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https://www.readbyqxmd.com/read/28550595/clinical-pharmacokinetics-and-pharmacodynamics-of-colistin
#1
REVIEW
Nicolas Grégoire, Vincent Aranzana-Climent, Sophie Magréault, Sandrine Marchand, William Couet
In this review, we provide an updated summary on colistin pharmacokinetics and pharmacodynamics. Colistin is an old molecule that is frequently used as last-line treatment for infections caused by multidrug-resistant Gram-negative bacteria. Colistin is a decapeptide administered either as a prodrug, colistin methanesulfonate (CMS), when used intravenously, or as colistin sulfate when used orally. Because colistin binds to laboratory materials, many experimental issues are raised and studies on colistin can be tricky...
May 26, 2017: Clinical Pharmacokinetics
https://www.readbyqxmd.com/read/28550529/single-administration-of-hbk-15-a-triple-5-ht1a-5-ht7-and-5-ht3-receptor-antagonist-reverses-depressive-like-behaviors-in-mouse-model-of-depression-induced-by-corticosterone
#2
Karolina Pytka, Monika Głuch-Lutwin, Magdalena Kotańska, Anna Waszkielewicz, Agnieszka Kij, Maria Walczak
Studies suggest that the blockade of 5-HT1A, 5-HT7, and 5-HT3 receptor may increase the speed of antidepressant response. 1-[(2,6-Dimethylphenoxy)ethoxyethyl]-4-(2-methoxyphenyl)piperazine hydrochloride (HBK-14) and 1-[(2-chloro-6-methylphenoxy)ethoxyethyl]-4-(2-methoxyphenyl)piperazine hydrochloride (HBK-15), dual 5-HT1A and 5-HT7 antagonists, showed significant antidepressant- and anxiolytic-like properties in our previous tests in rodents. In this study, we aimed to investigate their antidepressant potential using mouse model of corticosterone-induced depression...
May 26, 2017: Molecular Neurobiology
https://www.readbyqxmd.com/read/28550455/-effects-of-the-novel-relatively-short-acting-kappa-opioid-receptor-antagonist-ly2444296-in-behaviors-observed-after-chronic-extended-access-cocaine-self-administration-in-rats
#3
Marta Valenza, Eduardo R Butelman, Mary Jeanne Kreek
RATIONALE: The recruitment of the stress circuitry contributes to a shift from positive to negative reinforcement mechanisms sustaining long-term cocaine addiction. The kappa opioid receptor (KOPr) signaling is upregulated by stress and chronic cocaine exposure. While KOPr agonists induce anhedonia and dysphoria, KOPr antagonists display antidepressant and anxiolytic properties. Most of the knowledge on KOPr antagonism is based on drugs with unusual pharmacokinetic and pharmacodynamic properties, complicating interpretation of results...
May 27, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28550377/acceptability-of-and-adherence-to-an-antiretroviral-based-vaginal-microbicide-among-pregnant-women-in-the-united-states
#4
Elizabeth T Montgomery, Lisa M Noguchi, James Y Dai, Jason Pan, Joseph Biggio, Craig Hendrix, Karen Isaacs, D Heather Watts, Jill L Schwartz, Jeanna Piper, Richard Beigi
The MTN-008 trial was the first multi-dose study conducted to evaluate the safety of a microbicide gel (2:1 randomized to tenofovir 1% or hydroxycellulose (HEC) placebo gel) during pregnancy. The study aim was to evaluate safety, tolerability and pharmacokinetics of the study products. Procedures included daily gel administration, with Day 0 and Day 6 in clinic, and Days 1-5 at home. Because pregnancy may pose unique challenges to consistent gel use and acceptability, evaluation of adherence and acceptability was a secondary objective of the trial...
