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학술연구/단체지원/교육 등 연구자 활동을 지속하도록 DBpia가 지원하고 있어요.
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연구자들이 자신의 연구와 전문성을 널리 알리고, 새로운 협력의 기회를 만들 수 있는 네트워킹 공간이에요.
논문 기본 정보
- 자료유형
- 학술저널
- 저자정보
- 발행연도
- 2018.1
- 수록면
- 1 - 12 (12page)
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Background: Carvedilol is commonly used to treat hypertension as a β- and α1 -adrenoreceptor blocker, but it is metabolized by CYP2D6, and CYP2D6*10 allele is dominant in Asian population. The objective of this study was to assess the influence of CYP2D6 polymorphisms on the pharmacokinetic (PK) and pharmacodynamic (PD) characteristics of carvedilol in healthy Korean volunteers. Methods: A PK/PD study for a single and multiple dosing of carvedilol were conducted. All volunteers in 3 genotypic groups received single oral dose of carvedilol 12.5 mg for 3 days, then 25 mg QD for 5 days, and 12.5 mg QD for another 3 days. PK parameters for carvedilol and its three metabolites were determined using non-compartmental analysis. For PD properties, blood pressure, heart rate, and the chronotropic dose 25 (CD25) value were obtained. Results: The IM_2 group with two *10 alleles (intermediate metabolizers) exhibited lower clearance of carvedilol as well as higher area under the curve (AUC) for O-desmethyl carvedilol. The ratio of CD25 to baseline at multiple dosing was significantly higher in the combined IM group (IM_1 and IM_2) than in the EM group, however, the ratio of CD25 after single and multiple dosing and the other PD markers were not significantly different between the 3 genotypic groups compared with the baseline. Conclusion: These findings showed that CYP2D6 genotype influenced the PK characteristics of carvedilol and no differences in PD response were observed in Korean healthy volunteers. Registered at the ClinicalTrials.gov, NCT02286934.
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참고문헌 (24)
참고문헌 신청
McTavish D / 1993 / Carvedilol. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy / Drugs 45(2):232~258
Keating GM / 2003 / Carvedilol: a review of its use in chronic heart failure / Drugs 63(16):1697~1741
Zhou HH / 1995 / Stereoselective disposition of carvedilol is determined by CYP2D6 / Clin Pharmacol Ther 57(5):518~524
Bartsch W / 1990 / Pharmacological characteristics of the stereoisomers of carvedilol / Eur J Clin Pharmacol 38(Suppl 2):S104~S107
Neugebauer G / 1990 / Stereoselective disposition of carvedilol in man after intravenous and oral administration of the racemic compound / Eur J Clin Pharmacol 38(Suppl 2):S108~S111
Keating GM / 2003 / Carvedilol: a review of its use in chronic heart failure / Drugs 63(16):1697~1741
Zhou HH / 1995 / Stereoselective disposition of carvedilol is determined by CYP2D6 / Clin Pharmacol Ther 57(5):518~524
Bartsch W / 1990 / Pharmacological characteristics of the stereoisomers of carvedilol / Eur J Clin Pharmacol 38(Suppl 2):S104~S107
Neugebauer G / 1990 / Stereoselective disposition of carvedilol in man after intravenous and oral administration of the racemic compound / Eur J Clin Pharmacol 38(Suppl 2):S108~S111
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