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pharmacokinetics, antidepressant

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https://www.readbyqxmd.com/read/28648684/hbk-15-protects-mice-from-stress-induced-behavioral-disturbances-and-changes-in-corticosterone-bdnf-and-ngf-levels
#1
Karolina Pytka, Monika Głuch-Lutwin, Magdalena Kotańska, Elżbieta Żmudzka, Magdalena Jakubczyk, Anna Waszkielewicz, Paulina Janiszewska, Maria Walczak
Unlike majority of current antidepressants, HBK-15-a 5-HT1A and 5-HT7 receptor antagonist - showed memory-enhancing properties. In this study, we aimed to further characterize pharmacological profile of HBK-15 and investigate its antidepressant- and anxiolytic-like activity in the mouse model of unpredictable chronic mild stress. We used sucrose consumption test, forced swim test and elevated plus maze and evaluated the influence on brain-derived neurotrophic factor (BDNF) and nerve growth factor (NGF) levels in the hippocampus and prefrontal cortex, as well as body weight, relative adrenal glands weight and plasma corticosterone level in the stressed mice...
June 22, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/28648553/escitalopram-plasma-levels-and-antidepressant-response
#2
Vincenzo Florio, Stefano Porcelli, Alois Saria, Alessandro Serretti, Andreas Conca
Major Depression Disorder (MDD) has a highly variable treatment response due to the large inter-individual variation in the pharmacokinetics and pharmacodynamics of drug treatments. In detail the correlation between plasma level and efficacy has been much debated. Among first-line drugs for MDD, one of the most used is escitalopram. In the present study we investigated the association between serum concentration of escitalopram (SCE) and antidepressant response (AR). 70 MDD patients treated with escitalopram monotherapy were recruited and followed for three months...
June 22, 2017: European Neuropsychopharmacology: the Journal of the European College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28608235/ferulic-acid-supplementation-for-management-of-depression-in-epilepsy
#3
Tanveer Singh, Taranjot Kaur, Rajesh Kumar Goel
Neuroinflammation driven altered neurochemical milieu have been reported to play a significant role in pathogenesis of comorbid depression in epilepsy. Most of the antiepileptic drugs (AEDs) such as levetiracetam, taigabine, topiramate have not been reported any significant effect in alleviating neuroinflammation, which may explain their ineffectiveness in ameliorating depression associated with epilepsy. The supplementation of antidepressants (ADs) attracts various pharmacokinetic and pharmacodynamic interactions with AEDs and was considered unsafe in epilepsy...
June 12, 2017: Neurochemical Research
https://www.readbyqxmd.com/read/28579821/opioid-analgesics-related-pharmacokinetic-drug-interactions-from-the-perspectives-of-evidence-based-on-randomized-controlled-trials-and-clinical-risk-management
#4
REVIEW
Xiu-Qin Feng, Ling-Ling Zhu, Quan Zhou
BACKGROUND: Multimorbidity results in complex polypharmacy which may bear a risk of drug interactions. A better understanding of opioid analgesics combination therapy used for pain management could help warrant medication safety, efficacy, and economic relevance. Until now there has been no review summarizing the opioid analgesics-related pharmacokinetic drug interactions from the perspective of evidence based on randomized controlled trials (RCTs). METHOD: A literature search was performed using PubMed, MEDLINE, and the Cochrane Library, using a PRISMA flowchart...
2017: Journal of Pain Research
https://www.readbyqxmd.com/read/28579071/tranylcypromine-in-mind-part-ii-review-of-clinical-pharmacology-and-meta-analysis-of-controlled-studies-in-depression
#5
REVIEW
Roland Ricken, Sven Ulrich, Peter Schlattmann, Mazda Adli
It has been over 50 years since a review has focused exclusively on the monoamine oxidase (MAO) inhibitor tranylcypromine (TCP). A new review has therefore been conducted for TCP in two parts which are written to be read preferably in close conjunction: part I - pharmacodynamics, pharmacokinetics, drug interactions, toxicology; and part II - clinical studies with meta-analysis of controlled studies in depression, practice of TCP treatment, place in therapy. The irreversible and nonselective MAO-A/B inhibitor TCP has been confirmed as an efficacious and safe antidepressant drug...