May 26, 2017: AIDS and Behavior
https://www.readbyqxmd.com/read/28550375/exploring-inductive-linearization-for-pharmacokinetic-pharmacodynamic-systems-of-nonlinear-ordinary-differential-equations
#5
Chihiro Hasegawa, Stephen B Duffull
Pharmacokinetic-pharmacodynamic systems are often expressed with nonlinear ordinary differential equations (ODEs). While there are numerous methods to solve such ODEs these methods generally rely on time-stepping solutions (e.g. Runge-Kutta) which need to be matched to the characteristics of the problem at hand. The primary aim of this study was to explore the performance of an inductive approximation which iteratively converts nonlinear ODEs to linear time-varying systems which can then be solved algebraically or numerically...
May 26, 2017: Journal of Pharmacokinetics and Pharmacodynamics
https://www.readbyqxmd.com/read/28550352/efficacy-and-safety-of-full-length-pegylated-recombinant-factor-viii-with-extended-half-life-in-previously-treated-patients-with-hemophilia-a-comparison-of-data-between-the-general-and-japanese-study-populations
#6
Keiji Nogami, Midori Shima, Katsuyuki Fukutake, Teruhisa Fujii, Masashi Taki, Tadashi Matsushita, Satoshi Higasa, Tetsuji Sato, Michio Sakai, Morio Arai, Haruhiko Uchikawa, Werner Engl, Brigitt Abbuehl, Barbara A Konkle
Rurioctocog alfa pegol (BAX 855) is a novel third-generation recombinant factor VIII whose active ingredient is chemically modified with polyethylene glycol. A global multicenter phase 2/3 study of the product in 137 patients (including 11 patients from Japan) with severe hemophilia A aged 12-65 years, reported an extended half-life and a good tolerability profile, as well as a significantly lower annualized bleeding rate in the prophylactic treatment arm than in the on-demand treatment arm. Using descriptive statistics, a post hoc analysis was performed to compare the pharmacokinetics, safety, and efficacy profiles of the product in the Japanese subpopulation and the overall population...
May 26, 2017: International Journal of Hematology
https://www.readbyqxmd.com/read/28549802/design-synthesis-and-biological-evaluation-of-novel-androst-3-5-diene-3-carboxylic-acid-derivatives-as-inhibitors-of-5%C3%AE-reductase-type-1-and-2
#7
Kejing Lao, Jie Sun, Chong Wang, Weiting Lyu, Boshen Zhou, Ruheng Zhao, Qian Xu, Qidong You, Hua Xiang
5α-Reductase is a key enzyme responsible for dihydrotestosterone biosynthesis and has been recognized as an important target for discovering new drugs against benign prostatic hyperplasia (BPH). In this study, a series of novel steroidal androst-3,5-diene-3-carboxylic acids have been designed and synthesized. Biological evaluations were performed on their 5α-reductase inhibitory activities by both in vitro enzyme inhibition assay and in vivo by prostate weighing method. Results showed that most of them displayed excellent 5α-reductase inhibitory potency...
May 23, 2017: Steroids
https://www.readbyqxmd.com/read/28549690/albumin-binding-domain-from-streptococcus-zooepidemicus-protein-zag-as-a-novel-strategy-to-improve-the-half-life-of-therapeutic-proteins
#8
Cátia Cantante, Sara Lourenço, Maurício Morais, João Leandro, Lurdes Gano, Nuno Silva, Paula Leandro, Mónica Serrano, Adriano O Henriques, Ana Andre, Catarina Cunha-Santos, Carlos Fontes, João D G Correia, Frederico Aires-da-Silva, Joao Goncalves
Recombinant antibody fragments belong to the promising class of biopharmaceuticals with high potential for future therapeutic applications. However, due to their small size they are rapidly cleared from circulation. Binding to serum proteins can be an effective approach to improve pharmacokinetic properties of short half-life molecules. Herein, we have investigated the Zag albumin-binding domain (ABD) derived from Streptococcus zooepidemicus as a novel strategy to improve the pharmacokinetic properties of therapeutic molecules...
