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[PMID]:26408883
[Au] Autor:Sadeghi M; Farhoudian A; Vishteh HR; Rahimzadeh S; Fekri M; Movaghar AR; Sefatian S
[Ad] Endereço:IRSA Center for Psychology and Addiction Sciences, Tehran, Iran.
[Ti] Título:A tentative component analysis of Norjizak: A new abused drug in Iran.
[So] Source:Pak J Pharm Sci;28(5):1631-6, 2015 Sep.
[Is] ISSN:1011-601X
[Cp] País de publicação:Pakistan
[La] Idioma:eng
[Ab] Resumo:Norjizak is a new drug abused in the past few years in Iran with symptoms and complications distinct from other common forms of drug and characterized by higher rate of mortality. The present study aims to analyze the chemical components of this substance. Five samples were obtained from abusers referring from different areas of Tehran to a treatment clinic. All samples were 2 ml vials with yellowish fluid. Thin Layer Chromatography (TLC) was performed first to analyze the samples semi-quantitatively and the quantitative levels of components were then explored using high-performance liquid chromatography (HPLC). TLC revealed steroid (in form of betamethasone), heroin, codeine, morphine and thebaine in all five samples. Four samples contained acetaminophen and two samples contained caffeine. None of them contained amphetamine, benzodiazepine, tricyclic antidepressant, aspirin, barbiturates, tramadol and buprenorphine. HPLC revealed that heroin, codeine, morphine and thebaine constituted the narcotic foundation in all samples. In addition, the heroin to acetylcodeine ratio was significantly lower in three samples, which indicates their higher toxicity. The results of the present study on the chemical components of Norjizak showed that this substance is an opiate one similar to heroin and the heroin-based crack prevalent in Iran which contains betamethasone.
[Mh] Termos MeSH primário: Aspirina/análise
Cafeína/análise
Orfenadrina/análise
[Mh] Termos MeSH secundário: Betametasona/análise
Cromatografia Líquida de Alta Pressão
Cromatografia em Camada Delgada
Codeína/análise
Combinação de Medicamentos
Heroína/análise
Irã (Geográfico)
Transtornos Relacionados ao Uso de Substâncias
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Drug Combinations); 3G6A5W338E (Caffeine); 70D95007SX (Heroin); 88566-80-7 (Norgesic forte); 9842X06Q6M (Betamethasone); AL805O9OG9 (Orphenadrine); Q830PW7520 (Codeine); R16CO5Y76E (Aspirin)
[Em] Mês de entrada:1512
[Cu] Atualização por classe:150927
[Lr] Data última revisão:
150927
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150927
[St] Status:MEDLINE


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[PMID]:25437841
[Au] Autor:Yehia AM; Abd El-Rahman MK
[Ad] Endereço:Analytical Chemistry Department, Faculty of Pharmacy, Cairo University, El-Kasr El-Aini Street, 11562 Cairo, Egypt. Electronic address: aliyehia00@yahoo.com.
[Ti] Título:Application of normalized spectra in resolving a challenging Orphenadrine and Paracetamol binary mixture.
[So] Source:Spectrochim Acta A Mol Biomol Spectrosc;138:21-30, 2015 Mar 05.
[Is] ISSN:1873-3557
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Normalized spectra have a great power in resolving spectral overlap of challenging Orphenadrine (ORP) and Paracetamol (PAR) binary mixture, four smart techniques utilizing the normalized spectra were used in this work, namely, amplitude modulation (AM), simultaneous area ratio subtraction (SARS), simultaneous derivative spectrophotometry (S(1)DD) and ratio H-point standard addition method (RHPSAM). In AM, peak amplitude at 221.6nm of the division spectra was measured for both ORP and PAR determination, while in SARS, concentration of ORP was determined using the area under the curve from 215nm to 222nm of the regenerated ORP zero order absorption spectra, in S(1)DD, concentration of ORP was determined using the peak amplitude at 224nm of the first derivative ratio spectra. PAR concentration was determined directly at 288nm in the division spectra obtained during the manipulation steps in the previous three methods. The last RHPSAM is a dual wavelength method in which two calibrations were plotted at 216nm and 226nm. RH point is the intersection of the two calibration lines, where ORP and PAR concentrations were directly determined from coordinates of RH point. The proposed methods were applied successfully for the determination of ORP and PAR in their dosage form.
