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[PMID]:28086137
[Au] Autor:Agarwal S; Patel T; Shah N; Patel BM
[Ad] Endereço:Institute of Pharmacy, Nirma University, S.G. Highway, Ahmedabad, 382481, India. Electronic address: srbh.agarwal1@gmail.com.
[Ti] Título:Comparative study of therapeutic response to baclofen vs tolperisone in spasticity.
[So] Source:Biomed Pharmacother;87:628-635, 2017 Mar.
[Is] ISSN:1950-6007
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Spasticity from the upper motor neuron syndrome can result from a variety of conditions affecting the cortex or spinal cord. Some of the more common conditions associated with spasticity include spinal cord injury, cerebral palsy, and post-stroke syndrome. In this study we compared the efficacy and safety of baclofen vs tolperisone in spasticity. One hundred fifty patients with cerebral palsy or post stroke or spinal cord injury associated spasticity were enrolled in present study. Group I comprised of Seventy-five patients receiving baclofen and group II comprised of 75 patients receiving tolperisone. For efficacy measurement 4 evaluation methods were used, 1) Modified Ashworth Scale for muscle tone, 2) Medical research council scale for muscle strength and 3) Barthel Index for functional outcome 4) Coefficient of efficacy. In efficacy evaluation, both groups showed significant improvement in muscle tone, muscle strength and functional outcome at week 6 (Group I, 1.55±0.053, 2.79+0.032, 59.31±1.32; Group II, 1.57±0.053, 3.04±0.032, 73±1.32 respectively). In between the group analysis, there was no significant difference in muscle tone improvement in both the groups after 6 weeks (Group I, 1.055±0.053 vs Group II, 1.57±0.053, p>0.05). Group II showed non-significant but greater improvement in muscle strength (Week 6; Group I, 2.79±0.032 vs Group II, 3.04±0.032, p>0.07). Improvement in functional outcomes was greater in group II as compared to group I (Group I, 59.31±1.32 vs Group II, 73±1.32, p<0.05). Overall efficacy coefficient was greater for group II (3.6) as compared to group I (2.3). Baclofen showed more side effects compared to tolperisone in, asthenia being the most frequent. Tolperisone offers greater improvement in activities of daily living compared to baclofen. Tolperisone is more tolerable drug as compared to baclofen.
[Mh] Termos MeSH primário: Baclofeno/uso terapêutico
Relaxantes Musculares Centrais/uso terapêutico
Espasticidade Muscular/tratamento farmacológico
Tolperisona/uso terapêutico
[Mh] Termos MeSH secundário: Adolescente
Adulto
Idoso
Idoso de 80 Anos ou mais
Paralisia Cerebral/tratamento farmacológico
Criança
Pré-Escolar
Feminino
Seres Humanos
Masculino
Meia-Idade
Força Muscular/efeitos dos fármacos
Traumatismos da Medula Espinal/tratamento farmacológico
Acidente Vascular Cerebral/tratamento farmacológico
Adulto Jovem
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; RANDOMIZED CONTROLLED TRIAL
[Nm] Nome de substância:
0 (Muscle Relaxants, Central); F5EOM0LD8E (Tolperisone); H789N3FKE8 (Baclofen)
[Em] Mês de entrada:1702
[Cu] Atualização por classe:170710
[Lr] Data última revisão:
170710
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170114
[St] Status:MEDLINE


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[PMID]:27711973
[Au] Autor:Lindsay C; Kouzouna A; Simcox C; Pandyan AD
[Ad] Endereço:Department of Physiotherapy, South Eastern Health and Social Care Trust, Upper Newtownards Road, Belfast, Co Down, Northern Ireland, UK, BT161RH.
[Ti] Título:Pharmacological interventions other than botulinum toxin for spasticity after stroke.
[So] Source:Cochrane Database Syst Rev;10:CD010362, 2016 Oct 06.
