Oki rectal suppositories 160 mg 10 pcs. in Moscow

Oki rectal suppositories 160 mg 10 pcs. in Moscow

Pharmacological action: Inhibits the activity of COX-1 and COX-2, inhibits the synthesis of PG and LT. 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.

The anti-inflammatory effect occurs by the end of 1 week of use. The lysine salt of ketoprofen has equally pronounced anti-inflammatory, analgesic, and antipyretic effects.

In case of articular syndrome, it relieves pain in the joints at rest and during movement, reduces morning stiffness and swelling of the joints, and helps to increase the range of movements.

When taken orally, it is absorbed quickly and quite completely, bioavailability is about 90%. Cmax in the blood is achieved 0.5–2 hours after oral administration, 1.4–4 hours after rectal administration, 15–30 minutes after parenteral administration, and 5–8 hours after application to the skin. When taking retardated forms, the minimum effective concentration is determined after 2–3 hours, Cmax is usually achieved within 6–7 hours. When taken simultaneously with food, the total bioavailability (AUC) does not change, the rate of absorption slows down (for both regular and retardated forms) . Absorption is accompanied by a “first pass” effect through the liver. Binding to blood plasma proteins, mainly albumin - 99%. Equilibrium plasma concentrations are achieved 24 hours after the start of regular use. Easily passes through histohematic barriers and is distributed in tissues and organs. It does not penetrate the BBB in significant quantities. The level of ketoprofen in the synovial fluid is lower than in the blood, but remains within therapeutic limits for a longer time (6–8 hours). Metabolized in the liver by glucuronidation. It is excreted primarily by the kidneys - 80% within 24 hours, mainly in the form of a glucuronic derivative. T1/2 - (2.05±0.58) hours after i.v. administration; 2–4 hours after oral administration in the usual dosage form at a dose of 200 mg; (5.4±2.2) hours after taking the retarded form at a dose of 200 mg. In renal failure, excretion slows down.

Lysine salt of ketoprofen: Tmax after oral administration in the form of granules - 15 minutes, with parenteral administration - 20-30 minutes, with rectal administration - 45-60 minutes. When taken in the form of delayed-release capsules, the effective concentration is achieved within 20–30 minutes and persists for 24 hours.

Therapeutic concentration in synovial fluid persists for 18–20 hours. Metabolized by microsomal liver enzymes. Excreted by the kidneys, 60–80% in the form of glucuronide in 24 hours.

In elderly patients, plasma and renal clearance are reduced, the values ​​of Cmax, AUC and unbound fraction increase with increasing age (more in women than in men).

With cutaneous application, slow transdermal absorption of ketoprofen occurs, which ensures that its concentration in inflamed tissues is maintained within a therapeutic level for a long time. Penetrates well into synovial fluid and connective tissue. Absorption into the systemic circulation is insignificant, bioavailability for gel and spray is about 5%.

When using a solution for topical use (rinse solution) at a dose of 160 mg, Tmax is 1 hour, Cmax value is 350 mg/ml (4% of the concentration obtained by oral administration of 80 mg).

Carcinogenicity, mutagenicity, effect on fertility

Chronic toxicity studies in mice when administered orally (up to 32 mg/kg/day, 96 mg/m2/day, approximately 0.5 MRDC) did not reveal the carcinogenic effect of ketoprofen. In a two-year carcinogenicity study in rats at doses up to 6 mg/kg/day (36 mg/m2/day), no adverse oncogenic effects were detected. Moreover, animals in all groups received drugs for 104 weeks, with the exception of females who received 6 mg/kg/day (36 mg/m2/day) for 81 weeks due to low survival. Survival rate in groups receiving drugs for 104 weeks was 6% compared to the control group.

The mutagenicity of ketoprofen was not detected in the Ames test. When ketoprofen was administered to male rats (up to 9 mg/kg/day, 54 mg/m2/day), no significant effect on reproductive function and fertility was found. In female rats at doses of 6 or 9 mg/kg/day (36 or 54 mg/m2/day), a decrease in the number of implantations was noted.

At high doses, spermatogenesis is disrupted and inhibited in rats and dogs, and testicular weight decreases in dogs and baboon monkeys.

Oki 60mg 10 pcs. rectal suppositories for children

pharmachologic effect

Non-steroidal anti-inflammatory drug.

Composition and release form Oka 60 mg 10 pcs. rectal suppositories for children

Suppositories - 1 soup:

• active ingredient: ketoprofen lysine salt 60 mg;
• auxiliary components: semi-synthetic glycerides 1020 mg.

5 suppositories in a strip of A1 foil.

2 strips in a cardboard box with instructions for use.

Description of the dosage form

Suppositories are white to light yellow and torpedo-shaped.

Characteristic

NSAIDs.

Directions for use and doses

Children from 6 to 12 years old (body weight more than 30 kg) 1 suppository OKI 60 mg 1-2 times a day rectally.

Children over 12 years old up to 3 times a day. The daily dose is not more than 5 mg/kg body weight.

Do not use for more than 5 days without consulting a doctor.

Dosages used to treat children are insufficiently effective in treating adults.

Pharmacodynamics

It has anti-inflammatory, analgesic and antipyretic effects. By inhibiting cyclooxygenase types I and II, 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 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. Ketoprofen lysine salt is rapidly absorbed: the time to reach maximum concentration (Tmax) after rectal administration is 45-60 minutes. The plasma concentration depends linearly on the dose taken.

