Table of Content

Volume 14 Issue 8
26 August 2009

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In vitro prediction of CYP-mediated inhibitory drug and drug interaction

GUO Jian-jun, ZHAO Hua, WANG Jing-jing

2009, 14(8):  841-848. 

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Cytochrome P450 (CYP)-mediated inhibitory drug and drug interaction(DDI)potential must be well evaluated during the course of drug discovery and development .It is not uncommon that drug inhibition of CYPs may lead to severe prescribing restrictions, or withdrawal of drugs from market .Not only may this kind of DDI jeopardize patients' safety , but also cause huge financial losses for drugmakers. In vitro strategy , due to its simplicity and high throughput possibility , has been routinely used to evaluate the potential of CYP-mediated DDI .However , in vitro data only provide indirect information. For this reason, in vitro inhibition data are frequently used to predict in vivo CYP-mediated inhibitory DDI potential .Further, such predicted data can be taken into consideration in designing clinical trials.In recent years, this field has undergone rapid development .The purpose of this re-view was to present the fundamentals, predictive strategies, and essential considerations in predicting in vivo DDI properties from in vitro data.

Experimental study on the effects of liver cytochrome protein 450 (CYP450) induced by panax notoginsenoside injection in rats

LI Xiao-yu, LIU Gao-lin, ZHOU Jia-chun, QIAN Gang, GAO Jun-wei, SUN Bo, GUO Yan-kun

2009, 14(8):  849-854. 

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AIM: Enzymes probes were employed for the study on the effects of liver CYP450 induced by panax notoginsenoside injection (PNSi) in rats. METHODS: PNSi was intravenous administered to rats for 5 weeks at the dosage of 20 mg°kg^-1°d^-1. Then 5.0 mg/kg dosage of nimodipine or 20.0 mg/kg dosage of warfarin sodium was given to rats via intrave-nous or intragastric administration, respectively at the last time of PNSi .HPLC wasemployed for the determi-nation of nimodipine and warfarin sodium in rat plasma .Pharmacokinetic parameters which simulated by DAS software were used for the evaluation on the effects of CYP3A4, CYP2C9 and CYP1A2 induced by PNSi . Two-sides of students test was used for datum analysis. RESULTS: Sensitive, rapid and specificity HPLC method was developed and validated for the determina-tion of nimodipine and warfarin in rat plasma success-fully .There were no markedly changes of pharmacoki-netic parameters of nimodipine or warfarin in rats in-duced by PNSi .However, the AUC and clearance of nimodipine displayed the tendency of increasing or de-creasing, respectively and the t_max , t_1/2 and AUC of warfarin sodium showed the tendency of increasing after intravenous administration of PNSi for a long time. CONCLUSION: PNSi showed potential inhibitory effect on the activities of CYP3A4, CYP2C9 and CYP1A2.Potential drug-drug interaction should be more cared when PNSi was co-administered with nimo-dipine or warfarin sodium in clinic .

Effects of realgar bioleaching solution on the expression of MDRI mRNA and P-gp in K562/ADM cells

ZHANG Jing-hong, LI Hong-yu

2009, 14(8):  855-860. 

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AIM: To investigate the role of apop-tosis in K562/ADM cells induced by realgar bioleaching solution (RBS), and illustrate the possible molecular mechanism .METHODS: RBS was prepared by a new method of bioleaching with bacteria .The cell apoptosis was determined by annexin V/PI double staining .The expressions of MDRI mRNA and P-gp were detected by RT-PCRand flow cytometry, respectively.The parallel experiments with arsenic acid (H₃AsO₃)were conducted for comparison .RESULTS: RBS inhibited K562/ADM cells growth effectively, and the apoptosis rate of the cells by Annexin V/PI staining was obviously in-creased, the expressions of MDRI mRNA and P-gp were significantly down-regulated. With the same con-centration of As, the inducing effect of RBS was more stronger than H₃AsO₃ .CONCLUSION: RBS induces the apoptosis inK562/ADM cells. The down-regulation of MDRI P-gp expression may be the important molecular mechanisms in reversing the multi-drug resistance leukemia cells.

Application progress of thrombolytic therapy in cardiopulmonary resus-citation

JIANG Ya-bin, WANG Zhi-gang

2009, 14(8):  861-865. 

