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https://www.readbyqxmd.com/read/29786965/l-and-d-threo-ethylphenidate-concentrations-pharmacokinetics-and-pharmacodynamics-in-horses
#1
Heather K Knych, Dan S McKemie, Kelsey Seminoff, Petra Hartmann, Lynn Hovda, Dionne Benson
Ethylphenidate is a psychostimulant and analogue of the commonly prescribed compound, methylphenidate (Ritalin®). There are a limited number of studies describing the disposition and pharmacologic/toxicological effects of ethylphenidate in any species. The abuse potential in equine athletes along with the limited data available regarding administration in horses necessitates further study. The objectives of the current study were to describe drug concentrations, develop an analytical method that could be used to regulate its use and describe the pharmacodynamic effects of ethylphenidate in horses...
May 22, 2018: Drug Testing and Analysis
https://www.readbyqxmd.com/read/29786857/effect-of-oatp1b1-1b3-inhibitor-gdc-0810-on-the-pharmacokinetics-of-pravastatin-and-coproporphyrin-i-iii-in-healthy-female-subjects
#2
Lichuan Liu, Sravanthi Cheeti, Kenta Yoshida, Edna Choo, Eugene Chen, Buyun Chen, Mary Gates, Stina Singel, Roland Morley, Joseph Ware, Srikumar Sahasranaman
Developed as an oral anticancer drug to treat estrogen receptor-positive breast cancer, GDC-0810 was shown to be a potent inhibitor of organic anion-transporting polypeptide 1B1 and 1B3 (OATP1B1/1B3) from an in vitro assay. A clinical study was conducted to assess the drug-drug interaction potential between GDC-0810 and pravastatin, which is a relatively selective and sensitive OATP1B1/1B3 substrate. Fifteen healthy female subjects of non-childbearing potential were enrolled in the study. On day 1 in period 1, a single 10-mg dose of pravastatin was administered to all subjects...
May 22, 2018: Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/29786530/meta-analysis-of-safety-and-efficacy-of-oral-anti-coagulants-in-patients-requiring-catheter-ablation-for-atrial-fibrillation
#3
Hammad Rahman, Safi U Khan, Michael DePersis, Tehseen Hammad, Fahad Nasir, Edo Kaluski
BACKGROUND: The ideal oral anticoagulant agent during catheter ablation (CA) for atrial fibrillation (AF) remained unclear. HYPOTHESIS: Novel oral anticoagulants (NOACs) are safer and effective compared to uninterrupted vitamin K antagonists (U-VKA) among patients requiring CA for AF. METHODS: Four randomized controlled trials (RCTs) and 9 observational studies (OS) were selected using PubMed/Medline, EMBASE and the CENTRAL data bases (Inception-December-2017)...
May 9, 2018: Cardiovascular Revascularization Medicine: Including Molecular Interventions
https://www.readbyqxmd.com/read/29786508/-use-of-the-evalobs-%C3%A2-adherence-scale-in-an-unselected-french-population-of-treated-subjects-with-antihypertensive-hypolipemiants-or-oral-antidiabetics-medications-the-flahs-2017-adherence-survey
#4
X Girerd, O Hanon, B Vaïsse
OBJECTIVE: A Visual Analog Scale (VAS) is useful for diagnosing medication nonadherence and its validity has been evaluated using electronic pillbox as the gold standard. We have developed the EvaLobs® scale for use on paper or on smartphone and the aim of the study was to administrate the scale among FLAHS 2017 participants treated for an hypertension, a dyslipidemia or diabetes. In subjects treated with antihypertensive medications, participants completed the 6-item Girerd Scale and EvaLobs® ...
May 18, 2018: Annales de Cardiologie et D'angéiologie
https://www.readbyqxmd.com/read/29786006/rebound-inflammation-after-an-intravitreal-injection-in-vogt-koyanagi-harada-syndrome
#5
Richa Ranjan, Manisha Agarwal
A 43-year-old male with chronic Vogt-Koyanagi-Harada syndrome (VKH) presented with subfoveal choroidal neovascular membrane (CNVM) in the right eye with no evidence of active inflammation. He underwent intravitreal bevacizumab and dexamethasone injections. Postinjection he developed fresh keratic precipitates and exudative retinal detachment (RD). He received two more bevacizumab injections with oral corticosteroids and immunosuppressants causing resolution of exudative RD with scarred CNVM. We report this case to highlight that intravitreal injection may act as a trigger for rebound inflammation in VKH patients and may require anti-inflammatory drugs to be started even in the absence of an active inflammation...
