Naise, gel 1% 20 g

Pharmacological action – analgesic, antipyretic, anti-inflammatory.

Pharmacodynamics

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.

Pharmacokinetics

Absorption when taken orally is high. Food intake reduces the rate of absorption without affecting its degree. T_max 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. C_max is 3.5-6.5 mg/L. V_d – 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 T_1/2 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.

Indications

Active ingredient

How to take, the dosage

Interaction

With caution, use simultaneously with diuretics, blood pressure medications, other analgesic anti-inflammatory drugs, anti-diabetic drugs.

Special Instructions

Contraindications

Side effects

Overdose

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.

Pregnancy use

Naise is contraindicated in pregnancy and lactation.

Similarities