Nemulex granules for suspension preparation package 100mg N10
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Active ingredients
Nimesulide
Release form
Granules
Composition
1 bag contains: nimesulide (nimesulide) 100 g
Pharmacological effect
NSAIDs. It has anti-inflammatory, analgesic, antipyretic and antiplatelet effect. Unlike other NSAIDs, it selectively inhibits COX-2, inhibits the synthesis of prostaglandins in the focus of inflammation; It has a less pronounced inhibitory effect on COX-1 (rarely causes side effects associated with inhibition of the synthesis of prostaglandins in healthy tissues).
Pharmacokinetics
Suction Absorption by intake is high. Eating reduces the rate of absorption without affecting its degree. Tmax in plasma - 1.5-2.5 h. Cmax in plasma - 3.5-6.5 mg / l. DistributionPlasma binding to plasma - 95%, with erythrocytes - 2%, with lipoproteins - 1%, with acidic alpha1-glycoprotein 1%. Changing the dose does not affect the degree of binding. Vd - 0.19-0.35 l / kg. It penetrates well into the acidic environment of the focus of inflammation (40%), synovial fluid (43%). Easily penetrates through histohematogenous barriers. Metabolism Metabolized in the liver by tissue monooxygenases. The main metabolite, 4-hydroxynimesulide (25%), has similar pharmacological activity, but due to a decrease in the size of molecules, it is able to quickly diffuse through the hydrophobic channel of COX-2 to the active binding center of the methyl group. 4-hydroxynimesulide is a water-soluble compound, for the elimination of which glutathione and conjugation reactions of the second phase of metabolism (including sulfation, glucuronidation) are not required. 4-hydroxynimesulide undergoes enterohepatic recirculation. Excretion of T1 / 2 nimesulide - 1.56–4.95 h, 4-hydroxynimesulide - 2.89–4.78 h. 4-hydroxynimesulide is excreted by the kidneys (65%) and with bile (35%).
Indications
Rheumatoid arthritis; Osteoarthritis; Arthritis of various etiologies; Arthralgia; Myalgia; Postoperative and post-traumatic pains; Bursitis; Tendonitis; Apogismenorrhea; Tooth and headache.
Contraindications
Hypersensitivity, a complete or incomplete combination of bronchial asthma, recurrent nasal polyposis or paranasal sinuses, and intolerance to acetylsalicylic acid (ASA) and other NSAIDs (including history), erosive and ulcerative lesions of the mucous membrane of the stomach and the duodenal gut, in the ileetoid ileus of the intestinal intestine of the gastric mucosa and duodenal ileus, imitation of the gastric mucosa and duodenal ulcer bleeding,cerebrovascular or other bleeding, inflammatory bowel disease (Crohn's disease, ulcerative colitis) in the acute phase, hemophilia and other bleeding disorders, decompensated chronic heart failure (CHF), liver failure or any active liver disease, hepatotoxic reactions when using nimesulide in anamnesis alcoholism, drug addiction, severe chronic renal failure (CRF) (CC less than 30 ml / min), progressive kidney disease, confirmed hyperkalea mission, period after coronary artery bypass grafting, simultaneous use of other hepatotoxic drugs (drugs), children under 12 years old, pregnancy, breastfeeding period. With caution peripheral artery diseases, smoking, renal failure (CC less than 30-60 ml / min), anamnestic data on the development of ulcerative lesions of the gastrointestinal tract (GIT), the presence of Helicobacter p infection ylori, old age, long-term use of NSAIDs, severe somatic diseases, simultaneous taking of anticoagulants (including warfarin), antiplatelet agents (including ASA, clopidogrel), oral glucocorticosteroids (GCS), selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline).
Precautionary measures
To reduce the risk of side effects, it is necessary to use the drug in the minimum effective dose of the shortest duration. If the patient's condition does not improve, treatment should be stopped. It is necessary to stop taking the drug if the temperature rises or develops on the background of his reception of flu-like symptoms.
Use during pregnancy and lactation
Use during pregnancy and lactation (breastfeeding) is contraindicated. The use of nimesulide may adversely affect female fertility and is not recommended for women who are planning a pregnancy.
Dosage and administration
Inside. The content of 1 sachet of granulate is dissolved in 80-100 ml of water. The recommended dose for adults and adolescents aged 12-18 years is 100 mg (1 sachet) 2 times a day after meals.The maximum daily dose for adults and adolescents aged 12-18 years is 200 mg. No dose reduction is required for elderly patients. Patients with chronic renal failure require a reduction in the daily dose to 100 mg. The minimum effective dose should be administered for as short a period as possible in order to minimize the risk of adverse reactions. The maximum duration of the drug should not exceed 15 days.
