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Dextromethorphan

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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
#1
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
#2
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
#3
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
#4
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
#5
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
#6
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
#7
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
#8
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
#9
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
#10
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/28935657/use-of-hybrid-capillary-tube-setup-on-400mhz-nmr-for-quantitation-of-crucial-low-quantity-metabolites-using-asicco-signal
#11
Ranjeet Tiwari, Deepak Ahire, Hemantha Kumar, Sarmistha Sinha, Siddheshwar Kisan Chauthe, Murali Subramanian, Ramaswamy Iyer, Ramakanth Sarabu, Lakshmi Kant Bajpai
Metabolites of new chemical entities can influence safety and efficacy of a molecule and often times need to be quantified in preclinical studies. However, synthetic standards of metabolites are very rarely available in early discovery. Alternate approaches such as bio-synthesis needs to be explored to generate these metabolites. Assessing the quantity and purity of these small amounts of metabolites with a non-destructive analytical procedure becomes crucial. Quantitative nuclear magnetic resonance (qNMR) becomes the method of choice for these samples...
September 21, 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/28931647/randomized-open-label-trial-of-dextromethorphan-in-rett-syndrome
#12
RANDOMIZED CONTROLLED TRIAL
Constance L Smith-Hicks, Siddharth Gupta, Joshua B Ewen, Manisha Hong, Lisa Kratz, Richard Kelley, Elaine Tierney, Rebecca Vaurio, Genila Bibat, Abanti Sanyal, Gayane Yenokyan, Nga Brereton, Michael V Johnston, Sakkubai Naidu
OBJECTIVE: To determine safety and perform a preliminary assessment of dose-dependent efficacy of dextromethorphan in normalizing electrographic spikes, clinical seizures, and behavioral and cognitive functions in girls with Rett syndrome. METHODS: We used a prospective randomized, open-label trial in fast metabolizers of dextromethorphan to examine the effect of dextromethorphan on core clinical features of Rett syndrome. Interictal spike activity and clinical seizures were determined using EEG and parent reporting...
October 17, 2017: Neurology
https://www.readbyqxmd.com/read/28925030/drug-repurposing-may-generate-novel-approaches-to-treating-depression
#13
REVIEW
Mohamed Elsaed Ebada
OBJECTIVES: The breakthrough advancements in scientific medical research have greatly improved our understanding of the pathogenesis of depression, encouraging drug discoverers to take a shorter path than ever through drug repurposing to generate new antidepressant medications. In addition to reduced noradrenergic and serotonergic neurotransmission in the brain, other coincidence features such as glutamate neurotoxicity, inflammation and/or cerebrovascular insufficiency are implicated in the pathogenesis of major depressive disorder and late-life depression...
November 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28916283/deuterated-d6-dextromethorphan-elicits-antidepressant-like-effects-in-mice
#14
Linda Nguyen, Anna L Scandinaro, Rae R Matsumoto
The over-the-counter antitussive dextromethorphan (DM) may have rapid antidepressant actions based on its overlapping pharmacology with ketamine, which has shown fast antidepressant effects but whose widespread use remains limited by problematic side effects. We have previously shown that DM produces antidepressant-like effects in the forced swim test (FST) and tail suspension test (TST) that are mediated in part through α-amino-3-hydroxy-5-methyl-4-isoxazole propionic (AMPA) and sigma-1 receptors, two protein targets associated with a faster onset of antidepressant efficacy...
October 2017: Pharmacology, Biochemistry, and Behavior
https://www.readbyqxmd.com/read/28916251/mk-801-but-not-naloxone-attenuates-high-dose-dextromethorphan-induced-convulsive-behavior-possible-involvement-of-the-glun2b-receptor
#15
Hai-Quyen Tran, Yoon Hee Chung, Eun-Joo Shin, The-Vinh Tran, Ji Hoon Jeong, Choon-Gon Jang, Seung-Yeol Nah, Kiyofumi Yamada, Toshitaka Nabeshima, Hyoung-Chun Kim
Dextromethorphan (DM) is a dextrorotatory isomer of levorphanol, a typical morphine-like opioid. When administered at supra-antitussive doses, DM produces psychotoxic and neurotoxic effects in humans. Although DM abuse has been well-documented, few studies have examined the effects of high-dose DM. The present study aimed to explore the effects of a single high dose of DM on mortality and seizure occurrence. After intraperitoneal administration with a high dose of DM (80mg/kg), Sprague-Dawley rats showed increased seizure occurrence and intensity...