June 2018: Indian Journal of Ophthalmology
https://www.readbyqxmd.com/read/29785837/more-patients-reach-glycaemic-control-with-fixed-ratio-combination-of-insulin-glargine-and-lixisenatide-iglarlixi-than-with-basal-insulin-at-12-weeks-of-treatment-a-post-hoc-time-to-control-analysis-of-lixilan-o-and-lixilan-l
#6
Juan Frias, Manuel Puig Domingo, Luigi Meneghini, Raffaele Napoli, Minzhi Liu, Erika Soltes Rak, Vanita R Aroda
This post hoc analysis of two 30-week clinical trials compared efficacy and hypoglycaemia outcomes at early study visits with iGlarLixi (insulin glargine U100 [iGlar] and lixisenatide) vs iGlar alone in patients with type 2 diabetes (T2D) uncontrolled on oral antidiabetic drugs (OADs; LixiLan-O) or basal insulin (LixiLan-L). Time to control, defined as days to achieve glycated haemoglobin (HbA1c) <7% or fasting plasma glucose (FPG) ≤7.2 mmol/L, was estimated using the Kaplan-Meier method. In LixiLan-O and -L, 60% and 46% of patients, respectively, reached HbA1c <7% with iGlarLixi at 12 weeks, vs 45% and 24%, respectively, with iGlar...
May 21, 2018: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/29785666/evaluation-of-ostarine-as-a-selective-androgen-receptor-modulator-in-a-rat-model-of-postmenopausal-osteoporosis
#7
D B Hoffmann, M Komrakova, S Pflug, M von Oertzen, D Saul, L Weiser, T A Walde, M Wassmann, A F Schilling, W Lehmann, S Sehmisch
Selective androgen receptor modulators (SARMs) have shown beneficial effects on muscle wasting, general physical function and bone properties in male mammals. However, data on the effects of SARMs in postmenopausal osteoporotic bone are scarce. We evaluated the effects of the SARM drug ostarine on postmenopausal osteoporotic bone in a rat osteoporosis model. Ovariectomy was performed on 46 of 56 3-month-old female Sprague-Dawley rats. Eight weeks after ovariectomy, ostarine was orally administered daily for 5 weeks in dosages of 0...
May 21, 2018: Journal of Bone and Mineral Metabolism
https://www.readbyqxmd.com/read/29785574/in-situ-nanostructured-hydrogel-of-resveratrol-for-brain-targeting-in-vitro-in-vivo-characterization
#8
Amarjitsing Rajput, Aditi Bariya, Ahmed Allam, Sarah Othman, Shital B Butani
The purpose of conducting the present research work was to develop resveratrol nanostructured in situ gel for the treatment of Alzheimer's disease. Resveratrol loaded lipid carrier was prepared by melt emulsification-probe sonication method, and the final product was evaluated for particle size (132 ± 11.90 nm), polydispersity index (0.209 ± 0.005), zeta potential (- 23 ± 3.79 mV), drug loading (9.26 ± 3.79%), and entrapment efficiency (74 ± 11.40%). Following incorporation of the resveratrol nanostructured lipid carrier in gellan gum and xanthan gum, in situ gel was formulated and characterized...
May 21, 2018: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/29785508/lacosamide-a-review-in-focal-onset-seizures-in-patients-with-epilepsy
#9
Sheridan M Hoy
Lacosamide (Vimpat® ) is a functionalized amino acid (available orally and intravenously) approved in the EU and the USA for use as monotherapy and adjunctive therapy for the treatment of focal-onset seizures in adults, adolescents and children aged ≥ 4 years with epilepsy. In adults and adolescents (aged ≥ 16 years), oral lacosamide as adjunctive therapy to other antiepileptic drugs was generally effective in reducing seizure frequency during short-term (up to 18 weeks) treatment, with efficacy sustained over the longer-term (up to 8 years)...
May 21, 2018: CNS Drugs
https://www.readbyqxmd.com/read/29785276/food-intake-attenuates-the-drug-interaction-between-new-quinolones-and-aluminum
#10
Ayuko Imaoka, Kosuke Abiru, Takeshi Akiyoshi, Hisakazu Ohtani
Background: Intestinal absorption of new quinolones is decreased by oral administration of polyvalent metal cations. Some clinical studies have demonstrated this drug - drug interaction is more prominent under fasted condition. However, the effect of food intake on the extent of drug - drug interaction between new quinolones and metal cations remains to be investigated quantitatively and systematically. The aim of this study was to develop an animal model that enables to evaluate the effect of food intake on the extent of drug - drug interaction in the gastrointestinal tract by chelation and to apply the model to evaluate quantitatively the effect of food intake on the drug - drug interaction between two new quinolones, ofloxacin or ciprofloxacin and sucralfate...
