The Experts below are selected from a list of 360 Experts worldwide ranked by ideXlab platform
Gunnur Basar - One of the best experts on this subject based on the ideXlab platform.
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multicenter randomized double blinded placebo controlled trial of Thiocolchicoside in acute low back pain
Joint Bone Spine, 2003Co-Authors: Fikret Tuzun, Halil Unalan, Nazan Oner, Hayri Ozguzel, Yesim Kirazli, Afitap Icagasioglu, Banu Kuran, Sansin Tuzun, Gunnur BasarAbstract:Abstract Objective. – To evaluate the efficacy of intramuscular injection of Thiocolchicoside (4 mg-2 ml) compared to placebo administered twice daily for 5 days in patients suffering from acute low back pain. Patients and methods. – Multicenter, randomized, double-blinded, placebo-controlled trial. The study was conducted between July 1998 and March 2000 in five centers. Hospitalized patients with acute low back pain were included. The primary evaluation criterion was spontaneous pain at rest assessed by visual analog scale (VAS). Hand-to-floor distance, muscle spasm intensity, patients’ global evaluation and analgesic tablet (paracetamol) consumption were used as secondary evaluation criteria. Results. – One hundred and forty nine patients were included. Both groups showed improvement on spontaneous pain assessed by VAS at the end of day 1; however, improvement was statistically significant in Thiocolchicoside group on day 3 (P Conclusion. – Twice daily administration of 4 mg Thiocolchicoside for 5 days provides an efficient and safe treatment for patients with acute low back pain accompanied by muscle spasm.
Giuseppe Caggiano - One of the best experts on this subject based on the ideXlab platform.
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efficacy and safety of a fixed combination of intramuscular diclofenac 75 mg Thiocolchicoside 4 mg in the treatment of acute low back pain a phase iii randomized double blind controlled trial
European Journal of Physical and Rehabilitation Medicine, 2018Co-Authors: Egidio Sproviero, Emilio Albamonte, Cosimo Costantino, Attilio Giossi, Maurizio Mancuso, Alberto Rigamonti, Paolo Tornari, Giuseppe CaggianoAbstract:BACKGROUND The management of acute low back pain (LBP) is directed to obtain early and maximum relief of the local and regional pain, and to improve mobility and physical function. AIM To evaluate the effects of a 4 mL-volume diclofenac 75mg/Thiocolchicoside 4mg fixed dose combination (FDC) for intramuscular (IM) injection (test) compared to the separate injection of the two components (reference). DESIGN Phase III, randomized, controlled, double-blind (blind-observer), parallel-group. SETTING Twenty-two General Practitioners in Italy. POPULATION Adult outpatients with acute moderate-severe LBP at rest (≥50 mm at VAS) and stable muscle contracture (increase <5 cm in the distance between the two fingers of the examiner in the Schober test). METHODS Eligible patients were randomized to the test (N.=111) or reference (N.=112) treatment, both given IM once daily for 5 days. The primary efficacy endpoint of the study was the change from baseline in pain VAS score (0-100 mm) measured at rest 96±2 hours (day 5) from the start of treatment, one hour after the last injection. RESULTS Pain VAS Score markedly improved in both groups and the test was non-inferior to the reference in primary endpoint, i.e. the upper bound of the 95% confidence interval of the adjusted difference was lower than the pre-specified limit of 4 mm. There were no statistically significant differences between groups for improvements of pain measured at all time points before and one hour after injection, time to resolution of pain, improvements from baseline of muscle contracture, and time to first resolution of muscle contracture. Approximately 20% of patients in the two groups used rescue paracetamol for pain relief. Both the test and the reference treatment were well tolerated in terms of adverse effects, laboratory parameters and vital signs. CONCLUSIONS A 5-day treatment with IM diclofenac+Thiocolchicoside FDC in a 4-mL volume was as effective and well tolerated as the separate injection of the two components in improving pain symptoms in patients with acute moderate-severe LBP. CLINICAL REHABILITATION IMPACT The new diclofenac+Thiocolchicoside FDC formulation may allow treating effectively acute LBP while reducing the number of injections and hence the risk of local adverse reactions, and improving the patient's compliance.
Flaminio Cattabeni - One of the best experts on this subject based on the ideXlab platform.
