Artrum - instructions for use, dose, side effects, contraindications

kollidone SR (polyvinyl acetate 80%, povidone 19%, 30 mg sodium lauryl sulfate 0.8%, silicon dioxide 0.2%) lactose monohydrate (sugar milk) - 59.2 mg.

Weight of the tablet: 300 mg.

Description:Round, biconvex tablets are white or almost white, marble is allowed.

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

ATX: & nbsp

M.02.A.A.10 Ketoprofen

Pharmacodynamics:Ketoprofen is a non-steroidal anti-inflammatory drug (NSAID). Has anti-inflammatory, analgesic and antipyretic effect. Ketoprofen blocks the action of the enzyme cyclooxygenase 1 and 2 (COX₁ and COX₂) and, in part, lipoxygenase, which leads to suppression of the synthesis of prostaglandins (including in the central nervous system, most likely in the hypothalamus).

Stabilizes in vitro and in vivo liposomal membranes, at high concentrations in vitro ketoprofen inhibits the synthesis of bradykinin and leukotrienes.

Ketoprofen does not adversely affect the condition of the articular cartilage.

Pharmacokinetics:Absorption

Ketoprofen is easily absorbed from the gastrointestinal tract, bioavailability is 90%. Connection with blood plasma proteins - 99%. When administered 150 mg of ketoprofen, the maximum plasma concentrations of the drug (10.4 μg / ml) are reached after 4-6 hours.

Distribution

Ketoprofen is 99% bound to blood plasma proteins, mainly with the albumin fraction. The volume of distribution is 0.1 l / kg.

Ketoprofen penetrates into the synovial fluid and reaches there a concentration equal to 30% of the concentration in the blood plasma. Plasma clearance of ketoprofen is approximately 0.08 l / kg / h. Effective concentrations of ketoprofen are determined in the blood even after 24 hours after its administration.

Metabolism and excretion

Ketoprofen undergoes intensive metabolism under the action of microsomal liver enzymes, the half-life is less than 2 hours. Ketoprofen binds to glucuronic acid and is excreted from the body in the form of glucuronide. There are no active metabolites of ketoprofen.Up to 80% of ketoprofen is excreted by the kidneys within 24 hours, mainly in the form of ketoprofen glucuronide.

When using the drug in a dosage of 100 mg or more, excretion by the kidneys can be difficult. Patients with severe renal insufficiency most of the drug is secreted through the intestine.

When taking high doses, the liver clearance also increases. Up to 40% of the drug is excreted through the intestine.

Patients with hepatic insufficiency the plasma concentration of ketoprofen is doubled (probably due to hypoalbuminemia and, as a result, a high level of unbound active ketoprofen); such patients need to prescribe the drug in the minimum therapeutic dose.

Patients with renal insufficiency clearance of ketoprofen is reduced, but correction of doses is required only in the case of severe renal failure.

Patients old age metabolism and excretion of ketoprofen proceed more slowly, which is of clinical importance only for patients with severe renal insufficiency.

Indications:

Symptomatic therapy of painful and inflammatory processes of various origin, including:

- inflammatory and degenerative diseases of the musculoskeletal system:

- rheumatoid arthritis;

- seronegative arthritis: ankylosing spondylitis (Bechterew's disease), psoriatic arthritis, reactive arthritis (Reiter's syndrome);

- gout, pseudogout;

- osteoarthritis;

- tendonitis, bursitis, myalgia, neuralgia, sciatica;

- pain syndrome, including mild, moderate and severe:

- post-traumatic and postoperative pain syndrome;

- pain syndrome with oncological diseases, etc.

Contraindications:

- Hypersensitivity to ketoprofen or other components of the drug, as well as salicylates or other NSAIDs;

- bronchial asthma, bronchospasm, rhinitis or urticaria in history caused by the use of acetylsalicylic acid or other NSAIDs;

- ulcerative colitis, Crohn's disease; hemophilia and other bleeding disorders;

- children's age (up to 15 years);

- severe hepatic impairment;

- severe renal failure (creatinine clearance less than 30 ml / min);

- Decompensated heart failure; Postoperative period after coronary artery bypass grafting;

- peptic ulcer of the stomach or duodenum in the stage of exacerbation;

- gastrointestinal, cerebrovascular and other bleeding (or suspicion of bleeding);

- chronic dyspepsia;

- III trimester of pregnancy;

- the period of breastfeeding.

