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Clinical pharmacokinetics

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https://www.readbyqxmd.com/read/28212021/discovery-and-development-of-1-2-bromophenyl-sulfonyl-5-methoxy-3-4-methyl-1-piperazinyl-methyl-1h-indole-dimesylate-monohydrate-suvn-502-a-novel-potent-selective-and-orally-active-serotonin-6-5-ht6-receptor-antagonist-for-potential-treatment-of-alzheimer-s
#1
Ramakrishna Nirogi, Anil Shinde, Rama Sastry Kambhampati, Abdul Rasheed Mohammed, Sangram Keshari Saraf, Rajesh Kumar Badange, Thrinath Reddy Bandyala, Venugopalarao Bhatta, Kumar Bojja, Veena Reballi, Ramkumar Subramanian, Vijay Benade, Raghava Choudary Palacharla, Gopinadh Bhyrapuneni, Pradeep Jayarajan, Vinod Goyal, Venkat Jasti
Optimization of a novel series of 3-(piperazinylmethyl) indole derivatives as 5-hydroxytryptamine-6 receptor (5-HT6R) antagonists resulted in identification of 1-[(2-bromophenyl)sulfonyl]-5-methoxy-3-[(4-methyl-1-piperazinyl)methyl]-1H-indole dimesylate monohydrate (5al, SUVN-502) as a clinical candidate for potential treatment of cognitive disorders. It has high affinity at human 5-HT6R (Ki = 2.04 nM) and selectivity over 100 target sites which include receptors, enzymes, peptides, growth factors, ion channels, steroids, immunological factors, second messengers, and prostaglandins...
February 17, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28211198/safety-of-antifibrinolytics-in-cranial-vault-reconstructive-surgery-a-report-from-the-pediatric-craniofacial-collaborative-group
#2
Susan M Goobie, Franklyn P Cladis, Chris D Glover, Henry Huang, Srijaya K Reddy, Allison M Fernandez, David Zurakowski, Paul A Stricker
BACKGROUND: Antifibrinolytic therapy significantly decreases blood loss and transfusion in pediatric cranial vault reconstructive surgery; however, concern regarding the side effects profile limits clinical use. AIMS: The aim was to utilize the Pediatric Craniofacial Surgery Perioperative Registry database to identify the safety profile of antifibrinolytic therapy for cranial vault reconstructive surgery by reporting the incidence of adverse events as they relate to exposure to tranexamic acid and aminocaproic acid compared to no exposure to antifibrinolytics...
February 17, 2017: Paediatric Anaesthesia
https://www.readbyqxmd.com/read/28211169/a-first-in-human-study-of-ds-1040-an-inhibitor-of-the-activated-form-of-thrombin-activatable-fibrinolysis-inhibitor-in-healthy-subjects
#3
Jin Zhou, Jarema Kochan, Ophelia Yin, Vance Warren, Cynthia Zamora, George Atiee, Joseph Pav, Yasushi Orihashi, Vijay Vashi, Victor Dishy
BACKGROUND: Current treatments for acute ischemic stroke and venous thromboembolism, such as recombinant tissue plasminogen activator and thrombectomy, are limited by a narrow time window and the risk of bleeding. DS-1040 is a novel low-molecular weight compound inhibiting the activated form of thrombin-activatable fibrinolysis inhibitor (TAFIa), developed as a fibrinolysis enhancer for treatment of thromboembolic diseases. OBJECTIVES: This first-in-human, randomized, placebo-controlled, three-part, phase 1 study was conducted to evaluate the safety, pharmacokinetics (PK), and pharmacodynamics (PD) of DS-1040 in healthy subjects...
February 17, 2017: Journal of Thrombosis and Haemostasis: JTH
https://www.readbyqxmd.com/read/28210454/managing-patients-taking-edoxaban-in-dentistry
#4
REVIEW
Adrian Curto, Daniel Curto, Jorge Sanchez
BACKGROUND: Anticoagulation therapy is used in several conditions to prevent or treat thromboembolism. A new group of oral anticoagulants with clear advantages over classic dicoumarin oral anticoagulants (warfarin and acenocoumarol) has been developed in recent years. The Food and Drug Administration has approved edoxaban, dabigatran, rivaroxaban and apixaban. Their advantages include: predictable pharmacokinetics, drug interactions and limited food, rapid onset of action and short half-life...
