药物动力学在健康受试者口服甜菜碱和高胱氨酸尿患者。

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Schwahn BC, Hafner D, Hohlfeld T, Balkenhol N, Laryea医学博士万德尔在U

药物动力学在健康受试者口服甜菜碱和高胱氨酸尿患者。

Br中国新药杂志。2003年1月,(1):55 6-13。doi: 10.1046 / j.1365-2125.2003.01717.x。

PubMed ID

12534635 (在PubMed

]

文摘

目的:大量口服剂量的甜菜碱已被证明能有效地降低血浆同型半胱氨酸在严重hyperhomocysteinaemia。甜菜碱的药代动力学特征和代谢在人类尚未评估和甜菜碱治疗药物监测是不可用的。我们研究了甜菜碱的药物动力学及其代谢物dimethylglycine (DMG)在健康受试者和三个高胱氨酸尿患者。方法:12个男性志愿者进行了一个开放研究。后一个管理50毫克甜菜碱公斤体重和期间每天两次连续摄入50毫克公斤体重,串行血样和24小时尿收集确定甜菜碱和DMG血浆浓度和尿排泄,分别。一个剂量的甜菜碱后对患者进行评估。结果:我们发现快速吸收(t (1/2), abs 00.28 h,南达科他州。0.17)和销售(t(1/2),λ₁00.59 h,南达科他州。0.22)甜菜碱。0.94 Cmax更易与l - 1(其中。0.19)在最高温度达到00.90 h(其中0.33)。消除半衰期t (1/2), z是14.38 h(其中7.17)。重复剂量后,t(1/2),λ₁(01.77 h,南达科他州。0.75)和t (1/2)、z (41.17 h,南达科他州。13.50)显著增加(95% CI 0.73, 01.64 h, 19.90, 33.70 h,分别),而吸收保持不变。 DMG concentrations increased significantly after betaine administration and accumulation occurred to the same extent as with betaine. Renal clearance was low and urinary excretion of betaine was equivalent to 4% of the ingested dose. Distribution and elimination kinetics in homocystinuric patients appeared to be accelerated. CONCLUSIONS: Betaine plasma concentrations change rapidly after ingestion. Elimination half-life increased during continuous dosing over 5 days. Betaine is mainly eliminated by metabolism. More pharmacokinetic and pharmacodynamic studies in hyperhomocysteinaemic patients are needed to refine the current treatment with betaine.

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药物

甜菜碱