Ketonal Active granules for preparation of solution, for oral administration 40mg, No. 12

Inflammatory and degenerative diseases of the musculoskeletal system:

• rheumatoid arthritis;

• seronegative arthritis: ankylosing spondylitis (ankylosing spondylitis), psoriatic arthritis, reactive arthritis (Reiter's disease);

• gout, pseudogout;

• osteoarthritis;

• tendinitis

• bursitis,

• myalgia,

• neuralgia,

• radiculitis.

• pain syndrome, including mild, moderate and severe: headache;

• toothache;

• post-traumatic and postoperative pain syndrome;

• pain syndrome in cancer;

• algodismenorrhea.

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

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

Adults:

Dissolve the contents of two sachets in half a glass of drinking water and take orally up to 3 times a day with meals.

For elderly patients, the dose is set by the doctor, preferably a 2-fold reduction in the dosage.

Children (from 6 to 14 years old):

Dissolve the contents of one sachet in half a glass of drinking water and take orally up to 3 times a day with meals.

Children (from 14 to 18 years old):

Dosages of the drug correspond to those in adults.

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

One sachet (1 g) contains:

active substance:

ketoprofen lysine salt - 40.0 mg (equivalent to 25.0 mg of 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,

colloidal silicon dioxide - 1.5 mg.

• Hypersensitivity to the active substance and other components of the drug, as well as to other NSAIDs;

• complete or incomplete combination of bronchial asthma,

• recurrent polyposis of the nose and paranasal sinuses and intolerance to acetylsalicylic acid or other NSAIDs (including a history);

• 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 failure (creatinine clearance (CC) <30 ml / min), progressive kidney disease;

• confirmed hyperkalemia;

• children's age (up to 6 years old);

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

Pharmacological properties

Pharmacodynamics:

It has anti-inflammatory, analgesic and antipyretic effects.

By inhibiting type I and II cyclooxygenase, it inhibits the synthesis of prostaglandins.

It has anti-bradykinin activity, stabilizes lysosomal membranes and delays the release of enzymes from them that contribute to tissue destruction in chronic inflammation.

Reduces the release of cytokines, inhibits the activity of neutrophils.

Reduces morning stiffness and swelling of joints, increases range of motion.

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

Pharmacokinetics

Absorption Ketoprofen when taken orally is rapidly and completely absorbed from the gastrointestinal tract, its bioavailability is about 80%.

The maximum concentration in blood plasma when taken orally 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 adsorbed ketoprofen binds to plasma proteins, mainly albumin.

The volume of distribution is 0.1-0.2 l / kg.

Easily passes through histohematogenous 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 (lasts up to 30 hours).

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

Withdrawal

The metabolites are excreted by the kidneys.

The drug is not cumulated.

Application during pregnancy and during breastfeeding:

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

In the first and second trimesters of pregnancy, the appointment of the drug is possible only if the intended benefit to the mother outweighs the potential risk to the fetus.

The drug should not be used during breastfeeding.

Side effect

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

Immune system disorders, frequency unknown: anaphylactic reactions (including anaphylactic shock).

Disturbances from the nervous system and sensory organs are infrequent: headache, dizziness, drowsiness; rarely: paresthesias, blurred vision, tinnitus; frequency unknown: convulsions, dysgeusia, mood changes, irritability, insomnia.

Violations of the cardiovascular system, the frequency is unknown: heart failure, tachycardia, heart palpitations, hypertension, hypotension, vasodilation.

Respiratory system disorders are rare: bronchial asthma; frequency unknown: bronchospasm (especially in patients with confirmed hypersensitivity to acetylsalicylic acid and other NSAIDs), rhinitis, shortness of breath, laryngeal edema and spasm.

Disturbances from the gastrointestinal tract are often: nausea, vomiting, dyspepsia, abdominal pain; infrequently: constipation, diarrhea, bloating, gastritis; rarely: stomatitis, stomach and duodenal ulcers; frequency unknown: exacerbation of ulcerative colitis and Crohn's disease, gastrointestinal bleeding, perforation, heartburn.

Violations of the liver and biliary tract hepatitis, increased activity of 'hepatic' transaminases and an increase in the concentration of bilirubin in the blood serum, caused by impaired liver function.

Violations of the skin and subcutaneous tissue infrequently: rash, itching; frequency unknown: photosensitivity reactions, alopecia, urticaria, angioedema, bullous skin reactions, including Stevens-Johnson syndrome and toxic epidermal necrolysis (Lyell's syndrome), erythema and exanthema, maculopapular rash, dermatitis.

Renal and urinary tract disorders, the frequency is unknown: acute renal failure, tubulointerstitial nephritis and nephritic syndrome, abnormal values ??of renal function indicators. Other infrequent: swelling, fatigue; frequency unknown: allergic and anaphylactoid reactions, edema of the oral mucosa, periorbital edema.

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

Overdose:

Overdose cases have been reported when taking a dose of up to 2.5 g of ketoprofen.

In most cases, symptoms were limited to lethargy, drowsiness, nausea, vomiting, and epigastric pain.

Overdose management measures:

The specific antidote is unknown.

As symptomatic measures in ensuring vital functions (stabilization of blood circulation, respiration, elimination of acidosis), drugs and procedures are shown that reduce resorption and accelerate elimination (medical charcoal, forced diuresis).

Special instructions:

At the beginning of treatment, it is necessary to control 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 levels).

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

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

The drug can change the properties of platelets, but does not replace the preventive action of acetylsalicylic acid in cardiovascular diseases.

Taking the drug can mask the signs of infectious diseases.

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

The use of the drug may adversely affect female fertility and is not recommended for women planning a pregnancy.

The drug should be discontinued in women with fertility problems or undergoing fertility tests.

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, therefore 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 history) associated with taking NSAIDs, require careful monitoring and medical advice.

Clinical studies and epidemiological data indicate that the use of some 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 are insufficient data to exclude the above risk for ketoprofen lysine salt.

Patients with uncontrolled arterial hypertension, heart failure, established ischemic heart disease, peripheral arterial disease and / or cerebrovascular disease should use ketoprofen lysine salt only after a thorough examination.

Patients should undergo the same examination before starting long-term treatment with risk factors for the development of cardiovascular diseases (for example, arterial hypertension, hyperlipidemia, diabetes mellitus, smoking).

Influence on the ability to drive vehicles, mechanisms: e

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, after using the drug, drowsiness, dizziness or convulsions are noted, you should avoid driving vehicles and mechanisms, as well as other activities that require concentration.