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Fospropofol
Systematic (IUPAC) name
dihydrogen (2,6-diisopropylphenoxy)methyl phosphate
Identifiers
ATC code none
PubChem 3038497
Chemical data
Formula C13H21O5P 
Mol. mass 288.276 g/mol
Therapeutic considerations
Pregnancy cat.  ?
Legal status Schedule IV (US)
Routes Intravenous

Fospropofol (trade name Lusedra[1]) is a sedative/anesthetic drug which is classified as a Schedule IV controlled substance in the United States' Controlled Substances Act.[2] A range of water-soluble derivatives and prodrugs of the widely used sedative-hypnotic / anaesthetic drug propofol were developed, of which fospropofol was found to be the most suitable for clinical development.[3][4] It is metabolized into propofol by the liver. This fact means that blood levels of propofol after the administration of a bolus of fospropofol reach lower peak levels than for an equipotent dose of propofol and also that its clinical effect is more sustained.[5][6] These traits can be desirable for endoscopic procedures such as upper GI endoscopy, colonoscopy, bronchoscopy, as well as for some surgical procedures done under local or regional anesthesia. Often, fospropofol is administered in conjunction with an opioid such as fentanyl.

One advantage of fospropofol is that, being water-soluble, the problems associated with lipid formulated propofol (e.g., pain at the IV catheter site, potential for hyperlipidemia with long-term administration, and an increased chance for bacteremia) are expected to be less frequent.

Following the administration of fospropofol 12.5 mg/kg (the maximum recommended dose) loss of consciousness takes about four minutes, compared to one circulatory time with propofol 2.5 mg/kg (the maximum recommended dose).[7]

Contents

Metabolism

Metabolised by alkaline phosphatases to propofol, formaldehyde, and phosphate. Propofol is further metabolised to the glucuronide (34.8%) and the quinol glucuronides. Formaldehyde is a known carcinogen but label information states that the formaldehyde levels are similar to regular background levels. No long term studies have been done on the cancer risks. The parent drug has a terminal elimination half-life of 0.88+/-0.08 hours, which is non-renal.[8]

References

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Notes

  1. ^ http://www.asahq.org/news/asanews121508.htm
  2. ^ "Schedule of Controlled Substances; Placement of Fospropofol into Schedule IV," 74 Federal Register 192 (October 6, 2009), pp. 51234–51236.
  3. ^ Cooke A, Anderson A, Buchanan K, Byford A, Gemmell D, Hamilton N, McPhail P, Miller S, Sundaram H, Vijn P. Water-soluble propofol analogues with intravenous anaesthetic activity. Bioorganic and Medicinal Chemistry Letters. 2001 Apr 9;11(7):927-30. PMID 11294393
  4. ^ Bennett DJ, Anderson A, Buchanan K, Byford A, Cooke A, Gemmell DK, Hamilton NM, Maidment MS, McPhail P, Stevenson DF, Sundaram H, Vijn P. Novel water soluble 2,6-dimethoxyphenyl ester derivatives with intravenous anaesthetic activity. Bioorganic and Medicinal Chemistry Letters. 2003 Jun 16;13(12):1971-5. PMID 12781176
  5. ^ 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. PMID 18175095
  6. ^ Shah A, Mistry B, Gibiansky E, Gibiansky L. Fospropofol assay: issues and impact on pharmacokinetic and pharmacodynamic evaluation. European Journal of Anaesthesiology. 2009 Jan;26(1):81; discussion 81-2. PMID 19122558
  7. ^ Gan TJ (2006). "Pharmacokinetic and pharmacodynamic characteristics of medications used for moderate sedation". Clin Pharmacokinet 45 (9): 855–69. PMID 16928150. 
  8. ^ [1]

Sources


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