May 23, 2017: Journal of Biotechnology
https://www.readbyqxmd.com/read/28549679/one-should-avoid-retro-orbital-pharmacokinetic-sample-collections-for-intranasal-dosing-in-rats-illustration-of-spurious-pharmacokinetics-generated-for-anti-migraine-drugs-zolmitriptan-and-eletriptan
#9
Harilal Patel, Prakash Patel, Nirav Modi, Shaival Shah, Ashok Ghoghari, Bhavesh Variya, Ritu Laddha, Dipesh Baradia, Nitin Dobaria, Pavak Mehta, Nuggehally R Srinivas
Because of the avoidance of first pass metabolic effects due to direct and rapid absorption with improved permeability, intranasal route represents a good alternative for extravascular drug administration. The aim of the study was to investigate the intranasal pharmacokinetics of two anti-migraine drugs (zolmitriptan and eletriptan), using retro-orbital sinus and jugular vein sites sampling. In a parallel study design, healthy male Sprague-Dawley (SD) rats aged between 8 and 12weeks were divided into groups (n=4 or 5/group)...
May 23, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28549592/economic-outcomes-of-pharmacist-physician-medication-therapy-management-for-polypharmacy-elderly-a-prospective-randomized-controlled-trial
#10
Hsiang-Wen Lin, Chih-Hsueh Lin, Chin-Kai Chang, Che-Yi Chou, I-Wen Yu, Cheng-Chieh Lin, Tsai-Chung Li, Chia-Ing Li, Yow-Wen Hsieh
BACKGROUND/PURPOSE: With an increasing geriatric population, the need for effective management of chronic conditions and medication use in the elderly is growing. Medication use in the elderly presents significant challenges due to changes in pharmacodynamic and pharmacokinetic profiles. We aimed to examine the impact of a collaborative physician-pharmacist medication therapy management (MTM) program for polypharmacy elderly patients. METHODS: Elderly patients with multiple chronic conditions on polypharmacy were enrolled in this prospective, randomized, and controlled study over 16 months of implementation...
May 23, 2017: Journal of the Formosan Medical Association, Taiwan Yi Zhi
https://www.readbyqxmd.com/read/28549082/pharmacokinetics-and-pharmacodynamics-of-propofol-changes-in-patients-with-frontal-brain-tumours
#11
M M Sahinovic, D J Eleveld, T Miyabe-Nishiwaki, M M R F Struys, A R Absalom
Background: Models of propofol pharmacokinetics and pharmacodynamics developed in patients without brain pathology are widely used for target-controlled infusion (TCI) during brain tumour excision operations. The goal of this study was to determine if the presence of a frontal brain tumour influences propofol pharmacokinetics and pharmacodynamics and existing PK-PD model performance. Methods: Twenty patients with a frontal brain tumour and 20 control patients received a propofol infusion to achieve an induction-emergence-induction anaesthetic sequence...
May 26, 2017: British Journal of Anaesthesia
https://www.readbyqxmd.com/read/28548843/zwitterionic-nanocarrier-surface-chemistry-improves-sirna-tumor-delivery-and-silencing-activity-relative-to-polyethylene-glycol
#12
Meredith A Jackson, Thomas A Werfel, Elizabeth J Curvino, Fang Yu, Taylor Elizabeth Kavanaugh, Samantha M Sarett, Mary D Dockery, Kameron V Kilchrist, Ayisha N Jackson, Todd D Giorgio, Craig L Duvall
Although siRNA-based nanomedicines hold promise for cancer treatment, conventional siRNA-polymer complex (polyplex) nanocarrier systems have poor pharmacokinetics following intravenous delivery, hindering tumor accumulation. Here, we determined the impact of surface chemistry on the in vivo pharmacokinetics and tumor delivery of siRNA polyplexes. A library of diblock polymers was synthesized, all containing the same pH-responsive, endosomolytic polyplex core-forming block but different corona blocks: 5 kDa (benchmark) and 20 kDa linear PEG, 10 kDa and 20 kDa brush-like poly(oligo ethylene glycol) (POEGMA), and 10 kDa and 20 kDa zwitterionic phosphorylcholine-based polymers (PMPC)...
