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Dextromethorphan

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https://www.readbyqxmd.com/read/29327975/impact-of-cyp2d6-on-venlafaxine-metabolism-in-trinidadian-patients-with-major-depressive-disorder
#1
Lazara Karelia Montané Jaime, Jeffrey Paul, Anthony Lalla, George Legall, Andrea Gaedigk
AIM: This study aimed to assess the impact of CYP2D6 and CYP2C19 variation on venlafaxine (VEN) at steady state in patients from Trinidad and Tobago of Indian and African descent with major depressive disorder. PATIENTS & METHODS: Patients were phenotyped with dextromethorphan, genotyped for CYP2D6 and CYP2C19, and metabolic ratios for VEN obtained at 2-week intervals. RESULTS: Of 61 patients, 55 were genotyped and phenotyped and 47 completed 8 weeks of VEN treatment...
January 12, 2018: Pharmacogenomics
https://www.readbyqxmd.com/read/29327455/bioactivity-guided-fractionation-of-methanolic-extract-of-terminalia-arjuna-for-its-cyp3a-and-cyp2d-inhibition-in-rat-liver-microsomes
#2
Alice Varghese, Prachi Saboo, Sarika Wairkar
Terminalia arjuna (T. arjuna) is an Indian medicinal plant belonging to the family combretaceae and possesses numerous therapeutic activities including its immense cardio protective activity. In the present work, methanolic bark extract of T. arjuna was evaluated for the CYP3A and CYP2D inhibition potential in rat liver microsomes (RLM). Further, the methanolic bark extract was fractionated successively using increasing polarity solvents starting with petroleum ether, chloroform, ethyl acetate and n-butanol...
January 12, 2018: Biopharmaceutics & Drug Disposition
https://www.readbyqxmd.com/read/29311514/the-utility-of-the-artificial-taste-sensor-in-evaluating-the-bitterness-of-drugs-correlation-with-responses-of-human-taste2-receptors-htas2rs
#3
Tamami Haraguchi, Takahiro Uchida, Miyako Yoshida, Honami Kojima, Masaaki Habara, Hidekazu Ikezaki
The purpose of this study was to examine the ability of the artificial taste sensor to evaluate the bitterness of drugs by comparing the responses of the taste sensor with documented responses of human TASTE2 receptors (hTAS2Rs). For this purpose 22 bitter compounds, used as ingredients of pharmaceutical medicines in Japan and known ligands of hTAS2Rs, were selected for testing. Their solutions (0.01, 0.03, 0.1 mM) were evaluated by five different taste sensors (AC0, AN0, BT0, C00, AE1). Correlations between physicochemical parameters of the compounds and the responses of the taste sensors and hTAS2Rs were evaluated...
2018: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/29301012/diagnosis-of-heroin-overdose-in-an-8-year-old-boy-reliable-contribution-of-toxicological-investigations
#4
M Soichot, S Julliand, J Filatriau, A Hurbain, E Bourgogne, A Mihoubi, H Gourlain, B Delhotal-Landes
Toxicological investigations are often required by clinicians in comatose patients with suspected poisoning. However, the usefulness of toxicological analyses to support a diagnosis of acute poisoning is debated among clinicians and the interpretation of laboratory tests is challenging given the wide diversity of analytical techniques available. We report the case of an 8-year-old boy who was admitted to an intensive care unit with severe respiratory depression and neurological impairment. In order to formulate appropriate hypothesizes about the diagnosis and circumstances of intoxication, clinicians consulted toxicologists for a comprehensive toxicological screening...
December 28, 2017: Journal of Analytical Toxicology
https://www.readbyqxmd.com/read/29296031/dextromethorphan-in-cough-syrup-the-poor-man-s-psychosis
#5
Bridgette Martinak, Ramy A Bolis, Jeffrey Ryne Black, Rachel E Fargason, Badari Birur
Dextromethorphan (3-methoxy-N-methylmorphinan), also known as "DXM" and "the poor man's PCP," is a synthetically produced drug that is available in more than 140 over-the-counter cough and cold preparations. Dextromethorphan (DXM) has overtaken codeine as the most widely used cough suppressant due to its availability, efficacy, and safety profile at directed doses. However, DXM is subject to abuse. When consumed at inappropriately high doses (over 1500 mg/day), DXM can induce a state of psychosis characterized by Phencyclidine (PCP)-like psychological symptoms, including delusions, hallucinations, and paranoia...
