Artoxan ampoules 20mg №3

International non-proprietary name:

tenoxicam

Dosage Form:

lyophilisate for preparation of solution for intravenous and intramuscular administration.

Each bottle of the drug contains:

Active substance: tenoxicam - 20 mg.

Excipients: mannitol - 80.00 mg, Ascorbic acid - 0.400 mg, disodium edetate - 0.20 mg, trometamol - 3.30 mg, sodium hydroxide and hydrochloric acid - q.s.

Each ampule of solvent contains: water for injection - 2 ml.

Description:

Lyophilized powder or compacted mass in the form of tablets-green-yellow color, solvent: a colorless, transparent, odorless liquid.

Pharmacotherapeutic group:

nonsteroidal anti-inflammatory drug.

Pharmacological properties

Pharmacodynamics

Tenoxia, which is a thienothiazine oxycam derivative, is a nonsteroidal anti-inflammatory drug (NSAID). In addition to anti-inflammatory, analgesic and antipyretic effects, the drug also inhibits platelet aggregation. The basis of the mechanism of action is the inhibition of the activity of isoenzymes of cyclooxygenase-1 and cyclooxygenase-2, as a result of which the synthesis of prostaglandins in the focus of inflammation is reduced, as well as in other tissues of the body.In addition, tenoxicam reduces the accumulation of leukocytes in the focus of inflammation, reduces the activity of proteoglycanase and collagenase in human cartilage.

Anti-inflammatory effect develops by the end of the first week of therapy.

Pharmacokinetics

Suction.

Absorption is fast and complete. Bioavailability is 100%.

Distribution.

The maximum concentration in a blood plasma is noted in 2 hours. The distinctive ability of tenoxicam is a long duration of action and a long half-life of 72 hours. The drug is 99% bound to plasma proteins. Tenoxam well penetrates the synovial fluid. Easily penetrates histohematogenous barriers.

Metabolism.

Metabolized in the liver by hydroxylation to form 5-hydroxypyridyl.

Inference.

1/3 is excreted through the intestine with bile, 2/3 is excreted by the kidneys in the form of inactive metabolites.

Indications for use

- rheumatoid arthritis;

- osteoarthritis;

- ankylosing spondylitis;

- articular syndrome in acute exacerbation of gout;

- bursitis;

- tendovaginitis;

- pain syndrome (low and medium intensity): arthralgia, myalgia, neuralgia, migraine, toothache and headache, algomenorrhea;

- pain with injuries, burns;

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

Contraindications

- hypersensitivity to the active substance or auxiliary components of the drug.There is a possibility of cross-sensitivity to Acetylsalicylic acid, Ibuprofen and other NSAIDs;

- erosive and ulcerative lesions of the stomach and duodenum in the acute stage;

- Gastrointestinal bleeding (including a history);

- inflammatory bowel disease: Crohn's disease or ulcerative colitis in the acute stage;

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

- progressive kidney disease;

- severe liver failure;

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

- The established diagnosis of diseases of the blood coagulation system;

- decompensated heart failure;

- therapy of perioperative pain during coronary artery bypass surgery;

- pregnancy, breastfeeding period;

- age up to 18 years.

Carefully

Peptic ulcer and duodenal ulcer, ulcerative colitis and Crohn's disease without exacerbation, history of liver disease, hepatic porphyria, chronic renal failure (creatinine clearance 30-60 ml / min), chronic heart failure, hypertension, a significant decrease in circulating blood volume ( including after surgery), elderly patients (over 65) (includingreceiving diuretics, weakened and underweight patients), bronchial asthma, coronary heart disease, cerebrovascular diseases, dyslipidemia / hyperlipedia, diabetes, peripheral artery disease, smoking, infection Helicobacter pylori, prolonged use of NSAIDs, alcoholism, severe somatic diseases, autoimmune diseases (systemic lupus erythematosus (SLE) and mixed connective tissue disease), simultaneous administration of glucocorticosteroids (including prednisolone), anticoagulants (including warfarin), antiplatelet agents (including acetylsalicylic acid, clopidogrel), selective serotinin reuptake inhibitors (including citalopram, Fluoxetine, paroxetine, sertraline).

Pregnancy and breastfeeding

The use of the drug during pregnancy and during breastfeeding is contraindicated.

Dosage and administration

For intramuscular or intravenous administration.

Intramuscular or intravenous administration is used for short-term (1-2 days) treatment at a dose of 20 mg 1 time per day. If necessary, further therapy is transferred to the oral dosage forms of tenoxicam.

The solution for injection is prepared immediately before use by dissolving the contents of the vial with the attached solvent. After preparation, the needle is replaced. Intramuscular injections do deep.The duration of intravenous administration should not be less than 15 seconds.

