药物动力学pantoprazole的男人。

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Huber R,哈特曼M, Bliesath H, Luhmann R, Steinijans大众,泽赫K

药物动力学pantoprazole的男人。

Int中国新药杂志。1996年5月,34 (1):S7-16。

PubMed ID

8793599 (在PubMed

]

文摘

质子泵抑制剂pantoprazole是取代苯并咪唑亚砜治疗acid-related胃肠道疾病,如反流性食管炎、十二指肠溃疡和胃溃疡。Pantoprazole,管理作为一个40毫克肠涂布平板电脑,是定量吸收。它的绝对生物利用度为77%,对多个剂量不会改变。单剂口服后40毫克,Cmax大约是2.5 mg / l,达峰时间为2 - 3 h。AUC (0, inf。)大约是5 mgxh / l。Pantoprazole显示口服和静脉输液之后线性药物动力学。Pantoprazole广泛在肝脏代谢,血清总间隙为0.1 l / h /公斤,血清消除半衰期约为1.1 h,表观分布容积的0.15 l /公斤。98%的pantoprazole必将血清蛋白质。消除半衰期,间隙分布和体积是独立的剂量。形成的主要血清代谢物脱甲基四工位的吡啶环,其次是与硫酸结合。几乎80%的口服或静脉注射剂量在尿液代谢物排出; the remainder is found in feces and originates from biliary secretion. The pharmacokinetics of pantoprazole are unaltered in patients with renal failure. In patients with severe liver cirrhosis, the decreased rate of metabolism results in a half-life of 7-9 h. The clearance of pantoprazole is only slightly affected by age, its half-life being approximately 1.25 h in the elderly. Concomitant intake of food had no influence on the bioavailability of pantoprazole. Pantoprazole showed lack of cytochrome P450 interaction with concomitantly administered drugs in any of the studies conducted to date. Lack of interaction was also demonstrated with a coadministered antacid. The absence of inductive effects on metabolism after chronic administration was first shown by using antipyrine as a probe for mixed functional oxidative cytochrome P450 enzymes. Absence of CYP1A2 induction was confirmed using the specific probe caffeine. As sensitive probes for CYP3A enzyme induction, urinary excretion of D-glucaric acid and 6 beta-hydroxycortisol were also unchanged.

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药物

Pantoprazole