomal catabolism. It also modulates the structure and activity of cellular surface receptors affecting diverse pathways. Previously we demonstrated that NEU1 activates the insulin receptor (IR) and that NEU1-deficient CathAS190A-Neo mice (hypomorph of the NEU1 activator protein, cathepsin A/CathA) on a high-fat diet (HFD) develop hyperglycaemia and insulin resistance faster than wild-type animals...
April 21, 2018: Molecular Metabolism
https://www.readbyqxmd.com/read/29677152/optimization-of-the-critical-parameters-of-the-spherical-agglomeration-crystallization-method-by-the-application-of-the-quality-by-design-approach
#3
Orsolya Gyulai, Anita Kovács, Tamás Sovány, Ildikó Csóka, Zoltán Aigner
This research work presents the use of the Quality by Design (QbD) concept for optimization of the spherical agglomeration crystallization method in the case of the active agent, ambroxol hydrochloride (AMB HCl). AMB HCl spherical crystals were formulated by the spherical agglomeration method, which was applied as an antisolvent technique. Spherical crystals have good flowing properties, which makes the direct compression tableting method applicable. This means that the amount of additives used can be reduced and smaller tablets can be formed...
April 20, 2018: Materials
https://www.readbyqxmd.com/read/29595123/investigation-of-potential-drug-drug-interaction-between-salbutamol-and-ambroxol-and-bioequivalence-of-a-new-fixed-dose-combination-formulation-containing-two-drugs-in-healthy-chinese-subjects
#4
Yan Wang, Jin Lu, Tengfei Li, Shunbo Zhao, Wen Yang, Lingye Liu, Xing Shi, Li Ding
OBJECTIVES: The aims of the study were to investigate the potential drug-drug interaction between salbutamol and ambroxol, the bioequivalence of the new fixed-dose combination containing salbutamol and ambroxol compared with co-administration of the two separate formulations, and to describe the safety and tolerability of the fixed-dose combination formulation in healthy Chinese volunteers. MATERIALS AND METHODS: An open-label, single-dose, four-treatment, four-period crossover study for evaluation of drug-drug interaction and bioequivalence (n = 24) was performed...
March 29, 2018: International Journal of Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/29521616/n-acetyl-cysteine-increases-the-replication-of-chlamydia-pneumoniae-and-prolongs-the-clearance-of-the-pathogen-from-mice
#5
Dávid Kókai, Tímea Mosolygó, Dezső P Virók, Valéria Endrész, Katalin Burián
PURPOSE: Within the community, 10 % of acquired pneumonia is caused by Chlamydia pneumoniae. N-acetyl-cysteine (NAC) is one of the most commonly used mucolytics in respiratory diseases, but its effect on C. pneumoniae infection has not yet been investigated. In this study, our aim was to investigate whether NAC influences the replication of C. pneumoniae. After determining that NAC does have an effect on C. pneumoniae replication, the effect of an alternative drug called Ambroxol (Ax) was investigated...
March 9, 2018: Journal of Medical Microbiology
https://www.readbyqxmd.com/read/29441886/effects-and-mechanisms-of-ambroxol-inhalation-mucosolvan-%C3%A2-in-the-treatment-of-neonatal-pneumonia
#6
Zuqin Yang, Xiuman Xiao, Yumei Huang, Xiaoxiao He, Qinqin Lu, Shangqin Chen, Zhenlang Lin
Neonatal pneumonia is the leading cause of mortality in children aged <5 years. Ambroxol (Mucosolvan®) is a mucolytic and secretolytic drug and belongs to the group of expectorants with anti-oxidative and anti-inflammatory effects. The purpose of the present study was to observe the effects and mechanisms of Mucosolvan ® inhalation on neonatal pneumonia. Between January 2014 and October 2015, a total of 80 newborns with pneumonia were randomly divided into control and observation groups. While the patients in the control group were treated with conventional treatment only, those patients in the observation group were treated with Mucosolvan® in addition to the conventional treatment...
