This paper presents a comprehensive and critical analysis of the removal of pharmaceuticals (PhCs), the governing physicochemical properties, and removal mechanisms in constructed wetlands (CWs). The average removal efficiency of the most widely studied 34 PhCs ranges from 21% to 93%, with the exception of one PhC that exhibited negative removal. Moreover, CWs are effective in significantly reducing the environmental risk caused by many PhCs. Based on risk assessment, 12 PhCs were classified under high risk category (oxytetracycline > ofloxacin > sulfamethoxazole > erythromycin > sulfadiazine > gemfibrozil > ibuprofen > acetaminophen > salicylic acid > sulfamethazine > naproxen > clarithromycin), which could be considered for regular monitoring, water quality standard formulation and control purposes. Biodegradation (aerobic and anaerobic) is responsible for the removal of the majority of PhCs, often in conjunction with other mechanisms (e.g., adsorption/sorption, plant uptake, and photodegradation). The physicochemical properties of molecules play a pivotal role in the elimination processes, and could serve as important predictors of removal. The correlation and multiple linear regression analysis suggest that organic carbon sorption coefficient (Log Koc), octanol-water distribution coefficient (Log Dow), and molecular weight form a good predictive linear regression model for the removal efficiency of PhCs (R2 = 0.65, P-value <0.05).