[Mh] Termos MeSH primário: Acetaminofen/análise
Analgésicos não Entorpecentes/análise
Relaxantes Musculares Centrais/análise
Orfenadrina/análise
Espectrofotometria/métodos
[Mh] Termos MeSH secundário: Combinação de Medicamentos
Modelos Lineares
Reprodutibilidade dos Testes
[Pt] Tipo de publicação:EVALUATION STUDIES; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Analgesics, Non-Narcotic); 0 (Drug Combinations); 0 (Muscle Relaxants, Central); 362O9ITL9D (Acetaminophen); AL805O9OG9 (Orphenadrine)
[Em] Mês de entrada:1512
[Cu] Atualização por classe:150113
[Lr] Data última revisão:
150113
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:141202
[St] Status:MEDLINE


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[PMID]:25324526
[Au] Autor:Knittel JL; Vorce SP; Levine B; Hughes RL; Bosy TZ
[Ad] Endereço:Division of Forensic Toxicology, Armed Forces Medical Examiner System, Dover AFB, Dover, DE 19902, USA jessica.l.knittel.ctr@mail.mil.
[Ti] Título:Multidrug toxicity involving sumatriptan.
[So] Source:J Anal Toxicol;39(1):75-9, 2015 Jan-Feb.
[Is] ISSN:1945-2403
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:A multidrug fatality involving sumatriptan is reported. Sumatriptan is a tryptamine derivative that acts at 5-HT(1B/1D) receptors and is used for the treatment of migraines. The decedent was a 21-year-old white female found dead in bed by her spouse. No signs of physical trauma were observed and a large number of prescription medications were discovered at the scene. Toxicological analysis of the central blood revealed sumatriptan at a concentration of 1.03 mg/L. Following therapeutic dosing guidelines, sumatriptan concentrations do not exceed 0.095 mg/L. Sumatriptan was isolated by solid-phase extraction and analyzed using liquid chromatography-tandem mass spectrometry in multiple reaction monitoring mode. A tissue distribution study was completed with the following concentrations measured: 0.61 mg/L in femoral blood, 0.56 mg/L in iliac blood, 5.01 mg/L in urine, 0.51 mg/kg in liver, 3.66 mg/kg in kidney, 0.09 mg/kg in heart, 0.32 mg/kg in spleen, 0.01 mg/kg in brain, 15.99 mg/kg in lung and 78.54 mg/45 mL in the stomach contents. Carisoprodol, meprobamate, fluoxetine, doxylamine, orphenadrine, dextromethorphan and hydroxyzine were also present in the blood at the following concentrations: 3.35, 2.36, 0.63, 0.19, 0.06, 0.55 and 0.16 mg/L. The medical examiner ruled the cause of death as acute mixed drug toxicity and the manner of death as accident.
[Mh] Termos MeSH primário: Efeitos Colaterais e Reações Adversas Relacionados a Medicamentos/sangue
Sumatriptana/envenenamento
[Mh] Termos MeSH secundário: Autopsia
Carisoprodol/sangue
Cromatografia Líquida
Dextrometorfano/sangue
Doxilamina/sangue
Estudos de Avaliação como Assunto
Evolução Fatal
Feminino
Fluoxetina/sangue
Toxicologia Forense
Seres Humanos
Hidroxizina/sangue
Fígado/efeitos dos fármacos
Fígado/metabolismo
Meprobamato/sangue
Orfenadrina/sangue
Reprodutibilidade dos Testes
Manejo de Espécimes
Sumatriptana/farmacocinética
Espectrometria de Massas em Tandem
Distribuição Tecidual
Adulto Jovem
[Pt] Tipo de publicação:CASE REPORTS; JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
01K63SUP8D (Fluoxetine); 21925K482H (Carisoprodol); 30S50YM8OG (Hydroxyzine); 7355X3ROTS (Dextromethorphan); 8R78F6L9VO (Sumatriptan); 95QB77JKPL (Doxylamine); 9I7LNY769Q (Meprobamate); AL805O9OG9 (Orphenadrine)
[Em] Mês de entrada:1510
[Cu] Atualização por classe:150113
[Lr] Data última revisão:
150113
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:141018
[St] Status:MEDLINE
[do] DOI:10.1093/jat/bku120


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[PMID]:25205132
[Au] Autor:Chen YW; Tzeng JI; Chen YC; Hung CH; Wang JJ
[Ad] Endereço:Department of Physical Therapy, China Medical University, Taichung, Taiwan; Department of Medical Research, Chi-Mei Medical Center, Tainan City, Taiwan.
