Universal reference book for medicines
Name of the drug: NICE® (NISE)

Active substance: nimesulide

Type: NSAIDs.
Selective COX-2 inhibitor
Manufacturer: DR.
REDDY`S LABORATORIES (India)
Composition, form of production and packaging
Tablets of
white color with a yellowish shade, round, biconcave, with a smooth surface.

1 tab.

nimesulide 100 mg

Excipients: calcium hydrophosphate 75 mg, microcrystalline cellulose (type 114) 40 mg, corn starch 54 mg, sodium carboxymethyl starch 35 mg, magnesium stearate 3 mg, silicon dioxide colloid 2 mg, talc 1 mg.

10 pieces.
- blisters (1) - packs of cardboard.
10 pieces.
- blisters (2) - packs of cardboard.
10 pieces.
- blisters (10) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2015.

PHARMACHOLOGIC EFFECT

NSAIDs from the sulfonanilide class.
It is a selective competitive inhibitor of COX-2, inhibits the synthesis of prostaglandins in the inflammatory focus. The inhibitory effect on COX-1 is less pronounced (it rarely causes side effects associated with the inhibition of prostaglandin synthesis in healthy tissues). Has anti-inflammatory, analgesic and pronounced antipyretic effect.
PHARMACOKINETICS

Suction

After ingestion, nimesulide is well absorbed from the digestive tract.
The intake of food reduces the rate of absorption, without affecting its degree. C max nimesulide is 3.5-6.5 mg / l.
Distribution

Binding to plasma proteins is 95%, with erythrocytes - 2%, with lipoproteins - 1%, with acidic?
1- glycoproteins - 1%. The dose of the drug does not affect the degree of binding to blood proteins.
V d is 0.19-0.35 l / kg.
Penetrates into the tissue of the female genital organs, where after a single intake the concentration of nimesulide is about 40% of the concentration in the plasma. It penetrates into the acidic environment of the inflammatory focus (40%), synovial fluid (43%). Easily penetrates through the histohematological barriers.
Metabolism

Nimesulide is metabolized in the liver by tissue monooxygenases.
The main metabolite, 4-hydroxynimidesulide (25%), has similar pharmacological activity, but due to the reduction in the size of the molecules it is able to rapidly diffuse along the hydrophobic COX-2 channel to the active methyl group binding site. 4-hydroxyimidesulide is a water-soluble compound, for the removal of which glutathione and conjugation reactions of the second phase of metabolism (sulfation, glucuronidation and others) are not required.
Excretion

T 1/2 of nimesulide is 1.56-4.95 h, T 1/2 of 4-hydroxynimidesulide is 2.89-4.78 h. The metabolite is excreted by the kidneys (65%) and with bile (35%), is subjected to enethrohepatic recirculation.

Pharmacokinetics in special clinical cases

In patients with renal insufficiency (CK 30-80 ml / min), as well as in children and the elderly, the pharmacokinetic profile of nimesulide does not change significantly.

INDICATIONS

- rheumatoid arthritis;

- articular syndrome with exacerbation of gout;

- psoriatic arthritis;

ankylosing spondylitis;

osteochondrosis with radicular syndrome;

- osteoarthrosis;

- myalgia of rheumatic and non-rheumatic origin;

- inflammation of ligaments, tendons, bursitis, incl.
post-traumatic inflammation of soft tissues;
- pain syndrome of various genesis (including in the postoperative period, with trauma, algodismenorea, toothache, headache, arthralgia, lumboeishalgia).

The drug is intended for symptomatic therapy, reducing pain and inflammation at the time of use, the progression of the disease is not affected.

DOSING MODE

The drug should be applied at the lowest effective dose with the minimum possible short course.
Tablets are taken with a sufficient amount of water, preferably after eating. If there are diseases of the digestive tract, it is advisable to take the drug at the end of the meal or after eating.
Adults and children over 12 years - inside 1 tab.
2 times / day. The maximum daily intake for adults is 200 mg.
Patients with chronic renal failure require a reduction in the daily dose to 100 mg.

SIDE EFFECT

Determination of the frequency of side effects: often (1-10%), infrequently (0.1-1%), rarely (0.01-0.1%), very rarely (<0.01%), including individual reports.

Allergic reactions: rarely - hypersensitivity reactions;
very rarely - hives, angioedema, anaphylactoid reactions.
From the side of the central nervous system: infrequently - dizziness;
rarely - a sense of fear, nervousness, nightmarish dreams; very rarely - headache, drowsiness, encephalopathy (Reye syndrome).
On the part of the skin: infrequently - itching, rash, increased sweating;
rarely - erythema, dermatitis; very rarely - puffiness of the face, multi-form exudative erythema, incl. Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome).
From the urinary system: rarely - swelling;
rarely - dysuria, hematuria, urinary retention, hyperkalemia; very rarely - renal failure, oliguria, interstitial nephritis.
On the part of the digestive system: often - diarrhea, nausea, vomiting;
infrequently - constipation, flatulence, gastritis; very rarely - abdominal pain, stomatitis, tarry stool, gastrointestinal bleeding, ulcer and / or perforation of the stomach or duodenum.
From the liver and bile excretory system: often - increased hepatic transaminases;
very rarely - hepatitis, fulminant hepatitis, jaundice, cholestasis.
On the part of the organs of hematopoiesis: rarely - anemia, eosinophilia;
very rarely - thrombocytopenia, pancytopenia, purpura, prolonged bleeding time.
From the respiratory system: infrequently - shortness of breath;
very rarely - exacerbation of bronchial asthma, bronchospasm.
From the senses: rarely - blurred vision.

