Universal reference book for medicines
Product name: OKI

Active substance: ketoprofen

Type: NSAIDs

Manufacturer: DOMPE FARMACEUTICI (Italy)
Composition, form of production and packaging
Granules for solution for ingestion
from white to light yellow, with a characteristic smell of mint.

1 pack.
(2 g)
ketoprofen lysine (ketoprofen lysine salt) 80 mg,

which corresponds to the content of ketoprofen 50 mg

Auxiliary substances: mannitol - 1700 mg, povidone - 132 mg, silicon dioxide colloid - 3 mg, sodium chloride - 20 mg, sodium saccharinate - 15 mg, ammonium glycyrrhizinate 20 mg, flavoring mint - 30 mg.

2 g - sachets two-volume three-layer (12) - packs cardboard.

2 g - bags two-volume three-layer (20) - packs 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

After oral administration, it is quickly and sufficiently absorbed from the digestive tract, bioavailability is about 80%.
The time to reach C max after oral administration is 0.5-2 hours. The concentration in the plasma is linearly dependent on the dose taken.
Distribution

C ss is achieved 24 hours after the start of its regular intake.
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.
The drug does not cumulate.
INDICATIONS

For
of adults
Symptomatic treatment of inflammatory processes accompanied by pain syndrome, including:

- tendonitis, bursitis;

- myalgia;

- Neuralgia, sciatica;

- toothache;

- algodismenorea;

- post-traumatic and postoperative pain syndrome;

- pain syndrome in cancer diseases;

Inflammatory and degenerative diseases of the musculoskeletal system:

- rheumatoid arthritis;

- seronegative arthritis;

ankylosing spondylitis (Bekhterev's disease);

- gout, pseudogout;

- osteoarthrosis;

- psoriatic arthritis;

- reactive arthritis (Reiter's syndrome).

For
children (over the age of 6 years)
- short-term symptomatic treatment of inflammatory processes accompanied by pain syndrome in combination with heat or without it with diseases of the musculoskeletal system and otitis;

- relief of postoperative pain.

The drug is intended for symptomatic therapy, reducing pain and inflammation at the time of application, the progression of the disease is not affected.

DOSING MODE

For adults, the drug is given 80 mg 3 times / day during meals.
To get 1 full dose (80 mg), open a double sachet along the line labeled "full dose" and dissolve its contents in half a glass of water.
For elderly patients, the dose is determined by the doctor, it is desirable to reduce the dose by about 2 times.

For children aged 6 to 14 years , the drug is prescribed 40 mg 3 times per day during meals.
Before use, the contents of 1/2 double sachet (half the dose) should be dissolved in half a glass of water. To get half the dose (40 mg), you should open a double bag along the line labeled "half the dose."
Children between the ages of 14 to 18 years are prescribed a drug in a dose appropriate for adults.

To reduce the risk of developing adverse events from the gastrointestinal tract, the minimum effective dose should be used as short as possible.

SIDE EFFECT

According to the WHO, unwanted effects are classified according to their frequency of development as follows: very often (1/10), often (from 1/100 to? 1/10), infrequently (from 1/1000 to? 1/100), rarely (from 1/10 000 to? 1/1000), very rarely (? 1/10 000), the frequency is unknown (it is impossible to determine based on available data).

From the hemopoietic system: rarely - hemorrhagic anemia;
frequency unknown - thrombocytopenia, thrombocytopenic purpura, agranulocytosis, bone marrow dysfunction, leukocytopenia, leukocytosis, lymphangitis.
From the side of the central nervous system: infrequently - headache, dizziness, drowsiness;
rarely - paresthesia, blurred vision, tinnitus; frequency is unknown - cramps, dysgeusia, mood changes, irritability, insomnia.
From the cardiovascular system: the frequency is unknown - heart failure, tachycardia, heart palpitations, arterial hypertension, arterial hypotension, vasodilation.

From the respiratory system: rarely - bronchial asthma;
frequency unknown - bronchospasm (especially in patients with confirmed hypersensitivity to acetylsalicylic acid and other NSAIDs), rhinitis, dyspnea, edema and spasm of the larynx.
From the digestive system: often - nausea, vomiting, dyspepsia, abdominal pain;
infrequently - constipation, diarrhea, bloating, gastritis; rarely - stomatitis, stomach and duodenal ulcers, hepatitis, increased activity of hepatic transaminases and increased serum bilirubin caused by impaired liver function; frequency unknown - exacerbation of ulcerative colitis and Crohn's disease, gastrointestinal bleeding, perforation, heartburn.
From the side of the urinary system: the frequency is unknown - acute renal failure, tubulointerstitial nephritis and nephritic syndrome, changes in the values ​​of renal function indicators.

