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https://www.readbyqxmd.com/read/29046178/a-psychiatric-formulary-for-long-duration-spaceflight
#1
Eric Friedman, Brian Bui
Behavioral health is essential for the safety, well-being, and performance of crewmembers in both human spaceflight and Antarctic exploration. Over the past five decades, psychiatric issues have been documented in orbital spaceflight. In Antarctica, literature suggests up to 5% of wintering crewmembers could meet criteria for a psychiatric illness, including mood disorders, stressor-related disorders, sleep-wake disorders, and substance-related disorders. Experience from these settings indicates that psychiatric disorders on deep space missions must be anticipated...
November 1, 2017: Aerospace Medicine and Human Performance
https://www.readbyqxmd.com/read/29025271/psychotropic-drugs-and-cyp2d6-in-late-life-psychiatric-and-neurological-disorders-what-do-we-know
#2
Davide Seripa, Madia Lozupone, Eleonora Stella, Giulia Paroni, Paola Bisceglia, Maddalena La Montagna, Grazia D'onofrio, Carolina Gravina, Maria Urbano, Maria Giovanna Priore, Angela Lamanna, Antonio Daniele, Antonello Bellomo, Giancarlo Logroscino, Antonio Greco, Francesco Panza
Late-life psychiatric and neurological disorders (LLPND) are interesting models to understand the potential role of pharmacogenetics in drug management, since several pharmacological approaches for treating LLPND have proven to be ineffective or deleterious, thus resulting in therapeutic failures (TF) and adverse drug reactions (ADR). Common variants in the genes encoding the cytochrome P450 (CYP) enzyme system, the 'engine room' of drug metabolism, together with well-known age-related increased polypharmacy also contributed to the prevalence of TF and ADR observed in these patients, also rising number and time of hospital readmissions and rate of institutionalizations...
October 12, 2017: Expert Opinion on Drug Safety
https://www.readbyqxmd.com/read/28951668/development-and-evaluation-of%C3%A2-desvenlafaxine-loaded-plga-chitosan-nanoparticles-for-brain-delivery
#3
Gui-Feng Tong, Nan Qin, Li-Wei Sun
Depression is a debilitating psychiatric condition that remains the second most common cause of disability worldwide. Currently, depression affects more than 4 per cent of the world's population. Most of the drugs intended for clinical management of depression augment the availability of neurotransmitters at the synapse by inhibiting their neuronal reuptake. However, the therapeutic efficacy of antidepressants is often compromised as they are unable to reach brain by the conventional routes of administration...
September 2017: Saudi Pharmaceutical Journal: SPJ: the Official Publication of the Saudi Pharmaceutical Society
https://www.readbyqxmd.com/read/28951319/recent-advances-in-nanocarrier-loaded-gels-which-drug-delivery-technologies-against-which-diseases
#4
REVIEW
Marion Pitorre, Henri Gondé, Clotilde Haury, Marwa Messous, Jérémie Poilane, David Boudaud, Erdem Kanber, Glenn Alexis Rossemond Ndombina, Jean-Pierre Benoit, Guillaume Bastiat
The combination of pharmaceutical technologies can be a wise choice for developing innovative therapeutic strategies. The association of nanocarriers and gels provides new therapeutic possibilities due to the combined properties of the two technologies. Gels support the nanocarriers, localize their administration to the target tissue, and sustain their release. In addition to the properties afforded by the gel, nanocarriers can provide additional drug sustained release or different pharmacokinetic and biodistribution profiles than those from nanocarriers administered by the conventional route to improve the drug therapeutic index...
September 23, 2017: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/28948135/pharmacological-management-of-anxiety-disorders-in-the-elderly
#5
Elizabeth A Crocco, Sindy Jaramillo, Caroline Cruz-Ortiz, Katherine Camfield
Anxiety disorders are common in the elderly. Additionally, anxiety symptoms often accompany co-morbid psychiatric, medical, as well as neurodegenerative diseases in the older population. Anxiety in the elderly, often accompanied by depression, can lead to worsening physical, cognitive and functional impairments in this vulnerable population. Antidepressants are considered first line treatment. Both SSRIs and SNRIs are efficacious and well-tolerated in the elderly. Some SSRIs are strong inhibitors of the cytochrome P450 hepatic pathway whereas others have less potential for drug interaction...
