Instructions for Strepsils Intensive with honey and lemon lozenges 8.75 mg No. 16
Composition
active ingredient: flurbiprofen;
1 lollipop contains 8.75 mg of flurbiprofen;
excipients: macrogol 300, potassium hydroxide, lemon flavoring, levomenthol, glucose solution, sucrose solution, honey.
Dosage form
Lollipops.
Main physicochemical properties: round lollipops from pale yellow to brown in color with an embossed letter S on both sides.
Pharmacotherapeutic group
Drugs used for throat diseases. Flurbiprofen. ATX code R02A X01.
Pharmacological properties
Pharmacodynamics. Flurbiprofen is a propionic acid derivative from the group of nonsteroidal anti-inflammatory drugs (NSAIDs), which acts by inhibiting prostaglandin synthesis. In humans, flurbiprofen has potent analgesic, antipyretic and anti-inflammatory effects.
A dose of 8.75 mg dissolved in artificial saliva has been shown to inhibit prostaglandin synthesis in cultured human airway cells. Flurbiprofen is a mixed inhibitor of COX-1 and COX-2 with some selectivity for COX-1, according to whole blood assay data.
Preclinical data suggest that the R (-) enantiomer of flurbiprofen and other NSAIDs may have effects on the central nervous system; the proposed mechanism of action is inhibition of induced COX-2 at the spinal cord level.
An ex vivo model demonstrated the penetration of flurbiprofen in the dosage form of a lozenge, 8.75 mg, into human pharyngeal tissue, including the deep layers.
Significant pain relief was observed in patients after an average of 42.9 minutes with a single dose of flurbiprofen 8.75 mg, delivered locally to the throat when the lollipop was sucked, with the first signs of pain relief (manifestation of the analgesic effect) being observed after an average of 13.2 minutes.
It was demonstrated that relief of sore throat, including swelling and inflammation of the throat mucosa, is achieved by a significant reduction (least squares mean difference) in sore throat starting at 22 minutes (-5.5 mm), reaching a maximum at 70 minutes (-13.7 mm) and remaining significant for 240 minutes (-3.5 mm), including patients with streptococcal and non-streptococcal infections; a reduction in difficulty swallowing starting at 20 minutes (-6.7 mm), reaching a maximum at 110 minutes (-13.9 mm) and lasting for 240 minutes (-3.5 mm), and a reduction in the sensation of throat swelling at 60 minutes (-9.9 mm), reaching a maximum at 120 minutes (-11.4 mm) and lasting for 210 minutes (-5.1 mm).
The efficacy of multiple doses, measured as the sum of pain intensity differences (SPID) over 24 hours, demonstrated significant reductions in the intensity of throat pain (from -473.7 mm * h to -529.1 mm * h), difficulty swallowing (from -458.4 mm * h to -575.0 mm * h), and throat swelling (from -482.4 mm * h to -549.9 mm * h) with statistically greater total pain reduction at each time interval over 23 hours for all three measures and statistically significant greater relief of throat pain at each hour over the 6-hour assessment period. The efficacy of multiple doses was also demonstrated at 24 hours and for 3 days.
In patients taking antibiotics for streptococcal infection, statistically significant greater relief of sore throat was observed with flurbiprofen 8.75 mg 7 hours and longer after taking antibiotics. The analgesic effect of flurbiprofen 8.75 mg was not reduced when patients were taking antibiotics for streptococcal sore throat.
Two hours after the first dose of flurbiprofen 8.75 mg lozenges, there was significant relief of some of the associated symptoms of sore throat that were present before treatment, including cough (50% vs. 4%), loss of appetite (84% vs. 57%), and fever (68% vs. 29%).
The lozenge has been shown to be no less effective than a topical flurbiprofen spray, based on differences in pain intensity before and 2 hours after the drugs were used.
The lollipop dissolves in the mouth within 5–12 minutes and provides a significant calming and enveloping effect 2 minutes after application.
