Instructions Ultrafastin film-coated tablets 100 mg blister No. 20
Composition
active ingredient: ketoprofen;
1 tablet contains ketoprofen 100 mg;
excipients:
tablet core: microcrystalline cellulose, colloidal anhydrous silica, crospovidone, magnesium stearate;
shell: hypromellose, lactose monohydrate, triacetin, titanium dioxide (E 171), macrogol 3000, quinoline yellow (E 104), iron oxide yellow (E 172), iron oxide red (E 172).
Dosage form
Film-coated tablets.
Main physicochemical properties: pale yellow round biconvex tablets.
Pharmacotherapeutic group
Nonsteroidal anti-inflammatory and antirheumatic drugs. Propionic acid derivatives. Ketoprofen. ATC code M01A E03.
Pharmacological properties
Pharmacodynamics.
Ketoprofen, a derivative of phenylpropionic acid, belongs to the group of nonsteroidal drugs with anti-inflammatory and antirheumatic effects.
The mechanism of action is due to the inhibition of cyclooxygenase, an enzyme responsible for the synthesis of prostaglandins. Ketoprofen is also a bradykinin antagonist. Inhibits the synthesis of leukotrienes, reduces platelet aggregation, and affects lysosomal membranes.
In women, ketoprofen reduces the symptoms of primary dysmenorrhea due to inhibition of prostaglandin synthesis.
Pharmacokinetics.
Absorption. Ketoprofen is well absorbed from the gastrointestinal tract. The maximum concentration in the blood serum is detected approximately 60-90 minutes after oral administration. The bioavailability of ketoprofen is 90% and is directly proportional to the dose used. Food does not affect the bioavailability of the drug, but reduces the rate of absorption and maximum concentration in the blood.
Distribution. Ketoprofen is 99% bound to plasma proteins, mainly albumin. Ketoprofen penetrates into the synovial fluid and joint cavity: the joint capsule, synovial membrane and tissues around the joint. Ketoprofen penetrates into the cerebrospinal fluid and passes through the placental barrier. After repeated administration, ketoprofen does not accumulate in the body. The concentration of ketoprofen in the synovial fluid persists for up to 30 hours, so pain and stiffness of the joints are reduced for a long time. A stable concentration of ketoprofen in the blood plasma is achieved within 24 hours after taking oral forms.
Elimination. The plasma half-life of the drug is about 2 hours. Ketoprofen is biotransformed in the liver mainly by conjugation with glucuronic acid and partly by hydroxylation. Ketoprofen and its metabolites are excreted mainly in the urine.
Indication
Rheumatoid arthritis; seronegative spondyloarthritis (ankylosing spondylitis, psoriatic arthritis, reactive arthritis); gout, pseudogout; osteoarthritis; extra-articular rheumatism (tendinitis, bursitis, capsulitis of the shoulder joint);
pain syndrome of various etiologies, mild and moderate (lumbago; post-traumatic pain in joints, muscles);
algodismenorrhea
Contraindication
Hypersensitivity to ketoprofen or to any of the excipients;
contraindicated in patients in whom the use of ketoprofen, acetylsalicylic acid or other nonsteroidal anti-inflammatory drugs (NSAIDs) provokes bronchospasm, asthma attacks, urticaria, angioedema, acute rhinitis or other allergic reactions;
active phase or relapse of gastric and/or duodenal ulcer;
history of gastrointestinal bleeding/perforations/ulcers, cerebrovascular or other bleeding;
patients prone to hemorrhage;
severe liver or kidney failure;
severe heart failure;
treatment of postoperative pain during coronary artery bypass grafting surgery;
history of chronic dyspepsia.
Interaction with other medicinal products and other types of interactions
Risk of hyperkalemia.
Some drugs, such as potassium salts, diuretics, angiotensin converting enzyme inhibitors, angiotensin II receptor blockers, nonsteroidal anti-inflammatory drugs, heparins (low molecular weight or unfractionated), cyclosporine, tacrolimus, trimethoprim can cause hyperkalemia.
The development of hyperkalemia may depend on the presence of additional factors. The risk of hyperkalemia is increased by concomitant use of the above-mentioned drugs.
Risk due to the use of antiplatelet drugs.
A number of drugs cause interactions due to the effect of inhibiting platelet aggregation. These include acetylsalicylic acid and nonsteroidal anti-inflammatory drugs, ticlopidine, clopidogrel, tirofiban, eptifibatide, abciximab, iloprost.
Concomitant use of antiplatelet agents increases the risk of bleeding, as does concomitant administration of heparin, oral anticoagulants and thrombolytic agents. In such cases, the patient's clinical condition should be monitored and laboratory tests performed.
