1.Rational use of medications and risk assessment during lactation
Kai WEI ; Heng GUO ; Huawen XIN
Chinese Journal of Perinatal Medicine 2019;22(7):472-478
Pregnant and breastfeeding women are perhaps "the last true therapeutic orphans". Due to dearth of adequate research on certain medications and healthcare providers' poor knowledge of lactational pharmacology, nursing mothers are often ill-advised to give up breastfeeding or unlikely to receive appropriate treatment. Accumulating evidence-based data have shown that most medications are safe for nursing mothers. Besides safety concerns, infant's condition and maternal attitude should also be considered when making treatment decisions. Clear understanding of lactational pharmacology and risk assessment tools in breastfed infants would be beneficial to meet the medical needs of nursing mothers and promote breastfeeding.
2.Research Progress in Schisandra Chinensis Used in the Treatment of Drug-induced Liver Injury
Yangwen AI ; Weiliang LI ; Huawen XIN
China Pharmacist 2018;21(3):477-480
The main components of Schisandra chinensis are γ-schizandrin, schisandrin A,deoxyschizandrin,schisandra B, schisandrol B and so on. Schisandra contains a variety of bioactive ingredients mainly used in clinics and combined with other drugs. Many of the drugs currently used in clinical practice can cause drug-induced liver injury(DILI),which is one of the main adverse drug reactions,therefore,the clinical use of drugs for the prevention and treatment of liver damage is particularly important. In this paper, the effective components of Schisandra chinensis and their related therapeutic effects on DILI were reviewed.
3.Association of Genetic Polymorphism in ABCC2 with Cyclosporine Induced Liver Injury in Renal Transplant Recipients
Fan ZHOU ; Fei LIU ; Lei XIONG ; Airong YU ; Di DU ; Yangwen AI ; Xueyi ZHOU ; Jing YAN ; Huawen XIN
China Pharmacist 2018;21(6):1024-1028
Objective: To investigate the association between ABCC2 gene polymorphisms and cyclosporine-induced liver injury in re-nal transplant recipients. Methods: The renal transplant recipients were divided into the liver injury group and the control group. Five single nucleotide polymorphisms ( rs4919395, rs2804398, rs4148394, rs4148397 and rs3740065) of ABCC2 were detected by high-throughput technique. The genotypes and haplotypes were analyzed between the groups. Results: There were 35 patients and 182 patients respectively in the liver injury group and the control group. No significant differences in alleles and genotypes were found between the groups (P>0. 05), and the SNP haplotypes showed no significant difference between the groups (P>0. 05). Conclusion: There is no association of ABCC2 polymorphisms (rs4919395, rs2804398, rs4148394, rs4148397 and rs3740065) with the liver injury induced by cy-closporine.
4.Mechanism of Berberine in the Regulation of CYP3A4 and P-gp via PXR Signaling Pathway
Airong YU ; Weiliang LI ; Weiyu CHANG ; Yangwen AI ; Huawen XIN
China Pharmacist 2018;21(10):1711-1715
Objective: To investigate the regulation of CYP3A4 and P-gp by berberine hydrochloride ( BBR) via pregnane X re-ceptor (PXR) pathway. Methods: pLKO. 1-PXR vector, a lentivirus plasmid expressing PXR shRNA, was packaged into 293T cells. Human hepatoma (HepG2) cells were infected with the lentivirus and the cell clones stably expressing PXR shRNA were selected by puromycin according to pLKO. 1 vector characteristics. Real-time RT-PCR and Western blot were used to evaluate CYP3A4 and P-gp mRNA and protein in berberine treated HepG2 cells and PXR-silenced HepG2 cells. Results: The PXR expression in PXR silenced cells significantly decreased (P<0.01) when compared with that in HepG2 cells, while there was no significant difference (P >0. 05) in the expression of CYP3A4 and P-gp between the groups. Compared with that in HepG2 cells, the inhibition of berberine on the mRNA and protein expression of CYP3A4 and P-gp in PXR-silenced HepG2 cells was weakened (P<0. 05 or P<0. 01). Conclu-sion: Berberine can regulate the expression of CYP3A4 and P-gp via PXR signaling pathway, while it is not the only one.
