Strepsils® [Flurbiprofen]

Pharmacological properties

Pharmacodynamics: flurbiprofen is an NSAID that has a powerful analgesic, antipyretic and anti-inflammatory effect by inhibiting the synthesis of prostaglandins.

A decrease in the severity of pain, pain in the throat, as well as a decrease in swelling in the throat is observed 30 minutes after ingestion of the lollipop, the duration of action is 2-3 hours.

Analgesic and anti-inflammatory activity is due to inhibition of the COX enzyme and inhibition of prostaglandin synthesis. The drug has a local effect. Inhibits equally the effect of prostaglandins E₂ and E_2a due to the inhibition of endoperoxidase, which catalyzes the conversion of arachidonic acid to cyclic endoperoxide.

Pharmacokinetics C_max plasma flurbiprofen is noted 30–40 minutes after the resorption of the lollipop in the oral cavity. C_max flurbiprofen after applying the lollipop is achieved faster than after swallowing the equivalent dose, however, the concentration levels in both cases are similar. Flurbiprofen is rapidly distributed in the body. The drug is actively metabolized by methylation and hydroxylation, followed by elimination by the kidneys. The main metabolites of the drug are 4´-oxy-flurbiprofen and 3´-hydroxy-4´methoxy-flurbiprofen. Approximately 70% of the dose is excreted in the urine after 24 hours. T_½ 3–6 hours

Indications

For short-term symptomatic relief of sore throat in adults and children over the age of 12 years.

Application

Lozenges dissolve in the oral cavity until completely dissolved. Adults and children over the age of 12 take 1 lollipop every 3–6 hours until the pain is relieved. the maximum daily dose is 5 candies.

The lowest effective dose is applied over the minimum period necessary to reduce the severity of 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.

During resorption, the lollipop should be moved throughout the oral cavity to prevent irritation of the mucous membrane at the resorption site.

Due to limited clinical experience, elderly patients cannot be given general dose recommendations at this time. In elderly patients, there is an increased risk of severe consequences of adverse reactions.

Contraindications

Hypersensitivity to flurbiprofen or any of the components of the drug.

Hypersensitivity reactions (e.g. AD, bronchospasm, rhinitis, angioedema or urticaria) after the use of acetylsalicylic acid or other NSAIDs.

Relapsing stomach ulcer / bleeding in the anamnesis or in the phase of exacerbation (two or more clear episodes of exacerbation, confirmed by characteristic clinical manifestations) and intestinal ulcers.

A history of gastrointestinal bleeding or a history of perforation, severe colitis, hemorrhagic or hematopoietic disorders associated with previous treatment of NSAIDs.

Severe heart failure, severe renal failure, severe liver failure.

The last trimester of pregnancy.

Side effects

Hypersensitivity reactions to NSAIDs have been reported, which manifested as:

• non-specific allergic reaction and anaphylaxis;
• airway reactivity, for example, asthma, exacerbation of asthma, bronchospasm, shortness of breath;
• various skin reactions, such as pruritus, urticaria, angioneurotic edema, exfoliative and bullous dermatoses (including epidermal necrolysis and erythema multiforme) were less often noted.

In connection with NSAID therapy, phenomena such as edema, hypertension, and heart failure have been reported.Clinical studies and epidemiological data suggest that the use of certain NSAIDs (especially at high doses and with long-term treatment) may be associated with a slightly increased risk of arterial thrombotic complications (for example, myocardial infarction or stroke). There is insufficient data to exclude such a risk in the case of the use of lozenges with flurbiprofen of 8.75 mg.

The following is a list of side effects that are observed with the short-term use of flurbiprofen in over-the-counter doses.

(Very often: ≥1 / 10; often: from ≥1 / 100 to 1/10; infrequently: from ≥1 / 1000 to 1/100; rarely: from ≥1 / 10,000 to 1/1000; very rarely: 1 / 10,000, frequency unknown: it is not possible to estimate the frequency from the available data.)

