Pharmacological action Nabumetone 750 mg
NSAIDs. It is believed that Nabumetone relates to a selective COX-2 inhibitor.
Has anti-inflammatory, analgesic and to a lesser extent, antipyretic action. After absorption from the intestine enters the liver where it forms the main active metabolite – 6-methoxy-2 naphthylacetic acid (6-MNA), significantly superior to antitsiklooksigenaznoy activity of the substance. Thus, Nabumetone can be considered as prodrugs. Unlike most NSAIDs, 6-MNA inhibits COX-2 more than COX-1. COX-1 is detected in various organs and tissues involved in the formation of prostaglandins that provide the normal physiological functions. COX-2 in significant amounts determined in the inflammation, contributing to the accumulation of prostaglandins, which are mediators of the inflammatory response. Because of this circumstance, the application Nabumetone rarely experience side effects caused by inhibition of prostaglandin synthesis in different organs, rather than the use of other NSAIDs, inhibits COX-1 and COX-2 in approximately equal measure.
Pharmacokinetics Nabumetone 750 mg
Nabumetone rapidly and completely absorbed from the gastrointestinal tract. Bioavailability is 80%. Undergoes rapid metabolism to the formation of the active metabolite 6-MNA (35%) and 50% of unidentified metabolites. Plasma protein binding for 6-MNA – 99%, subject to a terminal metabolism in the liver to form inactive metabolites. T1 / 2 – 24 h. Write kidney – 75% of the dose within 48 hours
Dosage Nabumetone 750 mg
Average daily intake for adults – 1 g / 1 reception (preferably overnight). If necessary, the dose may be increased to 1.5 g.
Structure and Composition Nabumetone 750 mg
1 tablet, film coated contains Nabumetone 500 or 750 mg in bottles of 100 pieces., In box 1 bottle.
Drug Interactions Nabumetone 750 mg
Nabumetone increases effects of anticoagulants of indirect action, funds from a group of antidiabetic sulfonylureas, difenina (due to the exclusion of these funds from the complexes with transport proteins of plasma).
Nabumetone enhances the action of antiplatelet agents and fibrinolytics, as well as side effects of corticosteroids, oral contraceptives.
Antacids and kolestiramin slow Nabumetone absorption from the gastrointestinal tract.
Pregnancy and lactation
Nabumetone contraindicated during pregnancy and lactation (breastfeeding).
Side Effects Nabumetone 750 mg
Allergic reactions: urticaria, angioedema, photosensitivity, erythema multiforme, a malignant exudative erythema, toxic epidermal necrolysis.
From the digestive system: nausea, vomiting, diarrhea, dyspepsia, abdominal pain, constipation, flatulence, dry mouth, stomatitis, gingivitis, glossitis, gastritis, anorexia, jaundice, mucosal ulceration of the stomach and duodenal ulcers, dysphagia, gastroenteritis, increase in liver transaminases, duodenitis, cholelithiasis, pancreatitis.
CNS and peripheral nervous system: sleep disturbance, dizziness, headache, fatigue, asthenic syndrome, agitation, anxiety, depression, paresthesia, tremor, weakness, nightmares.
Cardio-vascular system: tachycardia, increased blood pressure, angina, myocardial infarction, syncope, thrombophlebitis, vasculitis.
With the respiratory system: dyspnea, eosinophilic pneumonia, pneumonitis against hypersensitivity, bronchial asthma, cough.
With the urinary system: albuminuria, hyperuricemia, nephrotic syndrome, interstitial nephritis, dysuria, hematuria, nephrolithiasis.
From the hemopoietic system: anemia, leukopenia, granulocytopenia, thrombocytopenia.
From the blood coagulation system: bleeding (including rectal, vaginal).
From the senses: visual disturbances, impaired sense of taste.
From a metabolism: the reduction or increase in body weight, increased sweating.
From the laboratory parameters: a positive reaction for blood in the stool.
Other: chills, fever, acne, alopecia, reduced potency.
Statement Nabumetone 750 mg
Rheumatoid arthritis, osteoarthritis.
Contraindications Nabumetone 750 mg
Gastric ulcer and duodenal ulcer, pregnancy, lactation, childhood, bronchial asthma, nasal polyposis, heart failure, peripheral edema, hemophilia, hypocoagulation, “Aspirin triad, increased sensitivity to Nabumetone.
Cautions
With caution is prescribed for digestive diseases, elderly patients, with hepatic and / or renal failure.
Nabumetone can increase skin sensitivity to ultraviolet irradiation.
Ultseratsiya gastric and duodenal ulcers, bleeding and perforation may develop at the beginning of treatment without the appearance of warning signs and have a tendency to increase with prolonged treatment. May be a delay of the liquid (should be considered when treating patients with hypertension), hyperglycemia, hypokalemia, azotemia, bilirubinuriya.
