Pharmacological action – analgesic, antipyretic, anti-inflammatory.
The NSAID of the class of sulfonanilides. It is a selective competitive inhibitor of COX-2, inhibits synthesis of GH in the inflammation focus. Its inhibitory effect on COX-1 is less pronounced (less often causes side effects associated with inhibition of GH synthesis in healthy tissues). It has anti-inflammatory, analgesic and antipyretic effects.
Absorption when taken orally is high. Food intake reduces the rate of absorption without affecting its degree. Tmax is 1.5-2.5 h. Binding with plasma proteins – 95%, with red blood cells – 2%, with lipoproteins – 1%, with acidic alpha1-glycoproteins – 1%. Changing the dose has no effect on the degree of binding. Cmax is 3.5-6.5 mg/L. Vd – 0.19-0.35 l/kg. It penetrates into the tissues of the female genitalia, where after a single administration its concentration is about 40% of the plasma concentration. It penetrates well into the acidic environment of the inflammation focus (40%) and synovial fluid (43%). Easily penetrates through histohematic barriers.
It is metabolized in liver by tissue monooxygenases. The main metabolite – 4-hydroxynimesulide (25%) – has similar pharmacological activity, but due to the reduced size of the molecules is able to rapidly diffuse through the COX-2 hydrophobic channel to the active binding center of the methyl group. 4-Hydroxynymesulide is a water-soluble compound that does not require glutathione and phase II metabolic conjugation reactions (including sulfation, glucuronidation) for excretion.
The T1/2 of nimesulide is 1.56-4.95 h, that of 4-hydroxynimesulide is 2.89-4.78 h. 4-hydroxynimesulide is excreted by the kidneys (65%) and with the bile (35%); it undergoes enterohepatic recirculation.
In patients with renal insufficiency (creatinine Cl 1.8-4.8 l/h or 30-80 ml/min), as well as in children and elderly persons the pharmacokinetic profile of nimesulide does not change significantly.
Sciatica, Osteochondrosis, Arthrosis, Bruises, Joint pain (arthralgia), Bursitis, Myalgia (muscle pain), Rheumatoid arthritis, Radiculitis, Back pain, Pain after injuries and operations, Arthritis, Myositis, Sprains and strains, Pain, Lumbago, Neck pain, Gout, Inflamed tendons<
How to take, the dosage
With caution, use simultaneously with diuretics, blood pressure medications, other analgesic anti-inflammatory drugs, anti-diabetic drugs.
It is recommended to apply the drug only to intact skin areas, avoiding contact with open wounds.
- High sensitivity to nimesulide and drug components;
- .Ulcerative lesions of gastro-intestinal tract in aggravation stage, bleeding from gastro-intestinal tract, dermatosis, epidermis damage and skin infections in the application area;
- Developed renal (creatinine clearance less than 30 ml/min) or hepatic insufficiency, indicated in anamnesulide.) or hepatic insufficiency, indication in the anamnesis of bronchospasm associated with the use of acetylsalicylic acid or other NSAIDs;
- Pregnancy and lactation;
- Children under 7 years of age.
- Hepatic failure;
- Hepatic failure;
- Veep heart failure;
- Arterial hypertension;
- Diabetes mellitus type 2;
- Elderly and childhood.
Local reactions: itching, urticaria, peeling, transient discoloration of the skin (not requiring withdrawal of the drug).
Symptoms: apathy, drowsiness, nausea, vomiting. These are usually reversible with supportive care. Gastrointestinal bleeding, arterial hypertension, acute renal failure, and respiratory depression may occur.
The treatment: symptomatic, supportive care of the patient; if overdose occurred within the last 4 hours – induction of vomiting, administration of activated charcoal (60-100 g per adult), osmotic laxatives. Forced diuresis, hemodialysis are ineffective due to high protein binding. There is no specific antidote to the drug.
Naise is contraindicated in pregnancy and lactation.
Naiz, Nimesil, Nimesulide, Nemulex, Nimesulide-TEVA, Nimulide, Nimesan tablets 100 mg 20 pcs, Naisulide, Mialais
|Conditions of storage|
At a temperature not exceeding 25 ºC.
Dr. Reddy's, India
gel for external use
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