[Is] ISSN:1469-493X
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: The long-term risk of stroke increases with age, and stroke is a common cause of disability in the community. Spasticity is considered a significantly disabling impairment that develops in people who have had a stroke. The burden of care is higher in stroke survivors who have spasticity when compared with stroke survivors without spasticity with regard to treatment costs, quality of life, and caregiver burden. OBJECTIVES: To assess if pharmacological interventions for spasticity are more effective than no intervention, normal practice, or control at improving function following stroke. SEARCH METHODS: We searched the Cochrane Stroke Group Trials Register (May 2016), the Cochrane Central Register of Controlled Trials (CENTRAL, 2016, Issue 5), MEDLINE (1946 to May 2016), Embase (2008 to May 2016), CINAHL (1982 to May 2016), AMED (1985 to May 2016), and eight further databases and trial registers. In an effort to identify further studies, we undertook handsearches of reference lists and contacted study authors and commercial companies. SELECTION CRITERIA: We included randomised controlled trials (RCTs) that compared any systemically acting or locally acting drug versus placebo, control, or comparative drug with the aim of treating spasticity. DATA COLLECTION AND ANALYSIS: Two review authors independently assessed the studies for inclusion and extracted the data. We assessed the included studies for both quality and risk of bias. We contacted study authors to request further information when necessary. MAIN RESULTS: We included seven RCTs with a total 403 participants. We found a high risk of bias in all but one RCT. Two of the seven RCTs assessed a systemic drug versus placebo. We pooled data on an indirect measure of spasticity (160 participants) from these two studies but found no significant effect (odds ratio (OR) 1.66, 95% confidence interval (CI) 0.21 to 13.07; I = 85%). We identified a significant risk of adverse events per participant occurring in the treatment group versus placebo group (risk ratio (RR) 1.65, 95% CI 1.12 to 2.42; 160 participants; I = 0%). Only one of these studies used a functional outcome measure, and we found no significant difference between groups.Of the other five studies, two assessed a systemic drug versus another systemic drug, one assessed a systemic drug versus local drug, and the final two assessed a local drug versus another local drug. AUTHORS' CONCLUSIONS: The lack of high-quality RCTs limited our ability to make specific conclusions. Evidence is insufficient to determine if systemic antispasmodics are effective at improving function following stroke.
[Mh] Termos MeSH primário: Espasticidade Muscular/tratamento farmacológico
Acidente Vascular Cerebral/complicações
[Mh] Termos MeSH secundário: Baclofeno/uso terapêutico
Toxinas Botulínicas Tipo A/uso terapêutico
Clonidina/análogos & derivados
Clonidina/uso terapêutico
Diazepam/uso terapêutico
Seres Humanos
Relaxantes Musculares Centrais/uso terapêutico
Ensaios Clínicos Controlados Aleatórios como Assunto
Tolperisona/uso terapêutico
[Pt] Tipo de publicação:JOURNAL ARTICLE; META-ANALYSIS; RESEARCH SUPPORT, NON-U.S. GOV'T; REVIEW
[Nm] Nome de substância:
0 (Muscle Relaxants, Central); 6AI06C00GW (tizanidine); E211KPY694 (onabotulinumtoxinA); EC 3.4.24.69 (Botulinum Toxins, Type A); F5EOM0LD8E (Tolperisone); H789N3FKE8 (Baclofen); MN3L5RMN02 (Clonidine); Q3JTX2Q7TU (Diazepam)
[Em] Mês de entrada:1611
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161007
[St] Status:MEDLINE


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[PMID]:26978504
[Au] Autor:Popov VV; Menenkova EY; Babakhina SN; Bezzubik EG; Isakova YA; Lezina DS; Dmukhovski DV; Merkulov YA; Merkulova DM
[Ad] Endereço:Semashko Research Clinical Center of the 'Russian Railways', Moscow; Sechenov First Moscow State Medical University, Moscow.
[Ti] Título:[A clinical efficacy of electrode pharmaphoresis in treatment of railway workers with low-back pain].
[So] Source:Zh Nevrol Psikhiatr Im S S Korsakova;115(12):118-122, 2015.
