OKI rectal suppositories 160mg, No. 10

Symptomatic treatment of inflammatory processes accompanied by fever and pain, including inflammatory and rheumatic diseases of the joints:

• rheumatoid arthritis

• spondyloarthritis

• osteoarthritis

• gouty arthritis

• inflammatory lesion of periarticular tissues

One suppository 2-3 times a day. The maximum daily dose is 480 mg.

In elderly patients, it is necessary to use no more than 2 suppositories per day.

One suppository contains:
Active ingredient - ketoprofen lysine salt 160 mg;
Auxiliary components: semi-synthetic glycerides 1640 mg

• Hypersensitivity (including to other NSAIDs),

• 'aspirin' asthma,

• peptic ulcer and 12 duodenal ulcer (exacerbation),

• ulcerative colitis (exacerbation),

• Crohn's disease,

• diverticulitis

• peptic ulcer,

• hemophilia and other blood clotting disorders,

• Chronic renal failure,

• children's age (up to 18 years old),

• pregnancy (III trimester), lactation period.

Carefully

- anemia, bronchial asthma, alcoholism, tobacco smoking, alcoholic cirrhosis of the liver, hyperbilirubinemia, liver failure, diabetes mellitus, dehydration, sepsis, CHF, edema, arterial hypertension, blood diseases (including leukopenia), glucose-6-phosphate dehydrogenase deficiency , stomatitis, advanced age, pregnancy (I, II trimester).
If the patient's condition worsens, treatment with the drug should be discontinued.

Trade name of the drug: OKI

International Non-Proprietary Name (INN): ketoprofen

Active substance name: ketoprofen lysine salt

Chemical name: Lysine 2- (3-benzoylphenyl) propionate LD

Dosage form:

rectal suppositories

Composition
One suppository contains:
Active ingredient - ketoprofen lysine salt 160 mg;
Auxiliary components: semi-synthetic glycerides 1640 mg

Description. Suppositories from white to light yellow torpedo-shaped.

Pharmacotherapeutic group. Non-steroidal anti-inflammatory drug (NSAID).

Pharmacological properties
It has anti-inflammatory, analgesic and antipyretic effects. By inhibiting type I and II cyclooxygenase, it inhibits the synthesis of prostaglandins. It has anti-bradykinin activity, stabilizes lysosomal membranes and delays the release of enzymes from them that contribute to tissue destruction in chronic inflammation. Reduces the release of cytokines, inhibits the activity of neutrophils.
Reduces morning stiffness and swelling of joints, increases range of motion. Ketoprofen lysine salt, unlike ketoprofen, is a rapidly dissolving molecule with a neutral pH and almost does not irritate the gastrointestinal tract.

Pharmacokinetics.
Suction. Ketoprofen lysine salt is rapidly absorbed: the time to reach the maximum concentration (Tmax) after rectal administration is 45-60 minutes. The plasma concentration is linearly dependent on the dose taken. Distribution. Up to 99% of absorbed ketoprofen binds to plasma proteins, mainly albumin. The volume of distribution is 0.1-0.2 l / kg. Easily passes through histohematogenous barriers and is distributed in tissues and organs. Ketoprofen penetrates well into synovial fluid and connective tissues. Although the concentrations of ketoprofen in synovial fluid are slightly lower than in plasma, they are more stable (persist up to 30 hours).
Metabolism. Ketoprofen is mainly metabolized in the liver, where it undergoes glucuronidation to form glucuronic acid esters. Excretion. Metabolites are excreted mainly in the urine (up to 76% after 24 hours). The drug does not cumulate.

Indications.

Symptomatic treatment of inflammatory processes accompanied by fever and pain, including inflammatory and rheumatic diseases of the joints:

• rheumatoid arthritis

• spondyloarthritis

• osteoarthritis

• gouty arthritis

• inflammatory lesion of periarticular tissues

Contraindications

Hypersensitivity (including to other NSAIDs), 'aspirin' asthma, peptic ulcer and 12 duodenal ulcer (exacerbation), ulcerative colitis (exacerbation), Crohn's disease, diverticulitis, peptic ulcer, hemophilia and other clotting disorders blood, chronic renal failure, children's age (up to 18 years), pregnancy (III trimester), lactation.