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Thrombolytic therapy was constantly re-garded as relative contraindication in cardiopulmonary resuscitation(CPR) for hemorrhage. Recent years, more and more researches indicated that it was feasible of thrombolytic therapy in CPR, as well as relatively safe and effective .This article reviews evidences and clinical applications of thrombolytic therapy in CPR, and conducts evaluations about its benefits and risks.

Expression of phospho-p38MAPK in asthmatic rats with airway remodeling the effect on proliferation of mucous cells and the regulation of budesonide

ZHENG Yang-ming, LI Chang-chong, Zhang Wei-xi, GUAN Xiao-jun

2009, 14(8):  866-871. 

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AIM: To investigate the protein ex-pression of phospho-p38MAPK in asthmatic rats with airway remodeling and its effects on proliferation of mu-cous cells and the regulation role of budesonide. METHODS: Thirty male rats were randomly divided into control group (Group C, n =10) , airway remodeling group(Group A, n=10) and budesonide treated group (Group B, n =10) .The asthmatic rat model with airway remodeling was established. The lung tis-sue was observed by Hematoxylin and eosin staining, Masson' s Trichrome stain, Periodic Acide Schiff' and immunohistochemistry staining .RESULTS: Pathological changes of airway remodeling were found under light microscope and TEM .Compared with Group A, the pathologic change in group B was relieved. The results of image analysis: compared with Group A, the total bronchial wall area(Wat) and the smooth muscle area (Wam) and the percentage of mucous cells in rat air-way epithelium were significantly decreased in Group C and Group B, but the Wat and Wam in group B were higher than those in Group C. Compared with Group A, the contents of phospho-p38MAPK protein in group B and group C were decreased .There were significant positive correlation between the contents of phospho-p38MAPK and percentage of mucous cells(n =30, r = 0.813, P<0.01) .CONCLUSION: High expression of phospho-p38MAPK might precipitate the proliferation of mucous cells in asthmatic rats. Budesonide can inhibit the expression of phospho-p38MAPK protein in the airway epithelium of asthmatic rats with airway re-modeling, by which might inhibit proliferation of mucous cells.

Expression of PTEN and the intervention effect of dexamethasone in the asthma rat model

XU Hui, DAI Yuan-rong, ZENG Wei-xian, HE Jian-bo, XIA Xiao-dong

2009, 14(8):  872-876. 

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AIM: To study the expression of PTEN and the intervention effect of dexamethasone(DXM) in the asthma rat model .METHODS: Twenty-four (200 ±10) g SD rats were randomly divided into three groups:control group(Group C) , asthma group(Group A) and DXM group(Group DXM) .The lung tissue was sampled from the left lung .The bronchoalveolar lavage fluid (BALF) was collected from the right lung .The differential count of cells in BALF was measured.The concentration of IL-13 in BALF wasmeasured by Sand-wich ELISA .The expression of PTEN protein and the changes of PTEN level in lung homogenate of each groupwere detected by immunohistochemical and West-ern blot method. RESULTS: The expression of bron-chial PTEN protein in Group C and Group DXM were 7.87±0.80, 1.80±0.23 which were higher than that in Group A(0.92 ±0.23, all P<0.01) , and the bronchial epithelial cell was the main expression cell. The expression of IL-13 in BALF of Group A was sig-nificantly increased, and which was higher than that in Group C (P<0.01) , and which in Group DXM was significantly decreased, compared with Group A, there was significant difference .There were significantly negative correlations between the expression of PTEN protein in lung homogenate and the level of IL-13 in BALF(r =-0.675, P<0.01) .CONCLUSION: The PTEN chief expression cell was tracheal epithelial cell .The expressions of PTEN protein in Group A were decreased.PTEN could decrease the expression of Th₂ factor.Dexamethasone could promote the expression of PTEN,which may be an important mechanism of inhib-iting asthmatic airway inflammation formation.

Comparison on in vitro antibacterial and anti-inflammation effects of the different decoctions of Dangguiliuhuang tang

ZHONG Zheng-ling, XIE Hai-tang, ZHANG Li-yan, TONG Jiu-cui, LI Jun, TIAN Wei-yi, LIANG Guang-yi, XIAN GUI-hua

2009, 14(8):  877-882. 

