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Serhan Sevim, Hakan Kaleağası, Bahar Taşdelen
BACKGROUND: Fatigue is the most frequent and often debilitating symptom for patients with multiple sclerosis (MS). There are no available effective therapies for fatigue associated with MS, and it is unclear whether a successful therapy of MS leads to clinical improvement. Sulbutiamine is a lipophilic compound that crosses the blood-brain barrier more readily than thiamine and increases the levels of thiamine and thiamine phosphate esters in the brain. Whereas several clinical trials have demonstrated the beneficial effects of sulbutiamine in patients with asthenia, there have been no reports on the effects of sulbutiamine on fatigue in patients with MS...
August 2017: Multiple Sclerosis and related Disorders
Nehal F Farid, Nada S Abdelwahab
Sulbutiamine (SUL) is an ester of thiazides with neurotropic action. A new stability indicating HPTLC method has been developed and validated for the determination of SUL in the presence of different degradation products. The drug was subjected to different stress conditions following ICH strategy such as hydrolytic degradation (neutral, alkaline and acidic hydrolysis), oxidation, photodegradation and dry heat degradation. The drug demonstrated degradation under all decomposition conditions except neutral hydrolysis and dry heat, where the drug was completely degraded with 0...
April 2016: Journal of Chromatographic Science
Aman Shah Abdul Majid, Zheng Qin Yin, Dan Ji
This study aimed to show if two different sulphur containing drugs sulbutiamine and acetylcysteine (NAC) could attenuate the effects of two different insults being serum deprivation and glutamate/buthionine sulfoximine (GB)-induced death to transformed retinal ganglion cell line (RGC-5) in culture. Cells were exposed to either 5 mM of GB for 24 h or serum deprivation for 48 h with inclusion of either NAC or sulbutiamine. Cell viability, microscopic evidence for apoptosis, caspase 3 activity, reactive oxygen species (ROS), glutathione (GSH), catalase and gluthathione-S-transferase (GST) were determined...
2013: Biological & Pharmaceutical Bulletin
K K Kiew, W B Wan Mohamad, A Ridzuan, M Mafauzy
Thirty patients with diabetic polyneuropathy were recruited from the diabetic clinic in Hospital Universiti Sains Malaysia from 1996 to 1998. They were randomly assigned either sulbutiamine (Arcalion(®)) (15 patients) or no treatment (control group; 15 patients). Glycaemic control was assessed by blood glucose and HbA1. Severity of neuropathy was assessed by symptom and sign score, and electrophysiological parameters (nerve conduction velocity and compound muscle action potential) at entry to the study and after 6 weeks...
January 2002: Malaysian Journal of Medical Sciences: MJMS
Jeehyun Kwag, Aman Shah Abdul Majid, Kui Dong Kang
Hippocampus is one of the earliest brain regions that gets affected by ischemia, however, no pharmacological therapy exists yet that can fully counteract the ischemic damage. Here we study the effect of sulbutiamine, a synthetic thiamine analogue that can cross the blood-brain barrier easily, on hippocampal neurons under an in vitro model of ischemia, oxygen-glucose deprivation (OGD). We find that exposure to OGD in the presence of sulbutiamine significantly increases neuronal viability and enhances electrophysiological properties such as excitatory synaptic transmissions and intrinsic neuronal membrane input resistance in a concentration-dependent manner...
2011: Biological & Pharmaceutical Bulletin
Tim Sobolevsky, Grigory Rodchenkov
Sulbutiamine (isobutyryl thiamine disulfide) is a lipophilic derivative of thiamine used for the treatment of asthenia and other related pathological conditions. It is available over-the-counter in several countries either as a component of nutritional supplements or as a pharmaceutical preparation. The presence of sulbutiamine in urinary doping control samples was monitored to evaluate the relevance of its use in sports. As one of the sulbutiamine metabolites has very close retention time and the same characteristic ion (m/z 194) as the main boldenone metabolite, the raw data files generated from the screening for anabolic steroids were automatically reprocessed to identify the samples containing sulbutiamine...
November 2010: Drug Testing and Analysis
Kui Dong Kang, Aman Shah Abdul Majid, Kyung-A Kim, Kyungsu Kang, Hong Ryul Ahn, Chu Won Nho, Sang Hoon Jung
Sulbutiamine is a highly lipid soluble synthetic analogue of vitamin B(1) and is used clinically for the treatment of asthenia. The aim of our study was to demonstrate whether sulbutiamine is able to attenuate trophic factor deprivation induced cell death to transformed retinal ganglion cells (RGC-5). Cells were subjected to serum deprivation for defined periods and sulbutiamine at different concentrations was added to the cultures. Various procedures (e.g. cell viability assays, apoptosis assay, reactive oxygen species analysis, Western blot analysis, flow cytometric analysis, glutathione (GSH) and glutathione-S-transferase (GST) measurement) were used to demonstrate the effect of sulbutiamine...
