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Background Nifedipine is a calcium channel blocker, which is used to treat hypertension and angina pectoris. The present study aimed to evaluate the effects of gene polymorphisms on pharmacokinetics of relevant metabolic genes with inconsistent or incomplete research conclusions and of others that exhibited an impact on pharmacodynamics, so as to provide a scientific basis for the inter-individual variation in nifedipine controlled-release tablet disposition. Methods A total of 33 healthy volunteers were administered a single 30 mg oral dose of nifedipine controlled-release tablets, and were genotyped for 17 SNPs within 12 genes, by StepOne Real-Time PCR System and the Matrix-assisted laser desorption ionization-time of flight. The plasma concentration levels were quantified by Ultra-performance liquid chromatography tandem mass spectrometry. Univariate and multivariate analyses were performed and the mean pharmacokinetic variables were compared according to genotypes. Results The CYP3A4 rs2242480, ABCB1 rs1045642, CACNA1D rs312481, CACNA1C rs2238032, ACE rs4646994 and SLC14A2 rs3745009 polymorphisms significantly influenced the pharmacokinetics of nifedipine controlled-release tablets with a greater effect being noted on CACNA1D, CACNA1C, and SLC14A2. These results continued to be statistically significant following multivariate correction. Conclusions The CYP3A4 rs2242480, ABCB1 rs1045642, CACNA1D rs312481, CACNA1C rs2238032, ACE rs4646994 and SLC14A2 rs3745009 polymorphisms significantly influenced the pharmacokinetics of nifedipine controlled-release tablets. Their pharmacokinetic properties were examined, so as to provide a theoretical basis for individual differences found during treatment. |