[Is] ISSN:1997-7298
[Cp] País de publicação:Russia (Federation)
[La] Idioma:rus
[Ab] Resumo:OBJECTIVE: To evaluate clinical efficacy and tolerability of electrode pharmaphoresis using preparations xefocam and mydocalm-richter in railway workers with low-back pain. MATERIAL AND METHODS: Authors carried out an open prospective noncomparative study of 16 patients, aged 21-82 years, with spinal osteochondrosis with root syndrome and radiculopathia of the lumbar/sacral spine with pain syndrome regardless of its duration. Treatment efficacy was assessed by the dynamics of pain syndrome severity based on the scores of a self-rated scale completed by the patient and the McGill Pain Questionnaire. Quality-of-life was assessed with the Oswestry Disability Index before and in the end of treatment. Clinical outcome was evaluated with the modified Nurick scale. Electrode pharmaphoresis (the "Farma T.E.B. Trans Epidermal Barrier Physio" apparatus) was administered to all patients using xefocam (solution for injections 8 mg, 2 ml per procedure) and mydocalm-richter (solution for injections 100 mg, 2 ml per injection) in the lumbar/sacral spine. RESULTS AND CONCLUSION: The high clinical efficacy of electrode pharmaphoresis using xefocam and mydocalm-richter was shown. The complex restoration study resulted in the reduction of pain syndrome in all patients. Pain severity was reduced to mild grade in 68.8% to the middle of treatment and in 93.8% patients in the end of treatment. As a consequence of pain reduction, the functional activity (quality of self-service, daily activities) increased significantly in 68.8% of patients. Positive treatment effect was noted in 100% of patients, good tolerability of this medication in 87.5%.
[Mh] Termos MeSH primário: Anti-Inflamatórios não Esteroides/administração & dosagem
Dor Lombar/tratamento farmacológico
Relaxantes Musculares Centrais/administração & dosagem
Piroxicam/análogos & derivados
Tolperisona/administração & dosagem
[Mh] Termos MeSH secundário: Adulto
Idoso
Idoso de 80 Anos ou mais
Eletrodos
Eletroforese/instrumentação
Eletroforese/métodos
Feminino
Seres Humanos
Dor Lombar/etiologia
Vértebras Lombares
Região Lombossacral
Masculino
Meia-Idade
Medição da Dor
Piroxicam/administração & dosagem
Estudos Prospectivos
Radiculopatia/complicações
Radiculopatia/tratamento farmacológico
Ferrovias/recursos humanos
Resultado do Tratamento
Adulto Jovem
[Pt] Tipo de publicação:ENGLISH ABSTRACT; EVALUATION STUDIES; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents, Non-Steroidal); 0 (Muscle Relaxants, Central); 13T4O6VMAM (Piroxicam); ER09126G7A (lornoxicam); F5EOM0LD8E (Tolperisone)
[Em] Mês de entrada:1604
[Cu] Atualização por classe:170621
[Lr] Data última revisão:
170621
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160316
[St] Status:MEDLINE
[do] DOI:10.17116/jnevro2015115112118-122


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[PMID]:26978502
[Au] Autor:Skoromets AA; Guekht AB; Galanov DV; Danilenko OA; Barantsevich ER; Lebedeva AV; Belova AN; Shprakh VV; Bogdanov EI; Prokopenko SV; Khabirov FA; Spirin NN; Baliazin VA; Miakotnykh VS; Volkova LI; Gafurov BG; Mishchenko TS; Toktomushev CT; Shyralieva RK; Musaev SK; Guseinov SG
[Ad] Endereço:Ural State Medical University, Ekaterinburg, Ural State Medical Academy, Ekaterinburg, Rostov State Medical University, Rostov-on-Don, Yaroslavl State Medical Academy, Yaroslsvl, Kazan State Medical Academy, Kazan, V.F.Voyno-Yasenetsky Krasnoyarsk State Medical University, Krasnoyarsk, Kazan State M
[Ti] Título:[The results of the multicenter pharmaco-epidemiological observational project on the use of mydocalm in the treatment of pain syndromes with the muscle spasm].