On the part of the blood system and lymphatic system: unknown - anemia, thrombocytopenia.

From the immune system: rarely - anaphylactic reactions.

Mental disorders: infrequently - insomnia.

From the cardiovascular and cerebrovascular system: unknown - edema, hypertension and heart failure.

From the nervous system: often - dizziness, headache, paresthesia; infrequently - drowsiness.

From the respiratory system, chest and mediastinal organs: often - irritation in the throat; infrequently - asthma exacerbation and bronchospasm, shortness of breath, wheezing, oropharyngeal blisters, pharyngeal hypesthesia.

From the digestive system: often - diarrhea, ulcers in the oral cavity, nausea, pain in the oral cavity, paresthesia of the oral cavity, pain in the oropharynx, discomfort of the oral cavity (feeling of warmth, burning or tingling in the mouth); infrequently - bloating, abdominal pain, constipation, dry mouth, dyspepsia, flatulence, glossodynia, dysgeusia, dysesthesia of the oral cavity, vomiting.

From the liver and biliary tract: unknown - hepatitis.

On the part of the skin and subcutaneous tissue: infrequently - 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: infrequently - pyrexia, pain.

In case of adverse reactions, stop treatment and consult a doctor.

special instructions

Manifestations of side effects can be reduced by briefly applying the minimum effective dose necessary to eliminate the symptoms.

In elderly patients, the incidence of adverse reactions caused by the use of NSAIDs increases, especially bleeding from the gastrointestinal tract or perforations, which can be fatal.

Bronchospasm may occur in patients with AD or allergic diseases at present or in history.

It is not recommended to use lozenges with flurbiprofen in parallel with other NSAIDs, including selective COX-2 inhibitors.

Systemic lupus erythematosus and systemic connective tissue diseases are an increased risk of aseptic meningitis.

Symptoms of renal failure: nephrotoxicity. There are reports that NSAIDs cause nephrotoxicity in various forms, including interstitial nephritis, nephrotic syndrome and renal failure, especially when using a combination of 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 provokes renal failure. The greatest risk of this reaction exists in patients with renal failure, heart failure, impaired liver function, patients taking diuretics, and the elderly. 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.

Impaired liver function.Mild to moderate hepatic impairment.

Effect on the cardiovascular and cerebrovascular system. Caution (after consultation with a doctor) should begin the use of drugs in patients who have had high blood pressure and / or heart failure, since NSAIDs reported fluid retention, high blood pressure and edema. Clinical studies and epidemiological studies suggest that the use of certain NSAIDs (especially at high doses and for a long time) increases the risk of developing arterial thrombotic complications (for example, myocardial infarction or stroke). There is not enough data to exclude such a risk in the case of 5 lozenges per day.

Manifestations of the nervous system. Headache caused by painkillers: in case of prolonged use of analgesics or non-compliance with the recommendations, a headache may occur that should not be treated with high doses of the drug.

Reproductive dysfunction in women. The use of flurbiprofen can impair fertility in women, so this drug is not recommended for women who are trying to become pregnant. Consideration should be given to the abolition of this drug for women who have difficulty getting pregnant, or undergoing infertility testing.

Effect on the digestive tract. When applying all NSAIDs at any stage of treatment, gastrointestinal bleeding, ulcer or perforation, which can be fatal, was reported, regardless of the presence of warning symptoms or severe gastrointestinal disturbances in the anamnesis. The risk increases with increasing doses of NSAIDs in patients with a history of peptic ulcer, especially complicated by bleeding or perforation, as well as in the elderly. These patients should start with the lowest dose available. Such patients, as well as patients who require the simultaneous use of low doses of acetylsalicylic acid or other drugs that may increase the risk of the gastrointestinal tract, are recommended combination therapy with protective drugs (for example, misoprostol or proton pump inhibitors). Patients should consult a doctor if any unusual symptoms of the gastrointestinal tract appear (especially gastrointestinal bleeding), in particular at the beginning of treatment. It should be used with caution in patients who receive concomitant therapy with drugs that increase the risk of peptic ulcer or bleeding, in particular oral corticosteroids, anticoagulants, such as warfarin, selective serotonin reuptake inhibitors, or antiplatelet agents, such as acetylsalicylic acid. In case of gastrointestinal bleeding or ulcers in patients receiving flurbiprofen, treatment should be discontinued. NSAIDs should be used with caution in patients with gastrointestinal diseases (ulcerative colitis, Crohns disease) in the anamnesis, since their condition may worsen.