Distribution. Up to 99% of absorbed ketoprofen is bound to plasma proteins, mainly albumin. Volume of distribution - 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 concentrations of ketoprofen in synovial fluid are slightly lower than in plasma, they are more stable (lasting up to 30 hours).

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

Excretion. Metabolites are excreted mainly in the urine (up to 76% after 24 hours). The drug does not accumulate.

Indications for use Oka 60 mg 10 pcs. rectal suppositories for children

Short-term symptomatic treatment of inflammatory processes accompanied by fever and pain, including diseases of the musculoskeletal system and otitis media. Relief of postoperative pain.

Contraindications

Hypersensitivity (including to other NSAIDs), aspirin-induced asthma, gastric and duodenal ulcers (exacerbation), ulcerative colitis (exacerbation), Crohn's disease, diverticulitis, peptic ulcers, hemophilia and other coagulation disorders blood, chronic renal failure, children's age (up to 6 years).

With caution: anemia, bronchial asthma, hyperbilirubinemia, liver failure, diabetes mellitus, dehydration, sepsis, CHF, edema, arterial hypertension, blood diseases (including leukopenia), glucose-6-phosphate dehydrogenase deficiency, stomatitis.

Application of Oka 60 mg 10 pcs. rectal suppositories for children during pregnancy and breastfeeding

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

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

Breastfeeding should be discontinued while using the drug.

special instructions

During treatment, 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 study.

Taking ketoprofen can mask the signs of an infectious disease.

If renal or liver function is impaired, 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.

Impact on the ability to drive vehicles and operate machinery

During the period of use of the drug, you should refrain from potentially hazardous activities associated with the need for concentration and rapid psychomotor reactions.

Overdose

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

Side effects of Oka 60 mg 10 pcs. rectal suppositories for children

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, tremor, vertigo, mood swings, anxiety, hallucinations, irritability, general malaise.

Sense organs: conjunctivitis, visual impairment.

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

Genitourinary 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, sensation of laryngeal spasm, laryngospasm, laryngeal edema, rhinitis.

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.

Drug interactions

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, glucocorticosteroids, estrogens. Reduces the effectiveness of antihypertensive and diuretic drugs.

Combined use with other NSAIDs, glucocorticosteroids, 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, cefoperazone, 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.

Okie

Oki (ketoprofen) is an NSAID whose precursor is methylacetic acid. It has analgesic, anti-inflammatory and antipyretic effects. The pharmacological activity of the drug is a consequence of its ability to inhibit the activity of the enzyme cyclooxygenase, which takes part in the metabolic reactions of the precursor of pain and inflammation mediators arachidonic acid. Prostaglandins, in turn, are a kind of instigator of a “biochemical revolution” in the body in the form of pain, fever and inflammation. The analgesic effect of the drug develops according to two physiological patterns: peripheral (supported by inhibition of the formation of the prostaglandins already mentioned above) and central (associated with the suppression of the synthesis of prostaglandins in the central nervous system and the influence on the biological activity of other substances that can interact with neurons and are involved in the release of algogenic neurotransmitters in the spinal brain). In addition to this, the drug suppresses the activity of bradykinin, stabilizes the state of lysosome membranes, and inactivates neutrophil granulocytes in individuals with infectious nonspecific polyarthritis. Prevents platelets from sticking to each other. When taken orally and in suppositories, it is well absorbed from the gastrointestinal tract. Peak concentration in the blood is observed at 2-5 hours (oral form) and 45-60 minutes (suppositories) from the moment of administration. Almost all of the incoming amount of the drug interacts with plasma proteins. Undergoes metabolic transformations in the liver. Elimination from the body occurs mainly through urine and, to a lesser extent, through feces. Half-life is 1.5-2 hours. Used for infectious nonspecific polyarthritis, deforming arthrosis, ankylosing spondylitis, inflammation of periarticular tissues of large joints (joint capsule, ligaments, surrounding tendons and muscles), synovial membrane of joints, inflammation and degeneration of tendon tissue, inflammation of the joint capsule, spinal pain, muscle pain , sports and household injuries (dislocations, bruises, sprains), as part of combined pharmacotherapy for inflammation of the vessels of the venous and lymphatic beds (inflammation of the venous walls, tissues surrounding the vein, lymphatic vessels and superficial lymph nodes).

The dose of the drug (initial, loading, maintenance) is set individually depending on the clinical picture and individual characteristics of the patient. Possible side effects: epigastric pain, vomiting, involuntary eruption of stomach contents through the mouth, constipation or diarrhea, loss of appetite, stomach pain, liver dysfunction, headaches, partial loss of balance, tinnitus, sleep disorder accompanied by a constant or periodic desire to sleep during times not intended for sleep, renal dysfunction, bronchospasm. The drug is not used for ulcers and erosions of the stomach and duodenum in the acute phase, intolerance to aspirin, severe disorders of the liver and kidneys, pregnancy, individual intolerance to the active component and any salicylates (oral form - granules), inflammation of the rectum and bleeding from the , incl. preceding treatment (for suppositories), weeping dermatitis, eczematous skin lesions, bacterially contaminated wounds in the treatment area (for topical solution). Persons suffering from diseases of the liver or kidneys, the digestive tract, with signs of dyspepsia while taking the drug should be under regular medical supervision with monitoring of the main functional indicators of the liver and kidneys. It is not recommended to use the drug with other NSAIDs: this increases the risk of damage to the mucous membrane of the digestive tract. When OCIs are used together with antihypertensive drugs, the effect of taking the latter is reduced.