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Lusedra (fospropofol disodium)

Company: Elan Pharmaceuticals
Approval Status: Approved December of 2008
Treatment for: sedation and anesthesia
Areas: Neurology & Nervous System

| General Information | Clinical Results | Side Effects | Mechanism of Action | Literature References | Additional Information |


General Information

Lusedra (fospropofol disodium) is a water soluble prodrug of propofol, a sedative/hypnotic/anesthetic drug. Its mechanism of action is uncertain, but it is postulated that its primary effect may be potentiation of the GABA-A and glycine receptors, possibly by slowing the channel closing time.

Lusedra is specifically indicated for monitored anesthesia care sedation in adult patients undergoing diagnostic or therapeutic procedures.

Lusedra is supplied an aqueous solution designed for intravenous injection. The recommended initial dose of the drug is as follows:

Standard Dosing Regimen: In adults aged 18 to <65 years who are healthy or have mild systemic disease- an initial intravenous bolus of 6.5 mg/kg followed by supplemental doses of 1.6 mg/kg intravenous (25 % of initial dosage) as needed to achieve the desired level of sedation. The dosage of Lusedra is limited by lower and upper weight bounds of 60 kg and 90 kg.

Modified Dosing Regimen: Adults >65 years of age or those with severe systemic disease- initial and supplemental intravenous dosages of 75 % of the standard dosing regimen.


Clinical Results

FDA Approval
FDA approval of Lusedra was based on the results of two trials. In both trials all subjects received 50 mcg of fentanyl citrate intravenously before study sedative medication. The primary endpoint was the rate of sedation success, defined as the proportion of patients who did not respond readily to their name spoken in a normal tone of voice (Modified Observer’s Assessment of Alertness/Sedation Scale score of 4 or less) on 3 consecutive measurements taken every 2 minutes and who completed the procedure without the use of alternative sedative medication and without the use of manual or mechanical ventilation. In both studies, an initial bolus dose and up to 3 supplemental doses at 25 % of the initial bolus of study sedative medication was administered intravenously to sedate patients so that they did not respond readily to their name spoken in a normal tone and to allow the investigator to start the procedure.

Study One
This randomized, blinded, dose-controlled study enrolled patients undergoing colonoscopy. The subjects were randomized to receive the Lusedra standard or modified dosing regimen or alternative sedative medication (midazolam). Both dosing regimens of Lusedra had a sedation success rate of 87% and required a mean number of supplemental doses of 2.3 (+1.4 SD). The median procedure duration of both regimens was 11 minutes.

Study Two
This randomized, blinded, dose-controlled study enrolled patients undergoing flexible bronchoscopy. The subjects were randomized to receive the Lusedra standard or modified dosing regimen or alternative sedative medication (midazolam). Both dosing regimens of Lusedra had a sedation success rate of 89 % and required a mean number of supplemental doses of 1.7 (+ 1.6 SD). The median procedure duration of both regimens was 10 minutes.