February 2017: Journal of Clinical and Experimental Dentistry
https://www.readbyqxmd.com/read/28210451/dental-management-of-patients-taking-novel-oral-anticoagulants-noas-dabigatran
#5
REVIEW
Adrian Curto, Alberto Albaladejo, Alfonso Alvarado
BACKGROUND: A new group of oral anticoagulants (dabigatran, rivaroxaban, apixaban and edoxaban) with clear advantages over classic dicoumarin oral anticoagulants (warfarin and acenocoumarol) has been developed in recent years. Patients being treated with oral anticoagulants are at higher risk for bleeding when undergoing dental treatments. MATERIAL AND METHODS: A literature search was conducted through April 2016 for publications in the ISI Web of Knowledge, PubMed and Cochrane Library using the keywords "dabigatran", "rivaroxaban", "apixaban", "edoxaban", "new oral anticoagulants", "novel oral anticoagulants", "bleeding" and "dental treatment"...
February 2017: Journal of Clinical and Experimental Dentistry
https://www.readbyqxmd.com/read/28210286/bilastine-in-allergic-rhinoconjunctivitis-and-urticaria-a-practical-approach-to-treatment-decisions-based-on-queries-received-by-the-medical-information-department
#6
REVIEW
Amalia Leceta, Ander Sologuren, Román Valiente, Cristina Campo, Luis Labeaga
BACKGROUND: Bilastine is a safe and effective commonly prescribed non-sedating H1-antihistamine approved for symptomatic treatment in patients with allergic disorders such as rhinoconjunctivitis and urticaria. It was evaluated in many patients throughout the clinical development required for its approval, but clinical trials generally exclude many patients who will benefit in everyday clinical practice (especially those with coexisting diseases and/or being treated with concomitant drugs)...
2017: Drugs in Context
https://www.readbyqxmd.com/read/28210077/clinical-impact-of-immunomonitoring-in-the-treatment-of-inflammatory-bowel-disease
#7
REVIEW
Donal Tighe, Deirdre McNamara
Despite improvement in outcomes, loss of response (LOR) to tumor necrosis factor-alpha (TNFα) therapies is a big concern in the management of inflammatory bowel disease. LOR is associated with flares of disease, increased hospitalisation rates, need for surgical interventions, and decline in quality of life. LOR may be multifactorial, but immunogenicity makes a significant contribution. Traditionally doses of anti-TNFα have been adjusted based on clinical response, using a standard approach. Immunomonitoring involves the measurement of anti-TNFα trough and antibody levels...
January 21, 2017: World Journal of Gastroenterology: WJG
https://www.readbyqxmd.com/read/28209466/pharmacokinetics-and-safety-of-cavosonstat-n91115-in-healthy-and-cystic-fibrosis-adults-homozygous-for-f508del-cftr
#8
Scott H Donaldson, George M Solomon, Pamela L Zeitlin, Patrick A Flume, Alicia Casey, Karen McCoy, Edith T Zemanick, Arun Mandagere, Janice M Troha, Steven A Shoemaker, James F Chmiel, Jennifer L Taylor-Cousar
BACKGROUND: Cavosonstat (N91115), an orally bioavailable inhibitor of S-nitrosoglutathione reductase, promotes cystic fibrosis transmembrane conductance regulator (CFTR) maturation and plasma membrane stability, with a mechanism of action complementary to CFTR correctors and potentiators. METHODS: A Phase I program evaluated pharmacokinetics, drug-drug interactions and safety of cavosonstat in healthy and cystic fibrosis (CF) subjects homozygous for F508del-CFTR...
February 13, 2017: Journal of Cystic Fibrosis: Official Journal of the European Cystic Fibrosis Society
https://www.readbyqxmd.com/read/28209351/an-indirect-stereoselective-analysis-of-nebivolol-glucuronides-in-plasma-by-lc-ms-ms-application-to-clinical-pharmacokinetics
#9
Carolina Pinto Vieira, Daniel Valente Neves, Evandro José Cesarino, Adriana Rocha, Séverine Poirier, Vera Lucia Lanchote
Nebivolol is a racemate of the d-isomer responsible for β1 adrenergic receptor antagonism and the l-isomer responsible for the release of nitric oxide from endothelial cells. Nebivolol is mainly metabolized to nebivolol glucuronide, which also contribute to the nebivolol β1 adrenoreceptor antagonism. This study reports the development and validation of an indirect stereoselective method of analysis of nebivolol glucuronides in plasma by LC-MS/MS. The method was applied to the investigation of stereoselectivity in the glucuronidation of nebivolol in elderly hypertensive patients (n=11) CYP2D6 phenotyped as EM and treated with a single oral dose of the racemate...