October 1, 2017: Die Pharmazie
https://www.readbyqxmd.com/read/29412172/in-vitro-pharmacology-of-ambroxol-potential-serotonergic-sites-of-action
#7
J D Hull, R A Lyon
AIMS: Ambroxol is a muco-active agent with multiple, clinically relevant effects in the airway. Despite its widespread use and well documented clinical efficacy, there are few data on its mechanism of action and receptor pharmacology beyond sodium channel blockade and inhibition of guanylate cyclase. Accordingly, in vitro studies were conducted to determine its overall receptor pharmacology and possible sites of action. MATERIALS AND METHODS: In vitro radioligand binding/enzyme inhibition studies were conducted at 62 receptors, ion channels and enzymes using standard techniques...
March 15, 2018: Life Sciences
https://www.readbyqxmd.com/read/29400127/glucocerebrosidase-and-parkinson-disease-molecular-clinical-and-therapeutic-implications
#8
Roberta Balestrino, Anthony H V Schapira
Parkinson disease (PD) is a complex neurodegenerative disease characterised by multiple motor and non-motor symptoms. In the last 20 years, more than 20 genes have been identified as causes of parkinsonism. Following the observation of higher risk of PD in patients affected by Gaucher disease, a lysosomal disorder caused by mutations in the glucocerebrosidase (GBA) gene, it was discovered that mutations in this gene constitute the single largest risk factor for development of idiopathic PD. Patients with PD and GBA mutations are clinically indistinguishable from patients with idiopathic PD, although some characteristics emerge depending on the specific mutation, such as slightly earlier onset...
February 1, 2018: Neuroscientist: a Review Journal Bringing Neurobiology, Neurology and Psychiatry
https://www.readbyqxmd.com/read/29362387/effects-of-ambroxol-on-the-autophagy-lysosome-pathway-and-mitochondria-in-primary-cortical-neurons
#9
J Magalhaes, M E Gegg, A Migdalska-Richards, A H Schapira
Glucocerebrosidase (GBA1) mutations are the major genetic risk factor for Parkinson's Disease (PD). The pathogenic mechanism is still unclear, but alterations in lysosomal-autophagy processes are implicated due to reduction of mutated glucocerebrosidase (GCase) in lysosomes. Wild-type GCase activity is also decreased in sporadic PD brains. Small molecule chaperones that increase lysosomal GCase activity have potential to be disease-modifying therapies for GBA1-associated and sporadic PD. Therefore we have used mouse cortical neurons to explore the effects of the chaperone ambroxol...
January 23, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29317199/polarized-light-microscopy-reveals-physiological-and-drug-induced-changes-in-surfactant-membrane-assembly-in-alveolar-type-ii-pneumocytes
#10
Thomas Haller, Alejandro Cerrada, Kristian Pfaller, Peter Braubach, Edward Felder
In alveolar type II (AT II) cells, pulmonary surfactant (PS) is synthetized, stored and exocytosed from lamellar bodies (LBs), specialized large secretory organelles. By applying polarization microscopy (PM), we confirm a specific optical anisotropy of LBs, which indicates a liquid-crystalline mesophase of the stored surfactant phospholipids (PL) and an unusual case of a radiation-symmetric, spherocrystalline organelle. Evidence is shown that the degree of anisotropy is dependent on the amount of lipid layers and their degree of hydration, but unaffected by acutely modulating vital cell parameters like intravesicular pH or cellular energy supply...
January 6, 2018: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/29165753/clinical-research-on-airway-intervention-before-tracheal-extubation-after-general-anesthesia-on-snoring-children
#11
Q Yang, Z-H Liu, Y-L Chang
OBJECTIVE: To analyze the method and the effect of airway intervention before tracheal extubation in post-anesthesia cure unit (PACU) after anesthesia when removing the tonsil under general anesthesia and adenoidectomy under nasal endoscope on children with snoring. PATIENTS AND METHODS: 46 cases diagnosed as snoring were executively selected in this study. The cases were randomly divided into the control group (n = 22) and the observation group (n = 24). For airway intervention after general anesthesia during the recovery period, the control group was treated with intravenous injection of 0...
