Nemulex granules for oral Suspension 100mg/2g, 30pcs

Composition

Active ingredient:  

nimesulide 100 mg;

Auxiliary substances:

macrogol cetostearate (cremophor A 25) – 100 mg;

citric acid anhydrous-19 mg;

colloidal silicon dioxide (aerosil) – 40 mg;

sucrose-1721 mg;

orange flavor-20 mg

Pharmacological action

Pharmaceutical group:

NSAIDs.

Pharmaceutical action:

Nemulex is an NSAID that has anti-inflammatory, analgesic, antipyretic and antiplatelet effects. In contrast to other NSAIDs, it selectively suppresses COX-2, inhibits Pg synthesis in the inflammatory focus, and has a less pronounced depressing effect on COX-1 (less often causes side effects associated with inhibition of Pg synthesis in healthy tissues).

Pharmacokinetics:  

Oral absorption is high (food intake reduces the rate of absorption without affecting its degree). The time to reach the maximum concentration in blood plasma (TStax) is 1.5-2.5 hours. The binding with plasma proteins is 95%, with red blood cells-2%, with lipoproteins-1%, with acidic alpha-1-glycoprotein-1%. Changing the dose does not affect the degree of binding. The maximum concentration (Ctax) is 3.5-6.5 mg/l. The volume of distribution is 0.19-0.35 l / kg. It penetrates well into the acidic environment of the inflammatory focus (40%), synovial fluid (43%).

Easily penetrates through histohematic barriers. It is 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 can quickly diffuse along the hydrophobic COX-2 channel to the active site of the methyl group binding. 4-hydroxynimesulide is a water-soluble compound that does not require glutathione and phase II conjugation reactions (sulfation, glucuronidation, etc. ) for its elimination.

The half-life (T 1/2) of nimesulide is 1.56-4.95 hours,4-hydroxynimesulide is 2.89-4.78 hours. 4-hydroxynimesulide is excreted by the kidneys (65%) and with bile (35%), undergoes enterohepatic recirculation.

Indications

tendinitis; algodismenorrhea; rheumatoid arthritis; osteoarthritis;arthritis of various etiologies;arthralgia; myalgia; postoperative and post-traumatic pain; bursitis; tooth and headache. The drug is intended for symptomatic therapy, reducing pain and inflammation at the time of use; it does not affect the progression of the disease.

Contraindications

hemophilia and other blood clotting disorder;decompensated chronic heart failure (CHF);liver failure or any active liver disease;hypersensitivity;complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose or paranasal sinuses and intolerance of acetylsalicylic acid (ASA) and other NSAIDs (including in the anamnesis);erosive-ulcerative lesions of the gastric mucosa and duodenal ulcer, active gastrointestinal bleeding;bleeding, including cerebrovascular;inflammatory bowel disease (Crohn’s disease, ulcerative colitis) in the acute phase;hepatotoxicity with the use of nimesulide in history;alcoholism;drug abuse;severe chronic renal failure (CRF) (creatinine Cl degenerative diseases of the kidneys; confirmed hyperkalemia;the period following the coronary artery bypass surgery;concomitant use of other hepatotoxic drugs;children up to age 12 years; pregnancy; breastfeeding. With caution: IHD, cerebrovascular diseases, CHF, dyslipidemia/hyperlipidemia, diabetes mellitus, peripheral arterial diseases, smoking, renal failure (creatinine clearance 30-60 ml/min), anamnestic data on the development of ulcerative lesions of the gastrointestinal tract, the presence of Helicobacter pylori infection, the elderly, long-term use of NSAIDs, severe somatic diseases, simultaneous use of anticoagulants (including warfarin), antiplatelet agents (including ASA, clopidogrel), oral corticosteroids, SSRIs (including citalopram, fluoxetine, paroxetine, sertraline).

Side effects

From the central nervous system: dizziness, fear, nervousness, nightmares, headache, drowsiness, encephalopathy (Reye’s syndrome). From the skin: pruritus, skin rash, increased sweating, erythema, dermatitis, urticaria, angioedema, facial edema, erythema multiforme exudative, including Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell’s syndrome). From the urinary system: edema, dysuria, hematuria, urinary retention, hyperkalemia, renal failure, oliguria, interstitial nephritis. From the gastrointestinal tract: diarrhea, nausea, vomiting, constipation, flatulence, gastritis, abdominal pain, stomatitis, tarry stools, gastrointestinal bleeding, ulceration and / or perforation of the stomach or duodenum. From the liver and biliary system: increased “hepatic” transaminases, hepatitis, lightning hepatitis, jaundice, cholestasis. Hematopoietic disorders: anemia, eosinophilia, thrombocytopenia, pancytopenia, purpura, prolonged bleeding time. From the respiratory system: shortness of breath, exacerbation of bronchial asthma, bronchospasm. From the side of the senses: blurred vision. From the cardiovascular system: arterial hypertension, tachycardia, hemorrhages, hot flashes. Allergic reactions: hypersensitivity reactions, anaphylactoid reactions. Other: general weakness, hypothermia.

