1.Effects of Four Dihydropyridine Calcium Antagonists on CYP3 A4 Enzyme Activity Induced By Dexametha-sone in Female Rats
Junan SUN ; Xuecheng HAN ; Zongling XIA ;
China Pharmacist 2014;(12):2007-2010
Objective:To study the inhibition effects of four dihydropyridine calcium antagonists felodipine, nicardipine, lercani-dipine and nifedipine on CYP3A4 enzyme to provide the theoretical basis for the understanding of the drug interactions between dihydro-pyridine calcium antagonists and other drugs. Methods:Using the probe drugs method, the SD female rats induced by 80 mg·kg-1 · d-1 dexamethasone for three days were divided into the negative control group, positive control group, four DHPs groups with six ones in each. Dapsone was used as the probe substrate, and the concentration was determined by HPLC. Data analysis software WinNonLin was used in the pharmacokinetic model fitting process and the paired t-test was used in the statistical analysis. Results: AUC0-24 and CL/F of dapsone in the negative control group showed statistically significant differences when compared with those in the four DHPs groups and the positive group (P<0. 05). Although the inhibition effect of the four DHPs was in the order of nifedipine inhibition >nicardipine > lercanidipine > felodipine, the difference was not statistically significant (P>0. 05). Cmax of dapsone in the DHPs groups and the positive group had no statistically significant difference when compared with that in the negative control group ( P>0. 05). Conclusion:Although there are different inhibition effects on CYP3A4 among the four DHPs, the differences are not significant in vivo, and there is no influence on the combination drugs which is not mainly metabolized by CYP3A4.
2.Application of CRUSADE score for evaluating of risk of gastrointestinal bleeding due to antiplatelet agents
Junan SUN ; Zongling XIA ; Can LUO
Adverse Drug Reactions Journal 2014;(4):209-212
Objective To explore the role of CRUSADE score for evaluating the risk of gastrointestinal bleeding due to antiplatelet agents. Methods The hospitalized patients with coronary heart disease and received antiplatelet therapy for more than 1 year before hospitalization in department of internal medicine in the Third People's Hospital of Cixi,Zhejiang Province from September 1010 to September 1013 were enrolled into the study. The patients were divided into the gastrointestinal bleeding group and the non-gastrointestinal bleeding group according to whether gastrointestinal bleeding occurred due to antiplatelet agents. The CRUSADE score was evaluated in the 1 groups and the relationship between the CRUSADE score and gastrointestinal bleeding was analyzed. Results A total of 787 patients with coronary heart disease who received antiplatelet therapy more than 1 year were collected. Forty patients with gastrointestinal bleeding were enrolled into the gastrointestinal bleeding group. One hundred and sixty patients were enrolled into the non-gastrointestinal bleeding group by equidistant sampling method randomly. The gastrointestinal bleeding group comprised 31 male and 9 female with age from 45 to 88( 71 ± 9 ) years. The non-gastrointestinal bleeding group comprised 100 male and 60 female with age from 36 to 89(65 ± 13)years. There was statistically significant difference in age between the 1 groups(P ﹤0. 05). The percentage of cases of receiving aspirin enteric-coated tablets,clopidogrel hydrogen sulfate tablets,and both the above-mentioned drugs in the gastrointestinal bleeding group and the non-gastrointestinal bleeding group were 55%(11/40),10%(4/40),35%(14/40)and 54%(86/160),7%(11/160),39%(63/160),respectively. The difference was not statistically significant(P ﹥0. 05). The percentage of cases who had history of gastroin-testinal bleeding and peptic ulcer in the gastrointestinal bleeding group and the non-gastrointestinal bleeding group were 30. 0%(11/40)and 11. 9%(19/160),respectively. The difference was statistically significant(P ﹤0. 05). There were 17. 5%(11/40)and 17. 5%(11/40)cases with the results of CRUSADE score at high risk and very high risk in the gastrointestinal bleeding group,8. 1%(13/160)and 10. 6%( 17/160 ) cases in the non-gastrointestinal bleeding group,respectively. The difference was statistically significant(P﹤0. 05). Conclusions CRUSADE score can help to evaluate the risk of gastrointestinal bleeding in patients with coronary heart disease who received antiplatelet therapy. It is suggested that the patients with coronary heart disease as well as the CRUSADE score of high risk and very high risk should receive the combination of antiplatelet agents and the proton pump inhibitor,in order to prevent or reduce the gastroin-testinal bleeding.