Children
No specific studies have been conducted in children. Studies of the efficacy and safety of flurbiprofen 8.75 mg lozenges have been conducted in children aged 12–17 years, however the small sample size used suggests that it is not possible to draw statistically significant conclusions.
The maximum concentration of flurbiprofen in the blood plasma is observed 30-40 minutes after resorption of the lozenge in the oral cavity. The maximum concentrations of flurbiprofen after the use of the lozenge are reached faster than after swallowing an equivalent dose, but the concentration levels in both cases are similar. Flurbiprofen is rapidly distributed in the body. The drug is actively metabolized by methylation and hydroxylation with subsequent elimination by the kidneys. The main metabolites of the drug are 4'oxy-flurbiprofen and 3'-oxy-4'methoxy-flurbiprofen. Approximately 70% of each dose is excreted in the urine after 24 hours. The half-life is 3-6 hours.
Indication
For short-term symptomatic relief of sore throat in adults and children aged 12 years and over.
Contraindication
Hypersensitivity to flurbiprofen or to any of the excipients of the drug.
History of hypersensitivity reactions (e.g. bronchial asthma, bronchospasm, rhinitis, angioedema or urticaria) after taking acetylsalicylic acid or other non-steroidal anti-inflammatory drugs (NSAIDs).
Recurrent peptic ulcer/bleeding in history or in the acute phase (two or more episodes confirmed by characteristic clinical manifestations) and intestinal ulcers.
History of gastrointestinal bleeding or perforation, severe colitis, hemorrhagic or hematopoietic disorders related to previous NSAID therapy.
The last trimester of pregnancy.
Severe heart failure, severe kidney failure, or severe liver failure.
Interaction with other medicinal products and other types of interactions
The concomitant use of flurbiprofen with:
other NSAIDs, including selective cyclooxygenase-2 (COX-2) inhibitors: the simultaneous use of two or more NSAIDs should be avoided, as this increases the risk of side effects (especially gastrointestinal side effects such as ulcers and bleeding);
acetylsalicylic acid (in low doses), unless aspirin has been prescribed by a doctor in low doses (no more than 75 mg per day), as this increases the risk of adverse reactions.
Flurbiprofen should be used with caution in combination with the following drugs:
Anticoagulants: NSAIDs may enhance the effect of anticoagulants such as warfarin;
antiplatelet agents: increased risk of gastrointestinal ulceration or bleeding;
Antihypertensives (diuretics, ACE inhibitors and angiotensin II antagonists): NSAIDs may reduce the effect of diuretics and other antihypertensive agents, as well as enhance nephrotoxicity caused by inhibition of cyclooxygenase, especially in patients with impaired renal function. (Patients should receive sufficient fluid intake);
alcohol: increases the risk of adverse reactions, especially bleeding in the gastrointestinal tract;
Cardiac glycosides: NSAIDs may exacerbate heart failure, reduce glomerular filtration rate and increase plasma glycoside levels. Monitoring of the patient's condition and, if necessary, dose adjustment is recommended;
cyclosporine: increased risk of nephrotoxicity;
corticosteroids: increase the risk of adverse reactions, especially of the gastrointestinal tract;
Lithium: possible increase in serum lithium levels, appropriate monitoring and, if necessary, dose adjustment;
Methotrexate: use of NSAIDs within 24 hours before or after methotrexate administration may lead to increased methotrexate concentrations and increased toxicity;
Mifepristone: NSAIDs should not be taken for 8-12 days after mifepristone administration, as NSAIDs may reduce the effect of mifepristone;
Oral antidiabetic agents: blood glucose levels may change (increased blood glucose control is recommended);
Phenytoin: an increase in phenytoin plasma levels is possible, therefore appropriate monitoring and, if necessary, dose adjustment are recommended;
Potassium-sparing diuretics: simultaneous use may cause hyperkalemia;
Probenecid, sulfinpyrazone, medicines containing probenecid or sulfinpyrazone: may cause slow release of flurbiprofen;
Quinolone antibiotics: Animal studies suggest that NSAIDs increase the risk of seizures associated with the use of quinolone antibiotics. Patients taking NSAIDs and quinolones are at increased risk of developing seizures;
selective serotonin reuptake inhibitors: increased risk of gastrointestinal ulceration or bleeding;
Tacrolimus: possible increased risk of nephrotoxicity with concomitant use of NSAIDs with tacrolimus;
Zidovudine: increased risk of hematological toxicity with concomitant use of NSAIDs with zidovudine.