February 3, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28209290/efficacy-safety-and-pharmacokinetics-of-biosimilars-of-anti-tumor-necrosis-factor-%C3%AE-agents-in-rheumatic-diseases-a-systematic-review-and-meta-analysis
#10
REVIEW
Yuga Komaki, Akihiro Yamada, Fukiko Komaki, Praneeth Kudaravalli, Dejan Micic, Akio Ido, Atsushi Sakuraba
OBJECTIVE: To evaluate the efficacy and safety of biosimilars of anti-tumor necrosis factor (TNF)-α agents compared to their reference agents in immune mediated diseases. METHODS: Electronic databases were searched for randomized controlled trials (RCTs) assessing the efficacy and safety of biosimilars of anti-TNF-α agents compared to their reference agents in patients with various immune mediated diseases. The outcomes were the rates of clinical response and adverse events among patients treated with biosimilars compared to their reference agents...
February 13, 2017: Journal of Autoimmunity
https://www.readbyqxmd.com/read/28206979/effect-of-gender-and-age-on-the-relative-bioavailability-of-doravirine-results-of-a-phase-i-trial-in-healthy-subjects
#11
Martin O Behm, Ka L Yee, Li Fan, Paul Fackler
BACKGROUND: Doravirine is a potent, once-daily, non-nucleoside reverse transcriptase inhibitor with a distinct resistance profile in Phase 3 development for the treatment of HIV-1. As doravirine may be administered to women and the elderly, we investigated the impact of gender and age in doravirine pharmacokinetics. METHODS: In this Phase 1, open-label, single-period, parallel-group investigation, doravirine 100 mg was administered to 36 healthy subjects in 3 groups: elderly men (n=12, 65-80 years), elderly women (n=12, 65-80 years), and young women (n=12, 18-50 years)...
February 16, 2017: Antiviral Therapy
https://www.readbyqxmd.com/read/28205455/commentary
#12
Christopher A Droege, Neil E Ernst
Obesity presents a growing challenge in critically ill patients because of variable medication pharmacokinetics and pharmacodynamics. Vasopressors used in the treatment of septic shock, including norepinephrine, are dosed using weight-based (WB) or non-weight-based (NWB) strategies. Retrospective research has evaluated the effect of total body weight and body mass index on vasopressor requirements, consequently finding that obese patients require less total vasopressor per kilogram to obtain clinical end points such as mean arterial pressure...
February 1, 2017: Annals of Pharmacotherapy
https://www.readbyqxmd.com/read/28205288/hematological-adverse-effects-and-pharmacokinetics-of-ribavirin-in-pigs-following-intramuscular-administration
#13
D-U Lee, S H Je, S J Yoo, T Kwon, J Y Shin, J J Byun, J-H Park, K-W Jeong, J-M Ku, Y S Lyoo
Ribavirin (RBV) is a synthetic guanosine analog that is used as a drug against various viral diseases in humans. The in vitro antiviral effects of ribavirin against porcine viruses were demonstrated in several studies. The purposes of this study were to evaluate the adverse effects and pharmacokinetics of ribavirin following its intramuscular (IM) injection in pigs. Ribavirin was formulated as a double-oil emulsion (RBV-DOE) and gel (RBV-Gel), which were injected into the pigs as single-dose IM injections...
February 15, 2017: Journal of Veterinary Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/28205258/simultaneous-quantification-of-antofloxacin-and-its-major-metabolite-in-human-urine-by-hplc-ms-ms-and-its-application-to-a-pharmacokinetic-study
#14
Yunsu Ma, Qianru Wang, Hongwen Zhang, Lijun Xie, Juan Chen, Mao Huang, Yun Liu, Yuanyuan Wang, Libin Wang, Luning Sun, Ning Ou
This study presents a high-performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) method for the simultaneous determination of antofloxacinin and its main metabolite-N-demethylated metabolite (N-DM) in human urine, ornidazole was used as the internal standard (IS). This was a clinical urine recovery study, in which 10 healthy Chinese volunteers were intravenously administered a single 200 mg antofloxacin hydrochloride. Compounds were extracted by albumen precipitation, after which, samples were isocratic eluted by a Poroshell 120 SB-C18 column, and were analysed using HPLC-MS/MS under electronic spray ionization (ESI) positive ion mode...
