Nimedar of the tab. of 100 mg No. 30

Pharmacological properties

Pharmacodynamics. medicine nimedar — npvp groups of metansulfonanilid, having the anti-inflammatory, anesthetizing and febrifugal effect. medical effect of medicine nimedar is caused by the fact that it interacts with a cascade of arachidonic acid and reduces biosynthesis of prostaglandins by an ingibition tsog.

Pharmacokinetics. In a human body Nimedar is well soaked up at oral administration, reaching the C _max in blood plasma through 2–3 h. Up to 97.5% of Nimesulide contacts proteins of blood plasma. Nimesulide is actively metabolized in a liver with the participation of CYP 2C9, P450 cytochrome isoenzyme. The main metabolite is parahydroxyderivative which also has pharmacological activity. T _½ — from 3.2 to 6 h. Nimesulide is removed from an organism with urine — about 50% of the accepted dose. About 29% of the accepted dose are removed with a stake in a metabolizirovanny look. Only 1-3% are brought out of an organism in not changed look. The pharmacokinetic profile at elderly people does not change.

Indication

Treatment at an acute pain, primary dysmenorrhea. Nimesulide should be applied only as medicine of the second line. the decision on prescribing of Nimesulide is required to be made on the basis of assessment of all risks for the specific patient.

Use

to minimize possible undesirable side effects, it is necessary to apply a minimal effective dose during the shortest time. it is recommended to take the medicament after consumption of food.

Maximum duration of a course of treatment the medicine Nimedar — 15 days

Adult. 100 mg of Nimesulide (1 one-dose package) 2 times a day after a meal.

Patients of advanced age. Dose adjustment is not required.

Children aged from 12 years. Dose adjustment is not required.

Patients with a renal failure. For patients with a slight or moderate renal failure (clearance of creatinine — 30–80 ml/min.) dose adjustment is not required while the heavy renal failure (clearance of creatinine of 30 ml/h) is a contraindication to Nimedar's application.

Contents of a package is poured out in a glass, dissolved in water and accepted orally.

Contraindication

Hypersensitivity to Nimesulide or any component of medicine. giperergichesky reactions in the anamnesis (bronchospasm, rhinitis, a small tortoiseshell) in connection with use of acetylsalicylic acid or others npvp. hepatotoxic reactions to Nimesulide in the anamnesis. the accompanying use of other substances with potential hepatotoxicity. the gastrointestinal bleedings or perforation in the anamnesis connected with the previous application npvp. ulcer of stomach or duodenum in an aggravation phase, existence in the anamnesis of an ulcer, perforation or bleeding in a digestive tract. existence in the anamnesis of cerebrovascular bleedings or other hemorrhages and also diseases which are followed by bleeding. heavy violations of fibrillation. heavy heart failure. heavy renal failures. abnormal liver function. the increased body temperature at the patient and/or grippopodobny symptoms. alcoholism and medicament addiction. children's age up to 12 years. iii trimester of pregnancy and period of feeding by a breast.

Side effects

from blood and lymphatic system: anemia, eosinophilia, thrombocytopenia, pancytopenia, purple.

from the immune system: hypersensitivity, anaphylaxis.

from metabolism: hyperpotassemia.

from mentality: feeling of fear, nervousness, night dreadful dreams.

from nervous system: dizziness, headache, drowsiness, encephalopathy (Ray's syndrome).

from an organ of sight: illegibility of sight, visual disturbance.

from an organ of hearing: vertigo (dizziness).

from a cardiovascular system: tachycardia, AG, hemorrhage, lability of the ABP, inflows.

from the respiratory system and bodies of mediastinum: short wind, OH, bronchospasm.

from a digestive tract: dyspepsia, diarrhea, nausea, vomiting, a lock, a meteorism, gastritis, bleedings in a digestive tract, an ulcer and perforation of a stomach or duodenum, an abdominal pain, stomatitis, a chair of black color, a hematemesis, a stomacace, exacerbation of colitis and Crohn's disease.

from a liver and a zhelchevydelitelny system: increase in level of enzymes of a liver, hepatitis, lightning (fulminantny) hepatitis with a lethal outcome, including jaundice, a cholestasia.

from skin and hypodermic cellulose: an itch, rash, an erythema, dermatitis, formation of bubbles, urticaria, a Quincke's disease, a face edema, a polymorphic erythema, Stephens's syndrome — Johnson, a toxic epidermal necrolysis, the increased sweating.

from an urinary system: dysuria, hamaturia, urination delay, renal failure, oliguria, interstitial nephrite.

