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Avaliação da bioequivalência de comprimidos contendo 10 mg de cloridrato de ciclobenzaprina; Bioequivalence avaliation of tables contain 10 mg of cyclobenzaprine hydrochloride

Brioschi, Tatiane Maria de Lima Souza
Fonte: Biblioteca Digitais de Teses e Dissertações da USP Publicador: Biblioteca Digitais de Teses e Dissertações da USP
Tipo: Dissertação de Mestrado Formato: application/pdf
Publicado em 13/11/2006 PT
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38.33%
A ciclobenzaprina é um relaxante muscular de ação central estruturalmente similar aos antidepressivos tricíclicos. O objetivo deste trabalho foi avaliar a bioequivalência de comprimidos contendo 10 mg de cloridrato de ciclobenzaprina em voluntários sadios. O estudo de bioequivalência entre o produto teste (Miosan®) e referência (Flexeril®) foi do tipo randomizado, aberto e cruzado. Os produtos foram administrados por via oral aos voluntários em dose única de 10 mg de cloridrato de ciclobenzaprina. Amostras de sangue foram coletadas até 240 horas após a administração do fármaco e quantificadas por método previamente validado através de cromatografia líquida de alta eficiência acoplada a um detector de massas. As curvas médias de decaimento plasmático dos produtos teste (Miosan®) e referência (Flexeril®) foram semelhantes ASC0-t (teste: 193,00 ngxh/mL; referência: 191,66 ngxh/mL) e ASC0∞ (teste: 211,34 ngxh/mL; referência: 209,35 ngxh/mL). Assim como os parâmetros farmacocinéticos relativos à absorção de ciclobenzaprina, Cmax (teste: 7,16 ng/mL; referência: 6,95 ng/mL), tmax (teste: 4,61 h; referência: 4,48 h), Ka (referência: 0,79; teste: 0,67) e t(1/2)a (referência: 1,79 h; teste: 2...

Macroestrutura do sono em pacientes com fibromialgia, antes e após tratamento; Sleep macrostructure in patients with fibromyalgia, before and after treatment.

Martori, Alexandre Henrique
Fonte: Biblioteca Digitais de Teses e Dissertações da USP Publicador: Biblioteca Digitais de Teses e Dissertações da USP
Tipo: Dissertação de Mestrado Formato: application/pdf
Publicado em 27/05/2011 PT
Relevância na Pesquisa
16.81%
MARTORI, AH. Macroestrutura do sono em pacientes com fibromialgia, antes e após tratamento. 2011. 59 f. Dissertação (Mestrado) Faculdade de Medicina de Ribeirão Preto, Universidade de São Paulo, Ribeirão Preto, 2011. Os objetivos do presente estudo foram: - avaliar a macroestrutura do sono de pacientes com Fibromialgia sem tratamento medicamentoso; - avaliar se há modificações na macroestrutura do sono, após a instituição de tratamento medicamentoso da síndrome com Amitripitilina ou Fluoxetina + Ciclobenzaprina; - avaliar a queixa de dor, através da Escala Analógica Visual (EVA), e de comprometimento do sono, utilizando escala semelhante adaptada para o sono (Escala de Qualidade do Sono EQS), antes e após o tratamento. Vinte pacientes (19 mulheres e 1 homem) foram selecionados do ambulatório de Reumatologia do HCFMRP-USP, entre aqueles com diagnóstico clínico definido de fibromialgia, sem tratamento medicamentoso atual para a síndrome. Os pacientes preencheram a EVA e a EQS, antes e após a introdução do medicamento de escolha, ao mesmo tempo em que foram submetidos a polissonografia (PSG), antes e após tratamento. As alterações da macroestrutura do sono na primeira PSG foram aumento de N1, redução de N3 e aumento do número de microdespertares...

