Piroxicam-Acry - instructions for use, dose, side effects, contraindications

active substance: piroxicam in terms of 100% of the substance - 10 mg or 20 mg; Excipients: cellulose microcrystalline 74 mg or 73.3 mg, potato starch 14 mg or 44.6 mg, silicon dioxide colloid 0.5 mg or 0.7 mg, talc 1.5 mg or 1.4 mg. Capsule composition: titanium dioxide 0.94 mg or 1.5 mg, gelatin 46.06 mg or 73.5 mg.

Description:

Hard gelatin capsules of white color No. 3 (for a dosage of 10 mg) and No. 1 (for a dosage of 20 mg). The contents of the capsules are powder from white with a creamy to white with a yellowish hue of color.

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

ATX: & nbsp

M.02.A.A.07 Piroxicam

Pharmacodynamics:

Nonsteroidal anti-inflammatory drug, has anti-inflammatory, analgesic, antiplatelet and antipyretic effect. Neklektivno suppresses cyclooxygenase (COX) 1 and 2. Analgesic effect manifests itself 30 minutes after oral intake, anti-inflammatory effect occurs by the end of 1 week of treatment.

Pharmacokinetics:

Well absorbed when taken orally. The food slows the rate of absorption, but does not affect the amount of absorption. The connection with plasma proteins is 99%.

Concentration in plasma is proportional to the dose. The time to reach the maximum concentration is 3-5 hours. After a single dose of 20 mg, the maximum concentration is 1.5-2 μg / ml, after a regular intake of 20 mg / day - 3-8 μg / ml. The equilibrium concentration is reached after - 5-7 days.

It penetrates into the synovial fluid (40-50%) and into breast milk (1-3%). Metabolised in the liver by hydroxylation of the pyridine ring of the side chain, followed by conjugation with glucuronic acid and the formation of inactive metabolites. The isozyme CYP2C9 also participates in the metabolism. The half-life is 36-45 hours. One of the metabolites is saccharin. It is excreted as conjugates by the kidneys and to a lesser extent by the intestines. In unchanged form - 5%.

Indications:

Inflammatory and degenerative diseases of the musculoskeletal system: rheumatoid and acute gouty arthritis, ankylosing spondylitis, osteoarthritis.

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

Contraindications:

Hypersensitivity; stomach ulcer and / or duodenal ulcer (including in the anamnesis), perforation or bleeding from the gastrointestinal tract (including in the anamnesis), gastritis, duodenitis, inflammatory diseases of the intestine (in including ulcerative colitis, Crohn's disease, diverticulitis), incl. in the anamnesis, malignant neoplasms of the gastrointestinal tract (including in the anamnesis); simultaneous intake of other NSAIDs (including selective inhibitors of COX-2 or acetylsalicylic acid in analgesic doses), anticoagulants; severe allergic reactions in the anamnesis, especially skin forms (including erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis); complete or incomplete combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses, and intolerance to acetylsalicylic acid or other NSAIDs (incl.in the anamnesis); severe renal failure (creatinine clearance less than 30 ml / min), progressive kidney disease, severe hepatic insufficiency or active liver disease, condition after aortocoronary bypass grafting, severe chronic heart failure; hyperkalemia, blood clotting disorders (including hemophilia, lengthening bleeding time, propensity to bleed, hemorrhagic diathesis); children's age (up to 14 years), age over 65, pregnancy, lactation.

Carefully:

Coronary heart disease, chronic heart failure of mild or moderate degree, cerebrovascular disease, dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral arterial disease, smoking, creatinine clearance 30-60 ml / min, presence of Helicobacter pylori infection, alcoholism, simultaneous intake of oral glucocorticosteroids including prednisolone), antiaggregants (including acetylsalicylic acid, clopidogrel), selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline ).

Dosing and Administration:

Treatment usually begins with 10 mg / day, if necessary, increase the dose to 20 mg / day in one session. The maximum daily dose is 20 mg / day. The effectiveness and safety of treatment is assessed every 14 days.

Treatment is carried out as short a course in the minimum effective dose.

Side effects:

From the digestive system: pain and discomfort in the abdomen (including epigastrium), flatulence, nausea, constipation, diarrhea, peptic ulcer, bleeding from the digestive tract, anorexia, vomiting, dyspepsia, stomatitis, glossitis, pancreatitis, hepatitis.

From the central nervous system: dizziness, headache, increased appetite, sedation, drowsiness, amnesia, anxiety, depression, anxiety, hallucinations, insomnia, unusual dreams, nervousness, paresthesia, personality change, tremor, akathisia.

From the sense organs: tinnitus, vertigo, deafness, blurred vision, irritation or swelling of the eyes.

