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Welcome to Chinese Journal of Clinical Pharmacology and Therapeutics,Today is Chinese

Table of Content

    Volume 16 Issue 9
    26 September 2011
    Regulatory of drug clinical trials in China
    ZHANG Zheng-fu, SHEN Yu-hong, LI Zheng-qi
    2011, 16(9):  961-964. 
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    Regulation of drug clinical trials in China is gradually being standardized and improved. This paper explores the regulatory measures of drug clinical trials suitable for China according to the current status and problems in the regulatory, and the aim is to improve the level of drug clinical trials in China.
    In vitro effect of A771726 on the secretion of nitric oxide of peritoneal macrophages from collagen-induced arthritis rats
    WANG Ting-yu, LI Jun, JIN Zhi-gui, WU Fei-hua, WANG Xiao-hua, ZHOU Qian
    2011, 16(9):  965-970. 
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    AIM: To study the effect and mechanism of A771726, the active metabolite of leflunomide, on the production of nitric oxide (NO) of peritoneal macrophages (PMФ) from collagen-induced arthritis (CIA) rats. METHODS: Collagen-induced arthritis (CIA) model was induced in rats and the PMФ were collected. A771726 were used in vitro. The dose-dependent and time-dependent effects of A771726 on the secretion of NO of PMФ from CIA rats were checked by nitric acid reduction synthase method; MTT reagent was used to detect the effect of A771726 on the cell viability of PMФ from CIA rats; RT-PCR was used to detect the expression of inducible NO synthase (iNOS) mRNA. Western blot was used to detect the expression of iNOS protein. RESULTS: A771726 could inhibit the secretion of NO of PMФ from CIA rats in a dose-dependent and time-dependent manner. The cytotoxicity of A771726 was not detected during the time course and dose range. A771726 (0.1, 1, 10 mol/L) significantly inhibited the expression of iNOS mRNA and iNOS protein in PMФ from CIA rats. CONCLUSION: A771726 (0.1, 1, 10 mol/L) can inhibit the transcription of iNOS mRNA in PMФ from CIA rats, and reduce the translation of iNOS protein, which leads to suppressing the secretion of NO. And the suppression is not related to the cytotoxicity of A771726.
    Effect of licorice extract on cyclosporine pharmacokinetics in rats
    ZHU Su-yan, HU Yi-jiang, CHEN Jiang-fei, XU Ping, LONG Zai-hao
    2011, 16(9):  971-974. 
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    AIM: To study the effect of licorice extract on cyclosporine pharmacokinetics in rats. METHODS: Experimental rats were randomly divided into the control and test groups which were administrated respectively with normal saline and extract of licorice. After pretreated with extract of licorice (0.5 g/kg, once daily) for 7 days, cyclosporine was given to the rats by intragastric administration in the 8th day. Whole blood cyclosporine concentrations were measured by a fluorescence polarization immunoassay (FPIA). Pharmacokinetic parameters between two groups were compared. RESULTS: There were no significant differences between the two groups in the main pharmacokinetic parameters of cyclosporine, such as Cmax,tmax,t1/ 2,AUC0-48 h,AUC0-∞,MRT,CL/F,V/F(P>0.05). CONCLUSION: The results suggest that treatment with extract of licorice (0.5 g/kg, once daily) for 7 days did not affect the pharmacokinetics of cyclosporine in rats.
    HMGA2 play important roles both in tumorigenesis and angiogenesis
    LV Ying-hui, GONG Yu-hua, DIAO Yong, XU Rui-an, WANG Qi-zhao
    2011, 16(9):  975-980. 
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    AIM: To analyze the roles of high mobility group A2 protein (HMGA2) in tumorigenesis and angiogenesis. METHODS: 5 siRNAs targeting HMGA2 gene (HMGA2 siRNA1-5) were designed, synthesized, and transfected into cells using Lipofactamine 2000. MTT assay, transwell assay and tube formation assay were applied to evaluate the effects of these siRNAs on cancer cells (SPC-A1 and Hela) and endothelial cells (ECV-304 and HUVEC). RESULTS: HMGA2 siRNA1, 3 and 5 inhibited the growth of all the cell lines that were tested. Among these siRNAs, HMGA2 siRNA5 show the best inhibition effect. The relative growth ratios were 63.2%±6.5% (P<0.01), 86.8%±3.5% (P<0.01), 58.5%±6.3% (P<0.01), and 60.3%±7.3% (P<0.01) for Hela, SPC-A1, EVC-304 and HUEVC cells, respectively. Furthermore, interfering the expression of HMGA2 affected the growth, migration, and tube formation of endothelial cells (P<0.01). CONCLUSION: HMGA2 protein plays important roles both in tumorigenesis and angiogenesis.