September 15, 2017: Psychopharmacology Bulletin
https://www.readbyqxmd.com/read/29260900/trends-in-dextromethorphan-cough-and-cold-products-2000-2015-national-poison-data-system-intentional-abuse-exposure-calls
#6
Sara Karami, Jacqueline M Major, Silvia Calderon, Jana K McAninch
CONTEXT: Recent restrictions in access to and availability of dextromethorphan (DXM) cough and cold medications may correlate with changes in abuse exposures. OBJECTIVE: To extend and update existing knowledge about DXM abuse, we describe recent trends and patterns of calls to poison control centers involving DXM abuse, by demographics, geography, common brands, and medical outcomes. METHODS: We utilized data from the National Poison Data System (NPDS) maintained by the American Association of Poison Control Centers (AAPCC), which captures data on calls to U...
December 20, 2017: Clinical Toxicology
https://www.readbyqxmd.com/read/29232638/engineering-a-self-sufficient-mycobacterium-tuberculosis-cyp130-by-gene-fusion-with-the-reductase-domain-of-cyp102a1-from-bacillus-megaterium
#7
Sandra Ortega Ugalde, Rosa A Luirink, Daan P Geerke, Nico P E Vermeulen, Wilbert Bitter, Jan N M Commandeur
CYP130 belongs to the subset of cytochrome P450s from Mycobacterium tuberculosis (Mtb) that have been structurally characterized. Despite several efforts for its functional characterization, CYP130 is still considered an orphan enzyme for which no endogenous or exogenous substrate has been identified. In addition, functional redox-partners for CYP130 have not been clearly established yet, hampering the elucidation of its physiological role. In the present study, a catalytically active fusion protein involving CYP130 and the NADPH reductase-domain of CYP102A1 from Bacillus megaterium was created...
December 7, 2017: Journal of Inorganic Biochemistry
https://www.readbyqxmd.com/read/29210063/opioid-induced-inhibition-of-the-human-serotonin-and-norepinephrine-transporters-in-vitro-link-to-clinical-reports-of-serotonin-syndrome
#8
Anna Rickli, Evangelia Liakoni, Marius C Hoener, Matthias E Liechti
BACKGROUND AND PURPOSE: Opioids may inhibit the serotonin and norepinephrine transporters (SERT and NET, respectively). NET inhibition may contribute to analgesia, and SERT inhibition or interactions with serotonin receptors may cause serotonergic toxicity. However, the effects of different opioids on the human SERT, NET, and serotonin receptors have not been sufficiently studied. EXPERIMENTAL APPROACH: We determined the potencies of different opioids to inhibit the SERT and NET in vitro using human transporter-transfected cells...
December 6, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29178272/evaluation-of-modafinil-as-a-perpetrator-of-metabolic-drug-drug-interactions-using-a-model-informed-cocktail-reaction-phenotyping-trial-protocol
#9
Angela Rowland, Madelé van Dyk, David Warncken, Arduino A Mangoni, Michael J Sorich, Andrew Rowland
AIM: To evaluate the capacity for modafinil to be a perpetrator of metabolic drug-drug interactions by altering cytochrome P450 activity following a single dose and dosing to steady state. METHODS: A single centre, open label, single sequence cocktail drug interaction trial. On days 0, 2 and 8 participants were administered an oral drug cocktail comprising 100 mg caffeine, 30 mg dextromethorphan, 25 mg losartan, 1 mg midazolam, and 20 mg enteric-coated omeprazole...
November 26, 2017: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/29162429/studies-with-psychedelic-drugs-in-human-volunteers
#10
REVIEW
Edward M Sellers, Myroslava K Romach, Deborah B Leiderman
Scientific curiosity and fascination have played a key role in human research with psychedelics along with the hope that perceptual alterations and heightened insight could benefit well-being and play a role in the treatment of various neuropsychiatric disorders. These motivations need to be tempered by a realistic assessment of the hurdles to be cleared for therapeutic use. Development of a psychedelic drug for treatment of a serious psychiatric disorder presents substantial although not insurmountable challenges...
November 21, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/29131506/development-of-a-capillary-electrophoresis-method-for-the-determination-of-the-chiral-purity-of-dextromethorphan-by-a-dual-selector-system-using-quality-by-design-methodology
#11
Sulaiman Krait, Matthias Heuermann, Gerhard K E Scriba
Dextromethorphan is a centrally acting antitussive drug, while its enantiomer levomethorphan is an illicit drug with opioid analgesic effects. As capillary electrophoresis has been proven as an ideal technique for enantiomer analysis, the present study was conducted in order to develop a capillary-electrophoresis-based limit test for levomethorphan. The analytical target profile was defined that the method should be able to determine levomethorphan with acceptable precision and accuracy at the 0.1 % level. From initial scouting experiments, a dual selector system consisting of sulfated β-cyclodextrin and methyl-α-cyclodextrin was identified...
