Nimesulide - instructions for use, dose, side effects, contraindications

Nimesulide is a non-steroidal anti-inflammatory drug (NSAID) from the sulfonanilide class. The action of nimesulide is associated with inhibition of the enzyme activity, which provides the synthesis of prostaglandins cyclooxygenase (COX). The drug has anti-inflammatory, analgesic and antipyretic effects. For nimesulide is characteristicgreater inhibitory activity against COX-2 and a lower affinity for COX-1.

Pharmacokinetics:

After oral administration nimesulide well absorbed from the gastrointestinal tract. The maximum concentration of active substance in the blood plasma after a single application in a dose of 100 mg is achieved after 1.5-2.5 hours after administration. Value AUC (area - under the pharmacokinetic curve "concentration-time") is 20-35 mg / l * h. At repeated admission in a dose of 100 mg 2 times a day, during 7 days there was no statistically significant difference from these figures. Binding to plasma proteins is about 97.5%.

Nimesulide is metabolized in the liver in various ways, including by using the cytochrome isoenzyme, P450 (CYP 2C9), so there is a possibility of its interaction with drugs that are metabolized with the participation of isoenzyme CYP 2C9. The main metabolite of nimesulide, para-hydroxy derivative, also has pharmacological activity. Time before the appearance of this metabolite in the blood is short (0,8 h), but its constant formation is small and significantly lower than the absorption constant of nimesulide. Hydroxynimesulide is the only metabolite found in blood plasma, it is almost completely conjugated. The period of its The elimination half-life is 3.2-6 h. Nimesulide is excreted mainly with urine (about 50% of the dose taken), only 1-3%. is displayed unchanged. Hydroxynimesulide, its main, metabolite, is detected in the urine only in the form of a glucuronide conjugate. About 29 % The dose is excreted with feces after metabolism. The kinetic profile of nimesulide in elderly people does not change. At moderately. marked renal failure (creatinine clearance 30-80 ml / min), the maximum concentration of nimesulide and its main metabolite in the blood plasma is not higher than in healthy volunteers. Repeated reception does not result in cumulation in the body.

Indications:

Rheumatoid arthritis, osteoarthritis, arthritis-various etiology, tendonitis, bursitis, acute pain syndrome; Algodismenorea, myalgia, dental and headache.

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

Contraindications:

Hypersensitivity, complete or incomplete combination, bronchial asthma, nasal polyposis retsidaviruyuschego or paranasal sinuses and intolerances atsetipsalischshovoy acid and other nonsteroidal anti-inflammatory drugs, erosive ulcerous lesion of gastric mucosa and 12the rectum, active gastrointestinal bleeding, cerebrovascular or other bleeding, inflammatory bowel disease (Crohn's disease, ulcerative colitis) in the acute phase, hemophilia and other bleeding disorders systems, decompensated congestive heart failure, hepatic insufficiency or any liver active disease, hepatotoxicity when using nimesulide in anamnesis, alcoholism, drug addiction, severe chronic renal failure, (creatinine clearance less than 30 ml / min), pr gressiruyuschee kidney disease confirmed, hyperkalemia since the aortocoronary bypass,simultaneous reception of other genototoxic drugs, pregnancy, the period of "lactation, children's age before 12 -let, lactase deficiency, lactose intolerance, glucose-galactose malabsorption.

Carefully:Coronary heart disease, cerebrovascular diseases, chronic heart failure, dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral arterial disease, smoking, kidney failure (creatinine clearance 30-60 ml / min), anamnestic data on the development of gastrointestinal ulcer, infection Helicobacter pylori, old age, prolonged use of NSAIDs, alcoholism; severe somatic diseases, simultaneous reception of anticoagulants (including warfarin), antiaggregants (including, acetylsalicylic acid, clopidogrel), oral glucocorticosteroids, selective serotonin reuptake inhibitors (including citalopram; fluoxetine, paroxetine, sertraline).

Pregnancy and lactation:

The use of the drug during pregnancy and breastfeeding is contraindicated.If you need to use the drug during breastfeeding, breastfeeding should be discarded.

The use of nimesulide may adversely affect female fertility, so the drug is not recommended for women planning a pregnancy, especially if a woman ;, undergoes a test for infertility. Since it is not known whether nimesulide in breast milk, the use of nimesulide is contraindicated in the period of breastfeeding.

Dosing and Administration:

Inside, after eating, drink plenty of water.

Adults: 100 mg (1 tablet) 2 times a day.

Children over 12 years of age with a body weight of more than 40 kg: 100 mg (1 tablet) 2 times a day. The maximum daily dose is 200 mg.

Children over 12 years of age with a body weight of less than 40 kg: from the calculation of a single dose of 1.5 mg / kg of body weight 2-3 times per day. The maximum daily dose is 5 mg / kg.

A minimum effective dose should be used with the minimum possible short course. Duration of treatment should not exceed 15 days.

Correction of dose to elderly patients is not required.

Side effects:

The frequency of adverse reactions listed below was determined according to the following: very often> =1/10; often> 1/100, <1/10; infrequently> 1/1000, <1/100; rarely>1/10 000, <1/1000; very rarely < 1/10 000, including individual messages.

Allergic reactions: infrequently - itchy skin rash; rarely erythema, exanthema; very rarely urticaria, toxic epidermal, necrolysis (Lyell's syndrome), Stevens-Johnson syndrome, angioedema, bronchospasm, anaphylactic shock.

From the side of the gastroduodenal tract: often - heartburn, nausea, vomiting; diarrhea; infrequently - constipation, bloating, gastritis; very rarely - pain in the stomach, ulceration of the mucous membrane of the gastrointestinal tract, tarry stool, melena, increased activity of hepatic transaminases, toxic hepatitis (including fatal outcome), ulcer and / or perforation of the stomach or 12the rectum.