    Effects of prazosin and phenylephrine on the proliferation and apoptosis of rat hepatic stellate cells
    CHEN Meng, MA Yong
    2011, 16(9):  981-985. 
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    AIM: To investigate the effects of agonist and antagonist of radenoreceptor (α1-AR) on the proliferation and apoptosis of rat hepatic stellate cells (HSC-T6). METHODS: After the drug was administered to the cultured HSC-T6; MTT assay was used to α1-evaluate the proliferation of HSC-T6; ELISA assay was used to evaluate the produce of cAMP in HSC-T6; flow cytometer (FCM) was used to test the apoptosis of HSC-T6; the expression of nuclear factor-κBp65 (NF-κBp65) protein was detected by immunocytochemical technique. RESULTS: In the in vitro experiments, phenylephrine (10-5,10-7,10-9 mol/L) significantly decreased the produce of cAMP in HSC-T6, promoted HSC-T6 proliferation, enhanced the expression of NF-κBp65 protein and inhibited the apoptosis of HSC-T6, on the contrary to the antagonist prazosin (10-5,10-7,10-9 mol/L) of α1-AR. CONCLUSION: Phenylephrine can promote proliferation and inhibit apoptosis of the cultured HSC-T6, while prazosin has opposite effect. Its mechanism might be associated with the α1-adenoreceptor by meditating the produce of cAMP and the expression of nuclear factor kappa Bp65 in HSC-T6.
    Pioglitazone attenuates cognitive impairment induced by intracerebroventricular streptozotocin injection in mice and underlying mechanisms
    WANG Wei-ping, TANG Su-su, XU Wen-ke, ZHANG Ting-ting, WANG Ping-jun, HONG Hao
    2011, 16(9):  986-991. 
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    AIM: To investigate the effects of pioglitazone on the cognitive impairment induced by intracerebroventricular streptozotocin injection in mice and underlying mechanisms. METHODS: Streptozotocin (0.5 mg/kg) was intracerebroventricularly injected to induce cognitive impairment in mice. Pioglitazone was administered through a gastric tube every day for consecutive 20 days. The cognition function was evaluated by Morris water maze test and Y maze test. The Ach, AchE and ChAT of the hippocampus and cortex, and the blood glucose level in mice were determined. RESULTS: Pioglitazone (9 mg·kg-1·d-1, 18 mg·kg-1·d-1) significantly decreased the escape latency in visible platform test, increased the time spent in the platform quadrant in the spatial probe test, and significantly increased the correct number in Y maze test. Pioglitazone also significantly increased Ach levels and ChAT activity, and decreased AchE activity in hippocampus and cortex of mice. The difference in the level of blood glucose was not observed among groups. CONCLUSION: Pioglitazone may improve the cognition impairment induced by intracerebroventricular streptozotocin injection through the elevation of Ach levels that results from the decreased activity of AchE and increased activity of ChAT.
    Effect of proanthocyanidins from grape seeds on c-Jun and c-Fos expression in colon tissues of recurrent colitis rats
    WANG Yan-hong, DING Yi-lan, YANG Xiao-lai, GEI Bin, LU Li, ZHANG Bao-lai, YU Hong-jian, LIU Dan, WU Yong-jie
    2011, 16(9):  992-997. 
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    AIM: To investigate the effect of proanthocyanidins from grape seeds (GSPE) on c-Jun and c-Fos expression in colon tissues of recurrent colitis rats. METHODS: Wistar male rats were randomized divided into six groups: normal control group, model control group, Sulfasalazine (SASP) group, and the 3 GSPE treatment groups. Rats were intragastrically administered different doses of GSPE (100, 200, and 400 mg/kg) per day for 7 days after recurrent colitis was twice-induced by TNBS-50% ethanol. Rats were killed after GSPE treatment 7 days. The colonic injury and inflammation were assessed by macroscopic and microscopic damage scores and myeloperoxidase (MPO) activity. The expression levels of c-Jun and c-Fos in the colon tissues were measured by enzyme-linked immunosorbent assay methods. RESULTS: Compared with the model group, the macroscopic and microscopic damage scores and the activity of MPO were significantly decreased in GSPE dosage group. Moreover, the expression levels of c-Jun and c-Fos in the colon tissues were significantly decreased. CONCLUSION: GSPE can inhibit the expression of c-Jun and c-Fos in the colon tissues of the recurrent colitis rats.