Studies conducted to date have not revealed any interactions between flurbiprofen and tolbutamide and antacids.
Application features
Side effects can be minimized by using the lowest effective dose necessary to control symptoms for the shortest period of time.
Respiratory effects: Bronchospasm may occur in patients with or a history of bronchial asthma or allergic diseases. Flurbiprofen lozenges should be used with caution in such patients.
Other NSAIDs: Flurbiprofen lozenges should be avoided in combination with other NSAIDs, including selective cyclooxygenase-2 (COX-2) inhibitors.
Systemic lupus erythematosus and mixed connective tissue disease: Patients with systemic lupus erythematosus and mixed connective tissue disease are at increased risk of aseptic meningitis.
Cardiac, renal and hepatic failure. Nephrotoxicity. NSAIDs have been reported to cause nephrotoxicity in various forms, including interstitial nephritis, nephrotic syndrome and renal failure, especially when used in combination with several analgesic drugs and in the case of long-term habitual use. The use of NSAIDs can lead to a dose-dependent decrease in prostaglandin production and provoke renal failure. The greatest risk of this reaction exists in patients with renal failure, cardiac failure, liver dysfunction, patients taking diuretics and elderly patients. In such patients, renal function should be monitored. However, this effect is usually not observed with short-term limited use of drugs such as flurbiprofen lozenges.
Cardiovascular and cerebrovascular effects: Caution should be exercised (after consultation with a physician) when initiating treatment in patients with a history of high blood pressure and/or heart failure, as fluid retention, high blood pressure and oedema have been reported with the use of non-steroidal anti-inflammatory drugs.
Clinical trials and epidemiological data suggest that the use of some NSAIDs (especially at high doses and over a long period of time) increases the risk of arterial thrombotic events (e.g. myocardial infarction or stroke). There is insufficient evidence to exclude such a risk with the use of 5 lozenges per day.
Liver: Mild to moderate liver dysfunction.
Nervous system manifestations. Headache caused by analgesics: in case of prolonged use of analgesics or in case of non-compliance with recommendations, headache may occur, which should not be treated with increased doses of the drug.
Gastrointestinal manifestations.
Gastrointestinal bleeding, ulceration or perforation, which can be fatal, has been reported with all NSAIDs at any time during treatment, regardless of the presence of warning symptoms or a history of severe gastrointestinal disorders. The risk increases with increasing NSAID doses, in patients with a history of ulcer disease, especially complicated by bleeding or perforation, and in elderly patients. These patients should start treatment with the lowest available dose. In such patients, as well as in patients requiring concomitant low-dose acetylsalicylic acid or other medicinal products that may increase the risk of gastrointestinal events, combination therapy with protective agents (e.g. misoprostol or proton pump inhibitors) is recommended. Patients should seek medical advice if they experience any unusual gastrointestinal symptoms (especially gastrointestinal bleeding), particularly at the start of treatment. The drug should be used with caution in patients receiving concomitant therapy with drugs that increase the risk of ulceration or bleeding, in particular oral corticosteroids, anticoagulants such as warfarin, selective serotonin reuptake inhibitors or antiplatelet agents such as acetylsalicylic acid. In the event of gastrointestinal bleeding or ulceration in patients receiving flurbiprofen, treatment with the drug should be discontinued. NSAIDs should be used with caution in patients with a history of gastrointestinal diseases (ulcerative colitis, Crohn's disease) as their condition may be aggravated.
