OKI, 80 mg 2 g 12 pcs

OCI has anti-inflammatory, analgesic and antipyretic effects. By inhibiting COX-1 and -2 it inhibits the synthesis of PG. It has anti-bradykinin activity, stabilizes lysosomal membranes and inhibits the release of enzymes from them that contribute to tissue destruction during chronic inflammation. It reduces release of cytokines, inhibits activity of neutrophils.

Limits morning stiffness and swelling of the joints and increases range of motion.

Ketoprofen lysine salt, unlike ketoprofen, is a rapidly soluble molecule with a neutral pH and is almost non-irritating to the gastrointestinal tract.

Pharmacokinetics

Intake. When administered orally, ketoprofen is quickly and completely absorbed from the gastrointestinal tract, its bioavailability is about 80%. Cmax in plasma is noticed after 0.5-2 hours when administered orally; its size depends on the dose taken; after rectal administration Tmax is 45-60 minutes. CSS of ketoprofen is reached 24 hours after the beginning of its regular use.

Distribution. Up to 99% of absorbed ketoprofen is bound to plasma proteins, mainly to albumin. Vd – 0.1-0.2 l/kg. It easily passes through histohematic barriers and is distributed in tissues and organs. Ketoprofen penetrates well into the synovial fluid and connective tissues. Although concentration of ketoprofen in synovial fluid is slightly lower than in plasma, it is more stable (remains up to 30 h).

Metabolism. Ketoprofen is mainly metabolized in the liver, where it undergoes glucuronidation with formation of glucuronic acid esters.

After the use of 160 mg of ketoprofen lysine salt in the dosage form of topical solution the concentration in plasma of ketoprofen is low – less than 400 ng/ml – and therefore not sufficient for a significant systemic pharmacological effect.

Indications

For adults

rheumatoid arthritis;
spondyloarthritis;
osteoarthritis;
gouty arthritis;
inflammatory damage to periarticular tissues.

Children (over 6 years old)

diseases of the musculoskeletal system;
otitis;
relief of postoperative pain.

Pharmacological effect

OKI has anti-inflammatory, analgesic and antipyretic effects. By inhibiting COX-1 and -2, it inhibits the synthesis of PG. It has anti-bradykinin activity, stabilizes lysosomal membranes and delays the release of enzymes from them that contribute to tissue destruction during 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 soluble molecule with a neutral pH and is almost non-irritating to the gastrointestinal tract.

Pharmacokinetics

Suction. When administered orally, ketoprofen is quickly and fairly completely absorbed from the gastrointestinal tract, its bioavailability is about 80%. Cmax in plasma when taken orally is observed after 0.5–2 hours, its value directly depends on the dose taken; after rectal use, Tmax is 45–60 minutes. CSS of ketoprofen is achieved 24 hours after the start of its regular use.

Distribution. Up to 99% of absorbed ketoprofen is bound to plasma proteins, mainly albumin. Vd – 0.1–0.2 l/kg. Easily passes through histohematic barriers and is distributed in tissues and organs. Ketoprofen penetrates well into synovial fluid and connective tissue. Although the concentration of ketoprofen in synovial fluid is slightly lower than in plasma, it is more stable (lasts up to 30 hours).

Metabolism. Ketoprofen is mainly metabolized in the liver, where it undergoes glucuronidation to form esters with glucuronic acid.

After using 160 mg of ketoprofen lysine salt in the dosage form of a topical solution, the plasma concentration of ketoprofen is low – less than 400 ng / ml – and, therefore, insufficient for a pronounced systemic pharmacological effect.

Special instructions

The drug OCI is prescribed with extreme caution to patients with liver and kidney diseases, diseases of the gastrointestinal tract, and immediately after major surgical interventions.

During treatment with the drug, systematic monitoring of liver and kidney function is necessary.

When prescribed simultaneously with anticoagulants, the risk of bleeding increases.

Active ingredient

Ketoprofen

Composition

Active ingredient:

ketoprofen lysine salt 80 mg;

Excipients:

mannitol – 1700 mg;

sodium chloride – 132 mg;

colloidal silicon dioxide – 3 mg;

ammonium glycerate – 20 mg;

PVP – 20 mg;

sodium saccharin – 15 mg;

mint flavoring – 30 mg

Pregnancy

Like other NSAIDs, OCI should not be used in the third trimester of pregnancy.

The use of the drug in the first and second trimesters should be carefully monitored by the attending physician.

Breastfeeding should be discontinued while using the drug.

Contraindications

erosive and ulcerative lesions of the gastrointestinal tract in the acute phase
“aspirin” asthma
severe impairment of liver and/or kidney function
hypersensitivity to the drug OKI.

Side Effects

From the gastrointestinal tract: abdominal pain, diarrhea, duodenitis, erosive and ulcerative lesions of the gastrointestinal tract, gastritis, hematomesis, esophagitis, stomatitis, melena.

From the liver: increased bilirubin levels, liver enzyme activity, hepatitis, liver failure, increased liver size.

From the nervous system: dizziness, hyperkinesia, tremor, vertigo, mood swings, anxiety, hallucinations, irritability, general malaise.

From the senses: conjunctivitis, visual impairment.

From the skin: urticaria, angioedema, erythematous exanthema, itching, maculopapular exanthema, increased sweating, exudative erythema multiforme (including Stevens-Johnson syndrome).

From the genitourinary system: painful urination, cystitis, edema, hematuria, menstrual irregularities.

From the hematopoietic organs: leukocytopenia, leukocytosis, lymphangitis, decreased PV, purpura, thrombocytopenia, thrombocytopenic purpura, enlarged spleen, vasculitis.

From the respiratory system: bronchospasm, dyspnea, sensation of laryngeal spasm, laryngospasm, laryngeal edema, rhinitis.

From the cardiovascular system: hypertension, hypotension, tachycardia, chest pain, syncope, peripheral edema, pallor.

Allergic reactions: anaphylactoid reactions, swelling of the oral mucosa, pharyngeal edema, periorbital edema.

Local reactions: burning, itching, heaviness in the anorectal area, exacerbation of hemorrhoids.

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 mineralcorticosteroids, corticosteroids, estrogens. Reduces the effectiveness of antihypertensive and diuretic drugs.

Combined use with other NSAIDs, corticosteroids, ethanol, corticotropin can lead to the formation of ulcers and the development of gastrointestinal bleeding, increasing the risk of developing renal dysfunction.

Co-administration with oral anticoagulants, heparin, thrombolytics, antiplatelet agents, cefaperazone, cefamandole and cefotetan increases the risk of bleeding.

Increases the hypoglycemic effect of insulin and oral hypoglycemic drugs (dose recalculation is necessary).

Co-administration with sodium valproate causes disruption of platelet aggregation. Increases plasma concentrations of verapamil and nifedipine, lithium preparations, methotrexate. Antacids and cholestyramine reduce absorption.

Storage conditions

At a temperature not exceeding 25 °C.

Shelf life

5 years

Manufacturer

Dompe Pharmaceutici S.p.A., Italy