On the part of the skin and subcutaneous tissue. Very rarely, with NSAIDs, severe skin reactions can occur that can be fatal, including exfoliative dermatitis, Stevens-Johnson syndrome, and toxic epidermal necrolysis. At the first signs of a skin rash, pathological changes in the mucous membranes, or with any other signs of hypersensitivity, lozenges with flurbiprofen should be canceled.

Infections Since there have been isolated cases of exacerbation of an infectious inflammatory process (for example, the development of necrotic fasciitis) observed temporarily due to the use of systemic NSAIDs as a class, it is recommended that the patient immediately consult a doctor if there are signs of a bacterial infection or worsen during treatment with lumbiprofen lollipops. The need for anti-infective antibiotic therapy should be considered.

Sugar intolerance. Patients with rare hereditary fructose intolerance, glucose / galactose malabsorption or sucrose-isomaltase deficiency should not use this drug.

If symptoms worsen or if new symptoms occur, treatment should be reviewed. If irritation occurs in the oral cavity, treatment should be discontinued.

Use during pregnancy and lactation

Pregnancy. Inhibition of prostaglandin synthesis may adversely affect pregnancy and / or embryo / fetal development. Epidemiological studies indicate an increased risk of miscarriage and congenital heart defects and gastroschisis after the use of an inhibitor of prostaglandin synthesis in early pregnancy. The absolute risk of heart defects increased from 1% to 1.5%. It is believed that the risk increases with increasing doses and increasing the duration of therapy. In animals, the use of an inhibitor of prostaglandin synthesis during organogenesis led to an increase in the number of cases of various malformations, including those from the cardiovascular system. Flurbiprofen should not be taken in the first two trimesters of pregnancy, unless it is absolutely necessary. If flurbiprofen is used by a woman who is trying to become pregnant, or during the first and second trimesters of pregnancy, the lowest possible dose should be used for a short period of time. During the third trimester of pregnancy, all prostaglandin synthesis inhibitors may present the following risks:

• for the fetus: cardiopulmonary toxicity (characterized by premature closure of the ductus arteriosus and pulmonary hypertension); impaired renal function, which can progress to renal failure, accompanied by oligohydramnios;
• for the mother at the end of pregnancy and the newborn: an increase in bleeding time, an antiplatelet effect that can develop even at very low doses, inhibition of uterine contractions, which leads to a delay or increase in the duration of labor.

Thus, flurbiprofen is contraindicated in the III trimester of pregnancy.

Lactation. In some studies, flurbiprofen was found in breast milk at a very low concentration. It is unlikely that he would have a negative effect on the infant who is being breast-fed. However, due to the possible side effects of NSAIDs in breast-fed infants, Strepsils Intensive with Honey and Lemon is not recommended for women who are breast-feeding.

Fertility. There is some evidence that drugs that inhibit prostaglandin / COX synthesis can lead to a deterioration in female fertility as a result of exposure to ovulation. This effect is reversible when the drug is discontinued.

Children. It is not recommended to use the drug in patients under the age of 12 years.

The ability to influence the reaction rate when driving vehicles or working with other mechanisms. A study of the ability to influence the reaction rate when driving vehicles or other mechanisms was not conducted.