It is not recommended to use ketoprofen simultaneously with:
oral anticoagulants and heparin, which is administered parenterally;
lithium;
Methotrexate (in doses above 15 mg/week). Severe, sometimes fatal toxicity has occurred after the use of ketoprofen together with methotrexate (mainly in high doses). The toxicity is due to an increase and prolongation of the concentration of methotrexate in the blood;
mifepristone, as its effect may be reduced. Nonsteroidal anti-inflammatory drugs should be taken 8-12 days after mifepristone administration.
Ketoprofen should be used with caution simultaneously with:
diuretics, angiotensin converting enzyme inhibitors and angiotensin II receptor blockers, as the risk of renal impairment increases. Ketoprofen may reduce the effects of antihypertensives and diuretics. Diuretics may increase the risk of nephrotoxicity of NSAIDs;
methotrexate (in doses less than 15 mg/week);
sulfonamides, anticoagulants, hydantoins, as dose adjustment may be required to prevent increased levels of these drugs due to competition for binding to blood plasma proteins;
anticoagulants, for example, warfarin, due to increased effect;
oral antidiabetic and antiepileptic drugs (phenytoin), due to increased effect;
cardiac glycosides due to the possibility of exacerbation of heart failure, a decrease in glomerular filtration rate and an increase in the level of glycosides in the blood plasma;
pentoxifylline due to the possibility of increased bleeding. It is necessary to monitor the state of the blood coagulation system.
When used simultaneously with ketoprofen, special attention should be paid to:
other drugs that inhibit platelet aggregation (ticlopidine, clopidogrel, tirofiban, eptifibatide, abciximab, iloprost), due to increased risk of bleeding; other drugs that cause hyperkalemia (potassium salts, angiotensin converting enzyme inhibitors, angiotensin II receptor blockers, other NSAIDs, heparins (low molecular weight or unfractionated), cyclosporine, tacrolimus, trimethoprim), due to risk of hyperkalemia;
drugs that block beta-adrenergic receptors, due to the risk of reducing the effectiveness of these drugs (due to inhibition of prostaglandin synthesis, ketoprofen reduces their antihypertensive effect);
cyclosporine, as there is an increased risk of nephrotoxicity, especially in elderly patients;
possible decrease in the effectiveness of intrauterine contraceptives;
oral hypoglycemic drugs, as the hypoglycemic effect of the latter may be enhanced;
corticosteroids, as there is an increased risk of gastrointestinal bleeding;
probenecid, as simultaneous use may lead to a significant decrease in the clearance of ketoprofen from blood plasma.
Ketoprofen may reduce glomerular filtration rate and increase serum concentrations of cardiac glycosides.
Aluminum compounds with a neutralizing effect do not reduce the absorption of ketoprofen.
Application features
Adverse reactions can be minimized by using the lowest effective dose necessary to control symptoms for the shortest duration possible (see section "Method of administration and dosage").
The concomitant use of ketoprofen with NSAIDs including selective cyclooxygenase-2 inhibitors should be avoided (see section "Interaction with other medicinal products and other types of interactions").
Elderly: Ketoprofen absorption is not altered, only the half-life of the drug is prolonged (3 hours) and renal and plasma clearance is reduced. Elderly patients are at increased risk of adverse reactions, especially gastrointestinal bleeding and perforation, which can be fatal. (See section 4.2). If NSAIDs are necessary, the lowest effective dose should be used for the shortest possible time. Regular monitoring for gastrointestinal bleeding should also be performed during NSAID therapy.
Patients with bronchial asthma and chronic rhinitis, chronic sinusitis and/or nasal polyposis are at increased risk of developing allergies to acetylsalicylic acid and other NSAIDs. Ketoprofen may cause asthma attacks and bronchospasm in them, especially in individuals with hypersensitivity to acetylsalicylic acid and other NSAIDs.
The use of ketoprofen may cause gastrointestinal bleeding, gastric and/or duodenal ulcers or perforation, which may occur even without prodromal symptoms. Ketoprofen should be administered with caution to patients with a history of gastrointestinal disorders. Gastrointestinal bleeding is more likely to occur in elderly patients prone to such bleeding, in patients with low body weight, as well as in people with impaired platelet function or those taking anticoagulants or platelet aggregation inhibitors. With the appearance of bleeding or symptoms of gastric and/or duodenal ulcers, the drug should be discontinued immediately. In the event of mild gastric symptoms, drugs that neutralize gastric acid or coat the gastric mucosa can be used. These patients should start treatment with the lowest dose. Such patients should be treated with combination therapy with protective drugs (e.g., misoprostol or proton pump inhibitors).