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autoradiographic localization of 3h Thiocolchicoside binding sites in the rat brain and spinal cord
Neuropharmacology, 2001Co-Authors: Walter Balduini, Valerio De Angelis, Erika Mazzoni, Henri Depoortere, Flaminio Cattabeni, Mauro CiminoAbstract:Abstract Thiocolchicoside is used in humans as a myorelaxant drug with anti-inflammatory and analgesic activity. Recently we established the experimental conditions that allowed the identification of [ 3 H ] Thiocolchicoside binding sites in synaptic membranes of rat spinal cord and cerebral cortex. The pharmacological characterization of these sites indicated that GABA and several of its agonists and antagonists, as well as strychnine, were able to interact with [ 3 H ] Thiocolchicoside binding in a dose-dependent manner and with different affinities. In order to gain more insight into the nature and the anatomical distribution of the binding sites labeled by [ 3 H ] Thiocolchicoside, in the present study we examined the localization of these sites on parasagittal and coronal sections of the rat brain and spinal cord, respectively, using receptor autoradiography. In the spinal cord an intense signal was observed in the gray matter, with the highest density occurring in the superficial layers of the dorsal horns. Strychnine completely displaced [ 3 H ] Thiocolchicoside binding, whereas GABA only partially removed the radioligand from its binding sites. In the brain, specific binding occurred in several areas and was displaced by both GABA and strychnine. The distribution of [ 3 H ] Thiocolchicoside binding sites in brain sections, however, did not match that found for [ 3 H ] muscimol. Furthermore, cold Thiocolchicoside was not able to completely displace [ 3 H ] muscimol binding, and showed a different efficacy in the various areas labeled by the radioligand. We conclude that Thiocolchicoside may interact with a subpopulation of GABAA receptors having low-affinity binding sites for GABA. Furthermore, the observed sensitivity to strychnine in the spinal cord indicates an interaction also with strychnine-sensitive glycine receptors, suggesting that the pharmacological effects of Thiocolchicoside may be the result of its interaction with different receptor populations.
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characterization of 3h Thiocolchicoside binding sites in rat spinal cord and cerebral cortex
European Journal of Pharmacology, 1999Co-Authors: Walter Balduini, Henri Depoortere, Mauro Cimino, Flaminio CattabeniAbstract:Thiocolchicoside, a semi-synthetic derivative of the naturally occurring compound colchicoside with a relaxant effect on skeletal muscle, has been found to displace both [3H]gamma-aminobutyric acid ([3H]GABA) and [3H]strychnine binding, suggesting an interaction with both GABA and strychnine-sensitive glycine receptors. In order to gain further insight into the interaction of Thiocolchicoside with these receptors, the binding of [3H]Thiocolchicoside in rat spinal cord-brainstem and cortical synaptic membranes was characterized. [3H]Thiocolchicoside binding was saturable in both tissues examined. In spinal cord-brainstem membranes, we found a K(D) of 254 +/- 47 nM and a Bmax of 2.39 +/- 0.36 pmol/mg protein, whereas in cortical membranes, a K(D) of 176 nM and a Bmax of 4.20 pmol/mg protein was observed. A similar K(D) value was found in kinetic experiments performed in spinal cord-brainstem membranes. Heterologous displacement experiments showed that GABA and strychnine displaced the binding in a dose-dependent manner, whereas glycine was ineffective. [3H]Thiocolchicoside binding was also displaced by several GABA(A) receptor agonists and antagonists, but not by baclofen, flunitrazepam, guvacine, picrotoxin or by other drugs unrelated to GABA transmission. In spinal cord-brainstem, and to a lower extent, in cortical membranes, GABA and its analogs were not able to completely displace [3H]Thiocolchicoside specific binding indicating that, besides GABA(A) receptors, Thiocolchicoside can bind to another unidentified site. Unlabelled Thiocolchicoside, however, completely displaced [3H]muscimol binding both in cortical and in spinal cord-brainstem synaptic membranes with an IC50 in the low microM range. Neurosteroids were found to modulate the binding in cortical but not in spinal cord-brainstem synaptic membranes. We conclude that [3H]Thiocolchicoside binding shows a pharmacological profile indicating an interaction with the GABA(A) receptor. The different affinities for the GABA(A) receptor agonists and antagonists and sensitivity to neurosteroids obtained in the cerebral cortex and in the spinal cord may indicate a preferential interaction of the compound with a subtype of the GABA(A) receptor. The data also indicate that [3H]Thiocolchicoside binds to another site(s), whose nature remains to be elucidated.
