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pharmacokinetics, antidepressant

Jennifer L Schroeck, James Ford, Erin L Conway, Kari E Kurtzhalts, Megan E Gee, Krista A Vollmer, Kari A Mergenhagen
PURPOSE: Insomnia is problematic for older adults. After behavioral modifications fail to show adequate response, pharmacologic options are used. The pharmacokinetics of agents used to treat insomnia may be altered. This review focuses on the safety and efficacy of medications used to treat insomnia. METHODS: A literature search of Medline, PubMed, and Embase was conducted (January 1966-June 2016). It included systematic reviews, randomized controlled trials, observational studies, and case series that had an emphasis on insomnia in an older population...
October 14, 2016: Clinical Therapeutics
R Rolke, S Rolke, S Hiddemann, M Mücke, H Cuhls, L Radbruch, F Elsner, V Peuckmann-Post
Cancer pain and pain associated with non-neoplastic diseases can be associated with pain mechanisms, such as a peripheral or central sensitization or deafferentation. The clarification allows indirect conclusions about the underlying mechanisms based on clinical signs, such as allodynia or hyperalgesia. Non-opioid analgesics are the basis of cancer pain therapy according to the World Health Organization (WHO) pain ladder. In the case of severe cancer pain, treatment can be escalated directly from level 1 to level 3...
October 2016: Der Internist
Anna Höflich, Andreas Hahn, Martin Küblböck, Georg S Kranz, Thomas Vanicek, Sebastian Ganger, Marie Spies, Christian Windischberger, Siegfried Kasper, Dietmar Winkler, Rupert Lanzenberger
Over the last years, a number of studies have been conducted to clarify the neurobiological correlates of ketamine application. However, comprehensive information regarding the influence of ketamine on cortical activity is still lacking. Using resting-state functional MRI and integrating pharmacokinetic information, a double-blind, randomized, placebo-controlled, crossover study was performed to determine the effects of ketamine on neuronal activation. During a 55 min resting-state fMRI scan, esketamine (Ketanest S(®)) was administered intravenously to 35 healthy volunteers...
August 30, 2016: Brain Structure & Function
Euitae Kim, Oliver D Howes, Bo-Hyung Kim, Myong-Wuk Chon, Seongho Seo, Federico E Turkheimer, Jae Sung Lee, Yun-Sang Lee, Jun Soo Kwon
BACKGROUND AND OBJECTIVE: Escitalopram is one of the most commonly prescribed selective serotonin reuptake inhibitors (SSRIs). It is thought to act by blocking the serotonin transporter (SERT). However, its dose-SERT occupancy relationship is not well known, so it is not clear what level of SERT blockade is achieved by currently approved doses. METHODS: To determine the dose-occupancy relationship, we measured serial SERT occupancy using [(11)C]DASB [3-amino-4-(2-dimethylaminomethylphenylsulfanyl)-benzonitrile] positron emission tomography (PET) and plasma drug concentrations after the administration of escitalopram in 12 healthy volunteers...
August 24, 2016: Clinical Pharmacokinetics
Cheedy Jaja, Nadine Barrett, Niren Patel, Matt Lyon, Hongyan Xu, Abdullah Kutlar
AIMS: Interindividual variability in drug response and adverse effects have been described for proton pump inhibitors, anticonvulsants, selective serotonin reuptake inhibitors, tricyclic antidepressants, and anti-infectives, but little is known about the safety and efficacy of these medications in patients with sickle cell disease (SCD). We genotyped the CYP2C19 gene which has been implicated in the metabolism of these drugs in an SCD patient cohort to determine the frequencies of reduced function, increased function, or complete loss-of-function variants...
October 2016: Genetic Testing and Molecular Biomarkers
Jennifer E Sager, Lauren S L Price, Nina Isoherranen
Bupropion is a widely used antidepressant, smoking cessation aid, and weight-loss therapy. It is administered as a racemic mixture, but the pharmacokinetics and activity of bupropion are stereoselective. The activity and side effects of bupropion are attributed to bupropion and its metabolites S,S- and R,R-OH-bupropion, threohydrobupropion, and erythrohydrobupropion. Yet the stereoselective metabolism in vitro and the enzymes contributing to the stereoselective disposition of bupropion have not been characterized...
October 2016: Drug Metabolism and Disposition: the Biological Fate of Chemicals
J D Bergiannaki, P Kostaras
The gender based or gender sensitive pharmacology is a new research area. Differences among sexes are observed in several parameters of their pharmacokinetic which may relate to alteration of their pharmacodynamic as well. Most psychotropics are given per os, and the greater part of their absorption takes place in the small intestine. Premenopausal women have slower gastric emptying times and lower gastrointestinal blood flow which probably reduces the extent of drug absorption. The distribution of drugs is influenced by the relative lower body mass index, the lower blood volume and flow and the greater percentage of body fat of women...
