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Agomelatine

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https://www.readbyqxmd.com/read/29151193/disturbances-of-diurnal-phase-markers-behavior-and-clock-genes-in-a-rat-model-of-depression-modulatory-effects-of-agomelatine-treatment
#1
K Højgaard, S L Christiansen, E V Bouzinova, O Wiborg
Major depressive disorder (MDD) is a growing problem worldwide. Though, the etiology remains unresolved, circadian rhythm disturbances are frequently observed in MDD and thus is speculated to play a key role herein. The present study focuses on circadian rhythm disturbances in the chronic mild stress (CMS) animal model of depression and examined whether the atypical antidepressant, agomelatine, which is mediating its action via melatonergic and serotonergic receptors, is capable of resynchronizing the perturbed rhythm...
November 19, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/29137746/ultrasonically-tailored-chemically-engineered-and-qbd-enabled-fabrication-of-agomelatine-nanoemulsion-optimization-characterization-ex-vivo-permeation-and-stability-study
#2
Shakeeb Ahmed, Azka Gull, Mahtab Alam, Mohd Aqil, Yasmin Sultana
The objective of present study was to develop a nanoemulsion formulation of agomelatine (BCS class II drug) for the solubility enhancement. Capmul MCM, Tween 80 and PEG-400 were selected as oil, surfactant and co-surfactant respectively. The high energy ultrasonication method was used for the preparation of nanoemulsion. Three-factor three-level central composite design was employed to get the best formulation. The independent variables selected for the optimization were % oil, %Smix and sonication time (second)...
March 2018: Ultrasonics Sonochemistry
https://www.readbyqxmd.com/read/29106542/dopamine-system-dysregulation-in-major-depressive-disorders
#3
Pauline Belujon, Anthony A Grace
Anhedonia is considered a core feature of major depressive disorder, and the dopamine system plays a pivotal role in the hedonic deficits described in this disorder. Dopaminergic activity is complex and under the regulation of multiple brain structures, including the ventral subiculum of the hippocampus and the basolateral amygdala. Whereas basic and clinical studies demonstrate deficits of the dopaminergic system in depression, the origin of these deficits likely lies in dysregulation of its regulatory afferent circuits...
June 29, 2017: International Journal of Neuropsychopharmacology
https://www.readbyqxmd.com/read/29102176/synthesis-and-biological-evaluation-of-new-naphtho-and-quinolinocyclopentane-derivatives-as-potent-melatoninergic-mt1-mt2-and-serotoninergic-5-ht2c-dual-ligands
#4
Romain Duroux, Marouan Rami, Elodie Landagaray, Mohamed Ettaoussi, Daniel-Henri Caignard, Philippe Delagrange, Patricia Melnyk, Saïd Yous
We recently reported a series of naphthofuranic compounds as constrained agomelatine analogues. Herein, in order to explore alternative ethyl amide side chain rigidification, naphthocyclopentane and quinolinocyclopentane derivatives with various acetamide modulations were synthesized and evaluated at both melatonin (MT1, MT2) and serotonin (5-HT2C) receptors. These modifications has led to compounds with promising dual affinity and high MTs receptors agonist activity. Enantiomeric separation was then performed on selected compounds allowing us to identify levogyre enantiomers (-)-17g and (-)-17k as the highest (MT1, MT2)/5-HT2C dual ligands described nowadays...
December 1, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29099859/agomelatine-venlafaxine-and-running-exercise-effectively-prevent-anxiety-and-depression-like-behaviors-and-memory-impairment-in-restraint-stressed-rats
#5
Sarawut Lapmanee, Jantarima Charoenphandhu, Jarinthorn Teerapornpuntakit, Nateetip Krishnamra, Narattaphol Charoenphandhu
Several severe stressful situations, e.g., natural disaster, infectious disease out break, and mass casualty, are known to cause anxiety, depression and cognitive impairment, and preventive intervention for these stress complications is worth exploring. We have previously reported that the serotonin-norepinephrine-dopamine reuptake inhibitor, venlafaxine, as well as voluntary wheel running are effective in the treatment of anxiety- and depression-like behaviors in stressed rats. But whether they are able to prevent deleterious consequences of restraint stress in rats, such as anxiety/depression-like behaviors and memory impairment that occur afterward, was not known...
