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- Injection, solution 35 mg/mL
Prodrug of propofol. Produces sedation/hypnosis with minimal excitation; decreases intraocular pressure and systemic vascular resistance; suppresses cardiac output and respiratory drive.
AUC and C max are dose proportional. T max is 12 min following a 6 mg/kg dose.
Propofol Vd is 5.8 L/kg. Both fospropofol and its active metabolite, propofol, are approximately 98% protein bound, primarily to albumin.
Fospropofol is metabolized by alkaline phosphatase to propofol, formaldehyde, and phosphate. Propofol is further metabolized to several metabolites, the major one being propofol glucuronide. Fospropofol is not a CYP substrate.
Total body Cl of propofol in patients is 2.74 L/h/kg and the half-life is approximately 2 h.
Special PopulationsRenal Function Impairment
Does not affect the pharmacokinetics.Hepatic Function Impairment
Pharmacokinetics have not been adequately studied.
Indications and Usage
For monitored anesthesia care sedation in adult patients undergoing diagnostic or therapeutic procedures.
Dosage and AdministrationAdults
IV Start with a 6.5 mg/kg bolus followed by 1.6 mg/kg as needed to achieve desired level of sedation. Adults weighing less than 60 kg should be dosed as if they weigh 60 kg. Adults weighing more than 90 kg should be dosed as if they weigh 90 kg.Dose Modification
IV Adults 65 yr of age and older or those with severe systemic disease should receive initial and supplemental doses that are 75% of the standard dose.
- Administer as an IV bolus.
- Use supplemental oxygen for patients undergoing sedation.
- Dosage should be individualized and titrated to the level of sedation required for the procedure.
- Supplemental doses should be based on the patient's level of sedation and the level of sedation required for the procedure.
- Do not mix with other drugs or fluids prior to administration.
- Fosprofolol is physically incompatible with meperidine and midazolam.
Store at 59° to 86°F.
Drug InteractionsCNS depressants, cardiorespiratory depressants
Additive CNS and cardiorespiratory depressant effects may occur.
Laboratory Test Interactions
None well documented.
Paresthesia (74%); headache (2%).
Nausea (4%); vomiting (3%).
Procedural pain (2%).
Patients should be continuously monitored and facilities for maintenance of a patent airway, providing artificial ventilation, administering supplemental oxygen, and instituting CV resuscitation must be immediately available. Monitor continuously during sedation and through recovery for early signs of airway obstruction, apnea, hypotension, and/or oxygen desaturation.
Category B .
Propofol is excreted in breast milk.
Safety and efficacy not established.
Modify dose in patients 65 yr of age and older.
No dosage adjustments are needed in patients with CrCl of 30 mL/min or more. Safety and efficacy not established in patients with CrCl less than 30 mL/min.
Use with caution.
Hypoxia, detectable by pulse oximetry, may occur.
Loss of spontaneous respiration may occur.
Patients may become unresponsive or minimally responsive to vigorous tactile or painful stimulation.
Cardiopulmonary depression, signs of formate toxicity such as anion-gap metabolic acidosis or hypocalcemia with paresthesia, muscle spasms, and seizures.
- Advise patient that a patient escort should be considered, especially when treated on an outpatient basis. When patients may again engage in activity requiring complete metal alertness, coordination, and/or physical dexterity such as operating hazardous machinery or driving a motor vehicle, must be individualized.
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