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pharmacokinetics, antidepressant

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https://www.readbyqxmd.com/read/29466824/qtc-time-correlates-with-amitriptyline-and-venlafaxine-serum-levels-in-elderly-psychiatric-inpatients
#1
Gudrun Hefner, Martina Hahn, Matthias Hohner, Sybille C Roll, Ansgar Klimke, Christoph Hiemke
INTRODUCTION: Many antidepressants cause QT prolongation but the classification of cardiac risk of these drugs varies markedly in different published lists. This retrospective study analyzed the correlation of QTc time with amitriptyline and venlafaxine serum level in elderly psychiatric inpatients. METHODS: Elderly inpatients aged≥65 years for whom venlafaxine or amitriptyline serum level had been measured were selected retrospectively from a therapeutic drug monitoring database and screened for an electrocardiogram measurement at the time of blood withdrawal...
February 21, 2018: Pharmacopsychiatry
https://www.readbyqxmd.com/read/29427845/duloxetine-loaded-microemulsion-system-to-improve-behavioral-activities-by-upregulating-serotonin-and-norepinephrine-in-brain-for-the-treatment-of-depression
#2
Pardeep Sindhu, Shobhit Kumar, Babar Iqbal, Javed Ali, Sanjula Baboota
Duloxetine is a well-known antidepressant molecule which is used in the treatment of depression but due to poor solubility it suffers with the drawback of low oral bioavailability. The objective of present work was to formulate and characterize duloxetine loaded microemulsion to enhance the oral bioavailability. Prepared microemulsion was studied for droplet size, zeta potential, refractive index, polydispersity index (PDI), percentage transmittance, viscosity and in vitro release study. Optimized microemulsion (D1) showed spherical droplets with mean diameter of 35...
January 31, 2018: Journal of Psychiatric Research
https://www.readbyqxmd.com/read/29399539/chirality-of-modern-antidepressants-an-overview
#3
EDITORIAL
Monica Budău, Gabriel Hancu, Aura Rusu, Melania Cârcu-Dobrin, Daniela Lucia Muntean
The majority of modern antidepressants (selective serotonin reuptake inhibitors and selective serotonin and norepinephrine reuptake inhibitors) have one or two centers of asymmetry in their structure; resulting in the formation of enantiomers which may exhibit different pharmacodynamic and pharmacokinetic properties. Recent developments in drug stereochemistry has led to understanding the role of chirality in modern therapy correlated with increased knowledge regarding the molecular structure of specific drug targets and towards the possible advantages of using pure enantiomers instead of racemic mixtures...
December 2017: Advanced Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/29385160/treatment-with-hc-070-a-potent-inhibitor-of-trpc4-and-trpc5-leads-to-anxiolytic-and-antidepressant-effects-in-mice
#4
Stefan Just, Bertrand L Chenard, Angelo Ceci, Timothy Strassmaier, Jayhong A Chong, Nathaniel T Blair, Randall J Gallaschun, Donato Del Camino, Susan Cantin, Marc D'Amours, Christian Eickmeier, Christopher M Fanger, Carsten Hecker, David P Hessler, Bastian Hengerer, Katja S Kroker, Sam Malekiani, Robert Mihalek, Joseph McLaughlin, Georg Rast, JoAnn Witek, Achim Sauer, Christopher R Pryce, Magdalene M Moran
BACKGROUND: Forty million adults in the US suffer from anxiety disorders, making these the most common forms of mental illness. Transient receptor potential channel canonical subfamily (TRPC) members 4 and 5 are non-selective cation channels highly expressed in regions of the cortex and amygdala, areas thought to be important in regulating anxiety. Previous work with null mice suggests that inhibition of TRPC4 and TRPC5 may have anxiolytic effects. HC-070 IN VITRO: To assess the potential of TRPC4/5 inhibitors as an avenue for treatment, we invented a highly potent, small molecule antagonist of TRPC4 and TRPC5 which we call HC-070...
2018: PloS One
https://www.readbyqxmd.com/read/29333862/pharmacokinetic-determination-and-analysis-of-nortriptyline-based-on-gc-ms-coupled-with-hollow-fiber-drop-to-drop-solvent-microextraction-technique
#5
Pratik Kumar Jagtap, Kavita Tapadia
AIM: A simple, sensitive and robust technique of hollow-fiber drop-to-drop solvent microextraction coupled with GC-MS has been successfully developed for the detection of antidepressant drug nortriptyline in human blood and urine samples. The recoveries of the drug from the spiked samples are found to be well within the range and appropriate to support the method. RESULTS: The LOD for the drug was obtained to be 0.007, 0.009 and 0.021 μg ml-1 in deionized water, urine and blood samples of human subjects, respectively...
