Ketoprofen-Akos injection solution 50mg / ml, 2ml No. 10

• Inflammatory and degenerative diseases of the musculoskeletal system (rheumatoid, psoriatic arthritis, Bechterew's disease / ankylosing spondylitis /, gouty arthritis, osteoarthritis);

• pain syndrome (myalgia, ossalgia, neuralgia, tendinitis, arthralgia, bursitis, sciatica, adnexitis, otitis media, headache and toothache, pain in cancer, post-traumatic and postoperative pain syndrome, accompanied by inflammation);

• algodismenorrhea.

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

Assign 100 mg i / m 1-2 times / day. The maximum daily dose is 200 mg. The drug should not be administered for more than 2-3 days, if necessary, then use other dosage forms of ketoprofen.

Composition per 100 g

Active substance

Ketoprofen - 5.0 g

Excipients Carbomer (carbopol), ethanol 96% (rectified ethyl alcohol), trolamine (triethanolamine), lavender oil, purified water.

• Complete or incomplete combination of bronchial asthma, recurrent hay fever of the nose and paranasal sinuses and intolerance to acetylsalicylic acid or other NSAIDs (including a history);

• peptic ulcer of the stomach and duodenum in the acute phase;

• ulcerative colitis (exacerbation);

• diverticulitis;

• peptic ulcer;

• hemophilia and other blood clotting disorders;

• active gastrointestinal bleeding;

• severe renal failure (CC less than 30 ml / min);

• progressive kidney disease;

• severe liver failure or active liver disease;

• condition after coronary artery bypass grafting;

• confirmed hyperkalemia;

• inflammatory bowel disease;

• children's age (up to 18 years old);

• pregnancy (III trimester);

• lactation period;

• hypersensitivity to the components of the drug and other NSAIDs.

  With care: anemia, bronchial asthma, alcoholism, tobacco smoking, alcoholic cirrhosis of the liver, hyperbilirubinemia, liver failure, dehydration, sepsis, chronic heart failure, edema, arterial hypertension, blood diseases (including leukopenia), stomatitis, ischemic heart disease, cerebrovascular diseases, dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral arterial disease, chronic renal failure (CC 30-60 ml / min), history of gastrointestinal ulcers, Helicobacter pylori infection, prolonged use of NSAIDs, severe somatic diseases, concomitant oral corticosteroids ( including prednisolone), anticoagulants (including warfarin), antiplatelet agents (including clopidogrel), selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline),advanced age, pregnancy (I and II trimester).

Pharmacokinetics

Absorption and distribution

Bioavailability is more than 90%. Plasma protein binding - 99%. The time to reach Cmax for parenteral administration is 15-30 minutes. The therapeutic concentration in the synovial fluid is maintained for 6-8 hours. It does not penetrate the BBB in a significant amount.

Metabolism and excretion

Almost completely metabolized in the liver by glucuronidation, undergoes the effect of the 'first pass' through the liver.

It is excreted mainly by the kidneys. Does not cumulate.

Side effect

From the digestive system: NSAIDs-gastropathy, abdominal pain, dyspepsia (nausea, vomiting, heartburn, flatulence, loss of appetite, diarrhea), stomatitis, liver dysfunction, ulceration of the gastrointestinal mucosa, gingival, gastrointestinal, hemorrhoidal bleeding; change in taste.

From the nervous system: headache, dizziness, insomnia, agitation, nervousness, drowsiness, depression, asthenia, confusion or loss of consciousness, forgetfulness, migraine, peripheral neuropathy.

From the senses: noise or ringing in the ears, blurred vision, conjunctivitis, dryness of the mucous membrane of the eye, pain in the eyes, conjunctival hyperemia, hearing loss, vertigo.

From the side of the cardiovascular system: increased blood pressure, tachycardia.

From the side of hematopoiesis: agranulocytosis, anemia, hemolytic anemia, thrombocytopenia, leukopenia.

From the urinary system: edema syndrome, cystitis, urethritis, impaired renal function, interstitial nephritis, nephrotic syndrome, hematuria.

Allergic reactions: skin rash (including erythematous, urticaria), itching of the skin, rhinitis, angioedema, bronchospasm, exfoliative dermatitis, anaphylactic shock.

Others: increased sweating, hemoptysis, nosebleeds, myalgia, muscle twitching, shortness of breath, thirst, photosensitivity, with prolonged use in high doses - vaginal bleeding.

Application during pregnancy and lactation

The use of the drug in the third trimester of pregnancy is contraindicated.

The use of ketoprofen in the I and II trimesters of pregnancy is possible only when the potential benefit to the mother outweighs the risk to the fetus.

If it is necessary to use ketoprofen during lactation, the question of stopping breastfeeding should be resolved.

Application for violations of liver function

Contraindicated in severe liver failure or active liver disease. With caution: alcoholic cirrhosis of the liver, hyperbilirubinemia, liver failure

Application for impaired renal function

Contraindicated in severe renal failure (CC less than 30 ml / min), progressive kidney disease. With care: chronic renal failure (CC 30-60 ml / min).

Application in children

Contraindicated in children under 18 years of age.

Use in elderly patients

With care: old age.

special instructions

During treatment, it is necessary to control the picture of peripheral blood and the functional state of the liver and kidneys.

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

Taking ketoprofen can mask the signs of an infectious disease.

In case of impaired renal and liver function, dose reduction and careful monitoring are necessary.

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

Influence on the ability to drive vehicles and use mechanisms

During the period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions.

Overdose

Symptoms: nausea, vomiting, abdominal pain, vomiting of blood, melena, impaired consciousness, respiratory depression, convulsions, impaired renal function, renal failure.

In case of overdose, symptomatic therapy, monitoring of respiratory and cardiovascular activity should be carried out, the use of histamine H2 receptor blockers, prostaglandin inhibitors is indicated. There is no specific antidote. Hemodialysis is ineffective.

Drug interactions

Pharmaceutically incompatible with tramadol solution.

Reduces the effectiveness of uricosuric drugs.

Strengthens the action of anticoagulants, antiplatelet agents, fibrinolytics, ethanol, side effects of GCS and mineralocorticosteroids, estrogens.

Reduces the effectiveness of antihypertensive drugs and diuretics.

Concomitant use with other NSAIDs, corticosteroids, ethanol, corticotropin can lead to the formation of ulcers and the development of gastrointestinal bleeding, to an increase in the risk of developing renal dysfunction.

Concomitant administration with oral anticoagulants, heparin, thrombolytics, antiplatelet agents, cefoperazone, cefamandol and cefotetan increases the risk of bleeding.

Increases the hypoglycemic effect of insulin and oral hypoglycemic drugs (dose recalculation is required).

Increases plasma concentration of verapamil and nifedipine, lithium preparations, methotrexate.

Myelotoxic drugs increase the manifestations of the drug's hematotoxicity.