[So] Source:Zh Nevrol Psikhiatr Im S S Korsakova;115(12):104-109, 2015.
[Is] ISSN:1997-7298
[Cp] País de publicação:Russia (Federation)
[La] Idioma:rus
[Ab] Resumo:The prospective multicenter open noncomparative pharmaco-epidemiological observational project on the use of mydocalm in real clinical practice has been completed in 2013. The project has been performed in 2090 clinical/rehabilitation settings in 284 cities of 13 countries using the results of 35,383 patients. The project aimed to assess the safety of treatment (percentage of patients with adverse-effects) and pain relieving efficacy as well as patient's satisfaction with the treatment. In total, 6603 (19%) adverse-effects were recorded. Their severity was evaluated as mild in 84,48%, no serious adverse-effects were noted. The high efficacy of mydocalm in the treatment of pain syndromes with the muscle spasm has been demonstrated. The high level of tolerability and absence of the clinically significant increase of adverse effects in the combination with nonsteroidal anti-inflammatory drugs have been confirmed.
[Mh] Termos MeSH primário: Relaxantes Musculares Centrais/uso terapêutico
Dor/tratamento farmacológico
Dor/epidemiologia
Espasmo/tratamento farmacológico
Espasmo/epidemiologia
Tolperisona/uso terapêutico
[Mh] Termos MeSH secundário: Adulto
Anti-Inflamatórios não Esteroides/uso terapêutico
Feminino
Seres Humanos
Masculino
Meia-Idade
Relaxantes Musculares Centrais/efeitos adversos
Dor/complicações
Farmacoepidemiologia
Estudos Prospectivos
Espasmo/complicações
Síndrome
Tolperisona/efeitos adversos
Resultado do Tratamento
[Pt] Tipo de publicação:CLINICAL TRIAL; ENGLISH ABSTRACT; JOURNAL ARTICLE; MULTICENTER STUDY; OBSERVATIONAL STUDY
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents, Non-Steroidal); 0 (Muscle Relaxants, Central); F5EOM0LD8E (Tolperisone)
[Em] Mês de entrada:1604
[Cu] Atualização por classe:170621
[Lr] Data última revisão:
170621
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160316
[St] Status:MEDLINE
[do] DOI:10.17116/jnevro2015115112104-109


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[PMID]:25953735
[Au] Autor:Pawlowska M; Bogiel M; Duda J; Sieradzki E
[Ad] Endereço:Institute of Biotechnology and Antibiotics, Warsaw, Poland. pawlowskam@iba.waw.pl.
[Ti] Título:Influence of CYP2D6 and CYP2C19 genetic polymorphism on the pharmacokinetics of tolperisone in healthy volunteers.
[So] Source:Eur J Clin Pharmacol;71(6):699-705, 2015 Jun.
[Is] ISSN:1432-1041
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:PURPOSE: This is the first study that connects pharmacokinetics of tolperisone with genetic polymorphism of the enzymes involved in its metabolism in human. We aimed to identify the influence of polymorphism of two main enzymes (CYP2D6 and CYP2C19) on pharmacokinetic profile of parent drug. METHODS: In a single-dose study, 28 healthy Caucasian male volunteers received an oral dose of 150 mg of tolperisone. The subjects were genotyped with respect to CYP2D6 and CYP2C19 enzymes. Plasma was sampled for up to 12 h post dose, followed by quantification of tolperisone by a fully validated HPLC-tandem mass spectrometry (MS/MS) method. The pharmacokinetic parameters were estimated using a non-compartmental method and compared statistically at level p < 0.05 across the genotyped groups. RESULTS: High variability (exceeded 100%) of main bioavailability parameters (AUCt, AUC(inf), C(max)) was observed in the whole group of subjects. An essential difference in the pharmacokinetics of tolperisone of quick metabolizers whose genotype expressed wild homozygote CYP2D6 *1/*1 with respect to heterozygous *1/*4 and *1/*5 subjects was demonstrated. The mean AUC(inf) was 2.1- and 3.4-fold higher in *1/*4 and *1/*5, respectively, than in *1/*1 subjects. In case of Cmax, the differences were greater and reached maximally 3.8 times (mean values 54.00, 98.85, and 205.20 ng/mL for CYP2D6 *1/*1, *1/*4, and *1/*5, respectively). Values of the parameters for the one subject that expressed *4/*4 genotype were even 8.5 times higher than in subjects with extensive or intermediate phenotype. Although CYP2C19 *1/*2 subjects had higher AUCt, AUC(inf), and Cmax values than *1/*1, no statistically significant differences were observed. Oral clearance (CL/F) significantly decreased by 65.7% in heterozygous *1/*2 relative to homozygous *1/*1 extensive metabolizers. CONCLUSION: In this study, we first demonstrated the effect of CYP2D6 polymorphism on pharmacokinetics of tolperisone in Caucasian subjects. The contribution of CYP2C19 enzyme seems to be less important.
