Abstract
Glycopeptides have emerged as life-saving therapeutics in treating various gram-positive bacterial infections. Vancomycin being the first therapeutically approved glycopeptide has turned out as a blockbuster drug in the mitigation of gram-positive infections. However, long-term misuse of these glycopeptides led to the development of resistance which became a bottleneck in tackling various infections. Antimicrobial resistance has become a global threat exposing their impact on the public health domain. Concomitant to this the second-generation glycopeptides were developed through structural alterations and were approved by the USFDA which are serving as a last resort for an effective treatment. However, resistance against these also might develop shortly when misused. In this aspect, strategic approaches concerning structural activity for enhancing the antimicrobial activity and overcoming resistance were conferred. The clinical use of glycopeptides were also limited due to associated toxicity concerns and unusual pharmacokinetics. Understanding the pharmacokinetics of glycopeptides in different clinical conditions are necessary in tackling drug-induced resistance due to overdosing. Hence, dose optimization and therapeutic drug monitoring in different clinical conditions is necessary for better safety profiles and toxicity reduction. So, this review provides insights into glycopeptide-induced resistances, aspects of structural modifications to overcome resistance and their implications on pharmacokinetics and pharmacodynamics in different clinical conditions.