Side effects
Allergic reactions: hypersensitivity reactions, anaphylactoid reactions. From the side of the central nervous system: dizziness, fear, nervousness, nightmares, headache, drowsiness, encephalopathy (Reye's syndrome). On the part of the skin: itching, skin rash, increased sweating, erythema, dermatitis, urticaria, angioedema, facial swelling, erythema multiforme exudative, including Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome). On the side of the urinary system: edema, dysuria, hematuria, urinary retention, hyperkalemia, renal failure, oliguria, interstitial nephritis. On the part of the gastrointestinal tract: diarrhea, nausea, vomiting, constipation, flatulence, gastritis, abdominal pain, stomatitis, tarry stools, gastrointestinal bleeding, ulcers and / or perforation of the stomach or duodenum. On the part of the liver and biliary system: an increase in "liver" transaminases, hepatitis, fulminant hepatitis, jaundice, cholestasis. From the side of blood-forming organs: anemia, eosinophilia, thrombocytopenia, pancytopenia, purpura, lengthening of the bleeding time. On the part of the respiratory system: shortness of breath, exacerbation of bronchial asthma, bronchospasm. From the senses: blurred vision. Since the cardiovascular system: arterial hypertension, tachycardia, hemorrhage, "hot flashes". Others: general weakness, hypothermia.
Overdose
Symptoms: nausea, vomiting, drowsiness, apathy, gastrointestinal bleeding, increased blood pressure, acute renal failure, respiratory depression. Treatment: symptomatic and supportive treatment is recommended. There is no specific antidote.Patients admitted to the hospital with symptoms of an overdose of the drug (within 4 hours after taking it or after taking a high dose) recommended gastric lavage, taking activated carbon (60-100 mg for adults) and / or osmotic type laxatives. Requires regular monitoring of liver and kidney function. There is no data on the possibility of removing nimesulide using hemodialysis. Forced diuresis, hemodialysis are ineffective due to the high degree of binding of the drug to proteins.
Interaction with other drugs
There is evidence that nimesulide can reduce the bioavailability of furosemide, compete for binding to plasma proteins of fenofibrate, salicylic acid, and tolbutamides. Nemulex can replace salicylic acid and furosemide (but not warfarin) in plasma proteins. Nemulex has no effect on drugs that affect blood glucose concentration and glucose tolerance in diabetic patients treated with sulfonylurea derivatives. Physiological concentrations of unsaturated fatty acids are not affected the binding of nimesulide with serum albumin. At therapeutic concentrations, the binding of nimesulide was not affected by warfarin, furosemide, glibenclamide, digitoxin. It is not recommended to take prep arata Nemulex concurrently with diuretics, which have a damaging effect on renal hemodynamics. Taking the drug Nemulex in therapeutic doses orally for a short period does not change the serum profile of digoxin in patients with mild heart failure. plasma increases with simultaneous administration of lithium and Nemulex. Nemulex can enhance the effects of cyclosporin on the kidneys. TERM drug application Nemulex with corticosteroids, serotonin reuptake inhibitors increases the risk of gastrointestinal bleeding.
special instructions
When patients taking Nemulex, symptoms that indicate liver damage (eg, anorexia, nausea, vomiting, abdominal pain, fatigue, dark urine), or increased activity of hepatic transaminases, the drug should be discontinued.Nemulex should not be prescribed to such patients in the future. Gastrointestinal bleeding or ulcer / perforation of the stomach or duodenum can develop at any time during the use of the drug and not be accompanied by clinically pronounced symptoms (including pain syndrome). If gastrointestinal bleeding or ulceration occurs, the drug should be discontinued. In case of deterioration of the kidney function, the drug should be canceled. In case of using the drug for more than 2 weeks, monitoring of liver function is necessary. Elderly patients most often develop side effects when taking the drug, including gastrointestinal bleeding, perforation, impaired function of the heart, kidneys and liver. Therefore, regular clinical monitoring of the patient’s condition is recommended. Impact on the ability to drive vehicles and control mechanisms If the application of the drug causes adverse events from the central nervous system and sensory organs, patients should refrain from driving vehicles and practicing activities that require increased concentration and psychomotor speed reactions.