[Mh] Termos MeSH primário: Citocromo P-450 CYP2C19/genética
Citocromo P-450 CYP2D6/genética
Relaxantes Musculares Centrais/farmacocinética
Polimorfismo Genético/genética
Tolperisona/farmacocinética
[Mh] Termos MeSH secundário: Adulto
Área Sob a Curva
Disponibilidade Biológica
Genótipo
Voluntários Saudáveis
Heterozigoto
Homozigoto
Seres Humanos
Masculino
Fenótipo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Muscle Relaxants, Central); EC 1.14.14.1 (CYP2C19 protein, human); EC 1.14.14.1 (Cytochrome P-450 CYP2C19); EC 1.14.14.1 (Cytochrome P-450 CYP2D6); F5EOM0LD8E (Tolperisone)
[Em] Mês de entrada:1602
[Cu] Atualização por classe:171117
[Lr] Data última revisão:
171117
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150509
[St] Status:MEDLINE
[do] DOI:10.1007/s00228-015-1856-5


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[PMID]:25772423
[Au] Autor:Martos V; Hofer KE; Rauber-Lüthy C; Schenk-Jaeger KM; Kupferschmidt H; Ceschi A
[Ad] Endereço:National Poisons Centre, Tox Info Suisse, Associated Institute of the University of Zurich , Zurich , Switzerland.
[Ti] Título:Acute toxicity profile of tolperisone in overdose: Observational poison centre-based study.
[So] Source:Clin Toxicol (Phila);53(5):470-6, 2015 Jun.
[Is] ISSN:1556-9519
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:INTRODUCTION: Tolperisone is a centrally acting muscle relaxant that acts by blocking voltage-gated sodium and calcium channels. There is a lack of information on the clinical features of tolperisone poisoning in the literature. The aim of this study was to investigate the demographics, circumstances and clinical features of acute overdoses with tolperisone. METHODS: An observational study of acute overdoses of tolperisone, either alone or in combination with one non-steroidal anti-inflammatory drug in a dose range not expected to cause central nervous system effects, in adults and children (< 16 years), reported to our poison centre between 1995 and 2013. RESULTS: 75 cases were included: 51 females (68%) and 24 males (32%); 45 adults (60%) and 30 children (40%). Six adults (13%) and 17 children (57%) remained asymptomatic, and mild symptoms were seen in 25 adults (56%) and 10 children (33%). There were nine adults (20%) with moderate symptoms, and five adults (11%) and three children (10%) with severe symptoms. Signs and symptoms predominantly involved the central nervous system: somnolence, coma, seizures and agitation. Furthermore, some severe cardiovascular and respiratory signs and symptoms were reported. The minimal dose for seizures and severe symptoms in adults was 1500 mg. In 11 cases the latency between the ingestion and the onset of symptoms was known and was reported to be 0.5-1.5 h. CONCLUSIONS: The acute overdose of tolperisone may be life-threatening, with a rapid onset of severe neurological, respiratory and cardiovascular symptoms. With alternative muscle relaxants available, indications for tolperisone should be rigorously evaluated.