May 26, 2017: ACS Nano
https://www.readbyqxmd.com/read/28548497/discovery-of-a-human-neuromedin-u-receptor-1-selective-hexapeptide-agonist-with-enhanced-serum-stability
#13
Kentaro Takayama, Kenji Mori, Akiko Tanaka, Erina Nomura, Yuko Sohma, Miwa Mori, Akihiro Taguchi, Atsuhiko Taniguchi, Toshiyasu Sakane, Akira Yamamoto, Naoto Minamino, Mikiya Miyazato, Kenji Kangawa, Yoshio Hayashi
Neuromedin U (NMU), activates two NMU receptors (NMUR1 and NMUR2), and is a useful anti-obesity drug lead. We report discovery of a hexapeptide agonist, 2-thienylacetyl-Trp(1)-Phe(4-F)(2)-Arg(3)-Pro(4)-Arg(5)-Asn(6)-NH2 (4). However, the NMUR1 selectivity and serum stability of this agonist were unsatisfactory. Through a structure-activity relationship study focused on residue 2 of agonist 4, serum stability, and pharmacokinetic properties, we report here the discovery of a novel NMUR1 selective hexapeptide agonist 7b that suppresses body weight gain in mice...
May 26, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28548028/developmental-differences-between-newborn-and-adult-mice-in-response-to-romiplostim
#14
Katherine A Sparger, Haley Ramsey, Viola Lorenz, Zhi-Jian Liu, Henry A Feldman, Nan Li, Tahirih Laforest, Martha C Sola-Visner
Thrombocytopenia is frequent among sick neonates. While most cases are transient, some neonates experience prolonged and severe thrombocytopenia. These infants often pose diagnostic and therapeutic challenges, and may receive large numbers of platelet transfusions. Romiplostim (ROM) is a thrombopoietin (TPO)-receptor-agonist approved for treatment of adults with chronic immune thrombocytopenia (ITP). The immature platelet fraction (IPF) is a novel measure of newly produced platelets, which could aid with the diagnostic evaluation of thrombocytopenic neonates...
May 26, 2017: Platelets
https://www.readbyqxmd.com/read/28547774/population-pharmacokinetics-pharmacodynamics-and-exploratory-exposure-response-analyses-of-apixaban-in-subjects-treated-for-venous-thromboembolism
#15
W Byon, K Sweeney, C Frost, R A Boyd
Apixaban is approved for treatment of venous thromboembolism (VTE) and prevention of recurrence. Population pharmacokinetics, pharmacokinetics-pharmacodynamics (anti-FXa activity), and exposure-response (binary bleeding and thromboembolic endpoints) of apixaban in VTE treatment subjects were characterized using data from phase I-III studies. Apixaban pharmacokinetics were adequately characterized by a two-compartment model with first-order absorption and elimination. Age, sex, and Asian race had less than 25% impact on exposure, while subjects with severe renal impairment were predicted to have 56% higher exposure than the reference subject (60-year-old non-Asian male weighing 85 kg with creatinine clearance of 100 mL/min)...
May 2017: CPT: Pharmacometrics & Systems Pharmacology
https://www.readbyqxmd.com/read/28547654/potential-teratogenic-effects-of-clomiphene-citrate
#16
REVIEW
Alessandra Scaparrotta, Francesco Chiarelli, Alberto Verrotti
Clomiphene citrate (CC) is the oldest drug used to regulate the process of ovulation. Considering the great use of CC over the last 40 years, it is important to understand the possible risks associated with its use. The aim of this review was to evaluate the possible teratogenic effects of CC, analyzing results obtained from animal and human studies. The pharmacokinetics of CC and possible mechanisms involved in teratogenesis are examined. Fetal exposure to CC is possible due to the long half-life of CC and its metabolites...
