Department of Pharmaceutical Chemistry, Era College of Pharmacy, Era University, Lucknow, 226003, Uttar Pradesh, India.
Laboratory Medicine Department, Faculty of Applied Medical Sciences, Umm Al‒Qura University, Makkah, 21955, Saudi Arabia.
Med Chem. 2024;20(3):268-292. doi: 10.2174/0115734064260853230926080134.
The success of the TB control program is hampered by the major issue of drug-resistant tuberculosis (DR-TB). The situation has undoubtedly been made more difficult by the widespread and multidrug-resistant (XDR) strains of TB. The modification of existing anti-TB medications to produce derivatives that can function on resistant TB bacilli is one of the potential techniques to overcome drug resistance affordably and straightforwardly. In comparison to novel pharmaceuticals for drug research and progress, these may have a better half-life and greater bioavailability, be more efficient, and serve as inexpensive alternatives. , which is drugsusceptible or drug-resistant, is effectively treated by several already prescribed medications and their derivatives. Due to this, the current review attempts to give a brief overview of the rifampicin derivatives that can overcome the parent drug's resistance and could, hence, act as useful substitutes. It has been found that one-third of the global population is affected by . The most common cause of infection-related death can range from latent TB to TB illness. Antibiotics in the rifamycin class, including rifampicin or rifampin (RIF), rifapentine (RPT), and others, have a special sterilizing effect on . We examine research focused on evaluating the safety, effectiveness, pharmacokinetics, pharmacodynamics, risk of medication interactions, and other characteristics of RIF analogs. Drug interactions are especially difficult with RIF because it must be taken every day for four months to treat latent TB infection. RIF continues to be the gold standard of treatment for drug-sensitive TB illness. RIF's safety profile is well known, and the two medicines' adverse reactions have varying degrees of frequency. The authorized once-weekly RPT regimen is insufficient, but greater dosages of either medication may reduce the amount of time needed to treat TB effectively.
结核病控制项目的成功受到耐多药结核病（DR-TB）这一主要问题的阻碍。广泛存在和耐多药（XDR）结核菌株无疑使情况更加困难。将现有的抗结核药物进行修改，生成能够作用于耐药结核杆菌的衍生物，是一种经济实惠且直接克服耐药性的潜在技术之一。与用于药物研究和进展的新型药物相比，这些药物可能具有更好的半衰期和更高的生物利用度，更有效，并且作为廉价替代品。耐多药或耐药结核病，已经有几种已开处方的药物及其衍生物可以有效地治疗。正因为如此，目前的综述试图简要概述可以克服母体药物耐药性的利福平衍生物，因此可以作为有用的替代品。研究发现，全球有三分之一的人口受到影响。最常见的感染相关死亡原因范围从潜伏性结核病到结核病疾病。利福霉素类抗生素，包括利福平或利福平（RIF）、 rifapentine（RPT）等，对具有特殊的杀菌作用。我们检查了专注于评估 RIF 类似物的安全性、有效性、药代动力学、药效学、药物相互作用风险和其他特征的研究。药物相互作用尤其困难，因为 RIF 必须每天服用四个月才能治疗潜伏性结核病感染。RIF 仍然是治疗药物敏感结核病的金标准。RIF 的安全性概况众所周知，两种药物的不良反应发生频率不同。授权的每周一次 RPT 方案是不够的，但增加两种药物中的任何一种的剂量都可能减少有效治疗结核病所需的时间。
