Flamax, ampoules 50 mg/ml, 2 ml, 10 pcs.

Composition

1 ampoule (2 ml) contains ketoprofen 100 mg;

excipients:

propylene glycol;

ethanol (95% ethyl alcohol in terms of 100% substance);

benzyl alcohol;

sodium hydroxide;

water for injection.

Pharmacological action

Pharmaceutical Group:

NSAIDs.

Pharmaceutical action: 

Flamax is a nonsteroidal anti-inflammatory drug derived from propionic acid. It has analgesic, anti-inflammatory and antipyretic effects, suppresses platelet aggregation. Ketoprofen acts on the cyclooxygenase and lipoxygenase components of arachidonic acid metabolism and inhibits the synthesis of prostaglandins, leukotrienes, and thromboxanes.

The analgesic effect is caused by both central and peripheral mechanisms. It has anti-radikinin activity, stabilizes lysosomal membranes.

Pharmacokinetics: 

Distribution.

Up to 99% of absorbed ketoprofen binds to plasma proteins, mainly albumin. The maximum concentration of the drug in plasma (Cmax) is reached quickly due to the low volume of distribution (0.1-0.2 l / kg). The steady-state concentration of ketoprofen is reached 24 hours after the start of its regular intake. Ketoprofen penetrates well into synovial fluid and connective tissues.

Significant levels of synovial fluid concentrations are reached as early as 15 minutes after a single intramuscular injection of 100 mg of ketoprofen. Although the concentrations of ketoprofen in synovial fluid are slightly lower than in plasma, they are more stable (they last up to 30 hours), as a result of which pain and joint stiffness are reduced for a long time.

Metabolism, elimination.

Ketoprofen is mainly metabolized in the liver, where it undergoes glucuronidation to form esters with glucuronic acid, which are mainly excreted by the kidneys. Excretion with fecal matter is less than 1%. The half-life of ketoprofen ranges from 1.6 to 1.9 hours. It doesn’t accumulate.

Indications

Inflammatory and degenerative diseases of the musculoskeletal system:

– rheumatoid arthritis; – seronegative arthritis: ankylosing spondylitis (Ankylosing spondylitis), psoriatic arthritis, reactive arthritis (Reiter’s syndrome);- gout, pseudogout; – osteoarthritis.

Pain syndrome:

– tendinitis, bursitis, myalgia, neuralgia, sciatica; – migraine;- post-traumatic and postoperative pain syndrome;- pain syndrome in cancer; – algodismenorrhea.

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

Contraindications

“Aspirin” asthma, peptic ulcer of the stomach and duodenum (exacerbation), ulcerative colitis (exacerbation), Crohn’s disease, diverticulitis, peptic ulcer, blood coagulation disorders (including hemophilia), renal and liver failure, children and adolescents under 18 years of age, pregnancy (III trimester).

Side effects

The following side effects (possibly related to the use of ketoprofen)have been reported in clinical trials:

Gastrointestinal disorders: dyspepsia (11%); 3-9% — nausea, abdominal pain, diarrhea/constipation, flatulence; >1% — anorexia, vomiting, stomatitis;>

From the nervous system and sensory organs: 3-9% – headache, agitation (including insomnia, nervousness, unusual dreams); >1% – dizziness, central nervous system depression (including drowsiness, malaise), tinnitus, visual impairment;>

Cardiovascular and blood disorders (hematopoiesis, hemostasis):

From the respiratory system: > 1% — dyspnoea, hemoptysis, nosebleeds, pharyngitis, rhinitis, bronchospasm, laryngeal edema.

From the genitourinary system: 3-9% – impaired renal function (edema, increased blood urea nitrogen); >1% – symptoms and signs of urinary tract irritation;>

Skin disorders: >1% – rash, alopecia, eczema, pruritis, urticaria, bullous rash, exfoliative dermatitis, photosensitization, skin discoloration, onycholysis, toxic epidermal necrolysis, erythema multiforme, Stevens-Johnson syndrome.

Interaction

With the simultaneous use of Flamax® and loop diuretics, the nephrotoxic effect of both drugs is enhanced. Reduces the effectiveness of uricosuric drugs, increases the effect of anticoagulants, antiplatelet agents, fibrinolytics, ethanol, side effects of glucocorticosteroids and mineralocorticosteroids, estrogens; reduces the effectiveness of antihypertensive drugs and diuretics.

Concomitant use with other NSAIDs, glucocorticosteroids, ethanol, and corticotropin may lead to ulceration and gastrointestinal bleeding, as well as an increased risk of developing impaired renal function. Concomitant use with oral anticoagulants, heparin, thrombolytics, antiplatelet agents, cefaperazone, cefamandol and cefotetan increases the risk of bleeding.

Increases the hypoglycemic effect of insulin and oral hypoglycemic drugs (dose recalculation is necessary). Inducers of microsomal oxidation in the liver (phenytoin, ethanol, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants) increase the production of hydroxylated active metabolites. Combined use with sodium valproate leads to a decrease in platelet aggregation.

Increases plasma concentrations of verapamil and nifedipine, lithium preparations, and methotrexate. Antacids and colestyramine reduce absorption.

Increases the hematotoxicity of myelotoxic drugs.

To avoid sediment, do not mix Flamax and tramadol in one bottle.

How to take, course of administration and dosage

Intramuscular administration: 100 mg (1 amp. ) 1-2 times a day.

Intravenous infusion of Flamax should be performed only in a hospital setting.

Short-term intravenous infusion: 100-200 mg (1-2 amp. ) of the drug, diluted in 100 ml of 0.9% sodium chloride solution, is administered within 0.5–1 h. Repeated administration is possible after 8 hours.

Prolonged intravenous infusion: 100-200 mg (1-2 amp. ) of the drug diluted in 500 ml of infusion solution (0.9% sodium chloride solution, lactate-containing Ringer’s solution,5% dextrose solution), administered for 8 hours. Repeated administration is possible after 8 hours.

The maximum dose is 200 mg / day.

The minimum effective dose should be used in the shortest possible course.

Overdose

Cases of overdose are not described.

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

Treatment: symptomatic.

Special instructions

Patients with concomitant use of Flamax® and warfarin or lithium preparations should be under strict medical supervision. Caution should be exercised 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 monitor 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 or kidney function, dose reduction and careful monitoring are necessary.

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

Influence on the ability to drive motor vehicles and manage mechanisms

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

Form of production

Solution for intravenous and intramuscular administration.

Storage conditions

In a dark place, at a temperature not exceeding 25°C.

Shelf

life is 3 years.

Active ingredient

Ketoprofen

Conditions of release from pharmacies

By prescription

Dosage form

solution for injection

Weight

Weight: 57 gr.