Source: Health Products Regulatory Authority (IE) Revision Year: 2021 Publisher: Reckitt Benckiser Ireland Ltd, 7 Riverwalk, Citywest Business Campus, Dublin 24, Ireland
Pharmacotherapeutic group: Respiratory System; Throat preparations; Other throat preparations.
ATC Code: R02AX01
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 and the 8.75mg dose dissolved in artificial saliva has been shown to reduce prostaglandin synthesis in cultured human and respiratory cells.
According to studies using the whole body 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 relieve pain by acting on the central nervous system. Reduction in throat soreness was observed after 15 minutes while onset of pain relief and reduction of throat swelling was observed 30 minutes after taking a lozenge. Duration of action extended up to 3 hours.
A single dose of flurbiprofen 8.75mg delivered locally to the throat in a lozenge has been demonstrated to relieve sore throat, including swollen and inflamed sore throats through a significant reduction (LS Mean Difference) in sore throat pain intensity from 22 minutes (-5.5mm), reaching a maximum at 70 minutes (-13.7mm) and remaining significant for up to 240 minutes (-3.5mm) including patients with streptococcal and non-streptococcal infections, reduction in difficulty swallowing from 20 minutes (-6.7mm), reaching a maximum at 110 minutes (-13.9mm) and for up to 240 minutes (-3.5mm) and reduction in the feeling of a swollen throat at 60 minutes (-9.9mm), reaching a maximum at 120 minutes (-11.4mm) and for up to 210 minutes (-5.1mm).
Multiple dose efficacy measured using Sum of Pain Intensity Differences (SPID) over 24 hours has demonstrated significant reduction in sore throat pain intensity (-473.7mm*h to -529.1mm*h), difficulty swallowing (-458.4mm*h to -575.0mm*h) and swollen throat (-482.4mm*h to -549.9mm*h) with statistically significant greater summed reduction in pain at each hourly interval over 23 hours for all three measures and statistically significantly greater sore throat relief each hour over the 6 hour assessment time. Efficacy of multiple doses after 24 hours and over 3 days has also been demonstrated.
For those patients taking antibiotics for streptococcal infection, there was statistically significant greater relief of sore throat pain intensity for flurbiprofen 8.75mg from 7 hours and onwards after antibiotics were taken. The analgesic effect of flurbiprofen 8.75 mg was not reduced by the administration of antibiotics to treat patients with streptococcal sore throat.
At 2 hours post first dose, flurbiprofen 8.75mg lozenges provided significant resolution of some of the associated symptoms of sore throat present at baseline including coughing (50% vs 4%), loss of appetite (84% vs 57%) and feverishness (68% vs 29%). The lozenge format dissolves in the mouth over 5-12 minutes and provides a measurable soothing and coating effect at 2 minutes.
No specific studies in children have been undertaken. Efficacy and safety studies on flurbiprofen 8.75mg lozenges have included children aged 12-17 years, although small sample size means that no statistical conclusions can be drawn.
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 conjugation in the liver 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.
There are no preclinical data of relevance additional to information already included in other relevant sections.
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