Strepsils^® Intensive (Tablets, Spray) Instructions for Use

ATC Code

R02AX01 (Flurbiprofen)

Active Substance

Flurbiprofen (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Topical NSAID for use in ENT practice and dentistry

Pharmacotherapeutic Group

NSAID

Pharmacological Action

Flurbiprofen is a propionic acid derivative from the NSAID group and has significant analgesic, anti-inflammatory, and antipyretic effects due to the suppression of COX-1 and COX-2, with some selectivity towards COX-1, resulting in reduced production of prostaglandins – mediators of pain, inflammation, and hyperthermic reaction.

An ex vivo study of the drug in the 8.75 mg lozenge dosage form demonstrated the penetration of flurbiprofen into pharyngeal tissues, including deep layers.

The drug exerts a local analgesic and anti-inflammatory effect on the mucous membrane of the oral cavity and pharynx: it reduces swelling, difficulty swallowing, pain, and the sensation of throat irritation.

The soothing effect begins from the 2nd minute. A significant reduction in the intensity of sore throat begins from the 22nd minute, reaching a maximum effect after 70 minutes and lasting up to 4 hours.

Two hours after the first use of the lozenges, a significant reduction in the manifestations of some accompanying symptoms observed before the start of therapy is noted, including cough, loss of appetite, and feverish condition.

Pharmacokinetics

Absorption and Distribution

The tablet dissolves completely in the oral cavity within 5-12 minutes. The degree of absorption is high; Flurbiprofen is rapidly and almost completely absorbed, distributed throughout the body, and largely bound to plasma proteins. Flurbiprofen is detected in the blood after 5 minutes, C_max of flurbiprofen in blood plasma is reached 40-45 minutes after dissolution.

Flurbiprofen can be absorbed in the oral cavity by passive diffusion. The absorption rate depends on the dosage form; when dissolving, C_max of flurbiprofen is reached faster than when taking an equivalent dose of flurbiprofen orally. Flurbiprofen is excreted in breast milk in insignificant amounts (<0.05 µg/ml).

Metabolism and Excretion

It undergoes metabolism in the liver by hydroxylation. It is excreted by the kidneys and, to a lesser extent, with bile. T_1/2 – 3-6 hours. Approximately 20-25% of the oral dose of flurbiprofen is excreted unchanged.

Indications

• As a symptomatic remedy for relieving sore throat in infectious and inflammatory diseases of the oral cavity and pharynx.

ICD codes

Dosage Regimen

Tablets

The drug is used topically.

For adults and children over 12 years old slowly dissolve 1 tablet every 3-6 hours. The maximum daily dose is 5 tablets.

The drug is intended for short-term use only. The duration of the treatment course is no more than 3 days.

If symptoms persist or worsen when taking the drug for 3 days, the patient must stop treatment and consult a doctor.

Spray

Orally or for dissolution in the appropriate dosage form.

The dose and frequency of application depend on the indications and the dosage form used.

Adverse Reactions

The use of some NSAIDs, especially in high doses and for a prolonged period, may be associated with a slight increase in the risk of arterial thrombotic events (e.g., myocardial infarction or stroke). Available data are insufficient to exclude such a risk for flurbiprofen in the 8.75 mg lozenge dosage form.

The development of hypersensitivity reactions to NSAIDs has been reported, which may manifest as

• Nonspecific allergic and anaphylactic reactions;
• Airway hyperreactivity, including asthma, asthma exacerbation, bronchospasm, dyspnea;
• Various skin reactions, e.g., pruritus, urticaria, angioedema and, less commonly, exfoliative and bullous dermatosis (including epidermal necrolysis and erythema multiforme).

Cases of edema, arterial hypertension, and heart failure have been reported in patients taking NSAIDs.

The risk of side effects can be minimized by taking the drug in a short course at the minimum effective dose necessary to relieve symptoms.

The adverse reactions listed below were observed with short-term use of the drug. When treating chronic conditions and with long-term use, other adverse reactions may occur.

The assessment of the frequency of adverse reactions is based on the following criteria: very common (≥1/10), common (from ≥1/100 to <1/10), uncommon (from ≥1/1000 to <1/100), rare (from ≥1/10000 to <1/1000), very rare (<1/10000), frequency not known (data for frequency assessment are insufficient).

Blood and lymphatic system disorders: frequency not known – hematopoiesis disorders (anemia, thrombocytopenia).

Nervous system disorders common – dizziness, headache, paresthesia; uncommon – drowsiness.

Psychiatric disorders: uncommon – insomnia.

Immune system disorders: rare – anaphylactic reactions.

Cardiac disorders: frequency not known – heart failure, edema, increased blood pressure.

Respiratory, thoracic and mediastinal disorders common – feeling of irritation in the throat; uncommon – asthma exacerbation and bronchospasm, dyspnea, wheezing, blisters in the oral cavity and pharynx, hypesthesia in the oral cavity and pharynx.

