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Marcos Emilio Frizzo
Sertraline (Zoloft) and fluoxetine (Prozac) are selective serotonin reuptake inhibitors whose antidepressant mechanism of action is classically attributed to an elevation of the extracellular levels of serotonin in the synaptic cleft. However, the biological effects of these drugs seem to be more complex than their traditionally described mechanism of action. Among their actions is the inhibition of different types of Na(+) and K(+) channels, as well as of glutamate uptake activity. The clearance of extracellular glutamate is essential to maintain the central nervous system within physiological conditions, and this excitatory neurotransmitter is removed from the synaptic cleft by astrocyte transporters...
2017: Current Therapeutic Research, Clinical and Experimental
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
William D Gwynne, Robin M Hallett, Adele Girgis-Gabardo, Bojana Bojovic, Anna Dvorkin-Gheva, Craig Aarts, Kay Dias, Anita Bane, John A Hassell
Breast tumors comprise an infrequent tumor cell population, termed breast tumor initiating cells (BTIC), which sustain tumor growth, seed metastases and resist cytotoxic therapies. Hence therapies are needed to target BTIC to provide more durable breast cancer remissions than are currently achieved. We previously reported that serotonergic system antagonists abrogated the activity of mouse BTIC resident in the mammary tumors of a HER2-overexpressing model of breast cancer. Here we report that antagonists of serotonin (5-hydroxytryptamine; 5-HT) biosynthesis and activity, including US Federal Food and Drug Administration (FDA)-approved antidepressants, targeted BTIC resident in numerous breast tumor cell lines regardless of their clinical or molecular subtype...
May 9, 2017: Oncotarget
Robin M Hallett, Adele Girgis-Gabardo, William D Gwynne, Andrew O Giacomelli, Jennifer N P Bisson, Jeremy E Jensen, Anna Dvorkin-Gheva, John A Hassell
Accumulating data suggests that the initiation and progression of human breast tumors is fueled by a rare subpopulation of tumor cells, termed breast tumor-initiating cells (BTIC), which resist radiotherapy and chemotherapy. Consequently, therapies that abrogate BTIC activity are needed to achieve durable cures for breast cancer patients. To identify such therapies we used a sensitive assay to complete a high-throughput screen of small molecules, including approved drugs, with BTIC-rich mouse mammary tumor cell populations...
August 16, 2016: Oncotarget
Suhair S Al-Nimry, Malak A Jaber
Sertraline hydrochloride has low solubility and undergoes first-pass metabolism resulting in low bioavailability. The main objective of this research was to enhance the dissolution rate of the drug. The drug was recrystallized in the presence of polymers and surfactant. The formulation was optimized by studying the effects of drug/polymer ratio, concentration of SLS, and type of polymer on particle size and drug release. The optimized formulation was characterized using different techniques and by evaluating in vitro release, stability, and flow properties...
May 2017: AAPS PharmSciTech
Young Ji Lee, Heidi Donovan
Fatigue continues to be one of the main symptoms that afflict ovarian cancer patients and negatively affects their functional status and quality of life. To manage fatigue effectively, the symptom must be understood from the perspective of patients. We utilized text mining to understand the symptom experiences and strategies that were associated with fatigue among ovarian cancer patients. Through text analysis, we determined that descriptors such as energetic, challenging, frustrating, struggling, unmanageable, and agony were associated with fatigue...
2016: Studies in Health Technology and Informatics
Thomas Kampfrath, Penny Peng, Valli Vairavan, Dayong Lee
CLINICAL HISTORY: HASH(0x36f1f50) PATIENT: 41-year-old Hispanic woman. Chief Complaint: Pain in the neck, joints, and shoulders that started in August 2013. History of Present Illness: The patient has a history of psychiatric illness. Her primary care physician from an outside facility had prescribed alprazolam (Xanax) to treat her depression. The patient reported that in 2011 she experienced pain in the right side of her back and was diagnosed with sciatica. In addition, she was diagnosed with systemic lupus erythematosus (SLE) based on a positive finding for antinuclear antibodies (ANA) and double-stranded DNA (ds-DNA)...