June 1, 2017: European Neuropsychopharmacology: the Journal of the European College of Neuropsychopharmacology
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
#6
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
#7
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/28511118/simultaneous-determination-of-selective-serotonin-reuptake-inhibitors-and-their-main-metabolites-in-human-breast-milk-by-liquid-chromatography-electrospray-mass-spectrometry
#8
Etienne Weisskopf, Alice Panchaud, Kim An Nguyen, Delphine Grosjean, Jean-Michel Hascoët, Chantal Csajka, Chin B Eap, Nicolas Ansermot
A bioanalytical method by high performance liquid chromatography coupled to electrospray mass spectrometry (HPLC-ESI-MS), adapted from a previously published method in plasma, was validated in breast milk for the simultaneous quantification of all antidepressants belonging to the class of selective serotonin reuptake inhibitors (citalopram, fluoxetine, fluvoxamine, paroxetine and sertraline) and their major metabolites (desmethylcitalopram and norfluoxetine). Milk samples (250μl) first underwent protein precipitation followed by solid-phase extraction on a reversed phase/cation exchange sorbent...
July 1, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/28501167/polyoxometalate-incorporated-polymer-monolith-microextraction-for-highly-selective-extraction-of-antidepressants-in-undiluted-urine
#9
Jiao Cai, Gang-Tian Zhu, Xiao-Mei He, Zheng Zhang, Ren-Qi Wang, Yu-Qi Feng
In this work, a polyoxometalate (POM) incorporated polymer monolith microextraction (PMME) was successfully proposed and employed in the selective extraction of basic antidepressants in undiluted urine sample. This hybrid monolith exhibited strong cation-exchange interaction (SCX) with positively charged antidepressants when pH was 3.0, because of the multiple ionizable moieties on polyanionic POM. As such, antidepressants in complex sample matrices were efficiently extracted by the monolith, and the matrix effect was significantly reduced...
August 1, 2017: Talanta
https://www.readbyqxmd.com/read/28474366/population-pharmacokinetic-analysis-of-lanicemine-azd6765-an-nmda-channel-blocker-in-healthy-subjects-and-patients-with-major-depressive-disorder
#10
F Agbo, K H Bui, D Zhou
WHAT IS KNOWN AND OBJECTIVE: Lanicemine (AZD6765) is a low-trapping N-methyl-d-aspartate receptor channel blocker that has demonstrated antidepressant efficacy in three of four clinical studies. The aim of this study was to develop a population pharmacokinetic model describing the concentration vs time profile of intravenously administered lanicemine in healthy subjects and patients with major depressive disorder (MDD) and to use the model to evaluate the impact of demographic and clinical factors and concomitant medication on the pharmacokinetics of lanicemine...
May 4, 2017: Journal of Clinical Pharmacy and Therapeutics
https://www.readbyqxmd.com/read/28442937/simultaneous-administration-of-fluoxetine-and-simvastatin-ameliorates-lipid-profile-improves-brain-level-of-neurotransmitters-and-increases-bioavailability-of-simvastatin
#11
Abdulrahman K Al-Asmari, Zabih Ullah, Aqeel Salman Al Masoudi, Ishtiaque Ahmad
Simvastatin (STT), a 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor, is widely prescribed for dyslipidemia, whereas fluoxetine (FLX) is the first-choice drug for the treatment of depression and anxiety. A recent report suggests that selective serotonin reuptake inhibitors can interact with the cytochrome P450 3A4 substrate, and another one suggests that STT enhances the antidepressant activity of FLX. However, the data are inconclusive. The present study was designed to explore the pharmacokinetic and pharmacodynamic consequences of coadministration of STT and FLX in experimental animals...