November 1, 2017: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/28900117/dextromethorphan-exhibits-anti-inflammatory-and-immunomodulatory-effects-in-a-murine-model-of-collagen-induced-arthritis-and-in-human-rheumatoid-arthritis
#16
Der-Yuan Chen, Chi-Chien Lin, Yi-Ming Chen, Ya-Hsuan Chao, Deng-Ho Yang
Dextromethorphan (d-3-methoxy-17-methylmorphinan, DXM) is a commonly used antitussive with a favorable safety profile. Previous studies have demonstrated that DXM has anti-inflammatory and immunomodulatory properties; however, the effect of DXM in rheumatoid arthritis (RA) remains unknown. Herein, we found that DXM treatment attenuated arthritis severity and proinflammatory cytokine expression levels, including TNF-α, IL-6, and IL-17A, in paw tissues of CIA mice. DXM treatment also reduced serum TNF-α, IL-6, and IL-17A levels of CIA mice and patients with RA...
September 12, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28891835/the-effect-of-dextromethorphan-premedication-on-cough-and-patient-tolerance-during-flexible-bronchoscopy-a-randomized-double-blind-placebo-controlled-trial
#17
Shahideh Amini, Soheil Peiman, Mahdi Khatuni, Marziyeh Ghalamkari, Besharat Rahimi
BACKGROUND: Patients undergoing bronchoscopy can experience problems such as anxiety and cough, requiring various doses of sedatives and analgesics. The purposes of this study were to investigate the effect of premedication with dextromethorphan on patients' cough and anxiety, and the use of analgesics/sedatives during flexible bronchoscopy (FB). METHODS: A randomized, double-blind, placebo-controlled, prospective study was performed to assess the effect of dextromethorphan premedication on patients who underwent diagnostic bronchoscopy...
October 2017: Journal of Bronchology & Interventional Pulmonology
https://www.readbyqxmd.com/read/28891561/online-monitoring-of-hepatic-rat-metabolism-by-coupling-a-liver-biochip-and-a-mass-spectrometer
#18
Franck Merlier, Rachid Jellali, Eric Leclerc
A microfluidic liver biochip was coupled with a mass spectrometer to detect in real time the drug metabolism of hepatocytes. The hepatocytes were cultivated in the biochip for 35 h. The biochip was placed in a small-scale incubator in which the temperature and CO2 concentration were controlled. The biochip was connected serially to a mass spectrometer, a peristaltic pump and a culture medium reservoir. The injection in the mass spectrometer was performed every 10 min for 11 h. The metabolism of midazolam, phenacetin, omeprazole, dextromethorphan, repaglinide, rosuvastatin, tolbutamide and caffeine was investigated...
September 25, 2017: Analyst
https://www.readbyqxmd.com/read/28877137/a-systematic-review-of-nmda-receptor-antagonists-for-treatment-of-neuropathic-pain-in-clinical-practice
#19
Rohit Aiyer, Neel Mehta, Semih Gungor, Amitabh Gulati
OBJECTIVE: To investigate the efficacy of N-methyl-D-aspartate receptor (NMDA) receptor antagonists for neuropathic pain and review literature to determine if specific pharmacologic agents provide adequate neuropathic pain relief. METHODS: Literature was reviewed on PubMed using a variety of key words for 8 NMDA receptor antagonists. These key words include: "Ketamine and Neuropathy", "Ketamine and Neuropathic Pain", "Methadone and Neuropathy", "Methadone and Neuropathic Pain", "Memantine and Neuropathic pain", "Memantine and Neuropathy", "Amantadine and Neuropathic Pain", "Amantadine and Neuropathy", "Dextromethorphan and Neuropathic Pain", "Dextromethorphan and Neuropathy", "Carbamazepine and Neuropathic Pain", "Carbamazepine and Neuropathy", "Valproic Acid and Neuropathy", "Valproic Acid and Neuropathic Pain", "Phenytoin and Neuropathy" and "Phenytoin and Neuropathic Pain"...
September 1, 2017: Clinical Journal of Pain
https://www.readbyqxmd.com/read/28867701/a-metabolic-study-on-the-biochemical-effects-of-chiral-illegal-drugs-in-rats-using-1-h-nmr-spectroscopy
#20
Kiyoshi Fukuhara, Akiko Ohno, Ruri Kikura-Hanajiri
Considering the pharmacological effects of chiral drugs, enantiopure drugs may differ from their racemic mixture formulation in efficacy, potency, or adverse effects. Levomethorphan (LVM) and Dextromethorphan (DXM) act on the central nervous system and exhibit different pharmacological features. LVM, the l-stereoisomer of methorphan, shows many similarities to opiates such as heroin, morphine and codeine, including the potential for addiction, while the d-stereoisomer, DXM, does not have the same opioid effect...
2017: Yakugaku Zasshi: Journal of the Pharmaceutical Society of Japan
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