The active ingredient is flurbiprofen.
Excipients/Inactive Ingredients: Betadex, Disodium phosphate dodecahydrate, Citric acid monohydrate, Methyl parahydroxybenzoate (E218), Propyl parahydroxybenzoate (E216), Sodium hydroxide, Mint flavour, Cherry flavour, N,2,3-Trimethyl-2-isopropylbutanamide, Saccharin sodium, Hydroxypropyl betadex and Purified water.
Pharmacology: Pharmacodynamics: 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 8.75 mg dose dissolved in artificial saliva has been shown to reduce prostaglandin synthesis in cultured human respiratory cells. 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.
A single dose of flurbiprofen 8.75 mg delivered locally to the throat as three sprays has been demonstrated to relieve sore throat, including swollen and inflamed sore throats through a significant change in the severity of throat soreness area under the change (AUC) from baseline curve (mean difference (standard deviation)) for active treatment versus placebo from 0 to 2 hours (-1.82 (1.35) vs -1.13 (1.14)), 0 to 3 hours (-2.01 (1.405) vs -1.31 (1.233)) and 0 to 6 hours (-2.14 (1.551) vs -1.50 (1.385)). Significant differences in the AUC from baseline curve from 0 - 6 hours compared to placebo were also seen for other qualities of sore throat including pain intensity (-22.50 (17.894) vs -15.64 (16.413)), difficulty swallowing (-22.50 (18.260) vs -16.01 (15.451)), swollen throat (-20.97 (18.897) vs -13.80 (15.565)) and sore throat pain relief (3.24 (1.456) vs 2.47 (1.248)). The change from baseline at individual time points across the different qualities of sore throat demonstrated significance starting from 5 minutes and lasting for up to 6 hours.
For those patients taking antibiotics for Strep infection, there was statistically significant greater relief of sore throat pain intensity for flurbiprofen 8.75 mg lozenge from 7 hours and onwards after antibiotics were taken. The analgesic effect of flurbiprofen 8.75 mg lozenge was not reduced by the administration of antibiotics to treat patients with streptococcal sore throat.
Multiple-dose efficacy over 3 days has also been demonstrated. The mint-flavoured spray is easy and convenient to use and reaches the sore area of the throat, improving the ability to talk and use the voice whilst providing a soothing and coating effect for the throat.
Paediatric Population: No specific studies in children have been undertaken with Strepsils Max Pro Direct Spray 8.75 mg per dose. Efficacy and safety studies on flurbiprofen 8.75 mg lozenges have included children aged 12 - 17 years, although small sample size means that no statistical conclusions can be drawn.
Pharmacokinetics: Absorption: A single dose of flurbiprofen 8.75 mg is delivered directly to the throat as three sprays and the flurbiprofen is readily absorbed, with detection in the blood between 2 and 5 minutes and plasma concentrations peaking at 30 minutes after administration, but remaining at a mean low level of 1.6 μg/mL which is approximately 4 times lower than a 50 mg tablet dose. Strepsils Max Pro Direct Spray 8.75 mg per dose demonstrates bioequivalence to flurbiprofen 8.75 mg lozenge. 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.
Distribution: Flurbiprofen is rapidly distributed throughout the body and is extensively bound to plasma proteins.
Metabolism/Excretion: 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.
Special Groups: 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.
Strepsils Max Pro Direct Spray 8.75 mg per dose is indicated for the short-term symptomatic relief of acute sore throat in adults.
Recommended Dosage: Adults aged 18 years and over: One dose (3 sprays) administered to the back of the throat every 3-6 hours as required, up to a maximum of 5 doses in a 24 hour period.
Do not inhale whilst spraying.
It is recommended that this product should be used for a maximum of three days.
Before first use, activate the pump by pointing the nozzle away from you and spraying a minimum of four times until a fine, consistent mist is produced. The pump is then primed and ready for use.
Between each dose, point the nozzle away from you and spray a minimum of once ensuring a fine, consistent mist is produced. Always ensure a fine consistent mist is produced before dosing the product.
Paediatric population: The safety and efficacy of Strepsils Max Pro Direct Spray 8.75 mg per dose in children or adolescents under 18 years has not been established.
