Аннотация
Context: The use of pregabalin in neuropathic pain management has been increasingly associated with concerns regarding toxicity, particularly in cases of overdose, misuse, and co-exposure with central nervous system depressants. In parallel, there is a growing need for reliable analytical methods to quantify pregabalin in biological matrices. Aims: To systematically evaluate the evidence on toxicological outcomes associated with pregabalin exposure and the analytical methods used for its detection and quantification. Methods: The literature retrieval process involved searching five electronic databases (PubMed, ScienceDirect, Web of Science, Scopus, and Google Scholar) for studies published between 2020 and 2025. Eligible records were screened using predefined criteria, and data were extracted on study design, population characteristics, exposure context, toxicological outcomes, and analytical techniques (e.g., LC–MS/MS, GC–MS, HPLC). Due to heterogeneity across study designs and outcomes, a narrative synthesis was performed. Results: A total of 20 studies were included, comprising observational clinical toxicology studies, forensic investigations, case reports/series, toxicological surveillance reports, systematic reviews, and analytical validation studies. The available evidence indicates that pregabalin toxicity is primarily characterized by dose-dependent central nervous system depression, with clinical manifestations ranging from mild sedation to severe complications such as coma and respiratory failure. More serious and fatal outcomes were mainly associated with overdose scenarios and concomitant use of other central nervous system depressants. Liquid chromatography–tandem mass spectrometry was the most frequently used analytical technique. Conclusions: Pregabalin toxicity demonstrates a clear dose- and context-dependent pattern, with increased risk in the presence of co-ingestants and renal impairment. Greater standardization of analytical validation and clinically interpretable concentration thresholds is required to improve consistency in clinical and forensic toxicology.