Absorption Nimesulide is well absorbed from the gastrointestinal tract. Food intake reduces the rate of absorption without affecting its degree.After oral administration of 100 mg of the drug reaches maximum concentration of the active substance in blood plasma -. 1.5 h 2.5 Maximum plasma concentration (C max ) is 3.5 – 6.5 mg / l. Increasing the drug concentration in blood plasma was dose-dependently.
Distribution The blood circulating in a bound form. Relationship to plasma proteins is 95%, with erythrocytes – 2%, from -1% lipoproteins, with acidic alpha1-glycoproteins – 1%. The volume of distribution is 0,19-0,35 l / kg. It penetrates into the inflammatory focus acidic environment (40%), synovial fluid (43%). Easily penetrates the blood-tissue barriers. The drug penetrates the tissues of female sexual organs, where, after a single dose of its concentration is about 40% of plasma concentrations. Therapeutic nimesulide concentration in plasma is maintained to 6 hours. Metabolism and excretion of drug is almost completely metabolized in the liver tissue monooxygenase undergoing biotransformation to form several metabolites: basic pharmacologically active hydroxynimesulide-4 (25%) and more active metabolites. The trenbolone side effects half-life (T½ ) of nimesulide is 1,56-4,95 hour, 4-hydroxynimesulide – 2,89-4,78 hour. 4 hydroxynimesulide excreted by the kidneys (65%) and bile (35%), undergoes enterohepatic recycling. From 1% to 3% of the drug excreted unchanged in urine. With prolonged use of the drug does not accumulates. In children and the elderly, and in patients with moderate renal impairment (creatinine clearance 30 – 80 ml / min), the pharmacokinetic profile of nimesulide varies slightly.
Acute and chronic pain of various origins (including migraine headache, toothache, tuberculosis, pre-operative and post-operative pain, post-traumatic pain, pain in dorsopathies).
Inflammatory diseases of the musculoskeletal system (arthritis of various etiologies, arthralgia), exacerbation of chronic diseases joints (rheumatoid arthritis, osteoarthritis, spondylitis, etc.), tendinitis, bursitis, myalgia, myositis.
It is intended for symptomatic therapy reduce pain and inflammation at the time of use, does not affect the progression of the disease.
- Hypersensitivity to nimesulide or auxiliary components;
- Full or partial combination of asthma, recurrent nasal polyposis, or paranasal sinuses and intolerance of aspirin and other nonsteroidal anti-inflammatory drugs (including history);
- Erosive and ulcerative lesions of the gastrointestinal tract in the acute stage, active gastrointestinal bleeding;
- Cerebrovascular or other bleeding;
- Hemophilia and other bleeding disorders;
- Inflammatory bowel disease (Crohn’s disease, ulcerative colitis) in the acute phase;
- Severe renal impairment (creatinine clearance (CC) – less than 30 ml / min), advanced kidney disease;
- Any active liver disease, hepatotoxicity using nimesulide in history;
- Decompensated heart failure, confirmed hyperkalemia, period after coronary artery bypass surgery;
- Simultaneous treatment with other trenbolone side effects hepatotoxic medicines;
- Patients with fever and / or flu-like symptoms;
- Alcoholism, drug addiction;
- Pregnancy and lactation;
- Children under 12 years old.
With caution : arterial hypertension, heart failure, in that the number of chronic ischemic heart disease, diabetes, cerebrovascular disease, dyslipidemia / hyperlipidemia, peripheral artery disease, smoking, renal insufficiency (creatinine clearance less than 60 mL / min), medical history data about the development of ulcerative lesions of the gastrointestinal tract, the presence of Helicobacter pylori infection, old age, long-term use of nonsteroidal anti-inflammatory drugs, alcoholism, severe somatic diseases, concomitant use of anticoagulants (including warfarin), antiplatelet agents (including acetylsalicylic acid, clopidogrel) , oral corticosteroids, selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline).
Dosing and dose
preparation in the form of dispersible tablets for oral administration. The tablet is dissolved in water or applied sublingually at the end or after a meal.
Adults and children over 12 years (body weight not less than 40 kg) – 100 mg 1-2 times a day. The maximum daily dose – 200 mg.
frequency classified by category, according to the occurrence of a case in percent: very often (> 10) and often (<10- <100), rare (<100- <1000), rare (<1000- <10000), very rare (<10,000). Gastrointestinal tract: often – diarrhea, nausea, vomiting; rarely – constipation, flatulence, heartburn, gastritis; very rare – abdominal pain, stomatitis, tarry stools, gastrointestinal bleeding, ulcers and / or perforation of the stomach or duodenum. Central nervous system : Infrequent – dizziness; rarely – a sense of fear, nervousness, nightmares; very rarely – headache, somnolence, encephalopathy (Reye’s syndrome). Respiratory : Infrequent – shortness of breath; very rare – asthma, bronchospasm. Cardiovascular system : Infrequent – hypertension; -tahikardiya rarely, hemorrhage, “hot flashes.” Senses : rarely – blurred vision, very rarely – dizziness. Skin and mucous membranes : rarely – itching, rash, increased sweating; rare: erythema, dermatitis; very rare: urticaria, angioneurotic edema, swelling of the face, erythema multiforme, including Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell’s syndrome). Liver and biliary system : often – increase in “liver” transaminase; very rarely – hepatitis, fulminant hepatitis, jaundice, cholestasis. The kidneys and urinary system : Infrequent – edema; rarely – dysuria, hematuria, urinary retention, hyperkalemia; very rarely – renal failure, oliguria, interstitial nephritis. hemopoiesis organs : rarely – anemia, eosinophilia; very rarely – thrombocytopenia, leukopenia, agranulocytosis, pancytopenia, purpura, prolonged bleeding Allergic reactions : seldom – hypersensitivity reaction; very rare – anaphylactoid reactions. Common reactions : rarely – weakness; very rarely -. Hypothermia In case of others, not mentioned above, side effects or worsening of state of health should immediately seek medical attention.
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Symptoms: increased severity of side effects, lethargy, drowsiness, nausea, vomiting. They are usually reversible when providing supportive care. There may be gastrointestinal bleeding, hypertension, acute renal failure, respiratory depression. Treatment : symptomatic trenbolone side effects treatment requires patient and supportive care of him. No specific antidote. If overdosage occurs during the last 4 hours necessary gastric lavage, appointment of activated carbon (60-100 g per human adult), osmotic laxatives. Forced diuresis, dialysis – are ineffective because of the high nimesulide being associated with plasma proteins. buy legal anabolic steroids online
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