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dextromethorphan The d-isomer of the codeine analog of levorphanol. Dextromethorphan shows high affinity binding to several regions of the brain, including the medullary cough center. This compound is an NMDA receptor antagonist and acts as a non-competitive channel blocker. It is one of the widely used antitussives, and is also used to study the involvement of glutamate receptors in neurotoxicity.


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(d-Methorphan, Delsym, Dextromethorphan Hydrobromide, Benylin DM, Creo-Terpin, Drixoral, Trocal)

Articles



PubmedDevelopmental Changes in Human Liver CYP2D6 Expression.
Authors:  Stevens JC, Marsh SA, Zaya MJ, Regina KJ, Le M, Hines RN
Journal: Drug Metab Dispos

PubmedDextromethorphan and quinidine combination for heroin detoxification.
Authors:  Akerele E, Bisaga A, Sullivan MA, Garawi F, Comer SD, Thomas AA, Nunes EV, Kleber HD
Journal: Am J Addict

PubmedMetabolite profiling in human urine by LC-MS/MS: Method optimization and application for glucuronides from dextromethorphan metabolism.
Authors:  Lutz U, Bittner N, Lutz RW, Lutz WK
Journal: J Chromatogr B Analyt Technol Biomed Life Sci

PubmedSocial reward-conditioned place preference: A model revealing an interaction between cocaine and social context rewards in rats.
Authors:  Thiel KJ, Okun AC, Neisewander JL
Journal: Drug Alcohol Depend

PubmedEffect of dextromethorphan on antinociception and tolerance induced by swim-stress in the formalin test.
Authors:  Fazli-Tabaei S, Maghsoudi A, Bazaz N, Modirzadeh A, Zarrindast MR
Journal: Arch Iran Med

PubmedAn update on the pharmacological management of post-herpetic neuralgia and painful diabetic neuropathy.
Authors:  Zin CS, Nissen LM, Smith MT, O'Callaghan JP, Moore BJ
Journal: CNS Drugs

PubmedDevelopment and validation of ELISA and GC-MS procedures for the quantification of dextromethorphan and its main metabolite dextrorphan in urine and oral fluid.
Authors:  Rodrigues WC, Wang G, Moore C, Agrawal A, Vincent MJ, Soares JR
Journal: J Anal Toxicol

PubmedEvaluation of HepaRG Cells as an In Vitro Model for Human Drug Metabolism Studies.
Authors:  Kanebratt KP, Andersson TB
Journal: Drug Metab Dispos

PubmedRole of endogenous sleep-wake and analgesic systems in anesthesia.
Authors:  Lu J, Nelson LE, Franks N, Maze M, Chamberlin NL, Saper CB
Journal: J Comp Neurol

PubmedPharmacokinetic effect of AMD070, an Oral CXCR4 antagonist, on CYP3A4 and CYP2D6 substrates midazolam and dextromethorphan in healthy volunteers.
Authors:  Nyunt MM, Becker S, MacFarland RT, Chee P, Scarborough R, Everts S, Calandra GB, Hendrix CW
Journal: J Acquir Immune Defic Syndr

PubmedLife-Threatening Dextromethorphan Intoxication Associated with Interaction with Amitriptyline in a Poor CYP2D6 Metabolizer: A Single Case Re-exposure Study.
Authors:  Forget P, le Polain de Waroux B, Wallemacq P, Gala JL
Journal: J Pain Symptom Manage

PubmedChanges in maternal liver Cyp2c and Cyp2d expression and activity during rat pregnancy.
Authors:  Dickmann LJ, Tay S, Senn TD, Zhang H, Visone A, Unadkat JD, Hebert MF, Isoherranen N
Journal: Biochem Pharmacol

PubmedBrain levels of dextromethorphan and the intensity of opioid withdrawal in mice.
Authors:  Bisaga A, Kos T, Wójcikowski J, Daniel WA, Popik P
Journal: Drug Alcohol Depend

PubmedIsobolographic analysis of epinephrine with bupivacaine, dextromethorphan, 3-methoxymorphinan, or dextrorphan on infiltrative anesthesia in rats: dose-response studies.
Authors:  Chen YW, Liu KS, Wang JJ, Chou W, Hung CH
Journal: Reg Anesth Pain Med

