Piroxicam, capsules 10mg, 20pcs

Pharmacological action

of NSAIDs, has anti-inflammatory, analgesic, antiplatelet and antipyretic effects. Nonselectively suppresses COX-1 and COX-2. The analgesic effect manifests itself 30 minutes after oral use, the anti-inflammatory effect occurs by the end of 1 week of treatment. Pharmacokinetics: It is well absorbed by oral use and rectal use. Food slows down the rate of absorption, but does not affect the amount of absorption. Binding to plasma proteins is 99%. The plasma concentration is proportional to the dose, TCmax-3-5 hours. After a single dose of 20 mg, Cmax is 1.5-2 mcg / ml, after regular intake of 20 mg / day-3-8 mcg / ml. TCSs – 5-7 days. Penetrates into synovial fluid (40-50%), breast milk (1-3%). It is metabolized 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 isoenzyme CYP2C9. T1/2 is also involved in metabolism – 36-45 hours. One of the metabolites is saccharin. It is excreted in the form of 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; it does not affect the progression of the disease.

Contraindications

Hypersensitivity; peptic ulcer of the stomach and/or duodenum (including in the anamnesis), perforation or bleeding from the gastrointestinal tract (including in the anamnesis), gastritis, duodenitis, inflammatory bowel diseases (including ulcerative colitis, Crohn’s disease, diverticulitis), including in the anamnesis, malignant neoplasms of the gastrointestinal tract (including in the anamnesis); simultaneous use of other NSAIDs (including in the anamnesis). selective COX-2 inhibitors or ASA 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 and paranasal sinus polyposis and intolerance to ASA or other NSAIDs (including in the anamnesis) severe CRF (creatinine clearance less than 30 ml/min), progressive kidney disease, severe hepatic insufficiency or active liver disease, condition after CABG, severe CHF; hyperkalemia, blood clotting disorders (including hemophilia, prolongation of bleeding time, tendency to bleed, hemorrhagic diathesis); children (up to 14 years), age over 65 years, pregnancy, lactation; for rectal use (optional)-proctitis, anorectal bleeding. With caution. IHD, mild or moderate CHF, cerebrovascular diseases, dyslipidemia/hyperlipidemia, diabetes mellitus, peripheral arterial diseases, smoking, CRF (creatinine clearance 30-60 ml/min), presence of Helicobacter pylori infection, alcoholism, concomitant use of oral corticosteroids (including prednisone), antiplatelet agents (including ASA, clopidogrel), selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline).

Side effects

From the digestive system: abdominal pain and discomfort (including epigastrium), flatulence, nausea, constipation, diarrhea, peptic ulcer, gastrointestinal bleeding, 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. Sensory disorders: tinnitus, vertigo, deafness, blurred vision, eye irritation or swelling. Laboratory parameters: increased activity of “liver” enzymes (LDH, ALP, transaminases), increased urea nitrogen concentration, hypercreatininemia, decreased Hb and hematocrit, hypoproteinemia, thrombocytopenia, leukopenia, anemia (including aplastic and hemolytic), hyperglycemia, hypoglycemia, detection of antinuclear antibodies. From the cardiovascular system: increased blood pressure, tachycardia, palpitation, “flushes” of blood to the skin. From the skin: rash (including petechial), purpura, including thrombocytopenic, ecchymoses, pruritus, onycholysis, alopecia, photosensitization, exfoliative dermatitis, erythema multiforme, Lyell’s syndrome, Stevens-Johnson syndrome, vesiculobullous reactions. From the genitourinary system: edema, dysuria, frequent urination, hematuria, oliguria, menorrhagia. Respiratory system disorders: nosebleeds, shortness of breath. Others: chest pain, thirst, chills, excessive sweating, weight gain or loss.

Interaction

Antiplatelet agents, anticoagulants increase the risk of bleeding. Displaces others from the connection with blood proteins. Drugs (clinically significant for coumarin derivatives, sulfonamides and sulfonylureas, hydantoin derivatives). CORTICOSTEROIDS, selective serotonin reuptake inhibitors increase the risk of ulceration of the gastrointestinal mucosa. Concomitant use with other NSAIDs and ASA increases the toxicity of piroxicam. ASA (more than 3.9 g/day) reduces the concentration of piroxicam in the blood serum by 20%. In combination with anticoagulants, it reduces blood clotting (risk of bleeding). Methotrexate increases the hematotoxicity of piroxicam (fatal outcomes are possible). Cimetidine increases the AUC and Cmax of piroxicam by 13-15%. Reduces the diuretic effect of furosemide. Reduces renal clearance and increases the Css of Li+ preparations (requires monitoring of its concentration).