January 15, 2018: Bioanalysis
https://www.readbyqxmd.com/read/29332567/nociceptin-orphanin-fq-peptide-nop-receptor-modulators-an-update-in-structure-activity-relationships
#6
Carlo Mustazza, Stefano Pieretti, Francesca Marzoli
Nociceptin /Orphanin FQ Peptide" receptor (NOPr) is a G-protein-coupled receptor with the nociceptin/orphanin FQ peptide (N/OFQ) as endogenous agonist. It is expressed in the nervous system as well as in some non-neural tissues. Its activation has pronociceptive effect at the supraspinal level, whereas at the spinal level it produces nociceptive effects at low doses and antinociceptive effects at higher doses. NOPr is also involved in mood and blood pressure regulation, immunoregulation, airway constriction, feeding, urination, bowel motility, learning and memory...
January 10, 2018: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/29332554/evaluating-the-dose-dependent-mechanism-of-action-of-trazodone-by-estimation-of-occupancies-for-different-brain-neurotransmitter-targets
#7
Luca Settimo, David Taylor
Trazodone is a drug that was introduced in the clinic almost 40 years ago. It is licensed to treat depression, but it is also commonly used off-label to treat insomnia. A recent study shows that it could be promising in preventing neurodegeneration in mice, and clinical trials to assess its possible beneficial effects on dementia and Alzheimer's disease are expected to start soon in humans. In this study, we describe the dose-dependent pharmacology of trazodone by carrying out pharmacokinetic simulations aiming to predict the brain concentrations of trazodone for different drug-dosing regimens and calculating occupancy for 28 different targets for which published trazodone-binding data are available...
January 2018: Journal of Psychopharmacology
https://www.readbyqxmd.com/read/29291438/synthesis-and-antidepressant-like-activity-of-novel-aralkyl-piperazine-derivatives-targeting-ssri-5-ht1a-5-ht7
#8
Zheng-Song Gu, Ai-Nan Zhou, Ying Xiao, Qing-Wei Zhang, Jian-Qi Li
A series of novel aralkyl piperazine derivatives were synthesized, and evaluated for their serotonin reuptake inhibitory and 5-HT1A/5-HT7 receptors affinities activity. Antidepressant activities in vivo of the compounds were screened using the forced swimming test (FST) and tail suspension test (TST). The results indicated that compounds 21k (RUI, IC50 = 31 nM; 5-HT1A, 5-HT7, ki = 62, 12 nM) and 21n (RUI, IC50 = 25 nM; 5-HT1A, 5-HT7, ki = 28, 3.3 nM) exhibited high affinities for the 5-HT1A/5-HT7 receptors coupled with potent serotonin reuptake inhibition...
December 20, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29288677/the-use-of-quetiapine-in-the-treatment-of-major-depressive-disorder-evidence-from-clinical-and-experimental-studies
#9
REVIEW
Zuleide Maria Ignácio, Ana Valquíria Calixto, Ritele Hernandez da Silva, João Quevedo, Gislaine Zilli Réus
Major depressive disorder (MDD) is a highly debilitating condition that is drawing considerable attention due to its high global prevalence and to the fact that treatments are still far from reaching the total number of patients affected. Among available treatment strategies, quetiapine is an important research target, due to antidepressant responses in patients resistant to classical treatments and in animals submitted to protocols that induce depressive-like behaviours. Quetiapine has a broad spectrum of action, within which are many mechanisms that seem to be related to the most effective antidepressant therapeutic responses...
December 27, 2017: Neuroscience and Biobehavioral Reviews
https://www.readbyqxmd.com/read/29230490/pharmacokinetic-study-of-tianeptine-and-its-active-metabolite-mc5-in-rats-following-different-routes-of-administration-using-a-novel-liquid-chromatography-tandem-mass-spectrometry-analytical-method
#10
Małgorzata Szafarz, Agnieszka Wencel, Krzysztof Pociecha, Filip A Fedak, Piotr Wlaź, Elżbieta Wyska
Tianeptine is an atypical antidepressant with a unique mechanism of action and recently it has been also reported that its major metabolite, compound MC5, possesses pharmacological activity similar to that of the parent drug. The current study aims to investigate the pharmacokinetics (PK) of both tianeptine and MC5 after intravenous or intraperitoneal administration of the parent drug as well as the metabolic ratio of MC5 in rats. To achieve these goals an LC-MS/MS method using the small sample volume for the quantitation of tianeptine and its active metabolite MC5 in rat plasma and liver perfusate has been developed and validated...