    Comparasion of anti-platelet aggregation and PAF decrease effect among EGB,Asprin and Plavix
    WANG Ru-wei, LV Shen, HUANG Li, XU Lu, DONG Zhi
    2011, 16(9):  998-1001. 
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    AIM: To compare the effect of anti-platelet aggregation function and the PAF's contect among the EGB preparation,Asprin and Plavix. METHODS: Experiment in vivo was used to observe the platelet aggregation effect induced by AA,ADP,PAF among the EGB preparation,Asprin,Plavix. RESULTS: Compared with saline group,EGB could significantly inhibit the platelet aggregation induced by AA,ADP,PAF (P<0.05, P<0.01), reduce the PAF's content in serum(P<0.05); Asprin could significantly inhibit the platelet aggregation induced by AA (P<0.01); Plavix could significantly inhibit the platelet aggregation induced by ADP (P<0.01); Asprin and Plovix had no significantly different on PAF's content(P>0.05). CONCLUSION: EGB has anti-platelet aggregation function, and can reduce the PAF's content in serum.
    Effect of propofol on serum TNF-α and IL-1β in rabbit with acute lung injury induced by oleic acid
    JIANG Liu-ming, JIN Jian-guo, ZHU Qing, JI Wei, LIN Li-na
    2011, 16(9):  1002-1005. 
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    AIM: To observe the effects of propofol on serum TNF-α, IL-1β in rabbit with acute lung injury (ALI) induced by oleic acid (OA) and explore its possible protective mechanism and provide evidence for the choice of anesthesia drug in clinical anesthesia. METHODS: Twenty four health Japanese white rabbits were randomly divided into three groups (n=8): control group (group Ⅰ), model group (groupⅡ) and propofol treatment group (group Ⅲ). The rabbits in group Ⅱ and Ⅲ were injected oleic acid (OA) (0.08 mL/kg) by marginal veins of ear to establish ALI models. The rabbits of group Ⅲ were injected propofol (8 mg·kg-1·h-1) with pump, while group Ⅰ and group Ⅱ were injected normal saline (0.8 mL·kg-1·h-1) to end of the experiment after establishing the ALI models successfully. The concentration of TNF-α and interleukin-1β in serum were detected by ELISA at the points of propofol or normal saline infusion (T0), 1 h after administration (T1), 2 h after administration (T2), 3 h after administration (T3), 4 h after administration (T4), and blood gas analysis of them had been performed to calculate the PaO2/FiO2 Ratio. RESULTS: The concentrations of TNF-α and interleukin-1β in serum in group Ⅰ had no difference at different points (P>0.05). The concentration of TNF-α began to increase at T1, reached to peak at T2 and decreased at T3, T4, but still higher than those of T0 (P<0.05). The concentrations of TNF-α in group Ⅱ increased more obviously than those of group Ⅰ(P<0.05) and were lower in group Ⅲ than those of group Ⅱ (P<0.05) at the corresponding time point. Compared with T0 the concentrations of interleukin-1β in groupⅠbegan to increase at T1, reached to the peak at T4 (P<0.05) and were higher than those of group Ⅰ at the corresponding time points (P<0.05), increased lowerly in group Ⅲ than those of group Ⅱ(P<0.05). The oxygenation index at different time points had no significant change in group Ⅰ, decreased gradually after establishing the ALI models successfully in group Ⅱ and Ⅲ, were lower in group Ⅱ and Ⅲ than those of group Ⅰ (P<0.05), while decrease less in group Ⅱ than group Ⅲ. CONCLUSION: Propofol can significantly decrease the concentrations of serum TNF-α and IL-1β and obviously improve the oxygenation index of rabbits with ALI, has a possible protective effect of ALI induced by oleic acid.
    Meta-analysis of flurbiprofen on preemptive analgesic effect
    ZHANG Xu-tong, HUANG Zhi-lian, LI Xing-wang, LI Jun
    2011, 16(9):  1006-1011. 
