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https://www.readbyqxmd.com/read/28103158/serotonin-receptor-targeted-therapy-for-migraine-treatment-an-overview-of-drugs-in-phase-i-and-ii-clinical-development
#1
P Barbanti, C Aurilia, G Egeo, L Fofi, R Palmirotta
Research has focused on serotonin (5-HT) 5-HT1D and 5-HT1F receptors to develop drugs acting through non-vasoconstrictive mechanisms for treating acute migraine and those targeting 5-HT2B and 5-HT7 receptors for preventing migraine. Areas covered: This paper reviews antimigraine drugs targeting 5-HT receptors in one phase I trial (sumatriptan iontophoretic transdermal system, TDS) and five phase II clinical trials (PNU-142633, LY334370, lasmiditan, NOX-188). Expert opinion: Data from our overview on investigational drugs in phase I and II clinical trials using the 5-HT1B/1D receptor agonist (sumatriptan TDS), 5-HT1D receptor agonist (PNU-142633), 5-HT1F receptor agonists (LY334370, lasmiditan) and a combined 5-HT1B/1D receptor agonist with nNOS inhibition (NOX-188) provided encouraging data for sumatriptan TDS and lasmiditan, disappointing results for PNU-142633, and promising findings for NOX-188...
January 19, 2017: Expert Opinion on Investigational Drugs
https://www.readbyqxmd.com/read/28103139/endotoxin-neutralization-by-an-o-antigen-specific-monoclonal-antibody-a-potential-novel-therapeutic-approach-against-klebsiella-pneumoniaest258
#2
Valéria Szijártó, Luis M Guachalla, Katharina Hartl, Cecília Varga, Adriana Badarau, Irina Mirkina, Zehra C Visram, Lukas Stulik, Christine A Power, Eszter Nagy, Gábor Nagy
Klebsiella pneumoniae ST258 is a globally distributed multi-drug resistant pathogen responsible for severe invasive infections. In this study, the different virulence potential of K. pneumoniae ST258 isolates in endotoxin susceptible versus resistant animal models was shown. Furthermore, ST258 clinical isolates were found highly sensitive to the bactericidal effect of naive animal and human serum. These observations imply that LPS, released from the rapidly lysed bacteria, may contribute to the high mortality associated with ST258 bacteremia cases...
January 19, 2017: Virulence
https://www.readbyqxmd.com/read/28102773/the-optimal-duration-of-anticoagulant-therapy-after-unprovoked-venous-thromboembolism-still-a-challenging-issue
#3
Giovanna Elmi, Giuseppe Di Pasquale, Raffaele Pesavento
As about 50 % of patients with unprovoked venous thromboembolism (VTE) will develop new episodes after discontinuing therapy, indefinite treatment is suggested in patients with low or moderate bleeding risk. Baseline and post-baseline factors can help clinicians to identify patients at high risk of recurrence, who require extended treatment. Residual vein obstruction and D-dimer assay have been shown to be suitable methods for assessing the risk of VTE recurrences after a first unprovoked VTE. In treatment for VTE the use of direct oral anticoagulants (DOAC) is growing instead of the standard adjusted dose of vitamin K antagonists...
January 19, 2017: VASA. Zeitschrift Für Gefässkrankheiten
https://www.readbyqxmd.com/read/28102731/microfluidic-whole-blood-testing-of-platelet-response-to-pharmacological-agents
#4
Ruizhi Li, Tilo Grosser, Scott L Diamond
Platelets present a number of intracellular and transmembrane targets subject to pharmacological modulation, either for cardiovascular disease reduction or as an unintended drug response. Microfluidic devices allow human blood to clot on a defined surface under controlled hemodynamic and pharmacological conditions. The potencies of a number of antiplatelet and anticancer drugs have been tested with respect to platelet deposition on collagen under flow. Inhibitors of cyclooxygenase-1 (COX-1) reduce platelet deposition, either when added ex vivo to blood or ingested orally by patients prior to testing...
January 19, 2017: Platelets
https://www.readbyqxmd.com/read/28102427/prospective-randomised-trial-of-the-time-dependent-antiplatelet-effects-of-500-mg-and-250-mg-acetylsalicylic-acid-i-%C3%A2-v-and-300-mg-p-%C3%A2-o-in-acs-acute
#5
Uwe Zeymer, Thomas Hohlfeld, Jürgen Vom Dahl, Raimund Erbel, Thomas Münzel, Ralf Zahn, Alexander Roitenberg, Stefanie Breitenstein, Ákos Ferenc Pap, Dietmar Trenk
Little is known about the onset of action after intravenous or oral administration of acetylsalicylic acid (ASA) in patients with acute coronary syndromes (ACS). The aim of the study was to compare intravenous 250 or 500 mg acetylsalicylic acid (ASA) with oral 300 mg in ASA naïve patients with ACS concerning the onset of antiplatelet effects measured by time dependent thromboxane inhibition. A total of 270 patients with ACS < 24 hours were randomised into one of three treatment arms comprising administration of a single dose of ASA as soon as possible after admission...