From the skin and subcutaneous tissues: infrequently - rash, itching;
frequency unknown - alopecia, erythema and exanthema, maculopapular rash, dermatitis.
Allergic reactions: frequency unknown - anaphylactic reactions (including anaphylactic shock), edema of the oral cavity, periorbital edema, photosensitivity reactions, urticaria, angioedema, bullous skin reactions, including Stevens-Johnson syndrome and toxic epidermal necrolysis (Lyell's syndrome).

Other: infrequently - swelling, fatigue.

If any adverse reactions occur, stop taking the medication immediately and consult a doctor.

CONTRAINDICATIONS

- complete or incomplete combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses and intolerance to acetylsalicylic acid or other NSAIDs (including in anamnesis);

- erosive and ulcerative lesions of the stomach and duodenum in the phase of exacerbation;

- active gastrointestinal, cerebrovascular or other bleeding;

- ulcerative colitis in the phase of exacerbation;

- Crohn's disease;

- Violations of blood clotting (including hemophilia);

Decompensated heart failure;

- period after aorto-coronary bypass;

- hepatic insufficiency of severe degree or liver disease in the active phase;

- renal failure of severe degree (QC less than 30 ml / min);

progressive kidney disease;

- Hyperkalemia;

- children's age till 6 years;

- III trimester of pregnancy;

- lactation period;

- Hypersensitivity to ketoprofen, other components of the drug or other NSAIDs.

With caution should prescribe the drug for peptic ulcer of the stomach and duodenal ulcer, ulcerative colitis, Crohn's disease, liver disease in history, liver porphyria, chronic kidney failure (KK 30-60 ml / min), chronic heart failure, hypertension, a significant decrease in BCC (including after surgery), bronchial asthma, IHD, cerebrovascular diseases, dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral arterial diseases, smoking, infection
(including prednisolone), anticoagulants (including warfarin), antiplatelet agents (including acetylsalicylic acid , clopidogrel), selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline), in the first and second trimesters of pregnancy, as well as in elderly patients (incl. after receiving diuretics, weakened patients and patients with low body weight).
PREGNANCY AND LACTATION

The use of ketoprofen in the III trimester of pregnancy is contraindicated.
In the first and second trimesters of pregnancy, the drug is only possible if the intended benefit to the mother exceeds the potential risk to the fetus.
The drug should not be used during lactation.

The use of the drug may adversely affect fertility in women, so it is not recommended for women planning a pregnancy.
In women with fertility problems or undergoing fertility research, the drug should be discontinued.
APPLICATION FOR FUNCTIONS OF THE LIVER

The drug is contraindicated in patients with severe renal insufficiency (QC less than 30 ml / min), progressive kidney disease.

With caution should prescribe the drug for chronic kidney failure (KK 30-60 ml / min).

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

The drug is contraindicated in cases of hepatic insufficiency of a serious degree or diseases of the liver in the active phase.

Care should be taken with liver diseases in history, liver porphyria.

APPLICATION FOR CHILDREN

The drug is contraindicated for children under 6 years.

For children aged 6 to 14 years , the drug is prescribed 40 mg 3 times per day during meals.
Before use, the contents of 1/2 double sachet should be dissolved in half a glass of water.
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.
APPLICATION IN ELDERLY PATIENTS

Use with caution in elderly patients.

For elderly patients, the dose should be reduced approximately 2-fold.

SPECIAL INSTRUCTIONS

At the beginning of treatment, it is necessary to monitor the pattern of peripheral blood and the functional state of the liver and kidneys.

After 2 weeks of using the drug, it is necessary to monitor the liver function (transaminase activity).

The use of ketoprofen in bronchial asthma can trigger an attack of suffocation.

If it is necessary to determine 17-ketosteroids, the drug should be discontinued 48 hours before the test.

Ketoprofen can alter the properties of platelets, but does not replace prophylactic use of acetylsalicylic acid in cardiovascular diseases.

Reception of ketoprofen can mask signs of an infectious disease.

Elderly patients, patients with a stomach ulcer or duodenal ulcer in the anamnesis, as well as patients taking low-dose acetylsalicylic acid or other drugs that may increase the risk of gastrointestinal reactions, show concurrent use of protective drugs (misoprostol or proton pump inhibitors).

The drug does not affect the effectiveness of low-calorie and controlled diets, and can be used in patients with diabetes mellitus.

The drug does not contain gluten, so the drug can be administered to patients with celiac disease.

The drug does not contain aspartame, so it can be prescribed to patients with phenylketonuria.

Cardiovascular and cerebrovascular effects

Patients with hypertension and / or heart failure of moderate severity, accompanied by fluid retention and edema (in the anamnesis) associated with the administration of NSAIDs require close monitoring and consultation.

