The Experts below are selected from a list of 444 Experts worldwide ranked by ideXlab platform
Andrea Pecori - One of the best experts on this subject based on the ideXlab platform.
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Efficacy and tolerability of eperisone and baclofen in spastic palsy: a double-blind randomized trial.
Advances in therapy, 2009Co-Authors: Nereo Bresolin, Claudio Zucca, Andrea PecoriAbstract:Introduction Few trials have compared different Central Muscle Relaxants in the treatment of spastic palsy. This head-to-head phase 3 trial compares oral eperisone, a Central Muscle Relaxant with a promising activity in spasticity therapy, and oral baclofen.
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Efficacy and tolerability of eperisone and baclofen in spastic palsy: A double-blind randomized trial
Advances in Therapy, 2009Co-Authors: Nereo Bresolin, Claudio Zucca, Andrea PecoriAbstract:INTRODUCTION: Few trials have compared different Central Muscle Relaxants in the treatment of spastic palsy. This head-to-head phase 3 trial compares oral eperisone, a Central Muscle Relaxant with a promising activity in spasticity therapy, and oral baclofen. METHODS: Patients (>18 years) with moderate to severe spastic palsy were eligible in this double-blind, randomized study; they received eperisone 300 mg/ day or baclofen 60 mg/day for 6 weeks. The efficacy evaluations included: functional analysis (Pedersen's scale, muscular tone, joint range of motion, 10-meter walking time); physiological and pathological reflexes; and electromyography (Hmax/Mmax amplitude ratio and the Wartenberg test). Physicians and patients globally assessed treatment efficacy. RESULTS: Both eperisone (n=40) and baclofen (n=40) significantly improved functionality of lower limbs versus baseline (eperisone: -9.1%, P
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Efficacy and tolerability of eperisone and baclofen in spastic palsy: a double-blind randomized trial
'Springer Science and Business Media LLC', 2009Co-Authors: Nereo Bresolin, Claudio Zucca, Andrea PecoriAbstract:Introduction: Few trials have compared different Central Muscle Relaxants in the treatment of spastic palsy. This head-to-head phase 3 trial compares oral eperisone, a Central Muscle Relaxant with a promising activity in spasticity therapy, and oral baclofen. Methods: Patients (>18 years) with moderate to severe spastic palsy were eligible in this double-blind, randomized study; they received eperisone 300 mg/ day or baclofen 60 mg/day for 6 weeks. The efficacy evaluations included: functional analysis (Pedersen's scale, muscular tone, joint range of motion, 10-meter walking time); physiological and pathological reflexes; and electromyography (Hmax/Mmax amplitude ratio and the Wartenberg test). Physicians and patients globally assessed treatment efficacy. Results: Both eperisone (n=40) and baclofen (n=40) significantly improved functionality of lower limbs versus baseline (eperisone: -9.1%, P
Nereo Bresolin - One of the best experts on this subject based on the ideXlab platform.
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Efficacy and tolerability of eperisone and baclofen in spastic palsy: a double-blind randomized trial.
Advances in therapy, 2009Co-Authors: Nereo Bresolin, Claudio Zucca, Andrea PecoriAbstract:Introduction Few trials have compared different Central Muscle Relaxants in the treatment of spastic palsy. This head-to-head phase 3 trial compares oral eperisone, a Central Muscle Relaxant with a promising activity in spasticity therapy, and oral baclofen.