5.Progress of Clinical Research on Tacrolimus in Treatment of Myasthenia Gravis
Huawen XIN ; Ran LI ; Fei LIU
Herald of Medicine 2017;36(6):597-600
Tacrolimus is a novel immunosuppressant used in the treatment of a variety of autoimmune diseases.More and more studies have shown that tacrolimus has a certain therapeutic effect on myasthenia gravis (MG).This article reviews the mechanism,clinical researches,adverse reactions,dosage and clinical evaluation of tacrolimus in the treatment of MG.
6.Pharmacogenomics and Clinical Pharmacists
Herald of Medicine 2017;36(9):956-961
Pharmacogenomics does not only bring the connection of genes,medicines and diseases,but also become a powerful tool for clinical pharmacists.Pharmacogenomics is commonly used in clinical practice,especially in the implementation of genetic-test results for guiding rational use of medicines.The genotyping results of genes can provide good individualized medication guidance for patients,which can be confirmed by clinical use of the clopidogrel and warfarin.As a member of the clinical treatment team,clinical pharmacists should take advantage of pharmaceutical and pharmacogenomics information to promote rational use of medicines.
7.Inhibitory Effects of Deoxyschizandrin on P-glycoprotein in Vitro and in Vivo
Weiliang LI ; Jianjun SONG ; Huawen XIN
Herald of Medicine 2017;36(2):162-166
Objective To investigate the influence of deoxyschizandrin (Deo) on P-glycoprotein (P-gp).Methods The effect of P-gp on Deo (20,40,80 μg·mL-1) was studied in the Caco-2 cell model in vitro,and the apparent permeability coefficient (Papp) of Deo (20-160 μg·mL-1) on a P-gp substrate,rhodamine123 or cyclosporine A,was calculated.Healthy male Sprague-Dawley rats were randomly divided into five groups:blank control group,verapamil group,low-,medium-and high-dose Deo group (8 rats in each group).Rats in the low-,medium-and high-dose Deo group were intragastrically administered once daily with Deo at 8,16 and 32 mg·kg-1 for 3 consecutive days,while rats similarly received gavagewith verapamil (4 mg·kg-1) in the verapamil group and equal volume of purified water in the blank control group.Thirty minutes after the rats were treated with their respective drugs,rhodamine123 (5 mg· kg-1) was orally administrated.Then the pharmacokinetic profiles of rhodamine 123 were analyzed to evaluate the inhibitory ability of Deo on P-gp in vivo.Results The bidirectional transport rates of Deo (20,40,80 μg·mL-1) were similar,with non-selectivity.Deo (20-160 pg·mL-1)significantly inhibited the basolateral→apical(BL→AP) directional transports of rhodamine 123 and cyclosporine A in Caco-2 cell model (P < 0.05) in a concentration-dependent manner.And Deo (8-32 mg· kg-1) also dose-dependently decreased the peak concentrations (Cm.) and the area under the plasma concentration-time curve (AUC0-t) of Rho123.Conclusion Deo can inhibit P-gp in vitro and in vivo,but it is not a P-gp substrate.
8.Research Progress in Tacrolimus Used in Children with Refractory Nephrotic Syndrome
China Pharmacist 2017;20(12):2228-2232
Tacrolimus is a kind of calcineurin inhibitor ( CNI) , and it is a novel immunosuppressant with similar efficacy to ciclos-porin. This paper reviewed the recent advances in the treatment of refractory nephrotic syndrome in children with tacrolimus, including the comparison of efficacy, dosage, adverse effects and clinical evaluation with the other immunosuppressive agents such as ciclosporin and mycophenolate mofetil in order to provide reference for clinics.