Gastrointestinal disorders common – diarrhea, oral ulceration, nausea, oral pain, oral paresthesia, oropharyngeal pain, oral discomfort (sensation of warmth, burning or tingling in the mouth); uncommon – abdominal distension, abdominal pain, constipation, dry mouth, dyspepsia, flatulence, glossalgia, dysgeusia, oral dysesthesia, vomiting; frequency not known – hepatitis.

Skin and subcutaneous tissue disorders uncommon – skin rash, pruritus; frequency not known – severe skin reactions such as bullous reactions, including Stevens-Johnson syndrome and toxic epidermal necrolysis (Lyell’s syndrome).

General disorders and administration site conditions uncommon – pyrexia, pain.

Contraindications

• Hypersensitivity to flurbiprofen or any of the components included in the drug;
• History of hypersensitivity reactions (bronchial asthma, bronchospasm, rhinitis, angioedema, urticaria, recurrent nasal or paranasal sinus polyposis) in response to the use of acetylsalicylic acid or other NSAIDs;
• Erosive and ulcerative diseases of the gastrointestinal tract (including peptic ulcer of the stomach and duodenum, Crohn’s disease, ulcerative colitis);
• Ulcer bleeding in the acute phase or in history (2 or more confirmed episodes of peptic ulcer or ulcer bleeding);
• History of gastrointestinal ulcer bleeding or perforation provoked by the use of NSAIDs;
• Glucose-6-phosphate dehydrogenase deficiency;
• Hemophilia and other blood clotting disorders (including hypocoagulation);
• Hemorrhagic diathesis;
• Severe hepatic failure or active liver disease;
• Severe renal failure (creatinine clearance <30 ml/min), confirmed hyperkalemia;
• Decompensated heart failure;
• Period after coronary artery bypass surgery;
• Sucrase/isomaltase deficiency, fructose intolerance, glucose-galactose malabsorption;
• Third trimester of pregnancy;
• Children under 12 years of age.

With caution

In the presence of the conditions listed in this section, a doctor should be consulted before using the drug.

Concomitant use of other NSAIDs; history of a single episode of gastric ulcer or gastrointestinal ulcer bleeding; history of gastrointestinal diseases (ulcerative colitis, Crohn’s disease), gastritis, enteritis, colitis, presence of Helicobacter pylori infection; bronchial asthma or allergic diseases in the acute phase or in history (possible development of bronchospasm); systemic lupus erythematosus or mixed connective tissue disease (Sharp’s syndrome), due to an increased risk of aseptic meningitis (with short-term use of flurbiprofen the risk is insignificant); renal failure, including with dehydration (creatinine clearance less than 30-60 ml/min), nephrotic syndrome; hepatic failure; liver cirrhosis with portal hypertension; hyperbilirubinemia; arterial hypertension and/or heart failure, edema; concomitant use of drugs that may increase the risk of ulcers or bleeding, in particular oral corticosteroids (including prednisolone), anticoagulants (including warfarin), antiplatelet agents (including acetylsalicylic acid, clopidogrel), selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline); first and second trimesters of pregnancy, breastfeeding period; elderly age; alcohol consumption.

Use in Pregnancy and Lactation

The use of the drug is contraindicated in the third trimester of pregnancy. The use of flurbiprofen in the first and second trimesters of pregnancy should be avoided; if it is necessary to use the drug, a doctor should be consulted.

There is evidence that Flurbiprofen may pass into breast milk in insignificant amounts without any negative consequences for the health of the breastfed infant, however, due to possible side effects of NSAIDs, the use of the drug during breastfeeding is not recommended.

Information for women planning pregnancy the drug suppresses COX and prostaglandin synthesis and may affect ovulation, disrupting female reproductive function (reversible after discontinuation of treatment).

Use in Hepatic Impairment

The drug should be used with caution in hepatic failure, liver cirrhosis with portal hypertension.

Contraindicated in severe hepatic failure, active liver disease.

Use in Renal Impairment

The drug should be used with caution in renal failure (creatinine clearance less than 30-60 ml/min), nephrotic syndrome.

Contraindicated in severe renal failure (creatinine clearance <30 ml/min).

Pediatric Use

Contraindicated in children under 12 years of age.

Geriatric Use

The drug should be used with caution in elderly patients.

Special Precautions

It is recommended to take the drug for the shortest possible course and at the minimum effective dose necessary to relieve symptoms.

Patients with diabetes should take into account that each honey-lemon lozenge contains about 2.5 g of sugar (0.21 Bread Units).

If symptoms of gastropathy appear, careful monitoring is indicated, including esophagogastroduodenoscopy, complete blood count (hemoglobin determination), fecal occult blood test.

If it is necessary to determine 17-ketosteroids, the drug should be discontinued 48 hours before the study.

Ethanol intake is not recommended during treatment.

