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Pharmacological properties

the active substance of the drug - nabumeton refers to NSAIDs. It has anti-inflammatory, antipyretic, analgesic effect. the mechanism of action is associated with tsog blockade, which leads to a violation of the metabolism of arachidonic acid and a decrease in the concentration of prostaglandins, thromboxane. inhibits exudative and proliferative processes in the focus of inflammation, reduces the concentration of bradykinin and histamine, and also increases the threshold of susceptibility of pain receptors. the hypothermic effect is due to a decrease in the concentration of pyrogens in the lubricant and hypothalamic zone, an increase in heat transfer (it does not affect the heat production).

A characteristic feature of nabumetone is the lack of effect on the gastric mucosa. A lower incidence of ulcer, bleeding, and perforation has been reported compared to other NSAIDs. It has a slight effect on platelet aggregation caused by collagen and does not affect bleeding time.

Pharmacokinetics After oral administration, nabumetone is rapidly and completely absorbed. Food or milk accelerates its absorption. Bioavailability is about 80%.

It is metabolized in the liver with the formation of an active metabolite - 6-methoxy-2-naphthylacetic acid (35%) and other unidentified metabolites (50%). Cmax active metabolite is reached after about 3 hours (range - 1-12 hours), communication with blood proteins is 99%, crosses the placental barrier and into breast milk. Also, the active metabolite undergoes terminal transformations in the liver by O-demethylation and compounds with glucuronic acid.

About 75% of the dose of nabumetone is excreted by the kidneys. T½ - 24 hours

Indications

Acute and chronic osteoarthritis. rheumatoid arthritis. soft tissue rheumatism. ankylosing spondylitis.

Application

The drug is used by adults inside during or after a meal.

The recommended initial dose is 500-750 mg once a day. The recommended daily dose is 500 mg – 1 g once a day before bedtime. In some cases, the dose can be increased to 1.5–2 g / day in 1 or 2 doses. The maximum daily dose is 2 g.

The drug should be used for a short time at the lowest effective dose necessary to control the symptoms of the underlying disease.

Contraindications

Hypersensitivity to the active substance or other components of the drug. hypersensitivity in history (e.g., BA, angioedema, urticaria, rhinitis) associated with the use of acetylsalicylic acid and other NSAIDs. active peptic ulcer or a history of gastrointestinal bleeding, perforation, or peptic ulcer (2 or more episodes). gastrointestinal bleeding or a history of perforation associated with NSAIDs. severe heart and / or liver and / or renal failure. cerebrovascular or other active form of bleeding, hemorrhagic diathesis.

Side effects

From the blood system and lymphatic system: thrombocytopenia, leukopenia, agranulocytosis, granulocytopenia, neutropenia, aplastic anemia, hemolytic anemia.

On the part of the immune system: hypersensitivity reactions, including anaphylactic shock, anaphylactoid reactions.

From the psyche: confusion, nervousness, insomnia, depression, hallucinations.

From the nervous system: drowsiness, dizziness, headache, paresthesia, agitation, aseptic meningitis.

From the side of the organ of vision: visual impairment, optic neuritis.

On the part of the organ of hearing and the vestibular apparatus: tinnitus, hearing impairment.

From the cardiovascular system: heart failure, arrhythmias, hypertension, arterial hypotension, edema, vasculitis.

From the respiratory system, chest and mediastinal organs: shortness of breath, respiratory failure, nosebleeds, interstitial pneumonitis, asthma, an increase in the severity of asthma, bronchospasm.

From the digestive system: diarrhea, constipation, dyspepsia, gastritis, nausea, abdominal pain, flatulence, ulcers of the mucous membrane of the digestive tract, gastrointestinal bleeding, exacerbation of ulcerative colitis and Crohns disease, gastrointestinal disorders, melena, vomiting, heartburn, stomatitis, dry mouth, pancreatitis.

From the hepatobiliary system: liver failure, jaundice.

From the urinary system: renal failure, nephrotic syndrome, interstitial nephritis, dysuria.

From the musculoskeletal system and connective tissue: myopathy.

On the part of the skin and subcutaneous tissue: rash, itching, photosensitivity, urticaria, increased sweating, bullous reactions, including toxic epidermal necrolysis, Stevens-Johnson syndrome, erythema multiforme, angioedema, pseudoporphyria, baldness, purpura.

From the reproductive system and mammary glands: metrorrhagia.

Common disorders: edema, asthenia, fatigue, malaise.

The results of laboratory and instrumental studies: an increase in hepatic transaminases, hematuria, crystalluria, albuminuria, azotemia.

Clinical and epidemiological studies indicate that the use of certain NSAIDs may be associated with a risk of developing arterial thrombotic complications (for example, myocardial infarction or stroke).

special instructions

Adverse reactions of the drug can be minimized by applying the lowest effective dose for the shortest period necessary to control the symptoms of the disease.

