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Propofol (P) is metabolized in humans by oxidation to 1,4-di-isopropylquinol (Q). P and Q are in turn conjugated with glucuronic acid to the respective glucuronides, propofol glucuronide (Pgluc), quinol-1-glucuronide (Q1G) and quinol-4-glucuronide (Q4G). Propofol and quinol with their glucuronide conjugates can be measured directly by gradient high-performance liquid chromatographic analysis without enzymic hydrolysis.
Time profile of mean renal excretion rate of propofol glucuronide, quinol-1-glucuronide (Q1gluc) and quinol-4-glucuronide (Q4gluc) in nine patients during OK surgery. The percentages are the percentage of the dose excreted in the urine during 60 h. (sd values are omitted for reasons of clarity in the figure.
Formaldehyde and phosphate plasma concentrations are comparable to endogenous levels when fospropofol disodium is administered as recommended. Formaldehyde is further metabolized to formate by several enzyme systems, including formaldehyde dehydrogenase, present in various tissues. Propofol liberated from fospropofol is further metabolized to major metabolites propofol glucuronide (34. 8%), quinol-4-sulfate (4. 6%), quinol-1-glucuronide.