Clinical studies and epidemiological data indicate that the use of certain NSAIDs (especially in high doses for a long time) may be associated with a slight increase in the risk of arterial thrombotic events (eg, myocardial infarction or stroke).
Data for eliminating the above risk for ketoprofen lysine salt is not enough.
Patients with uncontrolled hypertension, heart failure, coronary artery disease, peripheral arterial disease and / or cerebrovascular disease should be given ketoprofen lysine salt only after a thorough examination.
Similar patients should have patients with risk factors for cardiovascular diseases (eg, hypertension, hyperlipidemia, diabetes, smoking) before starting long-term treatment.
Impact on the ability to drive vehicles and manage mechanisms

The drug has a limited and moderate effect on the ability to drive vehicles or mechanisms due to the possible occurrence of dizziness and drowsiness.
If drowsiness, dizziness, or convulsions are observed with the drug, motor vehicle management and mechanisms should be avoided, as well as other activities requiring concentration.
OVERDOSE

Cases of overdose were observed with the use of ketoprofen in a dose of 2.5 g. In most cases, the symptoms were limited to lethargy, drowsiness, nausea, vomiting and pain in the epigastric region.

Treatment: a specific antidote is unknown.
As a symptomatic measure in the provision of vital functions (stabilization of blood circulation, equalization of acidosis, artificial respiration), measures that reduce resorption and accelerate excretion (reception of activated charcoal, forced diuresis) are shown.
DRUG INTERACTION

Combinations that must be avoided

Corticosteroids: increased risk of ulceration and gastrointestinal bleeding.

Anticoagulants (heparin, warfarin): increased risk of bleeding caused by inhibition of platelet function and damage to the mucous membrane of the stomach and intestines.
NSAIDs can enhance the effects of anticoagulants, such as warfarin.
Antiaggregants (clopidogrel, ticlopidine) and selective serotonin reuptake inhibitors: the risk of bleeding caused by inhibition of platelet aggregation and damage to the mucous membrane of the stomach and intestines is increased.
Patients should be monitored if joint use can not be avoided.
Other NSAIDs, including salicylates in high doses (> 3 g / day): simultaneous application of several NSAIDs may increase the risk of ulceration and gastrointestinal bleeding, which is due to a synergistic effect.

Lithium: NSAIDs increase the concentration of lithium in the plasma (reducing the excretion of lithium by the kidneys), which can reach toxic levels.
This parameter should be monitored at the beginning of treatment, with dose adjustment and after cessation of treatment with ketoprofen.
Methotrexate in high doses (more than 15 mg / week): the hematotoxicity of methotrexate is increased, t.
decreased its excretion by the kidneys, which occurs when using anti-inflammatory drugs. When used simultaneously with methotrexate in low doses (less than 15 mg / week), it is necessary to perform a general blood test 1 time / week during the first few weeks of treatment. It is necessary to carry out more frequent monitoring of the clinical state with even a slight impairment of kidney function, as well as in elderly patients.
Hydantoin and sulfonamides: the toxic effects of these substances can be exacerbated.

Combinations that require precautions

Diuretics, ACE inhibitors and angiotensin II antagonists: NSAIDs may reduce the effectiveness of diuretics and antihypertensive agents.
In patients with impaired renal function (eg, patients with dehydration or elderly patients) simultaneous use of ACE inhibitors or angiotensin II antagonists with preparations that inhibit COX can cause additional renal dysfunction, including. acute renal failure, usually reversible. Patients should receive enough fluid, after the initiation of concomitant therapy, it is necessary to monitor kidney function.
Petyxifylline: the risk of bleeding increases.
It is obligatory to conduct more frequent monitoring of the clinical condition and control of clotting time.
Zidovudine: the risk of toxicity to erythrocytes is increased by affecting reticulocytes with severe anemia a week after initiation of NSAID treatment.
It is necessary to perform a general blood test and monitor the amount of reticulocytes 1 or 2 times a week after the initiation of NSAID treatment.
Derivatives of sulfonylureas: NSAIDs can enhance the hypoglycemic effect of sulfonylurea derivatives, reducing their binding to plasma proteins.

Combinations that need to be taken into account

Beta-blockers: NSAIDs can reduce the antihypertensive effect of beta-blockers due to inhibition of prostaglandin synthesis.

Cyclosporin and tacrolimus: NSAIDs may increase nephrotoxicity due to effects associated with kidney prostaglandins.
When combined, it is necessary to monitor kidney function.
Thrombolytics: the risk of bleeding increases.

Probenecid: the concentration of ketoprofen in the plasma may increase, which may be due to an inhibitory mechanism in the place of renal tubular secretion and glucuron conjugation and requires correction of the dose 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 ° C.
Shelf life - 3 years.
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