Concomitant use with other drugs. The simultaneous use of the drug with other NSAIDs (including selective COX-2 inhibitors) should be avoided.

Effect on elderly patients. Elderly patients have an increased risk of adverse reactions, especially gastrointestinal bleeding and perforations, which can be fatal.

Effect on patients with AD. The drug should be used with caution in patients with AD or in patients with AD in history, since the use of NSAIDs has reported the development of bronchospasm in these categories of patients.

Effect on the organ of vision. When using NSAIDs, including nabumeton, visual impairment and a decrease in its severity were reported. In the case of the development of these disorders, patients should undergo an ophthalmological examination.

Impact on the reproductive system. The use of NSAIDs, including nabumetone, can lead to impaired fertility in women. The drug is not recommended for women planning a pregnancy. Consideration should be given to withdrawing the drug to women undergoing infertility testing or having difficulty conceiving.

Effect on the digestive tract. With the use of all NSAIDs, the development of gastrointestinal bleeding, ulcers and perforations, which can be fatal, was reported at any time during treatment with or without prior symptoms or serious gastrointestinal diseases in history.

Patients with a history of peptic ulcer disease (especially the elderly) should report any unusual abdominal symptoms, which is especially important in the initial stages of treatment.

The risk of such phenomena increases along with an increase in the dose of NSAIDs in patients with a history of ulcer in the digestive tract, especially complicated by bleeding or perforation, as well as in elderly patients. Treatment of such patients should begin with the lowest effective dose.Patients should be advised of any unusual abdominal symptoms, which is especially important in the initial stages of treatment. Caution should be used in patients with a history of gastrointestinal diseases (for example, ulcerative colitis or Crohns disease), since the course of these diseases can worsen.

The drug should be used with caution in patients with gastrointestinal diseases and patients taking medications that increase the risk of ulcers or bleeding, including corticosteroids, anticoagulants, selective serotonin reuptake inhibitors, antiplatelet agents (acetylsalicylic acid). For these patients, consideration should be given to the use of combination therapy using drugs such as misoprostol or proton pump inhibitors.

The drug should be used with caution during simultaneous therapy with agents that increase the risk of ulcers or bleeding, for example, oral contraceptives, anticoagulants (warfarin), NSAIDs, selective serotonin reuptake inhibitors, antiplatelet agents (acetylsalicylic acid, clopidogrel).

If ulcers or bleeding develop, discontinue use of the drug.

The drug should only be used after a thorough assessment of the benefit / risk ratio in patients with active peptic ulcer. Patients should be under close medical supervision.

Nabumetone is better tolerated than most other NSAIDs, including less affecting the digestive tract. Pre- and post-registration studies indicate that the average rates of perforation, ulcers and bleeding are lower with the use of nabumeton than other NSAIDs: during treatment 3–6 months, 1 year and 2 years, respectively, 0.3; 0.5 and 0.8%. However, doctors must remember that the occurrence of an ulcer is possible without its history.

Despite the relative safety for the digestive tract and kidneys, the drug should be used with caution in patients:

  • with an active ulcer of the digestive tract; appropriate treatment should be started before nabumetone therapy;
  • with the presence of AD, urticaria, or other hypersensitivity reactions associated with the use of NSAIDs; rarely reported the development of asthma with fatal outcome in such patients; the use of the drug should be carried out under control.

Effect on the skin and subcutaneous tissue. When using NSAIDs, including nabumetone, very rarely reported the development of serious skin reactions, including exfoliative dermatitis, Stevens-Johnson syndrome and toxic epidermal necrolysis, which can be fatal. The highest risk of developing these disorders is noted at the initial stages of treatment, in most cases - during the first month of therapy. In the event of skin rashes, lesions of the mucous membrane, or any other signs of hypersensitivity, discontinue use of the drug.

Effect on the cardiovascular system. The use of certain NSAIDs (especially in high doses over an extended period) can lead to an increased risk of arterial thrombotic complications (such as myocardial infarction or stroke). Since there are insufficient data to exclude such a risk for nabumetone, the drug should be used only after a thorough assessment of the condition: for patients with uncontrolled hypertension, congestive heart failure diagnosed with coronary artery disease, peripheral artery disease and / or cerebrovascular disease, and in case of prolonged therapy to patients with risk factors for cardiovascular vascular diseases such as hypertension, hyperlipidemia, diabetes mellitus, smoking.Periodic monitoring of the condition of patients with AH with a history of mild to moderate congestive heart failure should be carried out and, if necessary, recommendations should be made, since fluid retention and edema were reported.

