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https://www.readbyqxmd.com/read/28434133/stiripentol-in-the-management-of-epilepsy
#1
REVIEW
Katherine C Nickels, Elaine C Wirrell
Stiripentol is a structurally unique antiepileptic drug that has several possible mechanisms of action, including diverse effects on the gamma-aminobutyric acid (GABA)-A receptor and novel inhibition of lactate dehydrogenase. Because of its inhibition of several cytochrome P450 enzymes, it has extensive pharmacokinetic interactions, which often necessitates reduction in doses of certain co-therapies, particularly clobazam. Stiripentol also has a neuroprotective action, by reducing calcium-mediated neurotoxicity...
April 22, 2017: CNS Drugs
https://www.readbyqxmd.com/read/28433587/pharmacokinetic-and-toxicology-comparator-testing-of-biosimilar-drugs-assessing-need
#2
Paul Baldrick
A key element in the development of a biosimilar molecule is the comparability of the biological activity/nonclinical similarity to the innovator drug. Although some regulatory guidelines are encouraging little or no in vivo testing, currently a common practice is to perform at least one toxicology and/or one pharmacokinetic (PK) study to assess if any different findings occur for in-life, clinical pathology and histopathological parameters or in exposure. An exercise was performed in which the results of such testing were evaluated...
April 19, 2017: Regulatory Toxicology and Pharmacology: RTP
https://www.readbyqxmd.com/read/28433511/design-synthesis-and-pharmacological-evaluation-of-4-azolyl-benzamide-derivatives-as-novel-gpr52-agonists
#3
Kazuyuki Tokumaru, Yoshiteru Ito, Izumi Nomura, Takashi Nakahata, Yuji Shimizu, Emi Kurimoto, Kazunobu Aoyama, Kazuyoshi Aso
G protein-coupled receptor 52 (GPR52) agonists are expected to improve the symptoms of psychiatric disorders. During exploration for a novel class of GPR52 agonists with good pharmacokinetic profiles, we synthesized 4-(3-(3-fluoro-5-(trifluoromethyl)benzyl)-5-methyl-1H-1,2,4-triazol-1-yl)-2-methylbenzamide (4u; half maximal effective concentration (EC50)=75nM, maximal response (Emax)=122%) starting from a high-throughput screening hit 3 (EC50=470nM, Emax=56%). The structural features of a reported GPR52 agonist were applied to 3, led to design 4-azolylbenzamides as novel GPR52 agonists...
April 1, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28432941/validation-of-a-spe-hplc-uv-method-for-the-quantification-of-a-new-er-specific-photosensitizer-or-141-in-blood-serum-using-total-error-concept
#4
Emilie Bony, Yohan Mace, Adán Pinto, David Delvaux, Robert Kiss, Olivier Riant, Olivier Feron, Joëlle Quetin-Leclercq
The aim of this work is to develop the first validated HPLC-UV method quantification in blood serum for a new endoplasmic reticulum (ER)-specific benzophenazine photosensitizer (OR-141). A fast solid phase extraction (SPE) cleaning sample procedure was achieved on C18 encapped (ec) SPE cartridges and the separation was performed on a RP-18e column (5μM) using an isocratic elution with methanol. The method has been fully validated according to accuracy profiles based on total error and tolerance intervals. Calibration was performed in the matrix and trueness (<4...
April 13, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28432800/effect-of-n-methyl-deuteration-on-pharmacokinetics-and-pharmacodynamics-of-enzalutamide
#5
Xuehai Pang, Lingling Peng, Yuanwei Chen
Enzalutamide, a 2nd generation antiandrogen, has been developed for the treatment of CRPC. We synthesized the deuterated analogues 6 and found that it showed higher drug exposure and thus stronger anti-tumor potency in preclinical settings. Compound 6 is being developed clinically for the potential to be differentiated from enzalutamide through reduced dosages and a higher safety margin.
April 22, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/28432741/pharmacokinetic-and-pharmacodynamic-effects-of-two-omeprazole-formulations-on-stomach-ph-and-gastric-ulcer-scores
#6
S Raidal, F M Andrews, S G Nielsen, G Trope
REASONS FOR PERFORMING THE STUDY: Limited data are available on the relative pharmacokinetics and pharmacodynamics of different omeprazole formulations. OBJECTIVES: To compare pharmacokinetic and pharmacodynamic effects of a novel omeprazole formulation against a currently registered product. STUDY DESIGN: Masked two period, two treatment crossover. METHODS: Twelve clinically healthy horses were studied over two 6-day treatment periods...