November 2010: Neurochemical Research
Marie-Laure Volvert, Sandrine Seyen, Marie Piette, Brigitte Evrard, Marjorie Gangolf, Jean-Christophe Plumier, Lucien Bettendorff
BACKGROUND: Lipid-soluble thiamine precursors have a much higher bioavailability than genuine thiamine and therefore are more suitable for therapeutic purposes. Benfotiamine (S-benzoylthiamine O-monophosphate), an amphiphilic S-acyl thiamine derivative, prevents the progression of diabetic complications, probably by increasing tissue levels of thiamine diphosphate and so enhancing transketolase activity. As the brain is particularly sensitive to thiamine deficiency, we wanted to test whether intracellular thiamine and thiamine phosphate levels are increased in the brain after oral benfotiamine administration...
2008: BMC Pharmacology
H Ollat, B Laurent, S Bakchine, B-F Michel, J Touchon, B Dubois
The efficacy of the inhibitors of acetylcholinesterase in Alzheimer's Disease (AD) is moderated and some patients do not respond to these treatments. Sulbutiamine potentializes cholinergic and glutamatergic transmissions, mainly in hippocampus and prefrontal cortex. This multicentric, randomized and double-blind trial evaluates the effects of the association of sulbutiamine to an anticholinesterasic drug in cognitive functions in patients with AD at an early stage (episodic memory, working memory, executive functions, attention)...
March 2007: L'Encéphale
Athanasios Douzenis, Ioannis Michopoulos, Lefteris Lykouras
A case of a patient with bipolar disorder with a history of hospitalizations and addiction to sulbutiamine is presented. Sulbutiamine is a precursor of thiamine that crosses the blood-brain barrier and is widely available without prescription in most countries or over the internet. Because of this patient's need to consume ever increasing quantities of sulbutiamine, his psychiatric care was severely compromised through him defaulting appointments and frequent changes of psychiatrists. This paper reviews the current scientific knowledge about sulbutiamine, and some of the information and claims available on the web about its use and potential...
2006: World Journal of Biological Psychiatry
Jean-Charles Bizot, Alexandre Herpin, Stéphanie Pothion, Sylvain Pirot, Fabrice Trovero, Hélène Ollat
The effect of a sulbutiamine chronic treatment on memory was studied in rats with a spatial delayed-non-match-to-sample (DNMTS) task in a radial maze and a two trial object recognition task. After completion of training in the DNMTS task, animals were subjected for 9 weeks to daily injections of either saline or sulbutiamine (12.5 or 25 mg/kg). Sulbutiamine did not modify memory in the DNMTS task but improved it in the object recognition task. Dizocilpine, impaired both acquisition and retention of the DNMTS task in the saline-treated group, but not in the two sulbutiamine-treated groups, suggesting that sulbutiamine may counteract the amnesia induced by a blockade of the N-methyl-D-aspartate glutamate receptors...
July 2005: Progress in Neuro-psychopharmacology & Biological Psychiatry
Siddharth N Shah
AIMS OF THE STUDY: Asthenic symptoms such as weakness accompany illness. This study investigates whether the centrally acting cholinergic agent, vitamin B analogue (sulbutiamine), is effective and acceptable in relieving these symptoms in infectious disease when combined with specific anti-infective treatment. METHODOLOGY: In a prospective uncontrolled, non-randomised, commercial, observational study, 1772 patients with an infectious disease and asthenic symptoms, drawn from the practice of 350 randomly selected physicians throughout India, received vitamin B analogue (sulbutiamine) in addition to specific anti-infective treatment for 15 days...
September 2003: Journal of the Association of Physicians of India
O Van Reeth
Asthenia is the most frequent medical reason for people seeking help from their physician. In 75% of cases, the cause is functional (either reactive or psychiatric) and in 25% it is organic. In order to provide patients with rapid relief of symptoms, appropriate antiasthenic treatment should be initiated immediately, while at the same time, adequate clinical and laboratory assessments should be performed to detect the underlying cause of asthenia. Sulbutiamine, a highly lipophilic thiamine derivative, is the only antiasthenic compound known to cross the blood-brain barrier and to be selectively active on specific brain structures directly involved in asthenia...