December 12, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/29205993/should-patients-with-schizophrenia-receive-antidepressants
#11
REVIEW
Viacheslav Terevnikov, Jan-Henry Stenberg, Grigori Joffe
Antipsychotics play a key role in the pharmacological treatment of schizophrenia, and monotherapy is effective for most patients. Achieving an optimal treatment response is, however, often difficult. Combining an antidepressant drug to the antipsychotic regimen could potentially improve treatment outcomes, although the evidence supporting the use of such combinations is limited and contradictory. Positive evidence has mostly been obtained from the efficacy of antidepressants acting on monoamine receptors on the negative symptoms of schizophrenia...
2017: Duodecim; Lääketieteellinen Aikakauskirja
https://www.readbyqxmd.com/read/29189941/vortioxetine-clinical-pharmacokinetics-and-drug-interactions
#12
REVIEW
Grace Chen, Astrid-Maria Højer, Johan Areberg, George Nomikos
Vortioxetine is a novel antidepressant with multimodal activity currently approved for the treatment of major depressive disorder. Vortioxetine is orally administered once daily at 5- to 20-mg doses. The pharmacokinetics of vortioxetine are linear and dose proportional, with a mean terminal half-life of approximately 66 h and steady-state plasma concentrations generally achieved within 2 weeks of dosing. The mean absolute oral bioavailability of vortioxetine is 75%. No food effect on pharmacokinetics was observed...
November 30, 2017: Clinical Pharmacokinetics
https://www.readbyqxmd.com/read/29156365/antidepressant-polypharmacy-and-the-potential-of-pharmacokinetic-interactions-doxepin-but-not-mirtazapine-causes-clinically-relevant-changes-in-venlafaxine-metabolism
#13
Michael Paulzen, Ekkehard Haen, Christoph Hiemke, Bianca Fay, Sandra Unholzer, Gerhard Gründer, Georgios Schoretsanitis
BACKGROUND: To uncover pharmacokinetic interactions between venlafaxine and doxepin or mirtazapine in a naturalistic sample. METHODS: A therapeutic drug monitoring database containing plasma concentrations of venlafaxine (VEN) and its active metabolite O-desmethylvenlafaxine (ODVEN) was analyzed. We included 1067 of 1594 patients in the analysis. Three study groups were considered; a group of patients under venlafaxine without confounding medications, V0 (n = 905), a group of patients co-medicated with doxepin, VDOX (n = 25) and a second group, co-medicated with mirtazapine, VMIR, n = 137...
November 13, 2017: Journal of Affective Disorders
https://www.readbyqxmd.com/read/29138563/squarticles-as-the-nanoantidotes-to-sequester-the-overdosed-antidepressant-for-detoxification
#14
Chun-Han Chen, Tse-Hung Huang, Ahmed O Elzoghby, Pei-Wen Wang, Chia-Wen Chang, Jia-You Fang
The increasing death rate caused by drug overdose points to an urgent demand for the development of novel detoxification therapy. In an attempt to detoxify tricyclic antidepressant overdose, we prepared a lipid nanoemulsion, called squarticles, as the nanoantidote. Squalene was the major lipid matrix of the squarticles. Here, we present the animal study to investigate both the pharmacokinetic and pharmacodynamic effects of squarticles on amitriptyline intoxication. The anionic and cationic squarticles had average diameters of 97 and 122 nm, respectively...
2017: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/29135584/concomitant-medication-polypharmacy-interactions-and-imperfect-adherence-are-common-in-australian-adults-on-suppressive-antiretroviral-therapy
#15
Krista J Siefried, Limin Mao, Lucette A Cysique, John Rule, Michelle L Giles, Don E Smith, James McMahon, Tim R Read, Catriona Ooi, Ban K Tee, Mark Bloch, John de Wit, Andrew Carr
OBJECTIVES: We quantified concomitant medication polypharmacy, pharmacokinetic and pharmacodynamic interactions, adverse effects and adherence in Australian adults on effective antiretroviral therapy. DESIGN: Cross-sectional. METHODS: Patients recruited into a nationwide cohort and assessed for prevalence and type of concomitant medication (including polypharmacy, defined as ≥5 concomitant medications), pharmacokinetic or pharmacodynamic interactions, potential concomitant medication adverse effects and concomitant medication adherence...
January 2, 2018: AIDS
https://www.readbyqxmd.com/read/29134501/pharmacokinetic-properties-of-saffron-and-its-active-components
#16
Azar Hosseini, Bibi Marjan Razavi, Hossein Hosseinzadeh
Saffron as a medicinal plant has many therapeutic effects. Phytochemical studies have reported that saffron is composed of at least four active ingredients which include crocin, crocetin, picrocrocin and safranal. The carotenoids of saffron are sensitive to oxygen, light, heat and enzymatic oxidization. However, regulation of these factors is required for saffron quality. Some pharmacologic effects of saffron and its active compounds include cardioprotective, neuroprotective, memory enhancer, antidepressant and anxiolytic...
