Piroxicam

General characteristics. Structure:

Active ingredient: 10 mg or 20 mg of piroxicam in 1 capsule.

Excipients: cellulose powder, sodium carboxymethyl-starch (sodium of starch glikolit), potato starch, sodium lauryl sulfate, magnesium stearate, gelatin, titanium dioxide or gelatin, titanium dioxide, dye blue patent.

Has antiinflammatory, analgeziruyushchy and febrifugal effect. It is applied at rheumatic diseases, a pain syndrome and joint syndrome.

Pharmacological properties:

Pharmacodynamics. Non-steroidal anti-inflammatory drug, renders antiinflammatory, analgeziruyushchy, antiagregantny and febrifugal action. Not selectively suppresses cyclooxygenase-1 (TsOG1) and cyclooxygenase-2 (TsOG2). The analgetic effect is shown in 30 min. after oral administration, the antiinflammatory effect occurs by the end of 1 week of treatment. After a single dose action remains within 24 hours.

Pharmacokinetics. It is well soaked up at intake. Food slows down absorption speed, but does not influence absorption volume. Bioavailability - 100%. Communication with proteins of plasma - 97%.

Concentration in plasma is proportional to the used dose, time of achievement of the maximum concentration of drug in plasma (TCmax) - 3-5 h. After a single dose of 20 mg the maximum concentration of piroxicam in plasma (Cmax) - 1.5-2 mkg/ml, after regular reception of 20 mg/days - 3-8 mkg/ml. TCss - 7-12 days.

Gets into synovial fluid (40-50%), it is allocated with breast milk - 1-3%.

It is metabolized in a liver by a hydroxylation of a pyridinic ring of a side chain with the subsequent conjugation with glucuronic acid and formation of inactive metabolites. CYP2C9 isoenzyme also takes part in metabolism. An elimination half-life (T1/2) - 24-50 h. It is removed in the form of conjugates by kidneys and to a lesser extent - through intestines. In not changed look - 5%.

Indications to use:

Inflammatory and degenerative diseases of a musculoskeletal system: the rhematoid and gouty arthritis ankylosing a spondylarthritis (Bekhterev's disease), an osteoarthrosis.

Pain syndrome: a sciatica, a tendovaginitis, a bursitis, an arthralgia, neuralgia, a mialgiya, radiculitis, the posttraumatic and postoperative pain syndrome which is followed by an inflammation, альгодисменорея.

It is intended for symptomatic therapy, reduction of pain and an inflammation at the time of use, does not influence progressing of a disease.

Route of administration and doses:

Inside. At a pseudorheumatism, an osteoarthrosis and Bekhterev's disease - on 10-30 mg/days in 1 reception, for a long time.

At acute diseases of skeletal muscles - on 40 mg/days for one or several receptions within 2 days, in the next 7-10 days - on 20 mg/days.

At treatment of an attack of gout an initial dose - 40 mg, once, in the first 2 days, then for 4-6 days - 40 mg of 1 times or on 20 mg 2 times a day.

At algodismenory treatment it is necessary to begin at emergence of the first symptoms in an initial dose 40 mg/days in 1 or several receptions a current of 2 days. In the next 1-3 days - on 20 mg in 1 reception.

At a juvenile pseudorheumatism appoint 1 time a day: to children 14 years with a body weight more than 46 kg - 20 mg/days are more senior.

Features of use:

To patients with dysfunctions of digestive tract, after extensive surgical interventions, at advanced age, the patient with bronchial asthma or with chronic obstructive diseases of lungs in the anamnesis it is necessary to control a hemoglobin content in blood (risk of development of bleedings), function of kidneys and a liver.

At women decrease in contraceptive effect of VMK because of influence of piroxicam on a myometrium tone is possible.

Recommendations about use for children are not developed now.

During treatment it is necessary to exclude the ethanol use.

During treatment it is necessary to be careful during the driving of motor transport and occupation other potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

For decrease in risk of development of the undesirable phenomena from digestive tract it is necessary to use a minimal effective dose minimum possible short course.

Side effects:

From a nervous system: dizziness, headache, drowsiness, sleeplessness, depression, irritability, hallucinations, paresthesias, block, change of mood.

From an urinary system: renal failure, intersticial nephrite, papillary necrosis, nephrotic syndrome.

From the alimentary system: nausea, loss of appetite, abdominal pain, meteorism, locks or diarrhea, digestive tract erosive cankers, bleeding and perforation of digestive tract; abnormal liver functions, increase in activity of "hepatic" transaminases; dryness in a mouth, stomatitis.