[Ti] Título:Intrathecal orphenadrine elicits spinal block in the rat.
[So] Source:Eur J Pharmacol;742:125-30, 2014 Nov 05.
[Is] ISSN:1879-0712
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:The purpose of this study was to estimate the local anesthetic effect of orphenadrine, an anti-muscarinic agent, in spinal anesthesia and its comparison with the local anesthetic lidocaine. After the rat was injected intrathecally, the spinal block of orphenadrine and lidocaine was constructed in a dosage-dependent fashion. The potency and duration of spinal anesthesia with orphenadrine were compared with that of lidocaine. Our data demonstrated that orphenadrine and lidocaine elicited dose-dependent spinal blockades on the motor function, sensory, and proprioception. On the 50% effective dose (ED50) basis, the ranks of potency in motor function, nociception, and proprioception were orphenadrine>lidocaine (P<0.01). At equipotent doses (ED25, ED50, ED75), the block duration elicited by orphenadrine was greater than that elicited by lidocaine (P<0.01). Orphenadrine, but not lidocaine, exhibited longer duration of nociceptive/sensory blockade than that of motor blockade at equipotent doses. Ineffective-dose orphenadrine as adjuvant did not enhance spinal anesthesia with lidocaine. The preclinical data revealed that orphenadrine with a more sensory-selective action over motor block exhibited more potent and longer spinal anesthesia when compared to lidocaine.
[Mh] Termos MeSH primário: Raquianestesia/métodos
Anestésicos Locais/administração & dosagem
Orfenadrina/administração & dosagem
[Mh] Termos MeSH secundário: Animais
Relação Dose-Resposta a Droga
Injeções Espinhais
Lidocaína/administração & dosagem
Masculino
Antagonistas Muscarínicos/administração & dosagem
Nociceptividade/efeitos dos fármacos
Propriocepção/efeitos dos fármacos
Desempenho Psicomotor/efeitos dos fármacos
Ratos
Ratos Sprague-Dawley
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anesthetics, Local); 0 (Muscarinic Antagonists); 98PI200987 (Lidocaine); AL805O9OG9 (Orphenadrine)
[Em] Mês de entrada:1508
[Cu] Atualização por classe:141206
[Lr] Data última revisão:
141206
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:140911
[St] Status:MEDLINE


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[PMID]:25033559
[Au] Autor:Hubs'kyi IuI; Bukhtiarova TA; Horiushko HH; Litvinova NV; Paramonova HI; Kurapova TM; Velychko OM; Babenko LP
[Ti] Título:[Biophysical parameters of erythrocyte membranes and mechanisms of interaction with non-opioid analgesics under acute pain syndrome].
[So] Source:Ukr Biochem J;86(3):98-106, 2014 May-Jun.
[Is] ISSN:2409-4943
[Cp] País de publicação:Ukraine
[La] Idioma:ukr
[Ab] Resumo:Methods of fluorescent probing, spectrophotometry and microcalorimetry were applied to investigate the alterations in biophysical parameters of erythrocytes membranes, and specifically microviscosity, surface charge, molecular organization of lipid bilayer and lipid-protein interactions under conditions of acute pain syndrome produced by experimental chemical lesion. The distinctive features of non-opiod analgesics interactions and binding to the erythrocytes membranes of rats subjected to acute nociceptive pain accompanied with oxidative stress development were investigated. The abilities of analgesics under research, and namely paracetamol, aspirin, phenazone, ketorolac, pyrodazole, ketoprofenum, natrium mefenaminate, indometacin, nimesulide to make up physico-chemical complexes with lipoperoxidation modified erythrocytes surface and protein-lipid bilayer showed marked changes. The significance of oxidative damage of biophase under conditions of acute pain syndrome for analgesics effective pharmacodynamics and pharmacokinetics realization is under consideration.