General violations: hypostasis, indisposition, adynamy, hypothermia.

Most often at application of NPVP are noted by side reactions from a digestive tract.

Clinical and epidemiological trials demonstrate that some NPVP, especially in high doses and at prolonged use, can lead to emergence of arterial trombotichesky complications, for example a myocardial infarction or a stroke.

Special instructions

Undesirable side effects can be minimized, applying a minimal effective dose during the shortest period necessary for control of symptoms of a disease.

in the absence of efficiency of treatment therapy by medicine should be stopped.

during treatment by Nimesulide is recommended to avoid simultaneous use of hepatotoxic medicines and also to abstain from alcohol intake. Use of NPVP can mask the fervescence connected with a background bacterial infection. In case of fervescence or emergence of grippopodobny symptoms in the patients applying Nimesulide, administration of medicament needs to be cancelled.

. Patients at whom the symptoms similar to symptoms of damage of a liver, such as anorexia, nausea, vomiting, an abdominal pain, fatigue, dark color of urine are observed and patients at whom data of laboratory analyses of function of a liver deviate from norm have to stop administration of drug. Repeated prescribing of Nimesulide is contraindicated to such patients. During the Nimedar medicament treatment of the patient has to abstain from use of other analgetics. It is necessary to avoid the accompanying application of other NPVP, including selection TsOG-2 inhibitors.

Patients applying Nimesulide at emergence of grippopodobny symptoms have to stop its application.

frequency of undesirable reactions to NPVP is increased by

At elderly people, especially it concerns possible bleedings and perforation in a digestive tract which can be deadly.

Ulcer, bleeding or perforation in a digestive tract can threaten the patient's life, especially in the presence in the anamnesis of data that the similar phenomena arose at the patient at application of any other NPVP (without limitation period). The risk of the similar phenomena increases together with increase in a dose of NPVP at the patients having in the anamnesis the ulcer in a digestive tract which is especially complicated by bleeding or perforation and also at elderly people. Such patients should begin treatment with the minimum possible effective dose. For these patients and also for those who in parallel accept low doses of acetylsalicylic acid or other medicines increasing risk of emergence of complications from a digestive tract it is necessary to consider the possibility of application of combination therapy with use of protective substances, for example a mizoprostol or inhibitors of a proton pomp.

Sick with toxic damage of a digestive tract, especially elderly people, have to report about any unusual symptoms arising in a digestive tract, first of all about bleeding. It is especially important at initial stages of treatment. The patients taking the accompanying medicaments which increase risk of developing of an ulcer or bleeding, such as corticosteroids, anticoagulants, selective serotonin reuptake inhibitors, antithrombocytic means (acetylsalicylic acid) need to be informed on need to be careful at use of Nimesulide.

in case of emergence at the patient applying Nimedar of bleeding or ulcers of a digestive tract medicament treatment should be stopped.

NPVP with care is appointed to patients with Crohn's disease or nonspecific ulcer colitis in the anamnesis as Nimesulide can lead to their aggravation.

Simultaneous use of Nimesulide with other medicines, such as oral contraceptives, anticoagulants, antiagregant, can cause exacerbation of Crohn's disease and other diseases of a digestive tract.

Person with AG and/or heart failure in the anamnesis and also patients with a liquid delay in an organism and hypostases owing to application of NPVP demand the corresponding control of a state and consultation of the doctor.

Clinical trials and epidemiological data allow to draw a conclusion that some NPVP, especially in high doses and at prolonged use, can cause emergence of arterial trombotichesky episodes, for example a myocardial infarction and a stroke. For an exception of risk of emergence of such phenomena at use of Nimesulide of data it is not enough.

Sick with uncontrollable AG, an acute heart failure, an ischemic heart disease, diseases of peripheral arteries and/or cerebrovascular diseases should appoint Nimesulide by

only after careful assessment of a state. It also touches faces with risk factors of developing cardiovascular diseases, for example AG, lipidemias, diabetes, smoking.

Sick with a renal failure or with heart failure should appoint medicine by

with care in connection with a possibility of deterioration in kidney function. In case of aggravation of symptoms of the patient the treatment is required to be stopped.

Patients of advanced age demand careful observation as development of bleedings and a perforatsy GIT, deterioration in function of kidneys, a liver or heart is possible. As Nimesulide can influence function of platelets, it is necessary to appoint it with care the patient with hemorrhagic diathesis. However Nimesulide does not replace acetylsalicylic acid at prevention of cardiovascular diseases.