March 2017: Current Treatment Options in Psychiatry
https://www.readbyqxmd.com/read/28888484/prediction-of-human-efficacious-antidepressant-doses-using-the-mouse-forced-swim-test
#6
Eunice Yuen, Steven Swanson, Jeffrey M Witkin
The forced swim test (FST) is a commonly used preclinical animal behavioural model for prediction of antidepressant activity in humans. While the FST may qualitatively predict efficacy, less is known about the quantitative translation of FST data to human efficacious doses. Assessing quantitative translation allows better predictions of human efficacious doses and a higher chance of success in the drug development process. Dose-response and time-course FST experiments were carried out on mice using four marketed antidepressants (citalopram, desipramine, bupropion, desvenlafaxine) in addition to ketamine, all with varying mechanisms of action...
October 2017: Pharmacology, Biochemistry, and Behavior
https://www.readbyqxmd.com/read/28880242/synthesis-and-antidepressant-activity-profile-of-some-novel-benzothiazole-derivatives
#7
Ümide Demir Özkay, Ceren Kaya, Ulviye Acar Çevik, Özgür Devrim Can
Within the scope of our new antidepressant drug development efforts, in this study, we synthesized eight novel benzothiazole derivatives 3a-3h. The chemical structures of the synthesized compounds were elucidated by spectroscopic methods. Test compounds were administered orally at a dose of 40 mg/kg to mice 24, 5 and 1 h before performing tail suspension, modified forced swimming, and activity cage tests. The obtained results showed that compounds 3c, 3d, 3f-3h reduced the immobility time of mice as assessed in the tail suspension test...
September 7, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28876959/chirality-and-neuropsychiatric-drugs-an-update-on-stereoselective-disposition-and-clinical-pharmacokinetics-of-bupropion
#8
Ranjeet Prasad Dash, Rana Rais, Nuggehally R Srinivas
Bupropion, an antidepressant drug has been approved as a racemate containing equal amounts of R- and S- enantiomers. Recently, the chirality of bupropion has received significant attention in the delineation of stereoselective pharmacokinetic and disposition data. Although the non-stereoselective metabolism of bupropion was well established, the emerging data suggests that bupropion exhibits complex stereoselective metabolism, leading to the formation of various stereoisomeric metabolites. Along with the chiral pharmacokinetics of bupropion, hydroxybupropion, threohydrobupropion and erythrohydrobupropion, the metabolism data also provided insights into the roles of both CYP2B6 and CYP2C19 enzymes in the stereoselective disposition...
September 6, 2017: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/28858450/ketamine-for-depression-5-potential-pharmacokinetic-and-pharmacodynamic-drug-interactions
#9
REVIEW
Chittaranjan Andrade
Ketamine, administered in subanesthetic doses, is gaining recognition as an off-label treatment for severe and even treatment-refractory depression. This article explores potential pharmacokinetic and pharmacodynamic drug interactions of relevance to the use of ketamine in depression. Sparse evidence suggests that ketamine will not induce clinically significant drug interactions except to the extent that these are predictable by its clinical actions. A small body of literature indicates that drugs that induce cytochrome P450 (CYP)2B6 and CYP3A4 will reduce exposure to ketamine and that drugs that inhibit these enzymes will increase exposure to ketamine...
July 2017: Journal of Clinical Psychiatry
https://www.readbyqxmd.com/read/28838696/synthesis-and-optimization-of-4-5-6-7-tetrahydrooxazolo-4-5-c-pyridines-as-potent-and-orally-active-metabotropic-glutamate-receptor-5-negative-allosteric-modulators
#10
Wataru Hirose, Yoshihiro Kato, Itaru Natsutani, Makoto Takata, Maiko Kitaichi, Satoki Imai, Shun Hayashi, Yukiyo Arai, Kohei Hoshino, Kohzo Yoshida
We describe here the design, synthesis and characterization of a series of 4,5,6,7-tetrahydrooxazolo[4,5-c]pyridines as metabotropic glutamate receptor (mGluR) 5 negative allosteric modulators (NAMs). Optimization of the substituents led to the identification of several compounds with good pharmacokinetic profiles, including long half life and high oral bioavailability, in both rats and monkeys. The receptor occupancy test in the rat cortex revealed favorable brain penetration of these compounds. The reprsentative compound 13 produced oral antidepressant-like effect in the rat forced swimming test (MED: 0...