From bodies of a hemopoiesis and system of a hemostasis: anemia, aplastic anemia, hemolitic anemia, leukopenia, eosinophilia, thrombocytopenia, decrease in level of a hematocrit; hemorrhagic vasculitis (Shenleyna-Genokh's disease).

From cardiovascular system: increase in the ABP, decrease in the ABP, is rare - heartbeat, an asthma.

Others: hypostases of shins and feet, the increased sweating, increase in concentration of urea; hypoglycemia.

Allergic reactions: skin rash, itch, face edemas, throats, bronchospasm, malignant exudative erythema (Stephens-Johnson's syndrome), shock, photosensitization; vasculitis, serum disease.

Interaction with other medicines:

Piroxicam forces out other medicines from communication with blood proteins. Carefully it is necessary to appoint with the drugs which are strongly contacting proteins of a blood plasma (perhaps competitive oppression of binding of other drugs).

With care appoint drug along with indirect anticoagulants since strengthening of anticoagulative action is possible. Anticoagulants increase risk of bleedings.

Against the background of other non-steroidal anti-inflammatory drugs and corticosteroids the risk of ulcerogenic action (danger of gastrointestinal bleeding) increases, the risk of development of allergic reactions and side effects from digestive tract increases, acetylsalicylic acid reduces piroxicam level in a blood plasma to 80%.

Piroxicam increases risk of a hyperpotassemia at a combination to kaliysberegayushchy diuretics and other kaliysoderzhashchy drugs.

At simultaneous use of Piroxicam with Cimetidinum, probenetsidy and Sulfinpyrazonum concentration of piroxicam in blood increases.

At simultaneous use of piroxicam with drugs of lithium increase in content of lithium in blood serum is possible.

Phenobarbital can reduce concentration of piroxicam in a blood plasma.

Piroxicam increases concentration of Phenytoinum.

Piroxicam lowers efficiency of antihypertensives, diuretics (in connection with a delay of liquid, ions of sodium and potassium).

At use of piroxicam for 24 h to or after reception of a methotrexate concentration of the last in blood serum increases and its toxicity increases.

At simultaneous use of piroxicam with sulfonamides, Acidum nalidixicum, peroral hypoglycemic drugs, triiodothyronine, cyclophosphamide increase in their concentration in a blood plasma is possible.

Myelotoxic medicines strengthen manifestations of a gematotoksichnost of drug.

Contraindications:

Hypersensitivity, digestive tract erosive cankers (in an aggravation stage); a full or incomplete combination of bronchial asthma, the nose recuring a polypose and okolonosovy bosoms and intolerance of acetylsalicylic acid or other NPVP (including in the anamnesis); a heavy renal failure (the clearance of creatinine (CC) less than 30 ml/min.), active gastrointestinal bleeding, inflammatory diseases of digestive tract, the progressing diseases of kidneys, a heavy liver failure or an active disease of a liver, a state after performing the aortocoronary shunting (AS); the confirmed hyperpotassemia, disturbances of coagulability of blood (including hemophilia, lengthening of a bleeding time, tendency to bleedings, hemorrhagic diathesis); children's age (up to 14 years), pregnancy, the lactation period.

With care: chronic heart failure, coronary heart disease, cerebrovascular diseases, дислипидемия / a lipidemia, a diabetes mellitus, diseases of peripheral arteries, smoking, clearance of KK creatinine less than 60 ml/min., digestive tract cankers in the anamnesis, existence of an infection of N. of pylori, long use of non-steroidal anti-inflammatory drugs, alcoholism, heavy somatopathies, age is more senior than 65 years, a concomitant use of peroral glucocorticoids (including Prednisolonum), anticoagulants (including warfarin), antiagregant (including acetylsalicylic acid, клопидогреля), selective serotonin reuptake inhibitors (including a tsitaloprama, fluoxetine, a paroksetin, sertraline).

Overdose:

Symptoms: heartburn, dyspepsia, nausea, vomiting, drowsiness.

Treatment: a gastric lavage, absorbent carbon – 0,5 g/kg. The hemodialysis does not cause decrease in concentration of piroxicam in a blood plasma, because of high extent of its linkng with proteins.

Storage conditions:

List B. To store in the dry, protected from light place, at a temperature not above 25 °C. To store in the place, unavailable to children! A period of validity - 3 years. Not to use after the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Capsules of 10 mg, 20 mg. On 10 or 20 capsules in a blister strip packaging from a film of the polyvinyl chloride and printing aluminum foil varnished. On 1, 2, 3, 10 or 20 blister strip packagings together with the application instruction place in a pack from a cardboard.