April 22, 2017: Equine Veterinary Journal
https://www.readbyqxmd.com/read/28432691/tenapanor-administration-and-the-activity-of-the-h-coupled-transporter-pept1-in-healthy-volunteers
#7
Susanne Johansson, David P Rosenbaum, Johan Palm, Bergur Stefansson, Mikael Knutsson, Eleanor A Lisbon, Constanze Hilgendorf
AIM: Tenapanor (RDX5791/AZD1722), an inhibitor of gastrointestinal Na(+) /H(+) exchanger NHE3, is being evaluated for the treatment of patients with constipation-predominant irritable bowel syndrome and the treatment of hyperphosphataemia in patients with chronic kidney disease on dialysis. By reducing intestinal H(+) secretion, inhibition of NHE3 by tenapanor could indirectly affect H(+) -coupled transporter activity, leading to drug-drug interactions. We investigated the effect of tenapanor on the activity of the H(+) -coupled peptide transporter PepT1 via assessment of the pharmacokinetics of cefadroxil - a compound transported by PepT1 - in healthy volunteers...
April 22, 2017: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28432615/fabrication-physicochemical-characterization-and-performance-evaluation-of-biodegradable-polymeric-microneedle-patch-system-for-enhanced-transcutaneous-flux-of-high-molecular-weight-therapeutics
#8
Viral Shah, Bijaya Krushna Choudhury
A revolutionary paradigm shift is being observed currently, towards the use of therapeutic biologics for disease management. The present research was focused on designing an efficient dosage form for transdermal delivery of α-choriogonadotropin (high molecular weight biologic), through biodegradable polymeric microneedles. Polyvinylpyrrolidone-based biodegradable microneedle arrays loaded with high molecular weight polypeptide, α-choriogonadotropin, were fabricated for its systemic delivery via transdermal route...
April 21, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28432479/pharmacokinetics-and-efficacy-of-an-ivermectin-implant-for-long-term-prevention-of-dirofilaria-immitis-infection-in-dogs
#9
Marco Genchi, Anne Geneteau, Patrick Forget, Romain Delcombel, Claudio Genchi
An exploratory study was carried out to assess the in vivo efficacy of different prototypes of subcutaneous implants containing ivermectin (IVM) for the prevention of canine Dirofilaria immitis infection. The implants consisted of an ethylcellulose matrix containing IVM (3.0, 4.5, and 6.0 mg/implant; from 0.29 to 0.63 mg/kg bw) as active ingredient designed to release approximately 0.1 ng of IVM/mL in the plasma for at least 12 months. Six dogs were implanted on day -365. On day -12, three heartworm-free dogs were included in the study as a control group...
April 22, 2017: Parasitology Research
https://www.readbyqxmd.com/read/28432468/population-pharmacokinetics-of-intravenous-acetaminophen-in-japanese-patients-undergoing-elective-surgery
#10
Tsuyoshi Imaizumi, Shinju Obara, Midori Mogami, Yuzo Iseki, Makiko Hasegawa, Masahiro Murakawa
INTRODUCTION: Intravenous (i.v.) acetaminophen is administered during surgery for postoperative analgesia. However, little information is available on the pharmacokinetics of i.v. acetaminophen in Japanese patients undergoing surgery under general anesthesia. METHODS: The study was approved by the Institutional Review Board and registered at UMIN-CTR (UMIN000013418). Patients scheduled to undergo elective surgery under general anesthesia were enrolled after obtaining written informed consent...