January 19, 2017: Thrombosis and Haemostasis
https://www.readbyqxmd.com/read/28102361/effectiveness-and-tolerability-of-different-recommended-doses-of-ppis-and-h2ras-in-gerd-network-meta-analysis-and-grade-system
#6
Chao Zhang, Joey S W Kwong, Rui-Xia Yuan, Hao Chen, Chang Xu, Yi-Pin Wang, Gong-Li Yang, Jin-Zhu Yan, Le Peng, Xian-Tao Zeng, Hong Weng, Jie Luo, Yu-Ming Niu
Proton pump inhibitors (PPIs) and histamine-2-receptor antagonists (H2RAs) are used for gastro-esophageal reflux disease (GERD); however, the clinical evidence for treatment is poor. We evaluated the effectiveness and tolerability of different doses of PPIs, H2RAs and placebo in adults with GERD. Six online databases were searched through September 1, 2016. All related articles were included and combined with a Bayesian network meta-analysis from randomized controlled trials (RCTs). The GRADE systems were employed to assess the main outcome...
January 19, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28102110/evaluation-of-the-antidepressant-and-anxiolytic-like-effects-of-a-hydrophilic-extract-from-the-green-seaweed-ulva-sp-in-rats
#7
Nicolas Violle, Pascale Rozan, Hervé Demais, Pi Nyvall Collen, Jean-François Bisson
OBJECTIVES: The green seaweed Ulva sp. contains a large amount of ulvans, a family of sulphated polysaccharides. The present study was designed to investigate in rats the antidepressant- and anxiolytic-like effects of a hydrophilic extract of Ulva sp. (MSP) containing about 45% of ulvans. METHODS: After a 14-day administration of MSP at doses of 10, 20 and 40 mg/kg/day, 48 and 60 male adult Wistar rats were respectively tested in the elevated plus-maze (EPM) and the forced swimming test (FST)...
January 19, 2017: Nutritional Neuroscience
https://www.readbyqxmd.com/read/28102013/the-effect-of-potassium-diclofenac-and-dexamethasone-on-mmp-1-gene-transcript-levels-during-experimental-tooth-movement-in-rats
#8
G P Molina Da Silva, O M Tanaka, D F Campos Navarro, C E Repeke, G P Garlet, O Guariza-Filho, P C Trevilatto
OBJECTIVES: The aim of this study was to analyze MMP-1 transcript levels in periodontal tissues of rats that underwent orthodontic treatment using potassium diclofenac and dexamethasone at different stages of tooth movement. SETTING AND SAMPLE POPULATION: The sample comprised of ninety male Wistar rats. MATERIAL AND METHODS: A closed nickel-titanium coil spring was used to apply a force of 50 cN to move the maxillary right first molars mesially...
February 2017: Orthodontics & Craniofacial Research
https://www.readbyqxmd.com/read/28101875/sustanon-induces-dose-independent-hypertrophy-and-satellite-cell-proliferation-in-slow-oxidative-fibers-of-avian-skeletal-muscle
#9
Mohammed Z Allouh, Ahmad A Jarrar, Hasan A Asfour, Raed S Said, Emad I Shaqoura
Sustanon is a well-known anabolic drug that is used to treat hypogonadism and restore muscle mass and bone density. As research to date has been limited to its effects in glycolytic fibers, this study aimed to investigate the dose-related effects of Sustanon on the oxidative fibers of avian skeletal muscle. Adult female chickens were randomly divided into 4 groups: control (C), received a dose of 100 μl normal saline per injection; and Sustanon-1, -2, and -3 (S1, S2, and S3), that received a dose of 12.5, 25, or 50 mg/kg Sustanon per injection, respectively...