Masking of symptoms of underlying infections: Ultrafastin may mask the symptoms of an infectious disease, which may delay the initiation of appropriate treatment and thereby complicate the course of the disease. This has been observed in bacterial community-acquired pneumonia and bacterial complications of varicella. When Ultrafastin is used for fever or to relieve pain in an infection, monitoring for the infectious disease is recommended. In outpatient settings, the patient should consult a doctor if symptoms persist or worsen.
Ketoprofen should be prescribed with caution to patients with gastrointestinal disorders, closely monitoring patients for the appearance of diseases such as gastritis and/or duodenitis, nonspecific ulcerative colitis, and Crohn's disease.
The drug should be used with caution in patients with hemostasis disorders, hemophilia, von Willebrand disease, severe thrombocytopenia, impaired renal or hepatic function, as well as in individuals using anticoagulants (coumarin and heparin derivatives, mainly low molecular weight heparins).
Careful monitoring of diuresis and renal function is necessary in patients with hepatic impairment, in patients receiving diuretics, in hypovolemia due to major surgery, especially in elderly patients.
Ketoprofen should be used with caution in individuals suffering from alcoholism.
The drug should be used with caution in patients taking concomitant medications that may increase the risk of bleeding or ulceration, such as oral corticosteroids, anticoagulants (warfarin), selective serotonin reuptake inhibitors, and antithrombotic drugs (acetylsalicylic acid).
Patients with a history of hypersensitivity to sunlight or phototoxicity should also be carefully monitored when using ketoprofen. In the elderly and in patients with heart failure or liver dysfunction, chronic renal failure and disorders of water metabolism (e.g. dehydration due to diuretic use, hypovolemia after surgery), ketoprofen may cause renal dysfunction due to inhibition of prostaglandin synthesis.
During the initial period of treatment, such patients should be carefully monitored for diuresis and other indicators of renal function. Impaired renal function may cause edema and an increase in the concentration of non-protein nitrogen in the blood serum.
In patients with heart failure, especially the elderly, increased manifestation of adverse reactions may be observed due to fluid and sodium retention in the body. In such patients, cardiac and renal function should be monitored.
Appropriate monitoring and advice is required for patients with hypertension and a history of mild to moderate heart failure, as fluid retention and oedema have been reported in association with the use of NSAIDs.
There is evidence that the use of some NSAIDs (especially at high doses and long-term use) may be associated with a small increased risk of arterial thrombotic events (e.g. myocardial infarction, stroke).
Patients with uncontrolled arterial hypertension, chronic heart failure, established ischemic heart disease, peripheral arterial disease and/or cerebrovascular disease should only be treated with ketoprofen after careful monitoring. Patients with risk factors such as hyperlipidemia, diabetes mellitus or smoking should also be carefully examined before starting long-term treatment.
Patients with impaired liver function should be carefully monitored (periodic monitoring of transaminase activity) and the dose of the drug should be individually adjusted.
Patients with impaired liver function or a history of liver disease (hepatitis, jaundice) should have liver function monitored and transaminase levels periodically determined, and the dose of the drug should be individually adjusted, especially during long-term treatment.
During long-term treatment with ketoprofen, especially in elderly patients, it is necessary to monitor the blood count, as well as liver and kidney function. If creatinine clearance is below 0.33 ml/s (20 ml/min), the dose of ketoprofen should be adjusted.
The use of the drug must be discontinued before major surgical interventions.
Ketoprofen may impair female reproductive function and should not be used by women attempting to conceive. Ketoprofen should be discontinued in women who are unable to conceive or are undergoing infertility evaluation.
Taking the drug in the lowest effective dose for the shortest period necessary to relieve symptoms reduces the risk of side effects and the impact on the gastrointestinal tract and circulatory system.
Patients with systemic lupus erythematosus and systemic connective tissue diseases are at increased risk of developing aseptic meningitis.
The drug contains lactose, so it should not be administered to patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption.
Patients with impaired renal function: renal and plasma clearance is reduced, the half-life is prolonged in proportion to the severity of renal failure.
Patients with hepatic insufficiency: plasma clearance and half-life are unchanged; the amount of drug not bound to proteins increases almost twofold.
Use during pregnancy or breastfeeding.
In the I and II trimesters of pregnancy, the drug can be prescribed only if the expected benefit to the mother outweighs the potential risk to the fetus, only in the minimum effective dose, the duration of treatment should be as short as possible. Like other NSAIDs, the drug is contraindicated in the last trimester of pregnancy (possible inhibition of uterine contractility and premature closure of the ductus arteriosus in the fetus).