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AIM: To compare the difference of in vitro antibacterial and anti-inflammatory effects of different decoctions of Dangguiliuhuang tang. METHODS: The antibacterial effects of the two kinds different decoctions were compared by the agar bridge meth-od and test tube method .The anti-inflammatory effects were compared by ear swelling test in mice. RESULTS: The antibacterial effects of the two kinds of decoctions have no significance, but the inhibition ratio of inflammation of single decoction was higher than that of combination decoction. CONCLUSION: The re-search can provide for the reference on development of Dangguiliuhuang tang .

Expression and significance of neutrophil-activating peptide-2 in asthma rat

ZHOU Hua-fei, LUO Dong-jiao, TONG Xia-sheng, GUO Hai-yuan, RUAN Zheng-ying, YE Hui

2009, 14(8):  883-887. 

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AIM: To observe the effect of dexam-ethasone on the expression of neutrophil-activating pep-tide-2 (NAP-2)in neutrophil and explore the role of neutrophil in asthma rat .METHODS: In this experi-ment , the model rats of asthma were randomly divided into three groups on average, including asthma group, control group and dexamethasone treated group.Blood neutrophil were isolated and purified,the expression of NAP-2 protein in bronchial wall and in blood neutro-phil was detected by immunohistochemical assay .RESULTS: The expression of NAP-2 protein in blood neu-trophil from asthma group (0.198 ±0.016, optical density)was significant higher than that from control group (0.079 ±0.015, optical density)(P<0.01). And the expression of NAP-2 protein in blood neutro-phil from dexamethasone treated group (0.135 ± 0.021, optical density)was lower than that from asth-ma group, but was higher than that from control group (all P<0.01).While in bronchial wall , the expression of NAP-2 protein in asthma group (0.226 ±0. 050, optical density)was significant higher than that in control group (0.140±0 .012, optical density)(P<0.01).And the expression of NAP-2 protein in dex-amethasone treated group (0.175 ±0.028, optical density)was lower than that in asthma group, but was higher than that in control group (P<0.01).There were significant positive correlation between NAP-2 protein expression in blood neutrophil and the number of NEU in bronchoalveolar lavage fluid(n =29, r = 0.334, P<0.05).CONCLUSION: The levels of NAP-2 protein in blood neutrophil were increased in rat asthma .Neutrophil may be involved in asthma inflam-mation via NAP-2.The decreased inflammation of asth-ma by dexamethasone may partly depend on suppressing the synthesis of NAP-2 protein, which may be correlat-ed with the influx of neutrophil into lung tissue .

Comparison on in vitro antibacterial and anti-inflammation effects of the different decoctions of Dangguiliuhuang tang

ZHONG Zheng-ling, XIE Hai-tang, ZHANG Li-yan, TONG Jiu-cui, LI Jun, TIAN Wei-yi, LIANG Guang-yi, XIAN GUI-hua

2009, 14(8):  888-890. 

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AIM: To compare the difference of in vitro antibacterial and anti-inflammatory effects of different decoctions of Dangguiliuhuang tang. METHODS: The antibacterial effects of the two kinds different decoctions were compared by the agar bridge meth-od and test tube method .The anti-inflammatory effects were compared by ear swelling test in mice. RESULTS: The antibacterial effects of the two kinds of decoctions have no significance, but the inhibition ratio of inflammation of single decoction was higher than that of combination decoction. CONCLUSION: The re-search can provide for the reference on development of Dangguiliuhuang tang .

Inhibition of Dengzhanxixin injection on rat liver microsomal CYP3A

HAN Yong-long, YU Qi, MENG Xiang-le, LI Dan, BIAN Ka, GUO Cheng

2009, 14(8):  891-895. 

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AIM: To investigate the inhibition of Dengzhanxixin injection on rat liver microsome CYP3A in vitro .METHODS: The rat liver microsomes were incubated with different doses of Dengzhanxixin injection at the present of testosterone, a specific substrate of CYP3A, whose metabolite (6β-hydroxytestosterone) in incubation systems was measuered by HPLC to esti-mate the effect of Dengzhanxixin injection on the activity of CYP3A in rat liver microsome .Ketoconazole was used as a positive control. RESULTS: In in vitro in-cubation systems, Dengzhanxixin injection has inhibition on rat liver microsomal CYP3A, the IC50 value and Ki value are 0.40%and 0.24%(V/V) , respectively . CONCLUSION: Dengzhanxixin injection which can depress CYP3A activity, is a mixed inhibitor to CYP3A.

