Case-control study on spinal leveraging manipulation and medicine for the treatment of degenerative scoliosis / 中国骨伤

<p><b>OBJECTIVE</b>To compare clinical effects of spinal leveraging manipulation and medicine for the treatment of degenerative scoliosis in pain and function.</p><p><b>METHODS</b>From July 2010 to June 2013, 38 patients with degenerative scoliosis were randomly divided into spinal leveraging manipulation group and medicine group by coin tossing. In manipulation group, there were 9 males and 11 females aged from 58 to 74 years old with an average of (66.63±7.73), the courses of diseases ranged from 3 to 8 months with an average of (5.65±2.58), spinal leveraging manipulation(following meridian to straighten tendon,relieving spasm, osteopathy and massage, clearing and activating the channels and collaterals) were performed for 30 min, once a day, 4 days for a period treatment, totally 9 courses. In medicine group, there were 8 males and 10 females aged from 57 to 70 years old with an average of (63.51±6.61) the courses of diseases ranged from 3 to 5 months with an average of (4.82±1.43), celecoxib with eperisone hydrochloride were orally taken, 4 days for a period treatment, totally 9 courses. VAS score, Cobb angle and ODI score were measured.</p><p><b>RESULTS</b>After treatment, VAS score in manipulation group was (5.38±0.99), (6.36±1.31) in medicine group,and had significant meaning (t=2.618, P<0.05); there was significant differences in Cobb angle between manipulation group (16.51±4.89)° and medicine group (19.85±5.03) °(t=2.074,P<0.05); and had obviously meaning in ODI score between manipulation group (20.20±2.93) and medicine group (26.01±3.11) (t=5.592, P<0.05).</p><p><b>CONCLUSION</b>Spinal leveraging manipulation for degenerative scoliosis could regulate muscle balance on both side of spine, correct coronal imbalances in spine, recover normal sequence of spine, reduce and remove opperssion and stimulation of nerve root, relieve pain in leg and waist and further improve quality of life.</p>

Anaphylaxis caused by muscle relaxant (eperisone hydrochloride)

Eperisone hydrochloride is an antispasmodic drug, decreasing spasticity of skeletal muscle and alleviating stiffness, and as a consequence, controlling pain. It is preferably prescribed with other analgesics, beneficially less decreasing alertness compared with other antispasmodics. Its fatal drug adverse reactions were rarely reported. A 70 year-old female with hives, swollen face, hoarse voice, and near fainting admitted via emergency department. She suffered from the series of the fatal symptoms after administration of the pills, prescribed for her neck pain. Two months before, she had experienced hives on similar medications. At presentation, she revealed hypoxemia and hypotension, and treated with epinephrine, glucocorticoids and antihistamines. Among the medicines she took, eperisone hydrochloride was proven as the causative medicine and others were excluded in oral provocation tests. The positive result in intradermal test with eperisone hydrochloride suggested immediate-type hypersensitivity reaction. We report a case of anaphylaxis to eperisone hydrochloride, one of the widely prescribed medicines in clinical practice, previously without awareness of drug adverse reaction.

Oral Muscle Relaxant May Induce Immediate Allergic Reactions

Eperisone and afloqualone act by relaxing both skeletal and vascular smooth muscles to improve circulation and suppress pain reflex. These drugs are typically prescribed with non-steroidal anti-inflammatory drugs (NSAIDs) as painkillers. However, there have been no reports on serious adverse reactions to oral muscle relaxants; and this is the first report to describe three allergic reactions caused by eperisone and afloqualone. All three patients had histories of allergic reactions after oral intake of multiple painkillers, including oral muscle relaxants and NSAIDs, for chronic muscle pain. An open-label oral challenge test was performed with each drug to confirm which drugs caused the systemic reactions. All patients experienced the same reactions within one hour after oral intake of eperisone or afloqualone. The severity of these reactions ranged from laryngeal edema to hypotension. To confirm that the systemic reaction was caused by eperisone or afloqualone, skin prick testing and intradermal skin tests were performed with eperisone or afloqualone extract in vivo, and basophil activity tests were performed after stimulation with these drugs in vitro. In one patient with laryngeal edema, the intradermal test with afloqualone extract had a positive result, and CD63 expression levels on basophils increased in a dose-dependent manner by stimulation with afloqualone. We report three allergic reactions caused by oral muscle relaxants that might be mediated by non-immunoglobulin E-mediated responses. Since oral muscle relaxants such as eperisone and afloqualone are commonly prescribed for chronic muscle pain and can induce severe allergic reactions, we should prescribe them carefully.

