Drug intelligence / Profile preview

fospropofol disodium

Development stage
Approved
Lead developer
Eisai
Modality
Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

Fospropofol disodium is a water-soluble prodrug of propofol, developed as an intravenous sedative-hypnotic agent primarily indicated for monitored anesthesia care (MAC) sedation in adult patients undergoing diagnostic or therapeutic procedures. After intravenous administration, it is metabolized by alkaline phosphatases to release the active compound propofol, along with phosphate and formaldehyde. The released propofol acts mainly as an agonist at the gamma-aminobutyric acid type A (GABA-A) receptor in the central nervous system, increasing chloride conductance and causing neuronal hyperpolarization that results in sedation. Compared to lipid-based propofol formulations, fospropofol offers advantages such as reduced pain at the injection site and a smoother hemodynamic profile due to its slower onset and more prolonged action. It was approved by the FDA in December 2008 and is classified as a Schedule IV controlled substance in the United States[1][2][3][4][5][6].

Brand names
Lusedra
Other names
fospropofolfospropofol disodium injection
02

Targets

GABRR (GABA-A receptor subunit rho)NMDAR (Glutamate receptor ionotropic, NMDA)

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