Effect on the hepatobiliary system. When using NSAIDs, including nabumeton, the development of impaired liver function and, in rare cases, jaundice and liver failure has been reported, which in some cases can lead to death. In the case of signs / symptoms of impaired liver function or an increase in hepatic transaminases, a careful monitoring of the patients condition should be carried out to identify more serious disorders and, if necessary, stop using the drug.

Effect on the urinary system. The use of NSAIDs leads to a dose-dependent decrease in the synthesis of prostaglandins and can cause the development of renal failure. The drug should be used with caution in patients with risk factors, such as impaired renal and / or liver function, heart failure, the simultaneous use of diuretics, advanced age. Patients with moderate renal failure (creatinine clearance 30–49 ml / min) may require dose adjustment.

In some cases, patients receiving nabumeton developed aseptic meningitis. Although the appearance of this reaction is more likely in patients with systemic lupus erythematosus and other connective tissue diseases, the development of this complication has also been reported in patients without concomitant chronic diseases.

The use of NSAIDs, including nabumetone, can mask the symptoms of infectious diseases.

Use during pregnancy and lactation. Period of pregnancy. The safety and effectiveness of nabumetone in pregnant women have not been established. Nabumetone, like other NSAIDs, can cause premature closure of the ductus arteriosus in the fetus, the development of heart and lung defects.

The drug is contraindicated for use in the III trimester of pregnancy. The use of the drug in the I and II trimester of pregnancy is possible in the case when the potential benefit to the mother outweighs the possible risk to the fetus.

The period of breastfeeding. Nabumetone excretion into breast milk has not been investigated. In the case of the use of the drug should stop breast-feeding.

Children. The drug is not recommended for use in pediatric practice, since the safety and effectiveness of the use of nabumetone in children have not been established.

The ability to influence the reaction rate when driving vehicles or working with other mechanisms. When using the drug, such adverse reactions as dizziness, drowsiness, confusion, fatigue, and visual impairment may occur. In the event of these adverse reactions, one should refrain from driving vehicles or other mechanisms.

Interactions

With the simultaneous use of nabumetone with other drugs, the following interactions are possible:

  • with anticoagulants - increased effectiveness of the latter; drugs should be used with caution and monitor the symptoms of an overdose of anticoagulants;
  • with antihypertensive agents (for example, ACE inhibitors, angiotensin receptor antagonists), diuretics - a decrease in the effectiveness of the latter; in some patients with impaired renal function (elderly patients or dehydrated patients), concomitant use of ACE inhibitors and angiotensin II receptor antagonists with COX enzyme inhibitors can lead to additional impairment of renal function, including the possibility of acute renal failure; with the simultaneous use of drugs, frequent monitoring of the condition of patients should be carried out; patients should receive a sufficient amount of fluid;
  • with antiplatelet agents, selective serotonin reuptake inhibitors, corticosteroids - increased risk of gastrointestinal bleeding;
  • with other NSAIDs, including selective COX-2 inhibitors, an increased risk of adverse reactions; simultaneous use of these drugs should be avoided;
  • with zidovudine - increased risk of hematotoxicity; An increased risk of hemarthrosis and hematomas was reported in HIV-positive patients with hemophilia, with the simultaneous use of these drugs;
  • with potassium-sparing diuretics - the risk of developing hyperkalemia;
  • with lithium, methotrexate - a decrease in the excretion of the latter;
  • with mifepristone - a decrease in the effect of the latter; NSAIDs should be used 8-12 days after taking mifepristone;
  • with cardiac glycosides - an increase in the severity of heart failure, a decrease in glomerular filtration rate and an increase in plasma glycoside levels;
  • with cyclosporine, tacrolimus - increased risk of nephrotoxicity;
  • with quinolones - increased risk of seizures;
  • with colestyramine - slowing down the absorption of nabumetone.

The following drugs do not affect the metabolism and bioavailability of nabumetone: antacids, paracetamol, cemetidine, aluminum hydroxide, acetylsalicylic acid.

Nabumetone should be used with caution simultaneously with protein-binding drugs, such as sulfonamides, sulfonylureas, hydantoins, and to monitor the symptoms of an overdose.

Overdose

Symptoms: headache, nausea, vomiting, epigastric pain, gastrointestinal bleeding, diarrhea, disorientation, agitation, coma, drowsiness, dizziness, tinnitus, fainting, convulsions, in the case of severe poisoning, possible acute liver and liver damage.

Treatment: during the first hour after an overdose, activated charcoal should be taken, gastric lavage, forced diuresis should be carried out, further therapy is symptomatic. Care should be taken to monitor liver and kidney function. The patient should be closely monitored for at least 4 hours after an overdose.

Storage conditions

At a temperature not exceeding 25 ° C.

Tags: Synmeton® [Nabumeton]