洞察新型非甾体抗炎药原药在胃肠道毒性治疗中的应用前景:展望综述。

Rajat Goyal, Sumeet Gupta, Prabodh Sharma, Manu Sharma
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引用次数: 0

摘要

非甾体抗炎药(NSAIDs)因其治疗潜力而在医疗系统中有着悠久的历史。这些非甾体抗炎药在适度和持续使用时会导致溃疡、胃痛、胃肠道出血、粘膜出血和胰腺炎。随着研究人员的不断深入,治疗上述不良反应变得越来越困难。一种制造低渗透性和低致溃特性的非甾体抗炎药的方法是原药技术。在口服非甾体抗炎药原药的过程中,溃疡、肠道出血和粘膜出血明显减少。考虑到这一背景,本综述重点讨论了非甾体抗炎药原药及其理由、非甾体抗炎药诱发胃肠道毒性的发病机制以及不同抗氧化剂和间隔基的作用。与母药相比,原药在溶解性和亲油性方面具有更多优势。一般来说,非甾体抗炎药类原药能成功治疗急性和长期炎症和疼痛,而不会引起溃疡毒性和相关的胃肠道副作用,这从药物经济学角度减轻了其负担。
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Insights into Prospects of Novel NSAID Prodrugs in the Management of Gastrointestinal Toxicity: A Perspective Review.

Non-steroidal anti-inflammatory drugs (NSAIDs) have a long history in the healthcare system due to their therapeutic potential. These NSAIDs cause ulcerogenicity, stomach pains, gastrointestinal hemorrhage, mucosa bleeding, and pancreatitis when used moderately and consistently. With researchers, managing the aforementioned adverse effects therapeutically is getting increasingly difficult. One method for creating NSAID moieties with low penetration as well as ulcerogenic properties is the prodrug technique. During the oral consumption of NSAID-prodrugs, ulcerations, intestinal hemorrhage, and mucosa hemorrhage have significantly decreased. Considering this background, this review focussed on NSAID prodrugs as well as their justifications, the pathogenesis of NSAIDs inducing gastrointestinal toxicity, and the role of different antioxidants and spacer groups. Prodrug moieties have more advantages over parent medicines concerning both solubility and lipophilicity. In general, NSAID-class prodrugs can successfully treat both acute and long-term inflammation and aches without causing ulcerotoxicity and related gastrointestinal side effects, which reduces their burden from the pharmacoeconomic perspective.

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CiteScore
4.30
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