Patients with renal or hepatic impairment, as well as elderly patients and patients taking diuretics, should consult a doctor before using the drug, as there is a risk of worsening renal functional status. With short-term use of the drug, the risk is insignificant.

Patients with arterial hypertension, including in history, and/or chronic heart failure should consult a doctor before using the drug, as the drug may cause fluid retention, increased blood pressure, and edema.

If irritation in the oral cavity, skin rash, mucosal lesions, and other manifestations of an allergic reaction occur, the patient should stop using the drug and consult a doctor.

In case of worsening of existing symptoms or the appearance of new ones, including signs of a bacterial infection, the patient must immediately consult a doctor to review therapy.

Effect on ability to drive vehicles and operate machinery

Patients who experience dizziness, drowsiness, lethargy, or visual impairment when taking flurbiprofen should avoid driving vehicles or operating machinery.

Overdose

Symptoms nausea, vomiting, epigastric pain or, less commonly, diarrhea, tinnitus, headache, and gastrointestinal bleeding. In more severe cases, manifestations from the CNS are observed: drowsiness, rarely – agitation, convulsions, disorientation, coma. In cases of severe poisoning, metabolic acidosis and increased prothrombin time, acute renal failure, liver tissue damage, decreased blood pressure, respiratory depression, and cyanosis may develop. In patients with bronchial asthma, exacerbation of this disease is possible.

Treatment symptomatic, with mandatory maintenance of airway patency, ECG monitoring, and monitoring of basic vital signs until the patient’s condition normalizes. Oral administration of activated charcoal or gastric lavage within 1 hour after taking a potentially toxic dose of flurbiprofen is recommended. Frequent or prolonged convulsions should be controlled by intravenous administration of diazepam or lorazepam. In case of worsening bronchial asthma, the use of bronchodilators is recommended. There is no specific antidote for flurbiprofen.

Drug Interactions

Combinations to be avoided

Acetylsalicylic acid except for low doses of acetylsalicylic acid (not more than 75 mg/day) prescribed by a doctor, since concomitant use may increase the risk of side effects.

Other NSAIDs, including ibuprofen and selective COX-2 inhibitors simultaneous use of two or more drugs from the NSAID group should be avoided due to a possible increase in the risk of side effects.

Combinations to be used with caution

Anticoagulants NSAIDs may enhance the effect of anticoagulants, in particular, warfarin.

Antiplatelet agents and selective serotonin reuptake inhibitors increased risk of gastrointestinal bleeding.

Antihypertensive agents (ACE inhibitors and angiotensin II receptor antagonists) and diuretics NSAIDs may reduce the effectiveness of drugs in these groups and may increase nephrotoxicity due to COX inhibition, especially in patients with impaired renal function (adequate fluid replacement should be ensured in such patients).

Ethanol possible increase in the risk of adverse reactions, especially gastrointestinal bleeding.

Cardiac glycosides concomitant use of NSAIDs and cardiac glycosides may lead to worsening of heart failure, decreased glomerular filtration rate, and increased plasma concentration of cardiac glycosides.

Cyclosporine increased risk of nephrotoxicity with concomitant use of NSAIDs and cyclosporine.

Corticosteroids increased risk of gastrointestinal ulcers and gastrointestinal bleeding.

Lithium preparations there is evidence of a possible increase in plasma lithium concentration during the use of NSAIDs.

Methotrexate there is evidence of a possible increase in plasma methotrexate concentration during the use of NSAIDs. NSAIDs should be taken 24 hours before or after taking methotrexate.

Mifepristone NSAID use should be started no earlier than 8-12 days after the end of mifepristone use, as NSAIDs may reduce the effectiveness of mifepristone.

Quinolone antibiotics in patients receiving concomitant treatment with NSAIDs and quinolone antibiotics, an increased risk of convulsions is possible.

Tacrolimus concomitant use of NSAIDs and tacrolimus may increase the risk of nephrotoxicity.

Zidovudine concomitant use of NSAIDs and zidovudine may lead to increased hematotoxicity.

Oral hypoglycemic drugs possible change in blood glucose concentration (it is recommended to increase the frequency of blood glucose monitoring).

Phenytoin possible increase in serum phenytoin concentration (monitoring of serum phenytoin concentration and, if necessary, dose adjustment is recommended).

Potassium-sparing diuretics concomitant use of potassium-sparing diuretics and flurbiprofen may lead to hyperkalemia.

Probenecid and sulfinpyrazone drugs containing probenecid or sulfinpyrazone may delay the excretion of flurbiprofen.

Tolbutamide and antacids to date, studies have not revealed an interaction between flurbiprofen and tolbutamide or antacids.

Storage Conditions

The drug should be stored out of the reach of children at a temperature not exceeding 25°C (77°F).

Shelf Life

The shelf life is 3 years. Do not use the drug after the expiration date.

Dispensing Status

The drug is available without a prescription.

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.