[Mh] Termos MeSH primário: Dor Aguda/prevenção & controle
Analgésicos não Entorpecentes/metabolismo
Membrana Eritrocítica/metabolismo
Bicamadas Lipídicas/metabolismo
[Mh] Termos MeSH secundário: Acetaminofen/metabolismo
Acetaminofen/farmacologia
Analgésicos não Entorpecentes/farmacologia
Animais
Antipirina/metabolismo
Antipirina/farmacologia
Aspirina/metabolismo
Aspirina/farmacologia
Calorimetria
Fracionamento Celular
Membrana Eritrocítica/química
Corantes Fluorescentes
Indometacina/metabolismo
Indometacina/farmacologia
Cetoprofeno/metabolismo
Cetoprofeno/farmacologia
Cetorolaco/metabolismo
Cetorolaco/farmacologia
Bicamadas Lipídicas/química
Peroxidação de Lipídeos/efeitos dos fármacos
Masculino
Orfenadrina/metabolismo
Orfenadrina/farmacologia
Medição da Dor
Ratos
Espectrometria de Fluorescência
Sulfonamidas/metabolismo
Sulfonamidas/farmacologia
[Pt] Tipo de publicação:ENGLISH ABSTRACT; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Analgesics, Non-Narcotic); 0 (Fluorescent Dyes); 0 (Lipid Bilayers); 0 (Sulfonamides); 362O9ITL9D (Acetaminophen); 90Y4QC304K (Ketoprofen); AL805O9OG9 (Orphenadrine); R16CO5Y76E (Aspirin); T3CHA1B51H (Antipyrine); V4TKW1454M (nimesulide); XXE1CET956 (Indomethacin); YZI5105V0L (Ketorolac)
[Em] Mês de entrada:1408
[Cu] Atualização por classe:151119
[Lr] Data última revisão:
151119
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:140719
[St] Status:MEDLINE


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[PMID]:24905515
[Au] Autor:Rejdak K; Nieoczym D; Czuczwar M; Kis J; Wlaz P; Turski WA
[Ad] Endereço:Department of Neurology, Medical University of Lublin, Lublin, Poland. Electronic address: krejdak@europe.com.
[Ti] Título:Orphenadrine-induced convulsive status epilepticus in rats responds to the NMDA antagonist dizocilpine.
[So] Source:Pharmacol Rep;66(3):399-403, 2014 Jun.
[Is] ISSN:1734-1140
[Cp] País de publicação:Poland
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Identification of new molecular targets as well as the new models recapitulating different aspects of pathophysiology of status epilepticus (SE) in humans might prove essential for the breakthrough in the efforts against pharmacoresistance in epilepsy. Recently, we described a new model of generalized convulsive SE induced with orphenadrine (ORPH) in rats with unique characteristics [5]. The current study was aimed at assessing the efficacy of a new generation antiepileptic drugs (AEDs) and some of the experimental agents in suppressing ORPH-evoked seizures in rats. METHODS: ORPH was administered intraperitoneally (ip) in the dose of 80 mg/kg in male Wistar rats. The latency to first seizure, the number of seizure episodes and the duration of overt SE, as well as the incidence of deaths was scored with simultaneous electroencephalographic (EEG) recordings. RESULTS: ORPH induced seizures in 100% of animals at a dose of 80 mg/kg, associated with low mortality and good behavioural outcome. Among new generation AEDs: felbamate, levetiracetam, topiramate, lamotrigine and progabide did not affect the seizure incidence. Among the experimental drugs, only dizocilpine, the non-competitive NMDA antagonist, dose-dependently affected the occurrence of the SE (p<0.001). However, CGP-39551 competitive NMDA antagonist, the same as scopolamine and mecamylamine (muscarinic and nicotinic receptors antagonists, respectively) showed no effect. CONCLUSIONS: Based on the above findings, one may speculate that NMDA activation is partly involved in the proconvulsant activity of orphenadrine but may not be the primary pathomechanism. ORPH-induced seizures may provide an interesting option for studying novel targets for pharmacological interventions in status epilepticus.