March 1999: Drugs of Today
F Trovero, M Gobbi, J Weil-Fuggaza, M J Besson, D Brochet, S Pirot
Chronic treatment of rats by sulbutiamine induced no change in density of N-methyl-D-aspartate (NMDA) and (+/-)-alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid receptors in the cingular cortex, but a significant decrease of the kainate binding sites, as measured by quantitative autoradiography. In the same treated animals, an increase of D1 dopaminergic (DA) binding sites was measured both in the prefrontal and the cingular cortex, while no modification of the D2 binding sites was detected. Furthermore, an acute sulbutiamine administration induced a decrease of kainate binding sites but no change of the density of D1 and D2 DA receptors...
September 29, 2000: Neuroscience Letters
H Lôo, M F Poirier, H Ollat, S Elatki
UNLABELLED: Psycho-behavioural inhibition is characteristic of major depressive disorder and frequently recedes after the other depressive symptoms. This may induce an important psychosocial impairment which could be a risk factor for relapse. METHODS: The aim of this eight weeks, multicentric, randomized, double blind, placebo controlled trial was to assess the efficacy and safety of sulbutiamine (Arcalion) [600 mg p.d.] on the symptoms of psycho-behavioural inhibition of inpatients with DSM III-R defined Major Depressive Episode (MDE) treated by adjusted doses of clomipramine [75 to 150 mg pd]...
March 2000: L'Encéphale
M A Ahmed, M M Elbeshlawy
Five novel polyvinyl chloride (PVC) matrix membrane sensors for the selective determination of sulbutiamine (SBA) cation are described. These sensors are based on molybdate, tetraphenylborate, reineckate, phosphotun gestate and phosphomolybdate, as possible ion-pairing agents. These sensors display rapid near-Nernstian stable response over a relatively wide concentration range 1x10(-2)-1x10(-6) M of sulbutiamine, with calibration slopes 28 32.6 mV decade(-1) over a reasonable pH range 2-6. The proposed sensors proved to have a good selectivity for SBA over some inorganic and organic cations...
November 1999: Journal of Pharmaceutical and Biomedical Analysis
K P Tiev, J Cabane, J C Imbert
PURPOSE: Chronic fatigue remains a medical mystery and a therapeutic failure. The subgroup of chronic fatigue postinfectious fatigue (CPIF) is an interesting one since it is quite frequent in general practice. METHODS: We studied sulbutiamine (Su), isobutyryl-thiamine disulfide in this context. We included 326 general-practice patients suffering from CPIF: they received randomly either Su, 400 mg daily (n = 106), or Su, 600 mg daily (n = 111), or placebo (n = 109) for 28 days in a double-blind, parallel-group study...
October 1999: La Revue de Médecine Interne
L Bettendorff
Thiamine transport in cultured neuroblastoma cells is mediated by a high-affinity carrier (KM = 40 nM). In contrast, the uptake of the more hydrophobic sulbutiamine (isobutyrylthiamine disulfide) is unsaturable and its initial transport rate is 20-times faster than for thiamine. In the cytoplasm, sulbutiamine is rapidly hydrolyzed and reduced to free thiamine, the overall process resulting in a rapid and concentrative thiamine accumulation. Incorporation of radioactivity from [14C]thiamine or [14C]sulbutiamine into intracellular thiamine diphosphate is slow in both cases...
May 26, 1994: Biochimica et Biophysica Acta
L Bettendorff, P Wins, M Lesourd
The subcellular distribution of thiamine derivatives in rat brain was studied. Thiamine diphosphate content was highest in the mitochondrial and synaptosomal fractions, and lowest in microsomal, myelin and cytosolic fractions. Only 3-5% of total thiamine diphosphate was bound to transketolase, a cytosolic enzyme. Thiamine triphosphate was barely detectable in the microsomal and cytosolic fraction, but synaptosomes were slightly enriched in this compound compared to the crude homogenate. Both myelin and mitochondrial fractions contained significant amounts of thiamine triphosphate...
May 26, 1994: Biochimica et Biophysica Acta
L Bettendorff, B Hennuy, A De Clerck, P Wins
Incubation of rat brain homogenates with thiamine or thiamine diphosphate (TDP) leads to a synthesis of thiamine triphosphate (TTP). In membrane vesicles subsequently prepared from the homogenates, increased TTP content correlates with increased 36Cl- uptake. A hyperbolic relationship was obtained with a K0.5 of 0.27 nmol TTP/mg protein. In crude mitochondrial fractions from the brains of animals previously treated with thiamine or sulbutiamine, a positive correlation between 36Cl- uptake and TTP content was found...
July 25, 1994: Brain Research
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