临床药物动力学dipyrone及其代谢物。

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莱维M, Zylber-Katz E, Rosenkranz B

临床药物动力学dipyrone及其代谢物。

Pharmacokinet。1995年3月,28 (3):216 - 34。doi: 10.2165 / 00003088-199528030-00004。

PubMed ID
7758252 (在PubMed
]
文摘

dipyrone的药物动力学的特点是快速水解活性一半4-methyl-amino-antipyrine (MAA), 85%口服片剂形式的后生物利用度,和需要很短的时间内达到最大系统浓度(达峰时间为1.2 - 2.0小时)。绝对生物利用度后肌内和直肠管理局87年和54%,分别。MAA进一步代谢平均消除半衰期(t1/2) 2.6到3.5小时4-formyl-amino-antipyrine (FAA),这是一个end-metabolite,和4-amino-antipyrine (AA),然后乙酰化,4-acetyl-amino-antipyrine (AAA)的多态N-acetyl-transferase (t1/2 AA在快速乙酰化器3.8小时和5.5小时慢乙酰化器)。尿排泄这四个代谢物约占60%的服用剂量的dipyrone。beplayapp蛋白结合的4个主要代谢产物是不到60%。的体积分布MAA约1.15 L /公斤瘦体重。beplayapp所有4代谢产物分泌到乳汁。单剂研究(0.75,1.5和3 g)和multiple-dose研究(1 g一天三次连续吃七天)显示非线性药代动力学符合联邦航空局的共代谢转向AA。在多个政府明显MAA间隙减少了22%。在老年人MAA间隙降低了33%。 In patients with cirrhosis of the liver, the apparent clearance of all metabolites is generally reduced. In patients with renal disease, apparent clearance of MAA remains unchanged, whereas elimination of the renally excreted metabolites AAA and FAA is markedly impaired. No clinically important drug interactions have thus far been recognised. Dipyrone does not affect the pharmacodynamic response to alcohol (ethanol), glibenclamide (glyburide), oral anti-coagulants or furosemide (frusemide). The low toxicity of dipyrone and its efficacy support its use in clinical practice, despite some complex aspects of its disposition.

beplay体育安全吗DrugBank数据引用了这篇文章

药物
药物反应
反应
Metamizole
DB04817
    4-methyl-amino-antipyrine (MAA)
    DBMET03541
    		细节