Flamax solution for injection. 50mg / ml, 2ml # 10

Symptomatic treatment of pain and inflammation of various origins of moderate intensity:

• inflammatory and degenerative diseases of the musculoskeletal system - rheumatoid, psoriatic, juvenile chronic arthritis, ankylosing spondylitis (ankylosing spondylitis), gouty arthritis, rheumatic lesions of soft tissues, osteoarthritis of the peripheral joints and the spine (including with radicular syndrome);

• lumbago, sciatica, neuralgia;

• migraine;

• algodismenorrhea, inflammatory processes of the pelvic organs, incl. adnexitis;

• post-traumatic pain syndrome accompanied by inflammation;

• postoperative pain;

• toothache;

• pain syndrome in cancer.

It does not affect the progression of the disease.

V / v, v / m.

IM introduction: 100 mg (1 amp.) 1-2 times a day.

IV infusion of the drug should be carried out only in a hospital setting. The average time of infusion is 0.5-1 hours, the maximum is no more than 48 hours, while the dose of the drug should not exceed 300 mg.

Short intravenous infusion: 100-200 mg (1-2 amp.) Of the drug, diluted in 100 ml of 0.9% sodium chloride solution, is injected over 0.5-1 hours. Re-introduction is possible after 8 hours.

Long-term intravenous infusion: 100-200 mg (1-2 amp.) Of the drug diluted in 500 ml of solution for infusion (0.9% sodium chloride solution, lactate-containing Ringer's solution, 5% dextrose solution), injected over 8 hours ...

Re-introduction is possible after 8 hours.

Combined use

FlamaxЃ can be combined with central analgesics; it can be mixed with morphine in one bottle. Do not mix in the same bottle with tramadol due to precipitation. Parenteral administration of FlamaxЃ can be combined with the use of oral forms (tablets, capsules) or rectal suppositories, while the total daily dose should be increased to 300 mg or reduced to 100 mg, depending on the nature of the disease and the patient's condition.

You should use the minimum effective dose for the smallest possible short course (see 'Special instructions').

Solution for intravenous and intramuscular administration

1 amp. (2 ml)

active substance: ketoprofen 100 mg

excipients: propylene glycol - 800 mg; ethanol (ethyl alcohol 95% in terms of 100% substance) - 200 mg; benzyl alcohol - 40 mg; sodium hydroxide 1M solution - up to pH 6.5Ц7.5; water for injection - up to 2 ml

• Hypersensitivity (including to other NSAIDs or auxiliary components);

• erosive and ulcerative lesions of the gastrointestinal tract in the acute phase;

• bleeding from the gastrointestinal tract;

• inflammatory bowel disease in the acute phase (ulcerative colitis, Crohn's disease);

• severe liver failure or liver disease in the acute period;

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

• progressive kidney disease;

• hyperkalemia;

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

• violation of hematopoiesis, impaired hemostasis (including hemophilia);

• period after coronary artery bypass grafting;

• pregnancy (III trimester);

• lactation period;

• age up to 15 years.

With care: bronchial asthma; the presence of factors that increase gastrointestinal toxicity - alcoholism and cholecystitis, chronic heart failure, edema syndrome; arterial hypertension, impaired renal function, cholestasis, sepsis, concomitant use with other NSAIDs, advanced age (over 65 years), pregnancy (I Ц II trimester); coronary heart disease; cerebrovascular diseases; dyslipidemia / hyperlipidemia; diabetes; peripheral arterial disease; smoking; chronic renal failure (Cl creatinine 30-60 ml / min); anamnestic data on the development of ulcerative lesions of the gastrointestinal tract; confirmed fact of the presence of Helicobacter pylori infection; long-term use of NSAIDs; severe somatic diseases; concomitant therapy with the following drugs - anticoagulants (including warfarin), antiplatelet agents (incl.acetylsalicylic acid, clopidogrel), SSRIs (including citalopram, fluoxetine, paroxetine, sertraline), GCS (including prednisolone). 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.

pharmachologic effect

NSAID, a derivative of propionic acid. It has analgesic, anti-inflammatory and antipyretic effects, inhibits platelet aggregation.

Acting on the cyclooxygenase and lipoxygenase link of the metabolism of arachidonic acid, ketoprofen inhibits the synthesis of prostaglandins, leukotrienes and thromboxanes. The analgesic effect is due to both central and peripheral mechanisms.

