Composition

One sachet (1 g) contains:

Active ingredient:

ketoprofen lysine salt – 40.0 mg (equivalent to 25.0 mg ketoprofen);

excipients:

mannitol – 911.0 mg,

povidone (K 30) – 20.0 mg,

mint flavor – 10.0 mg,

sodium chloride -10.0 mg,

sodium saccharinate – 7.5 mg,

silicon dioxide colloidal – 1.5 mg.

Pharmacological action

It has an anti-inflammatory, analgesic and antipyretic effect.

Inhibiting cyclooxygenase I and type II inhibits prostaglandin synthesis. It has antiradikinin activity, stabilizes lysosomal membranes and delays the release of enzymes from them that contribute to the destruction of tissues in chronic inflammation. Reduces the release of cytokines, inhibits the activity of neutrophils.

Reduces morning stiffness and swelling of joints, increases the volume of movements.

Ketoprofen lysine salt, unlike ketoprofen, is a fast-soluble molecule with a neutral pH and almost does not cause irritation of the gastrointestinal tract (gastrointestinal tract).

Pharmacokinetics:

Suction

Ketoprofen, when taken orally, is quickly and completely absorbed from the gastrointestinal tract, its bioavailability is about 80%. The maximum concentration in the blood plasma when ingested is noted after 0.5-2 hours and directly depends on the dose taken. The equilibrium concentration of ketoprofen is reached 24 hours after the start of its regular intake.

Distribution

Up to 99% of the adsorbed ketoprofen binds to plasma proteins, mainly albumin. The volume of distribution is 0.1-0.2 l/kg. It easily passes through histohematic barriers and is distributed in tissues and organs. Ketoprofen penetrates well into synovial fluid and connective tissues. Although the concentration of ketoprofen in the synovial fluid is slightly lower than in the blood plasma, it is more stable (it lasts up to 30 hours).

Metabolism

Ketoprofen is mainly metabolized in the liver, where it undergoes glucuronidation to form esters with glucuronic acid.

Output

Metabolites are excreted by the kidneys. The drug is not accumulated.

Indications

Inflammatory and degenerative diseases of the musculoskeletal system:

– rheumatoid arthritis;

– seronegative arthritis: ankylosing spondylitis (Bekhterev’s disease), psoriatic arthritis, reactive arthritis (Reiter’s disease);

– gout, pseudopodagra;

– osteoarthritis;

– tendinitis, bursitis, myalgia, neuralgia, sciatica.

Pain syndrome, including mild, moderate and severe:

– headache;

– toothache;

– post-traumatic and postoperative pain syndrome;

– pain syndrome in oncological diseases;

– algodismenorrhea.

Children (over 6 years old): short-term symptomatic treatment of inflammatory processes accompanied by pain syndrome in combination with fever or without it in diseases of the musculoskeletal system, otitis media.

The drug is intended for symptomatic therapy, reducing pain and inflammation at the time of use, it does not affect the progression of the disease.

Use during pregnancy and lactation

In the third trimester of pregnancy, the use of ketoprofen is contraindicated.

In the first and second trimesters of pregnancy, the use of the drug is possible only in the case of, if the intended benefit to the mother exceeds the potential risk to the fetus.

The drug should not be used during breastfeeding.

Contraindications

– Hypersensitivity to the Active ingredient and other components of the drug, as well as to other NSAIDs;

– a complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose and paranasal sinuses and intolerance to acetylsalicylic acid or other NSAIDs (including in the anamnesis);

– erosive and ulcerative lesions of the stomach and duodenum in the acute stage;

– active gastrointestinal, cerebrovascular or other bleeding;

– inflammatory bowel diseases (ulcerative colitis, Crohn’s disease) in the acute stage;

– hemophilia and other blood clotting disorders;

– decompensated heart failure;

– period after coronary artery bypass grafting;

– severe liver failure or active liver disease;

– severe renal insufficiency (creatinine clearance (CC) <30 ml/min), progressive kidney diseases;

– confirmed hyperkalemia;

– children’s age (up to 6 years);

– pregnancy (III trimester) and the period of breastfeeding.

With caution:

Gastric and duodenal ulcer, ulcerative colitis, Crohn’s disease, liver disease (history), hepatic porphyria, chronic renal failure (CC 30-60 ml/min), chronic heart failure, hypertension, significant decrease in circulating blood volume (including after surgery), elderly patients (including those receiving diuretics, weakened patients and low body weight), bronchial asthma, simultaneous use of glucocorticosteroids (including prednisolone), anticoagulants (including warfarin), antiplatelet agents (including acetylsalicylic acid, clopidogrel), selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline), coronary heart disease, cerebrovascular diseases, dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral artery diseases, smoking, the presence of Helicobacter pylori infection, long-term use of NSAIDs, tuberculosis, severe osteoporosis, alcoholism, severe somatic diseases, pregnancy (I, II trimester).

