Approved December 12, 2008

FOSPROPOFOL DISODIUM
(FDA Category 2S)

LUSEDRA (Eisai): Fospropofol disodium is a watersoluble, phosphate ester prodrug, which is hydrolysed to release propofol, which interacts with the GABA receptors of the CNS resulting in sedation.

DOSING INFORMATION: Initiate fospropofol at a dose of 6.5 mg/kg IV bolus, followed immediately by supplemental doses at 1.6 mg/kg no more frequently than every 4 minutes as needed to achieve the desired level of sedation. Doses and rates of administration should be individualized and titrated to level of sedation required for the procedure.

PHARMACOKINETICS: The median time to sedation was 8 minutes. The median time to fully alert was 5 minutes. The time to peak concentration was 2 hours and 4 hours after 18 mg/kg and 6 mg/kg intravenous bolus doses, respectively. Protein binding is 98%. Fospropofol has a low volume of distribution of 0.33 +/- 0.069 L/kg and the liberated propofol has a large volume of distribution (5.8 L/kg). Fospropofol is completely metabolized by alkaline phosphatases and is not a substrate of CYP450 enzymes. The t 1/2 was 0.81 +/- 0.08 and 0.88 +/- 0.08 hours in healthy volunteers and patients, respectively.

CAUTIONS: Patients with compromised myocardial function, reduced vascular tone, or reduced intravascular volume may be at increased risk for complications due to propofol induced hypotension. There is an increased risk of respiratory depression in patients with severe systemic disease and the elderly. Nonsustained ventricular tachycardia and apnea have been reported. Common adverse effects were hypoxemia, paresthesia, and pruritus.

FDA APPROVED INDICATIONS: Fospropofol is indicated for monitored anesthesia care (MAC) in patients undergoing diagnostic or therapeutic procedures.