Description
Release form
Capsules.
Packing
20 pcs.
Pharmacological action
Pharmaceutical group: NSAIDs.
Pharmaceutical action: NSAIDs, has anti-inflammatory, analgesic, antiplatelet and antipyretic effects. Non-selectively suppresses COX-1 and COX-2.
The analgesic effect is manifested 30 minutes after oral administration, the anti-inflammatory effect occurs at the end of 1 week of treatment.
Pharmacokinetics: Absorbed well by ingestion and rectal administration. Food slows down the rate of absorption, but does not affect the amount of absorption. Communication with plasma proteins – 99%.
Plasma concentration is proportional to dose, TCmax – 3-5 hours. After a single dose of 20 mg Cmax – 1.5-2 μg / ml, after regular intake of 20 mg / day – 3-8 μg / ml. TCss – 5-7 days.
Penetrates into synovial fluid (40-50%), into breast milk (1-3%).
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 metabolism of CYP2C9 isoenzyme is also involved. T1 / 2 – 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. Unchanged – 5%.
Contraindications
Hypersensitivity peptic ulcer and / or duodenal ulcer (including history), perforation or bleeding from the gastrointestinal tract (including history), gastritis, duodenitis, inflammatory bowel disease (including including ulcerative colitis, Crohn ² ¢s disease, diverticulitis), including in the anamnesis, malignant neoplasms of the gastrointestinal tract (including in the anamnesis) simultaneous administration of other NSAIDs (including selective COX-2 or ASA inhibitors in analgesic doses),
anticoagulants, severe allergic reactions in the anamnesis, especially skin forms (including including erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis) a complete or incomplete combination of bronchial asthma, recurring polyposis of the nose and paranasal sinuses and intolerance to ASA or other NSAIDs (including a history of)
severe CRF (CC less than 30 ml / min), progressive disease kidney disease, severe liver failure or active liver disease, condition after CABG, severe heart failure, hyperkalemia, bleeding disorders (including hemophilia, prolonged bleeding time, tendency to bleeding, hemorrhagic diathesis)
children’s age (up to 14 years), age over 65 years, pregnancy, lactation period
for rectal administration (optional) – proctitis, anorectal bleeding.
Caution. IHD, CHF of mild or moderate degree, cerebrovascular disease, dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral arterial disease, smoking, chronic renal failure (CC 30-60 ml / min), the presence of Helicobacter pulori infection, alcoholism, simultaneous administration of oral corticosteroids including prednisone), antiplatelet agents (including ASA, clopidogrel), selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline).
Special instructions
Pyroxicam should be prescribed by doctors who are experienced in the diagnosis and treatment of inflammatory and degenerative joint diseases.
Concomitant use 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 intestines (including fatal ones). These phenomena can occur at any time of treatment and not even be accompanied by threatening symptoms. The risk of these phenomena is especially high for piroxicam 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 a rash, ulceration of the mucous membranes or other signs of hypersensitivity occur, piroxicam is immediately canceled.
Piroxicam, like other NSAIDs, increases the risk of thrombotic complications (including myocardial infarction and stroke), patients with risk factors, these drugs are prescribed with caution.
Piroxicam, like other NSAIDs, can contribute to the occurrence of arterial hypertension or worsen its course.
In women, the contraceptive effect of IUDs may be reduced due to the effect of piroxicam on myometrial tone.
Ethanol use should be excluded during treatment.
During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require an increased concentration of attention and speed of psychomotor reactions.
Side effects of the
Digestive system: pain and discomfort in the abdomen (including epigastrium), flatulence, nausea, constipation, diarrhea, peptic ulcer, gastrointestinal bleeding, anorexia, vomiting, dyspepsia, stomatitis, glossitis, glossitis, glossitis, hepatitis.
From the side of the central nervous system: dizziness, headache, increased appetite, sedation, drowsiness, amnesia, anxiety, depression, anxiety, hallucinations, insomnia, unusual dreams, nervousness, paresthesia, personality change, tremor, akathisia.
co anorexia, vomiting, dyspepsia, stomatitis, glossitis, pancreatitis, hepatitis.
From the side of the central nervous system: dizziness, headache, increased appetite, sedation, drowsiness, amnesia, anxiety, depression, anxiety, hallucinations, insomnia, unusual dreams, nervousness, paresthesia, personality change, tremor, akathisia.
co anorexia, vomiting, dyspepsia, stomatitis, glossitis, pancreatitis, hepatitis.
From the side of the central nervous system: dizziness, headache, increased appetite, sedation, drowsiness, amnesia, anxiety, depression, anxiety, hallucinations, insomnia, unusual dreams, nervousness, paresthesia, personality change, tremor, akathisia.
cosides of the sensory organs: tinnitus, vertigo, deafness, blurred visual perception, irritation or swelling of the eyes.
Laboratory indicators: increased activity of liver enzymes (LDH, alkaline phosphatase, transaminases), increased concentration of urea nitrogen, hypercreatininemia, decreased Hb and hematocrit, hypoproteinemia, thrombocytopenia, leukopenia, anemia (including aplastic and hemolytic), hypoglycemia, detection of antinuclear antibodies.
From the CCC side: increased blood pressure, tachycardia, palpitations, flushing of blood to the skin.
From the skin: rash (including petechial), purpura, including thrombocytopenic, ecchymosis, pruritus, onycholysis, alopecia, photosensitization, exfoliative dermatitis, erythema multiforme, Lyell’s syndrome, Stevens-Johnson syndrome, vesicle-bullous reactions.
From the genitourinary system: edema, dysuria, frequent urination, hematuria, oliguria, menorrhagia.
From the respiratory system: nosebleeds, shortness of breath.
Other: chest pain, thirst, chills, excessive sweating, increased or decreased body weight.
Drug Interactions
Antiplatelet agents, anticoagulants increase the risk of bleeding.
Displaces other drugs from communication with blood proteins (clinically significant for coumarin derivatives, sulfonamides and sulfanylurea derivatives, 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 blood serum by 20%. In combination with anticoagulants reduces blood coagulation (risk of bleeding).
Methotrexate increases hematotoxicity of piroxicam (deaths are possible).
Cimetidine increases AUC and Cmax of piroxicam by 13-15%.
Reduces the diuretic effect of furosemide.
Reduces renal clearance and increases Css of Li + drugs (requires monitoring of its concentration).
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 administration) reduces T1 / 2 of piroxicam by 50% and its bioavailability by 37%.
Forced diuresis, alkalization of urine, hemodialysis and hemoperfusion are ineffective (high connection with plasma proteins).
active substance
Piroxicam
lekarstvennaja form
kapsul
Manufacture of medicines, Russia
