Absorption is fast, bioavailability is more than 90%. Binding to plasma proteins – 99%. TCmax – 1-2 hours after oral administration, 1.4-4 hours – when administered rectally, 15-30 minutes – when administered parenterally.
When taking retard tablets, the minimum effective concentration is determined after 45-60 min. Css in plasma is reached 24 h after the beginning of regular administration. Therapeutic concentration in synovial fluid is maintained for 6-8 h. It does not penetrate through the HEB in significant amounts.
It is almost completely metabolized in the liver by glucuronidation, has a “first pass” effect through the liver.
It is eliminated by the kidneys (mainly) and the intestines (1%). T1/2 – 1.6-1.9 hours – for regular tablets and 5.4 hours – for sustained-action tablets. It does not cumulate.
Ketoprofen lysine salt: TCmax after oral administration as granules – 15 min, when parenteral administration – 20-30 min, when rectal administration – 45-60 min. Effective concentration is reached after 20-30 min and retained for 24 h. Therapeutic concentration in synovial fluid is retained for 18-20 hours.
It is metabolized by microsomal liver enzymes. It is excreted by the kidneys, 60-80% – as glucuronide in 24 hours.
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.
It is intended for symptomatic therapy, to reduce pain and inflammation at the time of use, has no effect on the progression of the disease.
Pain syndrome: myalgia, osalgia, neuralgia, tendinitis, arthralgia, bursitis, radiculitis, adnexitis, otitis, headache and toothache, with cancer, post-traumatic and postoperative pain syndrome accompanied by inflammation.
Algodysmenorrhea, childbirth (as an analgesic and tocolytic agent).
1 film-coated tablet contains:
ketoprofen 100 mg,
Hyprolose (Clucel LF) – 2.4 mg;
Mannitol (D-mannitol) – 21 mg;
croscarmellose sodium (primellose) – 5.4 mg;
MCC – 48.4 mg;
Colloidal silica (aerosil) – 1 mg;
p> magnesium stearate monohydrate – 1.8 mg,
Opadry II white (polyvinyl alcohol – 4 mg, titanium dioxide – 2.5 mg, macrogol (polyethylene glycol) – 2.02 mg, talc – 1.48 mg) – 10 mg
How to take, the dosage
Overly, during or immediately after a meal, without chewing, with enough water.
Adults are prescribed 1 tablet 1-2 times a day at intervals of 8 hours. The maximum daily dose is 200 mg.
Reduces the effectiveness of uricosuric drugs, increases the effect of anticoagulants, antiaggregants, fibrinolytics, ethanol, the side effects of GCS and mineralocorticosteroids, estrogens; reduces the effectiveness of hypotensive drugs and diuretics.
Combined use with other NSAIDs, GCS, ethanol, corticotropin may lead to ulceration and gastrointestinal bleeding, increased risk of renal dysfunction.
Simultaneous use with oral anticoagulants, heparin, thrombolytics, antiaggregants, cefoperazone, cefamandole and cefotetan increases the risk of bleeding.
Enhances 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 production of hydroxylated active metabolites.
Co-administration with sodium valproate causes impaired platelet aggregation.
Enhances plasma concentrations of verapamil and nifedipine, lithium drugs, methotrexate.
Antacids and colestyramine reduce absorption.
Myelotoxic drugs increase the manifestation of hematotoxicity of the drug.
When concomitant administration of ketoprofen and loop diuretics the nephrotoxic effects of both drugs are increased.
At the time of treatment, peripheral blood counts and liver and kidney function should be monitored. If it is necessary to determine 17-ketosteroids, the drug should be discontinued 48 hours before the study.
The administration of ketoprofen may mask the signs of infectious disease.
Dose reduction and close monitoring are necessary if renal and hepatic function is impaired.
Impact on the ability to drive vehicles and operate machinery. During treatment, caution should be exercised when driving motor vehicles and engaging in other potentially hazardous activities requiring increased concentration and quick psychomotor reactions.
- hypersensitivity to ketoprofen (including.