Side effects

According to the World Health Organization (WHO), adverse reactions are classified according to their frequency of development as follows: very common (≥1/10), common (≥1/100, <1/10), infrequent (≥1/1000, <1/100), rare (≥1/10000, <1/1000) and very rare (<1 /10000); the frequency is unknown (the frequency of occurrence of phenomena cannot be determined based on the available data).

Disorders of the blood and lymphatic system

rare: hemorrhagic anemia;

the frequency is unknown: thrombocytopenia, thrombocytopenic purpura, agranulocytosis, bone marrow dysfunction, leukocytopenia, leukocytosis, inflammation of lymphatic vessels, vasculitis.

Immune system disorders

frequency unknown: anaphylactic reactions (including anaphylactic shock).

Disorders of the nervous system and sensory organs

infrequently: headache, dizziness, drowsiness;

rare: paresthesia, blurred vision, tinnitus;

frequency unknown: convulsions, dysgeusia, mood changes, irritability, insomnia.

Disorders of the cardiovascular system

frequency unknown: heart failure, tachycardia, palpitations, hypertension, hypotension, vasodilation.

Respiratory system disorders

rare: bronchial asthma;

frequency unknown: bronchospasm (especially in patients with confirmed hypersensitivity to acetylsalicylic acid and other NSAIDs), rhinitis, shortness of breath, swelling and laryngeal spasm.

Disorders of the gastrointestinal tract

often: nausea, vomiting, dyspepsia, abdominal pain;

infrequently: constipation, diarrhea, bloating, gastritis;

rare: stomatitis, stomach and duodenal ulcer;

frequency unknown: exacerbation of ulcerative colitis and Crohn’s disease, gastrointestinal bleeding, perforation, heartburn.

Disorders of the liver and biliary tract

rare: hepatitis, increased activity of “hepatic” transaminases and increased concentration of bilirubin in blood serum caused by impaired liver function.

Disorders of the skin and subcutaneous tissues

infrequently: rash, itching;

frequency unknown: photosensitization reactions, alopecia, urticaria, angioedema, bullous reactions from the skin, including Stevens-Johnson syndrome and toxic epidermal necrolysis (Lyell’s syndrome), erythema and exanthema, maculopapular rash, dermatitis.

Kidney and urinary tract disorders

frequency unknown: acute renal failure, tubulointerstitial nephritis and nephritic syndrome, abnormal values of renal function indicators.

Other

infrequently: swelling, fatigue;

frequency unknown: allergic and anaphylactoid reactions, swelling of the oral mucosa, periorbital edema.

In case of any side effect, you should immediately stop taking the drug and consult a doctor.

Interaction

Combinations that should be avoided

Corticosteroids:the risk of ulceration of the gastrointestinal mucosa and gastrointestinal bleeding increases.

Anticoagulants (parenteral heparin, warfarin):the risk of bleeding caused by inhibition of platelet function and damage to the gastrointestinal mucosa increases. NSAIDs can enhance the effects of anticoagulants such as warfarin. Antiplatelet agents (clopidogrel, ticlopidine) and selective serotonin reuptake inhibitors: the risk of bleeding caused by inhibition of platelet aggregation and damage to the gastrointestinal mucosa increases. Patients should be monitored if co-use cannot be avoided.

Other NSAIDs, including high doses of salicylates (≥3 g/day):concomitant use of several NSAIDs may increase the risk of ulceration of the gastrointestinal mucosa and gastrointestinal bleeding, due to the synergistic effect.

Lithium:NSAIDs increase the plasma level of lithium (reduced excretion of lithium in the kidneys), which can reach toxic levels. This parameter should be monitored at the beginning of treatment, during dose adjustment and after discontinuation of ketoprofen treatment.

Methotrexate in high doses (more than 15 mg per week):the hematotoxicity of methotrexate increases, as its excretion by the kidneys decreases when taking anti-inflammatory drugs.

When combined with methotrexate in low doses (less than 15 mg per week)It is necessary to conduct a general blood test once a week during the first few weeks of treatment. It is mandatory to conduct more private monitoring of the patient’s clinical condition in the presence of even a slight deterioration in kidney function, as well as in elderly patients.

Hydantoin and sulfamides:The toxic effects of these substances may increase.

Combinations that require precautions

Diuretics, angiotensin converting enzyme (ACE) inhibitors and angiotensin II receptor antagonists:NSAIDs can reduce their effectiveness. In patients with impaired renal function (for example, patients with dehydration or elderly patients), concomitant use of ACE inhibitors or angiotensin II receptor antagonists with drugs that inhibit the cyclooxygenase system may cause additional renal dysfunction, including acute renal failure, usually reversible. Patients should be sufficiently hydrated before the start of concomitant therapy, after the start of therapy, renal function should be monitored.