October 2017: European Review for Medical and Pharmacological Sciences
https://www.readbyqxmd.com/read/29134721/atr-ftir-spectroscopy-and-%C3%AE-edxrf-spectrometry-monitoring-of-enamel-erosion-caused-by-medicaments-used-in-the-treatment-of-respiratory-diseases
#12
Raimundo Nonato Silva Gomes, Tanmoy T Bhattacharjee, Luis Felipe C S Carvalho, Luís Eduardo Silva Soares
Medicaments essential for alleviation of diseases may sometime adversely affect dental health by eroding the enamel, owing to their acidic nature. It is therefore highly desirable to be able to detect these effects quickly and reliably. In this study, we evaluated the erosive capacity of four most commonly prescribed respiratory disease syrup medicaments on enamel using micro-energy-dispersive X-ray fluorescence spectrometry (µ-EDXRF) and attenuated total reflection Fourier transform infrared spectroscopy (ATR-FTIR)...
February 2018: Microscopy Research and Technique
https://www.readbyqxmd.com/read/29078843/correlation-between-tumor-necrosis-factor-%C3%AE-and-interleukin-1%C3%AE-in-exhaled-breath-condensate-and-pulmonary-function
#13
Xuefeng Lin, Yichu Fan, Xiaodong Wang, Mingyou Chi, Xin Li, Xun Zhang, Daqiang Sun
BACKGROUND: Exhaled breath condensate (EBC) has emerged as a noninvasive method for assessing inflammation in lung diseases. Our aim is to investigate the correlation between tumor necrosis factor α (TNF-α) and interleukin 1β (IL-1β) in EBC and in lung tissue, and between these values in EBC with pulmonary function tests in patients with chronic obstructive pulmonary disease (COPD). MATERIALS AND METHODS: To ensure the availability of lung tissue, 60 patients undergoing resection for early lung cancer were divided into 3 groups: a COPD treatment group, a COPD control group and a non-COPD group...
October 2017: American Journal of the Medical Sciences
https://www.readbyqxmd.com/read/28993581/quantitative-detection-of-ambroxol-in-human-plasma-using-hplc-apci-ms-ms-application-to-a-pharmacokinetic-study
#14
Zhengsheng Mao, Xin Wang, Xin DI, Yangdan Liu, Yanan Zang, Dongke Ma, Youping Liu, Xin DI
In this study, a rapid and reliable high-performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) method for the determination of ambroxol in human plasma was developed and validated using palmatine as an internal standard (IS). Ambroxol and IS were extracted from 200 μL of human plasma via a simple protein precipitation preparation. Chromatographic separation was achieved on a Platisil C18 column (150 × 4.6 mm, 5 μm) using methanol-0.01% formic acid (70:30, v/v) as the mobile phase at a flow rate of 0...
2017: Analytical Sciences: the International Journal of the Japan Society for Analytical Chemistry
https://www.readbyqxmd.com/read/28942528/fast-monitoring-of-tooth-erosion-caused-by-medicaments-used-in-the-treatment-of-respiratory-diseases-by-atr-ftir-and-%C3%AE-edxrf-analysis
#15
Raimundo Nonato Silva Gomes, Tanmoy T Bhattacharjee, Luis Felipe C S Carvalho, Luís Eduardo Silva Soares
The present study aimed to evaluate the erosive potential of four most commonly prescribed syrup medicaments for respiratory diseases. Attenuated total reflectance-Fourier transform infrared (ATR-FTIR) spectroscopy combined with multivariate statistical analysis and micro-energy-dispersive X-ray fluorescence spectrometry (μ-EDXRF) mapping was performed. Fifty-five root dentin fragments obtained from the buccal surface of 30 bovine teeth were prepared and divided into five experimental groups (n = 10): control-artificial saliva (S), acebrofilin hydrochloride (AC), ambroxol hydrochloride (AM), bromhexine hydrochloride (BR), and salbutamol sulfate (SS)...
