Ketoprofen, pills 100 mg, 20 pcs.

Composition

1 film-coated tablet contains: 

Active ingredient:

ketoprofen 100 mg,

excipients:

giprolose (klucel LF) – 2.4 mg;

mannitol (D-mannitol) – 21 mg;

sodium croscarmellose (primellose) – 5.4 mg;

MCC — 48.4 mg;

colloidal silicon dioxide (aerosil) – 1 mg;

magnesium stearate monohydrate-1.8 mg,

film shell:

Opadry II white (polyvinyl alcohol-4 mg, titanium dioxide-2.5 mg, macrogol (polyethylene glycol) – 2.02 mg, talc-1.48 mg) – 10 mg

Pharmacological action

Absorption-fast, bioavailability-more than 90%. Binding to plasma proteins is 99%. TCmax – 1-2 hours after oral administration,1.4-4 hours-with rectal administration,15-30 minutes – with parenteral administration.

When taking retard tablets, the minimum effective concentration is determined after 45-60 minutes. Css in plasma is reached 24 hours after the start of regular administration. The therapeutic concentration in synovial fluid is maintained for 6-8 hours. It does not penetrate the BBB in significant amounts.

It is almost completely metabolized in the liver by glucuronidation, and has a “first pass” effect through the liver. It is excreted by the kidneys (mainly) and intestines (1%). T1/2 – 1.6-1.9 h – for regular tablets and 5.4 h-for long-acting tablets. It doesn’t accumulate.

Lysine salt of ketoprofen: TCmax after oral administration in the form of granules – 15 minutes, with parenteral administration – 20-30 minutes, with rectal administration-45-60 minutes. The effective concentration is reached in 20-30 minutes and is maintained for 24 hours. The therapeutic concentration in synovial fluid is maintained for 18-20 hours.

It is metabolized by microsomal liver enzymes. It is excreted by the kidneys,60-80% – in the form of glucuronide in 24 hours.

Indications

Inflammatory and degenerative diseases of the musculoskeletal system: rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis, gouty arthritis (with an acute attack of gout, fast-acting dosage forms are preferred), osteoarthritis.

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

Pain syndrome: myalgia, ossalgia, neuralgia, tendinitis, arthralgia, bursitis, sciatica, adnexitis, otitis media, headache and toothache, cancer, post-traumatic and postoperative pain syndrome accompanied by inflammation. Algodismenorrhea, childbirth (as an analgesic and tocolytic agent).

Contraindications

• hypersensitivity to ketoprofen (including other NSAIDs);
• Crohn’s disease;
• peptic ulcer of the stomach and duodenum (exacerbation);
• diverticulitis;
• blood clotting disorders, including hemophilia;
• chronic renal failure;
• pregnancy (third trimester);
• children (up to 6 years).
• hypersensitivity to other components of the drug and salicylates;
• severe heart failure;
• treatment of postoperative pain when performing coronary artery bypass surgery;
• chronic dyspepsia;
• active peptic ulcer or ulcerative/perforation;
• gastrointestinal, cerebrovascular or other bleeding, patients who are prone to hemorrhage;
• severe liver or kidney disease;
• asthma;
• rhinitis or urticaria in history, caused by taking aspirin or other NSAIDs;
• lactation.

With caution: anemia; bronchial asthma; alcoholism; tobacco smoking; alcoholic cirrhosis of the liver; hyperbilirubinemia; liver failure; chronic renal failure (creatinine clearance 30-60 ml/min); a history of ulcerative lesions of the gastrointestinal tract; the presence of Helicobacter pylori infection; long-term use of NSAIDs; diabetes mellitus; dehydration; sepsis; chronic heart failure; edema; arterial hypertension blood disorders (including leukopenia); stomatitis; coronary heart disease; cerebrovascular diseases; dyslipidemia/hyperlipidemia; peripheral artery diseases; severe somatic diseases; concomitant use of oral corticosteroids (including prednisone), anticoagulants (including warfarin), antiplatelet agents (including clopidogrel), SSRIs (including citalopram, fluoxetine, paroxetine, sertraline); old age; pregnancy (I and II trimester)

Side effects

The frequency is classified as rare-from 0.01 to 0.1%; very rare —

From the digestive system: NSAIDs-gastropathy, abdominal pain, dyspepsia (nausea, vomiting, heartburn, flatulence, loss of appetite, diarrhea), stomatitis, liver dysfunction; rarely — erosive and ulcerative lesions, bleeding and perforation of the gastrointestinal tract, taste changes.

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

From the sensory organs: noise or ringing in the ears, blurred visual perception; rarely-conjunctivitis, dryness of the mucous membrane of the eye, pain in the eyes, conjunctival hyperemia, hearing loss, dizziness; additionally for capsules-vertigo.

From the cardiovascular system: edema, increased blood pressure; rarely-tachycardia.

From the respiratory system: hemoptysis, shortness of breath, pharyngitis, rhinitis, bronchospasm, laryngeal edema (signs of anaphylactic reaction); rarely — asthma attacks.

Hematopoietic disorders: rarely-agranulocytosis, anemia, hemolytic anemia, thrombocytopenia, leukopenia. High doses of ketoprofen can inhibit platelet aggregation, thereby prolonging the bleeding time, and cause nosebleeds and bruising.

From the urinary system: edematous syndrome; rarely — cystitis, urethritis, renal dysfunction, interstitial nephritis, nephrotic syndrome; rarely-hematuria.

Immune system disorders: respiratory reactivity, including acute asthma; bronchospasm or shortness of breath (especially in patients with hypersensitivity to acetylsalicylic acid and other NSAIDs); very rarely — angioedema and anaphylaxis.

Allergic reactions: skin rash (including erythematous, urticaria), itchy skin, rhinitis; rarely-exfoliative dermatitis.

Other: increased sweating; rarely-hemoptysis, nosebleeds, myalgia, muscle twitching, shortness of breath, thirst, photosensitization, with prolonged use in large doses — vaginal bleeding.

Laboratory parameters: very often — deviation from the norm of liver function indicators.

Interaction

Reduces the effectiveness of uricosuric drugs, increases the effect of anticoagulants, antiplatelet agents, fibrinolytics, ethanol, side effects of corticosteroids and mineralocorticosteroids, estrogens; reduces the effectiveness of antihypertensive drugs and diuretics.

Concomitant use with other NSAIDs, corticosteroids, ethanol, and corticotropin may lead to ulceration and gastrointestinal bleeding, and increase the risk of developing impaired renal function.

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 necessary).

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

Co-administration with sodium valproate causes a violation of platelet aggregation.

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

Antacids and colestyramine reduce absorption.

Myelotoxic drugs increase the manifestations of hematotoxicity of the drug.

Concomitant administration of ketoprofen and loop diuretics increases the nephrotoxic effect of both drugs.

How to take, course of administration and dosage

Inside, during or immediately after a meal, without chewing, with enough water.

Adults are prescribed 1 tablet 1-2 times a day with an interval of 8 hours. The maximum daily dose is 200 mg.

Overdose

Cases of overdose of the drug are not described.

Treatment: symptomatic, there is no specific antidote to the drug.

Special instructions

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.

Taking ketoprofen may mask the signs of an infectious disease.

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

Influence on the ability to drive vehicles and work with 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

Film-coated tablets

Storage conditions

In a dark place, at a temperature not exceeding 30 °C.

Shelf

life is 2 years.

Active ingredient

Ketoprofen

Conditions of release from pharmacies

By prescription

Dosage form

of the tablet

Weight

Weight: 20 g.