Fospropofol

Pronunciation: fos-proe-POE-fol
Class: Sedative/Hypnotic

Trade Names

Lusedra
- Injection, solution 35 mg/mL

Pharmacology

Prodrug of propofol. Produces sedation/hypnosis with minimal excitation; decreases intraocular pressure and systemic vascular resistance; suppresses cardiac output and respiratory drive.

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Pharmacokinetics

Absorption

AUC and C max are dose proportional. T max is 12 min following a 6 mg/kg dose.

Distribution

Propofol Vd is 5.8 L/kg. Both fospropofol and its active metabolite, propofol, are approximately 98% protein bound, primarily to albumin.

Metabolism

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.

Elimination

Total body Cl of propofol in patients is 2.74 L/h/kg and the half-life is approximately 2 h.

Special Populations

Renal 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.

Contraindications

Standard considerations.

Dosage and Administration

Adults

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
Adults

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.

General Advice

  • 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.

Storage/Stability

Store at 59° to 86°F.

Drug Interactions

CNS depressants, cardiorespiratory depressants

Additive CNS and cardiorespiratory depressant effects may occur.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Hypotension (7%).

CNS

Paresthesia (74%); headache (2%).

Dermatologic

Pruritus (28%).

GI

Nausea (4%); vomiting (3%).

Respiratory

Hypoxia (11%).

Miscellaneous

Procedural pain (2%).

Precautions

Monitor

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.


Pregnancy

Category B .

Lactation

Propofol is excreted in breast milk.

Children

Safety and efficacy not established.

Elderly

Modify dose in patients 65 yr of age and older.

Renal Function

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.

Hepatic Function

Use with caution.

Hypotension

May occur.

Hypoxia

Hypoxia, detectable by pulse oximetry, may occur.

Respiratory depression

Loss of spontaneous respiration may occur.

Responsiveness

Patients may become unresponsive or minimally responsive to vigorous tactile or painful stimulation.

Overdosage

Symptoms

Cardiopulmonary depression, signs of formate toxicity such as anion-gap metabolic acidosis or hypocalcemia with paresthesia, muscle spasms, and seizures.

Patient Information

  • 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.

Copyright © 2009 Wolters Kluwer Health.

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