Skin and subcutaneous tissue disorders: Very rarely, severe skin reactions, which can be fatal, including exfoliative dermatitis, Stevens-Johnson syndrome and toxic epidermal necrolysis, may occur in association with NSAIDs. Flurbiprofen lozenges should be discontinued at the first appearance of skin rash, mucosal lesions or any other sign of hypersensitivity.
Infections: Since there have been isolated cases of exacerbation of infectious inflammations (e.g. development of necrotizing fasciitis) observed in temporal association with the use of systemic NSAIDs as a class, the patient is advised to seek medical advice immediately if signs of bacterial infection or deterioration of the condition occur during treatment with flurbiprofen lozenges. The need for anti-infective antibiotic therapy should be considered.
Sugar intolerance: Patients with rare hereditary problems of fructose intolerance, glucose/galactose malabsorption or sucrase-isomaltase insufficiency should not take this medicine.
If irritation occurs in the oral cavity, treatment should be discontinued.
Impaired fertility in women.
Flurbiprofen may impair female fertility and is therefore not recommended in women attempting to conceive. Discontinuation of this medicinal product should be considered in women who have difficulty conceiving or who are undergoing investigation of infertility.
Use during pregnancy or breastfeeding
Pregnancy.
Inhibition of prostaglandin synthesis may adversely affect pregnancy and/or embryo/foetal development. Epidemiological data indicate an increased risk of miscarriage and congenital heart defects and gastroschisis after use of a prostaglandin synthesis inhibitor in early pregnancy. The absolute risk of cardiac defects increased from less than 1% to approximately 1.5%. The risk is thought to increase with increasing dose and duration of treatment. In animals, use of a prostaglandin synthesis inhibitor during organogenesis has been shown to increase the incidence of various malformations, including cardiovascular malformations. Flurbiprofen should not be used during the first two trimesters of pregnancy unless clearly necessary. If flurbiprofen is used by a woman attempting to conceive, or during the first and second trimesters of pregnancy, the lowest possible dose should be used for the shortest duration possible.
During the third trimester of pregnancy, all prostaglandin synthesis inhibitors may pose the following risks:
for the fetus: cardiopulmonary toxicity (characterized by premature closure of the ductus arteriosus and pulmonary hypertension); renal dysfunction, which may progress to renal failure, accompanied by oligohydramnios;
for the mother at the end of pregnancy and the newborn: increased bleeding time, antiplatelet effect, which may develop even at very low doses; suppression of uterine contractions, leading to delayed or prolonged labor.
Therefore, flurbiprofen is contraindicated during the third trimester of pregnancy.
Breast-feeding.
In some studies, flurbiprofen has been found in breast milk at very low concentrations. It is unlikely that it would have any adverse effects on the breastfed infant. However, due to the possible adverse effects of NSAIDs on the breastfed infant, Strepsils® Intensive with Honey and Lemon is not recommended for use by breast-feeding women.
Fertility.
There is some evidence that drugs that inhibit prostaglandin/cyclooxygenase synthesis may impair female fertility through effects on ovulation. This effect is reversible upon discontinuation of the drug.
Ability to influence reaction speed when driving vehicles or other mechanisms
Studies on the ability to influence the reaction rate when driving vehicles or other mechanisms have not been conducted.
Method of administration and doses
Suck the lollipops until completely dissolved.
Adults and children over 12 years of age should take 1 lozenge every 3 to 6 hours until pain is relieved. The maximum daily dose is 5 lozenges.
Use the lowest effective dose for the shortest duration necessary to relieve symptoms. If symptoms persist, worsen, or last more than 3 days, consult a doctor.
It is not recommended to use the drug for more than 3 days.
When sucking, move the lollipop throughout the oral cavity to prevent irritation of the mucous membrane at the site of sucking.