PubmedLack of interaction of the NMDA receptor antagonists dextromethorphan and dextrorphan with P-glycoprotein.
Authors:  Kanaan M, Daali Y, Dayer P, Desmeules J
Journal: Curr Drug Metab

PubmedSigma ligands, but not N-methyl-D-aspartate antagonists, reduce levodopa-induced dyskinesias.
Authors:  Paquette MA, Brudney EG, Putterman DB, Meshul CK, Johnson SW, Berger SP
Journal: Neuroreport

PubmedAssessment of antitussive efficacy of dextromethorphan in smoking related cough: objective vs. subjective measures.
Authors:  Ramsay J, Wright C, Thompson R, Hull D, Morice AH
Journal: Br J Clin Pharmacol

PubmedDextromethorphan is protective against sensitized N-methyl-D-aspartate receptor-mediated excitotoxic brain damage in the developing mouse brain.
Authors:  Keller M, Griesmaier E, Auer M, Schlager G, Urbanek M, Simbruner G, Gressens P, Sárközy G
Journal: Eur J Neurosci

PubmedSex differences in NMDA antagonist enhancement of morphine antihyperalgesia in a capsaicin model of persistent pain: comparisons to two models of acute pain.
Authors:  Lomas LM, Terner JM, Picker MJ
Journal: Pharmacol Biochem Behav

PubmedEffect of the NMDA-receptor antagonist dextromethorphan in infant rat pneumococcal meningitis.
Authors:  Sellner J, Ringer R, Baumann P, Perey MJ, Schmitt B, Leib SL
Journal: Curr Drug Metab

PubmedCYP2D6 phenotype prediction from genotype: which system is the best?
Authors:  Kirchheiner J
Journal: Clin Pharmacol Ther

PubmedIt's nothing to laugh about: understanding disorders of emotional expression.
Authors:  Martin CM
Journal: Consult Pharm

PubmedNeuropsychotoxicity of abused drugs: potential of dextromethorphan and novel neuroprotective analogs of dextromethorphan with improved safety profiles in terms of abuse and neuroprotective effects.
Authors:  Shin EJ, Lee PH, Kim HJ, Nabeshima T, Kim HC
Journal: J Pharmacol Sci

PubmedCYP2D6 phenotyping with dextromethorphan.
Authors:  Wojtczak A, Rychlik-Sych M, Krochmalska-Ulacha E, Skretkowicz J
Journal: Pharmacol Rep

PubmedEffect of an Antiretroviral Regimen Containing Ritonavir Boosted Lopinavir on Intestinal and Hepatic CYP3A, CYP2D6 and P-glycoprotein in HIV-infected Patients.
Authors:  Wyen C, Fuhr U, Frank D, Aarnoutse R, Klaassen T, Lazar A, Seeringer A, Doroshyenko O, Kirchheiner J, Abdulrazik F, Schmeisser N, Lehmann C, Hein W, Schömig E, Burger D, Fätkenheuer G, Jetter A
Journal: Clin Pharmacol Ther

PubmedHigh-frequency rhythmic cortical myoclonus in a long-surviving patient with nonketotic hypergylcemia.
Authors:  Mastrangelo M, Canafoglia L, Franceschetti S, Oppezzo C, Mosca F, Menni F, Parini R, Ciano C, Scaioli V, Panzica F
Journal: J Child Neurol

PubmedEffect of sampling procedures of release testing on drug release and scale-up production feasibility of multiple-unit dextromethorphan resinate tablets: a technical note.
Authors:  Pongjanyakul T
Journal: AAPS PharmSciTech

PubmedNeonatal nonketotic hyperglycinemia.
Authors:  Bhamkar RP, Colaco P
Journal: Indian J Pediatr

PubmedDevelopment of sustained release fast-disintegrating tablets using various polymer-coated ion-exchange resin complexes.
Authors:  Jeong SH, Park K
Journal: Int J Pharm

Pubmed[Effect of Qingkailing injection on rat CYP1A2 and CYP2D6 activity]
Authors:  Liu Y, Wang J, Bao YY, Yu WJ, Zhu DL
Journal: Zhongguo Zhong Yao Za Zhi