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interaction of Thiocolchicoside with 3h strychnine binding sites in rat spinal cord and brainstem
European Journal of Pharmacology, 1996Co-Authors: Mauro Cimino, P Marini, Flaminio CattabeniAbstract:Radioreceptor binding assays and receptor autoradiography were used to investigate the activity of Thiocolchicoside on strychnine-sensitive binding sites in rat brain and spinal cord using [3H]strychnine as a ligand. Thiocolchicoside displaced the binding of [3H]strychnine with an affinity similar to that of unlabeled glycine, and showed a Hill coefficient and proportionality parameter (P) less than unity. The activity of Thiocolchicoside toward [3H]strychnine binding sites was confirmed in autoradiographic studies. The results suggest that Thiocolchicoside behaves as an allosteric compound acting on the strychnine-sensitive glycine receptor in rat brainstem and spinal cord, and that this may provide a possible mechanism for the myorelaxant activity of this colchicoside derivative, the first clinically useful drug acting on this receptor.
Fikret Tuzun - One of the best experts on this subject based on the ideXlab platform.
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multicenter randomized double blinded placebo controlled trial of Thiocolchicoside in acute low back pain
Joint Bone Spine, 2003Co-Authors: Fikret Tuzun, Halil Unalan, Nazan Oner, Hayri Ozguzel, Yesim Kirazli, Afitap Icagasioglu, Banu Kuran, Sansin Tuzun, Gunnur BasarAbstract:Abstract Objective. – To evaluate the efficacy of intramuscular injection of Thiocolchicoside (4 mg-2 ml) compared to placebo administered twice daily for 5 days in patients suffering from acute low back pain. Patients and methods. – Multicenter, randomized, double-blinded, placebo-controlled trial. The study was conducted between July 1998 and March 2000 in five centers. Hospitalized patients with acute low back pain were included. The primary evaluation criterion was spontaneous pain at rest assessed by visual analog scale (VAS). Hand-to-floor distance, muscle spasm intensity, patients’ global evaluation and analgesic tablet (paracetamol) consumption were used as secondary evaluation criteria. Results. – One hundred and forty nine patients were included. Both groups showed improvement on spontaneous pain assessed by VAS at the end of day 1; however, improvement was statistically significant in Thiocolchicoside group on day 3 (P Conclusion. – Twice daily administration of 4 mg Thiocolchicoside for 5 days provides an efficient and safe treatment for patients with acute low back pain accompanied by muscle spasm.
Mauro Cimino - One of the best experts on this subject based on the ideXlab platform.
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autoradiographic localization of 3h Thiocolchicoside binding sites in the rat brain and spinal cord
Neuropharmacology, 2001Co-Authors: Walter Balduini, Valerio De Angelis, Erika Mazzoni, Henri Depoortere, Flaminio Cattabeni, Mauro CiminoAbstract:Abstract Thiocolchicoside is used in humans as a myorelaxant drug with anti-inflammatory and analgesic activity. Recently we established the experimental conditions that allowed the identification of [ 3 H ] Thiocolchicoside binding sites in synaptic membranes of rat spinal cord and cerebral cortex. The pharmacological characterization of these sites indicated that GABA and several of its agonists and antagonists, as well as strychnine, were able to interact with [ 3 H ] Thiocolchicoside binding in a dose-dependent manner and with different affinities. In order to gain more insight into the nature and the anatomical distribution of the binding sites labeled by [ 3 H ] Thiocolchicoside, in the present study we examined the localization of these sites on parasagittal and coronal sections of the rat brain and spinal cord, respectively, using receptor autoradiography. In the spinal cord an intense signal was observed in the gray matter, with the highest density occurring in the superficial layers of the dorsal horns. Strychnine completely displaced [ 3 H ] Thiocolchicoside binding, whereas GABA only partially removed the radioligand from its binding sites. In the brain, specific binding occurred in several areas and was displaced by both GABA and strychnine. The distribution of [ 3 H ] Thiocolchicoside binding sites in brain sections, however, did not match that found for [ 3 H ] muscimol. Furthermore, cold Thiocolchicoside was not able to completely displace [ 3 H ] muscimol binding, and showed a different efficacy in the various areas labeled by the radioligand. We conclude that Thiocolchicoside may interact with a subpopulation of GABAA receptors having low-affinity binding sites for GABA. Furthermore, the observed sensitivity to strychnine in the spinal cord indicates an interaction also with strychnine-sensitive glycine receptors, suggesting that the pharmacological effects of Thiocolchicoside may be the result of its interaction with different receptor populations.