[Mh] Termos MeSH primário: Maleato de Dizocilpina/farmacologia
N-Metilaspartato/antagonistas & inibidores
Orfenadrina/farmacologia
Estado Epiléptico/induzido quimicamente
Estado Epiléptico/tratamento farmacológico
[Mh] Termos MeSH secundário: 2-Amino-5-fosfonovalerato/análogos & derivados
Animais
Anticonvulsivantes/farmacologia
Eletroencefalografia/métodos
Hipocampo/efeitos dos fármacos
Hipocampo/metabolismo
Masculino
N-Metilaspartato/metabolismo
Ratos
Ratos Wistar
Convulsões/tratamento farmacológico
Convulsões/metabolismo
Estado Epiléptico/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anticonvulsants); 127910-32-1 (CGP 39551); 6384-92-5 (N-Methylaspartate); 6LR8C1B66Q (Dizocilpine Maleate); 76726-92-6 (2-Amino-5-phosphonovalerate); AL805O9OG9 (Orphenadrine)
[Em] Mês de entrada:1502
[Cu] Atualização por classe:140609
[Lr] Data última revisão:
140609
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:140607
[St] Status:MEDLINE


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[PMID]:24613829
[Au] Autor:Desaphy JF; Carbonara R; Costanza T; Conte Camerino D
[Ad] Endereço:Section of Pharmacology, Department of Pharmacy & Drug Sciences, University of Bari-Aldo Moro, Bari I-70125, Italy. Electronic address: jeanfrancois.desaphy@uniba.it.
[Ti] Título:Preclinical evaluation of marketed sodium channel blockers in a rat model of myotonia discloses promising antimyotonic drugs.
[So] Source:Exp Neurol;255:96-102, 2014 May.
[Is] ISSN:1090-2430
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Although the sodium channel blocker mexiletine is considered the first-line drug in myotonia, some patients experiment adverse effects, while others do not gain any benefit. Other antimyotonic drugs are thus needed to offer mexiletine alternatives. In the present study, we used a previously-validated rat model of myotonia congenita to compare six marketed sodium channel blockers to mexiletine. Myotonia was induced in the rat by injection of anthracen-9-carboxylic acid, a muscle chloride channel blocker. The drugs were given orally and myotonia was evaluated by measuring the time of righting reflex. The drugs were also tested on sodium currents recorded in a cell line transfected with the human skeletal muscle sodium channel hNav1.4 using patch-clamp technique. In vivo, carbamazepine and propafenone showed antimyotonic activity at doses similar to mexiletine (ED50 close to 5mg/kg); flecainide and orphenadrine showed greater potency (ED50 near 1mg/kg); lubeluzole and riluzole were the more potent (ED50 near 0.1mg/kg). The antimyotonic activity of drugs in vivo was linearly correlated with their potency in blocking hNav1.4 channels in vitro. Deviation was observed for propafenone and carbamazepine, likely due to pharmacokinetics and multiple targets. The comparison of the antimyotonic dose calculated in rats with the current clinical dose in humans strongly suggests that all the tested drugs may be used safely for the treatment of human myotonia. Considering the limits of mexiletine tolerability and the occurrence of non-responders, this study proposes an arsenal of alternative drugs, which may prove useful to increase the quality of life of individuals suffering from non-dystrophic myotonia. Further clinical trials are warranted to confirm these results.
[Mh] Termos MeSH primário: Mexiletina/uso terapêutico
Músculo Esquelético/efeitos dos fármacos
Miotonia Congênita/tratamento farmacológico
Bloqueadores dos Canais de Sódio/uso terapêutico
[Mh] Termos MeSH secundário: Animais
Carbamazepina/farmacologia
Carbamazepina/uso terapêutico
Modelos Animais de Doenças
Flecainida/farmacologia
Flecainida/uso terapêutico
Células HEK293
Seres Humanos
Mexiletina/farmacologia
Orfenadrina/farmacologia
Orfenadrina/uso terapêutico
Piperidinas/farmacologia
Piperidinas/uso terapêutico
Propafenona/farmacologia
Propafenona/uso terapêutico
Ratos
Ratos Wistar
Riluzol/farmacologia
Riluzol/uso terapêutico
Bloqueadores dos Canais de Sódio/farmacologia
Tiazóis/farmacologia
Tiazóis/uso terapêutico
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Piperidines); 0 (Sodium Channel Blockers); 0 (Thiazoles); 1U511HHV4Z (Mexiletine); 33CM23913M (Carbamazepine); 68IQX3T69U (Propafenone); 7LJ087RS6F (Riluzole); AL805O9OG9 (Orphenadrine); K94FTS1806 (Flecainide); V2SIB71583 (lubeluzole)
[Em] Mês de entrada:1406
[Cu] Atualização por classe:170922
[Lr] Data última revisão:
170922
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:140312
[St] Status:MEDLINE


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[PMID]:24508877
[Au] Autor:Abdelrahman MM
[Ad] Endereço:Pharmaceutical Analytical Chemistry Department, Faculty of Pharmacy, Beni-Suef University, Alshaheed Shehata Ahmad Hegazy St., 62514 Beni-Suef, Egypt. Electronic address: maha.abdelrahman@pharm.bsu.edu.eg.
