phospropofol disodium

Phospropofol disodium is a water-soluble phosphate ester prodrug of the intravenous anesthetic propofol. Upon administration, it is rapidly hydrolyzed by endothelial alkaline phosphatases into propofol, formaldehyde, and inorganic phosphate. The active metabolite, propofol, acts as a positive allosteric modulator of the gamma-aminobutyric acid type A (GABA-A) receptor, enhancing inhibitory neurotransmission to induce dose-dependent sedation and anesthesia. Developed by MGI Pharma (later acquired by Eisai), phospropofol was FDA-approved in 2008 for monitored anesthesia care (MAC) sedation in adults undergoing diagnostic or therapeutic procedures. Unlike traditional propofol lipid emulsions, phospropofol is a clear aqueous solution that avoids injection-site pain and the risks associated with lipid formulations, such as hyperlipidemia or bacterial contamination, although it exhibits a slower onset and longer recovery profile due to the required metabolic conversion.

Brand names

Lusedra

Other names

phospropofolpropofol phosphate