Fospropofol, A New Sedative Anesthetic, and Its Utility in the Perioperative Period

Abstract

Fospropofol is an intravenous sedative-anesthetic agent that is FDA-approved for monitored anesthesia care (MAC) sedation in adult patients undergoing diagnostic or therapeutic procedures. As a prodrug of propofol, fospropofol's pharmacologic activity results from its breakdown by alkaline phosphatase and release of propofol, which is the active molecule. It exhibits a longer time to peak clinical effect and a more prolonged action compared to propofol. Thus patients may exhibit smoother hemodynamic and respiratory depression compared to propofol lipid emulsion bolus. Another advantage over propofol is that it does not induce a burning sensation on IV administration. Side effects include perineal paresthesia and itching, respiratory depression, hypoxemia, hypotension, loss of consciousness, and apnea with higher IV boluses. Therefore, current recommendations call for it to be administered only by clinicians trained in general anesthesia, who are thus skilled in advanced airway management. Fospropofol has a unique dosing regimen, with a standard dose for adults 18-65 years of age, and a modified dose (75% of the standard dose) for patients > 65 years of age and for sicker adult patients whose American Society of Anesthesiologists physical status score is ≥ 3. Also, the minimum and maximun IV bolus doses are body-weight adjusted to 60 and 90 kg respectively. Available evidence demonstrates that fospropofol in MAC sedation is successful in patients undergoing esophagogastroscopy, colonoscopy and flexible bronchoscopy. The use of fospropofol is also now being explored in many other perioperative settings. In light of current shortages of many anesthetic drugs, whether forspropofol can take the place of propofol in ICUs and operating rooms remains to be determined.

Nebulized dexmedetomidine-lidocaine inhalation as a premedication for flexible bronchoscopy: a randomized trial

“…An increasing number of recent studies have shown that MAC with laryngeal mask ventilation has unique advantages for outpatient flexible bronchoscopy management (18). It provides appropriate operating conditions for the bronchoscopist and accelerates recovery (19,20). Intravenous infusion of propofol and remifentanil combined with dexmedetomidine has been used for flexible bronchoscopy in previous reports (13).…”

The efficacy of dexmedetomidine-remifentanil versus dexmedetomidine-propofol in children undergoing flexible bronchoscopy

“…It cannot only provide excellent operating conditions for the bronchoscopist but also accelerate children rapid recovery. [16,20] Previously, benzodiazepines are one of the most commonly used drugs during flexible bronchoscopy. They play the role of muscle relaxant besides sedative, hypnotic and anxiolytic though the γ-aminobutyric acid receptor.…”

Structural Modification in Anesthetic Drug Development for Prodrugs and Soft Drugs

“…For prodrugs, due to the existence of enzymatic and/or chemical transformation processes, the therapeutic effects of the parent drug are usually delayed. Since the enzymatic conversion to propofol is timedependent, fospropofol may theoretically provide a better safety profile, especially in cardiac and respiratory functions (Abdelmalak et al, 2012). For example, recent studies have shown a decreased incidence of hypotension and respiratory depression with fospropofol because of its slower onset of action (Luo et al, 2022).…”