May 25, 2017: Drug Safety: An International Journal of Medical Toxicology and Drug Experience
https://www.readbyqxmd.com/read/28546950/genetic-polymorphisms-of-multidrug-and-toxin-extrusion-proteins-mate1-and-mate2-in-south-indian-population
#17
Gerard Marshall Raj, Jayanthi Mathaiyan, Mukta Wyawahare, Katiboina Srinivasa Rao, Rekha Priyadarshini
Introduction: Drug transporters are key determinants of pharmacokinetic and pharmacodynamic profiles of certain drugs. SLC47A1 (MATE1) and SLC47A2 (MATE2) are major efflux transporters involved in the hepatic and renal excretion of many cationic drugs including metformin. Our study was proposed to determine the normative frequencies of the single nucleotide polymorphisms (SNPs) rs2289669 and rs12943590 in the SLC47A1 and SLC47A2 genes, respectively, in South Indian population and also to compare those with those of the HapMap populations...
2017: BioImpacts: BI
https://www.readbyqxmd.com/read/28546766/abcb1-genetic-variants-in-leukemias-current-insights-into-treatment-outcomes
#18
REVIEW
Ravindran Ankathil
Despite improvements in treatment of different types of leukemia, not all patients respond optimally for a particular treatment. Some treatments will work better for some, while being harmful or ineffective for others. This is due to genetic variation in the form of single-nucleotide polymorphisms (SNPs) that affect gene expression or function and cause inherited interindividual differences in the metabolism and disposition of drugs. Drug transporters are one of the determinants governing the pharmacokinetic profile of chemotherapeutic drugs...
2017: Pharmacogenomics and Personalized Medicine
https://www.readbyqxmd.com/read/28546337/pet-guided-evaluation-and-optimization-of-internalized-antibody-drug-conjugates-targeting-erythropoietin-producing-hepatoma-a2-receptor
#19
Orit Jacobson, Haojun Chen, Gang Niu, Dale O Kiesewetter, Qing Li, Gengcheng Yang, Kimberly Cook, Lan Xu, William Dall'Acqua, Ping Tsui, Li Peng, Xiaoyuan Chen
The erythropoietin producing hepatoma A2 receptor (EphA2) is a tyrosine kinase overexpressed by tumor stroma and cancer cells. High expression level of EphA2 predicts poor prognosis, correlating with disease progression and metastasis. Therefore, EphA2 is a relevant therapeutic target for human cancer. Antibodies, selectively bound to EphA2 receptor, can induce rapid receptor phosphorylation that results in antibody internalization and degradation. This internalization mechanism has been exploited with the development of antibody-drug conjugates (ADC) for cancer chemotherapy...
May 25, 2017: Journal of Nuclear Medicine: Official Publication, Society of Nuclear Medicine
https://www.readbyqxmd.com/read/28546104/development-of-a-paediatric-physiologically-based-pharmacokinetic-model-to-assess-the-impact-of-drug-drug-interactions-in-tuberculosis-co-infected-malaria-subjects-a-case-study-with-artemether-lumefantrine-and-the-cyp3a4-inducer-rifampicin
#20
Olusola Olafuyi, Michael Coleman, Raj K S Badhan
The fixed dosed combination of artemether and lumefantrine (AL) is widely used for the treatment of malaria in adults and children in sub-Sahara Africa, with lumefantrine day 7 concentrations being widely used as a marker for clinical efficacy. Both are substrates for CYP3A4 and susceptible to drug-drug interactions (DDIs); indeed, knowledge of the impact of these factors is currently sparse in paediatric population groups. Confounding malaria treatment is the co-infection of patients with tuberculosis. The concomitant treatment of AL with tuberculosis chemotherapy, which includes the CYP3A4 inducer rifampicin, increases the risk of parasite recrudescence and malaria treatment failure...
May 22, 2017: European Journal of Pharmaceutical Sciences
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