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    AIM: Meta analysis of preoperative use of flurbiprofen on postoperative analgesia efficacy and safety. METHODS: 15 articles were sieved into the pump out of according to set a comprehensive search of the database search methods and research into the proposed standard from 267 documents, applications RevMan 5.0 software into the pump after the literature 4 h, 24 h two time points Meta-analysis of VAS score. RESULTS: 15 articles of the heterogeneity test showed the results of trials was significantly (P<0.05), select the random effects model analysis. Meta analysis showed that the forest plan: post- operative 4 h, 24 h of VAS combined effect of the amount of test score were statistically significant in analgesic effect between flurbiprofen group and control group (P<0.05). The number of patients in the combined adverse effects of the amount of testing was not statistically significant, still could not believe that flurbiprofen group and control group differences in adverse reactions. CONCLUSION: The available clinical data indicate that preoperative use of flurbiprofen can reduce postoperative pain, patients still can not believe that could reduce the incidence of adverse reactions.
    Pharmacokinetics of levobupivacaine for brachial plexus block in pediatric patients
    TANG Xiao-li, WANG Cheng-hai, CUI Xiao-ning, SUN Kao-xiang, SHANG Shu-jun, SHAO Wei
    2011, 16(9):  1012-1015. 
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    AIM: To evaluate the clinical pharmacokinetics of levobupivacaine for brachial plexus block in pediatric patients. METHODS: 9 pediatric patients,undergoing elective upper shoulder surgery,were injected with levobupivacaine 0.375﹪(0.4 mL/kg)for interscalene brachial plexus block.The plasma concentration of levobupivacaine were determined at 10,20,30,45,60,90,120,180,240,360,480 and 840 min after injection,and the pharmacokinetic parameters were calculated with 3P97 software package. RESULTS: The plasma concentration-time curve was fitted to a two-compartment model,and the main pharmacokinetic parameter such as t1/2β,tmax and Cmax was (4.77±0.52),(0.28±0.14) h and (1.02±0.22) mg/L. CONCLUSION: Levobupivacaine 0.375% can be used for brachial plexus block in children safely,and its clinical pharmacokinetics is fitted to a two-compartment model.
    Therapeutic effects of aripiprazole and olanzapine on the patients with first-episode acute schizophrenia and their influence on plasma prolactin level
    WU Xiao-li, WANG Ji-hui, ZHONG Zhi-yong, HAN Zi-li
    2011, 16(9):  1016-1020. 
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    AIM: To study the efficacy on first-episode acute schizophrenia treated with aripiprazole and olanzapine and the effect on plasma prolactin level. METHODS: 65 inpatients with first-episode acute schizophrenia were divided into either olanzapine group[n=42, M21, F21; age(23.9±6.6)year] or aripiprazole group[(n=23, M11, F12; age(23.7±7.2)year] for 4 week treatment. The plasma prolactin level, the Positive and Negative Syndrome Scale(PANSS) and clinical global impression-global improvement(CGI-I) were measured before and after 4 week treatment. RESULTS: The score of PANSS (59±13)after therapy in olanzapine group was significantly lower than that before therapy (103±15) (P<0.01). The score of PANSS (60±18)after therapy in aripiprazole group was significantly lower than that before therapy (101±13) (P<0.01). After therapy, there was no significant difference(P>0.05) in the CGI-I score between the two groups.The difference of negative symptoms and general psychopathological sub-scale scores changing from base to end between the two groups was statistically significant(P<0.01). Compared with the prolactin baseline level (547±382) uIu/mL,the plasma prolactin level (418±362) uIu/mL in olanzapine group was significantly decreased after treatment,and there was no difference. Compared with the prolactin baseline level (351±299) uIu/mL, the plasma prolactin level (123±114) uIu/mL in aripiprazole group was significantly decreased after treatment,and there was significant difference(P<0.01). CONCLUSION: The therapeutic effects were similar in the aripiprazole and olanzapine group for first-episode acute schizophrenia.Olanzapine is better for the general psychopathological symptoms,and aripiprazole is better for the negative symptoms.Aripiprazole maybe decrease the plasma prolactin level of first-episode acute schizophrenia.
    Effects of single-dose of parecoxib with fentanyl on postoperative intravenous analgesia in children with four limbs orthopaedics operation
    QIN Pei-shun, CAI Ming-yang, LI Jun, WANG Jian-guang, LIAN Qing-quan
    2011, 16(9):  1021-1025. 