Elderly patients: A general dose recommendation cannot be given, since to date clinical experience is limited.
The elderly are at increased risk of the serious consequences of adverse reactions.
The lowest effective dose should be administered for the shortest duration necessary to control symptoms (see Precautions).
Route of Administration: For oromucosal administration and short-term use only.
Symptoms: Most patients who have ingested clinically important amounts of NSAIDs will develop no more than nausea, vomiting, epigastric pain, or more rarely diarrhoea. Tinnitus, headache, and gastrointestinal bleeding are also possible. In more serious poisoning with NSAIDs, toxicity is seen in the central nervous system, manifesting as drowsiness, occasionally excitation, blurred vision and disorientation or coma. Occasionally patients develop convulsions. In serious poisoning with NSAIDs metabolic acidosis may occur and the prothrombin time/INR may be prolonged, probably due to interference with the actions of circulating clotting factors. Acute renal failure and liver damage may occur. Exacerbation of asthma is possible in asthmatics.
Management: Management should be symptomatic and supportive and include the maintenance of a clear airway and monitoring of cardiac and vital signs until stable. Consider oral administration of activated charcoal or gastric lavage and if necessary correction of serum electrolytes if the patient presents within one hour of ingestion or a potentially toxic amount. If frequent or prolonged, convulsions should be treated with intravenous diazepam or lorazepam. Give bronchodilators for asthma. There is no specific antidote to flurbiprofen.
Hypersensitivity to flurbiprofen or to any of the excipients.
Patients who have previously shown hypersensitivity reactions (e.g. asthma, bronchospasm, rhinitis, angioedema or urticaria) in response to acetylsalicylic acid or other NSAIDs.
Active, or history of recurrent peptic ulcer/haemorrhage (two or more distinct episodes of proven ulceration) and intestinal ulceration.
History of gastrointestinal bleeding or perforation, severe colitis, haemorrhagic or haematopoietic disorders related to previous NSAID therapy.
Last trimester of pregnancy (see Use in Pregnancy & Lactation).
Severe heart failure, severe renal failure or severe hepatic failure (see Precautions).
Children and adolescents below 18 years.
Undesirable effects may be minimised by using the lowest effective dose for the shortest duration necessary to control symptoms.
Infections: Since in isolated cases an exacerbation of infective inflammations (e.g. development of necrotising fasciitis) has been described in temporal association with the use of systemic NSAIDs as a class, the patient is advised to consult a physician immediately if signs of a bacterial infection occur or worsen during the flurbiprofen spray therapy. It should be considered whether initiation of an anti-infective antibiotic therapy is indicated.
In cases of purulent bacterial pharyngitis/tonsillitis, the patient is advised to consult a physician as the treatment needs to be re-evaluated.
Treatment should be administered for three days maximum.
If the symptoms get worse or if new symptoms occur, the treatment should be re-evaluated.
If mouth irritation occurs, flurbiprofen treatment should be withdrawn.
Respiratory: Bronchospasm may be precipitated in patients suffering from or with a previous history of bronchial asthma or allergic disease. Flurbiprofen spray should be used with caution in these patients.
Other NSAIDs: The use of flurbiprofen spray with concomitant NSAIDs including cyclooxygenase-2 selective inhibitors should be avoided (see Interactions).
Systemic lupus erythematosus and mixed connective tissue disease: Patients with systemic lupus erythematosus and mixed connective tissue disease may have an increased risk of aseptic meningitis (see Adverse Reactions), however, this effect is not usually seen with short-term limited use products such as flurbiprofen spray.
Cardiovascular and cerebrovascular effects: Caution (discussion with doctor or pharmacist) is required prior to starting treatment in patients with a history of hypertension and/or heart failure as fluid retention, hypertension and oedema have been reported in association with NSAID therapy.
Clinical trial and epidemiological data suggest that use of some NSAIDs, (particularly at high doses and in long-term treatment) may be associated with a small increased risk of arterial thrombotic events (for example, myocardial infarction or stroke). There are insufficient data to exclude such a risk for flurbiprofen when given at a daily dose of no more than 5 doses (3 sprays per dose). All NSAIDs should not be used perioperatively in patients who have recently undergone coronary artery bypass graft (CABG) surgery and revascularisation procedures.