November 13, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/29126076/a-rapid-and-sensitive-chiral-lc-ms-ms-method-for-the-determination-of-ketamine-and-norketamine-in-mouse-plasma-brain-and-cerebrospinal-fluid-applicable-to-the-stereoselective-pharmacokinetic-study-of-ketamine
#17
Hidetoh Toki, Takuya Ichikawa, Akiko Mizuno-Yasuhira, Jun-Ichi Yamaguchi
A novel method for the rapid and sensitive chiral determination of ketamine and norketamine in mouse plasma, brain and cerebrospinal fluid (CSF) was developed using liquid chromatography-tandem mass spectrometry (LC-MS/MS). This method reduces the required matrix volume, compared with a previously reported chiral assay method for ketamine and norketamine. The method involves the deproteinization of a small amount of biological matrix (corresponding to 5μL of plasma, 10mg of brain, or 2.5μL of CSF) using a water-miscible organic solvent containing (2)H4-norketamine as an internal standard, the direct injection of the organic supernatant into an LC-MS/MS system, chiral separation on a CHIRALPAK AS-3R column (4...
October 7, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/29125702/single-dose-pharmacokinetics-of-oral-cannabidiol-following-administration-of-ptl101-a-new-formulation-based-on-gelatin-matrix-pellets-technology
#18
Jacob Atsmon, Daphna Heffetz, Lisa Deutsch, Frederic Deutsch, Hagit Sacks
Cannabidiol (CBD) is the main nonpsychoactive component of the cannabis plant. It has been associated with antiseizure, antioxidant, neuroprotective, anxiolytic, anti-inflammatory, antidepressant, and antipsychotic effects. PTL101 is an oral gelatin matrix pellets technology-based formulation containing highly purified CBD embedded in seamless gelatin matrix beadlets. Study objectives were to evaluate the safety and tolerability of PTL101 containing 10 and 100 mg CBD, following single administrations to healthy volunteers and to compare the pharmacokinetic profiles and relative bioavailability of CBD with Sativex oromucosal spray (the reference product) in a randomized, crossover study design...
November 10, 2017: Clinical Pharmacology in Drug Development
https://www.readbyqxmd.com/read/29123929/palpitations-and-asthenia-associated-with-venlafaxine-in-a-cyp2d6-poor-metabolizer-and-cyp2c19-intermediate-metabolizer
#19
Sofia Garcia, Michael Schuh, Anvir Cheema, Herjot Atwal, Paldeep S Atwal
Cardiotoxicity has been extensively reported in venlafaxine (VEN) overdoses. Asthenia is also among the common side effects described for this antidepressant. VEN is metabolized mainly by CYP2D6 and to a minor extent by CYP2C19 to the major active metabolite O-desmethylvenlafaxine (ODV). Altered pharmacokinetic parameters in patients with polymorphisms in the CYP2D6 and CYP2C19 genes that result in decreased enzymatic activity have been documented. Here we describe a patient case of VEN associated palpitations and asthenia...
2017: Case Reports in Genetics
https://www.readbyqxmd.com/read/29115994/exploring-venlafaxine-pharmacokinetic-variability-with-a-phenotyping-approach-a-multicentric-french-swiss-study-marvel-study
#20
Célia Lloret-Linares, Youssef Daali, Sylvie Chevret, Isabelle Nieto, Fanny Molière, Philippe Courtet, Florence Galtier, Raphaëlle-Marie Richieri, Sophie Morange, Pierre-Michel Llorca, Wissam El-Hage, Thomas Desmidt, Frédéric Haesebaert, Philippe Vignaud, Jerôme Holtzmann, Jean-Luc Cracowski, Marion Leboyer, Antoine Yrondi, Fabienne Calvas, Liova Yon, Philippe Le Corvoisier, Olivier Doumy, Kyle Heron, Damien Montange, Siamak Davani, Julien Déglon, Marie Besson, Jules Desmeules, Emmanuel Haffen, Frank Bellivier
BACKGROUND: It is well known that the standard doses of a given drug may not have equivalent effects in all patients. To date, the management of depression remains mainly empirical and often poorly evaluated. The development of a personalized medicine in psychiatry may reduce treatment failure, intolerance or resistance, and hence the burden and costs of mood depressive disorders. The Geneva Cocktail Phenotypic approach presents several advantages including the "in vivo" measure of different cytochromes and transporter P-gp activities, their simultaneous determination in a single test, avoiding the influence of variability over time on phenotyping results, the administration of low dose substrates, a limited sampling strategy with an analytical method developed on DBS analysis...
November 7, 2017: BMC Pharmacology & Toxicology
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