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    AIM: To investigate the analgesic effect and safty of patient controlled intravenous analgesia (PCIA) by using fentanyl in association with Parecoxib after pediatric orthopaedics operation. METHODS: 84 ASA Ⅰ children undergoing four limbs orthopaedic operation were randomly divided into 4 groups: A, B, C, D. General anesthesia was induced by fentanyl 3 μg/kg, cisatracurium 0.2 mg/kg and propofol 3 mg/kg, children in each group except group A were administered with different single dosage of Parecoxib intravenously after intubation (group B 0.5 mg/kg, group C 1.0 mg/kg, group D 1.5 mg/kg respectively). Continuous fentanyl was infused postoperatively for PCIA within 48 hours. (continuous infusion 0.1 μg·kg-1·h-1, bolus injection 0.05 μg/kg, lockout interval 7 mins). Any children with pain score >3 were administered with a bolus injection (“press”) by a nurse. The vital signs(HR, RR, BP), SpO2, score of pain and sedation, degree of satisfaction, total dosage of fentanyl, frequency of press (D1), frequency of effective press (D2), adverse reactions were recorded postoperatively at 0.5 h, 1 h, 2 h, 4 h, 8 h, 24 h and 48 h respectively. RESULTS: (1) The pain score of group A was higher at 0.5 h, 1 h, 2 h, 4 h, 8 h compared with group C, as well as higher at 0.5 h, 1 h, 2 h, 4 h compared with group D. The pain score of group B was higher at 0.5 h, 1 h, 2 h compared with group C, as well as higher at 1 h, 2 h, 4 h compared with group D. (P<0.05)(2)The sedation score of group A was lower at 1 h compared with group C and D, and the sedation score of group B was lower at 0.5h and 1h compared with group C and D(P<0.05). (3) The total dosage of fentanyl and the total times of press of group A and B was higher compared with group C and D(P<0.01). (4)The incidence of postoperative adverse reactions in group A was higher compared with C and D, and the incidence of nausea and vomiting in group C was higher compared with group B(P<0.05). CONCLUSION: The intravenous single-dose of Parecoxib followed by fentanyl PCIA after padiatric orthopaedics operation is safe and can provide better analgesia. It can also reduce total dosage of fentanyl and the incidence of postoperative adverse reactions.
    Radiofrequency ablation of premature ventricular contractions with ECG like originating from the right ventricular outflow tract guided by CARTO
    JI Yuan, DING Zhi-jian, JIANG Jian-guang, LIU Zhi-ping, ZHOU Xue-jun
    2011, 16(9):  1026-1029. 
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    AIM: To assess the clinical efficacy of electro-anatomically guided mapping and radiofrequency ablation under CARTO system for frequent premature ventricularcontraction. METHODS: The CARTO electro-anatomical mapping system displays real time three dimensional chamber structure with electrical information related to signal mplitude and activation time. 22 patients with Drug refractory and frequent premature ventricular contractions were ablated under CARTO system. By preoperative and postoperative SF-36, the generally health, physical function and conduct scoring among patients after procedure were observed. RESULTS: Frequent premature ventricular contractions were successfully ablated in all 22 patients with mean 2.6±1.2 radiofrequency applications under CARTO system. 19/22 frequent premature ventricular contractions occurred in right ventricle, and 3/22 in left ventricule. After ablation, the premature ventricular contractions declined from (17932±3816) beats/24 h to (13±6) beats/24 h, and patient's symptoms almost disappeared. No recurrent case was found during following observation. The patient overall quality of life improved markedly. CONCLUSION: The CARTO electro-anatomical mapping system, referred to the electro physiologic data, may be applied in guiding the radiofrequency ablation of drug-refractory and frequent premature ventricular contractions in those patients who have no organic heart disease for its highly efficacy, safety and accurate orientation, and could significantly improve patient quality of life.
    Comparison of clinic efficacy between 99Tc-MDP and alendronate in patients with senile osteoporosis
    PAN Wei-min, WANG Shen-jian, YAN Wei-wen, XIE Quan, ZHOU Ying, WANG Chao-qun
    2011, 16(9):  1030-1032. 
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    AIM: To compare the clinical efficacy and safety of 99Tc-MDP and alendronate therapy on senile osteoporosis. METHODS: Adult patients (n=80) with senile osteoporosis were randomized into Group alendronate (n=40)and Group 99Tc-MDP(n=40), all patients were given full dosage of calcium agent and vitamin D therapy. Group alendronate (n=40) were given alendronate; Group 99Tc-MDP(n=40) were given 99Tc-MDP.After treatment,the efficacy was evaluated by the digital analog score (VAS)of the pain and detecting bone mineral density(BMD). RESULTS: After treatment,the lumbodorsal pain scores were decreased in two groups.While the efficacy of odynolysis in Group 99Tc-MDP was faster and better than that in Group alendronate(P<0.05); the BMD of two groups were increased to some extent, the peak clinical efficacy appeared at six months in Group 99Tc-MDP(P<0.05). CONCLUSION: 99Tc-MDP decreases pain more quickly and obviously,and can also increase the BMD in patients with severe senile osteoporosis. Alendronate shows higher safety in long-term treatment of senile osteoporosis.