January 19, 2017: Histology and Histopathology
https://www.readbyqxmd.com/read/28101833/gout-treatment-survey-of-brazilian-rheumatology-residents
#10
REVIEW
Rodrigo Balbino Chaves Amorim, Ana Beatriz Vargas-Santos, Leticia Rocha Pereira, Evandro Silva Freire Coutinho, Geraldo da Rocha Castelar-Pinheiro
To assess the current practices in gout management among Brazilian rheumatology residents. We performed a cross-sectional online survey among all the rheumatology residents and those rheumatologists who had just completed their training (post-residency (PR)) regarding their approach to gout management. Results were compared with the 2012 American College of Rheumatology (ACR) gout guidelines and with the responses of a previous survey with a representative sample of practicing Brazilian rheumatologists (RHE)...
January 19, 2017: Clinical Rheumatology
https://www.readbyqxmd.com/read/28101809/sequential-exposure-of-bortezomib-and-vorinostat-is-synergistic-in-multiple-myeloma-cells
#11
Charvi Nanavati, Donald E Mager
PURPOSE: To examine the combination of bortezomib and vorinostat in multiple myeloma cells (U266) and xenografts, and to assess the nature of their potential interactions with semi-mechanistic pharmacodynamic models and biomarkers. METHODS: U266 proliferation was examined for a range of bortezomib and vorinostat exposure times and concentrations (alone and in combination). A non-competitive interaction model was used with interaction parameters that reflect the nature of drug interactions after simultaneous and sequential exposures...
January 18, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28101765/tolerability-and-safety-of-commonly-used-antiepileptic-drugs-in-adolescents-and-adults-a-clinician-s-overview
#12
REVIEW
Martin J Brodie
This paper discusses the issues surrounding the tolerability and safety of the commonly used antiepileptic drugs (AEDs) in adolescents and adults. The content includes dose-related adverse effects, idiosyncratic reactions, behavioural and psychiatric comorbidities, chronic problems, enzyme induction and teratogenesis. Twenty-one AEDs are discussed in chronological order of their introduction into the UK, starting with phenobarbital and ending with brivaracetam. Wherever possible, advice is given on anticipating, recognising and managing these issues and thereby improving the lives of people with epilepsy, most of whom will need to take one or more of these agents for life...
January 18, 2017: CNS Drugs
https://www.readbyqxmd.com/read/28101656/off-label-use-of-antimicrobials-in-neonates-in-a-tertiary-children-s-hospital
#13
Niina Laine, Ann Marie Kaukonen, Kalle Hoppu, Marja Airaksinen, Harri Saxen
PURPOSE: Off-label (OL) use of drugs for hospitalized children is very common. OL use occurs especially in the youngest patients, neonates. This study focused on the OL use of antimicrobials in neonates. To our knowledge, only few studies have focused on the prevalence of OL use of antimicrobials in neonates. METHODS: We investigated the OL use of antimicrobials in neonates in a tertiary children's hospital. First, we investigated what were the most consumed OL antimicrobials in defined daily doses according to hospital's registry data from neonatal intensive care unit (NICU) during 2009-2014...
January 18, 2017: European Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28101622/-use-of-vasopressors-and-inotropics-in-cardiogenic-shock
#14
H Lemm, S Dietz, M Janusch, M Buerke
Vasoactive drugs and inotropic agents are important for the hemodynamic management of cardiogenic shock. In this article the use of different vasoactive and ionotropic drugs in cardiogenic shock is presented. Hemodynamic management during cardiogenic shock occurs after initial moderate volume delivery by dobutamine to increase inotropism. If adequate perfusion pressures are not achieved norepinephrine is administered. If a sufficient increase in cardiac performance can still not be achieved by the treatment, administration of levosimendan or phosphodiesterase (PDE) inhibitors may be necessary...
January 18, 2017: Herz
https://www.readbyqxmd.com/read/28101614/-dermatological-topical-and-systemic-therapy-during-pregnancy
#15
REVIEW
S Grunewald, P Staubach
During pregnancy, a successful and safe therapeutic management of patients is possible to lower the burden of disease. Often topical therapy in combination with intensive basic skin care is sufficient. Drug therapies may also be used, most often for systemic diseases such as autoimmune diseases or psoriasis. An early change in therapy is also key during planned pregnancies so that treatments can be switched, adjusted, reduced or closely monitored. Another point to consider is to keep drug dosing as low as possible (without occlusion in local therapy) or short termed (with the exception of autoimmune or malignant diseases)...