[Ti] Título:Selective spectrophotometric methods for determination of ternary mixture with overlapping spectra: a comparative study.
[So] Source:Spectrochim Acta A Mol Biomol Spectrosc;124:389-96, 2014 Apr 24.
[Is] ISSN:1873-3557
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Comparable double divisor ratio spectra derivative, area under curve of derivative ratio and mean centering of ratio spectra spectrophotometric methods were introduced for determination of orphenadrine citrate (ORPH), caffeine (CAF) and aspirin (ASP); a combination for symptomatic relief of mild to moderate pain of acute musculoskeletal disorders; with evident accuracy and precision. The suggested methods have the advantage over the previously published spectrophotometric method for determination of the same combination in that they did not require a preliminary separation step and able to resolve the ternary mixture, with severe overlapping spectra, with competent sensitivity and selectivity. The recommended methods allow the determination of ORPH, CAF and ASP in the range of 2-32, 2-28 and 3-28 µg mL(-1), respectively. The validity of the proposed methods was examined by analysis of different laboratory prepared mixtures of ORPH, CAF and ASP and assay of their tablet formulation where reliable results were obtained. Statistical analysis between the suggested spectrophotometric methods and the reported HPLC method using student's-t and F-ratio tests reveals that the suggested methods are as accurate and precise as the reported one.
[Mh] Termos MeSH primário: Aspirina/análise
Cafeína/análise
Orfenadrina/análise
Espectrofotometria/métodos
[Mh] Termos MeSH secundário: Área Sob a Curva
Química Farmacêutica
Cinética
Metanol/química
Padrões de Referência
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE
[Nm] Nome de substância:
3G6A5W338E (Caffeine); AL805O9OG9 (Orphenadrine); R16CO5Y76E (Aspirin); Y4S76JWI15 (Methanol)
[Em] Mês de entrada:1502
[Cu] Atualização por classe:140317
[Lr] Data última revisão:
140317
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:140211
[St] Status:MEDLINE


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[PMID]:24579304
[Au] Autor:Wang X; Black L
[Ad] Endereço:Absorption Systems LP, Exton, PA, USA.
[Ti] Título:Ex vivo percutaneous absorption of ketamine, bupivacaine, diclofenac, gabapentin, orphenadrine, and pentoxifylline: comparison of versatile cream vs. reference cream.
[So] Source:Int J Pharm Compd;17(6):520-5, 2013 Nov-Dec.
[Is] ISSN:1092-4221
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:This ex vivo human percutaneous absorption study evaluated a set of six model drugs (ketamine hydrochloride, bupivacaine hydrochloride, diclofenac sodium, gabapentin, orphenadrine citrate, pentoxifylline) from two popular formulations for topically applied compounding preparations. The compounded preparations used in this study were Versatile cream and a reference cream. Each formulation was applied to human trunk skin mounted on Franz Diffusion Cells, 50 mg/chamber (or 28.2 mg/cm2). Serial dermal receiver solutions were collected for 48 hours. Analysis of the resultant data supports the concept that the Versatile base formulation provides improved characteristics relative to the reference base. This is of key importance where the patient does not show clinical improvement when a conventional topical delivery vehicle is used in the formulation. From the results, it is reasonable to anticipate that, relative to the reference formulation, the Versatile formulation provides enhanced transdermal delivery of some analgesic medications.
