Department of Pharmacology, JIPMER, Puducherry, India.
Department of Neurology, JIPMER, Puducherry, India.
Indian J Pharmacol. 2019 Nov-Dec;51(6):384-388. doi: 10.4103/ijp.IJP_122_19. Epub 2020 Jan 16.
The aim of the study was to compare the dose-adjusted plasma levels of carbamazepine (CBZ) among expressers and nonexpressers of cytochrome P450 3A5 genotypes.
The study was carried out in 100 epileptic patients who were on CBZ monotherapy. Steady-state plasma CBZ levels were measured using reverse-phase high-performance liquid chromatography method, and genotyping of was done using real-time polymerase chain reaction method.
Patients inheriting variant (nonexpressers) had an increased plasma concentration of CBZ (4.86 μg/ml) when compared to patients inheriting either or (expressers) (4.3 μg/ml, = 0.004). Nonexpressers had significantly increased plasma concentrations of CBZ when adjusted for dose and weight when compared to expressers ( < 0.002 and < 0.001, respectively). The frequency of adverse reactions in expressers and nonexpressers was 12% and 9%, respectively.
There is a significant influence of genetic polymorphism (6986A>G) on dose-adjusted plasma levels of CBZ in epileptic patients in the South Indian population.
本研究旨在比较 CYP3A5 基因型表达者和非表达者的卡马西平（CBZ）剂量调整血浆水平。
该研究在 100 名接受 CBZ 单药治疗的癫痫患者中进行。使用反相高效液相色谱法测定稳态血浆 CBZ 水平，并使用实时聚合酶链反应法进行 基因分型。
与遗传 或 （表达者）的患者（4.3μg/ml，=0.004）相比，遗传 变异型（非表达者）的患者 CBZ 血浆浓度升高（4.86μg/ml）。与表达者相比，非表达者在调整剂量和体重后，CBZ 的血浆浓度显著升高（分别为 <0.002 和 <0.001）。表达者和非表达者的不良反应发生率分别为 12%和 9%。
在印度南部人群中，CYP3A5 基因多态性（6986A>G）对癫痫患者 CBZ 的剂量调整血浆水平有显著影响。
