Butea monosperma Reduces Haloperidol and Sulpiride Induced Hyperprolactinemia.

Background: Prolonged administration of neurolepticdrugs cause disrupted D dopamine receptor which 2leads to increased prolactin level, causesgyanaecomastia. Presently, dopamine receptor agonistis the choice of treatment for hyperprolactinemia. Aimand Objectives: The study aims to determine the antihyperprolactinemic effect of methanolic extract ofButea monosperma (MEBM) against haloperidol(HPL) and sulpiride (SPD) induced hyperprolactinemiaand to correlate with its active constituents. Materialand Methods: To induce hyperprolactinemia HPL 5mg/kg for 16 continuous days and SPD 20 mg/kg for 28continuous days was administred. MEBM 200mg/kg/day and 400 mg/kg/day were administered for16 and 28 days respectively half an hour beforeadministration of HPL and SPD. The serum prolactin(PRL) level, dopamine (DA) level and antioxidantstatus in the rat brain, hematological parameters weremeasured and histological examination of the anteriorpituitary gland, adrenal gland and spleen were done. Inaddition, antioxidant enzymes like superoxidedismutase (SOD) and catalase (CAT) were alsoestimated. Results: MEBM decreases serum PRL leveland increased DA level in brain significantly. Further,MEBM also restored SOD and CATstatus significantly.The inflammatory markers induced by HPL and SPDwere suppressed by MEBM. Discussion: Neuronal DAinhibition by neuroleptic drugs decreases the release ofDAwhich leads to hyperprolactinemia. MEBM (butrin)may activate DA neurones to ameliorate hyperprolactinaemia. The dopaminergic, anti-oxidant andanti-inflammatory effect of MEBM may be attributed toits anti-hyperprolactinemic effect. Conclusion: Buteamonosperma possesses anti-hyperprolactinemic effectwhich may be attributed to its marker constituent likeButrin.

Effects of Amisulpride Adjunctive Therapy on Working Memory and Brain Metabolism in the Frontal Cortex of Patients with Schizophrenia: A Preliminary Positron Emission Tomography/Computerized Tomography Investigation

OBJECTIVE: Dopamine plays a significant role in working memory by acting as a key neuromodulator between brain networks. Additionally, treatment of patients with schizophrenia using amisulpride, a pure dopamine class 2/3 receptor antagonist, improves their clinical symptoms with fewer side effects. We hypothesized that patients with schizophrenia treated with amisulpride and aripiprazole show increased working memory and glucose metabolism compared with those treated with cognitive behavioral therapy (CBT) and aripiprazole instead. METHODS: Sixteen patients with schizophrenia (eight in the amisulpride group [aripiprazole+amisulpride] and eight in the CBT group [aripiprazole+CBT]) and 15 age- and sex-matched healthy control subjects were recruited for a 12-week-long prospective trial. An [18F]-fluorodeoxyglucose-positron emission tomography/computerized tomography scanner was used to acquire the images. RESULTS: After 12 weeks of treatment, the amisulpride group showed greater improvement in the Letter-Number Span scores than the CBT group. Additionally, although brain metabolism in the left middle frontal gyrus, left occipital lingual gyrus, and right inferior parietal lobe was increased in all patients with schizophrenia, the amisulpride group exhibited a greater increase in metabolism in both the right superior frontal gyrus and right frontal precentral gyrus than the CBT group. CONCLUSION: This study suggests that a small dose of amisulpride improves the general psychopathology, working memory performance, and brain glucose metabolism of patients with schizophrenia treated with aripiprazole.

Galactocele medicamentosa pós-mamoplastia de aumento: relato de caso e revisão da literatura / Galactocele due to drugs prescribed after augmentation mammoplasty: a case report and literature review

A mamoplastia de aumento é um procedimento cirúrgico muito comum e seguro na cirurgia plástica, mas o mesmo não está isento de complicações. A galactocele após mamoplastia de aumento é raramente descrita na literatura. Este relato de caso refere-se a uma paciente de 34 anos de idade, que fazia uso de sulpirida há 2 anos e 4 meses e desenvolveu galactocele cerca de 100 dias após mamoplastia de aumento. O diagnóstico deve ser suspeitado quando se observar uma mama aumentada de volume, associada a calor local, dor ou desconforto mamário no pós-operatório. Acredita-se que a melhor conduta seja a drenagem cirúrgica, a fim de confirmar o diagnóstico de galactocele e excluir a presença de abscesso mamário.

