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Christoph Heinz, J Patrick Lutz, Eric M Simmons, Michael M Miller, William R Ewing, Abigail G Doyle
This report describes a three-component, Ni-catalyzed reductive coupling that enables the convergent synthesis of tertiary benzhydryl amines, which are challenging to access by traditional reductive amination methodologies. The reaction makes use of iminium ions generated in situ from the condensation of secondary N-trimethylsilyl amines with benzaldehydes, and these species undergo reaction with several distinct classes of organic electrophiles. The synthetic value of this process is demonstrated by a single-step synthesis of antimigraine drug flunarizine (Sibelium®) and high yielding derivatization of paroxetine (Paxil®) and metoprolol (Lopressor®)...
January 17, 2018: Journal of the American Chemical Society
Kate Womersley, Katherine Ripullone, Mark Agius
A literature review was conducted to elucidate the respective reproductive safety profiles of different SSRIs to inform the prescribing practices of doctors treating pregnant women with anxiety and depression. BACKGROUND: Women are most likely to be diagnosed with depression or anxiety between the ages of 25 and 44 years, which are also the years of childbearing potential (Burke et al., 1991). Therefore a substantial number of women face a decision about whether or not to take an antidepressant or anxiolytic during pregnancy...
September 2017: Psychiatria Danubina
Cecilia Vichier-Guerre, Margaret Parker, Yael Pomerantz, Richard H Finnell, Robert M Cabrera
The use of antidepressants in pregnant women is rising, with rates up to 7.5% in the United States. Selective serotonin reuptake inhibitors (SSRIs) are currently the most common antidepressant prescribed to pregnant women. The teratogenic effects of SSRI exposure are debated because of discrepancies in epidemiological studies. As an alternative to epidemiological and animal studies, human embryonic stem cell research (hESC) provides a human-based experimental model to examine the risks of prenatal SSRI exposure...
November 5, 2017: Toxicology Letters
Chris Stubbs, Lisa Mattingly, Steven A Crawford, Elizabeth A Wickersham, Jessica L Brockhaus, Laine H McCarthy
CLINICAL QUESTION: In menopausal women who experience regular hot flashes, does treatment with selective serotonin reuptake inhibitors (SSRIs) or serotonin-norepinephrine reuptake inhibitors (SNRIs) reduce the frequency and/or severity of hot flashes? ANSWER: Yes. Review of the literature suggests that treatment with SSRIs or SNRIs reduces the frequency and severity of hot flashes in menopausal and post-menopausal women. Studies demonstrated that paroxetine (Paxil), citalopram (Celexa) and escitolapram (Lexapro) were the most effective SSRIs, and venlafaxine (Effexor) was the most effective first line SNRI, with desvenlafaxine as a second option...
May 2017: Journal of the Oklahoma State Medical Association
Robert M Nevels, Samuel T Gontkovsky, Bryman E Williams
Paroxetine, also known by the trade names Aropax, Paxil, Pexeva, Seroxat, Sereupin and Brisdelle, was first marketed in the U.S. in 1992. Effective for major depression and various anxiety disorders, it quickly gained a sizable share of the antidepressant prescription market. By the late 1990s, paroxetine frequently was being associated with serious drug interactions and medication side effects. Most significantly, in a major Canadian epidemiological study examining the relationship between antidepressants and diseases, paroxetine was associated with a 620 percent increase in the rate of breast cancer in women who had taken it over a four-year period...
March 1, 2016: Psychopharmacology Bulletin
Shannon Marie Gaukler, James Steven Ruff, Wayne K Potts
While conducting a toxicity assessment of the antidepressant paroxetine (Paxil®), in wild-derived mice (Mus musculus), we observed that exposed dams (P0) produced female biased litters (32:68 M:F). Though numerous experimental manipulations have induced sex ratio bias in mice, none have assessed the fitness of the offspring from these litters relative to controls. Here, we retrospectively analyze experimentally derived fitness data gathered for the purpose of toxicological assessment in light of 2 leading hypothesis (Trivers-Willard hypothesis [TWH] and cost of reproduction hypothesis [CRH]), seeking to test if this facultative sex ratio adjustment fits into an adaptive framework...
July 2016: Behavioral Ecology: Official Journal of the International Society for Behavioral Ecology
Peter J Embi, Jessica D Tenenbaum
No abstract text is available yet for this article.
May 12, 2016: New England Journal of Medicine
Carl T Bergstrom
No abstract text is available yet for this article.
May 12, 2016: New England Journal of Medicine
Stuart Buck
No abstract text is available yet for this article.
May 12, 2016: New England Journal of Medicine
Dan L Longo, Jeffrey M Drazen
No abstract text is available yet for this article.
May 12, 2016: New England Journal of Medicine
Akira Dobashi, Kaori Kurata, Mitsuhiro Okazaki, Mari Nishizawa
PURPOSE: Spontaneous inquiries about the development of adverse drug reactions (ADRs) to medicines can be extracted based on the questions posted by the general public on the electronic Japanese bulletin board "Yahoo! Japan Chiebukuro". Our aim was to clarify the characteristics related to people's descriptions of suspected ADRs and determine the reasons for submitting a spontaneous inquiry. METHODS: Fifty brand names of medicines used for inquiry extraction were chosen by selecting 35 pharmaceutical products, based on the generic names that had the highest sales in Japan...