December 2017: Lasers in Medical Science
https://www.readbyqxmd.com/read/28860846/ambroxol-for-the-treatment-of-fibromyalgia-science-or-fiction
#16
Kai-Uwe Kern, Myriam Schwickert
Fibromyalgia appears to present in subgroups with regard to biological pain induction, with primarily inflammatory, neuropathic/neurodegenerative, sympathetic, oxidative, nitrosative, or muscular factors and/or central sensitization. Recent research has also discussed glial activation or interrupted dopaminergic neurotransmission, as well as increased skin mast cells and mitochondrial dysfunction. Therapy is difficult, and the treatment options used so far mostly just have the potential to address only one of these aspects...
2017: Journal of Pain Research
https://www.readbyqxmd.com/read/28753070/impact-of-mucolytic-agents-on-copd-exacerbations-a-pair-wise-and-network-meta-analysis
#17
Mario Cazzola, Paola Rogliani, Luigino Calzetta, Nicola A Hanania, Maria Gabriella Matera
Mucolytics are potentially useful for the management of chronic obstructive pulmonary disease (COPD), although there is conflicting advice on their use in different guideline documents. Furthermore, there is paucity of data comparing the efficacy of the different mucolytic agents in reducing the odds of COPD exacerbations. We performed pair-wise and network meta-analyses to evaluate the impact of mucoly-tics in COPD. Randomized clinical trials lasting at least 3 months and investigating the effects of mucolytics on COPD exacerbations were identified from published studies and repository databases...
October 2017: COPD
https://www.readbyqxmd.com/read/28741230/new-therapeutic-strategies-for-lewy-body-dementias
#18
REVIEW
Latha Velayudhan, Dominic Ffytche, Clive Ballard, Dag Aarsland
This article reviews current treatment strategies and recent advances for the Lewy body dementias (LBDs). Current available symptom treatment strategies are based on monoaminergic, cholinergic and glutaminergic neurotransmitter systems. Relatively robust evidence exists for cholinesterase inhibitors for cognitive impairment in LBD and in Parkinson's disease for antidepressants, clozapine and recently pimavanserin for psychosis. interpidine (RVT 101) and nelotanserin are currently under investigation. Non-pharmacological interventions, such as cognitive stimulation, physical exercises and neuromodulation strategies, may be useful in Parkinson's disease but have not yet been tested in dementias...
September 2017: Current Neurology and Neuroscience Reports
https://www.readbyqxmd.com/read/28736525/pharmaceutical-chaperones-and-proteostasis-regulators-in-the-therapy-of-lysosomal-storage-disorders-current-perspective-and-future-promises
#19
REVIEW
Fedah E Mohamed, Lihadh Al-Gazali, Fatma Al-Jasmi, Bassam R Ali
Different approaches have been utilized or proposed for the treatment of lysosomal storage disorders (LSDs) including enzyme replacement and hematopoietic stem cell transplant therapies, both aiming to compensate for the enzymatic loss of the underlying mutated lysosomal enzymes. However, these approaches have their own limitations and therefore the vast majority of LSDs are either still untreatable or their treatments are inadequate. Missense mutations affecting enzyme stability, folding and cellular trafficking are common in LSDs resulting often in low protein half-life, premature degradation, aggregation and retention of the mutant proteins in the endoplasmic reticulum...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28719814/enantiomeric-separation-of-seven-%C3%AE-agonists-by-nace-study-of-chiral-selectivity-with-diacetone-d-mannitol-boric-acid-complex
#20
Lili Lv, Lijuan Wang, Jun Li, Yajun Jiao, Shengnan Gao, Jiachang Wang, Hongyuan Yan
A rapid and effective nonaqueous capillary electrophoresis (NACE)-ultraviolet (UV) method was developed for the enantiomeric separation of seven β-agonists. Diacetone-d-mannitol-boric acid complex was used as a new chiral selector. It was in situ synthesized by the reaction of diacetone-d-mannitol and boric acid in methanol medium containing triethylamine. The effects of diacetone-d-mannitol, boric acid, and triethylamine concentrations on the enantioseparation were carefully investigated. Under the optimized conditions, baseline enantioseparation could be obtained for six of the tested β-agonists within 12min...
October 25, 2017: Journal of Pharmaceutical and Biomedical Analysis
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