Carefully:- Bronchial asthma in history;

- clinically expressed cardiovascular, cerebrovascular diseases and diseases of peripheral arteries;

- chronic heart failure;

- arterial hypertension;

- blood diseases;

- dyslipidemia;

- progressive liver disease;

- liver failure;

- hyperbilirubinemia;

- alcoholic cirrhosis of the liver;

- renal failure (creatinine clearance 30-60 ml / min);

- elderly age;

- dehydration;

- diabetes;

- anamnestic data on the development of ulcerative lesions of the gastrointestinal tract;

- infection Helicobacter pylori;

- smoking;

- concomitant therapy with anticoagulants (eg, warfarin), antiplatelet agents (for example, acetylsalicylic acid), glucocorticosteroids for oral administration (for example, prednisolone), selective serotonin reuptake inhibitors (eg, citalopram, sertraline), prolonged use of NSAIDs.

Pregnancy and lactation:Inhibition of prostaglandin synthesis may have an adverse effect on the course of pregnancy and / or on embryonic development. Data from epidemiological studies using prostaglandin synthesis inhibitors in early pregnancy confirm the increased risk of spontaneous abortion and heart disease (~ 1 - 1.5%).

Applying the drug to pregnant women in the I and II trimesters of pregnancy is only possible if the intended benefit to the mother exceeds the possible risk to the fetus.

Contraindicated in the use of ketoprofen in pregnant women during the third trimester of pregnancy because of the possibility of developing weakness in the uterine labor activity and / or premature closure of the arterial duct, a possible increase in bleeding time, lack of hydration and kidney failure.

To date, there is no data on the release of ketoprofen in breast milk, so if you need to use ketoprofen in a nursing mother, you should decide whether to stop breastfeeding.

Dosing and Administration:

Inside, the tablet is swallowed whole during or after a meal, washed down with water or milk (the volume of the liquid must be at least 100 ml).

The drug is prescribed for 1 tablet (150 mg) 1 time per day.

The maximum dose of ketoprofen is 200 mg / day.

Side effects:

According to the World Health Organization (WHO), undesirable effects are classified according to their frequency of development as follows:

- very often (≥ 1/10),

- often (≥ 100, <1/10),

- infrequently (≥ 1/1000, <1/100),

- rarely (≥ 1/10000, <1/1000),

- very rarely (<1/10000),

- frequency is unknown (the frequency of occurrence of phenomena can not be determined on the basis of available data).

Disturbances from the hematopoiesis and lymphatic system:

rarely: hemorrhagic anemia:

frequency is unknown: agranulocytosis, thrombocytopenia, impaired bone marrow function.

Immune system disorders:

frequency is unknown: anaphylactic reactions (including anaphylactic shock).

Disturbances from the nervous system:

infrequently: headache, dizziness, drowsiness;

rarely: paresthesia;

frequency is unknown: convulsions, a violation of taste.

Disorders of the psyche:

frequency is unknown: emotional lability.

Impaired sensory organs:

rarely: blurred vision, tinnitus.

Disorders from the cardiovascular system:

frequency is unknown: heart failure, increased blood pressure, vasodilation.

Disturbances from the respiratory system:

rarely: exacerbation of bronchial asthma;

frequency is unknown: bronchospasm (especially in patients with hypersensitivity to NSAIDs), rhinitis.

Disorders from the gastrointestinal tract:

often: nausea, vomiting, indigestion, pain in the abdomen;

infrequently: constipation, diarrhea, bloating, gastritis;

rarely: peptic ulcer, stomatitis;

rarely: exacerbation of ulcerative colitis or Crohn's disease, gastrointestinal bleeding, perforation.

Disorders from the liver and bile ducts:

rarely: hepatitis, increased activity of "hepatic" transaminases, increased bilirubin concentration.

Disturbances from the skin and subcutaneous tissues:

infrequently: skin rash, itchy skin;

frequency is unknown: photosensitivity, alopecia, urticaria, angioedema, erythema, bullous rash,including Stevens-Johnson syndrome, toxic epidermal necrolysis.

Disorders from the kidneys and urinary tract:

frequency is unknown: acute renal failure, interstitial nephritis, nephritic syndrome, nephrotic syndrome, abnormal values of renal function indicators.

Other:

infrequently: edema;

rarely: increase in body weight;

frequency is unknown: increased fatigue.

