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1.
Braz. j. med. biol. res ; 55: e11771, 2022. tab, graf
Article in English | LILACS-Express | LILACS | ID: biblio-1364560

ABSTRACT

Seizures are a disorder caused by structural brain lesions, life-threatening metabolic derangements, or drug toxicity. The present study describes the behavior related to proconvulsant activity induced by thiocolchicoside (TCC) in rats and investigates the electrocorticographic patterns of this behavior and the effectiveness of classic antiepileptic drugs used to control these seizures. Forty-nine adult male Wistar rats were used and divided into two phases of our experimental design: 1) evaluation of seizure-related behavior and electrocorticographic patterns induced by TCC and 2) evaluation of the efficacy of classical antiepileptic drugs to control the proconvulsive activity caused by TCC. Our results showed that TCC induced tonic-clonic seizures that caused changes in electrocorticographic readings, characteristic of convulsive activity, with average amplitude greater than that induced by pentylenetetrazole. Treatment with anticonvulsants, especially diazepam, reduced the electrocorticographic outbreaks induced by TCC. The results suggested that TCC caused seizures with increased power in brain oscillations up to 40 Hz and that diazepam may partially reverse the effects.

2.
Article | IMSEAR | ID: sea-200406

ABSTRACT

Background: Low back pain is one of the most common health problems in society which leads to considerable disability, loss of work days, and puts a huge burden on socioeconomic and healthcare system. It is often associated with musculoskeletal spasm. The aim of the study was to compare the efficacy and safety of tolperisone and thiocolchicoside in combination with etodolac in patients of acute low back pain associated with musculoskeletal spasm.Methods: it was a prospective, randomized, open label study which included patients of either sex between age 18-50 years of acute low back pain with musculoskeletal spasm. Patients were allocated in two groups. Patients in 慓roup A� were given tolperisone 150 mg + etodolac 400 mg twice a day and patients in 慓roup B� were given thiocolchicoside 4 mg + etodolac 400 mg twice a day. Efficacy of two drugs was assessed by decrease in finger to floor distance (FFD), decrease in pain as per visual analog scale (VAS) and global assessment of efficacy of treatment by physician. Follow-up of the patients was done on day 3 and 7 of treatment. Various side effects reported by patients in both the groups were also recorded and compared.Results: Both tolperisone and thiocolchicoside caused significant decrease in FFD, reduced pain score thus indicating decrease in pain and spasm. Side effects reported in both groups were mild and did not result in discontinuation of therapy.Conclusions: Tolperisone was found to have efficacy similar to that of thiocolchicoside though number of side effects reported was more with tolperisone.

3.
Article | IMSEAR | ID: sea-199727

ABSTRACT

Background: Skeletal muscle relaxants are a heterogeneous group of drugs. As a group, they are structurally and pharmacologically diverse. Skeletal muscle relaxants are usually used as adjunct therapy when initial therapy fails. They are commonly used to treat fibromyalgia, low back pain, neck pain, tension head ache, myofascial pain and muscle spasm.Methods: There were 28 mice were randomly divided into seven groups, each group consists of 4 mice. Group 1(Control): Mice were treated with normal saline and placed on rotating rod with a speed of 18 rpm (ideal speed). Group 2 (Standard-S1): Mice were treated with Nitrazepam at the dose of 2mg/kg body weight and placed on rotating rod. Group 3 (Standard-S2): Mice were treated with Nitrazepam at the dose of 3mg/kg body weight and placed on rotating rod. Group 4 (Standard-S3): Mice were treated with Nitrazepam at the dose of 4mg/kg body weight and placed on rotating rod. Group 5 (Test-T1): Mice were treated with Thiocolchicoside at the dose of 2mg/kg body weight and placed on rotating rod. Group 6 (Test-T2): Mice were treated with Thiocolchicoside at the dose of 3mg/kg body weight and placed on rotating rod. Group 7 (Test-T3): Mice were treated with Thiocolchicoside at the dose of 4mg/kg body weight and placed on rotating rod.Results: In this model inter drug comparisons were carried out with nitrazepam and thiocolchicoside. It was found that both nitrazepam and thiocolchicoside produced central muscle relaxant effect when assessed by rotarod. On iter drug comparision of nitrazepam and thiocolchicoside it was found that by increasing concentration of drug, increased the muscle relaxant property.Conclusions: When assessed by rotarod, it was found that both nitrazepam and thiocolchicoside demonstrated muscle relaxant property but with increased doses of thiocolchicoside produced more muscle relaxant property than the increase in doses of nitrazepam.