2017: PloS One
https://www.readbyqxmd.com/read/29082818/studies-into-the-anxiolytic-actions-of-agomelatine-in-social-isolation-reared-rats-role-of-corticosterone-and-sex
#6
Wilmie Regenass, Marisa Möller, Brian H Harvey
Anxiety disorders are severely disabling, while current pharmacological treatments are complicated by delayed onset, low remission rates and side-effects. Sex is also noted to contribute towards illness severity and treatment response. Agomelatine is a melatonin (MT1/MT2) agonist and serotonin (5-HT2C) antagonist purported to be anxiolytic in clinical and some pre-clinical studies. We undertook a detailed analysis of agomelatine's anxiolytic activity in a neurodevelopmental model of anxiety, the social isolation reared rat...
October 1, 2017: Journal of Psychopharmacology
https://www.readbyqxmd.com/read/29025027/maternal-melatonin-or-agomelatine-therapy-prevents-programmed-hypertension-in-male-offspring-of-mother-exposed-to-continuous-light
#7
You-Lin Tain, Yu-Ju Lin, Julie Y H Chan, Chien-Te Lee, Chien-Ning Hsu
Hypertension can originate from early-life insults, whereas maternal melatonin therapy can be protective in a variety of models of programmed hypertension. We hypothesize that melatonin or melatonin receptor agonist agomelatine can prevent programmed hypertension in adult offspring induced by maternal exposure to continuous light. Female Sprague-Dawley pregnant rats randomly divided into four groups: controls, rats exposed to continuous light, exposed to continuous light plus treated with agomelatine (50 mg/day i...
October 1, 2017: Biology of Reproduction
https://www.readbyqxmd.com/read/28989020/development-of-a-novel-amorphous-agomelatine-formulation-with-improved-storage-stability-and-enhanced-bioavailability
#8
Panagiotis Barmpalexis, Agni Grypioti, Elisavet Vardaka, Anna Karagianni, Kyriakos Kachrimanis
The present work describes the development of a novel formulation of amorphous agomelatine (AGM) that exhibits enhanced in vitro dissolution rate and bioavailability, as well as improved storage stability. Agomelatine was loaded on a mixture of microcrystalline cellulose with a high specific surface area excipient, namely colloidal silicon dioxide, employing a wet granulation method and the resultant AGM granules were subsequently formulated into immediate release film-coated tablets. Modulated differential scanning calorimetry (MT-DSC), hot-state light microscopy, powder X-Ray diffraction (PXRD), attenuated total reflection ATR-FTIR and micro-Raman spectroscopy revealed that the API existed primarily in the amorphous state within the prepared formulations, with some crystals of polymorph I also present...
October 5, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28967202/application-of-quinone-based-fluorophore-and-native-fluorescence-for-the-spectrofluorimetric-determination-of-agomelatine-in-dosage-form-identification-of-acidic-and-alkaline-induced-degradation-products-by-lc-ms-tof
#9
Fawzia Ibrahim, Asmaa Kamal El-Deen, Kuniyoshi Shimizu
Three spectrofluorimetric methods were developed for agomelatine (AGM) determination in commercial tablets. Method A is based on measuring the native fluorescence of AGM aqueous solution at 230/360 nm. Methods B and C are based on the formation of a charge transfer complex between AGM and 2,3-dichloro-5,6-dicyano-1,4-benzoquinone (DDQ) and 7,7,8,8-tetracyanoquinodimethane (TCNQ) with measurement of the formed fluorophore at 365/475 nm and 250/304 nm, respectively. The relative fluorescence intensity (RFI) of AGM-DDQ complex was greatly enhanced in the presence of methyl-β-cyclodextrin (CD)...
October 2, 2017: Luminescence: the Journal of Biological and Chemical Luminescence
https://www.readbyqxmd.com/read/28959452/predicting-early-transition-from-sub-syndromal-presentations-to-major-mental-disorders
#10
Shane P M Cross, Jan Scott, Ian B Hickie
BACKGROUND: Transition from at-risk state to full syndromal mental disorders is underexplored for unipolar and bipolar disorders compared with psychosis. AIMS: Prospective, trans-diagnostic study of rates and predictors of early transition from sub-threshold to full syndromal mental disorder. METHOD: One-year outcome of 243 consenting youth aged 15-25 years with a sub-syndromal presentation of a potentially severe mental disorder. Survival analysis and odds ratio (OR) for predictors of transition identified from baseline clinical and demographic ratings...