Augmentation mammaplasty is a common and safe plastic surgery procedure, but it is not free from complications. Galactocele after augmentation mammaplasty is rarely described in the literature. We discuss the case of a 34-year-old woman who had been taking sulpiride for 2 years and 4 months and developed galactocele approximately 100 days after augmentation mammaplasty. However, diagnosis should be suspected if breast size increases and it is associated with postoperative local heat, pain or breast discomfort. We believe that the surgeon must surgically drain galactocele to confirm diagnosis, especially to exclude the presence of breast abscess.

The Role of Spinal Dopaminergic Transmission in the Analgesic Effect of Nefopam on Rat Inflammatory Pain

BACKGROUND: Nefopam has been known as an inhibitor of the reuptake of monoamines, and the noradrenergic and/or serotonergic system has been focused on as a mechanism of its analgesic action. Here we investigated the role of the spinal dopaminergic neurotransmission in the antinociceptive effect of nefopam administered intravenously or intrathecally. METHODS: The effects of intravenously and intrathecally administered nefopam were examined using the rat formalin test. Then we performed a microdialysis study to confirm the change of extracellular dopamine concentration in the spinal dorsal horn by nefopam. To determine whether the changes of dopamine level are associated with the nefopam analgesia, its mechanism was investigated pharmacologically via pretreatment with sulpiride, a dopaminergic D2 receptor antagonist. RESULTS: When nefopam was administered intravenously the flinching responses in phase I of the formalin test were decreased, but not those in phase II of the formalin test were decreased. Intrathecally injected nefopam reduced the flinching responses in both phases of the formalin test in a dose dependent manner. Microdialysis study revealed a significant increase of the level of dopamine in the spinal cord by intrathecally administered nefopam (about 3.8 fold the baseline value) but not by that administered intravenously. The analgesic effects of intrathecally injected nefopam were not affected by pretreatment with sulpiride, and neither were those of the intravenous nefopam. CONCLUSIONS: Both the intravenously and intrathecally administered nefopam effectively relieved inflammatory pain in rats. Nefopam may act as an inhibitor of dopamine reuptake when delivered into the spinal cord. However, the analgesic mechanism of nefopam may not involve the dopaminergic transmission at the spinal level.

Extractive Spectrophotometric Method for the Determination of Some Antipsychotic Drugs Using Eriochrome Black T.

Simple, accurate, precise, and rapid extractive spectrophotometric method was developed for the determination of four antipsychotics drugs, namely sulpiride (SUP), olanzapine (OLP), clozapine (CLP) and aripiprazole (ARP) both in tablets and in biological fluids. The method was based on the formation of red colored ion-pair complex between the studied drugs and eriochrome black T (EBT) with absorption maxima at 514 nm. The stoichiometry of the complexes in either case was found to be 1: 1 and the conditional stability constant (Kf) of the complexes have been calculated. Reaction conditions were optimized to obtain the maximum color intensity. Beer’s law was obeyed in the concentration ranges of 4-30, 4-20, 2-18 and 4-26 μg/ml with SUP, OLP, CLP and ARP, respectively. Various analytical parameters have been evaluated and the results have been validated by satistical data. The proposed method was successfully applied to the analysis of commercial tablets containing the drugs and the results were in good agreement with those obtained with reported methods. The proposed method was further applied to the determination of the studied drugs in spiked human serum and urine. A proposal for the reaction pathway was postulated.