2018: Journal of Pharmaceutical Health Care and Sciences
https://www.readbyqxmd.com/read/29784841/the-metabolism-of-piperaquine-to-its-antiplasmodial-metabolites-and-their-pharmacokinetic-profiles-in-healthy-volunteers
#11
Huixiang Liu, Hongchang Zhou, Tianyu Cai, Aijuan Yang, Meitong Zang, Jie Xing
As a partner antimalarial for artemisinin drug-based combination therapy (ACT), piperaquine (PQ) can be metabolized into two major metabolites, including piperaquine N -oxide (M1) and N , N -dioxide (M2). To better understand the antimalarial potency of PQ, the antimalarial activity of PQ metabolites (M1 and M2) was studied in vitro ( Plasmodium strains Pf 3D7 and Pf Dd2) and in vivo (murine Plasmodium yoelii ) in this study. The recrudescence and survival time of infected mice were also recorded after drug treatment...
May 21, 2018: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/29784509/lactoferrin-modified-betulinic-acid-loaded-plga-nanoparticles-are-strong-anti-leishmanials
#12
Asim Halder, Divanshu Shukla, Suvadra Das, Partha Roy, Arup Mukherjee, Bhaskar Saha
Visceral Leishmaniasis (VL), caused by the protozoan parasite Leishmania donovani, is a potentially fatal disease. The only orally bioavailable drug miltefosine is toxic and the effective liposomal Amphotericin B (AmBisome) is limited by its prohibitive cost and requirement for parenteral administration. Therefore, finding a new potential drug candidate and an alternative delivery system is imperative. We report that Betulinic acid (BA), a pentacyclic triterpenoid from Betula alba bark, was loaded onto uniformly spherical PLGA nanoparticles (BANPs; diameter 187...
May 18, 2018: Cytokine
https://www.readbyqxmd.com/read/29784018/adding-colchicine-to-immunosuppressive-treatments-a-potential-option-for-biologics-refractory-adult-onset-still-s-disease
#13
Tomoyuki Asano, Makiko Yashiro Furuya, Shuzo Sato, Hiroko Kobayashi, Hiroshi Watanabe, Eiji Suzuki, Kiyoshi Migita
BACKGROUND: Adult-onset Still's disease (AOSD) is a rare inflammatory disorder characterized by the classical triad of daily spiking fever, arthritis, and typical salmon-colored rash. Resistance to first-line corticosteroids and second-line disease modified anti-rheumatic-drugs defines refractory AOSD, which mostly includes the polycyclic or chronic courses of the disease. Anti-cytokine therapies are recommended in AOSD patients who are refractory to traditional treatments. This is the first report on the efficacy of colchicine in a patient with AOSD which was refractory to immunosuppressive treatments including biologics...
May 21, 2018: BMC Research Notes
https://www.readbyqxmd.com/read/29783900/the-efficacy-comparison-of-citalopram-fluoxetine-and-placebo-on-motor-recovery-after-ischemic-stroke-a-double-blind-placebo-controlled-randomized-controlled-trial
#14
Marjan Asadollahi, Mahtab Ramezani, Ziba Khanmoradi, Ehsan Karimialavijeh
OBJECTIVE: The present study aimed to assess the effectiveness of oral citalopram, compared with fluoxetine and a placebo, in patients with post-stroke motor disabilities. DESIGN: A randomized double-blind placebo-controlled clinical trial was conducted between January 2015 and January 2016. SETTING: The neurology department of a university-affiliated urban hospital in Tehran, Iran. SUBJECTS: Ninety adult patients with acute ischemic stroke, hemiplegia, or hemiparesis and a Fugl-Meyer Motor Scale score of below 55 were included...
May 1, 2018: Clinical Rehabilitation
https://www.readbyqxmd.com/read/29783757/a-repurposed-drug-for-brain-cancer-enhanced-atovaquone-amorphous-solid-dispersion-by-combining-a-spontaneously-emulsifying-component-with-a-polymer-carrier
#15
Hiroyuki Takabe, Zachary N Warnken, Yajie Zhang, Daniel A Davis, Hugh D C Smyth, John G Kuhn, Steve Weitman, Robert O Williams Iii
Glioblastoma multiforme (GBM) is the most common and lethal central nervous system tumor. Recently, atovaquone has shown inhibition of signal transducer and activator transcription 3, a promising target for GBM therapy. However, it is currently unable to achieve therapeutic drug concentrations in the brain with the currently reported and marketed formulations. The present study sought to explore the efficacy of atovaquone against GBM as well as develop a formulation of atovaquone that would improve oral bioavailability, resulting in higher amounts of drug delivered to the brain...