2015: Laboratory Medicine
Adekola Alao, Claire Lewkowicz
OBJECTIVE: To describe the first case of sertraline-induced diplopia. METHOD: Medline and PubMed data search using the words sertraline, Zoloft, diplopia, double vision. A case summary of a patient who developed diplopia from sertraline. RESULT: This case describes a 34-year-old man who developed diplopia after treatment with sertraline. The diplopia resolved after discontinuation of sertraline and redeveloped upon rechallenge. CONCLUSION: Although incidences of diplopia caused by citalopram, another SSRI, have been described, to the best of our knowledge, this is the first reported case of sertraline-induced diplopia...
2015: International Journal of Psychiatry in Medicine
Mehdi Ben Said, Laurence Amar, David Smadja, Nadia Rivet, Sébastien Bertil, Anne-Marie Fischer, Dominique Helley, Pascale Gaussem
We report the case of a 20 years old man presenting two episodes of hematemesis. The patient was known to suffer from depression and was treated with sertraline (Zoloft®) for 6 months at the dosage of 100 mg/day. No endoscopic and radiological abnormality was found. The haemostasis report was normal. Exploration of platelet function was in favor of an abnormality of platelet secretion as evidenced by low epinephrine-induced aggregation, a slightly reduced aggregation for following agonists: TRAP, ADP 5 μM and 10 μM, and a longer latency to collagen...
September 2014: Annales de Biologie Clinique
Velthe Drinberg, Rivka Bitcover, Wolf Rajchenbach, Dan Peer
Inherent and acquired multiple drug resistance (MDR) to chemotherapeutic drugs is a major obstacle in cancer treatment. The ATP Binding Cassettes (ABC) transporter super family that act as extrusion pumps such as P-glycoprotein and multidrug-resistance-associated-proteins have prominent roles in cancer MDR. One of the most efficient strategies to modulate this active drug efflux from the cells is to physically block the pump proteins and thus change the balance between drug influx and efflux toward an accumulation of drug inside the cell, which eventually cumulates into cell death...
November 28, 2014: Cancer Letters
Athena K Petrides, Joshua Moskowitz, Kamisha L Johnson-Davis, Paul J Jannetto, Loralie J Langman, William Clarke, Mark A Marzinke
OBJECTIVES: Depression is a rapidly growing issue in the United States. There are many drug classes that may be used to treat depression, including the selective serotonin-reuptake inhibitors (SSRIs) citalopram (Celexa®) and sertraline (Zoloft®), as well as the aminoketone bupropion (Wellbutrin®). However, therapeutic efficacy and treatment success is often variable, requiring changes in dosing regimens or drug selection. Methods for drug quantification can become important tools in the assessment of drug efficacy to optimize treatment regimens...
October 2014: Clinical Biochemistry
Marnie G Silverstein, Colette Kirk El-Amin, Carol A Shively
Selective serotonin reuptake inhibitors (SSRI) are associated with an increased bleeding risk in humans. This report describes a bleeding event in a cynomolgus macaque (Macaca fascicularis) treated with the SSRI sertraline HCl (Zoloft). During the treatment course, the subject presented with a maculopapular rash, cutaneous bleeding, epistaxis, bleeding from the eye, melena, and a severe thrombocytopenia. To our knowledge, this report is the first description of an SSRI-related adverse event in a nonhuman primate...
June 2014: Comparative Medicine
Bryan W Brooks
A decade has now passed since our research group initially reported several adverse effects of fluoxetine to aquatic organisms commonly employed for developing environmental quality criteria, evaluating whole effluent toxicity, and monitoring ambient toxicity of surface waters and sediments. Our subsequent observation of fluoxetine, sertraline and their active metabolites (norfluoxetine and desmethylsertraline, respectively) accumulating in muscle, liver and brain tissues of three different fish species from an effluent-dominated stream was termed "Fish on Prozac...