Effect of xanthohumol on melanogenesis in B16 melanoma cells

Xanthohumol (XH), the principal prenylflavonoid of the hop plant (Humulus lupulus L.), dose-dependently inhibited isobutylmethylxanthine (IBMX)-induced melanogenesis in B16 melanoma cells, with little cytotoxicity at the effective concentrations. Decreased melanin content was accompanied by reduced tyrosinase enzyme activity, protein and mRNA expression. The levels of tyrosinase-related protein 1 and 2 mRNAs were decreased by XH. XH also inhibited alpha-melanocyte stimulating hormone- or forskolin-induced increases in melanogenesis, suggesting an action on the cAMP-dependent melanogenic pathway. XH downregulated the protein and mRNA expression of microphthalmia-associated transcription factor (MITF), a master transcriptional regulator of key melanogenic enzymes. These results suggest that XH might act as a hypo-pigmenting agent through the downregulation of MITF in the cAMP-dependent melanogenic pathway.

Pharmacokinetics and bioequivalence of eperisone hydrochloride tablet in healthy subjects / 药学学报

<p><b>AIM</b>To develop a HPLC-ESI-MS assay for determination of eperisone hydrochloride in human plasma and investigate the pharmacokinetics and bioequivalence of two eperisone hydrochloride tablets in human.</p><p><b>METHODS</b>Buflomedil hydrochloride was used as the internal standard. After alkalized with saturated sodium bicarbonate solution, plasma was extracted with diethylether-cyclohexane (1:1) and separated using HPLC on a reversed-phase C18 column with a mobile phase of 10 mmol x L(-1) ammonium acetate buffer solution (adjusted to pH 3.88 with acetic acid)-methanol (20:80). HPLC-ESI-MS was performed in the selected ion monitoring (SIM) mode using target ions at m/z 260 for eperisone and m/z 308 for the internal standard. A randomized crossover design was performed in 20 healthy volunteers. In the two study periods, a single 100 mg dose of each tablet was administered to each volunteer.</p><p><b>RESULTS</b>Calibration curve was linear over the range of 0.02-20 microg x L(-1). The limit of quantification for eperisone hydrochloride in plasma was 0.02 microg x L(-1). The main pharmacokinetics parameters T1/2, Tmax and Cmax were (2.7 +/- 0.4) h, (1.1 +/- 0.5) h and (2.8 +/- 2.8) microg x L(-1) for the reference tablet; (2.8 +/- 0.5) h, (1.1 +/- 0.4) h and (3 +/- 4) microg x L(-1) for the test tablet, respectively. The relative bioavalability of the test tablet was (101 +/- 13)%.</p><p><b>CONCLUSION</b>The assay was proved to be sensitive, accurate and convenient. The two formulations were bioequivalent.</p>

Uso da propafenona em cardiologia / Use of propafenone in cardiology

Por existirem inúmeros mecanismos capazes de produzir arritmias, torna-se difícil existir uma droga que seja considerada "antiarrítmico ideal", capaz de atuar tanto em arritmias supra quanto ventriculares com efeitos adversos mínimos. Isto leva a procura de novas drogas. Faz-se uma revisäo da literatura sobre o propafenon, concluindo-se ser esta droga muito eficaz na terapêutica das taquiarritmias supra e ventriculares, com mínimos efeitos colaterais, quando usada nas doses propostas

Propafenona intravenosa no tratamento de arritmias refratárias em unidade coronariana / Intravenous propafenone in the treatment of refractory arrythmias in coronary care units

Foram estudados 16 pacientes portadores de arritmias ventriculares ou supraventriculares refratárias aos antiarrítmicos habituais. A profanenona foi administrada nestes pacientes na dose de 1 a 2 mg/Kg de peso por via intravenosa lenta tendo-se verificado: 1§ Desaparecimento da arritmia em 4 dos 5 pacientes com arritmia ventricular. 2§ Reversäo para ritmo sinusal em todos os 7 casos de taquicardia supraventricular paroxística e do paciente com fibrilaçäo atrial. 3§ Ausência de reversäo nos 3 casos de uter atrial. 4§ Ausência de paraefeitos importantes. Conclui-se que a profanenona, usada por via intravenosa, é uma droga eficaz e segura para auxiliar o tratamento de arritmias refratárias em Unidade Coronariana

Efeitos da Propafenona sobre o estado contrátil, trabalho sistólico e perfusäo miocárdica do coraçäo "in situ" / Effects of Propafenon on contractile state stroke work and myocardial perfusion of heart \"in situ\"

Os efeitos de diferentes doses de Propafenona foram analisados em cäes, estudando-se as variaçöes do estado inotrópico e da performance do coraçäo. Os resultados demonstram que, na dose de 1 mg/kg de peso, o composto tem propriedade antiarrítmica, sem alterar significativamente o estado contrátil nem o desempenho cardíaco

Behaviour of 4- [3-oxo-13-diarylpropyl] -1-phenyl-3,5pyrazolidindiones towards some nucleophilic reagents