Olanzapine and sulpiride on treatment of schizophrenia patients were observed in 78 cases / 中国医师进修杂志

Objective To observe the curative effect of olanzapine combined with sulpiride for patients with schizophrenia.Methods From April 2013 to April 2015,156 cases of patients with schizophrenia were selected as the research object.All patients were randomly divided into observation group and control group,78 cases in each group.The observation group received olanzapine combined with sulphide in the treatment,the control group was given the olanzapine in the treatment of patients,observed the therapeutic effect of the two groups.Results After treatment,the BPRS score of the observation group was significantly relieved compared to the control group,the difference was statistically significant (P＜ 0.05).After treatment,the adverse reactions of the two groups were significantly less than those of the control group,the difference was statistically significant (P ＜ 0.05).After treatment,the two groups were treated with 38.46％ (30/78),significantly higher than the control group of 23.08％ (18/78);the observation group was 2.56％ (2/78),significantly lower than the control group 11.54％ (9/78),the difference was statistically significant (P ＜ 0.05).Conclusion Olanzapine combined with sulpiride for schizophrenic patients has better clinical curative effect,reduce the probability of the occurrence of adverse reactions.

The effect of tropisetron combined with sulpiride on chemotherapy-induced cisplatin program nausea and vomiting / 中国医师进修杂志

Objective To investigate the efficacy and safety of tropisetron combined with sulpiride in treatment of chemotherapy-induced cisplatin program nausea and vomiting,so as to explore the effect to motilin and gastrin.Methods A total of 84 patients with chemotherapy-induced cisplatin program nausea and vomiting were divided into study group (44 cases) and control group (40 cases) by random digits table method,the patients in two groups were given tropisetron hydrochloride intravenous injection,and the study group was added sulpiride.The efficacy and side effects and effect to motilin and gastrin were observed.Results The fully control rate and efficient rate in acute nausea was 59.09％ (26/44),37.50％ (15/40),and 90.91％ (30/44),72.50％ (29/40) in study group and control group,and there was significant difference (P ＜ 0.05).The fully control rate and efficient rate in acute vomiting was 61.36 ％ (27/44),37.50％ (15/40),and 88.64％ (39/44),67.50％ (27/40) in study group and control group,and there was significant difference (P ＜0.05).The fully control rate and efficient rate in delayed nausea was 54.54％ (24/44),32.50％ (13/40),and 79.55％ (35/44),57.50％ (23/40) in study group and control group,and there was significant difference (P ＜ 0.05).The fully control rate and efficient rate in delayed vomiting was 45.45 ％ (20/44),22.50％ (9/40),and 75.00％ (33/44),52.50％ (21/40) in study group and control group,and there was significant difference (P＜ 0.05).The plasma motilin after treatment was lower than that before treatment in study group and control group[(308.35 ± 14.59) ng/L vs.(370.59 ± 15.72) ng/L and(341.87 ± 18.38) ng/L vs.(365.36 ± 23.72) ng/L],gastrin was higher than that before treatment in study group and control group [(206.97 ± 12.29) ng/L vs.(164.56 ± 14.17) ng/L and (171.58 ± 13.53) ng/L vs.(158.42 ± 17.29) ng/L],and there was significant difference (P ＜ 0.05).There was significant difference in the plasma motilin and gastrin after treatment between two groups (P ＜ 0.05).There was no significant difference in the occurrence of adverse drug reactions between two groups (P ＞ 0.05).Conclusion Tropisetron combined with sulpiride than the routine use of tropisetron can obtain the better the antiemetic effect.

Response of I(Kr) and hERG Currents to the Antipsychotics Tiapride and Sulpiride

The human ether-a-go-go-related gene (hERG) channel is important for repolarization in human myocardium and is a common target for drugs that prolong the QT interval. We studied the effects of two antipsychotics, tiapride and sulpiride, on hERG channels expressed in Xenopus oocytes and also on delayed rectifier K+ currents in guinea pig cardiomyocytes. Neither the amplitude of the hERG outward currents measured at the end of the voltage pulse, nor the amplitude of hERG tail currents, showed any concentration-dependent changes with either tiapride or sulpiride (3~300 micrometer). However, our findings did show that tiapride increased the potential for half-maximal activation (V(1/2)) of HERG at 10~300 micrometer, whereas sulpiride increased the maximum conductance (G(max)) at 3, 10 and 100 micrometer. In guinea pig ventricular myocytes, bath applications of 100 and 500 micrometer tiapride at 36degrees C blocked rapidly activating delayed rectifier K+ current (I(Kr)) by 40.3% and 70.0%, respectively. Also, sulpiride at 100 and 500 micrometer blocked I(Kr) by 38.9% and 76.5%, respectively. However, neither tiapride nor sulpiride significantly affected the slowly activating delayed rectifier K+ current (I(Ks)) at the same concentrations. Our findings suggest that the concentrations of the antipsychotics required to evoke a 50% inhibition of IKr are well above the reported therapeutic plasma concentrations of free and total compound.