- Hypersensitivity to ketoprofen (including other NSAIDs);
- Cron’s disease;
- Gastric and duodenal ulcer (acute);
- blood-clotting disorders, including hemophilia;
- Chronic renal insufficiency;
- chronic renal failure;
- pregnancy (III trimester);
- children (under 6 years).
- hypersensitivity to other components of the drug and salicylates;
- severe heart failure;
- chronic dyspepsia;
- active peptic peptic ulcer or ulceration/perforation;
- gastrointestinal, cerebrovascular, or other bleeding, patients prone to hemorrhage;
- severe hepatic or renal dysfunction;
- bronchial asthma;
- rhinitis or urticaria in a history caused by taking acetylsalicylic acid or other NSAIDs;
- period of lactation.
Hypersensitivity to ketoprofen.
With caution: Anemia; bronchial asthma; alcoholism; tobacco smoking; alcoholic liver cirrhosis; hyperbilirubinemia; hepatic failure; chronic renal failure (creatinine Cl 30-60 ml/min); history of GI ulcers; presence of Helicobacter pylori infection; long-term NSAID use; diabetes mellitus; dehydration; sepsis; chronic heart failure; edema; arterial hypertension; blood disorders (incl.including leukopenia); stomatitis; coronary heart disease; cerebrovascular disease; dyslipidemia/hyperlipidemia; peripheral arterial disease; severe somatic diseases; concomitant use of oral GCS (including prednisolone).Prednisolone), anticoagulants (including warfarin), antiplatelet agents (including clopidogrel), SSRIs (including citalopram, fluoxetine, paroxetine, sertraline); old age; pregnancy (I and II trimester).
The frequency is classified as rare – 0.01 to 0.1%; very rare –
Digestive system disorders: NSAID gastropathy, abdominal pain, dyspepsia (nausea, vomiting, heartburn, flatulence, decreased appetite, diarrhea), stomatitis, liver dysfunction; rare – erosive ulcerative lesions, bleeding and perforation of the GI tract, changes in taste.
Nervous system disorders: headache, dizziness, insomnia, agitation, nervousness, drowsiness, depression, asthenia; rarely – confusion or loss of consciousness, forgetfulness, memory disturbance, migraine, peripheral neuropathy.
Senses: tinnitus or ringing in the ears, blurred vision; rarely – conjunctivitis, dry mucous membrane of the eye, eye pain, conjunctival hyperemia, decreased hearing, dizziness; additionally for capsules – vertigo.
Systemic system disorders: edema, increased BP; rarely – tachycardia.
Respiratory system: hemoptysis, dyspnea, pharyngitis, rhinitis, bronchospasm, laryngeal edema (signs of anaphylactic reactions); rarely – asthma attacks.
Hematopoietic organs: rare – agranulocytosis, anemia, hemolytic anemia, thrombocytopenia, leukopenia. High doses of ketoprofen may inhibit platelet aggregation, prolonging bleeding time, and cause nasal bleeding and formation of hematomas.
Urinary system disorders: edema syndrome; rarely – cystitis, urethritis, renal dysfunction, interstitial nephritis, nephrotic syndrome; rarely – hematuria.
The immune system: reactive respiratory system, including bronchial asthma, its exacerbation, bronchospasm or dyspnea (especially in patients with hypersensitivity to acetylsalicylic acid and other NSAIDs); very rare – angioedema and anaphylaxis.
Allergic reactions: skin rash (including erythematous, urticaria), skin itching, rhinitis; rarely – exfoliative dermatitis.
Others: increased sweating; rarely – hemoptysis, nasal bleeding, myalgia, muscle twitching, shortness of breath, thirst, photosensitization; with prolonged use in high doses – vaginal bleeding.
Laboratory measures: very often – abnormal liver function parameters.
In cases of overdose of the drug have not been described.
Treatment: symptomatic, there is no specific antidote to the drug.
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|Conditions of storage|
In the dark place at a temperature not exceeding 30 °C.
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