Comparative study of combined medication on improving left ventricu-lar remodeling in renal vascular hypertension rats

ZHOU Sui-fu, LONG Xiao-feng, LIU Yu-fei, LIU Hui, LV Zhen-fang

2009, 14(8):  896-899. 

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AIM: To investigate the effect of combined medication on treating hypertension and explore its role in left ventricular remodeling in renal vascular hypertension rats (two kidney one clip hypertensive rats) . METHODS: Forty-three SD rats were randomly di-vided into 4 groups:sham group (Group A, n =10) , hypertension group (Group B, n =11) , β-B +ACEI group (Group C, n =11 bisoprolol 5 mg°kg^-1 °d^-1 and benazepril 5 mg°kg^-1 °d^-1) , ACEI +CCB group (Group D, n =11 benazepril 5 mg°kg^-1 °d^-1 and am-lodipine 10 mg°kg^-1 °d^-1) .The rats were fed for 20 weeks, blood pressure and echocardiography of rats were monitored every 2 weeks.After 20 weeks, (rats were sacrificed and the blood and hearts were collect-ed, then the concentrationsof collagen Ⅲ, collagen Ⅳ and ANF were detected by immunohistochemistry .RESULTS: Compared with Group B, the blood pressure, the concentrations of collagen Ⅲ, collagen Ⅳ and ANF in medication groups were significantly reduced. Compared with Group A, the ANF was significantly in-creased in Group B, but the ANF was not significantly increased in medication groups(P<0.05). CONCLUSION: The combined effect of benazepril and amlodipine is better than bisoprolol and benazepril in reducing blood pressure and preventing target organ .

Effects of short-term fasting on energy metabolism and arrhythmia after myocardial ischemia/reperfusion in rats

BAI Xia, GUO Zhi-hong, ZHANG Fan, FAN Shu-duo

2009, 14(8):  900-905. 

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AIM: To observe the effects of short-term fasting (STF) on myocardial energy metabolism and arrhythmia after myocardial ischemia/reperfusion (I/R) in rats. METHODS: 80 SD ratswere randomly divided into 5 groups: normal control group, I/R group, STF group, amiodarone group, combination group (STF +amiodarone) .The I/R model of SD rats was established by deligation left anterior descending coronary artery 30 min, reperfusion 120 min .The stan-dard limbs Ⅱlead electrocardiogram (ECG) was moni-tered and the occurrence condition of ventricular arrhythmia (VA) was recorded. The activities of cyto-chrome-oxydase(COX) and H⁺-ATPase were detected, after the myocardial mitochondria was extracted .The high energy phosphates (ATP, ADP and AMP) levels in myocardium were measured by HPLC.The activities of Na⁺/K⁺ -ATPase and Ca²⁺/Mg²⁺ -ATPase in myo-cardium tissues were determined.The protection was observed to myocardium, and the resultswere compared with the protection in amiodarone group.RESULTS: Compared with I/Rgroup, the onset of ventricular pre-mature contraction (VPC) was delayed markedly (P< 0.01) , the duration of VPC was shorted (P<0.01) , the incidences of ventricular tachycardia (VT) and ventricular fibrillation (VF) were decreased (P<0.05) in STF group.The activities of COX, H⁺ -AT-Pase, Na⁺/K⁺ -ATPase, Ca²⁺/Mg²⁺-ATPase and the contents of myocardial adenine nucleotide were de-creased signifcantly in I/R group.STF could increase the levelsof COX, ATPase and myocardial adenine nu-cleotide contents (P<0.01) .The myocardial protec-tive effects of the combination group was the best . CONCLUSION: STF has antiarrhythmic effect in rats, the protective action is related to the improvement of energy metabolism .

In vitro inhibitory effects of papain on platelet aggregation

FEI Xian-ming, ZHOU Yong-lie, QI Jin-wen, WU Jian-guo, QIU Lian-nv, WANG Zhen-ni

2009, 14(8):  906-911. 