Overdose:As with other NSAIDs, with ketoprofen overdose, nausea, vomiting, abdominal pain, vomiting with blood, melena, impaired consciousness, respiratory depression, seizures, impaired renal function, and kidney failure may occur.

In case of overdosage, gastric lavage and the use of activated charcoal are indicated. Treatment is symptomatic; the effect of ketoprofen on the gastrointestinal tract can be weakened with the help of drugs that reduce the secretion of the gland of the stomach (for example, proton pump inhibitors or H blockers2histamine receptors) and prostaglandins.

Interaction:

Ketoprofen can weaken the action diuretics and antihypertensive drugs and strengthen action hypoglycemic drugs for oral administration and some anticonvulsants (phenytoin).

Joint application with other NSAIDs, salicylates, glucocorticosteroids, ethanol increases the risk of developing adverse events from the gastrointestinal tract.

Simultaneous application with anticoagulants (heparin, warfarin), thrombolytic agents, antiplatelet agents (ticlopidine, clopidogrel), pentoxifylline increases the risk of bleeding.

Simultaneous application with katia salts, potassium-sparing diuretics, angiotensin-converting enzyme inhibitors, NSAIDs, low molecular weight heparins, cyclosporin, tacrolimus and trimethoprim increases the risk of hyperkalemia.

Increases the concentration in the blood plasma cardiac glycosides, blockers of "slow" calcium channels, lithium preparations, cyclosporine, methotrexate and digoxin. Increases toxicity methotrexate and nephrotoxicity cyclosporine. Simultaneous application with probenecid significantly reduces the clearance of ketoprofen in the blood plasma.

Combination with glucocorticosteroids and others NSAIDs (including selective inhibitors of COX2) increases the likelihood of side effects (in particular, from the gastrointestinal tract).

NSAIDs may decrease effectiveness mifepristone. Admission of NSAIDs should be started no earlier than 8-12 days after the withdrawal of mifepristone.

Special instructions:Do not combine ketoprofen with other NSAIDs and / or COX inhibitors₂.

With prolonged use of NSAIDs, it is necessary to periodically evaluate the clinical analysis of blood, monitor kidney and liver function, especially in elderly patients (over 65 years of age), and conduct occult blood feces analysis.

It is necessary to be careful and more often to control blood pressure when using ketoprofen for the treatment of patients with arterial hypertension, cardiovascular diseases that lead to fluid retention in the body.

If abnormalities occur on the part of the visual organs, treatment should be stopped immediately.

Like other NSAIDs. ketoprofen can mask the symptoms of infectious and inflammatory diseases. In case of signs of infection or deterioration of well-being on the background of the use of the drug, it is necessary to immediately turn tothe doctor.

If there is a history of contraindications from the gastrointestinal tract (bleeding, perforation, peptic ulcer disease), prolonged therapy and high doses of ketoprofen, the patient should be under close medical supervision.

Because of the important role of prostaglandins in maintaining renal blood flow, caution should be exercised when using ketoprofen in patients with cardiac or renal insufficiency, as well as in the treatment of elderly patients taking diuretics and patients who, for whatever reason, blood.

The drug should be discontinued before a large surgical intervention.

The use of ketoprofen can affect women's fertility, so patients with infertility (including undergoing examination) are not recommended to use the drug.

Effect on the ability to drive transp. cf. and fur:Data on the negative effect of the drug Artrum in the recommended doses on the ability to drive or work with mechanisms there. At the same time, patients who are drowsy when the drug is used,dizziness or other unpleasant sensations on the part of the nervous system, including visual impairment, should refrain from controlling vehicles, mechanisms.

Form release / dosage:Long-acting tablets 150 mg.

Packaging:10 tablets in a contour mesh box made of a polyvinylchloride film and aluminum foil.

20 tablets in cans of orange glass type BTS, sealed with plastic pull-on lids with sealing element.

20 tablets in cans of polymer type BP.

Each bank or 1, 2, 3 contour mesh packages together with the instruction for use are placed in a pack of cardboard.

Storage conditions:In dry, dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-000610

Date of registration:21.09.2011 / 13.10.2016

Expiration Date:Unlimited

The owner of the registration certificate:BIOSINTEZ, PAO BIOSINTEZ, PAO Russia

Manufacturer: & nbsp

BIOSINTEZ, PAO Russia

Information update date: & nbsp09.10.2017

Illustrated instructions

Instructions

Artrum (Artrum)