April 2016: Psychiatrikē, Psychiatriki
Erin N Berry-Bibee, Myong-Jin Kim, Katharine B Simmons, Naomi K Tepper, Halley E M Riley, H Pamela Pagano, Kathryn M Curtis
OBJECTIVE: To examine whether the co-administration of hormonal contraceptives (HC) and psychotropic drugs commonly used to treat anxiety and/or depression results in safety or efficacy concerns for either drug. METHODS: We searched PubMed and Cochrane libraries for clinical or pharmacokinetic (PK) studies that examined co-administration of any HC with psychotropic drugs [selective serotonin reuptake inhibitors (SSRIs), serotonin-norepinephrine reuptake inhibitors (SNRIs), tricyclic antidepressants (TCAs), oral benzodiazepines, bupropion, mirtazapine, trazadone, buspirone, hydroxyzine, monoamine oxidase inhibitors (MAOIs), or atypical antipsychotics] in reproductive aged women...
July 18, 2016: Contraception
Hoa Q Nguyen, Ernesto Callegari, R Scott Obach
Major circulating drug metabolites can be as important as the drugs themselves in efficacy and safety, so establishing methods whereby exposure to major metabolites following administration of parent drug can be predicted is important. In this study, imipramine, a tricyclic antidepressant, and its major metabolite desipramine were selected as a model system to develop metabolite prediction methods. Imipramine undergoes N-demethylation to form the active metabolite desipramine, and both imipramine and desipramine are converted to hydroxylated metabolites by the polymorphic enzyme CYP2D6...
October 2016: Drug Metabolism and Disposition: the Biological Fate of Chemicals
Alan L Pehrson, Todd M Hillhouse, Nasser Haddjeri, Renaud Rovera, Joseph H Porter, Arne Mørk, Gennady Smagin, Dekun Song, David Budac, Manuel Cajina, Connie Sanchez
Major depressive disorder (MDD) is a common psychiatric disorder that often features impairments in cognitive function, and these cognitive symptoms can be important determinants of functional ability. Vortioxetine is a multimodal antidepressant that may improve some aspects of cognitive function in patients with MDD, including attention, processing speed, executive function, and memory. However, the cause of these effects is unclear, and there are several competing theories on the underlying mechanism, notably including regionally-selective downstream enhancement of glutamate neurotransmission and increased acetylcholine (ACh) neurotransmission...
September 2016: Journal of Pharmacology and Experimental Therapeutics
Yanwei Li, Lin Li, Christian Hölscher
Central neurodegenerative diseases, such as Alzheimer's disease (AD) and Parkinson's disease (PD), are one of the biggest health problems worldwide. Currently, there is no cure for these diseases. The Gardenia jasminoides fruit is a common herbal medicine in traditional Chinese medicine (TCM), and a variety of preparations are used as treatments for central nervous system (CNS) diseases. Pharmacokinetic studies suggest genipin is one of the main effective ingredients of G. jasminoides fruit extract (GFE). Accumulated research data show that genipin possesses a range of key pharmacological properties, such as anti-inflammatory, neuroprotective, neurogenic, antidiabetic, and antidepressant effects...
October 2016: CNS Drugs
Weronika Stasiuk, Anna Serefko, Aleksandra Szopa, Elżbieta Wyska, Katarzyna Świąder, Piotr Wlaź, Ewa Poleszak
BACKGROUND: The main objective of our study was to evaluate the influence of traxoprodil on the activity of the atypical antidepressant drugs (agomelatine, mianserin, tianeptine). METHODS: The forced swim test (FST) in mice was used to determine the antidepressant-like activity of the tested agents. Drugs levels in brain tissue were assessed by a high performance liquid chromatography method. RESULTS: Concurrent intraperitoneal administration of per se ineffective doses of traxoprodil (10mg/kg) and agomelatine (20mg/kg) shortened the immobility time of animals in the FST...
October 2016: Pharmacological Reports: PR
Vincenzo Prisco, Teresa Iannaccone, Adriano Tusciano, Mariangela Boccardi, Francesco Perris, Annalisa Capuano, Francesco Catapano, Michele Fabrazzo
OBJECTIVE: Monitoring drug-related side effects in psychiatric patients is highly recommended. In fact, frequent exposure to long-term polipharmacotherapy, poor compliance to pharmachological treatment and comorbidity with organic illnesses requiring the prescription of other drugs are causes of pharmacokinetic/pharmacodynamic interactions. These vulnerability factors result in a certain increase in adverse drug reactions (ADRs). METHODS: This study performes an analysis of Italian Medicine Agency data, in the section "signal analysis", to attempt an assessment of the safety warnings among the different psychotropic drug classes, belonging to the ATC class: N03 (antiepileptics), N05 (antipsychotics), N06 (psycho-analectic drugs)...
May 2016: Rivista di Psichiatria
Christopher M Bland, April Miller Quidley, Bryan L Love, Catherine Yeager, Bliss McMichael, P Brandon Bookstaver
PURPOSE: Pharmacists' role in optimizing long-term pharmacotherapy for bariatric surgery patients is detailed. SUMMARY: Bariatric surgery patients provide a difficult challenge in terms of many pharmacotherapy issues, especially in the chronic care setting, where data on long-term effects of bariatric surgery are limited. The most common procedures are Roux-en-Y gastric bypass (RYGB), adjustable gastric banding, and sleeve gastrectomy. Sleeve gastrectomy has become the most common procedure in the United States, primarily because it has less overall chronic malabsorption effects than RYGB...