Ongoing Study Commitments

  • Eisai has agreed to conduct a randomized, double-blind, dose-controlled clinical trial of fospropofol disodium injection in adolescent patients (12 through 18 years old) undergoing upper endoscopy. Pharmacokinetics will be studied using a population PK approach.
    Protocol Submission: by October 1, 2009
    Study Start Date: by March 1, 2010
    Final Report Submission: by April 1, 2012
  • Eisai has agreed to conduct a randomized, double-blind, dose-controlled clinical trial of fospropofol disodium injection in children (ages 3 up to 12 years old) undergoing sedation for magnetic resonance imaging (MRI). Pharmacokinetics will be studied using a population PK approach.
    Protocol Submission: January 1, 2012
    Study Start Date: June 1, 2012
    Final Report Submission: July 1, 2014
  • Eisai has agreed to conduct a randomized, double-blind, dose-controlled clinical trial of fospropofol disodium injection in infants and very young children (ages one month up to three years old) undergoing sedation for procedures such as lumbar puncture and/or MRI. Pharmacokinetics will be studied using a population PK approach.
    Protocol Submission: April 1, 2014
    Start Date: September 1, 2014
    Final Report Submission: August 1, 2016
  • Eisai has agreed to conduct a randomized, double-blind, dose-controlled clinical trial of fospropofol disodium injection in neonates (less than one month of age) undergoing sedation for procedures such as lumbar puncture, MRI, and/or circumcision. Pharmacokinetics will be studied using a population PK approach.
    Protocol Submission: October 1, 2014
    Start Date: October 1, 2016
    Final Report Submission: April 1, 2018
  • Eisai has agreed to A dose-ranging clinical trial to evaluate the risk-benefit ratio of Lusedra in patients classified as ASA III or IV, adult patients weighing less than 60 kg, and geriatric patients.
    Protocol Submission: by November 2009
    Trial Start Date: by April 2010
    Final Report Submission: by January 2012
  • Eisai has agreed to a single-dose, open-label, pharmacokinetic trial in breastfeeding women receiving fospropofol for a needed procedure. Concentrations of Lusedra will be assessed in maternal plasma and breast milk so as to estimate potential infant exposure.
    Protocol Submission: by August 1, 2009
    Trial Start Date: by July 1, 2010
    Final Report Submission: by November 1, 2012

Side Effects

Adverse events associated with the use of Lusedra may include, but are not limited to, the following:
  • Paresthesias
  • Pruritus
  • Hypotension
  • Hypoxemia
  • Nausea

Mechanism of Action

Lusedra (fospropofol disodium) is a water soluble prodrug of propofol, a sedative/hypnotic/anesthetic drug. Its mechanism of action is uncertain, but it is postulated that its primary effect may be potentiation of the GABA-A and glycine receptors, possibly by slowing the channel closing time.

Literature References

Silvestri GA, Vincent BD, Wahidi MM, Robinette E, Hansbrough JR, Downie GH A phase 3, randomized, double-blind study to assess the efficacy and safety of fospropofol disodium injection for moderate sedation in patients undergoing flexible bronchoscopy. Chest 2009 Jan;135(1):41-7

Cohen LB Clinical trial: a dose-response study of fospropofol disodium for moderate sedation during colonoscopy. Alimentary Pharmacology & Therapeutics 2008 Apr 1;27(7):597-608

Fechner J, Schwilden H, Schüttler J Pharmacokinetics and pharmacodynamics of GPI 15715 or fospropofol (Aquavan injection) - a water-soluble propofol prodrug. Handbook of Experimental Pharmacology 2008;(182):253-66

Struys MM, Vanluchene AL, Gibiansky E, Gibiansky L, Vornov J, Mortier EP, Van Bortel L AQUAVAN injection, a water-soluble prodrug of propofol, as a bolus injection: a phase I dose-escalation comparison with DIPRIVAN (part 2): pharmacodynamics and safety. Anesthesiology 2005 Oct;103(4):730-43

Gibiansky E, Struys MM, Gibiansky L, Vanluchene AL, Vornov J, Mortier EP, Burak E, Van Bortel L AQUAVAN injection, a water-soluble prodrug of propofol, as a bolus injection: a phase I dose-escalation comparison with DIPRIVAN (part 1): pharmacokinetics. Anesthesiology 2005 Oct;103(4):718-29

Fechner J, Ihmsen H, Hatterscheid D, Schiessl C, Vornov JJ, Burak E, Schwilden H, Schüttler J Pharmacokinetics and clinical pharmacodynamics of the new propofol prodrug GPI 15715 in volunteers. Anesthesiology 2003 Aug;99(2):303-13


Additional Information

For additional information regarding Lusedra or anesthesia care sedation, please visit the Lusedra web page.


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Lusedra Drug Information

The Lusedra drug information shown above is licensed from Thomson CenterWatch. The information provided here is for general educational purposes only and does not constitute medical or pharmaceutical advice which should be sought from qualified medical and pharmaceutical advisers.





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