PubmedAn evaluation of the genotoxicity of the antitussive drug Dextromethorphan.
Authors:  Aardema MJ, Robison SH, Gatehouse D, Johnston G
Journal: Regul Toxicol Pharmacol

PubmedPremedication with low-dose dextromethorphan does not reduce pain following oral surgery.
Authors:  Gordon SM
Journal: J Evid Based Dent Pract

PubmedDevelopment and validation of a chemical hydrolysis method for dextromethorphan and dextrophan determination in urine samples: application to the assessment of CYP2D6 activity in fibromyalgia patients.
Authors:  Daali Y, Cherkaoui S, Doffey-Lazeyras F, Dayer P, Desmeules JA
Journal: J Chromatogr B Analyt Technol Biomed Life Sci

PubmedBlockade of NMDA receptors prevents analgesic tolerance to repeated transcutaneous electrical nerve stimulation (TENS) in rats.
Authors:  Hingne PM, Sluka KA
Journal: J Pain

PubmedEffect of honey, dextromethorphan, and no treatment on nocturnal cough and sleep quality for coughing children and their parents.
Authors:  Paul IM, Beiler J, McMonagle A, Shaffer ML, Duda L, Berlin CM
Journal: Arch Pediatr Adolesc Med

PubmedCYP2D6-Mediated metabolism of a novel acyl coenzyme A:cholesterol acyltransferase inhibitor, pactimibe, and its unique plasma metabolite, R-125528.
Authors:  Kotsuma M, Tokui T, Ishizuka-Ozeki T, Honda T, Iwabuchi H, Murai T, Ikeda T, Saji H
Journal: Drug Metab Dispos

PubmedCytochrome P450 expression and regulation in CYP3A4/CYP2D6 double transgenic humanized mice.
Authors:  Felmlee MA, Lon HK, Gonzalez FJ, Yu AM
Journal: Drug Metab Dispos

PubmedDevelopment of CYP2D6 and CYP3A4 in the first year of life.
Authors:  Johnson TN, Tucker GT, Rostami-Hodjegan A
Journal: Clin Pharmacol Ther

PubmedInsights into drug metabolism by cytochromes P450 from modelling studies of CYP2D6-drug interactions.
Authors:  Maréchal JD, Kemp CA, Roberts GC, Paine MJ, Wolf CR, Sutcliffe MJ
Journal: Br J Pharmacol

PubmedSerotonin syndrome in dextromethorphan ingestion responsive to propofol therapy.
Authors:  Ganetsky M, Babu KM, Boyer EW
Journal: Pediatr Emerg Care

PubmedThe CYP2D6 activity score: translating genotype information into a qualitative measure of phenotype.
Authors:  Gaedigk A, Simon SD, Pearce RE, Bradford LD, Kennedy MJ, Leeder JS
Journal: Clin Pharmacol Ther

Pubmed[Dangerous party drugs: A2 and cough medicines. Increasing interest among Swedish adolescents]
Authors:  Knudsen K, Hultén P, Sass M, Sallin K
Journal: Lakartidningen

PubmedThe inhibitory effect of tannic acid on cytochrome P450 enzymes and NADPH-CYP reductase in rat and human liver microsomes.
Authors:  Yao HT, Chang YW, Lan SJ, Yeh TK
Journal: Food Chem Toxicol

Pubmed[Fibromyalgia syndrome: new developments in pharmacotherapy]
Authors:  Harten P
Journal: Z Rheumatol

PubmedEffect of methamphetamine on cytochrome P450 activity.
Authors:  Dostalek M, Jurica J, Pistovcakova J, Hanesova M, Tomandl J, Linhart I, Sulcova A
Journal: Xenobiotica

PubmedSimultaneous analysis of dextromethorphan and its three metabolites in human plasma using an improved HPLC method with fluorometric detection.
Authors:  Lin SY, Chen CH, Ho HO, Chen HH, Sheu MT
Journal: J Chromatogr B Analyt Technol Biomed Life Sci

PubmedThe effect of dextromethorphan in preventing cholecalciferol-induced poison shyness and sickness-induced anorexia in the laboratory Norway rat.
Authors:  Gould EM, Holmes SJ
Journal: Pest Manag Sci