June 2014: Aquatic Toxicology
Hien-Quang Do, E R R Chandrashekar, Gregory C Fu
A tertiary stereogenic center that bears two different aryl substituents is found in a variety of bioactive compounds, including medicines such as Zoloft and Detrol. We have developed an efficient method for the synthesis of enantioenriched 1,1-diarylalkanes from readily available racemic benzylic alcohols. Formation of a benzylic mesylate (which is not isolated), followed by treatment with an arylzinc reagent, LiI, and a chiral nickel/bis(oxazoline) catalyst, furnishes the Negishi cross-coupling product in high ee and good yield...
November 6, 2013: Journal of the American Chemical Society
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
Russell J Lewis, Mike K Angier, Kelly S Williamson, Robert D Johnson
Sertraline (Zoloft) is a selective serotonin reuptake inhibitor that is a commonly prescribed drug for the treatment of depression, obsessive-compulsive disorder, panic disorder, social anxiety disorder, premenstrual dysphoric disorder and post-traumatic stress disorder. Although the use of sertraline is relatively safe, certain side effects may negatively affect a pilot's performance and become a factor in an aviation accident. The authors' laboratory investigated the distribution of sertraline and its primary metabolite, desmethylsertraline, in various postmortem tissues and fluids obtained from 11 fatal aviation accident cases between 2001 and 2004...
May 2013: Journal of Analytical Toxicology
Graciela E Escudero, Verónica Ferraresi Curotto, Carlos H Laino, Reinaldo Pis Diez, Patricia A M Williams, Evelina G Ferrer
Mayor depression, obsessive-compulsive panic, social anxiety disorders are common diseases that are usually treated with sertraline hydrochloride which is the active ingredient of the well known drugs as Zoloft and Lustral. In this work, we presented a more complete vibrational characterization of the solid phase FT-IR spectra of Sertraline hydrochloride and its sertraline-iodine product in which the conformational space of the molecules was investigated performing molecular dynamic simulations within an NVT ensemble...
March 2013: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
A V Goriunov, M V Lobacheva
Efficacy and safety of sertraline (zoloft) have been assessed in 26 patients, aged from 7 to 15 years, with depressive states of different severity and psychopathological structure which are combined with obsessive-compulsive symptoms. Changes in patient's status are analyzed using psychometric scales during 6 weeks of treatment. It has been concluded that Zoloft is effective and safe drug for the treatment of mild to moderate depressive disorders concomitant to obsessive-compulsive disorders in children age...
2012: Zhurnal Nevrologii i Psikhiatrii Imeni S.S. Korsakova
N M Maksimova, O P Vertogradova
Peculiarities of the dynamics of anxious depression under the treatment with selective serotonergic antidepressants with different mechanisms of action on the serotonin reuptake were investigated. It was examined 61 patients with anxious depression (ICD-10 F32.1, F33.1, F34.1) treated with zoloft (sertraline) or coaxil (tianeptine) as a monotherapy. The following methods were used: clinical-psychopathological, psychometric (Hamilton Rating Scales for Depression and Anxiety, the Sheehan Patient-Related Anxiety Scale) and statistical analysis...
2012: Zhurnal Nevrologii i Psikhiatrii Imeni S.S. Korsakova
Ji Who Kim, Jae Sung Lee, Su Jin Kim, Lathika Hoigebazar, Kwang-Hee Shin, Kyung-Sang Yu, Wonsik Ahn, Jae Min Jeong, Dong Soo Lee
Sertraline hydrochloride (Zoloft®, Pfizer) is an antidepressant drug of the selective serotonin reuptake inhibitor (SSRI). The aims of this study were evaluating its in vivo distribution and kinetic models in human brain. Also, this study was to determine optimal scan duration of dynamic positron emission tomography (PET) for accurate [¹¹C]sertraline kinetic parameters and the feasibility of semi-quantitative approach for assessing distribution volume ratio (DVR). [¹¹C]sertraline dynamic PET and magnetic resonance imaging (MRI) scans were performed in 5 healthy males...
September 2012: Archives of Pharmacal Research
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