Ketoprofen - instructions for use, doses, side effects, contraindications

Non-selective reversible cyclooxygenase inhibitor, an enzyme that catalyzes the reaction of the conversion of arachidonic acid to prostaglandin H₂, which is the precursor of the remaining prostaglandins, thromboxane A₂ and prostacyclin. Has anti-inflammatory and analgesic, as well as antipyretic effect. It inhibits the aggregation of platelets.

Ketoprofen also inhibits the synthesis of leukotrienes, reduces bradykinin activity, stabilizes lysosomal membranes. With articular syndrome reduces the severity of arthralgia (at rest and during movement), morning stiffness and swelling of the joints, helps reduce the degree of their functional insufficiency. Ketoprofen does not have a catabolic effect on the cartilaginous tissue, and at concentrations of 10^-4 mole / l is able to stimulate the synthesis of proteoglycan in the cells of the immature cartilage of man.

Antipyretic activity is due to the effect on the center of thermoregulation in the hypothalamus.

Pharmacokinetics:

After ingestion, up to 90% is absorbed in the gastrointestinal tract. The maximum concentration in the blood plasma is achieved in 1-2 hours. With rectal application, the maximum concentration in the plasma is reached after 4 hours, with intramuscular injection - 15-45 minutes. The connection with plasma proteins is 99%. The therapeutic concentration persists longer in the synovial fluid than in the blood plasma.

Metabolism in the liver by conjugation with glucuronic acid.

The half-life is 1.1-4 hours. Elimination by the kidneys is the form of metabolites.

Indications:

It is used for the treatment of rheumatism, rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, sciatica, lumbago, tendovaginitis, synovitis, bursitis, trauma of the musculoskeletal system and soft tissues, pain syndrome of various genesis (including postoperative period), primary algodismenorea.

ICD-10

VI.G50-G59.G54.1 Lesions of the lumbosacral plexus

IX.I80-I89.I80.0 Phlebitis and thrombophlebitis of superficial vessels of lower extremities

IX.I80-I89.I89.1 Lymphangitis

X.J00-J06.J02.9 Acute pharyngitis, unspecified

XIII.M05-M14.M06.9 Rheumatoid arthritis, unspecified

XIII.M05-M14.M07.2 * Psoriatic spondylitis (L40.5 +)

XIII.M05-M14.M10.0 Idiopathic Gout

XIII.M05-M14.M13.9 Arthritis, unspecified

XIII.M15-M19.M19.9 Osteoarthritis, unspecified

XIII.M20-M25.M25.5 Pain in the joint

XIII.M40-M43.M42.9 Osteochondrosis of spine, unspecified

XIII.M40-M43.M43.6 Torticollis

XIII.M45-M49.M45 Ankylosing spondylitis

XIII.M50-M54.M54.1 Radiculopathy

XIII.M50-M54.M54.3 Sciatica

XIII.M50-M54.M54.5 Lower back pain

XIII.M65-M68.M65 Synovitis and tenosynovitis

XIII.M70-M79.M71 Other bursopathies

XIII.M70-M79.M79.1 Myalgia

XIV.N80-N98.N94.4 Primary dysmenorrhea

XVIII.R50-R69.R52.0 Acute pain

XVIII.R50-R69.R52.9 Pain, unspecified

XIX.S80-S89.S83.2 Meniscus rupture fresh

XIX.T08-T14.T09.5 Injury of unspecified muscle and tendon of the trunk

XIX.T08-T14.T13.2 Dislocation, stretching and overstrain of the capsular-ligament apparatus of the unspecified joint of the lower limb, level unspecified

XIX.T08-T14.T14.9 Injury, unspecified

XXI.Z100.Z100 * CLASS XXII Surgical Practice

Contraindications:

Peptic ulcer of the stomach and duodenum, ulcerative colitis, gastritis, individual intolerance, children under 15 years.

Carefully:

Severe renal and hepatic insufficiency.

Pregnancy and lactation:

Recommendations for FDA: in the first and second trimesters - B, in the third - D. Contraindicated in pregnancy and lactation.

Dosing and Administration:

The initial dose for ingestion: 300-400 mg per day for 2-3 doses, supporting - 150-200 mg per day.

Intramuscular injection: 100 mg 1-2 times a day.

Intravenous injection: 100-200 mg per 100-150 ml of a 0.9% solution of sodium chloride. Infusions are made only in a hospital!

Outer: the gel / cream / spray is applied to the skin and rubbed, it is permissible to apply a dry bandage.

The highest daily dose: 400 mg.

The highest single dose: 200 mg.

Side effects:

Central and peripheral nervous system: dizziness, drowsiness.

The system of hematopoiesis: rarely - thrombocytopenia.

Digestive system: nausea, heartburn, diarrhea.

Urinary system: rarely - oliguria.

Allergic reactions.

Overdose:

Pain in epigastrium, nausea, vomiting, drowsiness. Rarely - gastrointestinal bleeding, muscle twitching, respiratory depression, coma.

Symptomatic therapy.

Interaction:

With simultaneous use with barbiturates, narcotic analgesics, caffeine, phenothiazine derivatives, diphenhydramine, phenacetin, analgesic effects are enhanced.

Anti-inflammatory effect increases salicylates and metamizol sodium.

Special instructions:

Coagulogram monitoring with prolonged use of the drug. During treatment with the drug should refrain from driving the car and works requiring increased concentration of attention.

Instructions

Ketoprofen (Ketoprophenum)