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Efficacy and tolerability of eperisone and baclofen in spastic palsy: A double-blind randomized trial
Advances in Therapy, 2009Co-Authors: Nereo Bresolin, Claudio Zucca, Andrea PecoriAbstract:INTRODUCTION: Few trials have compared different Central Muscle Relaxants in the treatment of spastic palsy. This head-to-head phase 3 trial compares oral eperisone, a Central Muscle Relaxant with a promising activity in spasticity therapy, and oral baclofen. METHODS: Patients (>18 years) with moderate to severe spastic palsy were eligible in this double-blind, randomized study; they received eperisone 300 mg/ day or baclofen 60 mg/day for 6 weeks. The efficacy evaluations included: functional analysis (Pedersen's scale, muscular tone, joint range of motion, 10-meter walking time); physiological and pathological reflexes; and electromyography (Hmax/Mmax amplitude ratio and the Wartenberg test). Physicians and patients globally assessed treatment efficacy. RESULTS: Both eperisone (n=40) and baclofen (n=40) significantly improved functionality of lower limbs versus baseline (eperisone: -9.1%, P
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Efficacy and tolerability of eperisone and baclofen in spastic palsy: a double-blind randomized trial
'Springer Science and Business Media LLC', 2009Co-Authors: Nereo Bresolin, Claudio Zucca, Andrea PecoriAbstract:Introduction: Few trials have compared different Central Muscle Relaxants in the treatment of spastic palsy. This head-to-head phase 3 trial compares oral eperisone, a Central Muscle Relaxant with a promising activity in spasticity therapy, and oral baclofen. Methods: Patients (>18 years) with moderate to severe spastic palsy were eligible in this double-blind, randomized study; they received eperisone 300 mg/ day or baclofen 60 mg/day for 6 weeks. The efficacy evaluations included: functional analysis (Pedersen's scale, muscular tone, joint range of motion, 10-meter walking time); physiological and pathological reflexes; and electromyography (Hmax/Mmax amplitude ratio and the Wartenberg test). Physicians and patients globally assessed treatment efficacy. Results: Both eperisone (n=40) and baclofen (n=40) significantly improved functionality of lower limbs versus baseline (eperisone: -9.1%, P
Claudio Zucca - One of the best experts on this subject based on the ideXlab platform.
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Efficacy and tolerability of eperisone and baclofen in spastic palsy: a double-blind randomized trial.
Advances in therapy, 2009Co-Authors: Nereo Bresolin, Claudio Zucca, Andrea PecoriAbstract:Introduction Few trials have compared different Central Muscle Relaxants in the treatment of spastic palsy. This head-to-head phase 3 trial compares oral eperisone, a Central Muscle Relaxant with a promising activity in spasticity therapy, and oral baclofen.
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Efficacy and tolerability of eperisone and baclofen in spastic palsy: A double-blind randomized trial
Advances in Therapy, 2009Co-Authors: Nereo Bresolin, Claudio Zucca, Andrea PecoriAbstract:INTRODUCTION: Few trials have compared different Central Muscle Relaxants in the treatment of spastic palsy. This head-to-head phase 3 trial compares oral eperisone, a Central Muscle Relaxant with a promising activity in spasticity therapy, and oral baclofen. METHODS: Patients (>18 years) with moderate to severe spastic palsy were eligible in this double-blind, randomized study; they received eperisone 300 mg/ day or baclofen 60 mg/day for 6 weeks. The efficacy evaluations included: functional analysis (Pedersen's scale, muscular tone, joint range of motion, 10-meter walking time); physiological and pathological reflexes; and electromyography (Hmax/Mmax amplitude ratio and the Wartenberg test). Physicians and patients globally assessed treatment efficacy. RESULTS: Both eperisone (n=40) and baclofen (n=40) significantly improved functionality of lower limbs versus baseline (eperisone: -9.1%, P
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Efficacy and tolerability of eperisone and baclofen in spastic palsy: a double-blind randomized trial
'Springer Science and Business Media LLC', 2009Co-Authors: Nereo Bresolin, Claudio Zucca, Andrea PecoriAbstract:Introduction: Few trials have compared different Central Muscle Relaxants in the treatment of spastic palsy. This head-to-head phase 3 trial compares oral eperisone, a Central Muscle Relaxant with a promising activity in spasticity therapy, and oral baclofen. Methods: Patients (>18 years) with moderate to severe spastic palsy were eligible in this double-blind, randomized study; they received eperisone 300 mg/ day or baclofen 60 mg/day for 6 weeks. The efficacy evaluations included: functional analysis (Pedersen's scale, muscular tone, joint range of motion, 10-meter walking time); physiological and pathological reflexes; and electromyography (Hmax/Mmax amplitude ratio and the Wartenberg test). Physicians and patients globally assessed treatment efficacy. Results: Both eperisone (n=40) and baclofen (n=40) significantly improved functionality of lower limbs versus baseline (eperisone: -9.1%, P
Istvan Tarnawa - One of the best experts on this subject based on the ideXlab platform.
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Concerted action of antiepileptic and antidepressant agents to depress spinal neurotransmission: Possible use in the therapy of spasticity and chronic pain.
