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Objective:To investigate the clinical efficacy and safety of amisulpride in the treatment of schizophrenia.Methods:Ninety patients with schizophrenia admitted to Quzhou Third Hospital from August 2020 to March 2022 were included in this study. They were randomly divided into an observation group and a control group ( n = 45/group). The control group was treated with olanzapine, and the observation group was treated with amisulpride. All patients were treated for 8 consecutive weeks. Total response rate, Positive and Negative Syndrome Scale score, Clinical Global Impression Scale-Severity of Illness score, glucose and lipid metabolism indicators, Treatment Emergent Symptom Scale score, and adverse reactions were compared between the two groups. Results:Total response rate was 88.89% (40/45) in the control group and 93.33% (42/45) in the observation group. There was no significant difference in total response rate between the two groups ( χ2 = 0.14, P > 0.05). After treatment, the PANSS score [(52.14 ± 3.99) points] and CGI-S score [(3.05 ± 0.86) points] in the observation group were significantly lower than (56.38 ± 4.05) points and (4.34 ± 0.92) points in the control group ( t = 5.00, 6.87, both P < 0.001). The levels of fasting plasma glucose [(5.25 ± 0.33) mmol/L], total cholesterol [(4.08 ± 0.67) mmol/L], triglyceride [(1.29 ± 0.35) mmol/L], and low density lipoprotein-cholesterol [(2.60 ± 0.31) mmol/L] in the observation group were significantly lower compared with the control group [(6.02 ± 0.51) mmol/L, (4.71 ± 0.59) mmol/L, (1.61 ± 0.26) mmol/L, (2.91 ± 0.34) mmol/L, t = 8.50, 3.61, 4.92, 4.52, all P < 0.001]. High density lipoprotein-cholesterol level in the observation group was significantly higher than that in the control group [(1.57 ± 0.36) mmol/L vs. (1.18 ± 0.42) mmol/L t = -4.73, P < 0.001]. Treatment Emergent Symptom Scale score in the observation group was significantly lower than that in the control group [(2.39 ± 0.58) points vs. (2.87 ± 0.62) points, t = 3.79, P < 0.05]. The incidences of drowsiness [6.67% (3/45)], constipation [8.89% (4/45)], and weight gain [2.22% (1/45)] in the observation group were significantly lower than those in the control group [73.33% (33/45), 28.89% (13/45), 17.78% (8/45), χ2 = 4.14, 4.64, 4.44, P < 0.05]. Conclusion:The efficacy of sulfapride in the treatment of schizophrenia is equivalent to that of olanzapine. Sulfapride is better than olanzapine in improving symptoms and reducing disease severity and has better safety.
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Abstract Dyslipidemia is an abnormal lipid profile associated with many common diseases, including coronary heart disease and atherosclerosis. Cholesteryl ester transfer protein (CETP) is a hydrophobic plasma glycoprotein that is responsible for the transfer of cholesteryl ester from high-density lipoprotein athero-protective particles to pro-atherogenic very low-density lipoprotein and low-density lipoprotein particles. The requirement for new CETP inhibitors, which block this process has driven our current work. Here, the synthesis as well as the ligand-based and structure-based design of seven oxoacetamido-benzamides 9a-g with CETP inhibitory activity is described. An in vitro study demonstrated that most of these compounds have appreciable CETP inhibitory activity. Compound 9g showed the highest inhibitory activity against CETP with an IC50 of 0.96 µM. Glide docking data for compounds 9a-g and torcetrapib provide evidence that they are accommodated in the CETP active site where hydrophobic interactions drive ligand/CETP complex formation. Furthermore, compounds 9a-g match the features of known CETP active inhibitors, providing a rationale for their high docking scores against the CETP binding domain. Therefore, these oxoacetamido-benzamides show potential for use as novel CETP inhibitors
Subject(s)
Benzamides/adverse effects , Dyslipidemias/complications , Cholesterol Ester Transfer Proteins/antagonists & inhibitors , In Vitro Techniques/methods , Cholesterol Esters , Coronary Disease/pathology , Inhibitory Concentration 50 , Lipoproteins, HDL/classification , Lipoproteins, LDL/classificationABSTRACT
Objective To investigate mosapride in the treatment of functional dyspepsia(FD) and its effect on proximal stomach and gastric emptying function .Methods One hundred and two patients diagnosed of functional dyspepsia in our hospital were ran‐domly divided into observation group (with treatment of mosapride) and control group(with treatment of domperidone) ,and 51 ca‐ses were in each group .The clinical efficacy was observed ,and the LOGIQ‐GE2000 diagnostic apparatus were used to detect the de‐termination of proximal stomach and gastric emptying function before and after treatment .Results The clinical effective rate of the observation group was 86 .27% ,significantly higher than that of the control group(64 .71% ) .The difference was statistically signif‐icant between them(P0 .05) .Conclusion Mosapride in treatment of functional dyspepsia is better than domperi‐done ,and it could significantly improve the patient′s proximal stomach and the function of gastric motility .