April 21, 2017: Journal of Anesthesia
https://www.readbyqxmd.com/read/28432176/a-phase-i-study-of-the-cdk4-6-inhibitor-ribociclib-lee011-in-pediatric-patients-with-malignant-rhabdoid-tumors-neuroblastoma-and-other-solid-tumors
#11
Birgit Geoerger, Franck Bourdeaut, Steven G DuBois, Matthias Fischer, James I Geller, Nicholas G Gottardo, Aurélien Marabelle, Andrew D J Pearson, Shakeel Modak, Thomas Cash, Giles W Robinson, Marlyane Motta, Alessandro Matano, Suraj G Bhansali, Jason R Dobson, Sudha Parasuraman, Susan N Chi
Purpose: The cyclin-dependent kinase (CDK) 4/6 inhibitor, ribociclib (LEE011), displayed preclinical activity in neuroblastoma and malignant rhabdoid tumor (MRT) models. In this phase I study, the maximum tolerated dose (MTD) and recommended phase II dose (RP2D), safety, pharmacokinetics (PK), and preliminary activity of single-agent ribociclib were investigated in pediatric patients with neuroblastoma, MRT, or other cyclin D-CDK4/6-INK4-retinoblastoma pathway-altered tumors.Experimental Design: Patients (aged 1-21 years) received escalating once-daily oral doses of ribociclib (3-weeks-on/1-week-off)...
April 21, 2017: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
https://www.readbyqxmd.com/read/28432048/solithromycin-a-novel-ketolide-antibiotic
#12
Michael J Buege, Jack E Brown, Samuel L Aitken
PURPOSE: The pharmacology, pharmacokinetics, pharmacodynamics, antimicrobial activity, clinical safety, and current regulatory status of solithromycin are reviewed. SUMMARY: Solithromycin is a novel ketolide antibiotic developed for the treatment of community-acquired bacterial pneumonia (CABP). Its pharmacologic, pharmacokinetic, and pharmacodynamic properties provide activity against a broad range of intracellular organisms, including retained activity against pathogens displaying various mechanisms of macrolide resistance...
April 21, 2017: American Journal of Health-system Pharmacy: AJHP
https://www.readbyqxmd.com/read/28431964/microvillus-specific-protein-tyrosine-phosphatase-sap-1-plays-a-role-in-regulating-the-intestinal-paracellular-transport-of-macromolecules
#13
Shingo Mori, Noriyasu Kamei, Yoji Murata, Kozo Takayama, Takashi Matozaki, Mariko Takeda-Morishita
The stomach cancer associated protein tyrosine phosphatase 1 (SAP-1) is a receptor-type protein tyrosine phosphatase that is specifically expressed on the apical membrane of the intestinal epithelium. SAP-1 is known to maintain the balance of phosphorylation of proteins together with protein kinases, however, its biological function and impact on pharmacokinetics in the intestine remain unclear. The present study, therefore, aimed to clarify the relationship between SAP-1 and the intestinal absorption behaviors of typical transporter substrates and macromolecules...
April 18, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28431781/clenbuterol-hydrochloride
#14
Abdulrahman A Al-Majed, Nasr Y Khalil, Ibraheem Khbrani, Hatem A Abdel-Aziz
Clenbuterol (Broncodil and trade) is a direct-acting sympathomimetic agent with mainly beta-adrenergic activity and a selective action on β2 receptors (a β2 agonist). It has properties similar to those of salbutamol. It is used as a bronchodilator in the management of reversible airways obstruction, as in asthma and in certain patients with chronic obstructive pulmonary disease. The uses, applications, and the synthetic pathways of this drug are outlined. Physical characteristics including: ionization constant, solubility, X-ray powder diffraction pattern, thermal methods of analysis, UV spectrum, IR spectrum, mass spectrum are all produced...
2017: Profiles of Drug Substances, Excipients, and related Methodology
https://www.readbyqxmd.com/read/28431777/lomefloxacin
#15
Reem I Al-Wabli
Lomefloxacin is a second-generation difluorinated broad-spectrum quinolone antibiotic. It is used for the treatment of bronchitis, urinary tract infection, conjunctivitis, otitis externa, and otitis media. A comprehensive profile was performed on lomefloxacin including nomenclature, formulae, elemental composition appearance, and physical characteristics. Spectral methods including ultraviolet spectrum, vibrational spectrum, (1)H and (13)C nuclear magnetic resonance one- and two-dimensional spectra, and mass spectrum were used for both identification and analysis of the drug...