Treat stupor state by diazepam / 中国基层医药

Objective To explore the efficacy and method of diazepam in the treatment of stupor state. Methods Other antipsychotic drugs were stopped using patients were made sure to be healthy,inject with diazepam (first day 15～20mg,second day 20～30mg).Then,the similar patients who infused with sulpiride(300- 400mg everyday) were collected during the same period,all the cases were evaluated by SAPS and SANS.Analysis the re- sults by t-test.Results After injecting diazepam,19 patients' stupor state were improved in a short time,and didn't ap- lear adverse reaction.But after using sulpiride,only 2 cases improved,12 cases were better and 5 cases had no change,there were significant difference between two groups during the first week.Conclusion Using diazepam for stupor state is a safe and feasible treatment,with low cost,slight adverse reaction but high efficacy.

Effect of training on dopamine metabolism and appearance of c-fos in rat brain / 体力科学

Changes induced by physical training were examined by in vivo microdialysis monitoring of extracellular dopamine and its metabolites in the rat nucleus accumbens, and by an immunohistochemical staining for fos protein as an index of nerve cell excitation.<BR>The exercise training consisted of running on a treadmill 5 days/week for 4 weeks, with gradually increasing the running speed from 10 to 20 m/min for 20 min. The control group performed forced treadmill running for 3 days.<BR>The sulpiride-induced increase in both dopamine release and dopamine metabolism was significantly attenuated in the nucleus accumbens of training rats in comparison with the controls, which indicated that physical training induced subsensitive DA D<SUB>2</SUB> receptors in the central dopaminergic neurons.<BR>Fos protein expression following 1 h running was weaker in neurons of the raphe dorsalis, the locus ceruleus and the amygdala of trained rats than in those of controls. The present findings suggest that both neurochemical response to various stimuli, and adaptation induced by physical training differ from those in untrained animals.

Cost-effectiveness Analysis of Three Preventing Schemes for Cisplatin-induced Vomiting / 中国药房

OBJECTIVE:To discuss the economic effects of different therapeutic schemes in the treatment of the same illness.METHODS:202 cases receiving cisplatin chemotherapy were randomly divided into three groups according to the preventing schemes received:group Ⅰ,sulpiride;groupⅡ,ondansetron;groupⅢ,metoclopramide.Data was evaluated using pharmacoeconomic cost-effectiveness analysis.RESULTS:The effective rate of sulpiride was 87.1%,expense of one therapeutic course being 93.30 yuans and increase of 1% effective rate costed 1.07 yuans.The effective rate of ondansetron was 93.5%,expense of one therapeutic course being 448.26 yuans and increase of 1% effective rate costed 4.79 yuans.The effective rate of metoclopramide was 57.5%,expense of one therapeutic course being 54.33 yuans and increase of 1% effective rate costed 0.94 yuans.CONCLUSION:The sulpiride scheme is the most rational one.

Sulpiride in Meige's Syndrome: Possible Role of Glutamate

Sulpiride, a selective antagonist for adenylate cyclase-independent dopamine receptors, was administrated to 25 patients with blepharospasm and oromandibular dystonia(Meige's syndrome). Of the 25, 7 patients (28%) exhibited marked and lasting improvement with sulpiride and 12 patients (48%) showed mild or transient improvement. This favorable therapeutic response to sulpiride suggests that striatal glutamate underactivity may play a role in the pathophysiology of Meige's syndrome as a primary or secondary defect.