药代动力学研究利用5-methyltetrahydrofolate和叶酸的冠状动脉疾病患者。
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Willems FF,波尔人GH、布鲁姆HJ Aengevaeren WR, Verheugt弗兰克-威廉姆斯
药代动力学研究利用5-methyltetrahydrofolate和叶酸的冠状动脉疾病患者。
Br J杂志。2004年3月,141 (5):825 - 30。Epub 2004 2月9。
- PubMed ID
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14769778 (在PubMed]
- 文摘
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1。Methylenetetrahydrofolate还原酶(MTHFR)是一个调节酶folate-dependant同型半胱氨酸remethylation,因为它会刺激减少5、10 Methylenetetrahydrofolate 5-methyltetrahydrofolate (5-MTHF)。2。受试者为677 c - - > T突变纯合子MTHFR酶罹患心血管疾病的风险增加。可以推测的是直接管理5-MTHF相反的叶酸可以促进remethylation蛋氨酸的同型半胱氨酸。3所示。本研究的目的是确定口服的药代动力学性质管理6 (R, S) 5-MTHF与叶酸心血管患者677 c - - > T MTHFR的纯合性。4所示。这是一个open-controlled,双向,两期随机交叉研究。患者接受单剂量口服5毫克叶酸或5毫克5-MTHF在每一个时期。 The concentrations of the 6[S] 5-MTHF and 6[R] 5-MTHF diastereoisomers were determined in venous blood samples. 5. All pharmacokinetic parameters demonstrate that the bioavailability of 5-MTHF is higher compared to folic acid. The peak concentration of both isomers following the administration of 6[R,S] 5-MTHF is almost seven times higher compared to folic acid, irrespective of the patient's genotype. However, at 1 week after the administration of a single dosage 6[R,S] 5-MTHF, we detected 6[R] 5-MTHF following the administration of folic acid, indicating storage of this isomer in the body. 6. Our results demonstrate that oral 5-MTHF has a different pharmacokinetic profile with a higher bioavailability compared to folic acid, irrespective of the patient's genotype. Detrimental effects of the storage of high levels of the non-natural isomer 6[R] 5-MTHF cannot be excluded.
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