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Effect of aspirin, potential P-glycoprotein activator on intestinal absorption of ticagrelor : 잠재적 P-glycoprotein 활성제 아스피린이 티카그렐러 장내 흡수에 미치는 영향
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- Authors
- Advisor
- 노재규
- Major
- 자연과학대학 협동과정뇌과학전공
- Issue Date
- 2013-02
- Publisher
- 서울대학교 대학원
- Keywords
- Aspirin ; Ticagrelor ; P-glycoprotein ; Drug interaction ; Intestinal absorption
- Description
- 학위논문 (석사)-- 서울대학교 대학원 : 협동과정뇌과학전공, 2013. 2. 노재규.
- Abstract
- Background: Ticagrelor is a new P2Y12 receptor inhibitor, which is approved for use in patients with acute coronary syndrome in combination with aspirin. However, there is some evidence that high-dose aspirin reduces the effectiveness of ticagrelor. Given the fact that aspirin can enhance intestinal P-glycoprotein (P-gp) expression and ticagrelor is a substrate of P-gp, we hypothesized that concurrent treatment with aspirin may decrease the intestinal absorption of ticagrelor.
Methods and Results: In vitro assay using a monolayer of human epithelial colorectal (Caco-2) cells and in vivo study using the closed-loop method in rats were performed. Aspirin was administered to Caco-2 cells (0.5 and 1 mmol/l) in vitro for 72 hours and to rat intestine (10 mg/kg and 100 mg/kg) in vivo for 4 weeks, before administration of ticagrelor. Ticagrelor permeabilization in vitro was not affected by aspirin pre-treatment and was neither influenced by the P-gp inhibitor, tariquidar. Furthermore, different doses of aspirin (10 mg/kg and 100 mg/kg) pre-treatment did not affect the absorption of ticagrelor in the rat intestine.
Conclusion: The intestinal absorption of ticagrelor was not affected by enhancement of P-glycoprotein following prolonged aspirin treatment. Further studies will be necessary to clarify how aspirin attenuates the treatment effect of ticagrelor.
- Language
- English
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