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AIM: To observe the in vitro inhibito-ry effects of papain on platelet aggregation by washed platelet model, and explore the possible antithrombotic mechanism of papain .METHODS: Human washed platelets were mixed with different doses of papain. The maximal ratio of platelet aggregation induced by 5-adenosine liphosphate-disodium salt (ADP) , arachi-donic acid (AA) , collagen and thrombin, respective-ly, was measured with platelet aggregation analyzer. The expressions of fibrinogen receptor(FIB-R) and p-selectin(CD62p) on external membrane of activated platelet were determinated with flow cytometry .The changes of factin cytoskeletal structure in activated platelet were analyzed by SDS-PAGE .Platelet rich plasma(PRP) of patients with primary hypertension (PH) or acute myocardiac infarction(AMI) was treated to determinate the levels of aggregation and FIB-R ex-pression.RESULTS: Papain significantly inhibited platelet aggregation in a dose-dependent manner and reduced the levels of platelet aggregation, there was re-markably negative correlation between platelet aggrega-tion level and papain dose(P<0.01) .Papain notably inhibited FIB-R expression and decreased the levels of FIB-R expression activated by ADP in a dose-depen-dent manner.Papain reduced P-selectin expression on external membrane and lessened f-actins of platelet triggered by ADP .Papain significantly inhibited the levels of aggregation and FIB-R expression of platelets activated by ADP in patients with PH and AMI(P<0.01) .CONCLUSION: Papain can inhibit the ex-pression of fibrinogen receptor on external membrane of activated platelet and polymerization or release reac-tion, so the thrombocytic aggregation are inhibited in a dose-dependent manner, and papain has the effect of anti-thrombogenesis.

Systematic review on randomized controlled trials for treatment of ventricular premature beat(VPB) by ShensongYangxin capsule

LI Yan-hong, ZHU Huai-jun

2009, 14(8):  915-923. 

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AIM: To evaluate the curative effect difference between ShensongYangxincapsule and Con-trol Group and the safety of them on ventricular prema-ture beat (VPB) .METHODS: Meta-analysis of 21-ShensongYangxin Capsule on the parameters commonly used treatment of VPB and other research literature on drug treatment of VPB, its effectiveness and safety for homogeneity test and the combined effect size estimate. RESULTS: Homogeneity test :Clinical effectiveness of the ECG :χ²=25.20, df=17, P=0 .090;Clinical ef-fectiveness:χ²=26.10, df=11, P=0.006;Clinical effectiveness of ventricular premature beats:χ²=7.13, df=5, P=0.211;Security 1 χ²=31.14, df=20, P=0.053, Security 2χ²=30.37, df=20, P=0.064.Combined effect size estimates: Effectiveness: Clinical effectiveness of the ECG:OR affiliate=1.04, 95%confidence interval of OR was [1.00, 1.09], Clinical effectiveness: OR affiliate=1.33, 95% confi-dence interval of OR was [1.19, 1.48] , Clinical ef-fectiveness of ventricular premature beats:OR affiliate=1.25, 95 % confidence interval of OR was [1 .13, 1.39] , Security 1 :OR affiliate=0.38, 95% confi-dence interval of OR was [0.28, 0.52] , Security 2: OR affiliate=0.39, 95% confidence interval of OR was [0.29, 0.52].CONCLUSION: The treatment of VPB ShensongYangxin capsule is better than the control group, Comparison of safety is also better control group and there is a significant difference .

Pharmacokinetics and bioequivalence of two α-Lipoic acid preparations in Chinese healthy volunteers

SUN Li, YAO Xiao-dong, SU Ke-jian, SHEN Jin-fang

2009, 14(8):  924-927. 

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AIM: To develop a high performance liquid chromatography-mass spectrometry method for the determination of α-Lipoic acid in plasma , to study the pharmacokinetics of α-Lipoic acid and evaluate the bioequivalence of two preparations in healthy subjects. METHODS: A single oral dose of 200 mg α-Lipoic ac-id capsules and tablets was given to 22 healthy male volunteers according to an open randomized 2 way crossover design.Plasma concentrationsof α-Lipoic ac-id were determined by HPLC-MS method. The pharma-cokinetic parameters and relative bioavailability were calculated to evaluate the bioequivalence of the two preparations. RESULTS: The pharmacokinetic parameters of the two products were as follows:t max were (16 ±4)and (20±20)min, ρ_max were (1490±359)and (1537±290)ng/mL , AUC_0-t were (59559±18456) and (58210 ±15080)ng°mL^-1 ·min, AUC_0-∞ were (60068 ± 18556) and (58634 ± 15126) ng°mL^-1 ·min , respectively .The relative bioavailabili-ty of AUC_0-t and AUC_0-∞ were (102.97 ±18.28)% and (103.09 ±18.26)%.CONCLUSION: The re-sult demonstrated that two formations are bioequivalent by statistical analysis of variant , two one-side t-test and 90%confidential interval .