Interactions

The simultaneous use of flurbiprofen with:

other NSAIDs, including selective COX-2 inhibitors: the simultaneous use of two or more NSAIDs should be avoided, since this increases the risk of side effects (especially adverse reactions from the gastrointestinal tract, such as ulcers and bleeding), acetylsalicylic acid (in low doses), if it was not prescribed by a doctor in low doses (not higher than 75 mg / day), since this increases the risk of adverse reactions.

Caution is advised to use flurbiprofen in combination with such drugs:

anticoagulants: NSAIDs may enhance the effect of anticoagulants such as warfarin;

antiplatelet agents: increased risk of gastrointestinal ulcers or bleeding;

antihypertensive agents (diuretics, ACE inhibitors and angiotensin II antagonists): NSAIDs can reduce the effect of diuretics and other antihypertensive drugs, as well as enhance the nephrotoxicity caused by suppression of COX, especially in patients with impaired renal function (patients should receive a sufficient amount of fluid);

alcohol: increases the risk of adverse reactions, especially bleeding in the digestive tract;

cardiac glycosides: NSAIDs can exacerbate heart failure, reduce glomerular filtration rate and increase plasma glycoside levels. It is recommended to monitor the patients condition and, if necessary, dose adjustment;

cyclosporine: increased risk of nephrotoxicity;

corticosteroids: increase the risk of adverse reactions, especially the gastrointestinal tract;

lithium: it is possible to increase the level of lithium in the blood plasma, proper control and, if necessary, dose adjustment;

methotrexate: the use of NSAIDs within 24 hours before or after the use of methotrexate can lead to an increase in the concentration of methotrexate and an increase in the severity of its toxic effect;

mifepristone: do not take NSAIDs within 8-12 days after the use of mifepristone, since NSAIDs can reduce the severity of the action of mifepristone;

oral antidiabetic agents: blood glucose levels may vary (increased control of blood glucose levels is recommended);

phenytoin: an increase in the level of phenytoin in blood plasma is possible, therefore, appropriate control and, if necessary, dose adjustment are recommended;

potassium-sparing diuretics: simultaneous use can lead to hyperkalemia;

probenecid, sulfinpyrazone, medicines containing probenecid or sulfinpyrazone: may cause slow release of flurbiprofen;

quinolone antibiotics: data from animal studies show that NSAIDs increase the risk of seizures associated with quinolone antibiotics. Patients taking NSAIDs and quinolones have an increased risk of developing seizures;

selective serotonin reuptake inhibitors: increased risk of gastrointestinal ulcers or bleeding;

tacrolimus: may increase the risk of nephrotoxicity while the use of NSAIDs with tacrolimus;

zidovudine: increased risk of hematologic toxicity while using NSAIDs with zidovudine.

The studies that were conducted at present did not reveal the interaction of flurbiprofen with tobutamide and antacids.

Overdose

Symptoms most patients who have taken potentially toxic doses of NSAIDs may experience nausea, vomiting, epigastric pain, or very rarely diarrhea. tinnitus, headache, and bleeding from the digestive tract are also possible. with more severe poisoning, toxic central nervous system lesions can occur, manifested in the form of drowsiness, sometimes - excitement, as well as disorientation or coma. in severe poisoning, metabolic acidosis may develop, as well as prolongation of prothrombin time, probably due to the effect on blood coagulation factors circulating in the bloodstream. possibly the development of arrester and liver damage. in patients with BA, an exacerbation of the course of the disease may occur.

Treatment can be symptomatic and supportive, and also include ensuring airway patency, monitoring cardiac activity and other vital signs until a stable condition is achieved. Oral administration of activated carbon is recommended if the patient is treated within 1 hour after the use of a potentially toxic dose of the drug. With frequent or prolonged muscle spasms, iv diazepam or lorazepam should be given iv. In asthma, bronchodilators should be used.There is no specific antidote to flurbiprofen.

Storage conditions

At a temperature not exceeding 25 ° C.