A Review on the Pharmacokinetics and Toxicological Profile of Rabeprazole

Shivanee Yadav, Harikrishna Yadav, Nidhi Tyagi, Prashant Kumar Katiyar
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Abstract

Rabeprazole, a proton pump inhibitor, is used for individuals with ulcers. The prodrug is transformed into an active sulphenamide form by the acidic conditions present in the parietal cells. Rabeprazole inhibits the H+K+ ATPase of the gastric cells, leading to a decrease in the generation of stomach acid in both normal and stimulated situations. The present review was based on the pharmacokinetics and toxicological profile of Rabeprazole. Once absorbed into the body, approximately 96.3–97% of rabeprazole is bound to plasma proteins. In humans, the half-life of rabeprazole is approximately one hour. The peak concentration of rabeprazole in human plasma following a single oral dose does not appear until around 3.5 hours later. Rabeprazole is metabolised mostly by the liver. Once the liver has metabolised the medicine, 90% of it will be excreted via the kidneys. The elimination fraction is 10%. Rabeprazole is mostly metabolised by the cytochrome P450 enzymes CYP2C19 and CYP3A4. . It concluded that in the human pylorus, it decreased muscular tone, maximal contraction values, and contraction frequencies. When diclofenac sodium SR, glucosamine, diacerein, calcium, and vitamin D preparations were administered in addition to rabeprazole, the patients experienced GI bleeding, fatty liver grade 1, mild epigastric discomfort, black stools, and decreased haemoglobin content.
雷贝拉唑的药代动力学和毒理学特征综述
雷贝拉唑是一种质子泵抑制剂,用于治疗溃疡患者。在胃顶细胞的酸性条件下,该原药转化为具有活性的磺胺形式。雷贝拉唑可抑制胃细胞的 H+K+ ATP 酶,从而减少正常和受刺激情况下胃酸的产生。本综述基于雷贝拉唑的药代动力学和毒理学特征。雷贝拉唑被人体吸收后,约有 96.3-97% 与血浆蛋白结合。在人体内,雷贝拉唑的半衰期约为一小时。单次口服后,雷贝拉唑在人体血浆中的峰值浓度要到约 3.5 小时后才出现。雷贝拉唑主要由肝脏代谢。肝脏代谢后,90% 的药物将通过肾脏排出体外。排出量为 10%。雷贝拉唑主要由细胞色素 P450 酶 CYP2C19 和 CYP3A4 代谢。研究得出结论,在人体幽门中,雷贝拉唑会降低肌肉张力、最大收缩值和收缩频率。在服用雷贝拉唑的同时服用双氯芬酸钠 SR、氨基葡萄糖、地卡瑞林、钙和维生素 D 制剂时,患者出现消化道出血、脂肪肝 1 级、轻度上腹不适、黑便和血红蛋白含量下降。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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