PubmedThe in vitro inhibitory potential of trade herbal products on human CYP2D6-mediated metabolism and the influence of ethanol.
Authors:  Hellum BH, Nilsen OG
Journal: Basic Clin Pharmacol Toxicol

PubmedCurrently available cough suppressants for chronic cough.
Authors:  Chung KF
Journal: Lung

PubmedActive-site structure, binding and redox activity of the heme-thiolate enzyme CYP2D6 immobilized on coated Ag electrodes: a surface-enhanced resonance Raman scattering study.
Authors:  Bonifacio A, Millo D, Keizers PH, Boegschoten R, Commandeur JN, Vermeulen NP, Gooijer C, van der Zwan G
Journal: J Biol Inorg Chem

PubmedAre false-positive phencyclidine immunoassay instant-view multi-test results caused by overdose concentrations of Ibuprofen, metamizol, and dextromethorphan?
Authors:  Marchei E, Pellegrini M, Pichini S, Martín I, García-Algar O, Vall O
Journal: Ther Drug Monit

PubmedEffects of dextromethorphan on dopamine dependent behaviours in rats.
Authors:  Gaikwad RV, Gaonkar RK, Jadhav SA, Thorat VM, Jadhav JH, Balsara JJ
Journal: Indian J Exp Biol

PubmedDextromethorphan poisoning: an evidence-based consensus guideline for out-of-hospital management.
Authors:  Chyka PA, Erdman AR, Manoguerra AS, Christianson G, Booze LL, Nelson LS, Woolf AD, Cobaugh DJ, Caravati EM, Scharman EJ, Troutman WG,  
Journal: Clin Toxicol (Phila)

PubmedDextromethorphan as a potential neuroprotective agent with unique mechanisms of action.
Authors:  Werling LL, Lauterbach EC, Calef U
Journal: Neurologist

PubmedUse of isolated hepatocyte preparations for cytochrome P450 inhibition studies: comparison with microsomes for Ki determination.
Authors:  Brown HS, Chadwick A, Houston JB
Journal: Drug Metab Dispos

PubmedDextromethorphan-induced near-fatal suicide attempt in a slow metabolizer at cytochrome P450 2D6.
Authors:  Matin N, Kurani A, Kennedy CA, Liu QY
Journal: Am J Geriatr Pharmacother

PubmedTreatment of pathologic laughing and crying.
Authors:  Wortzel HS, Anderson CA, Arciniegas DB
Journal: Curr Treat Options Neurol

Pubmed[Simultaneous determination of the inhibitory potency of compounds on the activity of five cytochrome P-450 enzymes using a cocktail probe substrates method]
Authors:  Gao ZW, Shi XJ, Yu C, Li SJ, Zhong MK
Journal: Yao Xue Xue Bao

PubmedEffects of paracetamol combined with dextromethorphan in human experimental muscle and skin pain.
Authors:  Olesen AE, Staahl C, Ali Z, Drewes AM, Arendt-Nielsen L
Journal: Basic Clin Pharmacol Toxicol

PubmedA comparison of the binding profiles of dextromethorphan, memantine, fluoxetine and amitriptyline: treatment of involuntary emotional expression disorder.
Authors:  Werling LL, Keller A, Frank JG, Nuwayhid SJ
Journal: Exp Neurol

PubmedBone biology and physiology: implications for novel osteoblastic osteosarcoma treatments?
Authors:  Spangler JG
Journal: Med Hypotheses

PubmedEfficacy of pre- and postoperative oral dextromethorphan for reduction of intra- and 24-hour postoperative morphine consumption for transabdominal hysterectomy.
Authors:  Chau-In W, Sukmuan B, Ngamsangsirisapt K, Jirarareungsak W
Journal: Pain Med

PubmedEffect of cinacalcet hydrochloride, a new calcimimetic agent, on the pharmacokinetics of dextromethorphan: in vitro and clinical studies.
Authors:  Nakashima D, Takama H, Ogasawara Y, Kawakami T, Nishitoba T, Hoshi S, Uchida E, Tanaka H
Journal: J Clin Pharmacol