Pentoxifylline:the risk of bleeding increases. It is mandatory to monitor the patient’s clinical condition more frequently and monitor the blood clotting time.

Zidovudin:The risk of toxicity to red blood cells increases by affecting reticulocytes with the development of severe anemia a week after the start of NSAID treatment. It is necessary to conduct a general blood test and monitor the number of reticulocytes 1-2 times a week after the start of NSAID treatment.

Sulfonylurea: NSAIDs can enhance the hypoglycemic effect of sulfonylurea by reducing its binding to plasma proteins.

Combinations that need to be taken into account

Beta blockers:NSAIDs can reduce the hypotensive effect of beta-blockers due to inhibition of prostaglandin synthesis.

Cyclosporine and tacrolimus: NSAIDs may increase nephrotoxicity due to effects associated with prostaglandins of the kidneys. When used together, it is necessary to monitor kidney function.

Thrombolytics:the risk of bleeding increases.

Probenecid:the concentration of ketoprofen in the blood plasma may increase. This increase may be due to an inhibitory mechanism at the site of renal tubular secretion and glucuronoconjugation and requires dose adjustment of ketoprofen.

How to take, course of use and dosage

For adults:

The contents of two sachets should be dissolved in half a glass of drinking water and taken orally up to 3 times a day with meals.

The doctor sets the dose for elderly patients, it is desirable to reduce the dosage by 2 times.

Children (from 6 to 14 years old):

The contents of one sachet should be dissolved in half a glass of drinking water and taken orally up to 3 times a day with meals.

For children (from 14 to 18 years old):

The dosages of the drug correspond to those in adults.

To reduce the risk of adverse events from the gastrointestinal tract, the minimum effective dose should be used in the shortest possible course.

Overdose

Were registered cases of overdose when taking a dose of up to 2.5 g of ketoprofen. In most cases, symptoms were limited to lethargy, drowsiness, nausea, vomiting and pain in the epigastric region.

Measures to help with overdose

The specific antidote is unknown. As symptomatic measures to ensure vital functions (stabilization of blood circulation, respiration, elimination of acidosis), drugs and procedures that reduce resorption and accelerate elimination are shown (medical charcoal, forced diuresis).

Special instructions

At the beginning of treatment, it is necessary to monitor the picture of peripheral blood and the functional state of the liver and kidneys.

After 2 weeks of using the drug, it is necessary to monitor liver function indicators (transaminase level).

The use of ketoprofen in patients with bronchial asthma can lead to the development of a bronchial asthma attack.

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

Medication it can change the properties of platelets, but it does not replace the preventive actions of acetylsalicylic acid in cardiovascular diseases.

Taking the drug can mask the signs of infectious diseases.

Elderly patients, patients with a history of gastric and duodenal ulcer, as well as patients taking low doses of acetylsalicylic acid or other drugs that may increase the risk of gastrointestinal reactions, the combined use of gastroprotective drugs (misoprostol or proton pump inhibitors) has been shown.

The use of the drug can negatively affect female fertility and is not recommended for women planning pregnancy. The use of the drug should be discontinued in women with fertility problems or undergoing a fertility study.

The drug does not affect low-calorie and controlled diets and can be used in patients with diabetes mellitus.

The drug does not contain gluten, so it can be used in patients with celiac disease.

The drug does not contain aspartame, therefore it can be used in patients with phenylketonuria.

Cardiovascular and cerebrovascular effects

Patients with arterial hypertension and/or moderate heart failure, accompanied by fluid retention and edema (in the anamnesis) associated with taking NSAIDs, careful monitoring and consultation with a doctor is necessary.

Clinical studies and epidemiological data indicate that the use of certain NSAIDs (especially in high doses for a long time) may be associated with a slight increase in the risk of arterial thrombotic events (for example, myocardial infarction or stroke). There is insufficient data to exclude the above risk for ketoprofen lysine salt.

Patients with uncontrolled arterial hypertension, heart failure, established coronary artery disease, peripheral artery diseases and / or cerebrovascular diseases should use ketoprofen lysine salt only after a thorough examination. The same examination should be performed by patients before starting long-term treatment with risk factors for cardiovascular diseases (for example, hypertension, hyperlipidemia, diabetes mellitus, smoking).

Influence on the ability to manage transp. cf. and fur. :

The drug has a limited and moderate effect on the ability to drive vehicles or mechanisms due to the possible appearance of dizziness and drowsiness.

If drowsiness, dizziness or convulsions are noted after using the drug, driving vehicles and mechanisms, as well as other activities should be avoided, requiring concentration of attention.

Storage conditions

Store at a temperature not exceeding 25 °C.

Keep out of reach of children.

Shelf life

2 years.

Do not use the drug after the expiration date, indicated on the package.

Active ingredient

Ketoprofen

Conditions of release from pharmacies

By prescription

Dosage form

granules

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