Composition, form of production and packaging
Suppositories rectal (for children) from white to light yellow color, torpedo-shaped.
1 supp.
ketoprofen lysine salt 60 mg
Excipients: semi-synthetic glycerides - 1020 mg.
5 pieces. - Strips (2) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2016.
PHARMACHOLOGIC EFFECT
NSAIDs. Has anti-inflammatory, analgesic and antipyretic effect. Inhibiting COX-1 and COX-2, inhibits the synthesis of prostaglandins. It has anti-bradykinin activity, stabilizes lysosomal membranes, and delays the release of enzymes that promote tissue destruction in chronic inflammation. Reduces the secretion of cytokines, inhibits the activity of neutrophils.
Reduces the morning stiffness and swelling of the joints, increases the volume of movements.
Ketoprofen lysine salt, in contrast to ketoprofen, is a quick-dissolving compound with a neutral pH and, as a result, almost does not irritate the gastrointestinal tract.
PHARMACOKINETICS
Suction
Ketoprofen lysine salt is rapidly absorbed: after rectal administration, the time to reach C max is 45-60 minutes. The concentration in the plasma depends linearly on the dose taken.
Distribution
Up to 99% of ketoprofen binds to plasma proteins, mainly with albumin. V d is 0.1-0.2 l / kg. Easily penetrates through the histohematological barriers and is distributed in tissues and organs. Ketoprofen penetrates well into the synovial fluid and connective tissue. Although the concentration of ketoprofen in the synovial fluid is somewhat lower than in the plasma, it is more stable (lasts up to 30 hours).
Metabolism
Ketoprofen is mainly metabolized in the liver, where it undergoes glucuronization to form esters with glucuronic acid.
Excretion
Metabolites are excreted mainly with urine (up to 76% within 24 hours). The drug does not cumulate.
INDICATIONS
- short-term symptomatic treatment of inflammatory processes, accompanied by increased body temperature and painful sensations, incl. with diseases of the musculoskeletal system and otitis;
- relief of postoperative pain.
DOSING MODE
Rectal to children aged 6 to 12 years (body weight over 30 kg) appoint 1 suppository for children (60 mg) 1-2 times / day. Children over 12 years can be prescribed 1 suppository (60 mg) 3 times / day. The daily dose should not exceed 5 mg / kg of body weight.
The drug should not be used for more than 5 days without consulting a doctor.
Doses used to treat children do not have sufficient efficacy in the treatment of adults.
SIDE EFFECT
On the part of the hematopoiesis system: leukocytopenia, leukocytosis, lymphangitis, reduction of prothrombin time, thrombocytopenia, thrombocytopenic purpura, enlarged spleen, vasculitis.
From the side of the central nervous system: dizziness, hyperkinesia, tremor, vertigo, mood swings, anxiety, hallucinations, irritability, general malaise.
From the side of the organ of vision: conjunctivitis, impaired vision.
From the cardiovascular system: hypertension, hypotension, tachycardia, chest pain, syncopal conditions.
On the part of the respiratory system: bronchospasm, dyspnoea, sensation of spasm of the larynx, laryngospasm, laryngeal edema, rhinitis.
On the part of the digestive system: abdominal pain, diarrhea, stomatitis, esophagitis, gastritis, duodenitis, erosive and ulcerative gastrointestinal lesions, hematomasis, melena, increased bilirubin level, hepatic enzyme activity, hepatitis, hepatic insufficiency, liver enlargement.
From the urinary system: painful urination, cystitis, swelling, hematuria.
From the skin and subcutaneous tissues: erythematous exanthema, itching, maculopapular rash, increased sweating.
Allergic reactions: urticaria, angioedema, exudative erythema multiforme (including Stevens-Johnson syndrome), anaphylactoid reactions (edema of the oral mucosa, pharyngeal edema, periorbital edema).
Local reactions: burning, itching, heaviness in the anorectal area, exacerbation of hemorrhoids.
Other: disorder of the menstrual cycle, peripheral edema, pallor.
CONTRAINDICATIONS
- "aspirin" asthma;
- Stomach ulcer and duodenal ulcer in the phase of exacerbation;
- ulcerative colitis in the phase of exacerbation;
- Crohn's disease;
- diverticulitis;
- peptic ulcer;
- Violations of blood clotting (including hemophilia);
- chronic renal failure;
- children's age till 6 years;
- Hypersensitivity to ketoprofen or other NSAIDs.
With caution should prescribe the drug for anemia, bronchial asthma, hyperbilirubinemia, liver failure, diabetes mellitus, dehydration, sepsis, chronic heart failure, edema, arterial hypertension, blood diseases (including leukopenia), a deficiency of glikozo-6-phosphate dehydrogenase, stomatitis.
APPLICATION FOR FUNCTIONS OF THE LIVER
The drug in forms for systemic use is contraindicated in the presence of severe impairment of kidney function.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
At systemic application it is necessary to be cautious at an alcoholic cirrhosis of a liver, a hyperbilirubinemia, hepatic insufficiency.
APPLICATION FOR CHILDREN
The drug is contraindicated for children under 6 years.
SPECIAL INSTRUCTIONS
During treatment with Oka, periodic monitoring of the peripheral blood picture and the functional state of the liver and kidneys is necessary.
If it is necessary to determine 17-ketosteroids, the drug should be discontinued 48 hours before the test.
Admission Oka can mask the signs of an infectious disease.
If the kidney and liver function is impaired, a dose reduction and careful monitoring is necessary.
The use of Oka in bronchial asthma can trigger an attack of suffocation.
OVERDOSE
At present, cases of Oka overdose have not been reported.
DRUG INTERACTION
Inducers of microsomal oxidation in the liver (phenytoin, ethanol, barbiturates, flumecinol, rifampicin, phenylbutazone, tricyclic antidepressants) with simultaneous application with the Oca preparation increase the production of hydroxylated active metabolites.
Against the background of simultaneous application with the Oka drug, the effectiveness of uricosuric drugs decreases, the effect of anticoagulants, antiplatelet agents, fibrinolytic agents, ethanol, side effects of mineral corticoids, glucocorticoids, estrogens increases; decreases the effectiveness of antihypertensive drugs and diuretics.
The simultaneous use of Oka with other NSAIDs, GCS, ethanol, corticotropin can lead to the formation of ulcers and the development of gastrointestinal bleeding, an increased risk of kidney dysfunction.
Simultaneous appointment of Oka with oral anticoagulants, heparin, thrombolytic agents, antiaggregants, cefoperazone, cefamandol and cefotetan increases the risk of bleeding.
Oak preparation with simultaneous application increases hypoglycemic action of insulin and oral hypoglycemic drugs (dose recalculation is necessary).
The combined use of Oka with sodium valproate causes disruption of platelet aggregation.
Ketoprofen with simultaneous application increases the concentration in the plasma of verapamil and nifedipine, lithium, methotrexate.
Antacids and colestyramine reduce the absorption of ketoprofen.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored out of the reach of children at a temperature of no higher than 25 В° C. Shelf life - 3 years.