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Aims: The aims of the research were to synthesize, characterize some palmitoyl amino acids and their aromatic analogues and to screen the synthesized compounds for possible antibacterial activity Study Design: Synthesis, characterization and antibacterial screening of palmitoyl amino acids and their aromatic analogues. Place and Duration of Study: Department of Pharmaceutical and Medicinal Chemistry/ Department of Pharmaceutical Microbiology and Biotechnology, Faculty of Pharmacy, Niger Delta University, Wilberforce Island, between September 2012 and January 2013. Methodology: Palmitoylchloride was condensed with the respective amino acids (glycine, β-alanine, γ-amino butyric acid) to form the corresponding palmitoyl amino acids. The opening of the isatoic anhydride ring with the three amino acids and subsequent condensation with palmitoyl chloride led to the formation of the amino acid benzamides. The antibacterial screening was carried out using agar well diffusion method. Results: All the synthesized compounds were obtained in good yield and high purity; they were unequivocally characterized by the combination IR, 1H NMR, 13C NMR and MS. The compounds were however found to possess no antibacterial activity against the tested microorganisms Conclusion: This work has shown that both the straight chain and aromatic analogues of saturated long chain lipid amides are inactive against the tested strains of microorganism.
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Objective To investigate the role of prokinetic agent itopride in colonic preparation before colonoscopy examination in patients with constipation.Methods A total of 115 outpatients with history of chronic constipation who requested colonoscopy were collected.According to colonic preparation proposal,patients were divided into three groups.Group A (39 cases) took standard dosage of PEG-E solution six hours before colonoscopy examination.Group B (38 cases) took 150 mg itopride 30 minutes before administration of lavage solution.Group C (38 cases) took itopride 150 mg at 7 am,12 am and 8 pm the day before the examination and on the examination day took the same medicine as that of group B.The blood pressure,heart rate and blood electrolytes were monitored before and after taking medicine in the patients of three groups.Quality of colon cleansing of each group was observed and side effects were also observed.One-way analysis of variance (least significant difference,LSD) test was performed for pairwise comparisons among the three groups.Chi-square test was applied for count data.Results Both group A and group B excluded one patient because of malignant carcinoma with colon stricture under colonoscopy,and 113 patients completed the whole colon examination.There was no significant difference in the baseline patients' data of three groups.The colon cleaning score of group C (7.28±1.11) was higher than those of group A and B (6.55±1.18 and 6.51±1.16,LSD test,both P＜0.05).The frequency of bowel movements defecation of group C (8.31± 1.32) was more than those of group A and group B (7.11± 1.41 and 6.94± 1.51,LSD,test,both P＜0.05).There was no significant difference in terms of intestinal bubble scores,blood pressure,heart rate,blood electrolytes the uncomfortable degree of colonic preparation and rate of side effects of the three groups.Conclusion The colonic preparation can be safely and effectively improved by taking high dose of itopride one day before and on the day of colonoscopy examination.
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Objective To evaluate the efficacy and safety of mosapride in the treatment of gastroesophageal reflux disease (GERD). Methods Papers of PubMed,EMBASE,OVID,VIP Database and WANGFANG Data were searched and reviewed according to international Cochrane Collaboration.Results A total of 21 trials (1666 patients) were included.The treatment group was with mosapride and PPI,the control group was with single PPI or PPI and placebo.The Results of Meta analysis showed:for non-erosive negative reflux disease,there was no significant difference in efficacy between two groups.As for erosive esophagitis treated with mosapride (5mg):There was no significant difference in the 4-week healing rates between treatment group and control group (P =0.06).The 4-week symptom relief rate of treatment group was better than that of control group (P＜0.01).The 6-week healing rate of treatment group was better than that of control group (P＜0.01).The 6-week symptom relief rate of treatment group was better than that of control group (P＜0.01).There was no significant difference in the 8-week healing rate of esophagitis between treatment group and control group (P =0.05).The 8-week symptom relief rate of treatment group was better than that of control group (P＜0.01).For erosive esophagitis treated with mosapride 10mg,.The 8-week symptom relief rate of treatment group was better than that of control group (P=0.02).Conclusion According to the meta-analysis of these 21 trails,mosapride was safe and effective in the treatment of GERD.However due to the quality of the literatures,the above findings should be treated with caution.
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Objective To investigate the protective effects of 3-aminobenzamide on the kidney of STZ-induced diabetic rats.Methods Experimental rats were divided into normal control group(group NC),diabetic control group(group DC) and diabetic rats treated with 3-aminobenzamide(group DT).The indexes such as the creatinine clearance rate(Ccr),the ratio of kidney weight to body weight,the contents of blood glucose,24h urinary protein,malonaldehyde(MDA),superoxide dismutase(SOD),glutathione peroxidase(GSH-Px) were tested in each group after 4 weeks.The expression of PARP was tested by immunohistochemistry method.Results Compared with group DC,the 24h urinary protein,Ccr and the concentration of MDA were decreased in group DT,as well as the activity of SOD and GSH-Px was enhanced(all P