Laboratory indicators: increased activity of liver enzymes (lactate dehydrogenase, alkaline phosphatase, transaminases), increased urea nitrogen concentration, hypercreatininemia, decreased hemoglobin and hematocrit, hypoproteinemia, thrombocytopenia, leukopenia, anemia (incl.aplastic and hemolytic), hyperglycemia, hypoglycemia, detection of antinuclear antibodies.

From the side of the cardiovascular system: increased blood pressure, tachycardia, palpitations, "tides" of blood to the skin.

From the skin: rash (including petechial), purpura, incl. thrombocytopenic, ecchymosis, pruritus, onycholysis, alopecia, photosensitivity, exfoliative dermatitis, erythema multiforme, Lyell's syndrome, Stevens-Johnson syndrome, vesicular-bullous reactions.

From the genitourinary system: edema, dysuria, frequent urination, hematuria, oliguria, menorrhagia.

From the respiratory system: nosebleeds, shortness of breath.

Other: pain in the chest, thirst, chills, excessive sweating, increased or decreased body weight.

Overdose:

Symptoms: nausea, vomiting, abdominal pain, drowsiness, lethargy; bleeding from the gastrointestinal tract, increased blood pressure, acute renal failure, respiratory depression, coma.

Treatment: symptomatic. There is no specific antidote. With a recent overdose, it is necessary to induce vomiting, take osmotic laxatives, Activated carbon (60-100 g adults, children 1-2 g / kg). Multiple application of activated carbon (6 hours after administration) reduces the half-life of piroxicam by 50% and its bioavailability by 37%. Forced diuresis, alkalization of urine, hemodialysis and hemoperfusion are ineffective (high association with plasma proteins).

Interaction:

Antiaggregants, anticoagulants increase the risk of bleeding.

It displaces other drugs from the connection with blood proteins (it is clinically significant for coumarin derivatives, sulfonamides and sulfonylurea derivatives, hydantoin derivatives).

Glucocorticosteroids, selective serotonin reuptake inhibitors increase the risk of ulceration of the gastrointestinal mucosa.

Simultaneous reception with other NSAIDs and acetylsalicylic acid increases the toxicity of piroxicam.

Acetylsalicylic acid (more than 3.9 g / day) reduces the concentration of piroxicam in serum by 20%. In combination with anticoagulants reduces blood clotting (risk of bleeding).

Methotrexate increases the hematotoxicity of piroxicam (lethal outcomes are possible). Cimetidine increases the area of the concentration-time curve (AUC) and the maximum concentration of piroxicam by 13-15%.

Reduces the diuretic effect of furosemide.

Reduces renal clearance and increases the equilibrium concentration of lithium preparations (control of its concentration is required).

Special instructions:

Piroxicam should be prescribed by doctors with experience in the diagnosis and treatment of inflammatory and degenerative joint diseases.

Simultaneous reception with misoprostol, proton pump inhibitors, H2-histamine receptor blockers reduces gastrointestinal toxicity.

NSAIDs, including piroxicam, can cause severe side effects from the gastrointestinal tract, including bleeding, ulceration and perforation of the stomach, small and large intestine (including fatal). These phenomena can occur at any time of treatment and even not accompanied by threatening symptoms. The risk of these events is especially high for piroxicam; increases in the elderly.

The use of piroxicam significantly increases the risk of severe skin reactions (exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis), especially in the early stages of treatment. When the first signs of a rash, ulceration of the mucous membranes or other signs of hypersensitivity piroxicam immediately cancel.

Piroxicam, like other NSAIDs, increases the risk of thrombotic complications (including myocardial infarction and stroke), and patients with risk factors are prescribing these drugs with caution.

Piroxicam, like other NSAIDs, can contribute to the development of hypertension or worsen its course.

In women, the contraceptive effect of intrauterine contraceptives may be reduced because of the influence of piroxicam on myometrium tone.

During treatment should be excluded from the use of ethanol.

Effect on the ability to drive transp. cf. and fur:

During the period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities requiring increased attention and speed of psychomotor reactions.

Form release / dosage:

Capsules 10 mg and 20 mg.

Packaging:10 capsules in a planar cell package. 2 contour mesh packages together with instructions for use in a pack of cardboard.

Storage conditions:

In a dry, the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:4 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:P N003126 / 01

Date of registration:08.12.2008

The owner of the registration certificate:AKRIKHIN HFK, JSC AKRIKHIN HFK, JSC Russia

Manufacturer: & nbsp

AKRIKHIN HFK, JSC Russia

Information update date: & nbsp15.10.2015

Illustrated instructions

Instructions

Piroxicam-Acry® (Piroxicamum-Akri®)