Eficácia da melatonina no tratamento da dor miofascial crônica facial : ensaio clínico randomizado, duplo-cego, controlado com placebo

Vidor, Liliane Pinto
Fonte: Universidade Federal do Rio Grande do Sul Publicador: Universidade Federal do Rio Grande do Sul
Tipo: Dissertação Formato: application/pdf
POR
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28.22%
Cenário clínico: A síndrome dolorosa miofascial (SDM), causa comum de dor musculoesquelética, pode ser incapacitante e desafiadora terapeuticamente, devido à ineficácia dos tratamentos convencionais para dor. Intervenções terapêuticas alternativas precisam ser pesquisadas para alcançar vias do processo de doença não contempladas com a terapêutica clássica. Dentre estas, o uso da melatonina, com efeitos cronobiótico, ansiolítico e analgésico, tem se apresentado como uma opção terapêutica atrativa no tratamento da SDM, que cursa com alterações de sono, dor, sintomas depressivos e de ansiedade. Objetivos: Avaliar a eficácia da melatonina exógena na redução da dor, no limiar de dor à pressão (LDP) e na qualidade de sono de pacientes com SDM facial. Métodos e Resultados: Um estudo randomizado, controlado foi realizado em 45 mulheres com dor miofascial, com idades entre 18 e 40 anos, segundo critérios Research Diagnostic Criteria for Temporomandibular Disorder (RDC/TMD). A eficácia da melatonina oral foi avaliada na redução da dor e melhora tanto do limiar de dor a pressão (LDP) como da qualidade do sono. Os participantes foram randomizados para receber 5 mg / dia de melatonina, 5 mg / dia ciclobenzaprina...

Patient Education and Self-Care for the Management of Jaw Pain upon Awakening: A Randomized Controlled Clinical Trial Comparing the Effectiveness of Adding Pharmacologic Treatment with Cyclobenzaprine or Tizanidine

Alencar, Francisco Guedes Pereira Junior de; Sabino Viana, Patricia Gabriela; Zamperini, Camila Andrade; Becker, Anne Buss
Fonte: Quintessence Publishing Co Inc Publicador: Quintessence Publishing Co Inc
Tipo: Artigo de Revista Científica Formato: 119-127
ENG
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Aims: To compare the effectiveness of adding cyclobenzaprine, tizanidine, or placebo to patient education and a self-care management program for patients with myofascial pain and specifically presenting with jaw pain upon awakening. Methods: Forty-five patients with a diagnosis of myofascial pain based on the guidelines of the American Academy of Orofacial Pain participated in this 3-week study. The subjects were randomly assigned into one of three groups: placebo group, TZA group (tizanidine 4 mg), or CYC group (cyclobenzaprine 10 mg). Patients were evaluated for changes in pain intensity, frequency, and duration by using the modified Severity Symptoms Index and changes in sleep quality with the use of the Pittsburgh Sleep Quality Index. Data were analyzed by ANOVA and post-hoc or nonparametric statistical tests as appropriate. Results: All three groups had a reduction in pain symptoms and improvement of sleep quality based on a comparison of pretreatment and treatment scores. However, no significant differences among the groups were observed at the posttreatment evaluation. Conclusion: The use of tizanidine or cyclobenzaprine in addition to self-care management and patient education was not more effective than placebo for the management of patients with myofascial jaw pain upon awakening.

Element Determination in Pharmaceuticals Using Direct Solid Analysis- Electrothermal Vaporization Inductively Coupled Plasma Optical Emission Spectrometry

Kaczala,Suelem; Costa,Adilson B.; Posselt,Ederson L.; Barin,Juliano S.; Flores,Erico M. M.; Dressler,Valderi L.
Fonte: Sociedade Brasileira de Química Publicador: Sociedade Brasileira de Química
Tipo: Artigo de Revista Científica Formato: text/html
Publicado em 01/03/2015 EN
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16.81%
A solid sampling electrothermal vaporization inductively coupled plasma optical emission spectrometry (ETV-ICP OES) method for determination of As, Cd, Cr, Cu, Mn, Mo, Ni, Pb, Pd, Pt, Rh, Ru and V in pharmaceuticals is proposed. Tricyclic pharmaceuticals were directly analyzed due to their difficult decomposition with acids. Pyrolysis and vaporization temperature, sample mass, and reaction gas (Freon) flow rate were evaluated. The effect of organic and inorganic compounds was evaluated for matrix matching. The limits of detection ranged from 0.04 µg g−1 (Cu) to 107 µg g−1 (As) and the relative standard deviation was lower than 10%. The investigated elements were not detected in the analyzed samples with the exception of Cr in cyclobenzaprine hydrochloride. Since there was no certified reference materials available for metals and metalloids in pharmaceuticals, the accuracy of the method was evaluated by an independent technique and by analyte recovery. Inductively coupled plasma mass spectrometry was employed for analyte determination after sample decomposition by microwave induced combustion. The agreement of the results found by both techniques was better than 87% and analyte recoveries ranged from 91 to 103%.