Neurochemistry international, 2007Co-Authors: Márta Thán, Zsolt Szombathelyi, László Fodor, Pál Kocsis, Károly Tihanyi, Bence Farkas, Gyula Kovács, Ágnes Kis-varga, Istvan TarnawaAbstract:Abstract Chronic pain states and epilepsies are common therapeutic targets of voltage-gated sodium channel blockers. Inhibition of sodium channels results in Central Muscle Relaxant activity as well. Selective serotonin reuptake inhibitors are also applied in the treatment of pain syndromes. Here, we investigate the pharmacodynamic interaction between these two types of drugs on spinal neurotransmission in vitro and in vivo . Furthermore, the ability of serotonin reuptake inhibitors to modulate the anticonvulsant and windup inhibitory actions and motor side effect of the sodium channel blocker lamotrigine was investigated. In the hemisected spinal cord model, we found that serotonin reuptake inhibitors increased the reflex inhibitory action of sodium channel blockers. The interaction was clearly more than additive. The potentiation was prevented by blocking 5-HT 2 receptors and PKC, and mimicked by activation of these targets by selective pharmacological tools, suggesting the involvement of 5-HT 2 receptors and PKC in the modulation of sodium channel function. The increase of sodium current blocking potency of lamotrigine by PKC activation was also demonstrated at cellular level, using the whole-cell patch clamp method. Similar synergism was found in vivo , in spinal reflex, windup, and maximal electroshock seizure models, but not in the rotarod test, which indicate enhanced Muscle Relaxant, anticonvulsant and analgesic activities with improved side effect profile. Our findings are in agreement with clinical observations suggesting that sodium channel blocking drugs, such as lamotrigine, can be advantageously combined with selective serotonin reuptake inhibitors in some therapeutic fields, and may help to understand the molecular mechanisms underlying the interaction.
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Simple pharmacological test battery to assess efficacy and side effect profile of Centrally acting Muscle Relaxant drugs.
Journal of pharmacological and toxicological methods, 2005Co-Authors: Sandor Farkas, Pál Kocsis, Pal Berzsenyi, Egon Kárpáti, Istvan TarnawaAbstract:Abstract Introduction: Centrally Muscle Relaxants (CMRs) are used mainly for treating Muscle spasticities of neurological origin, and painful Muscle spasms due to rheumatologic conditions. Their use is frequently associated with dose-limiting adverse effects. New drugs with improved side-effect characteristics are badly needed. However, there is no general agreement in the pharmacological literature on what methods are adequate to assess CMR effect and side effects in behaving rodents, which may hinder the development of new drugs. Here we report on the establishment of a simple pharmacological test battery, which was used to compare efficacies and side effect profiles of 11 compounds with Central Muscle Relaxant action, in mice (intraperitoneal application). Methods: For measuring Muscle Relaxant activity, (1) a new tremor model (GYKI 20039-induced tremor) and (2) the morphine-induced Straub-tail assay were used. The former, newly developed method has advantages over harmaline- or LON-954-induced tremor. For detecting side effect liability (ataxia, sedation, impairment of voluntary motor functions), (1) the rota-rod test, (2) measurement of spontaneous motility, (3) the weight-lifting test and (4) the thiopental sleep test were used. Results: Among the 11 Muscle Relaxant compounds tested (tolperisone, eperisone, silperisone, diazepam, baclofen, tizanidine, afloqualon, mephenesin, zoxazolamine, memantine and carisoprodol), the calculated safety ratios (i.e. ID 50 for side effect/ID 50 for Muscle Relaxant effect) varied in a wide range. Silperisone seems to have the most advantageous profile (safety ratios range between 1.7 and 3.3 in the different pairs of assays) compared to the other tested drugs with lower (one or more ratios below 1.5, and often far below 1) and more varying ratios. Discussion: Therapeutic indices calculated from the results of these in vivo experiments for the clinically used Muscle Relaxants are in agreement with their adverse effect profiles in humans. Thus the present test battery seems to be suitable for predicting the possible clinical utility of newly synthesized compounds.
Sandor Farkas - One of the best experts on this subject based on the ideXlab platform.
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Simple pharmacological test battery to assess efficacy and side effect profile of Centrally acting Muscle Relaxant drugs.