2017: Journal of Experimental Pharmacology
https://www.readbyqxmd.com/read/28403542/chiral-analysis-of-ammuxetine-enantiomers-in-dog-plasma-using-online-spe-liquid-chromatography-with-tandem-mass-spectrometric-detection-after-precolumn-chiral-derivatization
#12
Jimei Yu, Xin Li, Jiezhao Zhou, Xiangyang Xie, Meiling Chen, Xinhua He, Yang Yang, Youzhi Zhang, Aiping Zheng, Xingguo Mei, Ying Li
Ammuxetine (AMT), a novel chiral antidepressant candidate compound, exhibits better antidepression effects than duloxetine in different animal models. In this article, a chiral derivatization method, combined with online solid phase extraction (online SPE) and liquid chromatography-tandem mass spectrometry (LC-MS/MS), was developed for the chiral separation of AMT enantiomers after administration of racemic AMT to dogs. The derivatization reaction employed 2,3,4,6-tetra-O-acetyl-b-glucopyr-anosyl isothiocyanate (GITC) as a precolumn chiral derivatization reagent...
May 2017: Chirality
https://www.readbyqxmd.com/read/28363155/novel-aryl-piperazines-for-alleviation-of-andropause-associated-prostatic-disorders-and-depression
#13
Sonal Gupta, Deepti Pandey, Dhanaraju Mandalapu, Vikas Sharma, Mahendra Shukla, Seema Singh, Nidhi Singh, Santosh Kumar Yadav, Dilip Kumar Tanpula, Surabhi Singh, Jagdamba P Maikhuri, Shubha Shukla, Jawahar Lal, Mohammad I Siddiqi, Gopal Gupta, Vishnu L Sharma
A series of seventeen piperazine derivatives have been synthesized and biologically evaluated for the management of andropause-associated prostatic disorders and depression. Five compounds 16, 19, 20, 21 and 22 significantly inhibited proliferation of androgen-sensitive LNCaP prostatic cell line with EC50 values of 12.4 μM, 15.6 μM, 11.8 μM, 10.4 μM, 12.2 μM respectively and decreased Ca(2+) entry through adrenergic-receptor α1A blocking activity. Anti-androgenic behaviour of compound 19 and 22 was evident by decreased luciferase activity...
May 26, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28303314/-genetic-tests-for-controlling-treatment-with-antidepressants
#14
T Bschor, C Baethge, C Hiemke, B Müller-Oerlinghausen
In clinical practice, there is a need for a more individualized selection of antidepressants and adequate dosage. The investigation of pharmacokinetically relevant genes is a promising approach to assist this selection. In the past 2 years, two commercially available tests have been subject of advertisement, a test from Stada, which analyses variants of the cytochrome P450 isoenzymes CYP2D6 and CYP2C19 and a test from HMNC Brain Health, which analyses variants of the ABCB1 gene. The costs for both kits are not covered by the statutory health insurance and it is therefore proposed that the patients are invoiced directly in the form of individual healthcare payment...
March 16, 2017: Der Nervenarzt
https://www.readbyqxmd.com/read/28288906/an-aop-analysis-of-selective-serotonin-reuptake-inhibitors-ssris-for-fish
#15
REVIEW
M Danielle McDonald
Pharmaceuticals and personal care products (PPCPs) are found in measureable quantities within the aquatic environment. Selective serotonin reuptake inhibitor (SSRI) antidepressants are one class of pharmaceutical compound that has received a lot of attention. Consistent with most PPCPs, the pharmacokinetics and physiological impacts of SSRI treatment have been well-studied in small mammals and humans and this, combined with the evolutionary conservation of the serotonergic system across vertebrates, allows for the read-across of known SSRI effects in mammals to potential SSRI impacts on aquatic organisms...