Prevention of the Emergence of Drug Resistance in Bacteria by Acridines, Phenothiazines, and Dibenzocycloheptenes

Heller, Carole S.; Sevag, M. G.
Fonte: PubMed Publicador: PubMed
Tipo: Artigo de Revista Científica
Publicado em /11/1966 EN
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It has been found that, like Atabrine, the phenothiazine tranquilizers promazine, chlorpromazine, promethazine, levopromethazine, and Stelazine; the antidepressants (dibenz-azepine and dibenzocycloheptene derivatives) Tofranil, Pertofrane, cyclobenzaprine, Elavil, protriptyline, and 3-chlorodibenzocycloheptene; and the acridine derivatives acridine orange, acriflavin, SKF no. 16214-A2, SKF no. 13231-A2, SKF no. 9200, and SKF no. 9836 are all to a greater or lesser extent than Atabrine, effective in preventing the emergence of resistant strains of Staphylococcus aureus and Escherichia coli in the presence of streptomycin, sulfathiazole, or chloramphenicol. The antimalarials chloroquine and hydroxychloroquine were also studied and found to be ineffective. The medical significance of these findings is discussed, as well as the effect of the structural variations of these compounds on their relative activities.

Rhabdomyolysis: a manifestation of cyclobenzaprine toxicity

Chabria, Shiven B
Fonte: BioMed Central Publicador: BioMed Central
Tipo: Artigo de Revista Científica
Publicado em 17/07/2006 EN
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27.85%
A case of cyclobenzaprine (flexeril) overdose and the resultant rhabdomyolysis is presented. A review of the range of clinical toxicity, management of overdose is described. The similarity of cyclobenzaprine to the tricyclic antidepressant class is emphasized; this report attempts to disseminate related information on this commonly prescribed centrally acting muscle relaxant.

Evidence that tricyclic small molecules may possess Toll-like receptor and MD-2 activity

Hutchinson, Mark R.; Loram, Lisa C.; Zhang, Yingning; Shridhar, Mitesh; Rezvani, Niloofar; Berkelhammer, Debra; Phipps, Simon; Foster, Paul S.; Landgraf, Kyle; Falke, Joseph J.; Rice, Kenner C.; Maier, Steven F.; Yin, Hang; Watkins, Linda R.
Fonte: PubMed Publicador: PubMed
Tipo: Artigo de Revista Científica
EN
Relevância na Pesquisa
16.81%
Opioids have been discovered to have Toll-like receptor (TLR) activity, beyond actions at classical opioid receptors. This raises the question whether other pharmacotherapies for pain control may also possess TLR activity, contributing to or opposing their clinical effects. We document that tricyclics can alter TLR4 and TLR2 signaling. In silico simulations revealed that several tricyclics docked to the same binding pocket on the TLR accessory protein, MD-2, as do opioids. Eight tricyclics were tested for effects on TLR4 signaling in HEK293 cells over-expressing human TLR4. Six exhibited mild (desipramine), moderate (mianserin, cyclobenzaprine, imiprimine, ketotifen) or strong (amitriptyline) TLR4 inhibition, and no TLR4 activation. In contrast, carbamazepine and oxcarbazepine exhibited mild and strong TLR4 activation, respectively, and no TLR4 inhibition. Amitriptyline but not carbamazepine also significantly inhibited TLR2 signaling in a comparable cell line. Live imaging of TLR4 activation in RAW264.7 cells and TLR4-dependent interleukin-1 release from BV-2 microglia revealed that amitriptyline blocked TLR4 signaling. Lastly, tricyclics with no (carbamazepine), moderate (cyclobenzeprine), and strong (amitriptyline) TLR4 inhibition were tested intrathecally (rats) and amitriptyline tested systemically in wildtype and knockout mice (TLR4 or MyD88). While tricyclics had no effect on basal pain responsivity...