September 2017: BJPsych Open
https://www.readbyqxmd.com/read/28954634/the-effect-of-agomelatine-and-melatonin-on-sleep-related-eating-a-case-report
#11
Angela Alexandra Zapp, Eva Caroline Fischer, Michael Deuschle
BACKGROUND: Sleep-related eating may occur in the context of mental illness, sleep disorders, or psychopharmacological treatment. Frequently, sleep-related eating leads to severe weight gain and, so far, there are no treatment options for the condition. CASE PRESENTATION: We report the case of a 54-year-old white woman with depression, panic disorder, and sleep apnea under treatment with various antidepressants who developed severe sleep-related eating. Her sleep-related eating completely vanished after addition of agomelatine, it reoccurred after cessation of agomelatine, and vanished again after her re-exposure to another melatonergic drug, extended melatonin...
September 28, 2017: Journal of Medical Case Reports
https://www.readbyqxmd.com/read/28883733/fan-the-flame-trazodone-induced-mania-in-a-unipolar-depressed-patient-with-stable-sertraline-treatment
#12
Jianbo Hu, Jianbo Lai, Hanzhi Zheng, Shaohua Hu, Yi Xu
Depressed patients often complain of sleep disturbance. Routine antidepressive strategies sometimes fail to deal with this intractable issue. Indeed, the supplementation of sleep promoting antidepressants (eg, trazodone, mirtazapine, and agomelatine) is prevalent in clinical practice. However, the combination of different antidepressants may increase the affective lability. Herein, we document a patient with unipolar depression who was compliant with sertraline treatment and who dramatically switched to mania after adding trazodone as a sleeping aid...
2017: Neuropsychiatric Disease and Treatment
https://www.readbyqxmd.com/read/28833192/effect-of-agomelatine-and-fluoxetine-on-ham-d-score-serum-brain-derived-neurotrophic-factor-and-tumor-necrosis-factor-%C3%AE-level-in-patients-with-major-depressive-disorder-with-severe-depression
#13
Keshav Gupta, Rachna Gupta, M S Bhatia, A K Tripathi, Lalit K Gupta
Evidence suggests that neurotrophic factors, inflammatory markers, and circadian rhythm dysfunctions could be involved in pathophysiology of major depressive disorder. This study evaluated the efficacy and tolerability of agomelatine, a melatonergic drug, and fluoxetine (positive comparator) and their effect on serum brain-derived neurotrophic factor (BDNF) and tumor necrosis factor (TNF)-α level in patients having major depressive disorder with severe depression. In the present study, we chose TNF-α and BDNF because reduction of TNF-α and rise in BDNF levels are linked with improvement in major depressive disorder...
August 17, 2017: Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28831842/transdermal-agomelatine-microemulsion-gel-pyramidal-screening-statistical-optimization-and-in-vivo-bioavailability
#14
Mayada Said, Ibrahim Elsayed, Ahmed A Aboelwafa, Ahmed H Elshafeey
Agomelatine is a new antidepressant having very low oral drug bioavailability less than 5% due to being liable to extensive hepatic 1st pass effect. This study aimed to deliver agomelatine by transdermal route through formulation and optimization of microemulsion gel. Pyramidal screening was performed to select the most suitable ingredients combinations and then, the design expert software was utilized to optimize the microemulsion formulations. The independent variables of the employed mixture design were the percentages of capryol 90 as an oily phase (X1), Cremophor RH40 and Transcutol HP in a ratio of (1:2) as surfactant/cosurfactant mixture 'Smix' (X2) and water (X3)...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28759866/oral-health-impacts-of-medications-used-to-treat-mental-illness
#15
N Cockburn, A Pradhan, M W Taing, S Kisely, P J Ford
BACKGROUND: Many psychotropic medications affect oral health. This review identified oral side effects for antidepressant, antipsychotic, anticonvulsant, antianxiety and sedative drugs that are recommended in Australia for the management of common mental illnesses and provides recommendations to manage these side-effects. METHODS: The Australian Therapeutic Guidelines and the Australian Medicines Handbook were searched for medications used to treat common mental health conditions...
