Fospropofol, a sedative-hypnotic agent, serves as a solution for monitored anesthesia care (MAC) sedation in adults undergoing diagnostic or therapeutic procedures. As a water-soluble prodrug, it transforms into propofol within the liver. This short-acting agent is employed for hypnotic, sedative, and anesthetic purposes. It notably lacks the propensity to induce injection-site pain, unlike propofol, due to its inability to activate TRPA1. FDA-approved in December 2008, it is classified as a Schedule IV controlled substance under the Controlled Substances Act in the United States. Specifically designed for monitored anesthesia care sedation during procedures such as bronchoscopy, colonoscopy, and minor surgeries like arthroscopy and bunionectomy, fospropofol offers a suitable solution. As a prodrug of propofol, fospropofol differs in its water solubility, allowing administration in aqueous solutions. 1.86 mg of fospropofol is equivalent to 1 mg of propofol in terms of molar equivalence. Following its conversion into propofol by endothelial alkaline phosphatase in vivo, propofol traverses the blood-brain barrier, binding to GABA-A receptors and acting as an agonist. This binding increases chloride conductance, leading to the inhibition of post-synaptic neuron firing. Sufficient sedation is achieved approximately 7 minutes after a 10 mg/kg IV bolus dose. Recovery from fospropofol-induced sedation takes between 21 to 45 minutes. After an intravenous bolus of 6 mg/kg in a healthy subject, fospropofol's pharmacokinetic parameters include: Cmax = 78.7 μg/mL; Tmax = 4 minutes; AUC(0-∞) = 19.0 μg ⋅ h/mL.

Fospropofol Pathway References