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| Clinical data | |
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| AHFS/Drugs.com | Monograph |
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| Dependence liability | unknown |
| Routes of administration | Intravenous |
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| Pharmacokinetic data | |
| Protein binding | 98%[1] |
| Metabolism | Hepaticglucuronidation |
| Eliminationhalf-life | 0.81 hours[1] |
| Excretion | Renal |
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| Chemical and physical data | |
| Formula | C13H21O5P |
| Molar mass | 288.280 g·mol−1 |
| 3D model (JSmol) | |
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Fospropofol (INN[3]), often used as thedisodium salt (trade nameLusedra[4]) is anintravenoussedative-hypnotic agent. It is currently approved for use in sedation of adult patients undergoingdiagnostic ortherapeutic procedures such asendoscopy.
Severalwater-soluble derivatives andprodrugs of the widely used intravenous anesthetic agentpropofol have been developed, of which fospropofol has been found to be the most suitable for clinical development thus far.[5][6] Purported advantages of this water-solublechemical compound include less pain at the site of intravenous administration, less potential forhyperlipidemia with long-term administration, and less chance forbacteremia.[citation needed] Often, fospropofol is administered in conjunction with an opioid such asfentanyl.[citation needed]
Fospropofol is a prodrug of propofol; as anorganophosphate it is metabolized byalkaline phosphatases tophosphate andformaldehyde and theactive metabolite, propofol.
Initial trial results on fospropofol pharmacokinetics were retracted by the investigators. As of 2011, new results were not available.[7]
Following the administration of fospropofol 12.5 mg/kg (the maximum recommended dose)loss of consciousness takes about four minutes, compared to one arm-brain circulation time with propofol 2.5 mg/kg (the maximum recommended dose).[8]
Fospropofol ismetabolized in theliver by alkaline phosphatases to propofol,formaldehyde, andphosphate. The hepatic metabolism of this prodrug to an active metabolite means that peakplasma levels of propofol after the administration of a bolus of fospropofol are lower than for anequipotent dose of propofol and also that its clinical effect is more sustained.[9][10] These features can be desirable for endoscopic procedures such asesophagogastroduodenoscopy,colonoscopy,bronchoscopy, as well as for some surgical procedures done underlocal orregional anesthesia.
Propofol is further metabolised to propofolglucuronide (34.8%) andquinol glucuronide.[11] Formaldehyde is a knowncarcinogen but label information states that serum formaldehyde levels are similar to background levels. No long term studies have been done on thecancer risks. The parent drug has a terminalelimination half-life of 0.88+/-0.08 hours, which is non-renal.[12]
Fospropofol is classified as aSchedule IV controlled substance in the United States'Controlled Substances Act.[13]