November 13, 2017: Journal of Separation Science
https://www.readbyqxmd.com/read/29128750/reduction-of-interferences-in-the-analysis-of-children-s-dimetapp-using-ultraviolet-spectroscopy-data-and-target-factor-analysis
#12
Huggins Z Msimanga, Truong Thach Ho Lam, Nathaniel Latinwo, Mihyang Kristy Song, Newsha Tavakoli
A calibration matrix has been developed and successfully applied to quantify actives in Children's Dimetapp®, a cough mixture whose active components suffer from heavy spectral interference. High-performance liquid chromatography/photodiode array instrument was used to identify the actives and any other UV-detectable excipients that might contribute to interferences. The instrument was also used to obtain reference data on the actives, instead of relying on the manufacturer's claims. Principal component analysis was used during the developmental stages of the calibration matrix to highlight any mismatch between the calibration and sample spectra, making certain that "apples" were not compared with "oranges"...
November 3, 2017: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
https://www.readbyqxmd.com/read/29118196/the-involvement-of-n-methyl-d-aspartate-receptors-in-plasticity-induced-by-paired-corticospinal-motoneuronal-stimulation-in-humans
#13
Siobhan C Donges, Jessica M D'Amico, Jane E Butler, Janet L Taylor
Plasticity can be induced at human corticospinal-motoneuronal synapses by delivering repeated, paired stimuli to corticospinal axons and motoneurones in a technique called paired corticospinal-motoneuronal stimulation (PCMS). To date, the mechanisms of the induced plasticity are unknown. To determine whether PCMS-induced plasticity is dependent on N-methyl-D-aspartate receptors (NMDARs), the effect of the non-competitive NMDAR antagonist, dextromethorphan, on PCMS-induced facilitation was assessed in a two-day, double-blind, placebo-controlled experiment...
November 8, 2017: Journal of Neurophysiology
https://www.readbyqxmd.com/read/29116367/double-blind-comparison-of-the-two-hallucinogens-psilocybin-and-dextromethorphan-similarities-and-differences-in-subjective-experiences
#14
Theresa M Carbonaro, Matthew W Johnson, Ethan Hurwitz, Roland R Griffiths
RATIONALE: Although psilocybin and dextromethorphan (DXM) are hallucinogens, they have different receptor mechanisms of action and have not been directly compared. OBJECTIVE: This study compared subjective, behavioral, and physiological effects of psilocybin and dextromethorphan under conditions that minimized expectancy effects. METHODS: Single, acute oral doses of psilocybin (10, 20, 30 mg/70 kg), DXM (400 mg/70 kg), and placebo were administered under double-blind conditions to 20 healthy participants with histories of hallucinogen use...
November 7, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/29115994/exploring-venlafaxine-pharmacokinetic-variability-with-a-phenotyping-approach-a-multicentric-french-swiss-study-marvel-study
#15
Célia Lloret-Linares, Youssef Daali, Sylvie Chevret, Isabelle Nieto, Fanny Molière, Philippe Courtet, Florence Galtier, Raphaëlle-Marie Richieri, Sophie Morange, Pierre-Michel Llorca, Wissam El-Hage, Thomas Desmidt, Frédéric Haesebaert, Philippe Vignaud, Jerôme Holtzmann, Jean-Luc Cracowski, Marion Leboyer, Antoine Yrondi, Fabienne Calvas, Liova Yon, Philippe Le Corvoisier, Olivier Doumy, Kyle Heron, Damien Montange, Siamak Davani, Julien Déglon, Marie Besson, Jules Desmeules, Emmanuel Haffen, Frank Bellivier
BACKGROUND: It is well known that the standard doses of a given drug may not have equivalent effects in all patients. To date, the management of depression remains mainly empirical and often poorly evaluated. The development of a personalized medicine in psychiatry may reduce treatment failure, intolerance or resistance, and hence the burden and costs of mood depressive disorders. The Geneva Cocktail Phenotypic approach presents several advantages including the "in vivo" measure of different cytochromes and transporter P-gp activities, their simultaneous determination in a single test, avoiding the influence of variability over time on phenotyping results, the administration of low dose substrates, a limited sampling strategy with an analytical method developed on DBS analysis...
