KMCRIC

The administration of grapefruit juice concomitantly with terfenadine may lead to an increase in terfenadine bioavailability and increase the risk of cardiotoxicity [​34​;​35​;​38​]. A randomized crossover trail investigated the effects of grapefruit juice on terfenadine. Cmax was higher [​38​]. Terfenadine carboxylate AUC, Cmax, and tmax were also increased but t½ was not altered. Another study involving six healthy volunteers reported a significant increase in the AUC of terfenadine by concomitant grapefruit administration (median values 40.6 vs. 16.3ng.mL-1.h) and the Cmax (median values 7.2 vs. 2.1ng/mL); the tmax was not significantly increased and there was no significant change in the median QTc interval despite the increased terfenadine levels [​35​]. The mechanism likely involved reduced presystemic drug elimination by inhibition of more than one metabolic pathway [​34​;​38​].

... 연구하였다. 최고 혈중 농도는 더욱 높았다 [​38​]. 테르페나딘 카르복실산염 곡선 하 면적, 최고 혈중 농도, 최고 혈중 농도 도달 시간 역시 증가되었으나 반감기는 변화가 없었다. 6명의 건강한 지원자를 포함한 다른...

Grapefruit juice has been shown to increase Cmax and AUC of antimalarial agents such as artemether, halofantrine, and primaquine [​128​;​107​;​129​;​130​]. Halofantrine is metabolized into N-debutyl-halofantrine by CYP450 3A4. In a randomized crossover study, grapefruit juice increased halofantrine bioavailability and halofantrine-induced QT interval prolongation. Compared with water, grapefruit juice increased halofantrine AUC and peak plasma concentration by 2.8-fold ± 1.5-fold (p<0.0001) and 3.2-fold ± 1.3-fold (p<0.0001), respectively [​128​]. Grapefruit juice significantly (p=0.001) increased Cmax of artemether more than two-fold from 42ng/mL to 107ng/mL. The tmax with grapefruit juice was 2.1 hours. The AUC almost doubled with grapefruit juice from 177ng.hour/mL to 336ng.hour/mL (p=0.003). The elimination half-life remained unchanged (1.0 hours vs. 1.3 hours). No signs of bradycardia or QTc prolongation were observed with coadministration of artemether and grapefruit juice [​129​]. Results suggested that CYP3A4 in the gut wall is one of the metabolizing enzymes of artemether [​129​;​130​].Grapefruit juice has been found to have no effect on quinine pharmacokinetics [9]. Grapefruit juice increased the bioavailability of primaquine, with marked interindividual differences [​107​].

... 유발된 QT파 간격 연장을 증가시켰. 물과 비교하여, 자몽 주스는 할로판트린의 곡선 하 면적과 최고 혈중 농도를 각각 2.8-배 ± 1.5-배 (p<0.0001) 그리고 3.2-배 ± 1.3-배 (p<0.0001) 증가시켰다 [​128​]. 자몽 주스는...