Drug Repurposing from an Academic Perspective

Oprea, Tudor I.; Bauman, Julie E.; Bologa, Cristian G.; Buranda, Tione; Chigaev, Alexandre; Edwards, Bruce S.; Jarvik, Jonathan W.; Gresham, Hattie D.; Haynes, Mark K.; Hjelle, Brian; Hromas, Robert; Hudson, Laurie; Mackenzie, Debra A.; Muller, Carolyn Y.
Fonte: PubMed Publicador: PubMed
Tipo: Artigo de Revista Científica
Publicado em //2011 EN
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Academia and small business research units are poised to play an increasing role in drug discovery, with drug repurposing as one of the major areas of activity. Here we summarize project status for a number of drugs or classes of drugs: raltegravir, cyclobenzaprine, benzbromarone, mometasone furoate, astemizole, R-naproxen, ketorolac, tolfenamic acid, phenothiazines, methylergonovine maleate and beta-adrenergic receptor drugs, respectively. Based on this multi-year, multi-project experience we discuss strengths and weaknesses of academic-based drug repurposing research. Translational, target and disease foci are strategic advantages fostered by close proximity and frequent interactions between basic and clinical scientists, which often result in discovering new modes of action for approved drugs. On the other hand, lack of integration with pharmaceutical sciences and toxicology, lack of appropriate intellectual coverage and issues related to dosing and safety may lead to significant drawbacks. The development of a more streamlined regulatory process world-wide, and the development of pre-competitive knowledge transfer systems such as a global healthcare database focused on regulatory and scientific information for drugs world-wide...

Identifying mechanism-of-action targets for drugs and probes

Gregori-Puigjané, Elisabet; Setola, Vincent; Hert, Jérôme; Crews, Brenda A.; Irwin, John J.; Lounkine, Eugen; Marnett, Lawrence; Roth, Bryan L.; Shoichet, Brian K.
Fonte: National Academy of Sciences Publicador: National Academy of Sciences
Tipo: Artigo de Revista Científica
EN
Relevância na Pesquisa
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Notwithstanding their key roles in therapy and as biological probes, 7% of approved drugs are purported to have no known primary target, and up to 18% lack a well-defined mechanism of action. Using a chemoinformatics approach, we sought to “de-orphanize” drugs that lack primary targets. Surprisingly, targets could be easily predicted for many: Whereas these targets were not known to us nor to the common databases, most could be confirmed by literature search, leaving only 13 Food and Drug Administration—approved drugs with unknown targets; the number of drugs without molecular targets likely is far fewer than reported. The number of worldwide drugs without reasonable molecular targets similarly dropped, from 352 (25%) to 44 (4%). Nevertheless, there remained at least seven drugs for which reasonable mechanism-of-action targets were unknown but could be predicted, including the antitussives clemastine, cloperastine, and nepinalone; the antiemetic benzquinamide; the muscle relaxant cyclobenzaprine; the analgesic nefopam; and the immunomodulator lobenzarit. For each, predicted targets were confirmed experimentally, with affinities within their physiological concentration ranges. Turning this question on its head, we next asked which drugs were specific enough to act as chemical probes. Over 100 drugs met the standard criteria for probes...

Neuropsychiatric side effects of cyclobenzaprine

Shprecher, David; Sloan, Colgan T; Sederholm, Benson
Fonte: BMJ Publishing Group Publicador: BMJ Publishing Group
Tipo: Artigo de Revista Científica
Publicado em 02/05/2013 EN
Relevância na Pesquisa
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Cyclobenzaprine is commonly used as a muscle relaxant and analgesic. Given its tricyclic properties, serotonin syndrome is a potential side effect of this drug. We report an unusual case of a patient who experienced symptoms of delirium and hyperkinetic movement disorders shortly after initiating treatment with cyclobenzaprine and oxycodone. Symptoms resolved within 48 h of discontinuing cyclobenzaprine. This case serves to remind clinicians to monitor for serotonin syndrome when initiating cyclobenzaprine, and when adding opiate or antidepressant medications to the regimen.

