Flamax, 50 mg capsules 25 pcs

Pharmacodynamics

Non-steroidal anti-inflammatory drug (NSAID), propionic acid derivative. It has anti-inflammatory, analgesic and antipyretic, anti-aggregation effects.

Inhibits activity of cyclooxygenases 1 and 2 which regulate synthesis of prostaglandins. Analgesic effect is caused by both central and peripheral mechanisms. It has anti-bradykinin activity and stabilizes lysosomal membranes.

Pharmacokinetics

Absorption – fast, bioavailability – 90%. Up to 99 % of absorbed ketoprofen is bound with plasma proteins, mainly with albumin. Maximal concentration of the preparation in plasma (Cmax) is reached quickly (0.5-2 hours after oral administration) due to low volume of distribution (0.1-0.2 l/kg).

The equilibrium plasma concentration (Csс) of ketoprofen is reached 24 hours after the beginning of its regular administration. Ketoprofen penetrates well into the synovial fluid and connective tissues.

The maximum concentration in synovial fluid is 30% of the concentration in the serum, and 4-6 hours after intake exceeds it. Ketoprofen penetrates through the blood-brain barrier. It is almost completely metabolized in the liver by glucuronidation, has a “first pass” effect through the liver. It is excreted by kidneys (mainly) and intestines (1-8%).

The half-life of ketoprofen (T1/2) is 1.6-1.9 hours. In elderly patients the half-life increases to 3-5 hours, in patients with renal insufficiency (creatinine clearance 20-60 ml/min) it is about 3.5 hours. It does not cumulate.

Indications

Inflammatory and degenerative diseases of the musculoskeletal system: Rheumatoid, psoriatic arthritis, Bechterew’s disease (ankylosing spondylitis), gouty arthritis (in an acute attack of gout, fast-acting dosage forms are preferred), osteoarthritis.

Pain syndrome: myalgia, ossalgia, neuralgia, tendinitis, arthralgia, bursitis, radiculitis, adnexitis, otitis, headache and toothache, with cancer, post-traumatic and postoperative pain syndrome accompanied by inflammation. Algodysmenorrhea.

Active ingredient

Composition

active ingredient:

50 mg ketoprofen,

excipients:

lactose monohydrate,

microcrystalline cellulose,

croscarmellose sodium,

sodium lauryl sulfate,

povidone,

silicon dioxide colloid.

Composition of the gelatin capsule:

Titanium dioxide, gelatin, indigo carmine FD&C blue.

How to take, the dosage

Ingestion, with meals. In rheumatic diseases 1 capsule in the morning, 1 in the afternoon and 2 in the evening, or 4 times a day 1 capsule. Combined use of dosage forms is possible.

In patients with renal insufficiency the dose is reduced to 33-50%, in elderly patients the dose is adjusted for age.
In the treatment of pain syndrome and algodysmenorrhea the dose if necessary is 25-50 mg of ketoprofen every 6-8 hours.
The maximum daily dose is 300 mg.

Interaction

Reduces the effectiveness of uricosuric drugs, increases the effect of anticoagulants, antiaggregants, fibrinolytics, ethanol, the side effects of glucocorticosteroids and mineralocorticosteroids, estrogens; reduces the effectiveness of hypotensive drugs and diuretics.

Co-administration with other NSAIDs, glucocorticosteroids, ethanol, corticotropin may lead to ulcer formation and development of gastrointestinal bleeding, to increased risk of renal dysfunction.

The simultaneous use of oral anticoagulants, heparin, thrombolytics, antiaggregants, cefoperazone, cefamandole and cefotetan increases the risk of bleeding.

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

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

Co-administration with sodium valproate causes impairment of platelet aggregation.

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

Myelotoxic drugs increase manifestations of hematotoxicity of the drug.

Special Instructions

When concomitant use of ketoprofen and warfarin, as well as coumarin anticoagulants or lithium salts, patients should be under close medical supervision.

Caution should be exercised when prescribing the drug in patients with a history of gastrointestinal ulcers, renal or hepatic insufficiency. During the treatment it is necessary to monitor peripheral blood count and functional state of liver and kidneys. In case of renal and hepatic dysfunction (increase of ALT activity is the most sensitive indicator of NSAID-induced liver dysfunction) the dose should be reduced and closely monitored.
If it is necessary to determine 17-ketosteroids, the drug should be discontinued 48 hours before the study.

Like other drugs in this group, it may mask signs of infectious disease.

In case of development of visual disorders, an ophthalmologist should be consulted.

When using the drug, caution must be exercised while driving motor transport and engaging in other potentially dangerous activities requiring increased concentration and quick psychomotor reactions.

Contraindications

– hypersensitivity to ketoprofen or any component of the drug;
– history of bronchial asthma caused by ketoprofen, other non-steroidal anti-inflammatory drug or acetylsalicylic acid;
– recurrent gastric and duodenal ulcer;
– peptic ulcer;
– expressed hepatic insufficiency;
– expressed renal insufficiency;
– circulatory system insufficiency;
– gastrointestinal, cerebrovascular and other bleeding (or suspected bleeding);
– pregnancy and lactation;
– childhood (under 15 years);
– hemophilia and other blood clotting disorders;
– ulcerative colitis, Crohn’s disease, diverticulitis.

With caution
Anemia, bronchial asthma, alcoholism, tobacco smoking, alcoholic cirrhosis of the liver, hyperbilirubinemia, hepatic and renal (because the The drug is mainly excreted by the kidneys) insufficiency, diabetes mellitus, dehydration, sepsis, chronic heart failure, edema, arterial hypertension, coronary heart disease, blood diseases (including leukopenia), stomatitis, childhood age (over 15 years), old age.
Pregnancy and lactation
The use of ketoprofen is contraindicated in pregnancy and lactation.

Side effects

– Digestive system disorders: NSAID gastropathy, abdominal pain, dyspepsia (nausea, vomiting, heartburn, flatulence, decreased appetite, diarrhea), stomatitis; change of taste, ulceration and perforation of the mucous membrane of the gastrointestinal tract,
gingival, gastrointestinal, hemorrhoidal bleeding; increased activity of “liver” transaminases in the blood serum, hepatitis.

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

– Sensory organs: tinnitus or ringing in the ears, blurred vision, conjunctivitis, dry mucous membrane of the eye, eye pain, conjunctival hyperemia, decreased hearing, vertigo.

– Cardiovascular system: increase in blood pressure, tachycardia.

– Blood organs: rarely – agranulocytosis, anemia, hemolytic anemia, thrombocytopenia, leukopenia.

– Urinary system disorders: edema syndrome, cystitis, urethritis, renal dysfunction, interstitial nephritis, nephrotic syndrome, hematuria.

– Respiratory system: hemoptysis, dyspnea, bronchospasm, rhinitis, laryngeal edema, nasal bleeding, shortness of breath.

– Skin disorders: skin rash, alopecia and eczema, erythema exudative including Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell’s syndrome), photodermatitis.

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

– Other: increased sweating, myalgia, muscle twitching, shortness of breath, thirst, vaginal bleeding.

Overdose

Symptoms: possible drowsiness, nausea, vomiting, abdominal pain, bleeding, liver and kidney dysfunction.

The treatment is symptomatic: gastric lavage and/or activated charcoal and/or other sorbents. There is no specific antidote.

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