Journal of pharmacological and toxicological methods, 2005Co-Authors: Sandor Farkas, Pál Kocsis, Pal Berzsenyi, Egon Kárpáti, Istvan TarnawaAbstract:Abstract Introduction: Centrally Muscle Relaxants (CMRs) are used mainly for treating Muscle spasticities of neurological origin, and painful Muscle spasms due to rheumatologic conditions. Their use is frequently associated with dose-limiting adverse effects. New drugs with improved side-effect characteristics are badly needed. However, there is no general agreement in the pharmacological literature on what methods are adequate to assess CMR effect and side effects in behaving rodents, which may hinder the development of new drugs. Here we report on the establishment of a simple pharmacological test battery, which was used to compare efficacies and side effect profiles of 11 compounds with Central Muscle Relaxant action, in mice (intraperitoneal application). Methods: For measuring Muscle Relaxant activity, (1) a new tremor model (GYKI 20039-induced tremor) and (2) the morphine-induced Straub-tail assay were used. The former, newly developed method has advantages over harmaline- or LON-954-induced tremor. For detecting side effect liability (ataxia, sedation, impairment of voluntary motor functions), (1) the rota-rod test, (2) measurement of spontaneous motility, (3) the weight-lifting test and (4) the thiopental sleep test were used. Results: Among the 11 Muscle Relaxant compounds tested (tolperisone, eperisone, silperisone, diazepam, baclofen, tizanidine, afloqualon, mephenesin, zoxazolamine, memantine and carisoprodol), the calculated safety ratios (i.e. ID 50 for side effect/ID 50 for Muscle Relaxant effect) varied in a wide range. Silperisone seems to have the most advantageous profile (safety ratios range between 1.7 and 3.3 in the different pairs of assays) compared to the other tested drugs with lower (one or more ratios below 1.5, and often far below 1) and more varying ratios. Discussion: Therapeutic indices calculated from the results of these in vivo experiments for the clinically used Muscle Relaxants are in agreement with their adverse effect profiles in humans. Thus the present test battery seems to be suitable for predicting the possible clinical utility of newly synthesized compounds.
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Tolperisone-Type Drugs Inhibit Spinal Reflexes via Blockade of Voltage-Gated Sodium and Calcium Channels
Journal of Pharmacology and Experimental Therapeutics, 2005Co-Authors: Pál Kocsis, Norbert Bielik, Márta Thán, Sándor Kolok, Anikó Gere, László Fodor, Sandor Farkas, Mónika CsejteiAbstract:The spinal reflex depressant mechanism of tolperisone and some of its structural analogs with Central Muscle Relaxant action was investigated. Tolperisone (50–400 μM), eperisone, lanperisone, inaperisone, and silperisone (25–200 μM) dose dependently depressed the ventral root potential of isolated hemisected spinal cord of 6-day-old rats. The local anesthetic lidocaine (100–800 μM) produced qualitatively similar depression of spinal functions in the hemicord preparation, whereas its blocking effect on afferent nerve conduction was clearly stronger. In vivo, tolperisone and silperisone as well as lidocaine (10 mg/kg intravenously) depressed ventral root reflexes and excitability of motoneurons. However, in contrast with lidocaine, the Muscle Relaxant drugs seemed to have a more pronounced action on the synaptic responses than on the excitability of motoneurons. Whole-cell measurements in dorsal root ganglion cells revealed that tolperisone and silperisone depressed voltage-gated sodium channel conductance at concentrations that inhibited spinal reflexes. Results obtained with tolperisone and its analogs in the [H]batrachotoxinin A 20-α-benzoate binding in cortical neurons and in a fluorimetric membrane potential assay in cerebellar neurons further supported the view that blockade of sodium channels may be a major component of the action of tolperisone-type Centrally acting Muscle Relaxant drugs. Furthermore, tolperisone, eperisone, and especially silperisone had a marked effect on voltagegated calcium channels, whereas calcium currents were hardly influenced by lidocaine. These data suggest that tolperisone-type Muscle Relaxants exert their spinal reflex inhibitory action predominantly via a presynaptic inhibition of the transmitter release from the primary afferent endings via a combined action on voltage-gated sodium and calcium channels.
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[Mydeton: a Centrally acting Muscle Relaxant drug from Gedeon Richter LTD.]
Acta Pharmaceutica Hungarica, 2002Co-Authors: Pál Kocsis, Gyula Kovács, Zsolt Szombathelyi, Sandor FarkasAbstract:Since its introduction in 1959 tolperisone hydrochloride (Mydeton) is still one of the leading products of Gedeon Richter Ltd. It has been successfully applied for treating different painful Muscle spasms. The compound is successfully marketed also by several foreign, mostly Japanese, pharmaceutical companies, as a Central Muscle Relaxant agent. The present summary overviews the pharmacology of tolperisone, with special emphasize on its still partly understood way of action. Data from the scientific literature as well as our own experimental results strongly support the hypothesis that inhibition of voltage gated sodium channels is a major component of the mechanism of action of tolperisone. The paper also summarizes the clinical results with tolperisone and the perspectives of the therapeutic use of Centrally acting Muscle Relaxants.