Pharmacokinetics and Bioequivalence Evaluation of Cyclobenzaprine Tablets

Brioschi, Tatiane Maria de Lima Souza; Schramm, Simone Grigoleto; Kano, Eunice Kazue; Koono, Eunice Emiko Mori; Ching, Ting Hui; Serra, Cristina Helena dos Reis; Porta, Valentina
Fonte: Hindawi Publishing Corporation Publicador: Hindawi Publishing Corporation
Tipo: Artigo de Revista Científica
EN
Relevância na Pesquisa
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The purpose of this study was to investigate cyclobenzaprine pharmacokinetics and to evaluate bioequivalence between two different tablet formulations containing the drug. An open, randomized, crossover, single-dose, two-period, and two-sequence design was employed. Tablets were administered to 23 healthy subjects after an overnight fasting and blood samples were collected up to 240 hours after drug administration. Plasma cyclobenzaprine was quantified by means of an LC-MS/MS method. Pharmacokinetic parameters related to absorption, distribution, and elimination were calculated. Cyclobenzaprine plasma profiles for the reference and test products were similar, as well as absorption pharmacokinetic parameters AUC (reference: 199.4 ng∗h/mL; test: 201.6 ng∗h/mL), Cmax (reference: 7.0 ng/mL; test: 7.2 ng/mL), and Tmax (reference: 4.5 h; test: 4.6 h). Bioequivalence was evaluated by means of 90% confidence intervals for the ratio of AUC (93%–111%) and Cmax (93%–112%) values for test and reference products, which were within the 80%–125% interval proposed by FDA. Cyclobenzaprine pharmacokinetics can be described by a multicompartment open model with an average rapid elimination half-life (t(1/2)β) of 3.1 hours and an average terminal elimination half-life (t(1/2)γ) of 31.9 hours.

Linking Pharmacology to Clinical Reports: Cyclobenzaprine and Its Possible Association With Serotonin Syndrome

Mestres, J; Seifert, SA; Oprea, TI
Fonte: PubMed Publicador: PubMed
Tipo: Artigo de Revista Científica
EN
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28.07%
The link between cyclobenzaprine (Flexeril) administration and serotonin syndrome (SS) is subject to debate. Establishing such a connection is difficult because of the limited number of case reports available and the almost complete ignorance of its preclinical pharmacology. In this context, evidence is provided here that cyclobenzaprine blocks the serotonin and norepinephrine transporters and binds to another set of five serotonin receptors. SS should be considered when indicative signs occur in the context of cyclobenzaprine use.

Detection and Quantification of Tricyclic Antidepressants and Other Psychoactive Drugs in Urine by HPLC/MS/MS for Pain Management Compliance Testing

Poklis, Justin L.; Wolf, Carl E.; Goldstein, Ashley; Wolfe, M. Lauren; Poklis, Alphonse
Fonte: PubMed Publicador: PubMed
Tipo: Artigo de Revista Científica
Publicado em /07/2012 EN
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16.81%
A sensitive, specific, and rapid high-pressure liquid chromatography/mass spectrometry/mass spectrometry method was developed for the quantitation of 11 tricyclic antidepressants and/or their metabolites; fluoxetine and norfluoxetine; cyclobenzaprine; and trazodone in urine. Samples were alkalinized with 0.2 N NaOH and extracted into 2 ml of hexane: ethyl acetate (1:1), evaporated to dryness, and reconstituted with 100 μl of 20 mM ammonium formate: methanol (20:80). The chromatographic separation was performed using an Allure Biphenyl 100 × 3.2 mm, 5-μ column with a mobile phase consisting of 20 mM ammonium formate: methanol (20:80 v/v) at a flow rate of 0.5 ml/min. The detection was accomplished by multiple-reaction monitoring via electrospray ionization source operating in the positive ionization mode. The calibration curve was linear over the investigated concentration range, 25–2,000 ng/ml, for each analyte using 1.0 ml of urine. The lower limit of quantitation for each analyte was 25 ng/ml. The intra- and inter-day precisions had coefficient of variation less than 15% and the accuracy was within the range from 88% to 109%. The method proved adequate for the tricyclic antidepressants analysis of urine for emergency clinical toxicology and pain management compliance testing.

A Predictive In Vitro Model of the Impact of Drugs with Anticholinergic Properties on Human Neuronal and Astrocytic Systems