A Controlled study on ibuprofen pseudoephedrine hydrochloride and chlorpheniramine Maleate tablets and paracetamol pseudoephedrine hydrochloride and chlorphenamine maleate tablets in the treatment of upper respiratory tract infection

XUE Cheng, JIANG Jing-han, WANG Wei-hua, ZHANG Jian-chu, XIONG Sheng-dao, ZHANGWei, LIU Chun

2009, 14(8):  928-932. 

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AIM: To evaluate the efficacy and safety of ibuprofen pseudoephedrine hydrochloride and chlorpheniramine Maleate tablets for the treatment of upper respiratory tract infection. METHODS: A multi-center,double-blind, randomizde controlled and positive drug parallel trial was conducted.226 patients were enrolled and divided into two groups.Group A (112 cases)were treated with ibuprofen pseudoephedrine hydrochloride and chlorpheniramine Maleate tablets and Group B (114 cases)were treated with paracetamol pseudoephedrine hydrochloride and chlorphenamine maleate tablets.The method to take the medicine was one tablet three times a day for 3-5d.RESULTS: The total efficacy rate of Group A was 100%,with the total obvious effective rate of 98.21%;while the efficacy rate and the total obvious effective rate of Group B were 99.12%and 97.37% respectively .The results indi-cate that the difference between the efficacy rates of the 2 groups had no statistical significance (P>0.05). The occurrence rate of the adverse reaction in Group A and Group B was 20.18% and 24.79% respectively (P>0.05).CONCLUSION: Both ibuprofen pseudo-ephedrine hydrochloride and chlorpheniramine Maleate tablets and paracetamol pseudoephedrine hydrochloride and chlorphenamine maleate tablets are safe and effec-tive medicine in the treatment of upper respiratory symptoms caused by cold.

Effect of intravenous infusion of lidocaine on return of bowel function and stress response after hysterectomia surgery

WANG Jun-hui, WANG Hong-zhu, YANG Ling-jun, LI Shang-geng

2009, 14(8):  933-936. 

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AIM: To investigate the effect of intra-venous infusion of lidocaine on postoperative pain, re-turn of bowel function and stress response after hyster-ectomia surgery. METHODS: Sixty patients scheduled to undergo hysterectomia surgery were randomly divided into two groups with thirty in each group.Group L re-ceived intravenous lidocaine bolus injection of 1.5 mg/kg at induction of anesthesia, then continuous infu-sion of 1 mg°kg^-1°h^-1 intraoperatively and infusion of 100 mg plus sulfentanyl 50 mg for 48 h postperatively . Group S received an equal volume saline and infusion of sulfentanyl 100mg for 48 h postperatively .Postoper-ative pain score at rest and cough were recorded by VAS .The times of first flatus, enterocinesia were recorded and the levels of motilin, cortisol and serum glucose were measured .RESULTS: Lidocaine signifi-cantly reduced postoperative pain, nause and vomit scores.Times to first flatus, enterocinesia were signifi-cantly shorter in patients who received lidocaine .the levels of motilin were significantly higher, but the lev-els of cortisol and serum glucose were significantly low-er in Group L than in GroupS. CONCLUSION: In-travenous lidocaine relieves postoperative pain, improve bowel function through increasing plasma motilin levels and decreasing stress responses after hysterectomia sur-gery .

Analysis of deproteinized extract of calf blood (DECB) in treatment of ischemic cerebral infarction

LE Chun, XU Hai-song

2009, 14(8):  937-940. 