Carefully

- anemia, bronchial asthma, alcoholism, tobacco smoking, alcoholic cirrhosis of the liver, hyperbilirubinemia, liver failure, diabetes mellitus, dehydration, sepsis, CHF, edema, arterial hypertension, blood diseases (including leukopenia), glucose-6-phosphate dehydrogenase deficiency , stomatitis, advanced age, pregnancy (I, II trimester).
If the patient's condition worsens, treatment with the drug should be discontinued.

Method of administration and dosage

One suppository 2-3 times a day. The maximum daily dose is 480 mg. In elderly patients, it is necessary to use no more than 2 suppositories per day.

Side effects
Gastrointestinal tract: abdominal pain, diarrhea, duodenitis, erosive and ulcerative lesions of the gastrointestinal tract, gastritis, hematomesis, esophagitis, stomatitis, melena.
Liver: increased bilirubin, increased liver enzymes, hepatitis, liver failure, increased liver size.
Nervous system: dizziness, hyperkinesia, tremors, vertigo, mood swings, anxiety, hallucinations, irritability, general malaise.
Sense organs: conjunctivitis, visual impairment.
Skin: urticaria, angioedema, erythematous exanthema, pruritus, maculopapular exanthema, increased sweating, exudative erythema multiforme (including Stevens-Johnson syndrome).
Urogenital system: painful urination, cystitis, edema, hematuria, menstrual irregularities.
Hematopoietic organs: leukocytopenia, leukocytosis, lymphangitis, decreased prothrombin time, purpura, thrombocytopenia, thrombocytopenic purpura, enlarged spleen, vasculitis.
Respiratory system: bronchospasm, dyspnea, laryngeal spasm sensation, laryngospasm, laryngeal edema, rhinitis.
Cardiovascular system: hypertension, hypotension, tachycardia, chest pain, syncope, peripheral edema, pallor.
Allergic reactions: anaphylactoid reactions, edema of the oral mucosa, pharyngeal edema, periorbital edema.
Local reactions: burning, itching, heaviness in the anorectal region, exacerbation of hemorrhoids.

Overdose.
Currently, no cases of OCI overdose have been reported.

Interaction
Inducers of microsomal oxidation in the liver (phenytoin, ethanol, barbiturates, flumecinol, rifampicin, phenylbutazone, tricyclic antidepressants) increase the production of hydroxylated active metabolites.
Reduces the effectiveness of uricosuric drugs, enhances the effect of anticoagulants, antiplatelet agents, fibrinolytics, ethanol, side effects of mineral corticosteroids, glucocorticosteroids, estrogens. Reduces the effectiveness of antihypertensive and diuretics.
Joint reception with other NSAIDs, glucocorticosteroids, ethanol, corticotropin can lead to the formation of ulcers and the development of gastrointestinal bleeding, to an increase in the risk of developing renal dysfunction.
Concomitant administration with oral anticoagulants, heparin, thrombolytics, antiplatelet agents, cefaperazone, cefamandol and cefotetan increases the risk of bleeding.
Increases the hypoglycemic effect of insulin and oral hypoglycemic drugs (dose recalculation is required).
Co-administration with sodium valproate causes impaired platelet aggregation. Increases plasma concentration of verapamil and nifedipine, lithium preparations, methotrexate. Antacids and cholestyramine reduce absorption.
Application during pregnancy and lactation. Like other NSAIDs, OCI should not be used in the third trimester of pregnancy. The use of the drug in the I and II trimester should be carefully monitored by the attending physician. Breastfeeding while using the drug should be discontinued.

Special instructions.
During treatment, it is necessary to control 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 can mask the signs of an infectious disease. In case of impaired renal and liver function, dose reduction and careful monitoring are necessary. The use of ketoprofen by patients suffering from bronchial asthma can lead to an attack of bronchial asthma.
Women planning pregnancy should refrain from taking the drug, because the likelihood of egg implantation may decrease.
Influence on the ability to drive vehicles and control mechanisms.
During the period of use of the drug, one should refrain from potentially hazardous activities associated with the need for concentration of attention and rapid psychomotor reactions.