2016: Patient Preference and Adherence
Bruce A Davis, Anu Nagarajan, Lucy R Forrest, Satinder K Singh
The serotonin transporter (SERT) is an integral membrane protein that exploits preexisting sodium-, chloride-, and potassium ion gradients to catalyze the thermodynamically unfavorable movement of synaptic serotonin into the presynaptic neuron. SERT has garnered significant clinical attention partly because it is the target of multiple psychoactive agents, including the antidepressant paroxetine (Paxil), the most potent selective serotonin reuptake inhibitor known. However, the binding site and orientation of paroxetine in SERT remain controversial...
April 1, 2016: Scientific Reports
Nicholas A White, Kerem E Ozboya, Darrin M Flanigan, Tomislav Rovis
A concise enantioselective synthesis of (-)-paroxetine (Paxil) and (-)-femoxetine has been achieved. Key to these syntheses is a N-heterocyclic carbene catalyzed homoenolate addition to a nitroalkene followed by in situ reduction of the nitro-group to rapidly access δ-lactams.
April 2014: Asian Journal of Organic Chemistry
Constance Guille, Roger Newman, Leah D Fryml, Clay K Lifton, C Neill Epperson
The mainstays of treatment for peripartum depression are psychotherapy and antidepressant medications. More research is needed to understand which treatments are safe, preferable, and effective. Postpartum depression, now termed peripartum depression by the DSM-V, is one of the most common complications in the postpartum period and has potentially significant negative consequences for mothers and their families. This article highlights common clinical challenges in the treatment of peripartum depression and reviews the evidence for currently available treatment options...
November 2013: Journal of Midwifery & Women's Health
Umesh Nandkumar Khatavkar, Shamkant Laxman Shimpi, K Jayaram Kumar, Kishor Dattatraya Deo
The objective of this study is to develop, in vitro and in vivo evaluation of novel approaches for controlled release of paroxetine hydrochloride hemihydrate (PHH) in comparison to patented formulation PAXIL CR(®) tablets of GlaxoSmithKline (Geomatrix™ technology). In one of the approaches, hydrophilic core matrix tablets containing 85% of the dose were prepared and further coated with methacrylic acid copolymer to delay the release. An immediate release coating of 15% was given as top coat. The tablets were further optionally coated using ethyl cellulose...
August 2013: Drug Development and Industrial Pharmacy
Jerry C Chang, Ian D Tomlinson, Michael R Warnement, Hideki Iwamoto, Louis J DeFelice, Randy D Blakely, Sandra J Rosenthal
The serotonin (5-hydroxytryptamine, 5-HT) transporter (SERT) protein plays a central role in terminating 5-HT neurotransmission and is the most important therapeutic target for the treatment of major depression and anxiety disorders. We report an innovative, versatile, and target-selective quantum dot (QD) labeling approach for SERT in single Xenopus oocytes that can be adopted as a drug-screening platform. Our labeling approach employs a custom-made, QD-tagged indoleamine derivative ligand, IDT318, that is structurally similar to 5-HT and accesses the primary binding site with enhanced human SERT selectivity...
November 9, 2011: Journal of the American Chemical Society
Kouichirou Nishi, Youichi Yanagawa, Tomonori Imamura, Naoto Matsumoto, Toshihisa Sakamoto
BACKGROUND: A high density area (HDA) that may represent ingested drugs was detected in the stomach of a patient with a drug overdose (OD) by computed tomography (CT). However, there is no prior evidence that drugs can be visualized as an HDA by abdominal CT. We investigated whether drugs can be imaged as an HDA by CT. METHODS: Ten tablets, 5 tablets, 1 tablet and 0.1 tablet of either Solanax (0.4 mg) or Depas (0.5 mg) or Tryptanol (10 mg) or Paxil (10 mg) or Wintermin (25 mg) or Phenobal (30 mg) or Hiberna (25 mg) were each added to 10 ml of artificial gastric juice...
September 2011: Chūdoku Kenkyū: Chūdoku Kenkyūkai Jun Kikanshi, the Japanese Journal of Toxicology
Robert H Howland
Publication bias and outcome reporting bias contribute to distorted perceptions of drug efficacy and the underreporting of adverse events. To demonstrate these biases, this article describes how the clinical profile of the antidepressant agent agomelatine (Valdoxan(®)) has been presented in the literature. Agomelatine has been systematically assessed in 10 short-term placebo-controlled studies and three long-term placebo-controlled relapse prevention studies. Five published trials demonstrated clinically modest but statistically significant benefits over placebo...
September 2011: Journal of Psychosocial Nursing and Mental Health Services
Meredith Wadman
No abstract text is available yet for this article.
July 14, 2011: Nature
Yann Ferrand, Christina M L Kelton, Jeff J Guo, Martin S Levy, Yan Yu
BACKGROUND: Medicaid programs' spending on antidepressants increased from $159 million in 1991 to $2 billion in 2005. The National Institute for Health Care Management attributed this expenditure growth to increases in drug utilization, entry of newer higher-priced antidepressants, and greater prescription drug insurance coverage. Rising enrollment in Medicaid has also contributed to this expenditure growth. OBJECTIVES: This research examines the impact of specific events, including branded-drug and generic entry, a black box warning, direct-to-consumer advertising (DTCA), and new indication approval, on Medicaid spending on antidepressants...
March 2011: Research in Social & Administrative Pharmacy: RSAP
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