PubmedEffect of sodium ozagrel on the activity of rat CYP2D6.
Authors:  Wu H, Yu W, Huang L, Wang J, Tang X, Yang W, Liu Y, Yu H, Zhu D
Journal: Eur J Pharmacol

PubmedThe spinal anaesthetic effect of dextromethorphan, dextrorphan, and 3-methoxymorphinan.
Authors:  Chen YW, Chen YC, Lin CN, Chu CC, Lin MT, Wang JJ, Kao CH
Journal: Eur J Pharmacol

PubmedFDA halts sales of some anti-vomiting suppositories...and are cough medications effective in children?
Authors:
Journal: Child Health Alert

PubmedMucolytics, expectorants, and mucokinetic medications.
Authors:  Rubin BK
Journal: Respir Care

PubmedInactivation of CYP2D6 by methylenedioxymethamphetamine in different recombinant expression systems.
Authors:  Van LM, Hargreaves JA, Lennard MS, Tucker GT, Rostami-Hodjegan A
Journal: Eur J Pharm Sci

PubmedOral administration of dextromethorphan does not produce neuronal vacuolation in the rat brain.
Authors:  Carliss RD, Radovsky A, Chengelis CP, O'Neill TP, Shuey DL
Journal: Neurotoxicology

PubmedBiotechnological synthesis of drug metabolites using human cytochrome P450 2D6 heterologously expressed in fission yeast exemplified for the designer drug metabolite 4'-hydroxymethyl-alpha-pyrrolidinobutyrophenone.
Authors:  Peters FT, Dragan CA, Wilde DR, Meyer MR, Zapp J, Bureik M, Maurer HH
Journal: Biochem Pharmacol

PubmedNeuroprotective evaluation of standardized extract of Centella asciatica in monosodium glutamate treated rats.
Authors:  Ramanathan M, Sivakumar S, Anandvijayakumar PR, Saravanababu C, Pandian PR
Journal: Indian J Exp Biol

PubmedIn vitro interaction cocktail assay for nine major cytochrome P450 enzymes with 13 probe reactions and a single LC/MSMS run: analytical validation and testing with monoclonal anti-CYP antibodies.
Authors:  Tolonen A, Petsalo A, Turpeinen M, Uusitalo J, Pelkonen O
Journal: J Mass Spectrom

PubmedDextromethorphan in Wisconsin drivers.
Authors:  Cochems A, Harding P, Liddicoat L
Journal: J Anal Toxicol

PubmedIn vitro assessment of cytochrome P450 inhibition: strategies for increasing LC/MS-based assay throughput using a one-point IC(50) method and multiplexing high-performance liquid chromatography.
Authors:  Lin T, Pan K, Mordenti J, Pan L
Journal: J Pharm Sci

PubmedElectron density analyses of opioids: a comparative study.
Authors:  Scheins S, Messerschmidt M, Morgenroth W, Paulmann C, Luger P
Journal: J Phys Chem A

PubmedMethamphetamine exposure antagonizes N-methyl-D-aspartate receptor-mediated neurotoxicity in organotypic hippocampal slice cultures.
Authors:  Smith KJ, Self RL, Butler TR, Mullins MM, Ghayoumi L, Holley RC, Littleton JM, Prendergast MA
Journal: Brain Res

PubmedEffect of gender and age on the pharmacokinetics of repinotan.
Authors:  Heinig R, Sundaresan P, Shah A, Boettcher M
Journal: Clin Drug Investig

PubmedOTC product: Theraflu Thin Strips.
Authors:  Franks AS
Journal: J Am Pharm Assoc (2003)

PubmedOTC product: Zicam Cold and Flu Medicated Spoons.
Authors:  Olenak JL
Journal: J Am Pharm Assoc (2003)

PubmedOTC product: PediaCare Long-Acting Cough Freezer Pops.
Authors:  Marciniak MW
Journal: J Am Pharm Assoc (2003)

Pubmed"Pharming": the abuse of prescription and over-the-counter drugs in teens.
Authors:  Levine DA
Journal: Curr Opin Pediatr

Pubmed"Crystal dex:" free-base dextromethorphan.
Authors:  Hendrickson RG, Cloutier RL
Journal: J Emerg Med