Side effect

The frequency of side effects is classified according to the recommendations of the World Health Organization: very often (> 1/10); often (from> 1/100, <1/10); infrequently (> 1/1000, <1/100); rarely (> 1/10000, <1/1000); very rarely (<1/10000), not established.

From the digestive system: very often - dyspepsia (nausea, vomiting, heartburn, diarrhea, flatulence), NSAIDs, gastropathy, abdominal pain, stomatitis, anorexia, abnormal liver function; rarely, ulceration of the mucous membrane of the gastrointestinal tract, bleeding (gastrointestinal, uterine, hemorrhoidal), perforation of the intestinal walls.

Cardiovascular: rarely - heart failure, tachycardia, high blood pressure.

From the side of the central nervous system: often - dizziness, headache, drowsiness, depression, agitation, hearing loss, tinnitus, eye irritation, blurred vision.

Violations of the skin and subcutaneous tissue: often - pruritus, rash, urticaria and erythema; very rarely - photodermatitis, Stephen-sa-Johnson syndrome, Lyell's syndrome.

Violations of the urinary system: Often - an increase in the content of urea nitrogen and creatinine in the blood.

From the side of blood formation organs: often - agranulocytosis, leukopenia, rarely - anemia, thrombocytopenia, leukopenia, pancytopenia.

Disorders of the hepatobiliary system: often - increased activity of ALT, AST, gamma-GT and serum bilirubin level.

Laboratory values: hypercreatininemia, hyperbilirubinemia, increased urea nitrogen concentration and liver transaminase activity, prolongation of bleeding time.

On the background of treatment, mental disorders and metabolic disorders can be observed.

Overdosage

Symptoms (with a single injection): abdominal pain, nausea, vomiting, erosive and ulcerative lesions of the gastrointestinal tract, impaired renal function and liver, metabolic acidosis.

Treatment: symptomatic (maintenance of vital body functions). Hemodialysis is ineffective.

Interaction with other drugs

Tenoksikam has a high degree of binding to albumin and can, like all NSAIDs, enhance the anticoagulant effect of Warfarin and other anticoagulants. It is recommended to monitor blood parameters when used together with anticoagulants and hypoglycemic preparations for oral administration, especially in the initial stages of Artok-San.

No possible interaction with Digoxin was noted.

As with the use of other NSAIDs, it is recommended to use the drug along with cyclosporine with caution due to the increased risk of nephrotoxicity.

Combined use with quinolones may increase the risk of seizures.

Salicylates can displace tenoxicam from association with albumin and, accordingly, increase clearance and distribution of the drug.It is necessary to avoid the simultaneous use of salicylates or two or more NSAIDs (increased risk of complications from the gastrointestinal tract).

There is evidence that NSAIDs reduce the excretion of lithium. In this regard, patients receiving therapy with lithium, should often control the concentration of lithium in the blood.

NSAIDs can cause sodium, potassium and fluid retention in the body, causing the action of natriuretic diuretics. This must be remembered when used together with such diuretics in patients with CHF and arterial hypertension.

With caution is recommended to use NSAIDs with Methotrexate, NSAIDs reduce the excretion of methotrexate and may increase its toxicity.

NSAIDs should not be used within 8-12 hours after applying mifepristone, as may reduce its effect.

It is necessary to take into account the increased risk of gastrointestinal bleeding when used together with corticosteroids.

Reduces the effectiveness of uricosuric drugs, enhances the effect of anticoagulants, fibrinolytics, side effects of mineralocorticosteroids and glucocorticosteroids, estrogens; reduces the effectiveness of antihypertensive drugs and diuretics.

Inductors of microsomal oxidation in the liver (phenytoin, ethanol, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants) increase the production of hydroxylated active metabolites.

Combined use with antiplatelet agents and selective serotonin reuptake inhibitors increases the risk of gastrointestinal bleeding.

Cardiac glycosides when taken in conjunction with NSAIDs can enhance heart failure, reduce the glomerular filtration rate and increase the plasma level of cardiac glycosides.

No interaction was found with the use of tenoxicam with cimetidine.
No clinically significant interaction was found with treatment with tenoxicam and penicillamine or parenteral gold.

The risk of nephrotoxicity increases with the combined use of NSAIDs with tacrolimus.

The risk of hematologic toxicity increases with the use of NSAIDs with zidovudine.

special instructions

During treatment, it is necessary to control the picture of peripheral blood and the functional state of the liver and kidneys, the prothrombin index (against the background of taking indirect anticoagulants), the concentration of glucose in the blood (against the background of hypoglycemic agents).

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

There may be an increase in bleeding time, which should be considered during surgical interventions.

It is necessary to consider the possibility of sodium and water retention in the body when prescribing with diuretics in patients with arterial hypertension and heart failure.

Patients with uncontrolled arterial hypertension, chronic heart failure, peripheral arterial disease, confirmed IHD and / or cerebrovascular diseases should take the drug under medical supervision.

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