Propofol
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| 2,6-bis(1-methylethyl)-phenol
or 2,6-diisopropylphenol | |
| CAS number 2078-54-8 | ATC code N01AX10 |
| Chemical formula | C12H18O |
| Molecular weight | 178.273 |
| Bioavailability | ? |
| Metabolism | Hepatic glucuronidation |
| Elimination half-life | 30-60 minutes
(Distribution half-life 2-4 minutes) |
| Excretion | Renal excretion of inactive metabolites |
| Pregnancy category | B (USA) C (Australia) |
| Legal status | Legend drug (USA) |
| Routes of administration | 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 intensive care unit (ICU) sedation for intubated, mechanically ventilated adults.
Propofol is approved for the induction and maintenance of anesthesia in more than 50 countries.
Propofol.jpg
Initial clinical trials were in 1977, in a form solubilised in cremophor EL, but due to anaphylactoid reactions it was withdrawn from the market. It was subsequently reformulated as an acqueous emulsion in intralipid and re-launched in 1986 by AstraZeneca with the brand name Diprivan. The current preparation is 1% propofol solubilised with 2.25% glycerol, 10% soybean oil and 1.2% purified egg phospholipid, and has a pH between 6.0 and 8.5.
It is highly protein bound in vivo and is metabolised by conjugation in the liver. Its mechanism of action is uncertain, but it is postulated that its primary effect may be at the GABA-A receptor.
Aside from the hypotension in induction doses, one of its most frequent side-effects is its pain on injection, especially in smaller veins.
It appears to be safe for use in porphyria, and does not trigger malignant hyperpyrexia. Although the elimination half-life is 2-4 hours, its clinical effect is much shorter because of its rapid redistribution.
External link
- Diprivan web site (http://www.diprivan.com/) run by AstraZeneca
- Detailed pharmaceutical information (http://www.drugs.com/MMX/Propofol.html)