May 19, 2018: Pharmaceutics
https://www.readbyqxmd.com/read/29783755/a-miniaturized-extruder-to-prototype-amorphous-solid-dispersions-selection-of-plasticizers-for-hot-melt-extrusion
#16
Matthias E Lauer, Reto Maurer, Anne T De Paepe, Cordula Stillhart, Laurence Jacob, Rajesh James, Yuki Kojima, Rene Rietmann, Tom Kissling, Joost A van den Ende, Sabine Schwarz, Olaf Grassmann, Susanne Page
Hot-melt extrusion is an option to fabricate amorphous solid dispersions and to enhance oral bioavailability of poorly soluble compounds. The selection of suitable polymer carriers and processing aids determines the dissolution, homogeneity and stability performance of this solid dosage form. A miniaturized extrusion device (MinEx) was developed and Hypromellose acetate succinate type L (HPMCAS-L) based extrudates containing the model drugs neurokinin-1 (NK1) and cholesterylester transfer protein (CETP) were manufactured, plasticizers were added and their impact on dissolution and solid-state properties were assessed...
May 19, 2018: Pharmaceutics
https://www.readbyqxmd.com/read/29782992/single-ultra-high-dose-cholecalciferol-to-prevent-vitamin-d-deficiency-in-pediatric-hematopoietic-stem-cell-transplantation
#17
Gregory Wallace, Sonata Jodele, Kasiani C Myers, Christopher E Dandoy, Javier El-Bietar, Adam Nelson, Ashley Teusink-Cross, Pooja Khandelwal, Cynthia Taggart, Catherine M Gordon, Stella M Davies, Jonathan C Howell
BACKGROUND: Vitamin D (vitD) deficiency is prevalent among childhood hematopoietic stem cell transplantation (HSCT) recipients and associated with inferior transplant survival at 100 days after transplantation. Achieving and maintaining therapeutic vitD levels in HSCT recipients is extremely challenging in the first 3-6 months after transplant due to poor compliance in the setting of mucositis, and concomitant use of critical transplant drugs that interfere with vitD absorption. We sought to evaluate the safety and efficacy of a single, ultra-high dose of vitD given prior to childhood HSCT to maintain levels in a therapeutic range during the peri-transplantation period...
May 18, 2018: Biology of Blood and Marrow Transplantation
https://www.readbyqxmd.com/read/29782971/pharmaceutical-grade-oral-films-as-substrates-for-printed-medicine
#18
M Wimmer-Teubenbacher, C Planchette, H Pichler, D Markl, W K Hsiao, A Paudel, S Stegemann
In contact-less printing, such as piezo-electric drop on demand printing used in the study, the drop formation process is independent of the substrate. This means that having developed a printable formulation, printed pharmaceutical dosage forms can be obtained on any pharmaceutical grade substrate, such as polymer-based films. In this work we evaluated eight different oral films based on their suitability as printing substrates for sodium picosulfate. The different polymer films were compared regarding printed spot morphology, chemical stability and dissolution profile...
May 18, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29782822/simultaneous-determination-of-intestinal-permeability-and-potential-drug-interactions-of-complex-mixtures-using-caco-2-cells-and-high-resolution-mass-spectrometry-studies-with-rauwolfia-serpentina-extract
#19
Thomas J Flynn, Sanah N Vohra
Caco-2 cells are a commonly used model for estimating the intestinal bioavailability of single chemical entity pharmaceuticals. Caco-2 cells, when induced with calcitriol, also express other biological functions such as phase I (CYP) and phase II (glucuronosyltransferases) drug metabolizing enzymes which are relevant to drug-supplement interactions. Intestinal bioavailability is an important factor in the overall safety assessment of products consumed orally. Foods, including herbal dietary supplements, are complex substances with multiple chemical components...
May 18, 2018: Chemico-biological Interactions
https://www.readbyqxmd.com/read/29782805/maintaining-supersaturation-of-nimodipine-by-pvp-with-or-without-the-presence-of-sodium-lauryl-sulfate-and-sodium-taurocholate
#20
Yipshu Pui, Yuejie Chen, Huijun Chen, Shan Wang, Chengyu Liu, Wouter Tonnis, Linc Chen, Peter Serno, Stefan Bracht, Feng Qian
Amorphous solid dispersion (ASD) is one of the most versatile supersaturating drug delivery system to improve the dissolution rate and oral bioavailability of poorly water soluble drugs. PVP based ASD formulation of nimodipine (NMD) has been marketed and effectively used in clinic for nearly 30 years, yet the mechanism by which PVP maintains the supersaturation and subsequently improves the bioavailability of NMD was rarely investigated. In this research, we first studied the molecular interactions between NMD and PVP by solution NMR using CDCl3 as the solvent, and drug-polymer Flory-Huggins interaction parameter...
May 21, 2018: Molecular Pharmaceutics
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