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AIM: To explore the application value of deproteinized extract of calf blood (DECB) in pa- tients with ischemic cerebral infarction. METHODS: 66 cases of patients with ischemic cerebral infarction were randomly divided into control group and DECB treatment group.DECB treatment group was given 30 mL DECB intravenous drip, once a day, for three weeks.Control groupwas not given DECB treatment in addtion with other treatment .The hemorheology and neurological deficits and changes in the two groups of patients were analyzed before and after treatment. RESULTS: The obvious effective rate of DECB treatment group was 72.7%, which was significantly higher than that in control group (45.5%, P<0.05) .After treatment, the whole blood viscosity (low shear) , he- matocrit and platelet aggregation in DECB treatment group were significantly lower than those in control group (P<0.05) .which were also significantly lower than pre-treatment (P<0.05) .The plasma viscosity had no statistical difference between the groups.The score of neurological deficit of DECB treatment group was significantly lower than that in control group (P< 0.05).CONCLUSION: The DECB has the exact ef- ficacy on patients of ischemic cerebral infarction.No adverse reactionswere found in clinic.It can be used in clinical practice .

Progress in effects of VDR variant mediated transcriptional regulation on its downstream target gene

LI Bao-qun, SHEN Jie, ZHOU Hong-hao

2009, 14(8):  941-945. 

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1,25-(OH)₂D₃ is an essential vitamin that belongs to steroid hormone, the principal recognized biological effect of 1,25-(OH)₂D₃, is to main-tain calcium/phosphate ion homeostasis , regulate cell growth or differentiation and prevent rickets osteomala-cia ;through its combined actionson classical endocrine target tissues including intestine, bone , and kidney , liganding of the vitamin D receptor (VDR)with1,25-(OH)₂D₃ mediates the effects of the 1,25-dihydroxyvi-tamin D3 hormone to alter a series of target gene tran-scription of downstream .In addition , VDR may play an important role in drug metabolism , transportation and therapeutic effect .Mounting epidemiological and experimental evidence also implicates 1, 25-(OH)₂D₃ as an epithelialcell anti-cancer and chemopreventative agent .The 1,25-(OH)₂D₃ ligand and several synthet-ic vitamin D analogs are known to possess potent anti-proliferative , prodifferentiation, and/or cell cycle arrest activities in epithelial cells, whereas 1,25-(OH)₂D₃ likely afford some degree of chemoprotection, another mechanism that could contribute to the antitumor activi-ty of 1,25-(OH)₂D₃ in certain cell types is induction of drug-metabolizing enzyme proteins to initiate enzy-matic detoxification of dietary xenobiotics and deleteri-ous endobiotic compounds.This article reviews the function of VDR on transcriptional regulation to drug-metabolizing enzyme and its relationship between gene polymorphisms and some diseases.

Clinical application of insulin pump and research prospects of pharmacoeconomics

LU Qiong, PENG Liu-bao

2009, 14(8):  946-950. 

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Insulin resistance and dysfunction of pancreatic beta cells are central abnormalities of diabetes, which is charactered by hyperglycemia .Continuous subcutaneous insulin infusion(CSII) is the optimization administration for diabetes at present .The clinic appli-cation of CSII and its pharmacoeconomics is discussed in the present paper.

Application progress of thrombolytic therapy in cardiopulmonary resus-citation

JIANG Ya-bin, WANG Zhi-gang

2009, 14(8):  951-954. 

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Thrombolytic therapy was constantly re-garded as relative contraindication in cardiopulmonary resuscitation(CPR) for hemorrhage. Recent years, more and more researches indicated that it was feasible of thrombolytic therapy in CPR, as well as relatively safe and effective .This article reviews evidences and clinical applications of thrombolytic therapy in CPR, and conducts evaluations about its benefits and risks.

Research progress of pharmacotherapy on delayed cerebral vasospasm after subarachnoid hemorrhage

XIONG Fang-ling, GAO Yi-lu

2009, 14(8):  955-960. 

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Delayed cerebral vasospasm (DCVS) is an important incapacitating or lethal cause after sub-arachnoid hemorrhage (SAH) , but the patho-physiolog-ical process was vague .The effective drugs of treating DCVS are particularly important including ion channel blockers or openers, endothelin synthetic inhibitor or receptor antagonist, anti-inflammatory agents, antioxi-dants, fibrinolytic agents, traditional Chinese herbs, etc. The article reviews the research progress in the preclin-ical and clinical pharmacotherapy on DCVS after SAH, and explores the applications and effects and debates about these therapeutic drugs at present .