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Omeprazole

消化

关键词消化 药物 质子泵抑制药,消化道溃疡

词汇介绍

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解析

omeprazole  ['ɔmipreizəul]

释义   n. 奥美拉唑

例句   To study the relation of CYP2C19 genotype to omeprazole metabolism in Chinese healthy subjects.

观察中国健康人群中CYP2C19基因与奥美拉唑新陈代谢的关系。


概述

奥美拉唑是1979年合成并用于临床的质子泵抑制药,是一种取代的苯并咪唑化合物,左旋体和右旋体各占50%。该药口服易吸收,首次用药生物利用度约35%,随着用药次数的增加生物利用度可达60%,Tmax为1~3小时。血浆蛋白结合率为95%,肝、肾、胃及十二指肠含量较高,不易透过血脑屏障。主要经肝脏CYP2C19代谢,t1/2与pH有关,平均为1小时,80%代谢产物经肾排泄,少量随粪便排出。 药理作用与机制(1)抑制胃酸分泌;(2)位粘膜保护作用;(3)抗幽门螺杆菌。 临床应用(

Concomitant intake of Coca-Cola® to manage the drug -drug interaction between velpatasvir and omeprazole studied in healthy volunteers.复制标题

同时摄入可口可乐®管理健康志愿者研究的velpatasvir和奥美拉唑之间的药物-药物相互作用。

发表时间:2019-07-17

影响因子:6.3

作者: van Seyen M

期刊:Clin Pharmacol Ther

The fixed-dose combination of the NS5B polymerase inhibitor sofosbuvir (SOF) and the NS5A inhibitor velpatasvir (VEL) is a pan-genotypic, once-daily tablet for the treatment of chronic hepatitis C virus (HCV) infection. VEL is a lipophilic weak base (Log D 6.31 (pH 8); acid dissociation constants [pKa] 3.2 and 4.6(1)) with pH dependent solubility ranging from soluble at pH 1.2 (> 36 mg/mL) to practically insoluble above pH4.5 (< 0.1 mg/mL) (2, 3). As a result, pH-dependent dissolution of the drug is a rate-limiting step for absorption. In general, proton pump inhibitors (PPIs) elevate the stomach pH and achieve a gastric pH>4 by reducing gastric secretion (4). This increase in gastric pH impairs VEL absorption. It has been shown that in subjects treated with omeprazole, the absorption of VEL is reduced by 26-56%, depending on the dose of omeprazole, concomitant food intake, and timing/sequence of VEL versus omeprazole intake (5, 6). This is the reason why concomitant use of SOF/VEL with PPIs (such as omeprazole) is not recommended. The package insert recommends to administer SOF/VEL with food and taken 4 hours before PPI at maximum doses comparable to omeprazole 20 mg, if PPI use is necessary (6).

译文

NS5B聚合酶抑制剂sofosbuvir(SOF)和NS5A抑制剂velpatasvir(VEL)的固定剂量组合是用于治疗慢性丙型肝炎病毒(HCV)感染的泛基因型,每日一次的片剂。 VEL是亲脂性弱碱(Log D 6.31(pH 8);酸解离常数[pKa] 3.2和4.6(1)),pH依赖性溶解度范围从pH 1.2(> 36 mg / mL)可溶至pH4以上几乎不溶.5(<0.1 mg / mL)(2,3)。结果,药物的pH依赖性溶解是限制吸收的步骤。通常,质子泵抑制剂(PPI)通过减少胃分泌来提高胃的pH并达到胃pH> 4(4)。胃pH的这种增加损害了VEL的吸收。已经表明,在用奥美拉唑治疗的受试者中,VEL的吸收减少26-56%,这取决于奥美拉唑的剂量,伴随的食物摄入以及VEL与奥美拉唑摄入的时间/顺序(5,6)。这就是为什么不推荐同时使用SOF / VEL和PPI(如奥美拉唑)的原因。如果需要使用PPI,包装说明书建议在食品中使用SOF / VEL,并在PPI前4小时服用,最大剂量与奥美拉唑20 mg相当(6)。