Pyroxicam, 20 mg capsules 20 pcs

Pharmacotherapeutic group

Non-steroidal anti-inflammatory drug (NSAID)

ATX code: M02AA07

Pharmacodynamics:

Pyroxicam is a nonsteroidal anti-inflammatory drug (NSAID) with anti-inflammatory analgesic and antipyretic effects.

Nonselectively inhibits activity of cyclooxygenase 1 and cyclooxygenase 2 (COX1 and COX2) inhibits the synthesis of prostaglandins in the inflammation focus and in the central nervous system, suppresses the exudative and proliferative phases of inflammation. Inhibits the aggregation of neutrophils and the formation of superoxide anions in them the migration of polymorphonuclear cells and monocytes to the inflammation focus. Reduces the release of lysosomal enzymes from stimulated leukocytes.

Decreases pyrogenic effect of prostaglandins on the center of thermoregulation. Reduces the severity of the pain syndrome of medium intensity by increasing the threshold of pain sensitivity to biological amines. Analgesic effect appears 30 min after oral administration. After a single dose, the effect lasts for 24 hours. In joint syndrome, it relieves or reduces inflammation and pain at rest when moving reduces morning stiffness and joint swelling and helps to increase range of motion. With algodysmenorrhea (being an inhibitor of prostaglandin synthesis in the endometrium) relieves pain.

Pharmacokinetics:

When taken orally the drug is well absorbed from the gastrointestinal tract, maximum plasma concentration is proportional to the dose used. Maximum plasma concentrations are reached 3-5 hours after oral administration. After a single dose of 20 mg, Cmax is 15-2 mcg/ml after regular administration of 20 mg/day – 3-8 mcg/ml. Food slows down the rate of absorption but does not affect the volume of absorption. Bioavailability is almost 100%. Time to reach equilibrium concentration is 7-12 days. It penetrates into the synovial fluid (40-50 %) is excreted with the breast milk – 1-3 %. It easily binds with blood plasma proteins (almost 98 %).

The elimination half-life is 24-50 h in liver disease may be prolonged. The drug is metabolized in liver through hydroxylation of pyridine ring of side chain with subsequent conjugation with glucuronic acid and formation of inactive metabolites. It is excreted as conjugates by the kidneys and, to a lesser extent, through the intestines. About 5% is excreted unchanged.

Indications

Diseases of the musculoskeletal system: rheumatoid arthritis osteoarthritis spondylitis sciatica psoriatic arthropathy gout tendovaginitis bursitis Bechterew disease (ankylosing spondylitis) spinal pain neuralgia myalgia postoperative and posttraumatic pain extraarticular rheumatic diseases soft tissue inflammation.

Algodysmenorrhea.

Designed for symptomatic therapy to reduce pain and inflammation at the time of use has no effect on the progression of the disease.

Active ingredient

Pyroxicam

Composition

In one capsule:

Pyroxicam (in terms of 100% substance) – 20 mg.

Excipients: – microcrystalline cellulose, potato starch, talcum powder, colloidal silicon dioxide. Solid gelatin capsules: gelatin, titanium dioxide, iron oxide yellow, indigo carmine, water.

How to take, the dosage

Adults and children over 15 years of age – orally with meals.

Musculoskeletal system diseases joint diseases (rheumatoid arthritis osteoarthritis spondylitis) the initial and maintenance dose is 10-20 mg per day in 1 or 2 doses.

If necessary, the dose may be temporarily increased to 30 mg per day (once or in divided doses) or reduced to 10 mg per day.

Acute musculoskeletal disorders: the first 2 days, 40 mg daily, once or in multiple doses. The maintenance dose is 20 mg per day for 1-2 weeks.

An acute attack of gout: take 40 mg for 4-6 days.

Postoperative and post-traumatic pain: the initial dose is 20 mg once a day.

In some cases, it is possible to increase the dose with a prescription of 40 mg once daily or in divided doses for the first two days.

In algodysmenorrhea: treatment should be started when the first symptoms appear In an initial dose of 40 mg/day in 1 or more doses over 2 days. On the following 1-3 days, 20 mg at 1 dose.

The maximum daily dose of the drug for adults and children over 15 years of age should not exceed 40 mg.

The recommended daily dose should not be exceeded because it increases the risk of side effects.

Interaction

In the simultaneous use of piroxicam and:

• glucocorticosteroids and/or NSAIDs – increased risk of gastrointestinal side effects including bleeding;
• phenobarbital – decreases the level of pyroxicam serum concentrations;
• Cimetidine probenecid and sulfinpyrazone – serum levels of piroxicam may increase, leading to increased side effects of piroxicam;
• phenytoin and/or lithium and potassium-saving diuretics and K+ donors – plasma levels of lithium and potassium phenytoin may increase;
• phenobarbitalanticoagulants – platelet aggregation capacity decreases (risk of bleeding);
• acetylsalicylic acid – decreases the serum concentration of piroxicam and increases the risk of gastrointestinal erosive ulcers;
• selective serotonin reuptake inhibitors (citalopram fluoxetine paroxetine sertraline) – increased risk of gastrointestinal erosive ulcers;
• metotrexate – may lead to increased concentrations of methotrexate and increase its toxic effects.