From the central nervous system: not often - dizziness; rarely anxiety, irritability, sleep disorder, nightmares; very rarely, headache, encephalopathy, drowsiness, Reye's syndrome.

Co side of the blood and lymphatic system: rarely - anemia, eosinophilia, lengthening of bleeding time; very rarely - thrombocytopenia, agran ulocytosis, pancytopenia, - purpura.

From the side of the kidneys and urinary tract: rarely - dysuria, hematuria, urinary retention; very rarely - oliguria, renal insufficiency, interstitial nephritis.

Cardiovascular system: infrequently - increased blood pressure; rarely - tachycardia, palpitation, "hot flashes".

Other: infrequently^_ swelling, shortness of breath; rarely - visual impairment, vertigo, malaise, asthenia, hyperkalemia; very rarely - hypothermia.

If any of the side effects indicated in the instruction are aggravated, or if you notice any other side effects not listed in the instructions, inform the doctor about it.

Overdose:

When an overdose is observed lethargy, drowsiness, nausea, vomiting, pain in epigastric region, gastrointestinal bleeding, arterial hypertension, epileptic seizures, acute renal failure, respiratory depression, anaphylactic reactions, and coma.

In case of an overdose of nimesulide, symptomatic or maintenance therapy is indicated. There is no specific antidote.

There is no information on the excretion of nimesulide in hemodialysis, it has a high degree of binding to plasma proteins (97.5%), hemodialysis is most likely useless.

Nimesulide is also not excreted when taking diuretics and when applying hemoperfusion, urine alkalization, forced diuresis.

If an overdose has occurred within the last 4 hours, you should take Activated carbon (60-100 g for adults), a drug that causes vomiting or an osmotic laxative. In case of an overdose, it is necessary to monitor kidney and liver function.

Interaction:

Nimesulide inhibits isoenzyme CYP 2C9, therefore the concentration in, blood plasma of drugs metabolized with the participation of this isoenzyme, while using with nimesulide can increase.

With simultaneous use with antiepileptic drugs (valproic acid), antifungal agents (ketoconazole), antituberculous drugs (isoniazid), amiodarone, methotrexate, methyldopa, amoxicillin in combination with clavulanic acid, additive hepatotoxic effect is possible. Care should be taken if the interval between taking nimesulide and methotrexate is less than 24 hours. Nimesulide may increase the possibility of side effects with simultaneous administration of methotrexate.

Possible loss of nephrotoxicity of cyclosporine with simultaneous application with nimesulide.

Nimesulide can reduce the oral bioavailability of furosemide, therefore, reduces the effectiveness of furosemide action on glomerular filtration, renal blood flow. The simultaneous use of nimesulide and furosemide requires caution in patients with impaired renal and cardiac function.

Simultaneous reception of nimesulide with warfarin and similar anticoagulants, acetylsalicylic acid is not recommended, as the risk of bleeding increases, and patients with severe blood clotting disorder are contraindicated. If the use of such a combination is necessary, control of the action of anticoagulants is required.

There are data that non-steroidal anti-inflammatory drugs reduce the clearance of lithium, which leads to an increase in the concentration of lithium in the blood plasma and increase its toxicity. Therefore, with the simultaneous use of nimesulide andLithium it is necessary to regularly monitor the concentration of lithium in the blood plasma. Clinically significant interactions of nimesulide with glibenclamide, theophylline, digoxin, cimetidane, and antacids (combinations of aluminum and magnesium compounds) have not been identified.

Special instructions:

When appearing in patients receiving nimesulide, symptoms indicative of liver damage (eg, anorexia, nausea, vomiting, abdominal pain, increased fatigue, dark urine), or abnormal results of functional hepatic samples, the drug should be discontinued. Such patients are not recommended to take nimesulide and further.

During treatment with nimesulide, simultaneous use of hepatotoxic drugs, analgesics, other NSAIDs (with the exception of low doses of acetylsalicylic acid used in antiplatelet doses) and the use of ethanol should be avoided.

Gastrointestinal bleeding or ulcer / perforation can develop at any time with the use of the drug, with or without warning signs, both with and without gastrointestinal complications in the history. If there is a gastrointestinal bleeding or ulcers, the drug should be discarded.

If the kidney function worsens, the drug should be discarded.

Patients with hemorrhagic diathesis nimesulide should be used under constant supervision.

After two weeks of using the drug should be monitored the activity of hepatic transaminases. "

In elderly patients the most frequent side effects are when taking the drug, including gastrointestinal bleeding, perforation, impaired heart, kidney and liver function, so regular clinical monitoring of the patient's condition is recommended.

Effect on the ability to drive transp. cf. and fur:

Due to nimesulide may cause dizziness and drowsiness, care should be taken when driving vehicles, while servicing moving mechanisms, and when engaging in other potentially hazardous activities requiring increased attention and speed of psychomotor reactions.

Form release / dosage:

Tablets of 100 mg.

By 10, 15, 20, 30 tablets into a contour cell pack of film

polyvinylchloride and aluminum foil printed lacquered.

For 1, 2, 3, 4, 5, 6 contour mesh packages together with instructions for use in a pack of cardboard.

Storage conditions:

In a dry, protected from light place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-001625

Date of registration:05.04.2012

The owner of the registration certificate:OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC Russia

Manufacturer: & nbsp

OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC Russia

Information update date: & nbsp14.08.2015

Illustrated instructions

Instructions

Nimesulide (Nimesulid)