Nise pills 100mg №30

pharmachologic effect

NSAIDs from the class of sulfonanilides. It is a selective competitive inhibitor of COX-2, inhibits the synthesis of prostaglandins in the focus of inflammation. The inhibitory effect on COX-1 is less pronounced (less likely to cause side effects associated with inhibition of prostaglandin synthesis in healthy tissues). It has anti-inflammatory, analgesic and pronounced antipyretic effect.

Pharmacokinetics

Suction

After oral Nimesulide is well absorbed from the gastrointestinal tract. Eating reduces the rate of absorption without affecting its degree. C_max nimesulide is 3.5-6.5 mg / l.

Distribution

Plasma protein binding is 95%, with erythrocytes - 2%, with lipoproteins - 1%, with acidic α₁- 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 the tissue of the female genital organs, where after a single dose, the concentration of nimesulide is about 40% of the concentration in plasma. It penetrates well into the acidic environment of the focus of inflammation (40%), synovial fluid (43%). Easily penetrates histohematogenous barriers.

Metabolism

Nimesulide 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 is able to quickly diffuse through the hydrophobic channel of COX-2 to the active binding center of the methyl group. 4-hydroxynimesulide is a water-soluble compound, for the elimination of which glutathione and conjugation reactions of the second phase of metabolism (sulfation, glucuronide and others) are not required.

Removal

T_1/2 nimesulide is 1.56-4.95 h, T_1/2 4-hydroxynimesulide - 2.89–4.78 h. The metabolite is excreted by the kidneys (65%) and, with bile (35%), undergoes enoterohepatic recirculation.

Pharmacokinetics in special clinical situations

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;

- osteoarthritis;

- myalgia of rheumatic and non-rheumatic genesis;

- inflammation of ligaments, tendons, bursitis, incl. post-traumatic inflammation of soft tissues;

- pain syndrome of various genesis (including in the postoperative period, with injuries, algomenorrhea, toothache, headache, arthralgia, lumbar ischalgia).

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

Dosing regimen

The drug should be used in the minimum effective dose of the shortest possible course. pills are taken with a sufficient amount of water, preferably after meals. In the presence of gastrointestinal diseases, it is desirable to take the drug at the end of a meal or after a meal.

Adults and children over 12 years old - inside 1 tab. 2 times / day. The maximum daily intake for adults is 200 mg.

Patients with chronic renal failure required reduction in 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 messages.

Allergic reactions:rarely, hypersensitivity reactions; very seldom - urticaria, angioedema, anaphylactoid reactions.

From the side of the central nervous system:infrequently - dizziness; rarely - a feeling of fear, nervousness, nightmares; very rarely - headache, drowsiness, encephalopathy (Reye's syndrome).

From the skin:infrequently - itching, rash, increased sweating; rarely - erythema, dermatitis; very rarely - swelling of the face, multiforme exudative erythema, incl. Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome).

Urogenital:infrequently - swelling; rarely - dysuria, hematuria, urinary retention, hyperkalemia; very rarely - renal failure, oliguria, interstitial nephritis.

Gastrointestinal:often - diarrhea, nausea, vomiting; infrequently - constipation, flatulence, gastritis; very rarely - abdominal pain, stomatitis, tarry stools, Gastrointestinal bleeding, ulcers and / or perforation of the stomach or duodenum.

Liver and biliary system:often - increased hepatic transaminases; very rarely - hepatitis, fulminant hepatitis, jaundice, cholestasis.

From the side of blood-forming organs:rarely - anemia, eosinophilia; very rarely - thrombocytopenia, pancytopenia, purpura, lengthening of the bleeding time.

Respiratory:infrequently - shortness of breath; very rarely - exacerbation of asthma, bronchospasm.

Special senses:rarely blurred vision.

Cardiovascular:infrequently - arterial hypertension; rarely - tachycardia, hemorrhage, hot flashes.

Other:rarely, general weakness; very rarely - hypothermia.

Contraindications

- A complete or incomplete combination of asthma, recurrent nasal polyposis or paranasal sinuses and intolerance to Acetylsalicylic acid and other NSAIDs (including a history of);

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

- active gastrointestinal bleeding;

- cerebrovascular or other bleeding;

- inflammatory bowel disease (Crohn's disease, ulcerative colitis) in the acute phase;

- hemophilia and other bleeding disorders;

- decompensated heart failure;

- liver failure or any active liver disease;

- indications in the history of the development of hepatotoxic reactions in the use of drugs nimesulide;

- concomitant use of potentially hepatotoxic substances;

- alcoholism, drug addiction;

- renal failure severe (CC <30 ml / min);

- progressive kidney disease;

- confirmed hyperkalemia;

- the period after coronary artery bypass surgery;

- pregnancy;

- lactation period (breastfeeding);

- children's age up to 12 years;

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

with caution:IHD, cerebrovascular diseases, congestive heart failure, arterial hypertension, dyslipidemia / hyperlipidemia, diabetes mellitus, diseases of the peripheral arteries, QC <60 ml / min, a history of the development of ulcerative gastrointestinal lesions, the presence of Helicobacter pylori infection, severe diseases of the gastric ulcer, the presence of Helicobacter pylori infection, severe diseases of the ulcer ulcer of the gastrointestinal anticoagulants (for example, warfarin), antiplatelet agents (for example, acetylsalicylic acid, clopidogrel), oral GCS (for example, prednisolone), selective serotonin reuptake inhibitors ( for example, citalopram, Fluoxetine, paroxetine, sertraline), long-term use of NSAIDs, advanced age, smoking, frequent use of alcohol.

Use during pregnancy and lactation

Use of the drug is contraindicated.^® during pregnancy and lactation (breastfeeding).

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

Application for violations of the liver

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

Application for violations of kidney function

Contraindicated in severe renal failure (CC <30 ml / min), with progressive kidney disease.

Patients with chronic renal failure required reduction in daily dose to 100 mg.

Use in children

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

Use in elderly patients

with caution the drug 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 QC.

Considering reports of visual impairment in patients taking other NSAIDs, treatment should be stopped immediately if any visual impairment appears and the eye doctor should examine the patient.

The drug can cause fluid retention in the tissues, therefore, patients with high blood pressure and cardiovascular disorders Nise^® should be used with extreme caution.

Regular medical supervision is required if the patient, along with nimesulide, takes medications that are characterized by an effect on the gastrointestinal tract.

If there are signs of liver damage (skin itching, jaundice of the skin, nausea, vomiting, abdominal pain, dark urine, increased activity of hepatic transaminases), you should stop taking the drug and consult your doctor.

Do not use the drug at the same time as other NSAIDs.

The drug can change the properties of platelets, but does not replace the prophylactic action of acetylsalicylic acid in cardiovascular diseases.

After 2 weeks of use of the drug, control of biochemical parameters of liver function is necessary.

Use in pediatrics

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

Influence on ability to drive motor transport and control mechanisms

The drug can cause drowsiness, dizziness and blurred vision, so care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and psychomotor speed.

Overdose

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

Treatment: conducting symptomatic and supportive therapy. There is no specific antidote. If an overdose occurred during the last 4 hours, it is necessary to induce vomiting, to receive Activated carbon (60-100 g per adult), osmotic laxatives. Forced diuresis, hemodialysis are ineffective because of the high degree of drug binding to plasma proteins.

Drug interaction

The action of drugs that reduce blood clotting, increases with their simultaneous use with nimesulide.

Nimesulide can reduce the effects of Furosemide.

Nimesulide may increase the possibility of adverse reactions while taking Methotrexate.

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