9.Study on the Association of Synergistic Effects of Wuzhi Capsules on Tacrolimus with CYP3A5*3 Gene Polymorphism
Yan YANG ; Huawen XIN ; Fei LIU ; Lei XIONG ; Weiliang LI ; Airong YU
China Pharmacy 2017;28(5):581-585
OBJECTIVE:To investigate the association of synergistic effects of Wuzhi capsules on tacrolimus with CYP3A5*3 (6986A>G,rs776746) gene polymorphisms. METHODS:One hundred and severty patients underwent renal transplantation receiving tacrolimus maintenance therapy after surgery were selected from our hospital during Jan. 1997-Dec. 2015,and then divided into Wuzhi capsules(+)group(74 cases)and Wuzhi capsules(-)group(96 cases)according to the use of Wuzhi capsules. Both groups received tacrolimus+mycophenolate mofetil+prednisone;Wuzhi capsules (+)group was additionally given Wuzhi capsules,one capsule each time,bid,for more than 12 months. Trough concentration of tacrolimus was detected by CMIA 0,1,3,6,12 months after medica-tion,and the blood concentrations(C0/D)were calculated at different time points after correcting daily dose. CYP3A5*3 gene polymor-phisms was detected by PCR-RFLP. The association of C0/D value with gene polymorphism was investigated by analysis of covariance. RESULTS:Among 170 patients,there were 65 cases of CYP3A5 GG genotype,83 cases of AG genotype and 22 cases of AA geno-type;genotype frequencies were 38.2%,48.8% and 12.9%,which was in line with Hardy-Weinberg balance (P>0.05). There was statistical significance in the distribution frequencies of GG,AG+AA genotype between Wuzhi capsules(+)group and Wuzhi capsules (-)group (P<0.05). After 1 month of medication,C0/D of tacrolimus in GG genotype was significantly higher in Wuzhi capsules (+)group than in Wuzhi capsules(-)group. After 1,3,6,12 months of medication,C0/D of tacrolimus in AG+AA genotype was sig-nificantly higher in Wuzhi capsules(+)group than in Wuzhi capsules(-)group,with statistical significance(P<0.05). There was no statistical significance in C0/D of tacrolimus in GG genotype between 2 groups after 3,6,12 months of treatment(P>0.05). CON-CLUSIONS:Wuzhi capsules can increase C0/D of tacrolimus in CYP3A5*3 AG+AA genotype,but have no significant effect on C0/D of tacrolimus in GG genotype;CYP3A5*3 genotype should be considered when using Wuzhi capsules as synergist of tacrolimus.
10.Determination of Rhodamine 123 in Rat Plasma by High Performance Liquid Chromatography
Xia TANG ; Huawen XIN ; Meng OUYANG ; Jianxun ZHONG
Herald of Medicine 2017;36(9):971-973
Objective To establish a sensitive method for the determination of rhodamine 123 (Rh123) in rat plasma by high performance liquid chromatography (HPLC).Methods The plasma samples were extracted by acetonitrile,and then separated on a Hypersil BDS C18 colunm (4.6 mm×100 mm,5 μm) equipped with a guard column kept at 25 ℃.The mobile phase consisted of acetonitrile and phosphate buffer (0.02 mol·L-1,pH4.0) (60:40) and was pumped at a constant rate of 1.0 mL·min-1.The peak was detected using a fluorescence detector set at FLD1A:Ex=485 nm,Em=546 nm.Results In this study,the method was validated for the Rh123 range of 0.1 to 32.0 μg·L-1,and the lower limit of quantitation (LLO Q) was 0.1 μg·L-1.The intra-and inter-day precisions for Rh123 were less than 7%,and the mean recoveries of Rh123 were 87.93%,89.03%,86.11% at low,mid,and high concentrations,respectively.Conclusion A simple,rapid and reproducible HPLC method was developed for the determination of Rh123 in rat plasma,which was an applicable method in modeling and description of the possible pharmacological interactions between the medicines and P-glycolprotein transporter.

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