2017: Profiles of Drug Substances, Excipients, and related Methodology
https://www.readbyqxmd.com/read/28431776/gliclazide
#16
Fatmah A M Al-Omary
Gliclazide is a second-generation oral hypoglycemic drug used for the treatment of noninsulin-dependent diabetes mellitus. It belongs to the sulfonylurea class that stimulates insulin secretion from pancreatic β-cells by inhibiting ATP-dependent potassium channels. Gliclazide also possesses unique antioxidant properties and other beneficial hemobiological effects. This profile represents a comprehensive description of the physical properties, chemical synthesis, spectroscopic characterization (FTIR, (1)H NMR, (13)C NMR, UV, and single-crystal X-ray), methods of analysis, pharmacological actions, and pharmacokinetic and pharmacodynamic properties of the title drug...
2017: Profiles of Drug Substances, Excipients, and related Methodology
https://www.readbyqxmd.com/read/28431775/cinacalcet-hydrochloride
#17
Gamal A E Mostafa, Abdullah A Al-Badr
Cinacalcet hydrochloride is a calcimimetic agent that increases the sensitivity to the extracellular calcium of the calcium-sensing receptors of the parathyroid gland which regulates parathyroid hormone secretion. This comprehensive profile on cinacalcet hydrochloride starts with a description: nomenclature, formulae, chemical structure, elemental composition, and appearance. The uses and applications of the drug are included. The methods of preparation of cinacalcet hydrochloride are described and their respective schemes are outlined...
2017: Profiles of Drug Substances, Excipients, and related Methodology
https://www.readbyqxmd.com/read/28431749/pharmacological-advances-in-the-multimodal-management-of-perioperative-analgesia
#18
M Matute Crespo, A Montero Matamala
The concept of multimodal analgesia is currently widespread in our clinical practice. The aim of multimodal analgesia is to reduce the side effects derived from the drugs or techniques used for the control of pain together with greater effectiveness (combination of multiple mechanisms of action) with the maximum efficiency, that is, to combine different pharmacodynamics (synergistic or additive effects) and pharmacokinetics, in the context of a predictable acute pain model, thus allowing a prior strategy such as the model of acute postoperative pain...
April 18, 2017: Revista Española de Anestesiología y Reanimación
https://www.readbyqxmd.com/read/28431340/first-macrocyclic-3-rd-generation-alk-inhibitor-for-treatment-of-alk-ros1-cancer-clinical-and-designing-strategy-update-of-lorlatinib
#19
REVIEW
Sulman Basit, Zaman Ashraf, Kwangho Lee, Muhammad Latif
Non-small cell lung cancers (NSCLC) harboring anaplastic lymphoma kinase (ALK) gene rearrangements invariably develop resistance to 2(nd)-generation ALK inhibitors. Lorlatinib (PF-06463922) (6) is a 3(rd)-generation macrocyclic ALK-TKI that demonstrates many advantages over 2(nd)-generation ALK inhibitors. Lorlatinib has demonstrated decent kinase selectivity, promising pharmacokinetic profile, selective brain-penetration and strong antiproliferative activity in several ALK/ROS1-driven tumor models. The current review describes the activity spectrum, key events from discovery to clinical applications and the evidences that lorlatinib acts as an ALK/ROS1 inhibitor in clinical settings...
April 13, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28431329/stealth-recombinant-human-serum-albumin-nanoparticles-conjugating-5-fluorouracil-augmented-drug-delivery-and-cytotoxicity-in-human-colon-cancer-ht-29-cells
#20
Ankita Sharma, Amanpreet Kaur, Upendra Kumar Jain, Ramesh Chandra, Jitender Madan
BACKGROUND AND OBJECTIVE: 5-Fluorouracil (5-FU) is a first-line chemotherapeutic drug in colorectal cancer. However, intravenous administration of 5-FU at the dose of 7-12mg/kg exhibits curbs like short half-life (20min) and toxic side-effects on bone marrow cells. Therefore, in present investigation, 5-FU was conjugated to poly (ethylene glycol) anchored recombinant human serum albumin nanoparticles (5-FU-rHSA-PEG-NPs) to improve the pharmacokinetic and therapeutic profiles. METHODS AND RESULTS: The mean particle size of 5-FU-rHSA-NPs was measured to be 44...
April 12, 2017: Colloids and Surfaces. B, Biointerfaces
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