January 18, 2017: Der Hautarzt; Zeitschrift Für Dermatologie, Venerologie, und Verwandte Gebiete
https://www.readbyqxmd.com/read/28101573/combining-doxorubicin-with-a-phenolic-extract-from-flaxseed-oil-evaluation-of-the-effect-on-two-breast-cancer-cell-lines
#16
Eliana Guerriero, Angela Sorice, Francesca Capone, Gabriella Storti, Giovanni Colonna, Gennaro Ciliberto, Susan Costantini
Breast cancer is one of the most frequently diagnosed forms of cancer and different treatments are used to block its progression. However, it still represents a very common cause of death in women. Doxorubicin (Dox) is reported as an effective agent in breast cancer treatment nonetheless it induces many side‑effects. For this reason, many laboratories are engaged in understanding how it is possible to decrease the drug concentration, considering that one of the possible solutions is to use drug synergy, combining it with natural substances...
February 2017: International Journal of Oncology
https://www.readbyqxmd.com/read/28101470/protective-roles-of-n-acetyl-cysteine-and-or-taurine-against-sumatriptan-induced-hepatotoxicity
#17
Javad Khalili Fard, Hossein Hamzeiy, Mohammadreza Sattari, Mohammad Ali Eghbal
Purpose: Triptans are the drug category mostly prescribed for abortive treatment of migraine. Most recent cases of liver toxicity induced by triptans have been described, but the mechanisms of liver toxicity of these medications have not been clear. Methods: In the present study, we obtained LC50 using dose-response curve and investigated cell viability, free radical generation, lipid peroxide production, mitochondrial injury, lysosomal membrane damage and the cellular glutathione level as toxicity markers as well as the beneficial effects of taurine and/or N-acetyl cysteine in the sumatriptan-treated rat parenchymal hepatocytes using accelerated method of cytotoxicity mechanism screening...
December 2016: Advanced Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28101469/concurrent-inflammation-augments-antimalarial-drugs-induced-liver-injury-in-rats
#18
Hossein Niknahad, Reza Heidari, Roya Firuzi, Farzaneh Abazari, Maral Ramezani, Negar Azarpira, Massood Hosseinzadeh, Asma Najibi, Arastoo Saeedi
Purpose: Accumulating evidence suggests that drug exposure during a modest inflammation induced by bacterial lipopolysaccharide (LPS) might increase the risk of drug-induced liver injury. The current investigation was designed to test if antimalarial drugs hepatotoxicity is augmented in LPS‑treated animals. Methods: Rats were pre-treated with LPS (100 µg/kg, i.p). Afterward, non-hepatotoxic doses of amodiaquine (25, 50 and 100 mg/kg, oral) and chloroquine (25, 50 and 100 mg/kg, oral) were administered. Results: Interestingly, liver injury was evident only in animals treated with both drug and LPS as estimated by pathological changes in serum biochemistry (ALT, AST, LDH, and TNF-α), and liver tissue (severe hepatitis, endotheliitis, and sinusoidal congestion)...
December 2016: Advanced Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28101344/evaluation-of-pharmacological-relaxation-effect-of-the-natural-product-naringin-on-in-vitro-cultured-airway-smooth-muscle-cells-and-in-vivo-ovalbumin-induced-asthma-balb-c-mice
#19
Yue Wang, Yun Lu, Mingzhi Luo, Xiaohao Shi, Yan Pan, Huilong Zeng, Linhong Deng
Asthma has become a common chronic respiratory disease worldwide and its prevalence is predicted to continue increasing in the next decade, particularly in developing countries. A key component in asthma therapy is to alleviate the excessive bronchial airway narrowing ultimately due to airway smooth muscle contraction, which is often facilitated by a smooth muscle relaxant, such as the β2-adrenergic agonists. Recently, bitter taste receptor (TAS2R) agonists, including saccharin and chloroquine, have been found to potently relax the airway smooth muscle cells (ASMCs) via intracellular Ca(2+) signaling...
December 2016: Biomedical Reports
https://www.readbyqxmd.com/read/28101320/variation-in-dose-and-plasma-level-of-lamotrigine-in-patients-discharged-from-a-mental-health-trust
#20
Petrina Douglas-Hall, Olubanke Dzahini, Fiona Gaughran, Ahmed Bile, David Taylor
BACKGROUND: The objectives of this study were to investigate the dose of lamotrigine when prescribed with an enzyme inhibitor or enzyme inducer in patients discharged from a mental health trust and to determine the corresponding lamotrigine plasma concentrations and the factors that may affect these. METHODS: All patients discharged on lamotrigine between October 2007 and September 2012 were identified using the pharmacy dispensing database. We recorded demographic details, lamotrigine dose and plasma levels and coprescribed medication...
January 2017: Therapeutic Advances in Psychopharmacology
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