AIM To assess the pharmacokinetic profile of single doses of meloxicam in healthy Chinese volunteers. METHODS The plasma concentrations of meloxicam after an oral dose of 15 mg to twenty healthy male volunteers were a...AIM To assess the pharmacokinetic profile of single doses of meloxicam in healthy Chinese volunteers. METHODS The plasma concentrations of meloxicam after an oral dose of 15 mg to twenty healthy male volunteers were analized by means of a validated HPLC method. The pharmacokinetic parameters were subjected to Shapiro Wilk test to determine whether these data were fitted to a normal distribution. RESULTS The twenty volunteers can be classified into extensive metabolizers and poor metabolizers according to pharmacokinetic parameters. The main parameters in the two groups obtained were as follows: T 1/2 were 21±4 and 38±9 h, AUC 0-∞ were 49±10 and 110±8 μg·h·mL -1 , respectively. Even the AUC data in extensive metabolizers were 1 7 times as that reported in White volunteers following the same doses of meloxicam. CONCLUSION There were significant individual differences in the pharmacokinetics of meloxicam in Chinese volunteers, which may be due to the genetic polymorphism of CYP2C9.展开更多
据WHO推荐的标准治疗方案,初治结核病患者2个月的强化期采用利福平(rifampin,RIF)+异烟肼(isoniazid,INH)+吡嗪酰胺(pyrazinamide,PZA)+乙胺丁醇(ethambutol,EMB)的四联法则进行治疗。治疗药物监测(therapeutic drug monitoring,TDM)和...据WHO推荐的标准治疗方案,初治结核病患者2个月的强化期采用利福平(rifampin,RIF)+异烟肼(isoniazid,INH)+吡嗪酰胺(pyrazinamide,PZA)+乙胺丁醇(ethambutol,EMB)的四联法则进行治疗。治疗药物监测(therapeutic drug monitoring,TDM)和药物代谢酶基因多态性检测可减少药物不良反应,提高患者依从性。本文对TDM和药物基因检测在“四联”抗结核药物的临床治疗中的作用予以综述,优化治疗、增加疗效,降低药物不良反应。展开更多
Polymorphisms associated with genes coding for a variety of drug-metabolizing enzymes （DMEs） and associated transport proteins can influence the drug metabolism rate of individuals, potentially affecting the efficac...Polymorphisms associated with genes coding for a variety of drug-metabolizing enzymes （DMEs） and associated transport proteins can influence the drug metabolism rate of individuals, potentially affecting the efficacy of drug and the occurrence of adverse reactions. Single nucleotide polymorphisms （SNPs） are prevalent in all types of genetic variations. Reliable SNP genotyping provides excellent markers for detecting genetic polymolphisms, genetic disorders, and resistance of pathogen to drug, which are needed for the genetic diagnosis of disease and subtle genetic factors. With a large number of SNP genotyping studies being conducted, a lot of novel SNP identifying methods have been developed. Several SNP genotyping methods and techniques have been introduced for clinical test. These include TaqMan drug metabolism genotyping assays, pH-sensing semiconductor system, high-resolution melting curve analysis （HRM） of polymerase chain reaction （PCR） amplicons, novel multiplexed electrochemical biosensor with non-fouling surface, DNA hybridization detection using less than 10-nm gap silicon nanogap structure, tetra-primer ARMS-PCR method, acoustic detection of DNA conformation in genetic assays combined with PCR, microbeads-mass spectrometry （MEMS）-based approach, and liquid chromatography-electrospray ionization mass spectrometry. Personalized medicine has changed the conventional ways of using drugs according to experiences. It focuses on making the individualized pattern for each individual based on their own characteristics. Lots of researchers are using the analysis of clinical samples to explain the relationship between the drug adverse reactions and genetic polymorphisms. But it takes a long time from collecting the blood samples for DNA extraction and genotyping to getting results on the side effect of drug through clinical study. Therefore, it is desirable to develop improved in vitro methods to study the drug metabolizing-enzymes and transport protein genetic polymorphisms.展开更多
文摘AIM To assess the pharmacokinetic profile of single doses of meloxicam in healthy Chinese volunteers. METHODS The plasma concentrations of meloxicam after an oral dose of 15 mg to twenty healthy male volunteers were analized by means of a validated HPLC method. The pharmacokinetic parameters were subjected to Shapiro Wilk test to determine whether these data were fitted to a normal distribution. RESULTS The twenty volunteers can be classified into extensive metabolizers and poor metabolizers according to pharmacokinetic parameters. The main parameters in the two groups obtained were as follows: T 1/2 were 21±4 and 38±9 h, AUC 0-∞ were 49±10 and 110±8 μg·h·mL -1 , respectively. Even the AUC data in extensive metabolizers were 1 7 times as that reported in White volunteers following the same doses of meloxicam. CONCLUSION There were significant individual differences in the pharmacokinetics of meloxicam in Chinese volunteers, which may be due to the genetic polymorphism of CYP2C9.
文摘据WHO推荐的标准治疗方案,初治结核病患者2个月的强化期采用利福平(rifampin,RIF)+异烟肼(isoniazid,INH)+吡嗪酰胺(pyrazinamide,PZA)+乙胺丁醇(ethambutol,EMB)的四联法则进行治疗。治疗药物监测(therapeutic drug monitoring,TDM)和药物代谢酶基因多态性检测可减少药物不良反应,提高患者依从性。本文对TDM和药物基因检测在“四联”抗结核药物的临床治疗中的作用予以综述,优化治疗、增加疗效,降低药物不良反应。
基金The Influence of Artesunate on β-catenin Signaling Pathway of Hetatic Atellate Cells(Grant No.2011CDB491)
文摘Polymorphisms associated with genes coding for a variety of drug-metabolizing enzymes （DMEs） and associated transport proteins can influence the drug metabolism rate of individuals, potentially affecting the efficacy of drug and the occurrence of adverse reactions. Single nucleotide polymorphisms （SNPs） are prevalent in all types of genetic variations. Reliable SNP genotyping provides excellent markers for detecting genetic polymolphisms, genetic disorders, and resistance of pathogen to drug, which are needed for the genetic diagnosis of disease and subtle genetic factors. With a large number of SNP genotyping studies being conducted, a lot of novel SNP identifying methods have been developed. Several SNP genotyping methods and techniques have been introduced for clinical test. These include TaqMan drug metabolism genotyping assays, pH-sensing semiconductor system, high-resolution melting curve analysis （HRM） of polymerase chain reaction （PCR） amplicons, novel multiplexed electrochemical biosensor with non-fouling surface, DNA hybridization detection using less than 10-nm gap silicon nanogap structure, tetra-primer ARMS-PCR method, acoustic detection of DNA conformation in genetic assays combined with PCR, microbeads-mass spectrometry （MEMS）-based approach, and liquid chromatography-electrospray ionization mass spectrometry. Personalized medicine has changed the conventional ways of using drugs according to experiences. It focuses on making the individualized pattern for each individual based on their own characteristics. Lots of researchers are using the analysis of clinical samples to explain the relationship between the drug adverse reactions and genetic polymorphisms. But it takes a long time from collecting the blood samples for DNA extraction and genotyping to getting results on the side effect of drug through clinical study. Therefore, it is desirable to develop improved in vitro methods to study the drug metabolizing-enzymes and transport protein genetic polymorphisms.