From the side of the cardiovascular system: infrequently - arterial hypertension;
rarely - tachycardia, hemorrhages, hot flashes.
Other: rarely - general weakness;
very rarely - hypothermia.
CONTRAINDICATIONS

- complete or incomplete combination of bronchial asthma, recurrent nasal polyposis or paranasal sinuses and intolerance to acetylsalicylic acid and other NSAIDs (including in the anamnesis);

- erosive and ulcerative changes in the mucous membrane of the stomach and duodenum;

- active gastrointestinal hemorrhage;

- cerebrovascular or other bleeding;

- Inflammatory bowel disease (Crohn's disease, ulcerative colitis) during the exacerbation phase;

- hemophilia and other disorders of blood coagulability;

Decompensated heart failure;

- liver failure or any active liver disease;

- indications in the anamnesis for the development of hepatotoxic reactions with the use of nimesulide preparations;

- concomitant use of potentially hepatotoxic substances;

- Alcoholism, drug addiction;

- renal failure of severe degree (CK <30 ml / min);

progressive kidney disease;

- confirmed hyperkalemia;

- period after aortocoronary shunting;

- Pregnancy;

- the period of lactation (breastfeeding);

- children's age till 12 years;

- Hypersensitivity to the active substance or auxiliary components of the drug.

With caution: IHD, cerebrovascular disease, congestive heart failure, arterial hypertension, dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral arterial disease, CC <60 ml / min, history of the development of gastric ulcer, presence of Helicobacter pylori infection, severe somatic diseases , concomitant anticoagulant therapy (eg, warfarin), antiplatelet agents (eg, acetylsalicylic acid, clopidogrel), oral GCS (eg, prednisolone), selective reverse transcriptase inhibitors
serotonin (eg, citalopram, fluoxetine, paroxetine, sertraline), prolonged use of NSAIDs, elderly age, smoking, frequent use of alcohol.
PREGNANCY AND LACTATION

Contraindicated in the use of Nise ® during pregnancy and lactation (breastfeeding).

The use of the drug may adversely affect female fertility and is not recommended for women planning pregnancy.

APPLICATION FOR FUNCTIONS OF THE LIVER

Contraindicated in renal failure of severe degree (CK <30 ml / min), with progressive diseases of the kidneys.

Patients with chronic renal failure require a reduction in the daily dose to 100 mg.

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

Contraindicated in hepatic insufficiency or any active liver disease, history of development of hepatotoxic reactions with the use of nimesulide drugs, concomitant use of potentially hepatotoxic substances.

APPLICATION FOR CHILDREN

The use of tablets (100 mg) is contraindicated in childhood to 12 years, tablets dispersible (50 mg) in children under 7 years of age.

APPLICATION IN ELDERLY PATIENTS

With caution should be used in elderly patients.

SPECIAL INSTRUCTIONS

Since nimesulide is partially excreted by the kidneys, its dose for patients with impaired renal function should be reduced, depending on the value of the CC.

Given reports of visual impairment in patients taking other NSAIDs, treatment should be stopped immediately if any visual impairment occurs and the oculist should examine the patient.

The drug can cause fluid retention in the tissues, so patients with high blood pressure and with cardiac abnormalities Naise ® should be used with extreme caution.

Regular medical supervision is required if the patient, along with nimesulide, takes medications for which the effect on the digestive tract is characteristic.

If there are signs of liver damage (itchy skin, icterus of the skin, nausea, vomiting, abdominal pain, darkening of the urine, increased activity of liver transaminases), stop taking the drug and consult a doctor.

Do not use the drug simultaneously with other NSAIDs.

The drug can alter the properties of platelets, but does not replace the preventive effect of acetylsalicylic acid in cardiovascular diseases.

After 2
weeks of drug use requires monitoring of biochemical parameters of liver function.
Use in Pediatrics

The drug is contraindicated in children under 12 years of age.

Impact on the ability to drive vehicles and manage mechanisms

The drug can cause drowsiness, dizziness and blurred vision, so you need to be careful when driving and taking other potentially dangerous activities that require increased concentration and speed of psychomotor reactions.

OVERDOSE

Symptoms: apathy, drowsiness, nausea, vomiting, gastrointestinal bleeding, increased blood pressure, acute renal failure, respiratory depression.

Treatment: symptomatic and maintenance therapy.
There is no specific antidote. In case an overdose has occurred within the last 4 hours, it is necessary to induce vomiting, to receive activated charcoal (60-100 g per adult person), osmotic laxatives. Forced diuresis, hemodialysis are ineffective because of the high degree of binding of the drug to plasma proteins.
DRUG INTERACTION

The effect of drugs that reduce blood coagulability, increases with their simultaneous use with nimesulide.

Nimesulide is able to reduce the action of furosemide.

Nimesulide may increase the possibility of developing adverse reactions while taking methotrexate.

The concentration of lithium in plasma increases with simultaneous intake of lithium and nimesulide preparations.

Because of the high degree of binding of nimesulide to plasma proteins, patients who are treated with hydantoin and sulfonamides at the same time should be under the supervision of a physician, passing the examination at short intervals.

Nimesulide can enhance the action of cyclosporin on the kidneys.

When used simultaneously with SCS, serotonin reuptake inhibitors increase the risk of developing gastrointestinal bleeding.

TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

The drug should be stored out of reach of children, dry, protected from light at a temperature of no higher than 25 ° C.
Shelf life - 3 years.
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