    Clinical application of Gonadotropin-release hormone agonist (GnRH-a) down-regulation in early follicle phase combined with ovarian stimulation by human menopausal gonadotropin (HMG) protocol for patients who have decreased ovarian reserve
    YU Rong, ZHAO Jun-zhao, XIAO Shi-quan, WANG Pei-yu, LIN Jia, YANG Hai-yan
    2011, 16(9):  1033-1038. 
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    AIM: To investigate the effect of the GnRH-a down-regulation in early follicle phase combined with ovarian stimulation by HMG protocol for patients who have decreased ovarian reserve. METHODS: Clinical retrospective analysis was performed on 109 cycles in total 109 patients received IVF or ICSI treatment between May 2010 and March 2011. The 109 cycles were divided into three groups by stimulation protocol. Group A consisted of cycles with GnRH-a down-regulation protocol. Group B consisted of cycles with mild stimulation protocol. Group C consisted of cycles with GnRH-a flare-up protocol. The clinical and laboratory outcome of three groups were compared. RESULTS: The gonadotropin used in Group B was significantly less than that of Group A and C(P<0.01). The serum level of LH in Group A was significantly lower than that of Group B and C(P<0.01). Group C showed a significant higher level of E2 compared with Group A and B (P<0.01). No significant difference was observed in the number of oocytes retrieved and the rate of maturation and fertilization(P>0.05). There was no significant difference in the clinical pregnancy rate per transfer in three groups(33.33% vs 32.35% vs 36.00%, P>0.05). The cancel rate was significantly higher in Group B (34.62%) when compared with Group A (11.11%)(P=0.02), but the difference was not significant when it was compared with Group C (16.67%)(P=0.05).The first-trimester abortion rate of Group C (33.33%)was significantly higher than that of Group A (12.50%, P=0.028) and Group B (18.18%,P=0.03). CONCLUSION: GnRH-a down-regulation in early follicle phase combined with HMG protocol could reach a comparable pregnancy rate as mild stimulation protocol and GnRH-a flare-up protocol for patient with decreased ovarian reserve. Furthermore, the cancel rate and the first-trimester abortion rate could be decreased.
    Comparative study of risperidone and olanzapine on plasma non-enzyme antioxidants levels in the schizophrenic patients
    WEN Sheng-lin, CHENG Min-feng, WANG Hou-liang
    2011, 16(9):  1039-1041. 
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    AIM: To compare the effects of risperidone and olanzapine on plasma non-enzyme antioxidants levels in the schizophrenic patients. METHODS: Using randomized study, schizophrenic patients were divided into risperidone and olanzapine group respeetively for four weeks treatment, and evaluated by the Positive and Negative Syndrome Scale (PANSS). Serum levels of Albumins, Uric Acid, and Bilirubin were tested. RESULTS: (1)There were no difference between two groups about the levels of Albumins, Uric Acid, and Bilirubin before treatment and after 4 weeks treatment (P>0.05). The levels of Albumins and Bilirubin after 4 weeks treatment in risperidone group were lower than those before treatment (P<0.05). The levels of Bilirubin after 4 weeks trea tment in olanzapine group were lower than tho se before treatment (P<0.05).(2)There were no difference between two groups about the effective rate (P>0.05). CONCLUSION: Plasm a non-enzy meantioxidants levels in the schizophrenic patients changed after treatment, and there are no signif-icant differences in the effects of rispe ridone and olanzapine on plasma non-enzy me antiox idants levels.
    The control research of Bupropion combined with Lithium Carbonate in the treatment of bipolar depression
    SHEN Zhong-xia, QIAN Ming-cai, SHEN Xing-hua, CHEN Hai-zhi, LIN Min
    2011, 16(9):  1042-1046. 
