alendronate的药物动力学。

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波勒斯AG)、荷兰SD、格茨BJ

alendronate的药物动力学。

Pharmacokinet。1999年5月,36 (5):315 - 28。doi: 10.2165 / 00003088-199936050-00002。

PubMed ID
10384857 (在PubMed
]
文摘

Alendronate (alendronic酸;4-amino-1-hydroxybutylidene二磷酸盐)已经证明有效性口头在绝经后骨质疏松症的治疗和预防,类固醇诱导性骨质疏松和骨的佩吉特氏病。其主要的作用机制包括监测骨吸收的抑制作用。的药物动力学和药效学alendronate必须解释在其独特的属性,其中包括针对骨架和纳入骨骼矩阵。功能型,alendronate不是在动物新陈代谢,清除从等离子体吸收到骨头和消除通过肾脏排泄。尽管不久政府药物在体内分布广泛,随后快速瞬态是骨骼组织的不饱和的再分配。口服生物利用度约为0.9到1.8%,明显抑制口腔beplayapp吸收食物。药物的去除骨反映了底层框架的周转率。肾清除率似乎涉及到肾小球滤过和专业分泌途径。临床,药物动力学的alendronate特征几乎完全基于尿排泄数据由于极低浓度后口服。 After intravenous administration of radiolabelled alendronate to women, no metabolites of the drug were detectable and urinary excretion was the sole means of elimination. About 40 to 60% of the dose is retained for a long time in the body, presumably in the skeleton, with no evidence of saturation or influence of one intravenous dose on the pharmacokinetics of subsequent doses. The oral bioavailability of alendronate in the fasted state is about 0.7%, with no significant difference between men and women. Absorption and disposition appear independent of dose. Food substantially reduces the bioavailability of oral alendronate; otherwise, no substantive drug interactions have been identified. The pharmacokinetic properties of alendronate are evident pharmacodynamically. Alendronate treatment results in an early and dose-dependent inhibition of skeletal resorption, which can be followed clinically with biochemical markers, and which ultimately reaches a plateau and is slowly reversible upon discontinuation of the drug. These findings reflect the uptake of the drug into bone, where it exerts its pharmacological activity, and a time course that results from the long residence time in the skeleton. The net result is that alendronate corrects the underlying imbalance in skeletal turnover characteristic of several disease states. In women with postmenopausal osteoporosis, for example, alendronate treatment results in increases in bone mass and a reduction in fracture incidence, including at the hip.

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药物