September 15, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28806704/chiral-pharmaceuticals-a-review-on-their-environmental-occurrence-and-fate-processes
#11
REVIEW
Edmond Sanganyado, Zhijiang Lu, Qiuguo Fu, Daniel Schlenk, Jay Gan
More than 50% of pharmaceuticals in current use are chiral compounds. Enantiomers of the same pharmaceutical have identical physicochemical properties, but may exhibit differences in pharmacokinetics, pharmacodynamics and toxicity. The advancement in separation and detection methods has made it possible to analyze trace amounts of chiral compounds in environmental media. As a result, interest on chiral analysis and evaluation of stereoselectivity in environmental occurrence, phase distribution and degradation of chiral pharmaceuticals has grown substantially in recent years...
November 1, 2017: Water Research
https://www.readbyqxmd.com/read/28783942/codeine-precipitating-serotonin-syndrome-in-a-patient-in-therapy-with-antidepressant-and-triptan
#12
Giulia Milano, Werner Maria Natta, Alfredo Bello, Antonietta Martelli, Francesca Mattioli
The serotonin syndrome is a serioius medical condition due due to an intensive stimulation of setonin receptors. It is a rare, but severe, consequence of interaction between serotomimetic agents. This is a report of a 70-year-old woman steadily in therapy with venlafaxine and rizatriptan for migraine and major depressive syndrome. She was admitted to neurology unit for decreased light reflex with miotic pupils, global hyperreflexia, tremor, anxiety, ataxia and incoordination. The patient was diagnosed as a probable case of serotonin syndrome due to a pharmacological interaction between venlafaxine and rizatriptan trigged by opioid intake...
August 31, 2017: Clinical Psychopharmacology and Neuroscience: the Official Scientific Journal of the Korean College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28782316/rediscovering-chirality-role-of-s-metoprolol-in-cardiovascular-disease-management
#13
Jagdish C Mohan, Siddharth N Shah, Sunny Chinchansurkar, Arindam Dey, Rishi Jain
BACKGROUND: The process of drug discovery and development today encompass a myriad of paths for bringing a new therapeutic molecule that has minimal adverse effects and of optimal use to the patient. Chirality was proposed in the direction of providing a purer and safer form of drug [Ex- cetrizine and levocetrizine]. Decades have passed since the introduction of this concept and numerous chiral molecules are in existence in therapeutics, yet somehow this concept has been ignored. This review aims to rediscover the ignored facts about chirality, its benefits and clear some common myths considering the example of S-Metoprolol in the management of Hypertension and other cardiovascular diseases...
June 2017: Journal of the Association of Physicians of India
https://www.readbyqxmd.com/read/28762173/methylene-blue-and-its-analogues-as-antidepressant-compounds
#14
REVIEW
Anzelle Delport, Brian H Harvey, Anél Petzer, Jacobus P Petzer
Methylene Blue (MB) is considered to have diverse medical applications and is a well-described treatment for methemoglobinemias and ifosfamide-induced encephalopathy. In recent years the focus has shifted to MB as an antimalarial agent and as a potential treatment for neurodegenerative disorders such as Alzheimer's disease. Of interest are reports that MB possesses antidepressant and anxiolytic activity in pre-clinical models and has shown promise in clinical trials for schizophrenia and bipolar disorder. MB is a noteworthy inhibitor of monoamine oxidase A (MAO-A), which is a well-established target for antidepressant action...
