Propofol
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Propofol
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| Systematic (IUPAC) name | |
| 2,6-diisopropylphenol | |
| Identifiers | |
| CAS number | |
| ATC code | N01 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C12H18O |
| Mol. mass | 178.271 g/mol |
| Pharmacokinetic data | |
| Bioavailability | NA |
| Protein binding | 95 to 99% |
| Metabolism | Hepatic glucuronidation |
| Half life | 30 to 60 min |
| Excretion | Renal |
| Therapeutic considerations | |
| Pregnancy cat. | |
| Legal status |
℞-only (U.S.) |
| Routes | Intravenous |
Propofol is a short-acting intravenous anesthetic agent used for the induction of general anesthesia in adult patients and pediatric patients older than 3 years of age; maintenance of general anesthesia in adult patients and pediatric patients older than 2 months of age; and sedation in medical contexts, such as intensive care unit (ICU) sedation for intubated, mechanically ventilated adults, and in procedures such as colonoscopy.
Propofol is approved for the induction and maintenance of anesthesia in more than 50 countries.
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[edit] Chemistry
Propofol is a water-immiscible oil and so cannot be injected per se. Initial clinical trials were in 1977, in a form solubilised in cremophor EL, but due to anaphylactic reactions it was withdrawn from the market. It was subsequently reformulated as an emulsion of a soya oil/propofol mixture in water, and re-launched in 1986 by AstraZeneca with the brand name Diprivan (Shortened version of DI-isoPRopyl IV ANesthetic). The current preparation is 1% propofol, 10% soybean oil and 1.2% purified egg phospholipid (emulsifier), with 2.25% of glycerol as a tonicity adjusting agent, and sodium hydroxide to adjust the pH. Diprivan contains EDTA as an antimicrobial agent. Newer generic formulations contain sodium metabisulfite or benzyl alcohol. Propofol emulsion appears as a highly opaque white fluid due to the scattering of light from the tiny (~150 nm) oil droplets that it contains.
[edit] Pharmacology
Propofol is highly protein bound in vivo and is metabolised by conjugation in the liver. Its rate of clearance exceeds hepatic blood flow, suggesting an extrahepatic site of elimination as well. Its mechanism of action is uncertain, but it is postulated that its primary effect may be potentiation of the GABA-A receptor, possibly by slowing the closing channel time. Recent research has also suggested the endocannabinoid system may contribute significantly to Propofol's anesthetic action and to its unique properties.[1]
The elimination half-life of propofol has been estimated to be between 2-24 hours. However, its duration of clinical effect is much shorter because propofol is rapidly distributed into peripheral tissues.
[edit] Side effects
Aside from the hypotension and transient apnea following induction doses, one of propofol's most frequent side effects is pain on injection, especially in smaller veins. This pain can be mitigated by pretreatment with lidocaine.[2] Patients tend to show great variability in their response to propofol, at times showing profound sedation with small doses. Many medical professionals believe that it should only be administered by anesthesiologists who are trained in airway management.[attribution needed]
Propofol appears to be safe for use in porphyria, and has not been known to trigger malignant hyperpyrexia.
[edit] Trivia
A common hospital-worker slang term for Propofol is "Milk of Amnesia", due to its milky appearance.
Also known as "Mother's Milk"
[edit] References
- ^ Fowler, CJ. "Possible involvement of the endocannabinoid system in the actions of three clinically used drugs." Trends Pharmacol. Sci. 2004 Feb;25(2):59-61.
- ^ Propofol Drug Information,Professional. drugs.com. Retrieved on January 2, 2007.
[edit] External links
- Diprivan web site run by AstraZeneca
- Detailed pharmaceutical information
- Links to external chemical sources
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| Barbiturates | Hexobarbital, Methohexital, Narcobarbital, Thiopental |
| Ethers | Diethyl ether,Desflurane, Enflurane, Isoflurane, Methoxyflurane, Methoxypropane, Sevoflurane, Vinyl ether |
| Haloalkanes | Chloroform, Halothane, Trichloroethylene |
| Opioids | Alfentanil, Anileridine, Fentanyl, Phenoperidine, Remifentanil, Sufentanil |
| Others | Alfaxalone, Droperidol, Esketamine, Etomidate, Hydroxybutyric acid, Ketamine, Minaxolone, Nitrous oxide, Propanidid, Propofol, Xenon |