[Mh] Termos MeSH primário: Overdose de Drogas/diagnóstico
Relaxantes Musculares Centrais/envenenamento
Centros de Controle de Intoxicações
Envenenamento/diagnóstico
Tolperisona/envenenamento
[Mh] Termos MeSH secundário: Doença Aguda
Adolescente
Adulto
Idoso
Idoso de 80 Anos ou mais
Anti-Inflamatórios não Esteroides/efeitos adversos
Sistema Cardiovascular/efeitos dos fármacos
Sistema Cardiovascular/fisiopatologia
Sistema Nervoso Central/efeitos dos fármacos
Sistema Nervoso Central/fisiopatologia
Criança
Pré-Escolar
Overdose de Drogas/mortalidade
Overdose de Drogas/fisiopatologia
Overdose de Drogas/terapia
Feminino
Seres Humanos
Lactente
Pulmão/efeitos dos fármacos
Pulmão/fisiopatologia
Masculino
Meia-Idade
Envenenamento/mortalidade
Envenenamento/fisiopatologia
Envenenamento/terapia
Prognóstico
Estudos Retrospectivos
Medição de Risco
Fatores de Risco
Índice de Gravidade de Doença
Suíça
Fatores de Tempo
Adulto Jovem
[Pt] Tipo de publicação:JOURNAL ARTICLE; OBSERVATIONAL STUDY; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents, Non-Steroidal); 0 (Muscle Relaxants, Central); F5EOM0LD8E (Tolperisone)
[Em] Mês de entrada:1507
[Cu] Atualização por classe:150508
[Lr] Data última revisão:
150508
[Sb] Subgrupo de revista:AIM; IM
[Da] Data de entrada para processamento:150317
[St] Status:MEDLINE
[do] DOI:10.3109/15563650.2015.1022896


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[PMID]:25632432
[Au] Autor:Miura N; Saito T; Taira T; Yamagiwa T; Morita S; Inokuchi S
[Ti] Título:Rapid simultaneous determination of eperisone, tolperisone, and tizanidine in human serum by using a MonoSpin® C18 extraction column and liquid chromatography/tandem mass spectrometry.
[So] Source:J AOAC Int;97(6):1546-51, 2014 Nov-Dec.
[Is] ISSN:1060-3271
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:A method was developed for rapid toxicological analysis of eperisone, tolperisone, and tizanidine in human serum using a MonoSpin® C18 extraction column and LC/MS/MS. The method was validated for LOD, linearity, precision, and extraction recovery. This method was rapid with an LOD of 0.5 ng/mL, linearity range 1-500.0 ng/mL (r2 = 0.999), and RSD value below 14.6%. Extraction recovery from the sample was greater than 98.6, 98.8, and 88.5% for eperisone, tolperisone, and tizanidine, respectively. Results showed that combination of the MonoSpin C18 extraction column and LC/MS/MS is a simple and rapid method for the analysis of these three analytes, and a method is described for simultaneous quantitative determination of the analytes in human serum by LC/MSIMS. This method was used to determine the serum levels of eperisone in a patient with eperisone poisoning, and could be successfully applied for screening analyses in clinical cases other than poisoning.
[Mh] Termos MeSH primário: Cromatografia Líquida de Alta Pressão/métodos
Clonidina/análogos & derivados
Relaxantes Musculares Centrais/sangue
Propiofenonas/sangue
Espectrometria de Massas em Tandem/métodos
Tolperisona/sangue
[Mh] Termos MeSH secundário: Cromatografia Líquida de Alta Pressão/economia
Clonidina/sangue
Feminino
Seres Humanos
Limite de Detecção
Meia-Idade
Espectrometria de Massas por Ionização por Electrospray/métodos
Espectrometria de Massas em Tandem/economia
[Pt] Tipo de publicação:JOURNAL ARTICLE; VALIDATION STUDIES
[Nm] Nome de substância:
0 (Muscle Relaxants, Central); 0 (Propiophenones); 2M2P0551D3 (eperisone); 6AI06C00GW (tizanidine); F5EOM0LD8E (Tolperisone); MN3L5RMN02 (Clonidine)
[Em] Mês de entrada:1502
[Cu] Atualização por classe:150129
[Lr] Data última revisão:
150129
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150130
[St] Status:MEDLINE


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[PMID]:25033566
[Au] Autor:Sapegin VI; Sapegin ID; Il'chenko FN
[Ti] Título:[Influence of mydocalm on the degree of intra-abdominal hypertension and local blood circulation in the intestinal wall in experiment].