Woehrling, Elizabeth K.; Parri, H. Rheinallt; Tse, Erin H. Y.; Hill, Eric J.; Maidment, Ian D.; Fox, G. Christopher; Coleman, Michael D.
Fonte: Public Library of Science Publicador: Public Library of Science
Tipo: Artigo de Revista Científica
Publicado em 04/03/2015 EN
Relevância na Pesquisa
17.85%
The link between off-target anticholinergic effects of medications and acute cognitive impairment in older adults requires urgent investigation. We aimed to determine whether a relevant in vitro model may aid the identification of anticholinergic responses to drugs and the prediction of anticholinergic risk during polypharmacy. In this preliminary study we employed a co-culture of human-derived neurons and astrocytes (NT2.N/A) derived from the NT2 cell line. NT2.N/A cells possess much of the functionality of mature neurons and astrocytes, key cholinergic phenotypic markers and muscarinic acetylcholine receptors (mAChRs). The cholinergic response of NT2 astrocytes to the mAChR agonist oxotremorine was examined using the fluorescent dye fluo-4 to quantitate increases in intracellular calcium [Ca2+]i. Inhibition of this response by drugs classified as severe (dicycloverine, amitriptyline), moderate (cyclobenzaprine) and possible (cimetidine) on the Anticholinergic Cognitive Burden (ACB) scale, was examined after exposure to individual and pairs of compounds. Individually, dicycloverine had the most significant effect regarding inhibition of the astrocytic cholinergic response to oxotremorine, followed by amitriptyline then cyclobenzaprine and cimetidine...

Evidence that tricyclic small molecules may possess toll-like receptor and myeloid differentiation protein 2 activity

Hutchinson, M.; Loram, L.; Zhang, Y.; Shridhar, M.; Rezvani, N.; Berkelhammer, D.; Phipps, S.; Foster, P.; Landgraf, K.; Falke, J.; Rice, K.; Maier, S.; Yin, H.; Watkins, L.
Fonte: Pergamon-Elsevier Science Ltd Publicador: Pergamon-Elsevier Science Ltd
Tipo: Artigo de Revista Científica
Publicado em //2010 EN
Relevância na Pesquisa
16.81%
Opioids have been discovered to have Toll-like receptor (TLR) activity, beyond actions at classical opioid receptors. This raises the question whether other pharmacotherapies for pain control may also possess TLR activity, contributing to or opposing their clinical effects. We document that tricyclics can alter TLR4 and TLR2 signaling. In silico simulations revealed that several tricyclics docked to the same binding pocket on the TLR accessory protein, myeloid differentiation protein 2 (MD-2), as do opioids. Eight tricyclics were tested for effects on TLR4 signaling in HEK293 cells over-expressing human TLR4. Six exhibited mild (desipramine), moderate (mianserin, cyclobenzaprine, imiprimine, ketotifen) or strong (amitriptyline) TLR4 inhibition, and no TLR4 activation. In contrast, carbamazepine and oxcarbazepine exhibited mild and strong TLR4 activation, respectively, and no TLR4 inhibition. Amitriptyline but not carbamazepine also significantly inhibited TLR2 signaling in a comparable cell line. Live imaging of TLR4 activation in RAW264.7 cells and TLR4-dependent interleukin-1 release from BV-2 microglia revealed that amitriptyline blocked TLR4 signaling. Lastly, tricyclics with no (carbamazepine), moderate (cyclobenzeprine), and strong (amitriptyline) TLR4 inhibition were tested intrathecally (rats) and amitriptyline tested systemically in wildtype and knockout mice (TLR4 or MyD88). While tricyclics had no effect on basal pain responsivity...

Muscle relaxants for pain management in rheumatoid arthritis

Richards, B.L.; Whittle, S.L.; Buchbinder, R.
Fonte: Cochrane Collaboration Publicador: Cochrane Collaboration
Tipo: Artigo de Revista Científica
Publicado em //2012 EN
Relevância na Pesquisa
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BACKGROUND Pain management is a high priority for patients with rheumatoid arthritis (RA). Muscle relaxants include drugs that reduce muscle spasm (for example benzodiazepines such as diazepam (Valium), alprazolam (Xanax), lorazepam (Ativan) and non-benzodiazepines such as metaxalone (Skelaxin) or a combination of paracetamol and orphenadrine (Muscol)) and drugs that prevent increased muscle tone (baclofen and dantrolene). Despite a paucity of evidence supporting their use, antispasmodic and antispasticity muscle relaxants have gained widespread clinical acceptance as adjuvants in the management of patients with chronic musculoskeletal pain. OBJECTIVES The aim of this review was to determine the efficacy and safety of muscle relaxants in pain management in patients with RA. The muscle relaxants that were included in this review are the antispasmodic benzodiazepines (alprazolam, bromazepam, chlordiazepoxide,cinolazepam, clonazepam, cloxazolam, clorazepate, diazepam, estazolam, flunitrazepam, flurazepam, flutoprazepam, halazepam, ketazolam, loprazolam, lorazepam, lormetazepam, medazepam, midazolam, nimetazepam, nitrazepam, nordazepam, oxazepam, pinazepam, prazepam, quazepam, temazepam, tetrazepam, triazolam), antispasmodic non-benzodiazepines (cyclobenzaprine...