[Mh] Termos MeSH primário: Analgésicos/farmacocinética
Absorção Cutânea
[Mh] Termos MeSH secundário: Administração Cutânea
Aminas/farmacocinética
Analgésicos/administração & dosagem
Bupivacaína/farmacocinética
Química Farmacêutica
Ácidos Cicloexanocarboxílicos/farmacocinética
Diclofenaco/farmacocinética
Seres Humanos
Ketamina/farmacocinética
Pomadas
Orfenadrina/farmacocinética
Pentoxifilina/farmacocinética
Ácido gama-Aminobutírico/farmacocinética
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Amines); 0 (Analgesics); 0 (Cyclohexanecarboxylic Acids); 0 (Ointments); 144O8QL0L1 (Diclofenac); 56-12-2 (gamma-Aminobutyric Acid); 690G0D6V8H (Ketamine); 6CW7F3G59X (gabapentin); AL805O9OG9 (Orphenadrine); SD6QCT3TSU (Pentoxifylline); Y8335394RO (Bupivacaine)
[Em] Mês de entrada:1405
[Cu] Atualização por classe:140303
[Lr] Data última revisão:
140303
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:140304
[St] Status:MEDLINE


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Fotocópia
[PMID]:23665939
[Au] Autor:Morita R; Yafune A; Shiraki A; Itahashi M; Ishii Y; Akane H; Nakane F; Suzuki K; Shibutani M; Mitsumori K
[Ad] Endereço:Laboratory of Veterinary Pathology, Tokyo University of Agriculture and Technology, Japan. rmorita@cc.tuat.ac.jp
[Ti] Título:Liver tumor promoting effect of orphenadrine in rats and its possible mechanism of action including CAR activation and oxidative stress.
[So] Source:J Toxicol Sci;38(3):403-13, 2013.
[Is] ISSN:1880-3989
[Cp] País de publicação:Japan
[La] Idioma:eng
[Ab] Resumo:Orphenadrine (ORPH), an anticholinergic agent, is a cytochrome P450 (CYP) 2B inducer. CYP2B inducers are known to have liver tumor-promoting effects in rats. In this study, we performed a rat two-stage liver carcinogenesis bioassay to examine the tumor-promoting effect of ORPH and to clarify its possible mechanism of action. Male rats were given a single intraperitoneal injection of N-diethylnitrosamine (DEN) as an initiation treatment. Two weeks after DEN administration, rats were fed a diet containing ORPH (0, 750, or 1,500 ppm) for 6 weeks. One week after the ORPH-administration rats were subjected to two-thirds partial hepatectomy for the acceleration of hepatocellular proliferation. The number and area of glutathione S-transferase placental form-positive foci significantly increased in the DEN-ORPH groups. Real-time RT-PCR revealed increased mRNA expression levels of Cyp2b1/2, Mrp2 and Cyclin D1 in the DEN-ORPH groups and of Gpx2 and Gstm3 in the DEN-High ORPH group. Microsomal reactive oxygen species (ROS) production and oxidative stress markers such as thiobarbituric acid-reactive substances and 8-hydroxydeoxyguanosine were increased in the DEN-High ORPH group. Immunohistochemically, constitutively active/androstane receptor (CAR) were clearly localized in the nuclei of hepatocytes in the DEN-ORPH groups. These results suggest that ORPH causes nuclear translocation of CAR resulting in the induction of the liver tumor-promoting activity. Furthermore, oxidative stress resulting from ROS production is also involved in the liver tumor-promoting activity of ORPH.
[Mh] Termos MeSH primário: Antagonistas Colinérgicos/toxicidade
Neoplasias Hepáticas/induzido quimicamente
Antagonistas Muscarínicos/toxicidade
Orfenadrina/toxicidade
Estresse Oxidativo/efeitos dos fármacos
Espécies Reativas de Oxigênio/metabolismo
Receptores Citoplasmáticos e Nucleares/metabolismo
[Mh] Termos MeSH secundário: Animais
Núcleo Celular/metabolismo
Antagonistas Colinérgicos/administração & dosagem
Dietilnitrosamina/administração & dosagem
Dietilnitrosamina/toxicidade
Hepatócitos/citologia
Hepatócitos/metabolismo
Masculino
Antagonistas Muscarínicos/administração & dosagem
Orfenadrina/administração & dosagem
Ratos
Ratos Endogâmicos F344
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Cholinergic Antagonists); 0 (Muscarinic Antagonists); 0 (Reactive Oxygen Species); 0 (Receptors, Cytoplasmic and Nuclear); 0 (constitutive androstane receptor); 3IQ78TTX1A (Diethylnitrosamine); AL805O9OG9 (Orphenadrine)
[Em] Mês de entrada:1310
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:130514
[St] Status:MEDLINE



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