Chemical formula: C₁₅H₁₃FO₂ Molecular mass: 244.261 g/mol PubChem compound: 3394
Flurbiprofen is a propionic acid derivative NSAID which acts through inhibition of prostaglandin synthesis. In humans flurbiprofen has potent analgesic, antipyretic and anti-inflammatory properties. These are thought to result from the drug’s ability to inhibit prostaglandin synthesis. According to studies using the whole blood assay, flurbiprofen is a mixed COX-1/COX-2 inhibitor with some selectivity towards COX-1.
Pre-clinical studies suggest that the R (-) enantiomer of flurbiprofen and related NSAIDs may act on the central nervous system; the suggested mechanism is by inhibition of induced COX-2 at the level of the spinal cord.
Ophthalmic surgery causes prostaglandin release, with the effect that prostaglandin-mediated miosis may occur. Treatment with flurbiprofen prior to surgery has been shown to inhibit intra-operative miosis and it is believed that this is brought about by inhibition of ocular prostaglandin release.
The sympathetic nervous system is not affected by this mechanism and acetylcholine-induced miosis has not been found to be inhibited in clinical trials.
Prostaglandins have also been shown to be mediators of certain kinds of intraocular inflammatory processes. In studies performed on animal eyes, prostaglandins have been shown to produce disruption of the blood-aqueous humour barrier, vasodilation, increased vascular permeability, leukocytosis and increased intraocular pressure.
Flurbiprofen is readily absorbed from the gastrointestinal tract, with peak plasma concentrations occurring about 90 minutes after ingestion. It is about 99% protein-bound and has an elimination half-life of about three to four hours.
The rate of urinary excretion of flurbiprofen and its two major metabolites ([2-(2-fluoro-4′-hydroxy-4-biphenylyl) propionic acid] and [2-(2-fluoro-3′-hydroxy-4′-methoxy-4-biphenylyl) propionic acid]) in both free and conjugated states is similar for both the oral and rectal routes of administration. Metabolic patterns are quantitatively similar for both routes of administration.
Flurbiprofen 8.75mg lozenges dissolve over 5–12 minutes and the flurbiprofen is readily absorbed, with detection in the blood at 5 minutes and plasma concentrations peaking at 40-45 minutes after administration but remaining at a mean low level of 1.4µg/mL which is approximately 4.4 times lower than a 50mg tablet dose. Absorption of flurbiprofen can occur from the buccal cavity by passive diffusion. Rate of absorption is dependent on pharmaceutical form with peak concentrations achieved more rapidly than, but of similar magnitude to, those achieved after an equivalent swallowed dose.
Flurbiprofen is rapidly distributed throughout the body and is extensively bound to plasma proteins.
Flurbiprofen is mainly metabolised by hydroxylation and excreted via the kidneys. It has an elimination half-life of 3 to 6 hours. Flurbiprofen is excreted in very small amounts in human milk (less than 0.05 µg/ml). Approximately 20-25% of a flurbiprofen oral dose is excreted unchanged.
No difference in pharmacokinetic parameters between elderly and young adult volunteers has been reported following oral administration of flurbiprofen tablets. No pharmacokinetic data have been generated in children below 12 years of age following administration of flurbiprofen 8.75 mg however administration of both flurbiprofen syrup and suppository formulations indicate no significant differences in pharmacokinetic parameters compared with adults.
Flurbiprofen concentrations of 213 ng/ml in aqueous humour have been reported following half hourly treatment for two hours preceding surgery.
Not applicable.
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