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    AIM: To explore the efficacy and safety of Bupropion combined with Lithium Carbonate in the treatment of bipolar depression. METHODS: An open prospective randomized study was applied in this research which lasted 8 weeks. 78 inpatients meet the diagnosis criteria of DSM-IV were divided into two groups, one group(the research group, n=40) were treated with Bupropion combined with Lithium Carbonate, the other group(the control group, n=38) were treated with Lithium Carbonate only, HAMD-17 was applied to evaluate the efficacy on the baseline and the end of 1st, 2nd, 4th, 8th week,the BRMS was applied to evaluate the mania state, while the TESS and laboratory tests were applied to evaluate the side effects. RESULTS: HAMD scores of both group declined significantly at the end of 4th and 8th week respectively (P<0.01), but there were no significant difference between two groups(P>0.05). HAMD scores of research group were lower than those of control group at the end of 1st, 2nd week (P<0.05). There were no significant difference at the end of 8th week of remission rate and response rate between two groups(90% vs 89.5%,62.5% vs 60.5%,P>0.05), while the research group had a greater rate at the end of 2nd week(30% vs 10.5%, 20% vs 2.6%,P<0.05). There were no significant difference in side effects and cases switching to mania between two groups. CONCLUSION: Either Bupropion combined with Lithium Carbonate or Lithium Carbonate only would be effective and safe for bipolar depression, but the former can cut down the initial time to become effective and would not increase the risk of turning to mania.
    Study of sedation effect with dexmedetomidine on patients after general anaesthesia
    CAI Chang, GUO Jian-rong
    2011, 16(9):  1047-1051. 
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    AIM: To observe the safety and the appropriate amount of sedation of dexmedetomidine on the recovery period after general anesthesia. METHODS: Sixty patients undergoing abdominal gynecological surgery after general anesthesia, aged 40-55 yrs, weight 50-75 kg, the operation time between 1-2.5 h. Patients were induced and maintained according to the same kilogram of body weight, then sent into the recovery room after surgery. They were randomly divided into four groups: Saline control group, D1 group: dexmedetomidine group 0.2 μg/kg, D2 Group: dexmedetomidine group 0.4 μg/kg, D3 Group: dexmedetomidine group 0.6 μg/kg. The blood pressure, heart rate, respiration rate, pulse oxygen saturation and Ramsay sedation scores were monitored before(T1) and after using the drugs 5 min(T2), 30 min(T3), before(T4) and after tracheal extubation(T5), and leaving room(T6). Blood gas was recorded before(T1) and after using the drugs 30 min(T3), and leaving room(T6). Time of extubation and leaving room, then sleep, bradycardia, hypotension and other side effects were observed. RESULTS: Compared with before administration, the blood pressure and heart rate decreased in the three groups after administration(P<0.05). The blood pressure and heart rate in D2 Group and D3 Group were lower than the other groups at T2, T4-T6(P<0.05). RS in NS Group and D1 Group were higher than D2 Group and D3 Group (P<0.05). OAAS and BIS in D3 Group were lower than other groups. Ramsay sedation scores in D3 Group were higher than the other groups (P<0.05). D3 Group had the higher risk back to sleep and bradycardia (P<0.05). CONCLUSION: It is safe that DEX is used in patients with sedation during the recovery period after general anesthesia. It improves the quality of awakening.
    Determination EC50 of sufentanyl in preventing rocuronium induced withdrawal movements
    LIN Xian-ju, CHEN Ling-yang, XIANG Hai-fei
    2011, 16(9):  1052-1056. 
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    AIM: To determine the effect-site target concentration (Ce) of sufentanyl at which there was 50% probability of preventing movement from pain in response to the injection rocuronium(EC50). METHODS: Fifty-three ASA Ⅰ patients scheduled for general anesthesia were divided into male group(n=27) and femal group(n=26)according gender.Anesthesia was induced with a propofol target-controlled infusion(TCI Marsh model) and sufentanyl TCI(Bovill model).Effect-site target concentration of propofol was 2.8 μg/mL.Ce of sufentanyl for the first patient started st 0.15 ng/mL.Ce of sufentanyl for each subsequent patient by the Dixon up-and-down method with an interval of 0.02 ng/mL. After both drugs reached target concentration,rocuronium 0.8 mg/kg was administered and the pain response wan observed. RESULTS: The EC50 of sufentanly for preventing rocuronium induced withdrawal movements was (0.080±0.023),(0.103±0.019) ng/mL, respectively in male group and female group. From probit analysis, the EC50 of sufentanly in male group and female group was 0.071 ng/mL(95% confidence limits 0.051-0.085 ng/mL), 0.098 ng/mL(95% confidence limits 0.085-0.108 ng/mL)and the EC95 was 0.103 ng/mL(95% confidence limits 0.087-0.195 ng/mL), 0.120 ng/mL(95% confidence limits 0.109-0.176 ng/mL). EC50 of sufentanly was significant higher in female group than that in male group. CONCLUSION: It is effective to prevent the movement from pain in response to the injection rocuronium with sufentanyl by TCI,and EC50 of sufentanly is significant higher in female patients than that in male patients.