December 1, 2017: Journal of Affective Disorders
https://www.readbyqxmd.com/read/28745530/agomelatine-based-in-situ-gels-for-brain-targeting-via-the-nasal-route-statistical-optimization-in-vitro-and-in-vivo-evaluation
#16
Ahmed M Fatouh, Ahmed H Elshafeey, Ahmed Abdelbary
Agomelatine (AGM) is an antidepressant drug with a low absolute bioavailability due to the hepatic first pass metabolism. AGM-loaded solid lipid nanoparticles were formulated in the form of an in situ gel to prolong the intranasal retention time and subsequently to increase the absorbed amount of AGM. The optimized in situ gel formula had a sol-gel transition temperature of 31 °C ± 1.40, mucociliary transport time of 27 min ±1.41%, released after 1 and 8 h of 46.3% ± 0.85 and 70.90% ± 1...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28744157/the-abc7-regimen-a-new-approach-to-metastatic-breast-cancer-using-seven-common-drugs-to-inhibit-epithelial-to-mesenchymal-transition-and-augment-capecitabine-efficacy
#17
Richard E Kast, Nicolas Skuli, Samuel Cos, Georg Karpel-Massler, Yusuke Shiozawa, Ran Goshen, Marc-Eric Halatsch
Breast cancer metastatic to bone has a poor prognosis despite recent advances in our understanding of the biology of both bone and breast cancer. This article presents a new approach, the ABC7 regimen (Adjuvant for Breast Cancer treatment using seven repurposed drugs), to metastatic breast cancer. ABC7 aims to defeat aspects of epithelial-to-mesenchymal transition (EMT) that lead to dissemination of breast cancer to bone. As add-on to current standard treatment with capecitabine, ABC7 uses ancillary attributes of seven already-marketed noncancer treatment drugs to stop both the natural EMT process inherent to breast cancer and the added EMT occurring as a response to current treatment modalities...
2017: Breast Cancer: Targets and Therapy
https://www.readbyqxmd.com/read/28730851/agomelatine-for-the-treatment-of-generalized-anxiety-disorder
#18
Massimiliano Buoli, Silvia Grassi, Marta Serati, A Carlo Altamura
Agomelatine is a melatonergic antidepressant, approved for the treatment of Major Depressive Disorder (MDD) in Europe and Australia, but not in the United States. This compound seems to be promising in the short-term and maintenance treatment of Generalized Anxiety Disorder (GAD). Areas covered: This paper presents an evaluation of the available data about the clinical efficacy and tolerability of agomelatine in the treatment of GAD. Expert opinion: First-line GAD treatments are limited by high rates of lack of clinical response...
July 28, 2017: Expert Opinion on Pharmacotherapy
https://www.readbyqxmd.com/read/28684900/intranasal-agomelatine-solid-lipid-nanoparticles-to-enhance-brain-delivery-formulation-optimization-and-in-vivo-pharmacokinetics
#19
Ahmed M Fatouh, Ahmed H Elshafeey, Ahmed Abdelbary
PURPOSE: Agomelatine is a novel antidepressant drug suffering from an extensive first-pass metabolism leading to a diminished absolute bioavailability. The aim of the study is: first to enhance its absolute bioavailability, and second to increase its brain delivery. METHODS: To achieve these aims, the nasal route was adopted to exploit first its avoidance of the hepatic first-pass metabolism to increase the absolute bioavailability, and second the direct nose-to-brain pathway to enhance the brain drug delivery...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28679194/acute-urinary-retention-after-venlafaxine-use
#20
Şaban Oğuz Demirdöğen, Esen Yıldırım Demirdöğen, Şenol Adanur
We describe a case of lower urinary system symptoms (LUSSs) and acute urinary retention that developed after treatment with a low dose of venlafaxine. A 48-year-old male patient was admitted to our clinic because of difficulty urinating, an intermittent stream, and trickling at the end of urination, together with urinary retention that had started about 45 days ago. The patient had been taking venlafaxine for the previous 6 months. The drug had been prescribed by the psychiatry department for a diagnosis of major depression, and the dose had been increased from 75 mg/day to 150 mg/day 1...
June 30, 2017: Archivio Italiano di Urologia, Andrologia
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