Clinical and pharmacological group: & nbsp

Other non-narcotic analgesics, including non-steroidal and other anti-inflammatory drugs

Included in the formulation
АТХ:

M.01.A.X.01   Nabumeton

Pharmacodynamics:

A prodrug is metabolized in the liver to form an active metabolite. Non-selectively inhibits COX by providing an anti-inflammatory, analgesic and antipyretic effect. The anti-inflammatory effect is due to inhibition of COX-2 activity, which leads to a decrease in the production of inflammatory mediators - prostaglandins Pg D2, E2 and I2. The analgesic effect is associated with a decrease in the synthesis of PgE2, which prevents sensitization of pain receptors to bradykinin, histamine and other chemicals synthesized or released in the inflammatory focus. The antipyretic effect is caused by the impairment of the production of the eicosanoid PgE2, which, when inflamed, stimulates the thermoregulatory center in the anterior parts of the hypothalamus, while only febrile body temperature decreases due to increased heat transfer as a result of increased sweating and peripheral vascular expansion, normal body temperature does not decrease.

Pharmacokinetics:

Absorption from the gastrointestinal tract is rapid and complete, increases with admission with food and milk. The maximum accumulation in the synovial fluid is 8 h.Biotransformation in the liver (effect of the first passage) with the formation of an active metabolite (35-38% of the dose) - 6-methoxy-2-naphthylacetic acid (6-MNA). Relationship with plasma proteins for 6-MNA> 99%. The half-life for 6-MNA is 23 ± 3.7 h. Elimination of 6-MNA by kidneys is 80% of the dose taken, during 48-75 h, complete elimination ends after 168 h.

Indications:

Rheumatoid arthritis, osteoarthritis, gout.

XIII.M05-M14.M06.9   Rheumatoid arthritis, unspecified

XIII.M05-M14.M06   Other rheumatoid arthritis

XIII.M05-M14.M05.9   Seropositive rheumatoid arthritis, unspecified

XIII.M05-M14.M05.8   Other seropositive rheumatoid arthritis

XIII.M05-M14.M05.3   Rheumatoid arthritis with involvement of other organs and systems

XIII.M05-M14.M05   Seropositive rheumatoid arthritis

XIII.M05-M14.M10.9   Gout, unspecified

XIII.M05-M14.M10.3   Gout due to impaired renal function

XIII.M05-M14.M10.2   Drug Gout

XIII.M05-M14.M10.0   Idiopathic Gout

XIII.M05-M14.M10   Gout

XIII.M15-M19.M19.9   Osteoarthritis, unspecified

XIII.M15-M19.M19.8   Other specified arthrosis

Contraindications:Hypersensitivity, stomach ulcer and duodenal ulcers, bronchial asthma, polyposis of the nose, heart failure, peripheral edema, hemophilia, hypocoagulation, pregnancy, breast-feeding, children's age.
Carefully:

Induced acute hepatic porphyria, severe hepatic and / or renal insufficiency, chronic heart failure, elderly age.

Pregnancy and lactation:

Category FDA FROM.

Qualitative and well-controlled studies on humans have not been conducted. Animals had no teratogenic effect, fetotoxic effect was noted (in therapeutic concentrations for humans). There is no information on the penetration into breast milk. Contraindicated in pregnancy and lactation.

Dosing and Administration:

The average daily intake for adults is 1 g once inside after meals. In some cases, the dose may be increased to 1.5-2 g per day in 2 divided doses. The highest daily dose is 2 g.

Side effects:

Allergic reactions: urticaria, angioedema, photosensitization, erythema multiforme, malignant exudative erythema, toxic epidermal necrolysis.

On the part of the digestive system: nausea, vomiting, diarrhea, dyspepsia, abdominal pain, constipation, flatulence, dry mouth, stomatitis, gingivitis, glossitis, gastritis, anorexia, jaundice, ulceration of the stomach and duodenal mucosa, dysphagia, gastroenteritis,increased activity of hepatic transaminases, duodenitis, cholelithiasis, pancreatitis.

From the central nervous system and peripheral nervous system: sleep disturbances, dizziness, headache, fatigue, asthenic syndrome, agitation, anxiety, depression, paresthesia, tremor, general weakness, nightmares.

From the cardiovascular system: tachycardia, increased blood pressure, stenocardia, myocardial infarction, syncope, thrombophlebitis, vasculitis.

On the part of the respiratory system: dyspnea, eosinophilic pneumonia, pneumonitis on a background of hypersensitivity, bronchial asthma, cough.

From the urinary system: albuminuria, hyperuricemia, nephrotic syndrome, interstitial nephritis, dysuria, hematuria, nephrolithiasis.

On the part of the hematopoiesis system: anemia, leukopenia, granulocytopenia, thrombocytopenia.

From the coagulation system of the blood: bleeding (including rectal, vaginal).

From the sense organs: blurred vision, a violation of taste.

From the side of metabolism: decrease or increase in body weight, increased sweating.

On the part of laboratory indicators: a positive response to blood in the stool.

Others: chills, fever, acne, alopecia, decreased potency.
Overdose:

Symptoms generally reflect the toxic effect of the drug on the gastrointestinal tract, kidneys, and central nervous system; hypoprothrombinemia.

Treatment is symptomatic.

Interaction:

Nabumetone enhances the effects of indirect anticoagulants, antidiabetic agents from the group of the sulfonylureas, diphenylhydantoin (due to displacement of said means of transport complexes with plasma proteins), antiplatelet agents, and enhances the action of fibrinolytics and side effects of corticosteroids, oral contraceptives.

Antacids and colestramine slow the absorption of nabumetone from the digestive tract.

Special instructions:

Nabumetone can increase the sensitivity of the skin to ultraviolet radiation.

Ulceration of the gastric mucosa and duodenal ulcers, bleeding and perforation may develop at the beginning of treatment without the occurrence of warning signs and tend to increase with prolonged treatment. Possible fluid retention (should be considered in the treatment of patients with arterial hypertension), Hyperglycemia, hypokalemia, azotemia, bilirubinuria.

Instructions
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