[So] Source:Eksp Klin Farmakol;77(5):15-9, 2014.
[Is] ISSN:0869-2092
[Cp] País de publicação:Russia (Federation)
[La] Idioma:rus
[Ab] Resumo:The effect of mydocalm (tolperison, 5 mg/kg single dose) on the dynamics of intra-abdominal hypertension (IAH), blood circulation regulation, and oxygen balance in the tissues of intestinal wall were studied in acute experiments on rabbits. Using a special stand of original design, the initial IAH level was modeled at 200 mm H2O with the subsequent stopping of further receipt of liquid during 3 hours in an elastic container in the abdominal cavity. During 3-h observation without drug administration, no changes in IAH due to the tone of muscles of the frontal abdominal wall takes place, but there is progressive deceleration of local blood flow (-35.33 + 0.99%, p < 0.01), suppressed dilation (-20.02 + 0.54%, p < 0.01) and constriction (-60.45 + 1.17%, p < 0.01) reactivity of vessels, and decreased oxygen tension (-47.18 + 0.75%, p < 0.01) in the intestinal wall at the end of experiment. The introduction of mydocalm reduces the tone of muscles of the frontal abdominal wall, which leads to a decrease in IAH (maximum effect after 1.5 hours, -20.81 + 0.84%, p < 0.01) and prevents decrease in the local blood flow (-26.77 + 0.41%, p < 0.01), suppression of dilation (-16.51 + 0.34%, p < 0.01) and constriction (-37.85 + 0.61%, p < 0.01) reactivity of vessels, and reduction in oxygen tension (-36.60 + 1.18%, p < 0.01) at the end of experiment. The administration of mydocalm can extend the limits of application of a conservative therapy for patients with IAH and to improve the results.
[Mh] Termos MeSH primário: Hemorragia Gastrointestinal/fisiopatologia
Intestinos/irrigação sanguínea
Hipertensão Intra-Abdominal/fisiopatologia
Relaxantes Musculares Centrais/farmacologia
Fluxo Sanguíneo Regional/efeitos dos fármacos
Tolperisona/farmacologia
[Mh] Termos MeSH secundário: Animais
Feminino
Hemorragia Gastrointestinal/patologia
Intestinos/patologia
Intestinos/fisiopatologia
Hipertensão Intra-Abdominal/patologia
Masculino
Coelhos
[Pt] Tipo de publicação:ENGLISH ABSTRACT; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Muscle Relaxants, Central); F5EOM0LD8E (Tolperisone)
[Em] Mês de entrada:1408
[Cu] Atualização por classe:140718
[Lr] Data última revisão:
140718
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:140719
[St] Status:MEDLINE


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[PMID]:23505060
[Au] Autor:Owada Y; Takahashi M; Iwasa S; Ichiba H; Sadamoto K; Fukushima T
[Ad] Endereço:Department of Clinical Science, Faculty of Pharmaceutical Sciences, Toho University, 2-2-1 Miyama, Funabashi-shi, Chiba, 274-8510, Japan.
[Ti] Título:Enantiomeric separation of tolperisone and eperisone by reversed-phase HPLC with cellulose tris(3-chloro-4-methylphenylcarbamate)-coated chiral column.
[So] Source:Biomed Chromatogr;28(1):102-5, 2014 Jan.
