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Fospropofol

Catalog No. DB06716 Name DrugBank
CAS Number 258516-87-9 Website http://www.ualberta.ca/
M. F. C13H19Na2O5P Telephone (780) 492-3111
M. W. 332.240261 Fax (780) 492-1071
Purity Email david.wishart@ualberta.ca
Storage Chembase ID: 4453

SYNONYMS

IUPAC name
disodium 2,6-bis(propan-2-yl)phenoxymethyl phosphate
IUPAC Traditional name
dipotassium 2,6-diisopropylphenoxymethyl phosphate
Brand Name
Lusedra

DATABASE IDS

CAS Number 258516-87-9
PubChem SID 99443268
PubChem CID 3038497

PROPERTIES

DETAILS

Description (English)
Item Information
Drug Groups approved
Description Fospropofol is a prodrug and gets converted into Propofol in the liver. Fospropofol is, therefore, a short acting hypnotic/sedative/anesthetic agent. It has uses in general anesthesia, procedure sedation, and veterinary medicine.
Indication Used for induction and/or maintenance of anaesthesia and for management of refractory status epilepticus.
Pharmacology Fospropofol is a prodrug of propofol, a sedative hypnotic drug. Unlike propofol, fospropofol is water soluble and can be administered in an aqueous solution. Fospropofol is metabolized to propofol by phosphatases into propofol, fomaldehyde and phosphate. Propofol is a sedative-hypnotic agent for use in the induction and maintenance of anesthesia or sedation. Intravenous injection of a therapeutic dose of propofol produces hypnosis rapidly with minimal excitation, usually within 40 seconds from the start of an injection (the time for one arm-brain circulation).
Toxicity Overdosage may increase pharmacologic and adverse effects or cause death.
Biotransformation Hepatically metabolized mainly by glucuronidation at the C1-hydroxyl. Hydroxylation of the benzene ring to 4-hydroxypropofol may also occur via CYP2B6 and 2C9 with subsequent conjugation to sulfuric and/or glucuronic acid. Hydroxypropofol has approximately 1/3 of hypnotic activity of propofol.
Absorption Rapid - time to onset of unconsciousness is 15-30 seconds, due to rapid distribution from plasma to the CNS. Distribution is so rapid that peak plasma concentrations cannot be readily measured. Duration of action is 5-10 minutes.
Elimination It is chiefly eliminated by hepatic conjugation to inactive metabolites which are excreted by the kidney.
References
Garnock-Jones KP, Scott LJ: Fospropofol. Drugs. 2010 Mar 5;70(4):469-77. doi: 10.2165/11204450-000000000-00000. [Pubmed]
Schywalsky M, Ihmsen H, Tzabazis A, Fechner J, Burak E, Vornov J, Schwilden H: Pharmacokinetics and pharmacodynamics of the new propofol prodrug GPI 15715 in rats. Eur J Anaesthesiol. 2003 Mar;20(3):182-90. [Pubmed]
External Links
Wikipedia

REFERENCES

  • Garnock-Jones KP, Scott LJ: Fospropofol. Drugs. 2010 Mar 5;70(4):469-77. doi: 10.2165/11204450-000000000-00000. Pubmed
  • Schywalsky M, Ihmsen H, Tzabazis A, Fechner J, Burak E, Vornov J, Schwilden H: Pharmacokinetics and pharmacodynamics of the new propofol prodrug GPI 15715 in rats. Eur J Anaesthesiol. 2003 Mar;20(3):182-90. Pubmed