November 7, 2017: BMC Pharmacology & Toxicology
https://www.readbyqxmd.com/read/29055108/semi-quantitative-analysis-of-tramadol-dextromethorphan-and-metabolites-in-decomposed-skeletal-tissues-by-ultra-performance-liquid-chromatography-quadrupole-time-of-flight-mass-spectrometry-uplc-qtof-ms
#16
H M Cornthwaite, L Labine, J H Watterson
The use of filtration/pass-through extraction (FPTE) and ultra-performance liquid chromatography quadrupole time-of-flight mass spectrometry (UPLC-qTOF-MS) to detect tramadol (TRAM), dextromethorphan (DXM) and metabolites from skeletal remains is described. Rats (n=5) received 50 mg/kg tramadol and were euthanized by CO2 asphyxiation approximately 30 min post-dose. Rats (n=4) received 75 mg/kg dextromethorphan and were euthanized by CO2 asphyxiation approximately 45 min post-dose. Remains decomposed to skeleton outdoors and vertebral bones were collected...
October 20, 2017: Drug Testing and Analysis
https://www.readbyqxmd.com/read/29049110/evidence-for-the-efficacy-of-systemic-opioid-sparing-analgesics-in-pediatric-surgical-populations-a-systematic-review
#17
REVIEW
Alyssa Zhu, Hubert A Benzon, T Anthony Anderson
While a large number of studies has examined the efficacy of opioid-sparing analgesics in adult surgical populations, fewer studies are available to guide postoperative pain treatment in pediatric patients. We systematically reviewed available publications on the use of systemic nonopioid agents for postoperative analgesia in pediatric surgical populations. A comprehensive literature search identified meta-analyses and randomized controlled trials (RCTs) assessing the effects of systemic, nonopioid agents on postoperative narcotic requirements or pain scores in pediatric surgical populations...
November 2017: Anesthesia and Analgesia
https://www.readbyqxmd.com/read/29019074/in-vitro-inhibitory-effect-of-gymnema-sylvestre-extracts-and-total-gymnemic-acids-fraction-on-select-cytochrome-p450-activities-in-rat-liver-microsomes
#18
Madhuri Vaghela, Krishna Iyer, Nancy Pandita
BACKGROUND AND OBJECTIVES: Gymnema sylvestre R. Br. is a well-known Indian medicinal herb. Gymnemic acids are pentacyclic triterpenes saponins and active phytoconstituents of Gymnema sylvestre. The study aimed at evaluation of the in vitro rat liver cytochrome P450 (CYP) inhibition potential of extracts and total gymnemic acid (TA)-enriched fractions from G. sylvestre. METHODS: Standardization of G. sylvestre [ethanolic (EL), hydroethanolic (HE), total acid of ethanolic (TAE), total acid of hydroethanolic (TAHE) and total acid of aqueous (TAAQ) extract] was done with respect to deacyl gymnemic acid (DAGA), using reverse phase-high performance liquid chromatography (RP-HPLC)...
October 10, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28940476/impact-of-cyp2d6-functional-allelic-variations-on-phenoconversion-and-drug-drug-interactions
#19
F Storelli, A Matthey, S Lenglet, A Thomas, J Desmeules, Y Daali
We investigated whether CYP2D6 extensive metabolizers (EM) carrying a non-functional allele are at higher risk of phenoconversion to poor metabolizers in presence of CYP2D6 inhibitors. Seventeen homozygous carriers of two fully-functional alleles and seventeen heterozygous carriers of one fully-functional and one non-functional allele participated in this trial. Dextromethorphan 5mg and tramadol 10mg were given at each of the three study sessions. CYP2D6 was inhibited by duloxetine 60mg (session 2) and paroxetine 20mg (session 3)...
September 23, 2017: Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/28936010/dextromethorphan-in-cough-syrup-the-poor-man-s-psychosis
#20
Bridgette Martinak, Ramy A Bolis, Jeffrey Ryne Black, Rachel E Fargason, Badari Birur
Dextromethorphan (3-methoxy-N-methylmorphinan), also known as "DXM" and "the poor man's PCP," is a synthetically produced drug that is available in more than 140 over-the-counter cough and cold preparations. Dextromethorphan (DXM) has overtaken codeine as the most widely used cough suppressant due to its availability, efficacy, and safety profile at directed doses. However, DXM is subject to abuse. When consumed at inappropriately high doses (over 1500 mg/day), DXM can induce a state of psychosis characterized by Phencyclidine (PCP)-like psychological symptoms, including delusions, hallucinations, and paranoia...
September 15, 2017: Psychopharmacology Bulletin
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