[Is] ISSN:1099-0801
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Enantiomeric separations of centrally acting muscle relaxants, that is, tolperisone (TOL) and eperisone (EP), that are marketed as racemates were investigated by reversed-phase high-performance liquid chromatography (HPLC) on a polysaccharide-based chiral column. Both TOL and EP are basic drugs because they contain a tertiary amino group and have similar chemical structures with the exception of the p-methylphenyl and p-ethylphenyl groups in TOL and EP, respectively. A reversed-phase chiral column, that is, a Chiralcel OZ-RH column, which bears cellulose tris(3-chloro-4-methylphenylcarbamate) as the chiral moiety, was effective for the enantiomeric separation of TOL and EP enantiomers. The separation factor and resolution values obtained for TOL were 1.22 and 1.66, respectively, and those for EP were 1.21 and 2.24, respectively, using a 20 mm ammonium acetate in H2 O (pH 8.0 and 7.0, respectively)-CH3 CN (70:30) mobile phase. Using the proposed HPLC conditions, it was found that (R)-TOL eluted faster than (S)-TOL, as revealed by the optical rotation and circular dichroism spectroscopy. In contrast, EP was easily racemized under the experimental conditions, and hence, the elution order was not determined.
[Mh] Termos MeSH primário: Cromatografia Líquida de Alta Pressão/métodos
Cromatografia de Fase Reversa/métodos
Propiofenonas/química
Tolperisona/química
[Mh] Termos MeSH secundário: Celulose/análogos & derivados
Celulose/química
Cromatografia Líquida de Alta Pressão/instrumentação
Cromatografia de Fase Reversa/instrumentação
Fenilcarbamatos/química
Propiofenonas/isolamento & purificação
Estereoisomerismo
Tolperisona/isolamento & purificação
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Phenylcarbamates); 0 (Propiophenones); 0 (cellulose tris(3-chloro-4-methylphenylcarbamate)); 2M2P0551D3 (eperisone); 9004-34-6 (Cellulose); F5EOM0LD8E (Tolperisone)
[Em] Mês de entrada:1408
[Cu] Atualização por classe:131216
[Lr] Data última revisão:
131216
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:130319
[St] Status:MEDLINE
[do] DOI:10.1002/bmc.2892


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[PMID]:24555245
[Au] Autor:Lipták J
[Ti] Título:[Comparative effectiveness of different muscle relaxants in the rehabilitation of post-stroke patients with spasticity].
[Ti] Título:Különbözo izomrelaxánsok hatásosságának összehasonlítása a stroke után spasztikus betegek rehabilitációjában..
[So] Source:Ideggyogy Sz;66(11-12):429, 2013 Nov 30.
[Is] ISSN:0019-1442
[Cp] País de publicação:Hungary
[La] Idioma:hun
[Mh] Termos MeSH primário: Relaxantes Musculares Centrais/uso terapêutico
Espasticidade Muscular/tratamento farmacológico
Reabilitação do Acidente Vascular Cerebral
Acidente Vascular Cerebral/complicações
[Mh] Termos MeSH secundário: Idoso
Baclofeno/uso terapêutico
Clonidina/análogos & derivados
Clonidina/uso terapêutico
Pesquisa Comparativa da Efetividade
Dantroleno/uso terapêutico
Feminino
Seres Humanos
Masculino
Relaxantes Musculares Centrais/administração & dosagem
Relaxantes Musculares Centrais/efeitos adversos
Espasticidade Muscular/etiologia
Espasticidade Muscular/reabilitação
Tono Muscular/efeitos dos fármacos
Recuperação de Função Fisiológica
Autorrelato
Tolperisona/uso terapêutico
Resultado do Tratamento
Caminhada
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Muscle Relaxants, Central); 6AI06C00GW (tizanidine); F5EOM0LD8E (Tolperisone); F64QU97QCR (Dantrolene); H789N3FKE8 (Baclofen); MN3L5RMN02 (Clonidine)
[Em] Mês de entrada:1404
[Cu] Atualização por classe:161125
[Lr] Data última revisão:
161125
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:140222
[St] Status:MEDLINE



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