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characterization of 3h Thiocolchicoside binding sites in rat spinal cord and cerebral cortex
European Journal of Pharmacology, 1999Co-Authors: Walter Balduini, Henri Depoortere, Mauro Cimino, Flaminio CattabeniAbstract:Thiocolchicoside, a semi-synthetic derivative of the naturally occurring compound colchicoside with a relaxant effect on skeletal muscle, has been found to displace both [3H]gamma-aminobutyric acid ([3H]GABA) and [3H]strychnine binding, suggesting an interaction with both GABA and strychnine-sensitive glycine receptors. In order to gain further insight into the interaction of Thiocolchicoside with these receptors, the binding of [3H]Thiocolchicoside in rat spinal cord-brainstem and cortical synaptic membranes was characterized. [3H]Thiocolchicoside binding was saturable in both tissues examined. In spinal cord-brainstem membranes, we found a K(D) of 254 +/- 47 nM and a Bmax of 2.39 +/- 0.36 pmol/mg protein, whereas in cortical membranes, a K(D) of 176 nM and a Bmax of 4.20 pmol/mg protein was observed. A similar K(D) value was found in kinetic experiments performed in spinal cord-brainstem membranes. Heterologous displacement experiments showed that GABA and strychnine displaced the binding in a dose-dependent manner, whereas glycine was ineffective. [3H]Thiocolchicoside binding was also displaced by several GABA(A) receptor agonists and antagonists, but not by baclofen, flunitrazepam, guvacine, picrotoxin or by other drugs unrelated to GABA transmission. In spinal cord-brainstem, and to a lower extent, in cortical membranes, GABA and its analogs were not able to completely displace [3H]Thiocolchicoside specific binding indicating that, besides GABA(A) receptors, Thiocolchicoside can bind to another unidentified site. Unlabelled Thiocolchicoside, however, completely displaced [3H]muscimol binding both in cortical and in spinal cord-brainstem synaptic membranes with an IC50 in the low microM range. Neurosteroids were found to modulate the binding in cortical but not in spinal cord-brainstem synaptic membranes. We conclude that [3H]Thiocolchicoside binding shows a pharmacological profile indicating an interaction with the GABA(A) receptor. The different affinities for the GABA(A) receptor agonists and antagonists and sensitivity to neurosteroids obtained in the cerebral cortex and in the spinal cord may indicate a preferential interaction of the compound with a subtype of the GABA(A) receptor. The data also indicate that [3H]Thiocolchicoside binds to another site(s), whose nature remains to be elucidated.
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interaction of Thiocolchicoside with 3h strychnine binding sites in rat spinal cord and brainstem
European Journal of Pharmacology, 1996Co-Authors: Mauro Cimino, P Marini, Flaminio CattabeniAbstract:Radioreceptor binding assays and receptor autoradiography were used to investigate the activity of Thiocolchicoside on strychnine-sensitive binding sites in rat brain and spinal cord using [3H]strychnine as a ligand. Thiocolchicoside displaced the binding of [3H]strychnine with an affinity similar to that of unlabeled glycine, and showed a Hill coefficient and proportionality parameter (P) less than unity. The activity of Thiocolchicoside toward [3H]strychnine binding sites was confirmed in autoradiographic studies. The results suggest that Thiocolchicoside behaves as an allosteric compound acting on the strychnine-sensitive glycine receptor in rat brainstem and spinal cord, and that this may provide a possible mechanism for the myorelaxant activity of this colchicoside derivative, the first clinically useful drug acting on this receptor.