February 16, 2017: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/28205247/a-novel-freeze-dried-storage-and-preparation-method-for-the-determination-of-mycophenolic-acid-in-plasma-by-high-performance-liquid-chromatography
#15
Lei Wang, Wei Qiang, Ying Li, Zeneng Cheng, Mengmeng Xie
Plasma samples were conventionally stored at freezing conditions until the time of detection. Such a technique, when carried out over an extended period, is energy-consuming, in addition, preparation and transportation of stored samples is inconvenient. In this study, a freeze-dried storage and preparation method was proposed to determine the presence of mycophenolic acid (MPA) in plasma. Fresh plasma samples were freeze-dried using a device, and then stored at ambient temperature. After the stored samples were soaked with methanol spiked with the internal standard, high-performance liquid chromatography was conducted to detect MPA...
February 15, 2017: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/28205246/pharmacokinetics-of-valnemulin-after-intravenous-intramuscular-and-oral-administration-in-layer-chickens
#16
F Sun, R Fan, J Wang, L Xiong, J Shen, S Zhang, X Cao
The pharmacokinetic characteristics of valnemulin in layer chickens were studied after single intravenous, intramuscular, and oral administration at a dose of 15 mg/kg body weight. Plasma samples at certain time points were collected and the drug concentrations in them by ultra high-performance liquid chromatography tandem mass spectrometry (UHPLC-MS). The concentration-time data for each individual were plotted by noncompartmental analysis for the whole three routes. Following intravenous administration, the plasma concentration showed tiny fluctuation...
February 15, 2017: Journal of Veterinary Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/28205039/a-pooled-analysis-of-clinical-pharmacology-trials-investigating-the-pharmacokinetic-and-pharmacodynamic-characteristics-of-fast-acting-insulin-aspart-in-adults-with-type-1-diabetes
#17
Tim Heise, Thomas R Pieber, Thomas Danne, Lars Erichsen, Hanne Haahr
BACKGROUND: Fast-acting insulin aspart (faster aspart) is insulin aspart (IAsp) in a new formulation aiming to mimic the fast endogenous prandial insulin release more closely than currently available insulin products. In a post hoc analysis of pooled data from six clinical pharmacology trials, the pharmacological characteristics of faster aspart and IAsp were compared. METHODS: The analysis included 218 adult subjects with type 1 diabetes from six randomised, double-blind, crossover trials in the faster aspart clinical development programme...
February 15, 2017: Clinical Pharmacokinetics
https://www.readbyqxmd.com/read/28205038/clinical-trial-simulations-and-pharmacometric-analysis-in-pediatrics-application-to-inhaled-loxapine-in-children-and-adolescents
#18
Min Dong, Tsuyoshi Fukuda, Sally Selim, Mark A Smith, Laura Rabinovich-Guilatt, James V Cassella, Alexander A Vinks
BACKGROUND AND OBJECTIVES: Loxapine for inhalation is a drug-device combination product approved in adults for the acute treatment of agitation associated with schizophrenia or bipolar I disorder. The primary objective of this study was to develop a clinical trial protocol to support a phase I pharmacokinetic study in children aged 10 years and older. In addition, this report details the results of the clinical study in relation to the predicted likelihood of achieving the target exposure associated with therapeutic effect in adults...
February 15, 2017: Clinical Pharmacokinetics
https://www.readbyqxmd.com/read/28205004/maturation-of-oxycodone-pharmacokinetics-in-neonates-and-infants-a-population-pharmacokinetic-model-of-three-clinical-trials
#19
Pyry Välitalo, Merja Kokki, Veli-Pekka Ranta, Klaus T Olkkola, Andrew C Hooker, Hannu Kokki
PURPOSE: The aim of the current population pharmacokinetic study was to quantify oxycodone pharmacokinetics in children ranging from preterm neonates to children up to 7 years of age. METHODS: Data on intravenous or intramuscular oxycodone administration were obtained from three previously published studies (n = 119). The median [range] postmenstrual age of the subjects was 299 days [170 days-7.8 years]. A population pharmacokinetic model was built using 781 measurements of oxycodone plasma concentration...
February 15, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28204953/pharmacokinetics-of-coadministration-of-levothyroxine-sodium-and-alendronate-sodium-new-effervescent-formulation
#20
H G Bone, M A Walter, M E Hurley, S Epstein
: No clinically important pharmacokinetic interference of alendronate occurred between a new effervescent formulation of alendronate and levothyroxine when coadministered. The combination does not materially affect levothyroxine absorption. INTRODUCTION: Concurrent treatment of osteoporosis with alendronate (Aln) and hypothyroidism with levothyroxine (LT4) may be problematic because both drugs are to be taken separately after fasting overnight. The primary objective was to assess pharmacokinetic interactions between a new effervescent formulation of Aln (Aln-NEF) and LT4...
February 16, 2017: Osteoporosis International
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