ABSTRACT Pravastatin (PRV), a highly hydrophilic statin used to treat hypercholesterolemia and prevent cardiovascular disease, presents certain analytical challenges due to its low bioavailability, tendency to lactonize, and potentially complex metabolism. This review aims to consolidate and critically evaluate the analytical procedures developed for the determination of PRV and its metabolites in pharmaceutical and biological matrices. This review aims to comprehensively summarize four decades of analytical methodologies developed for PRV and its metabolites, comparing chromatographic, spectroscopic, electrochemical, and capillary electrophoresis approaches in terms of sensitivity, selectivity, and matrix applicability. This review also evaluates essential bioanalytical nuances, including PRV's lactone–acid interconversion, matrix‐induced ion suppression, pH‐dependent instability, low ng–pg·mL −1 plasma levels, and metabolite‐specific detection challenges alongside pharmaceutical analytical considerations. The literature demonstrates that liquid chromatography–tandem mass spectrometry and high‐performance liquid chromatography remain the most sensitive and reliable platforms for ultratrace bioanalysis, while spectrophotometric and electrochemical methods provide cost‐effective alternatives for formulations and higher concentration samples, and capillary electrophoresis offers efficient separation with low solvent use. Future analytical advances should prioritize metabolite‐resolved quantification, green extraction strategies, microfluidic and point‐of‐care designs, and AI‐assisted data processing to improve sensitivity, stability assessment, and high‐throughput monitoring of PRV in clinical and environmental settings.