Pharmacokinetics

Distribution

Up to 99% of ketoprofen binds to plasma proteins, mainly albumin. Cmax is reached quickly due to the low Vd (0.1-0.2 l / kg). Css of ketoprofen is reached 24 hours after the start of its regular use. Ketoprofen penetrates well into synovial fluid and connective tissues. A significant concentration in the synovial fluid is reached within 15 minutes after a single intramuscular injection of ketoprofen at a dose of 100 mg. Although the concentrations of ketoprofen in the synovial fluid are slightly lower than in plasma, they are more stable (persist up to 30 hours), as a result of which pain and joint stiffness are reduced for a long time. In a significant amount, it does not penetrate the BBB. Does not cumulate.

Metabolism

Ketoprofen is mainly metabolized in the liver, where it undergoes glucuronidation to form glucuronic acid esters, which are excreted mainly by the kidneys. Undergoes a 'first pass' effect through the liver.

Withdrawal

It is excreted mainly in the urine. Excretion in feces is less than 1%. T1 / 2 of ketoprofen ranges from 1.6 to 1.9 hours.

Side effect

From the digestive system: abdominal pain, dyspepsia (nausea, vomiting, heartburn, flatulence, loss of appetite, diarrhea), stomatitis, impaired liver function, change in taste. With prolonged use in high doses - ulceration of the gastrointestinal mucosa, gingival, gastrointestinal, hemorrhoidal bleeding.

From the nervous system: headache, dizziness, insomnia, agitation, nervousness, drowsiness, depression, asthenia, confusion or loss of consciousness, memory impairment, 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 hematopoietic system: 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.

With the development of any of the above side effects, as well as with the appearance of other side effects not listed in the instructions, the patient should inform the doctor about it.

Application during pregnancy and lactation

The use of FlamaxЃ in the third trimester of pregnancy and during breastfeeding is contraindicated (you should refuse breastfeeding for the period of use of the drug).

The use of the drug in the I and II trimesters of pregnancy is allowed if the intended benefit to the mother outweighs the potential risk to the fetus.

Application for violations of liver function

Contraindicated for use in severe liver failure or liver disease in the acute period.

Application for impaired renal function

Contraindicated for use in severe renal failure (CC <30 ml / min); progressive kidney disease.

The drug should be prescribed with caution in case of impaired renal function, chronic renal failure (CC 30-60 ml / min).

Application in children

Contraindicated for use in children under 15 years of age.

Use in elderly patients

The drug should be prescribed with caution in elderly patients (over 65 years).

special instructions

With the simultaneous use of FlamaxЃ and warfarin or lithium preparations, patients should be under strict medical supervision.

Care must be taken when prescribing the drug to patients with a history of gastrointestinal ulcers, renal or hepatic insufficiency, as well as receiving coumarin anticoagulants.

Like other drugs in this group, it can mask the symptoms of infectious diseases.

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.

In case of impaired liver and kidney 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 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

Overdose cases are not described.

Symptoms: dizziness, vomiting, headache, shortness of breath, abdominal pain, bleeding, liver and kidney dysfunctions may occur.

Treatment: carrying out symptomatic therapy.

Drug interactions

FlamaxЃ can be combined with central analgesics; can be mixed with morphine in one bottle. Should not be mixed in the same vial with tramadol due to precipitation.

Parenteral administration of FlamaxЃ can be combined with the use of oral forms (tablets, capsules) or rectal suppositories, while the total daily dose can be increased to 300 mg or reduced to 100 mg, depending on the nature of the disease and the patient's condition.

With the simultaneous use of FlamaxЃ and loop diuretics, the nephrotoxic effect of both drugs is enhanced.

Ketoprofen reduces the effectiveness of uricosuric drugs.

Strengthens the action of anticoagulants, antiplatelet agents, fibrinolytics, ethanol, side effects of glucocorticosteroids and mineralocorticosteroids, estrogens; reduces the effectiveness of antihypertensive drugs and diuretics.

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

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

Inducers of microsomal oxidation enzymes in the liver (phenytoin, ethanol, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants) increase the production of hydroxylated active metabolites.

Simultaneous use with sodium valproate leads to a decrease in platelet aggregation.

Ketoprofen increases the plasma concentration of verapamil and nifedipine, lithium preparations, methotrexate.

Antacids and cholestyramine reduce the absorption of ketoprofen.

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