Fospropofol for Procedural Sedation: A Narrative Review of Pharmacology, Efficacy, and Safety Considerations

Fospropofol is an aqueous-soluble prodrug of propofol designed for short-term sedation in diagnostic and therapeutic interventions under monitored anaesthesia care. In contrast to lipid formulations of propofol, fospropofol is enzymatically converted to active propofol, exhibiting a slower onset of action but with several benefits, including decreased pain on injection, improved chemical stability, and a significantly lower risk of microbial contamination. This review provides an overall discussion of fospropofol’s chemical structure, pharmacologic profile, pharmacokinetic properties, and pharmacodynamic actions, highlighting its unique characteristics when compared with conventional propofol. Fospropofol offers well-tolerated and effective sedation, with high patient satisfaction and a good safety profile. Potential side-effects, particularly those affecting the respiratory and cardiovascular systems, are examined. The review discusses regulatory factors, formulary issues, comparative assessment with other sedatives, and clinical use considerations. New indications, off-label uses, and future research directions are investigated to inform both immediate clinical practice and future innovation. This review aims to educate anaesthesiologists and clinicians on the evolving role of fospropofol and to encourage further studies into its expanding clinical applications. This review highlights the evolving role of fospropofol in sedation, underscoring its potential as a safer alternative to traditional propofol, with unique pharmacologic benefits and promising opportunities for future therapeutic applications.