Nervous System effects: Analgesic induced headache - In the event of prolonged use of analgesics or use beyond the regulations headache may occur, which must not be treated with increased doses of the medicinal product.
Gastrointestinal: NSAIDs should be given with care to patients with a history of gastrointestinal disease (ulcerative colitis, Crohn's disease) as these conditions may be exacerbated (see Adverse Reactions).
Gastrointestinal bleeding, ulceration or perforation, which can be fatal, has been reported with all NSAIDs at anytime during treatment, with or without warning symptoms or a previous history of serious GI events.
The risk of GI bleeding, ulceration or perforation is higher with increasing NSAID doses, in patients with a history of ulcer, particularly if complicated with haemorrhage or perforation (see Contraindications), and in the elderly, however this effect is not usually seen with short-term limited use products such as flurbiprofen spray.
Patients with a history of GI toxicity, particularly when elderly, should report any unusual abdominal symptoms (especially GI bleeding) to their healthcare professional.
Caution should be advised in patients receiving concomitant medications which could increase the risk of ulceration or bleeding, such as oral corticosteroids, anticoagulants such as warfarin, selective serotonin-reuptake inhibitors or antiplatelet agents such as acetylsalicylic acid (see Interactions).
If GI bleeding or ulceration occurs in patients receiving flurbiprofen, the treatment should be withdrawn.
Haematological effects: Flurbiprofen, like other NSAIDs, may inhibit platelet aggregation and prolong bleeding time. Flurbiprofen spray should be used with caution in patients with a potential for abnormal bleeding.
Dermatological: Serious skin reactions, some of them fatal, including exfoliative dermatitis, Stevens-Johnson syndrome and toxic epidermal necrolysis, have been reported very rarely in association with the use of NSAIDs (see Adverse Reactions). Flurbiprofen spray should be discontinued at the first appearance of skin rash, mucosal lesions, or any other sign of hypersensitivity.
This product contains methyl parahydroxybenzoate and propyl parahydroxybenzoate which may cause allergic reactions (possibly delayed).
Risk of GI Ulceration, Bleeding and Perforation with NSAID: Serious GI toxicity such as bleeding, ulceration and perforation can occur at any time, with or without warning symptoms, in patients treated with NSAID therapy. Although minor upper GI problems (e.g. dyspepsia) are common, usually developing early in therapy, prescribers should remain alert for ulceration and bleeding in patients treated with NSAIDs even in the absence of previous GI tract symptoms.
Studies to date have not identified any subset of patients not at risk of developing peptic ulceration and bleeding.
Patients with prior history of serious GI events and other risk factors associated with peptic ulcer disease (e.g. alcoholism, smoking, and corticosteroid therapy) are at increased risk. Elderly or debilitated patients seem to tolerate ulceration or bleeding less than other individuals and account for most spontaneous reports for fatal GI events.
Cardiovascular, Renal and Hepatic Impairment: NSAIDs have been reported to cause nephrotoxicity in various forms including interstitial nephritis, nephrotic syndrome and renal failure. The administration of an NSAID may cause a dose-dependent reduction in prostaglandin formation and precipitate renal failure. Patients at greatest risk of this reaction are those with impaired renal function, cardiac impairment, liver dysfunction, those taking diuretics and the elderly, however, this effect is not usually seen with short-term, limited use products such as flurbiprofen spray.
Hepatic: Mild to moderate hepatic dysfunction (see Contraindications and Adverse Reactions).
Use in the Elderly: The elderly have an increased frequency of adverse reactions to NSAIDs especially gastrointestinal bleeding and perforation which may be fatal.
Pregnancy: Inhibition of prostaglandin synthesis may adversely affect the pregnancy and/or the embryo/foetal development.