3.Application of CRUSADE score for evaluating of risk of gastrointestinal bleeding due to antiplatelet agents
Junan SUN ; Zongling XIA ; Can LUO
Adverse Drug Reactions Journal 2014;(4):209-212
Objective To explore the role of CRUSADE score for evaluating the risk of gastrointestinal bleeding due to antiplatelet agents. Methods The hospitalized patients with coronary heart disease and received antiplatelet therapy for more than 1 year before hospitalization in department of internal medicine in the Third People's Hospital of Cixi,Zhejiang Province from September 1010 to September 1013 were enrolled into the study. The patients were divided into the gastrointestinal bleeding group and the non-gastrointestinal bleeding group according to whether gastrointestinal bleeding occurred due to antiplatelet agents. The CRUSADE score was evaluated in the 1 groups and the relationship between the CRUSADE score and gastrointestinal bleeding was analyzed. Results A total of 787 patients with coronary heart disease who received antiplatelet therapy more than 1 year were collected. Forty patients with gastrointestinal bleeding were enrolled into the gastrointestinal bleeding group. One hundred and sixty patients were enrolled into the non-gastrointestinal bleeding group by equidistant sampling method randomly. The gastrointestinal bleeding group comprised 31 male and 9 female with age from 45 to 88( 71 ± 9 ) years. The non-gastrointestinal bleeding group comprised 100 male and 60 female with age from 36 to 89(65 ± 13)years. There was statistically significant difference in age between the 1 groups(P ﹤0. 05). The percentage of cases of receiving aspirin enteric-coated tablets,clopidogrel hydrogen sulfate tablets,and both the above-mentioned drugs in the gastrointestinal bleeding group and the non-gastrointestinal bleeding group were 55%(11/40),10%(4/40),35%(14/40)and 54%(86/160),7%(11/160),39%(63/160),respectively. The difference was not statistically significant(P ﹥0. 05). The percentage of cases who had history of gastroin-testinal bleeding and peptic ulcer in the gastrointestinal bleeding group and the non-gastrointestinal bleeding group were 30. 0%(11/40)and 11. 9%(19/160),respectively. The difference was statistically significant(P ﹤0. 05). There were 17. 5%(11/40)and 17. 5%(11/40)cases with the results of CRUSADE score at high risk and very high risk in the gastrointestinal bleeding group,8. 1%(13/160)and 10. 6%( 17/160 ) cases in the non-gastrointestinal bleeding group,respectively. The difference was statistically significant(P﹤0. 05). Conclusions CRUSADE score can help to evaluate the risk of gastrointestinal bleeding in patients with coronary heart disease who received antiplatelet therapy. It is suggested that the patients with coronary heart disease as well as the CRUSADE score of high risk and very high risk should receive the combination of antiplatelet agents and the proton pump inhibitor,in order to prevent or reduce the gastroin-testinal bleeding.
4.Empirical study on protective effect of preparations from Tiaogan Lipi prescription on mouse with hepatic injury induced by ethanol
Xiulan DENG ; Junan FENG ; Xiaojing ZHANG ; Binbin GUAN ; Qian ZHU ; Dayong CAI ; Jinhui SUN
China Journal of Traditional Chinese Medicine and Pharmacy 2005;0(05):-
Objective: To compare the protective effect of various preparations from Tiaogan Lipi prescription on mouse ethanol hepatic injury.Methods:The hepatic injury model of mice was replicated with ethanol.Comparing with Fufang Biejia Ruan’gan prescription,three preparations from Tiaogan Lipi prescription were administrated for protecting the hepatic injury.The contents of AST,ALT,CHOL and TG in serum and the MDA and SOD in liver tissue were tested.The pathological changes of the liver had been evaluated.Results:Three preparations from Tiaogan Lipi reduces the level of ASTALTCHOL TG,lowers the content of MDA(P

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