March 10, 2017: Comparative Biochemistry and Physiology. Toxicology & Pharmacology: CBP
https://www.readbyqxmd.com/read/28286537/smoking-and-antidepressants-pharmacokinetics-a-systematic-review
#16
REVIEW
Pedro Oliveira, Joana Ribeiro, Helena Donato, Nuno Madeira
BACKGROUND: Despite an increasingly recognized relationship between depression and smoking, little is known about how smoking influences antidepressant response and treatment outcomes. The aim of this study was to systematically review the evidence of the impact of smoking on new-generation antidepressants with an emphasis on the pharmacokinetic perspective. METHODS: We present a systematic review of clinical trials comparing the serum levels of new-generation antidepressants in smokers and nonsmokers...
2017: Annals of General Psychiatry
https://www.readbyqxmd.com/read/28245750/pharmacokinetic-profiles-contribute-to-the-differences-in-behavioral-pharmacology-of-071031b-enantiomers-as-novel-serotonin-and-norepinephrine-reuptake-inhibitors
#17
Rui Xue, Ying Li, Xin-Hua He, Zeng-Liang Jin, Shi-Yong Fan, Ting-Ting Zhang, Nuo-Min Li, Li Yuan, Ai-Ping Zheng, Bo-Hua Zhong, Yun-Feng Li, You-Zhi Zhang
Our previous study indicated that a chiral compound 071031B was a novel serotonin and noradrenaline reuptake inhibitor with superior antidepressant activity compared to duloxetine. The present study aimed to investigate chiral pharmacology differences of 071031B enantiomers, S-071031B and R-071031B, and disclose mechanisms underlying the behavioral differences based on target profiles and pharmacokinetic profiles. In vivo behavioral tests indicated that S-071031B was more potent than R-071031B in two depression models (the forced swimming test in mice and rats) and two pain models (the acetic acid-induced writhing and formalin tests in mice)...
March 2017: Journal of Psychopharmacology
https://www.readbyqxmd.com/read/28244813/pharmacogenomics-of-autism-spectrum-disorder
#18
Jacob T Brown, Seenae Eum, Edwin H Cook, Jeffrey R Bishop
Autism spectrum disorder (ASD) is characterized by persistent deficits in social communication and interactions as well as restricted, repetitive behaviors and interests. Pharmacologic interventions are often needed to manage irritability, aggressive behaviors and hyperactivity. Pharmacogenomic studies have investigated genetic associations with treatment response and side effects in an attempt to better understand drug mechanisms in hopes of optimizing the balance of symptom improvement versus side effects...
March 2017: Pharmacogenomics
https://www.readbyqxmd.com/read/28236991/-how-to-assess-curative-and-or-preventive-effects-of-psychotropic-drugs
#19
T Bottai, D Pringuey, R Belzeaux, M Adida, J-M Azorin
Proving the efficacy of a psychotropic drug is a medical, scientific and ethical need. Psychotropic drug development is now a highly complex process, which takes several years and which is very expensive. It involves multiple steps of preclinical and clinical pharmacological refinement and testing. Methodology of studies to prove curative or preventive effect of psychotropic drugs is well codified. Preclinical studies include pharmacokinetic data, toxicology and performance in various animal models of pathology...
December 2016: L'Encéphale
https://www.readbyqxmd.com/read/28229443/-desvenlafaxine-and-neuropathic-pain-additional-clinical-benefits-of-a-second-generation-serotonin-noradrenaline-reuptake-inhibitor
#20
REVIEW
A Alcantara-Montero
INTRODUCTION: Desvenlafaxine is the third antidepressant within the group of serotonin-norepinephrine reuptake inhibitors. The latest clinical practice guidelines consulted agree that tricyclic antidepressants, dual (venlafaxine/duloxetine) and gabapentin/pregabalin antiepileptics, are the first-line drugs in the treatment of neuropathic pain, being tramadol, lidocaine 5% patches and capsaicin 8% patches of second-line drugs, while strong opioids constitute a third line treatment. The interaction between the binomial pain and depression is very frequent, being the psychological complication more frequent in patients with chronic pain...
March 1, 2017: Revista de Neurologia
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