Data from epidemiological studies suggest an increased risk of miscarriage and of cardiac malformation and gastroschisis after use of a prostaglandin synthesis inhibitor in early pregnancy. The absolute risk for cardiovascular malformation was increased from less than 1%, up to approximately 1.5%. The risk is believed to increase with dose and duration of therapy. In animals, administration of a prostaglandin synthesis inhibitor has been shown to result in increased pre- and post-implantation loss and embryo-foetal lethality. In addition, increased incidences of various malformations, including cardiovascular, have been reported in animals given a prostaglandin synthesis inhibitor during the organogenetic period. During the first and second trimester of pregnancy, flurbiprofen should not be given.
During the third trimester of pregnancy, all prostaglandin synthesis inhibitors may expose: the foetus to: cardiopulmonary toxicity (with premature closure of the ductus arteriosus and pulmonary hypertension); renal dysfunction, which may progress to renal failure with oligo-hydroamniosis; the mother and the neonate, at the end of pregnancy, to: possible prolongation of bleeding time, an anti-aggregating effect which may occur even at very low doses; inhibition of uterine contractions resulting in delayed or prolonged labour.
Consequently, flurbiprofen is contraindicated during the third trimester of pregnancy (see Contraindications).
Breast-feeding: In limited studies, flurbiprofen appears in the breast milk in very low concentration and is unlikely to affect the breast-fed infant adversely. However, because of possible adverse effects of NSAIDs on breast-fed infants, flurbiprofen spray is not recommended for use in nursing mothers.
Fertility: There is some evidence that drugs which inhibit cyclooxygenase/prostaglandin synthesis may cause impairment of female fertility by an effect on ovulation. This is reversible on withdrawal of treatment.
Hypersensitivity reactions to NSAIDs have been reported and these may consist of: (a) Non-specific allergic reactions and anaphylaxis; (b) Respiratory tract reactivity, e.g. asthma, aggravated asthma, bronchospasm, dyspnoea; (c) Various skin reactions, e.g. pruritus, urticaria, angioedema and more rarely exfoliative and bullous dermatoses (including epidermal necrolysis and erythema multiforme).
Oedema, hypertension and cardiac failure have been reported in association with NSAID treatment. There is insufficient data to exclude such a risk for flurbiprofen oromucosal spray, solution.
The following list of adverse effects relates to those experienced with flurbiprofen at OTC doses for short-term use. (Very common (≥1/10), Common (≥1/100 to <1/10), Uncommon (≥1/1000 to <1/100), Rare (≥1/10000 to <1/1000), Very rare (<1/10000), not known (cannot be estimated from the available data)).
Blood and lymphatic system disorders: Not known: anaemia, thrombocytopenia.
Cardiovascular and cerebrovascular disorders: Not known: Oedema, hypertension, cardiac failure.
Nervous System disorders: Common: dizziness, headache, paresthesia. Uncommon: somnolence.
Respiratory, thoracic and mediastinal disorders: Common: throat irritation. Uncommon: exacerbation of asthma and bronchospasm, dyspnoea, wheezing, oropharyngeal blistering, pharyngeal hypoaesthesia.
Gastrointestinal disorders: Common: diarrhoea, mouth ulceration, nausea, oral pain, paraesthesia oral, oropharyngeal pain, oral discomfort (warm or burning feeling or tingling of the mouth). Uncommon: abdominal distension, abdominal pain, constipation, dry mouth, dyspepsia, flatulence, glossodynia, dysgeusia, oral dysaesthesia, vomiting.
Skin and subcutaneous tissue disorders: Uncommon: various skin rashes, pruritus. Not known: severe forms of skin reaction such as bullous reactions, including Stevens-Johnson syndrome and toxic epidermal necrolysis.
General disorders and administration site conditions: Uncommon: pyrexia, pain.
Immune System disorders: Rare: anaphylactic reaction.
Psychiatric disorders: Uncommon: insomnia.
Hepatobiliary disorders: Not known: hepatitis.
(See table.)
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No studies so far have revealed any interactions between flurbiprofen and tolbutamide or antacids.
Paediatric population: No additional information available.
Do not store above 30°C. Do not refrigerate or freeze. Do not use this medicine for more than 6 months after the first use.
R02AX01 - flurbiprofen ; Belongs to the class of other throat preparations.
Strepsils Max Pro Spray oromucosal spray 8.75 mg
(mint-cherry flavour) 15 mL x 1's
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