How to take, course of use and dosage

Inside, in / m, rectally, externally. Inside. For rheumatoid arthritis, osteoarthritis and ankylosing spondylitis-10-30 mg/day. in 1 session, for a long time. In acute diseases of skeletal muscles-40 mg/day. for 1 or several doses for 2 days, in the next 7-10 days-20 mg/day. In the treatment of acute gout, the initial dose is 40 mg, once, in the first 2 days, then for 4-6 days-40 mg 1 time or 20 mg 2 times a day. In dysalgomenorrhea, treatment should be initiated at the first onset of symptoms at an initial dose of 40 mg / day. in 1 or more sessions over 2 days. In the next 1-3 days-20 mg in 1 reception. As an antipyretic drug-10-20 mg/day; if it is necessary to quickly achieve the effect-in the first 2 days,40 mg/day is prescribed. with subsequent dose reduction. When juvenile rheumatoid arthritis is prescribed 1 time a day: children with a body weight of less than 15 kg-5 mg/day.,16-25 kg-10 mg/day.,26-45 kg-15 mg/day., more than 46 kg-20 mg/day. In/m. For the treatment of acute conditions or relief of exacerbation of the chronic process-20-40 mg once a day. After stopping the acute stage of the process, they switch to maintenance therapy with tablets or capsules. Rectally,10-40 mg 1-2 times a day. Externally, a gel or cream is applied to the affected areas (5-10 mm column) 3-4 times a day; an occlusive dressing is not applied.

Overdose

Symptoms: nausea, vomiting, abdominal pain, drowsiness, lethargy; gastrointestinal bleeding, increased blood pressure, acute renal failure, respiratory depression, coma. Treatment: symptomatic. There is no specific antidote. In case of a recent overdose, it is necessary to induce vomiting, take osmotic laxatives, activated charcoal (60-100 g for adults, children-1-2 g / kg). Repeated use of activated carbon (6 hours after ingestion) reduces piroxicam T1/2 by 50% and its bioavailability by 37%. Forced diuresis, urinary alkalinization, hemodialysis, and hemoperfusion are ineffective (high plasma protein binding).

Special instructions

Piroxicam should be prescribed by doctors experienced in the diagnosis and treatment of inflammatory and degenerative joint diseases. Concomitant use with misoprostol, proton pump inhibitors, and H2-histamine receptor blockers reduces gastrointestinal toxicity. NSAIDs, including piroxicam, can cause severe gastrointestinal side effects, including bleeding, ulceration and perforation of the stomach, small and large intestine (including fatal outcome). These phenomena can occur at any time of treatment and are not even accompanied by threatening symptoms. The risk of these events is especially high for piroxicam; it increases in the elderly. Taking 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 rash, ulceration of the mucous membranes or other signs of hypersensitivity occur, piroxicam is immediately discontinued. Piroxicam, like other NSAIDs, increases the risk of thrombotic complications (including myocardial infarction and stroke), and patients with risk factors should be prescribed these drugs with caution. Piroxicam, like other NSAIDs, can contribute to the development of arterial hypertension or worsen its course. In women, the contraceptive effect of IUD may decrease due to the effect of piroxicam on myometrial tone. During treatment, the use of ethanol should be excluded. During the treatment period, care should be taken when driving vehicles and doing other activities. potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.

Form of production

Capsules.

Active ingredient

Piroxicam

Conditions of release from pharmacies

By prescription

Dosage form

Capsules

Purpose

For adults, Children over 14 years of age, Children as prescribed by a doctor, Pregnant women in the first and second trimester as prescribed by a doctor, For adults as prescribed by a doctor

Indications

Bursitis, Periarthritis, Dislocations and Sprains, Arthrosis and Arthritis, Osteochondrosis, Rheumatoid Arthritis, Osteoarthritis, Gout, Sciatica, Bruises, Tendon Inflammation