Substituted pyrazolidinedione have received considerable attention in recent years and their application as dyes for plastics, paper and varnishes have been reported. Pyrazolidinedione derivatives exhibiting analgesic antipyretic, antirheumatic and antiphlogistic activities also have been reported. This prompted us to synthesize new pyrazolidinedione derivatives through the nucleophilic addition of l-phenyl-3, 5-pyrazolidinedione to chalcone and study the behaviour of the adducts towards different reagents

Reactivity centres among nucleophilic substituted arylidene acetophenone towards attack by active methylene group [Part XI] synthesis of newer carboxylic acids, cyclic hydrazides, isoxazole and pyridine derive

Hans stobbe [1] stated that alpha beta-unsaturated ketones failed to undergo the Stobbe condensation but form Michael adducts. Patwardhan [2] generalized the reactivity of the carbonyl group in the presence of potassium tert-butoxide, giving the corresponding half-esters in a low yield. Recently [3], we have reported on the reactivity of both centers with special attention to the participation in the Michael and Stobbe condensation. The results obtained in the present study are considered to be rather conclusive in establishing the role of the polar factor in the reactivity of the carbonyl carbon in chalkones. To undergo the Stobbe condensation in a good yield, there must be an electron donating substituents which favours the formation of the intermediate lactone proposed in the currently accepted mechanism[4]] Secondly there must be high concentration of ester group for consuming the protonium ion in alcohol formation. The protonium ion assumed as a by-product [5] and leading to the formation of the competing Michael addition at the expense of the Stobbe condensation. The present investigation was planned to substantiate this conclusion. Thus twelve chalkones having substituents of different polar nature were condensed with succinic ester in the presence of potassium tert-butoxide and the composition of the reaction products were determined. The results obtained may be considered as a contribution characterized to the work done by Hans Stobbe and Patwardhan. An elegant support for the importance of the polar factor can be shown by the failure of the alpha, beta-unsaturated ketones having an electron attracting group to undergo the Stobbe condensation, where the maximum yield range from 3-10 percent it is interesting to note that the yields of the half-esters increase with the increase of the number of the methyl and methoxyl substituents, whereby the half-ester attains 70 percent when the tetra-substituted chalkone was utilized in the Stobbe condensation. For this purpose we reacted 4,4'- dimethoxy, 4-methoxy 3/4'-dimethyl and 2.3-dimethoxy 3', 4'-dimethyl chalkones with dimethyl succinate to verify good yields of the half-esters [see Experimental]. The IR spectra of these compounds showed absorption bands of the dimeric carboxylic groups for esters and acids. Alkaline hydrolysis of the half-esters gave the corresponding dibasic acids of the type [Ib] and [IIb]. The structure of these acids was supported by analytical data, IR spectra and the facile conversion into the corresponding cyclic hydrazide [IIIa],upon treatment with hydrazine hydrate. The IR spectrum of compound IIIa showed characteristic absorption bands at 3380, 1660, 1620 and 1600 cm[-1] The reactions with dimethyl sulphate [6] and methyl isocyanate to form dimethyl and dicarba-mate succinhydrazide derivatives, IIIb, c were considered as additional evidence for the assigned structure IIIa The reaction of chalkones and cyanoacetamide in the presence of ammonium acetate afforded cyanopyridones [IVa],[IVb] and cyanodihydropyridone [V] [7], rested upon correct analytical and spectral data. When 4-methoxy 3',4'-dimethyl chalkone was brominated in acetic acid, it afforded the dibromide which upon treatment with hydroxylamine hydro-chloride under conditions similar to those described by Nakata [8] for isoxazole synthesis, compound VI was obtained, the structure of which is supported by a study of electronic spectrum which is similar to that previously described [9]. It has been assumed [10] that the isoxazoles are obtained through the formation of acetylenic oxime presumably formed as an intermediate through dehydrobromination, followed by intramolecular cycloaddition. The reaction of 4-methoxy 3,'4'-dimethyl chalkone with ethylcyanoacetate in presence of ammonium acetate, afforded VII. Whether the reaction was carried out with or without a solvent, the same product was obtained. However, compound VII is not identical with that formed by Sakurai and Midorikawa [11] for the reaction of unsubstituted alpha, beta- unsaturated ketones with ethylcyanoacetate as shown by spectral and analytical data. The reaction of 4-methoxy 3', 4 -dimethyl chalkone with malononitrile [12] afforded cyanoaminopyridine [VIII]. The IR spectrum showed the frequency bands due to asymmetric and symmetric stretching vibrations of primary amines as multiple bands of medium intensity. The corresponding bending vibrations cause absorption in the 1630 cm[-1] region as 2-amino pyridine, in addition to the characteristic absorption bands for the cyano group