August 15, 2016: American Journal of Health-system Pharmacy: AJHP
Pone Kamdem Boniface, Sabrina Baptista Ferreira, Carlos Roland Kaiser
ETHNOPHARMACOLOGICAL RELEVANCE: Alchornea cordifolia (Schumach. & Thonn.) Muell. Arg. (Euphorbiaceae) (A. cordifolia) is widely distributed throughout tropical Africa, where it is used extensively in traditional medicine. Conditions for which the plant has enjoyed wide use are: coughs, gonorrhoea, infertility, prostatitis, bacterial infections, diarrhoea, ulcers, pain, inflammation, fever and bronchial troubles. This review summarizes the achievements of the investigations in traditional uses, ethnobotany, phytochemistry, biological activities and toxicological profile of A...
September 15, 2016: Journal of Ethnopharmacology
Malik Nassan, Wayne T Nicholson, Michelle A Elliott, Carolyn R Rohrer Vitek, John L Black, Mark A Frye
Antidepressants are commonly prescribed medications in the United States, and there is increasing interest in individualizing treatment selection for more than 20 US Food and Drug Administration-approved treatments for major depressive disorder. Providing greater precision to pharmacotherapeutic recommendations for individual patients beyond the large-scale clinical trials evidence base can potentially reduce adverse effect toxicity profiles and increase response rates and overall effectiveness. It is increasingly recognized that genetic variation may contribute to this differential risk to benefit ratio and thus provides a unique opportunity to develop pharmacogenetic guidelines for psychiatry...
July 2016: Mayo Clinic Proceedings
Monika Banach, Monika Popławska, Barbara Błaszczyk, Kinga K Borowicz, Stanisław J Czuczwar
INTRODUCTION: Epilepsy may be frequently associated with psychiatric disorders and its co-existence with depression usually results in the reduced quality of life of patients with epilepsy. Also, the efficacy of antiepileptic treatment in depressed patients with epilepsy may be significantly reduced. AREAS COVERED: Results of experimental studies indicate that antidepressants co-administered with antiepileptic drugs may either increase their anticonvulsant activity, remain neutral or decrease the protective action of antiepileptic drugs in models of seizures...
September 2016: Expert Opinion on Drug Metabolism & Toxicology
Andrea R Masters, Brandon T Gufford, Jessica Bo Li Lu, Ingrid F Metzger, David R Jones, Zeruesenay Desta
Bupropion, widely used as an antidepressant and smoking cessation aid, undergoes complex metabolism to yield numerous metabolites with unique disposition, effect, and drug-drug interactions (DDIs) in humans. The stereoselective plasma and urinary pharmacokinetics of bupropion and its metabolites were evaluated to understand their potential contributions to bupropion effects. Healthy human volunteers (n = 15) were administered a single oral dose of racemic bupropion (100 mg), which was followed by collection of plasma and urine samples and determination of bupropion and metabolite concentrations using novel liquid chromatography-tandem mass spectrometry assays...
August 2016: Journal of Pharmacology and Experimental Therapeutics
James E Tisdale
Torsades de pointes (TdP) is a life-threatening arrhythmia associated with prolongation of the corrected QT (QTc) interval on the electrocardiogram. More than 100 drugs available in Canada, including widely used antibiotics, antidepressants, cardiovascular drugs and many others, may cause QTc interval prolongation and TdP. Risk factors for TdP include QTc interval >500 ms, increase in QTc interval ≥60 ms from the pretreatment value, advanced age, female sex, acute myocardial infarction, heart failure with reduced ejection fraction, hypokalemia, hypomagnesemia, hypocalcemia, bradycardia, treatment with diuretics and elevated plasma concentrations of QTc interval-prolonging drugs due to drug interactions, inadequate dose adjustment of renally eliminated drugs in patients with kidney disease and rapid intravenous administration...
May 2016: Canadian Pharmacists Journal: CPJ, Revue des Pharmaciens du Canada: RPC
Qiong-Yin Fan, Rui Xue, Ying Li, Ting-Ting Zhang, Xin-Hua He, Shi-Yong Fan, Yun-Feng Li, Bo-Hua Zhong, You-Zhi Zhang, Jin Li
AIMS: The present study was conducted to evaluate the antidepressant-like effects of ZBH2012001, a novel potential serotonin and norepinephrine reuptake inhibitor (SNRI). METHODS: Competitive binding assays, calcium flow, and cAMP detection methods were used to determine the affinity of ZBH2012001 for serotonin transporters (SERTs) and norepinephrine transporters (NETs), as well as its selectivity over dopamine transporters (DATs) and 16 other G-protein-coupled receptors (GPCRs) or iron channels...
August 2016: CNS Neuroscience & Therapeutics
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