4.
Article | IMSEAR | ID: sea-199572

ABSTRACT

Background: Aceclofenac is a non steroidal anti-inflammatory drug commonly prescribed in patients with acute low back pain. Thiocolchicoside is a skeletal muscle relaxant which is used in combination with NSAIDs. The efficacy of a combination of aceclofenac and thiocolchicoside has to be proved over aceclofenac alone in patients with acute low back pain. Objective of this study was to compare the safety and efficacy of a combination of aceclofenac and thiocolchicoside against aceclofenac alone in patients with acute low back pain.Methods: This study was undertaken as a prospective comparative study. Patients with acute low back pain receiving either aceclofenac 100 mg or a combination of aceclofenac 100 mg and thiocolchicoside 4 mg twice daily were enrolled in the study and were divided into two groups of 50 each. The primary efficacy parameter was pain intensity measured on a visual analogue scale. Adverse effects if any were monitored at the follow up visit.Results: At the start of the study, pain intensity, measured on visual analogue scale was comparable in both the groups. At the end point, there was a reduction in pain intensity in both the groups and the reduction was more significant in the combination group (p <0.001). Adverse effects reported in both the groups were found to be comparable.Conclusions: Combination of aceclofenac and thiocolchicoside is superior to aceclofenac alone in patients with acute low back pain.

5.
Rev. cuba. farm ; 49(2)abr.-jun. 2015. ilus, tab
Article in Spanish | LILACS, CUMED | ID: lil-776404

ABSTRACT

Objetivo: determinar la eficacia y la tolerabilidad de la combinación a dosis fija, en una sola tableta, de tiocolchicósido 4 mg más diclofenaco potásico 50 mg en la reducción de la contractura muscular aguda estriada dolorosa comparado contra placebo y el uso de paracetamol tabletas de 500 mg como medicación de rescate. Métodos: fueron reclutados 97 pacientes de 2 ciudades ecuatorianas, Quito y Guayaquil, en tres centros de investigación, públicos y privados, con cervicalgia, dorsalgia y lumbalgia, principalmente de causa funcional. Los pacientes fueron asignados al azar en dos grupos: 1) grupo medicación activa, tiocolchicósido más diclofenaco potásico, 50 pacientes, 2) grupo placebo 47 pacientes. La eficacia en ambos grupos se evaluó por la reducción de la contractura muscular apreciada por inspección, palpación y reducción del dolor medido por una escala visual análoga, después de 5 días de tratamiento. Resultados: la evolución del grado de contractura muscular en el grupo medicación activa por evaluación visual pasó de un 100 por ciento con contractura visible con o sin actividad antiálgica fija a 96 por ciento sin signos visibles de contractura; de un 82 por ciento de contractura moderada a severa con o sin dolor evocado por palpación a un 74 por ciento de contractura leve sin dolor y 26 por ciento de ausencia de contractura. El promedio de dolor según la escala visual análoga disminuyó de 6,66 cm antes del tratamiento a 0,86 cm al finalizar el quinto día de tratamiento. Los efectos adversos fueron leves en el grupo tratado. Conclusiones: la combinación fija de tiocolchicósido 4 mg más diclofenaco potásico 50 mg en una sola tableta, administrado dos veces al día, es eficaz en el manejo de la contractura muscular aguda dolorosa de diversa etiología de manera estadísticamente significativa, bien tolerada y no altera el rendimiento psicomotor(AU)


Objective: to determine the efficacy and tolerability of a combination at a set dose in a single tablet of thiocolchicoside 4 mg plus potassium diclofenac 50 mg in the reduction of painful acute muscle spasm compared with the placebo and the use of 500 mg paracetamol as rescue medication. Methods: ninety seven patients from two Ecuador cities, named Quito and Guayaquil, were recruited in three research centers, both public and private. They suffered cervical pain, low back pain and dorsal pain, mainly of functional cause. The patients were randomly assigned in two groups 1) active medication group with 50 patients treated with thiocolchicoside plus potassium diclofenac and 2) placebo group with 47 patients. The efficacy of both groups was evaluated by the reduction of muscle spams observed in checking, palpation and pain reduction measured in an analogue visual scale after 5 days of treatment. Results: the progress of the muscle spasm degree in the active medication group according to visual evaluation went from 100 percent with visible spasm with or without fixed antialgic activity to 96 percent with no visible signs of spasm; from 82 percent of moderate spasm to severe with or without evoked pain by palpation to 74 percent of mild spasm without pain and 26 percent of spasm-free muscle. The pain average according to the visual scale decreased from 6.66 cm before treatment to 0,86 cm after the 5th day. The adverse effects were mild in t he treated group. Conclusions: the fixed combination of thiocolchicoside 4mg plus potassium diclofenac 50 mg in a single tablet, administered two times a day is efficacious in the painful acute muscle spasm of diverse etiology in a statistically significant way, well-tolerated and with no alteration of the psychomotor performance(AU)


Subject(s)
Humans , Diclofenac/therapeutic use , Low Back Pain/drug therapy , Neck Pain/drug therapy , Acetaminophen/therapeutic use , Muscle Contraction , Multicenter Study , Ecuador
6.
Article in English | IMSEAR | ID: sea-153102