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Special Instructions

To prevent unwanted effects, the drug should only be used as prescribed by a physician at the lowest effective dose for the shortest possible course.

The simultaneous use of multiple non-steroidal anti-inflammatory drugs increases the risk of side effects, and the therapeutic effect is not improved.

The drug may alter platelet function, but it does not replace the preventive action of acetylsalicylic acid in cardiovascular disease.

Particular caution should be used with patients with impaired hepatic or renal function who use diuretics after major surgery in older patients. Such patients should have their blood cell composition and renal function monitored.

After 2 weeks of using the drug it is necessary to monitor the liver function parameters (transaminases).

In order to decrease the risk of gastrointestinal adverse events, the lowest effective dose should be used for the shortest possible course.

If the patient develops signs of gastrointestinal ulceration during therapy with the drug, treatment must be discontinued; if it is absolutely necessary to use the drug, treatment must be under medical supervision with concomitant use of antacids.

The drug is not recommended for patients with bronchial asthma allergic rhinitis nasal polyps and chronic obstructive airway diseases.

The use of the drug may adversely affect female fertility and is not recommended for women planning to become pregnant.

Alcohol should not be consumed during treatment with the drug.

There is currently no recommendation for use in children under 15 years of age.

Influence on ability to drive:

When taking this medicine, caution must be exercised while driving motor vehicles and engaging in other potentially dangerous activities that require increased concentration and quick psychomotor reactions.

Contraindications

• hypersensitivity to pyroxicam and other non-steroidal anti-inflammatory drugs components of the drug;
• complete or incomplete combination of bronchial asthma recurrent polyposis of nasal mucosa or paranasal sinuses and intolerance to acetylsalicylic acid and other NSAIDs (including history history)
• erosive and ulcerative changes of the mucous membrane of the stomach or duodenum active gastrointestinal bleeding; cerebrovascular or other bleeding;
• inflammatory bowel disease (Crohn’s disease ulcerative colitis) in the acute phase;
• hemophilia and other disorders of blood clotting;
• decompensated heart failure;
• hepatic insufficiency or any active liver disease;
• explicit renal insufficiency (creatinine clearance less than 30 mL/min) advanced renal disease confirmed hyperkalemia;
• period after coronary artery bypass surgery;
• pregnancy breastfeeding period;
• children under 15 years of age.

With caution:

• age over 65 years old;
• ischemic heart disease cerebrovascular disease congestive
• heart failure;
• dyslipidemia/hyperlipidemia;
• arterial hypertension;
• diabetes mellitus;
• peripheral artery disease;
• bronchial asthma;
• presence of hepatic porphyria;
• creatinine clearance of 30-60 ml/min;
• postoperative period;
• dehydration;
• smoking;
• History of gastrointestinal ulcers

presence of Helicobacter pylori infection long-term use of NSAIDs frequent alcohol consumption severe somatic diseases concomitant therapy with the following drugs:

– anticoagulants (e.g., warfarin);
– antiaggregants (e.g., acetylsalicylic acid clopidogrel);
– Oral glucocorticosteroids (e.g., prednisolone);
– Selective serotonin reuptake inhibitors (e.g., citalopram fluoxetine paroxetine sertraline).

Side effects

Most commonly manifested gastrointestinal and digestive tract disorders: pain in epigastric region belching nausea decreased appetite vomiting constipation or diarrhea flatulence erosive ulcerative lesions of the gastrointestinal tract gastrointestinal bleeding which in exceptional cases can cause anemia perforation of gastrointestinal tract; dry mouth stomatitis.

Hepatobiliary system disorders: liver function disorders – increased “hepatic” transaminase activity; increased plasma concentrations of nitrogen and creatinine.

Urinary system disorders: renal dysfunction interstitial nephritis papillary necrosis nephrotic syndrome erythrocyturia proteinuria hyper- or hypokalemia glomerulonephritis nephrosis.

Central nervous system disorders: dizziness headache tinnitus somnolence insomnia less frequently – depression irritability hallucinations paresthesias lethargy mood changes.

Hematopoietic and hemostatic disorders: anemia including aplastic and hemolytic decrease in hemoglobin decreasing hematocrit index; leukopenia – eosinophilia rarely – thrombocytopenia haemorrhage thrombocytopenic purpura (Schönlein-Henoch disease); suppression of bone marrow function.

Cardiovascular system disorders: increase or decrease of blood pressure signs of heart failure rarely – palpitation dyspnea.

Allergic reactions: skin rash itching erythema reaction photosensitization Lyell’s syndrome facial edema larynx bronchospasm malignant exudative erythema (Stevens-Johnson syndrome) anaphylactic shock vasculitis serum sickness.

Others: visual impairment swelling of shins and feet increased sweating increased concentration of urea; weight gain or decrease.

The incidence of the above disorders increases with increasing daily dose of the drug.

Overdose

Symptoms: abdominal pain, nausea, vomiting, drowsiness visual impairment at very high doses – loss of consciousness coma.

Treatment: gastric lavage with activated charcoal to slow down absorption antacids are used. In case of severe poisoning the patient should be hospitalized. There is no specific antidote. Treatment is symptomatic.

Similarities

Pyroxicam, Pyroxicam, Pyroxicam