The growing prevalence of pharmaceutical compounds in the environment raises significant concerns due to their potential impacts on ecological and human health. This present manuscript focuses on the methods used to extract and determine these pharmaceuticals in water samples. It provides a comprehensive analysis of the extraction techniques and analytical approaches employed for the identification and quantification of pharmaceuticals in environmental water. Due to their chemical properties and widespread use, pharmaceuticals persist in the environment and contaminate water bodies, soil, and sediments. The presence of pharmaceuticals in the aquatic environment has been linked to several adverse effects on aquatic organisms, including the disruption of physiological processes and reproductive impairment. Furthermore, pharmaceuticals in the environment can affect human health through food and drinking water contamination and contribute to antibiotic resistance. The analysis of pharmaceutical contaminants in water samples presents several challenges due to the complex matrix and low concentrations of target substances. Various sample preparation techniques and protocols, including solid-phase extraction (more than 76% of the studied literature) and QuEChERS (quick, easy, cheap, effective, rugged, and safe), coupled with liquid chromatography–tandem-mass spectrometry, are commonly used for their determination. These methods offer high sensitivity, selectivity, and efficiency in identifying and quantifying pharmaceuticals in environmental samples. It is, therefore, essential that ongoing research is conducted in order to develop more efficient analytical methods and mitigation strategies to address pharmaceutical contamination in the environmental water effectively. It is also crucial that increased awareness and regulatory measures are put in place in order to minimize the environmental and human health risks associated with pharmaceutical pollutants.