Elderly patients: Due to limited clinical experience, no general dose recommendations can be given at this time. Elderly patients are at increased risk of severe adverse reactions.
Children
Do not use in children under 12 years of age.
Overdose
Symptoms. In most patients, the use of clinically significant amounts of NSAIDs caused only nausea, vomiting, epigastric pain or, less commonly, diarrhea. Tinnitus, headache and gastrointestinal bleeding may also occur. In more severe poisoning, toxic lesions of the central nervous system in the form of drowsiness are possible, sometimes - agitation, visual disturbances, disorientation or coma. In severe poisoning, metabolic acidosis and an increase in prothrombin time may occur, probably due to interaction with blood clotting factors circulating in the bloodstream. Acute renal failure and liver damage may occur. In patients with bronchial asthma, exacerbation of the course of asthma is possible.
Treatment. Treatment should be symptomatic and supportive, and include maintaining a patent airway and monitoring cardiac function and vital signs until the patient's condition is normal. Oral administration of activated charcoal is recommended within 1 hour of a potentially toxic dose. Frequent or prolonged muscle spasms should be treated with intravenous diazepam or lorazepam. Bronchodilators should be used in the presence of bronchial asthma. There is no specific antidote to flurbiprofen.
Adverse reactions
- nonspecific allergic reactions and anaphylaxis;
- airway reactivity, for example: bronchial asthma, exacerbation of bronchial asthma, bronchospasm, shortness of breath;
- various skin reactions, for example: itching, urticaria, angioedema,
less often - exfoliative and bullous dermatoses (including epidermal necrolysis and erythema multiforme).
Events such as oedema, hypertension and heart failure have been reported in association with NSAID treatment. Clinical trials and epidemiological data suggest that the use of some NSAIDs (particularly at high doses and in long-term treatment) may be associated with a slightly increased risk of arterial thrombotic events (e.g. myocardial infarction or stroke). There is insufficient data to exclude such a risk with flurbiprofen lozenges 8.75 mg.
The following adverse reactions have been observed with short-term use of flurbiprofen at non-prescription doses.
(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, frequency not known: frequency cannot be estimated from the available data).
Blood and lymphatic system disorders: not known: anemia, thrombocytopenia.
Immune system disorders: Rare: anaphylactic reactions.
Psychiatric disorders: uncommon: insomnia.
Cardiovascular and cerebrovascular system: unknown: edema, hypertension and heart failure.
Nervous system disorders: common: dizziness, headache, paresthesia; uncommon: drowsiness.
Respiratory, thoracic and mediastinal disorders: Common: throat irritation; uncommon: exacerbation of bronchial asthma and bronchospasm, dyspnoea, wheezing, oropharyngeal blisters, pharyngeal hypoesthesia.
Gastrointestinal: common: diarrhea, mouth ulcers, nausea, oral pain, oral paresthesia, oropharyngeal pain, oral discomfort (feeling of warmth, burning or tingling in the mouth); uncommon: abdominal distension, abdominal pain, constipation, dry mouth, dyspepsia, flatulence, glossodynia, dysgeusia, oral dysesthesia, vomiting.
Hepatobiliary disorders: not known: hepatitis.
Skin and subcutaneous tissue disorders: uncommon: various skin rashes, itching; unknown: severe forms of skin reactions, such as bullous-type reactions, including Stevens-Johnson syndrome and toxic epidermal necrolysis.
General disorders and local reactions: uncommon: pyrexia, pain.
If adverse reactions occur, treatment should be discontinued and a doctor should be consulted.
Expiration date
3 years.
Storage conditions
Store at a temperature not exceeding 25 ° C.
Keep out of reach of children.
Packaging
8 lollipops in a blister, 2 blisters in a cardboard box.
Release category: Over-the-counter.
Producer
Reckitt Benckiser Healthcare International Limited.
Location of the manufacturer and its business address
Nottingham site, Thane Road, Nottingham, NG90 2DB, United Kingdom.