PubmedThe metabolism of midazolam and comparison with other CYP enzyme substrates during intestinal absorption: in vitro studies with rat everted gut sacs.
Authors:  Arellano C, Philibert C, Vachoux C, Woodley J, Houin G
Journal: J Pharm Pharm Sci

PubmedCough mixture abuse as a novel cause of folate deficiency: a prospective, community-based, controlled study.
Authors:  Au WY, Tsang SK, Cheung BK, Siu TS, Ma ES, Tam S
Journal: Haematologica

PubmedEfficacy of a single evening dose of syrup containing paracetamol, dextromethorphan hydrobromide, doxylamine succinate and ephedrine sulfate in subjects with multiple common cold symptoms.
Authors:  Mizoguchi H, Wilson A, Jerdack GR, Hull JD, Goodale M, Grender JM, Tyler BA
Journal: Int J Clin Pharmacol Ther

PubmedSaturable uptake of lipophilic amine drugs into isolated hepatocytes: mechanisms and consequences for quantitative clearance prediction.
Authors:  Hallifax D, Houston JB
Journal: Drug Metab Dispos

PubmedComparative metabolic capabilities and inhibitory profiles of CYP2D6.1, CYP2D6.10, and CYP2D6.17.
Authors:  Shen H, He MM, Liu H, Wrighton SA, Wang L, Guo B, Li C
Journal: Drug Metab Dispos

PubmedNovel approach to performing metabolite identification in drug metabolism.
Authors:  Nassar AE, Lee DY
Journal: J Chromatogr Sci

PubmedDextromethorphan: a review of N-methyl-d-aspartate receptor antagonist in the management of pain.
Authors:  Siu A, Drachtman R
Journal: CNS Drug Rev

PubmedActivity of human P450 2D6 in biphasic solvent systems.
Authors:  Zhao J, Tan E, Ferras J, Auclair K
Journal: Biotechnol Bioeng

PubmedDextromethorphan or dextrorphan have a local anesthetic effect on infiltrative cutaneous analgesia in rats.
Authors:  Chen YW, Chu KS, Lin CN, Tzeng JI, Chu CC, Lin MT, Wang JJ
Journal: Anesth Analg

PubmedSimultaneous analysis of cytochrome P450 probes-dextromethorphan, flurbiprofen and midazolam and their major metabolites by HPLC-mass-spectrometry/fluorescence after single-step extraction from plasma.
Authors:  Kumar A, Mann HJ, Remmel RP
Journal: J Chromatogr B Analyt Technol Biomed Life Sci

PubmedSeparation of cold medicine ingredients using a precise MEKC method at elevated pH.
Authors:  Hasemann P, ter Balk M, Preu L, Wätzig H
Journal: Electrophoresis

PubmedIn vitro LC-MS cocktail assays to simultaneously determine human cytochrome P450 activities.
Authors:  Dixit V, Hariparsad N, Desai P, Unadkat JD
Journal: Biopharm Drug Dispos

PubmedTherapeutic use of dextromethorphan: key learnings from treatment of pseudobulbar affect.
Authors:  Miller A, Panitch H
Journal: J Neurol Sci

PubmedTimolol metabolism in human liver microsomes is mediated principally by CYP2D6.
Authors:  Volotinen M, Turpeinen M, Tolonen A, Uusitalo J, Mäenpää J, Pelkonen O
Journal: Drug Metab Dispos

PubmedInvoluntary emotional expression disorder: treating the untreated.
Authors:  Brooks BR
Journal: CNS Spectr

PubmedDevelopment and full validation of six inhibition assays for five major cytochrome P450 enzymes in human liver microsomes using an automated 96-well microplate incubation format and LC-MS/MS analysis.
Authors:  Yao M, Zhu M, Sinz MW, Zhang H, Humphreys WG, Rodrigues AD, Dai R
Journal: J Pharm Biomed Anal

PubmedThe neuropsychiatry of multiple sclerosis: a review of recent developments.
Authors:  Ghaffar O, Feinstein A
Journal: Curr Opin Psychiatry

PubmedMicrobial transformation of dextromethorphan by Cunninghamella blakesleeana AS 3.153.
Authors:  Lin L, Huang H, Zhang P, Qi X, Zhong D
Journal: Chem Pharm Bull (Tokyo)





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