    Effect of different doses of tropisetron in postoperative nausea and vomiting
    ZHANG Hang, ZHANG Fan, LI Feng
    2011, 16(9):  1057-1058. 
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    AIM: To study the analgesic effect of different doses of tropisetron in preventing postoperative nausea and vomiting. METHODS: ASA grade Ⅰ-Ⅱ score of 150 cases, which was admitted for elective thoracic surgery in our hospital from January 2005 to December 2010, were divided into A, B, C three groups, n=50, A group using the analgesia adding 5 mg tropisetron, B group using the analgesia with 10 mg tropisetron, C group using 0.9% saline, compared the postoperative nausea and vomiting efficacy and adverse drug reactions of three groups of patients. RESULTS: A, B groups had no significant efficacy differences in the prevention of postoperative nausea and vomiting, but were significantly better than C group, P<0.05. The adverse reactions of A, B groups were significantly more than C Group, P<0.05, but can be tolerated.P<0.05. A, B groups of adverse reactions was significantly more than Group C, P<0.05, but can be tolerated. CONCLUSION: The analgesic effects in preventing postoperative nausea and vomiting of 5 mg, 10 mg tropisetron are more satisfied, and adverse reactions can be tolerated.
    Polymorphism of CYP2D6 gene and the influence on the metabolism of metoprolol
    XIONG Dan, XIONG Yu-qing
    2011, 16(9):  1059-1064. 
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    As one of major cytochrome P450s, CYP2D6 is responsible for the metabolism of many important drugs. Genetic polymorphism of CYP2D6 is the basis of lager interindividual and racial variability in the metabolism of drug. Metoprolol is a selective β1-adrenoceptor antagonist, there is an obvious individual difference in clinic. It is metabolized in the liver, in vivo data indicate that approximately 70% of the metabolism of metoptolol depends upon CYP2D6. Genetic polymorphism of CYP2D6 have a great influence on the metabolism of metoprolol. Here we summarize the polymorphism of CYP2D6 gene and the influence on the metabolism of metoprolol.
    Mechanism of pharmacogenetics on drug withdrawal
    CHEN Wang-qing, ZHANG Wei
    2011, 16(9):  1065-1071. 
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    Drug safety, pharmacokinetics and pharmacodynamics are the most important indicators that determine whether the candidate compounds can can be developed into drugs. The listed drugs withdrawn from the market were often of serious adverse drugs reactions. Drugs in different individuals/groups may have different pharmacokinetics and pharmacodynamics, and even cause adverse drug reactions(ADR). While pharmacogenetics focuses on the influence of genetic factors on both. To clarify the mechanism of abnormal reactions caused by genetic variations, not only enhance drugs safety, with a more comprehensive description of the indications, but also could rewrite the fate of drugs to be withdrawn, which can make it better service to humanity.
    Anti-inflammatory mechanism of estrogens
    SUN Ai-jing, XU Xian-xiang, XU Rui-an
    2011, 16(9):  1072-1076. 
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    As an important hormone in vivo, estrogen is of a variety of biological activities beyond a modulator of reproductive system. It has been reported that anti-inflammatory effects of estrogens are obvious, and their mechanisms are very complicated. The present paper gives an overview of the anti-inflammatory mechanism of estrogens.
    Trastuzumab associated cardiac adverse effects in breast cancer
    SHENG Li-ming, DU Xiang-hui
    2011, 16(9):  1077-1080. 
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    Trastuzumab has been used widely for the treatment of women with human epidermal growth factor receptor-2(HER2) overexpressing breast cancer in the early and advanced disease. However, cardiac toxicity has emerged as a rare but potentially serious risk that limits its therapeutic potential in a subset of women.Asymptomatic decreasing left ventricular ejection fraction (LVEF) was a common complication and generally reversible and manageable.The increasing risk of trastuzumab-induced cardiac toxicity may be influenced by factors such as age, hypertension and the use of anthracyclines-based chemotherapy.Rigorous cardiac monitoring should be performed for all patients receiving trastuzumab currently in clinic.