Assessment of cyclobenzaprine in the treatment of spasticity

Ashby, Peter; Burke, David; Rao, Sudhakar; Jones, Richard F.
Fonte: PubMed Publicador: PubMed
Tipo: Artigo de Revista Científica
Publicado em /10/1972 EN
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27.85%
The efficacy of cyclobenzaprine 60 mg/day in the treatment of spasticity was assessed in a double-blind crossover trial of two weeks' duration in 15 patients suffering from cerebral or spinal spasticity. Independent clinical and electromyographic methods were used. The effects of cyclobenzaprine did not differ significantly from those of placebo. The administration of a higher dosage, 150 mg/day, to one patient revealed a dose-related response, but the degree of improvement was clinically small. Apart from a skin rash there were no significant untoward effects of therapy.

Rhabdomyolysis as a manifestation of clomipramine poisoning

Santana,Nathalie Oliveira de; Góis,Aécio Flávio Teixeira de
Fonte: Associação Paulista de Medicina - APM Publicador: Associação Paulista de Medicina - APM
Tipo: Artigo de Revista Científica Formato: text/html
Publicado em 01/01/2013 EN
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16.81%
CONTEXT: Tricyclic antidepressive agents are widely used in suicide attempts and present a variety of deleterious effects. Rhabdomyolysis is a rare complication of such poisoning. CASE REPORT: A 55-year-old woman ingested 120 pills of 25 mg clomipramine in a suicide attempt two days before admission. After gastric lavage in another emergency department on the day of intake, 80 pills were removed. On admission to our department, she was disoriented, complaining of a dry mouth and tremors at the extremities. An electrocardiogram showed a sinus rhythm with narrow QRS complexes. Laboratory results showed high creatine phosphokinase (CK = 15,094 U/l on admission; normal range = 26 to 140 U/l), hypocalcemia, slightly increased serum transaminases and mild metabolic acidosis. The patient's medical history included depression with previous suicide attempts, obsessive-compulsive disorder, hypothyroidism and osteoporosis. She presented cardiac arrest with pulseless electric activity for seven minutes and afterwards, without sedation, showed continuous side-to-side eye movement. She developed refractory hypotension, with need for vasopressors. Ceftriaxone and clindamycin administration was started because of a hypothesis of bronchoaspiration. The patient remained unresponsive even without sedation...

Bioavailability of a controlled-release cyclobenzaprine tablet and influence of a high fat meal on bioavailability

Arancibia, Aquiles; Costa, E.; Gai, María Nella
Fonte: DUSTRI-VERLAG DR KARL FEISTLE Publicador: DUSTRI-VERLAG DR KARL FEISTLE
Tipo: Artículo de revista
EN
Relevância na Pesquisa
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Objective: To evaluate the systemic bioavailability of a new controlled release cyclobenzaprine tablet, and the influence of a high fat meal on its bioavailabillty. Subjects, materials and methods: 24 and 12 healthy male subjects were recruited for the bioavailability and influence of diet studies, respectively. Experimental design for both studies was an open randomized, 2-period, single dose, crossover study. In the bioavailability study, each subject received in different occasions, a single oral dose of cyclobenzaprine of immediate (10 mg) or controlled release (20 mg) tablet, followed by a 2-week washout period. In the influence of diet study, the volunteers received the controlled-release tablet concomitantly with a high fat meal or in a state of fasting. Results: In the bioavailability study, plasma cyclobenzaprine profiles were in agreement with a controlled release system. This formulation presented a 92.8% of relative bioavailability (IC 85.5 - 105%) and a significant reduction in C-max (IC 58 - 65.5%), when compared with equal dose of the immediate release tablet. The presence of food increased AUC (11.6%) and C-max (48%). For both parameters the calculated 90% confidence interval was not in the bioequivalence interval, 97.4 - 125.8% for AUC and 111.7 - 184.2% for C-max. Conclusions: The controlled release tablet showed a relative bioavailability comparable with equal dose of the immediate release product and produced a significantly lower C-max...