July 31, 2017: Metabolic Brain Disease
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
#15
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/28734960/pharmacokinetic-interactions-of-curcuminoids-with-conventional-drugs-a-review
#16
REVIEW
Roodabeh Bahramsoltani, Roja Rahimi, Mohammad Hosein Farzaei
ETHNOPHARMACOLOGICAL RELEVANCE: Herb-drug interactions are of great concern in health practices. Curcumin is a natural polyphenol extracted from turmeric, a spice widely used all over the world. Curcumin is clinically used due to its acceptable safety profile and therapeutic efficacy. AIM OF THE STUDY: Current paper aims to highlight the effect of curcumin on concomitantly used drugs. METHODS: Electronic databases including PubMed, Scopus and Science Direct were searched with the keywords "curcumin" in the title/abstract and "drug interaction," "drug metabolism," "cytochrome," "P-glycoprotein" and "P450" in the whole text...
July 19, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28732807/pharmacology-and-toxicology-of-%C3%AE-and-%C3%AE-asarone-a-review-of-preclinical-evidence
#17
REVIEW
Ranjithkumar Chellian, Vijayapandi Pandy, Zahurin Mohamed
BACKGROUND: Asarone is one of the most researched phytochemicals and is mainly present in the Acorus species and Guatteria gaumeri Greenman. In preclinical studies, both α- and β-asarone have been reported to have numerous pharmacological activities and at the same time, many studies have also revealed the toxicity of α- and β-asarone. PURPOSE: The purpose of this comprehensive review is to compile and analyze the information related to the pharmacokinetic, pharmacological, and toxicological studies reported on α- and β-asarone using preclinical in vitro and in vivo models...
August 15, 2017: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
https://www.readbyqxmd.com/read/28714606/treating-depression-during-pregnancy-are-we-asking-the-right-questions
#18
REVIEW
Cara Angelotta, Katherine L Wisner
BACKGROUND: Major depressive disorder (MDD) is a common complication of pregnancy. Once the diagnosis of MDD is made, the physician must assist the pregnant woman in developing a treatment plan. METHODS: In considering antidepressants, the benefit of medication treatment for maternal disease control must be balanced against the risk of the drug to the developing embryo-fetus. This is an individualized decision depending on the disease characteristics, likelihood of maternal depression response, probability of adverse fetal effects, and patient characteristics and values...
July 17, 2017: Birth defects research
https://www.readbyqxmd.com/read/28707591/new-generation-non-ssri-antidepressants-therapeutic-drug-monitoring-and-pharmacological-interactions-part-1-snris-smss-saris
#19
Roberto Mandrioli, Michele Protti, Laura Mercolini
BACKGROUND: New-generation antidepressants (NGAs) are the latest additions to the clinician's arsenal in the fight against depression. After the introduction of selective serotonin reuptake inhibitors (SSRIs), a plethora of other groups followed, identified by their main mechanisms of activity: serotonin and norepinephrine reuptake inhibitors (SNRI); serotonin modulators and stimulators (SMS); serotonin antagonists and reuptake inhibitors (SARI); noradrenergic and selective serotonergic antidepressants (NaSSA); norepinephrine reuptake inhibitors (NeRI); serotonin, norepinephrine and dopamine reuptake inhibitors (SNDRI) or triple reuptake inhibitors (TRI); and melatonin and serotonin agonists (MaSA)...
July 12, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28694764/2-pyrazoline-derivatives-in-neuropharmacology-synthesis-adme-prediction-molecular-docking-and-in-vivo-biological-evaluation
#20
Savita Upadhyay, Avinash C Tripathi, Sarvesh Paliwal, Shailendra K Saraf
A novel series of 1,3,5-trisubstituted-2-pyrazoline derivatives (PFC-1 to PFC-16) were synthesized in a three step reaction using conventional and microwave assisted green chemistry approach. The synthesized derivatives were characterized and their chemical structures were established by various physicochemical methods such as IR, Mass, (1)H-NMR, (13)C-NMR and elemental analysis. The synthesized compounds were tested for their neuropharmacological potential. The compounds exhibited significant antidepressant and anti-anxiety activities against various behavioral in vivo models...
2017: EXCLI journal
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