Inhibition of prostaglandin synthesis may have adverse effects on pregnancy and/or embryo-foetal development. Epidemiological data suggest an increased risk of miscarriage and/or cardiac malformations and gastroschisis following use of a prostaglandin synthesis inhibitor in early pregnancy. The absolute risk of cardiovascular malformations has been increased from less than 1% to approximately 1.5%.
It is possible that the risk increases with increasing dose and duration of treatment. From the 20th week of pregnancy, the use of Ultrafastin tablets may cause oligohydramnios as a result of fetal renal dysfunction. Renal impairment may occur almost immediately after initiation of treatment and is usually reversible after discontinuation of ibuprofen. In addition, narrowing of the ductus arteriosus has been reported following treatment in the second trimester of pregnancy, which resolved after discontinuation of treatment.
Antenatal monitoring for oligohydramnios and narrowing of the ductus arteriosus may be advisable after use of ibuprofen for several days, starting from the 20th week of pregnancy. Ketoprofen should be discontinued if signs of oligohydramnios or narrowing of the ductus arteriosus are detected.
It has been shown that in animals, administration of a prostaglandin synthesis inhibitor results in increased pre- and post-implantation losses and embryo/fetal lethality.
In addition, an increased incidence of various malformations, including cardiovascular, has been reported in animals treated with a prostaglandin synthesis inhibitor during organogenesis. If the drug is used in women attempting to conceive or during the first trimester of pregnancy, the dose should be kept as low and the duration of treatment as short as possible.
The use of ketoprofen in the third trimester of pregnancy and during breastfeeding is contraindicated.
During the third trimester of pregnancy, all prostaglandin synthesis inhibitors may affect the fetus in the following ways:
cardiopulmonary toxicity (with premature narrowing/closure of the ductus arteriosus and pulmonary hypertension);
renal impairment, which may progress to renal failure with oligohydramnios (see above).
For the mother and newborn, as well as at the end of pregnancy:
possible prolongation of bleeding time, antiplatelet effect, which can be observed even at very low doses;
inhibition of uterine contractions, leading to delayed or prolonged labor.
There is no data on the excretion of ketoprofen in breast milk, therefore, the use of ketoprofen during breastfeeding is not recommended.
Ability to influence reaction speed when driving vehicles or other mechanisms
Until the individual reaction to the drug is determined (there may be visual impairment, dizziness, drowsiness or other central nervous system disorders), it is recommended to exercise caution when driving or working with other mechanisms.
Method of administration and doses
The lowest effective dose should be used for the shortest time necessary to relieve symptoms (see section "Special instructions").
The recommended dose for adults is 1 tablet 2 times a day.
The recommended dose for the treatment of rheumatoid arthritis and osteoarthritis is 1 tablet 2 times a day.
The recommended dose for mild to moderate pain and dysmenorrhea is 1 tablet once a day.
The duration of treatment depends on the severity and course of the disease, but adverse reactions can be minimized by using the lowest effective dose for the shortest time necessary to relieve symptoms.
The maximum daily dose of ketoprofen is 200 mg. The risk/benefit ratio should be carefully considered before prescribing a maximum daily dose of 200 mg. The use of a higher dose is not recommended.
The tablets should be taken during meals with water. The tablets should be swallowed whole, without chewing.
To prevent the negative effects of ketoprofen on the mucous membranes of the gastrointestinal tract, antacids can be taken simultaneously.
Use in elderly patients.
Elderly patients are at increased risk of adverse reactions. If NSAIDs are necessary, the lowest effective dose should be used for the shortest duration possible. Regular monitoring for signs of gastrointestinal bleeding should also be performed during NSAID therapy.
Children.
The safety of ketoprofen in children has not been established, so the drug should not be prescribed to children.
Overdose
Symptoms. In case of overdose with ketoprofen, the following symptoms were observed: headache, drowsiness, nausea, vomiting, diarrhea, abdominal pain, decreased renal function and impaired renal function. In case of significant overdose: arterial hypotension or arterial hypertension, suffocation, respiratory depression, impaired consciousness, gastrointestinal bleeding; rarely - coma, convulsions, acute renal failure.
Treatment. In case of overdose, the drug should be stopped immediately. If no more than 1 hour has passed since the overdose, gastric lavage should be performed and activated charcoal should be taken at a dose of 60-100 g for adults and 1-2 g/kg of body weight for children and symptomatic treatment should be initiated to support vital functions. Increased diuresis may be indicated. In case of renal failure, hemodialysis can be used to remove the drug from the body. H2-receptor antagonists, proton pump inhibitors and prostaglandins alleviate the dangerous effects of ketoprofen on the digestive tract. There is no specific antidote.
