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pharmacokinetics, antidepressant

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https://www.readbyqxmd.com/read/29615471/pharmacological-characterizations-of-h05-a-novel-potent-serotonin-and-noradrenaline-reuptake-inhibitor-with-moderate-5-ht2a-antagonist-activity-for-anti-depression
#1
Xiangqing Xu, Yaqin Wei, Qiang Guo, Song Zhao, Zhiqiang Liu, Ting Xiao, Yani Liu, Yinli Qiu, Yuanyuan Hou, Guisen Zhang, Kewei Wang
Multi-target antidepressants selectively inhibiting monoaminergic transporters and 5-HT2A receptors have demonstrated higher efficacy and fewer side effects than selective serotonin reuptake inhibitors (SSRIs). In the present study, we synthesized a series of novel 3-(benzo[d] [1, 3] dioxol-4-yloxy)-3-arylpropyl amine derivatives, among which H05 was identified as a lead compound with potent inhibition effects on both serotonin (Ki=4.81 nM) and norepinephrine (Ki=6.72 nM) transporters and moderate 5-HT2A antagonist activity (IC50=60...
April 3, 2018: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/29596146/vortioxetine-disposition-in-obesity-potential-implications-for-patient-safety
#2
David J Greenblatt, Jerold S Harmatz, Christina R Chow
BACKGROUND: Obesity and depression are common comorbid conditions. The objective of the study was to evaluate the effect of obesity on the pharmacokinetics of the serotonergic antidepressant vortioxetine. METHODS: Vortioxetine pharmacokinetics were evaluated in 16 otherwise healthy obese volunteers (mean weight, 119 kg; mean body mass index (BMI) 41.8 kg/m) and in 14 normal-weight subjects (mean weight, 68 kg; mean BMI, 23.0 kg/m) matched for age. All subjects received a single 5-mg oral dose of vortioxetine once daily for 29 days...
March 28, 2018: Journal of Clinical Psychopharmacology
https://www.readbyqxmd.com/read/29593860/potential-drug-drug-interactions-with-direct-oral-anticoagulants-in-elderly-hospitalized-patients
#3
Heather L Forbes, Thomas M Polasek
Background: To determine the prevalence and nature of potential drug-drug interactions (DDIs) with direct oral anticoagulants (DOACs) in elderly hospitalized patients. Methods: This was a retrospective observational study. Inclusion criteria were: aged over 65 years; taking apixaban, rivaroxaban or dabigatran; and admitted to the Repatriation General Hospital between April 2014 and July 2015. A list of clinically relevant 'perpetrator' drugs was compiled from product information, the Australian Medicines Handbook, the Australian National Prescribing Service resources, and local health network guidelines...
October 2017: Therapeutic Advances in Drug Safety
https://www.readbyqxmd.com/read/29556193/pharmacokinetic-study-of-7-compounds-following-oral-administration-of-fructus-aurantii-to-depressive-rats
#4
Xianhua Zhang, Linran Han, Jin Liu, Qiuyue Xu, Yuxin Guo, Wan Zheng, Jian Wang, Xi Huang, Ping Ren
In the present study, the pharmacokinetics of multi-components (naringenin, nobiletin, meranzin hydrate, narirutin, naringin, hesperidin, and neohesperidin) were investigated in acute depressive rats following oral administration of Fructus Aurantii (Zhi-Qiao, ZQ) extract (20 g/kg). A rapid and reliable liquid chromatography-tandem mass spectrometry (LC-MS/MS) method was established to quantitatively or qualitatively analyze the 7 absorbed ingredients in the plasma, hippocampus and cortex of acute depressive rats...
2018: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29507385/lack-of-metabolism-in-r-ketamine-s-antidepressant-actions-in-a-chronic-social-defeat-stress-model
#5
Kai Zhang, Yuko Fujita, Kenji Hashimoto
Since the metabolism of (R,S)-ketamine to (2R,6R)-hydroxynorketamine (HNK) is reported to be essential for ketamine's antidepressant effects, there is an increasing debate about antidepressant effects of (2R,6R)-HNK. Using pharmacokinetic and behavioral techniques, we investigated whether intracerebroventricular (i.c.v.) infusion of (R)-ketamine or (2R,6R)-HNK show antidepressant effects in a chronic social defeat stress (CSDS) model of depression. Low levels of (2R,6R)-HNK in the brain after i.c.v. infusion of (R)-ketamine were detected, although brain levels of (2R,6R)-HNK were markedly lower than those after i...
March 5, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29497300/drug-drug-interactions-involving-antidepressants-focus-on-desvenlafaxine
#6
REVIEW
Yvette Low, Sajita Setia, Graca Lima
Psychiatric and physical conditions often coexist, and there is robust evidence that associates the frequency of depression with single and multiple physical conditions. More than half of patients with depression may have at least one chronic physical condition. Therefore, antidepressants are often used in cotherapy with other medications for the management of both psychiatric and chronic physical illnesses. The risk of drug-drug interactions (DDIs) is augmented by complex polypharmacy regimens and extended periods of treatment required, of which possible outcomes range from tolerability issues to lack of efficacy and serious adverse events...
2018: Neuropsychiatric Disease and Treatment
https://www.readbyqxmd.com/read/29466824/qtc-time-correlates-with-amitriptyline-and-venlafaxine-serum-levels-in-elderly-psychiatric-inpatients
#7
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
#8
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
#9
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
#10
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
#11
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...
February 2018: Bioanalysis
https://www.readbyqxmd.com/read/29332567/nociceptin-orphanin-fq-peptide-nop-receptor-modulators-an-update-in-structure-activity-relationships
#12
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
#13
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-ht-1a-5-ht-7
#14
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...
January 20, 2018: 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
#15
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...
March 2018: 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
#16
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...
February 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/29205993/should-patients-with-schizophrenia-receive-antidepressants
#17
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
#18
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
#19
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...
February 2018: Journal of Affective Disorders
https://www.readbyqxmd.com/read/29138563/squarticles-as-the-nanoantidotes-to-sequester-the-overdosed-antidepressant-for-detoxification
#20
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
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