Description of the active substance:
This information is a reference and it is not enough that the drug has been prescribed by a doctor ..
PHARMACHOLOGIC EFFECT
NSAIDs, in the structure of which there is a sulfonilide group. It is believed that nimesulide is a selective inhibitor of COX-2. Has a pronounced anti-inflammatory, as well as analgesic and to a lesser degree antipyretic effect. The mechanism of action is associated with inhibition of prostaglandin synthesis. Suppresses the synthesis of prostaglandins in the inflammation region to a greater extent than in the gastric mucosa or kidneys, which is due to inhibition of predominantly COX-2.
In addition, in the mechanism of anti-inflammatory action of nimesulide, its ability to inhibit the formation of free oxygen radicals (without affecting haemostasis and phagocytosis) is important and inhibit the release of the myeloperoxidase enzyme.
PHARMACOKINETICS
After ingestion, nimesulide is well absorbed from the gastrointestinal tract, C max in the blood plasma is reached after 1-2 hours.
Binding to proteins is 99%. After ingestion of a single dose of 100 mg of nimesulide is present in the tissues of female genital organs in a concentration of 40% of the concentration in the plasma.
Metabolized in the liver, the main metabolite hydroxynimidesulide has pharmacological activity.
T 1/2 from the plasma is 2-3 hours.
It is excreted from the body mainly with urine, about 98% of the dose is excreted within 24 hours. With prolonged therapy of cumulation, nimesulide is not observed.
INDICATIONS
Osteoarthritis, extra-articular rheumatic diseases, pain and inflammation after surgery, pain and fever in acute inflammatory processes in the upper respiratory tract, pain associated with dysmenorrhea.
DOSING MODE
Inside adults to 100-200 mg 2 times / day, children - 1.5 mg / kg 2-3 times / day.
The maximum dose for children is 5 mg / kg / day in 2-3 divided doses.
SIDE EFFECT
On the part of the digestive system: heartburn, nausea, stomach pain; in some cases - tarry stool, melena (associated with bleeding and erosive-ulcerative lesions of the gastrointestinal tract).
From the side of the central nervous system: rarely - headaches, dizziness, drowsiness.
Allergic reactions: skin rash, erythema, urticaria.
Other: rarely - oliguria, fluid retention in the body, local or systemic edema; in some cases - thrombocytopenic purpura.
CONTRAINDICATIONS
Peptic ulcer of the stomach and duodenum in the acute phase, acute bleeding from the gastrointestinal tract, moderate and severe hepatic insufficiency, renal failure (QC less than 30 ml / min), pregnancy, lactation; increased sensitivity to nimesulide and other NSAIDs (including acetylsalicylic acid).
PREGNANCY AND LACTATION
Nimesulide is contraindicated in pregnancy and lactation.
Direct indications of embryotoxic and tocolytic action of nimesulide are not available.
APPLICATION FOR FUNCTIONS OF THE LIVER
Contraindicated in renal failure (QC less than 30 ml / min).
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Contraindicated with moderate and severe hepatic impairment.
APPLICATION FOR CHILDREN
When used in pediatrics, dosage forms intended for children should be used. In children under the age of 6 years, when using nimesulide, external monitoring of the doctor is required.
APPLICATION IN ELDERLY PATIENTS
In case of external application, the doctor needs to monitor the condition of elderly patients with impaired renal function, liver function, and congestive heart failure.
SPECIAL INSTRUCTIONS
It should be used with caution in patients with impaired renal function, with arterial hypertension, with cardiac disorders, and visual impairment.
In case of external application, the doctor needs to monitor the condition of elderly patients with impaired renal function, liver function, and congestive heart failure.
When used in pediatrics, dosage forms intended for children should be used. In children under the age of 6 years, when using nimesulide, external monitoring of the doctor is required.
Impact on the ability to drive vehicles and manage mechanisms
Due to the fact that nimesulide ingestion can cause dizziness and drowsiness, it should be used with caution in patients engaged in potentially hazardous activities that require increased concentration of attention and rapid psychomotor reactions.
DRUG INTERACTION
Possible manifestations of drug interaction with the simultaneous ingestion of nimesulide with digoxin, phenytoin, lithium preparations, diuretics, antihypertensive drugs, other NSAIDs, anticoagulants, cyclosporine, methotrexate, oral hypoglycemic agents.