Side effects
Classification of side effects by organ system and frequency of occurrence: very common (≥ 1/10), common (≥ 1/100, < 1/10), uncommon (≥ 1/1000, < 1/100), rare (≥ 1/10000, < 1/1000), very rare (< 1/10000), including isolated reports.
Side effects are usually transient. Gastrointestinal disorders are more common.
From the digestive tract: very common - dyspepsia, common - nausea, vomiting, diarrhea, constipation, abdominal pain, flatulence, anorexia, stomatitis; rarely observed gastritis; very rarely - colitis, intestinal perforation (as a complication of diverticulitis), melena, hematimesis, exacerbation of ulcerative colitis or Crohn's disease, enteropathy with perforation, stenosis. Peptic ulcers, perforation, or gastrointestinal bleeding may occur.
Enteropathy may be accompanied by mild bleeding with protein loss.
There have been reports of a case of rectal perforation in an elderly woman.
Ulceration, hemorrhage, or perforation may develop in 1% of patients after 3-6 months of treatment or in 2-4% of patients after 1 year of treatment with NSAIDs.
From the blood system: uncommon - hemorrhagic anemia, hemolysis, purpura, thrombocytopenia, agranulocytosis, bone marrow failure. High doses of ketoprofen can inhibit platelet aggregation, thereby prolonging bleeding time, and cause epistaxis and hematoma formation.
Immune system disorders: exacerbation of asthma, bronchospasm or dyspnoea (especially in patients with hypersensitivity to acetylsalicylic acid and other NSAIDs); very rarely - angioedema and anaphylaxis, hypersensitivity, anaphylactic reaction, including shock. In patients with existing autoimmune disorders (systemic lupus erythematosus, systemic connective tissue diseases), isolated cases of aseptic meningitis with symptoms such as stiff neck, headache, nausea, vomiting, fever or disorientation have been observed.
Psychiatric disorders: common - depression, nervousness, nightmares, drowsiness; rare - delirium with visual and auditory hallucinations, disorientation, speech disorders.
Nervous system disorders: common – headache, asthenia, discomfort, fatigue, weakness, dizziness, paresthesia, mood changes, weight gain; rare – dysgeusia; very rare – there have been isolated reports of cases of pseudotumor cerebri; uncommon – convulsions.
On the part of the organs of vision: common - visual impairment; very rare - conjunctivitis.
On the part of the auditory system: common - tinnitus.
Clinical trials and epidemiological data suggest that the use of some NSAIDs (especially at high doses and in long-term use) may be associated with a small increased risk of arterial thrombotic events (e.g. myocardial infarction, stroke). There are insufficient data to exclude such a risk for ketoprofen.
Respiratory system: uncommon - hemoptysis, shortness of breath, pharyngitis, rhinitis, bronchospasm, laryngeal edema (signs of anaphylactic reaction); rare - asthma attacks.
On the part of the hepatobiliary system: very rarely - severe liver dysfunction accompanied by jaundice and hepatitis, abnormal renal function tests.
Skin: common - skin rashes; uncommon - alopecia, eczema, purpura-like rashes, sweating, urticaria, exfoliative dermatitis, spherobizh; rare - photosensitivity, photodermatitis; very rare - bullous reactions, including Stevens-Johnson syndrome and toxic epidermal necrolysis.
From the urinary system: very rarely - acute renal failure, interstitial nephritis, nephrotic syndrome, acute pyelonephritis; frequency unknown - abnormal renal function tests.
From the reproductive system: uncommon - menometrorrhagia.
Laboratory indicators: very common - deviations from the norm of liver transaminase levels, increased levels of transaminases, bilirubin in the blood serum due to disorders associated with diabetes; uncommon - during treatment with NSAIDs, ALT and AST levels increase significantly.
Ketoprofen reduces platelet aggregation, thereby prolonging bleeding time.
Expiration date
3 years.
Do not use after the expiry date stated on the packaging.
Storage conditions
Store in a dry place, protected from light, at a temperature not exceeding 25 °C.
Keep out of reach of children.
Packaging
10 tablets in a blister.
10 (1 blister), 20 (2 blisters) or 20 (1 blister) in a cardboard box.
Vacation category
According to the recipe.
Producer
Pharmaceutical Plant "POLPHARMA" S.A.
Location of the manufacturer and its business address.
Production branch in Nowa Dębka, Metalowca Street 2, 39-460 Nowa Dębka, Poland.