Interaction

It is not recommended to take nimesulide simultaneously with diuretics that have a damaging effect on renal hemodynamics. Physiological concentrations of unsaturated fatty acids do not affect the binding of nimesulide to serum albumin. At therapeutic concentrations, nimesulide binding was not affected by warfarin, furosemide, glibenclamide, or digitoxin. In the presence of nimesulide, the free fractions of methotrexate can significantly increase. There is evidence that nimesulide may reduce the bioavailability of furosemide, act as a competitor for binding plasma proteins to fenofibrate, salicylic acid, tolbutamide. Nimesulide can replace salicylic acid and furosemide (but not warfarin) in plasma proteins. It has no effect on drugs that affect blood glucose concentration and glucose tolerance in diabetic patients treated with various drugs containing sulfonylureas. Oral use of nimesulide in therapeutic doses for a short period of time does not change the serum profile of digoxin in patients with mild heart failure. The concentration of lithium in plasma increases with simultaneous use of lithium and nimesulide preparations. Nimesulide may increase the effect of cyclosporine on the kidneys. The use of Nemulex with glucocorticosteroids, serotonin reuptake inhibitors increases the risk of gastrointestinal bleeding.

How to take, course of use and dosage

Inside. The contents of 1 sachet of Nemulex granulate are dissolved in 80-100 ml of water. The recommended dose for adults and adolescents aged 12-18 years is 100 mg (1 sachet of Nemulex) 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 need to reduce the daily dose to 100 mg.

The minimum effective dose of Nemulex should be administered for as short a period of time as possible in order to minimize the risk of adverse reactions.

The maximum duration of taking Nemulex should not exceed 15 days.

Overdose

Symptoms: increased blood pressure, acute renal failure, nausea, vomiting, drowsiness, apathy, gastrointestinal bleeding, respiratory depression; Treatment: symptomatic and supportive treatment is recommended. There is no specific antidote for Nimesulide. Patients admitted to the hospital with symptoms of overdose of the drug (within 4 hours after taking it or after taking a high dose) are recommended to wash the stomach, take activated charcoal (adults-60-100 mg) and/or an osmotic laxative. Regular monitoring of liver and kidney function is necessary. There are no data on the possibility of elimination of nimesulide by hemodialysis. Formed diuresis and hemodialysis are ineffective due to the high binding of the drug to proteins.

Special instructions

To reduce the risk of side effects, it is necessary to use Nemulex at the lowest effective dose with the shortest duration. If the patient’s condition does not improve, treatment should be discontinued. It is necessary to stop taking the drug if the temperature rises or flu-like symptoms develop against the background of taking it.

If patients taking Nimesulide develop symptoms that indicate liver damage (for example, anorexia, nausea, vomiting, abdominal pain, fatigue, dark urine), or an increase in the level of “liver” transaminases, the drug should be discontinued. Such patients are not recommended to be prescribed Nimesulide in the future. Gastrointestinal bleeding or ulceration/perforation of the stomach or duodenum can develop at any time during the use of the drug, which may 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 renal function, Nemulex should be discontinued. If the drug is used for more than 2 weeks, monitoring of liver function indicators is necessary. In patients with cirrhosis of the liver or with renal insufficiency with hypoalbuminemia or hyperbilirubinemia, the binding of nimesulide decreases.

Elderly patients most often develop side effects when taking the drug, including gastrointestinal bleeding, perforation, impaired heart, kidney and liver function. Therefore, regular clinical monitoring of the patient’s condition is recommended. The use of nimesulide may negatively affect female fertility and is not recommended for women planning pregnancy.

If the use of the drug Nemulex causes undesirable effects from the central nervous system and sensory organs, it is necessary to refrain from driving vehicles and engaging in activities that require increased concentration of attention and speed of psychomotor reactions.

Form of production

Granules for the preparation of a suspension for oral use.

Storage conditions

List B. : In a dry place, protected from light, at a temperature not exceeding 25 °C.

Shelf life

4 years

Active ingredient

Nimesulide

Conditions of release from pharmacies

By prescription

Dosage form

suspension for oral use

Purpose

Children as prescribed by a doctor, Adults as prescribed by a doctor, Children over 12 years of age

Indications

Bursitis, Sprains and Sprains, Tendon Inflammation, Sciatica, Gout, Rheumatoid Arthritis, Migraines, Sciatica, Osteochondrosis, Osteoarthritis, Arthrosis, Arthritis, Lumbago, Myositis