ABSTRACT

A stability indicating RP-UPLC method was developed and validated for the simultaneous determination of Thiocolchicoside (TCC) and Aceclofenac (ACF) in tablet dosage form. The chromatographic separation was carried out by Thermo Scientific UPLC Instrument, Accela 1250 Pump, auto sampler with PDA detector, using column Thermo Scientific hypersil gold C18, (50 x 2.1mm) particle size 1.9μm using 5% ammonium acetate buffer and methanol in the ratio of 40:60, pH was adjusted to 5 with ortho phosphoric acid as mobile phase at a flow rate of 250 μl/min with the detection at 276nm. The run times of the TCC and ACF were about 0.697 and 1.125 minutes, respectively. The detector response is linear from 4.8 μg/ml to 7.2 μg/ml and 63.8 μg/ml to 96 μg/ml concentrations for TCC and ACF respectively. The linear regression equation was found to be y = 20620x-677.68 (r2 = 0.9996) for TCC and y= 50931x-319.3 (r2 = 0.9997) for ACF. The detection limit and quantification limit was 0.076μg and 0.23μg for TCC and 0.27μg and 0.71μg for ACF. The percentage of assay of TCC and ACF were about 99.50% and 99.96% respectively. The stability indicating capability was established by forced degradation experiments. The method was satisfactorily validated as per the ICH guidelines.

7.
Article in English | IMSEAR | ID: sea-167977

ABSTRACT

A stability indicating RP-UPLC method was developed and validated for the simultaneous determination of Thiocolchicoside (TCC) and Aceclofenac (ACF) in tablet dosage form. The chromatographic separation was carried out by Thermo Scientific UPLC Instrument, Accela 1250 Pump, auto sampler with PDA detector, using column Thermo Scientific hypersil gold C18, (50 x 2.1mm) particle size 1.9μm using 5% ammonium acetate buffer and methanol in the ratio of 40:60, pH was adjusted to 5 with ortho phosphoric acid as mobile phase at a flow rate of 250 μl/min with the detection at 276nm. The run times of the TCC and ACF were about 0.697 and 1.125 minutes, respectively. The detector response is linear from 4.8 μg/ml to 7.2 μg/ml and 63.8 μg/ml to 96 μg/ml concentrations for TCC and ACF respectively. The linear regression equation was found to be y = 20620x-677.68 (r2 = 0.9996) for TCC and y= 50931x-319.3 (r2 = 0.9997) for ACF. The detection limit and quantification limit was 0.076μg and 0.23μg for TCC and 0.27μg and 0.71μg for ACF. The percentage of assay of TCC and ACF were about 99.50% and 99.96% respectively. The stability indicating capability was established by forced degradation experiments. The method was satisfactorily validated as per the ICH guidelines.

8.
Article in English | IMSEAR | ID: sea-151698

ABSTRACT

The objective of this study was to evaluate the utility of derivative spectrophotometric method for analysis of Diclofenac sodium (DIC) and Thiocolchicoside (THIO) in combination. Derivative spectrophotometry has allowed specific determination of Diclofenac sodium at 249 nm with negligible contribution by Thiocolchicoside. Similarly, Thiocolchicoside was determined at 246nm with negligible interference by Diclofenac sodium. The described method obeyed Beer’s law in the range of and 4-36μg/ml for DIC 2-10μg/ml for THIO. Validation parameters such as linearity, accuracy, precision, specificity, and LOD and LOQ values were performed. The percentage recovery was 99.52% for DIC and 99.32% for THIO. Intra and Interday precision %RSD values were <2. Thus from the results obtained it can be concluded that proposed method is simple, rapid and specific.

9.
Asian Spine Journal ; : 115-122, 2012.
Article in English | WPRIM | ID: wpr-92980

ABSTRACT

STUDY DESIGN: We performed a multicentric, randomized, comparative clinical trial. Eligible patients were randomly assigned to receive 150 mg of Tolperisone thrice daily or 8 mg of Thiocolchicoside twice daily for 7 days. PURPOSE: To assess the efficacy and tolerability of Tolperisone in comparison with Thiocolchicoside in the treatment of acute low back pain with spasm of spinal muscles. OVERVIEW OF LITERATURE: No head on clinical trial of Tolperisone with Thiocolchicoside is available and so this study is done. METHODS: The assessment of muscle spasm was made by measuring the finger-to-floor distance (FFD), articular excursion in degrees on performing Lasegue's maneuver and modified Schober's test. Assessment of pain on movement and spontaneous pain (pain at rest) of the lumbar spine was made with the help of visual analogue scale score. RESULTS: The improvement in articular excursion on Lasegue's maneuver was significantly greater on day 3 (p = 0.017) and day 7 (p = 0.0001) with Tolperisone as compared to Thiocolchicoside. The reduction in FFD score was greater on day 7 (p = 0.0001) with Tolperisone. However there was no significant difference in improvement in Schober's test score on day 3 (p = 0.664) and day 7 (p = 0.192). The improvement in pain score at rest and on movement was significantly greater with Tolperisone (p = 0.0001). CONCLUSIONS: Tolperisone is an effective and well tolerated option for treatment of patients with skeletal muscle spasm associated with pain.


Subject(s)
Humans , Colchicine , Head , Low Back Pain , Muscle Spasticity , Muscle, Skeletal , Muscles , Spasm , Spine , Tolperisone
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