, some of them can be deadly, for example: exfoliative dermatitis, Stephens's syndrome — Johnson, a toxic epidermal necrolysis. If within the first month of earlier appointed course of treatment there were these reactions, then the risk of their development in patients considerably increases. The medicament Nimedar needs to be cancelled at emergence of the first symptoms of skin rash, damage of a mucous membrane and other allergic reactions.

Use of Nimesulide can break female fertility and is not recommended to the women planning pregnancy. Women, it is difficult to them to become pregnant or which undergo inspection concerning infertility are not recommended to appoint Nimesulide.

Use during pregnancy and feeding by a breast. Suppression of synthesis of prostaglandins can adversely influence pregnancy and/or fetation. The data received at epidemiological researches allow to draw a conclusion that in the early stages of pregnancy the use of the medicines suppressing prostaglandin synthesis increases risk of a misbirth, emergence at a fruit of heart diseases and a gastroshizis. Absolute risk of development of anomaly of a cardiovascular system increases from 1 to ≈1.5%. It is considered that the risk increases with increase in a dose and increase in duration of application.

should not accept Nimesulide in I and II trimester of pregnancy without emergency. In case of prescribing of medicine the women who try to become pregnant or in I and II trimester of pregnancy should choose the minimum possible dose and the smallest possible duration of treatment.

all inhibitors of synthesis of prostaglandin can lead

In the III trimester of pregnancy to development in a fruit:

• cardiopulmonary toxic defeat (with premature closing of arterial channels and hypertensia in the system of a pulmonary artery);
• dysfunction of kidneys which can progress to a renal failure with development of an oligoamnios.

At mother and a fruit at the end of pregnancy perhaps:

• increase in a bleeding time and anti-aggregation effect which can arise even at use of medicine in very low doses;
• suppression of sokratitelny activity of a uterus that can lead to a delay or lengthening of the period of childbirth.

Therefore Nimesulide is contraindicated to

in the III trimester of pregnancy.

Use of Nimesulide can worsen fertile function at women therefore the women trying to become pregnant are not recommended to appoint medicine. The women who are experiencing difficulties with approach of pregnancy or passing researches on an infertility occasion should stop use of Nimesulide. If pregnancy is established during use of Nimesulide, then the doctor has to be informed on it.

As NPVP oppress synthesis of prostaglandins, Nimesulide can cause premature closing batalovy channels, pulmonary hypertensia, an oliguria, an oligoamnios. Risk of developing bleeding, weakness of patrimonial activity and peripheral hypostasis increases. Newborns whose mothers applied Nimesulide at the end of pregnancy have data on developing of a renal failure. Researches on animals proved atypical reproductive toxicity of medicine, but there are no reliable data concerning use of Nimesulide for pregnant women.

As does not know to

whether Nimesulide gets into breast milk, its application is contraindicated during feeding by a breast.

Children. The medicament Nimedar aged up to 12 years is contraindicated to children.

Ability to influence speed of response at control of vehicles or work with other mechanisms. Researches of influence of Nimesulide on ability to steer vehicles or work with other mechanical means were not conducted, but if at use of Nimesulide for patients there is a headache, dizziness or drowsiness, then they should refuse control of vehicles or work with other mechanisms.

Interaction

Pharmakodinamichesky interactions. corticosteroids: the risk of developing of an ulcer of a digestive tract or bleeding increases.

Antithrombocytic means and selective serotonin reuptake inhibitors: the risk of developing of bleedings in a digestive tract increases.

Anticoagulants: NPVP can strengthen effect of anticoagulants, such as warfarin or acetylsalicylic acid therefore such combination is contraindicated to patients with heavy violations of coagulation. If such combination therapy cannot be avoided, it is necessary to carry out careful control of indicators of fibrillation.

Diuretic means, APF inhibitors and antagonists of angiotensin II. NPVP can weaken effect of diuretics and other antihypertensive medicines. At some patients with reduced function of kidneys (for example at the dehydrated patients or elderly people) at the combined use of the APF inhibitors, antagonists of angiotensin II or substances suppressing the COG system, perhaps further deterioration in function of kidneys and emergence of OPN which, as a rule, is reversible. These interactions should be considered when the patient uses the medicament Nimedar combined with APF inhibitors or antagonists of angiotensin II. It is necessary to be careful, applying such combination, especially to elderly people. Patients have to receive enough liquid, and renal function is required to be controlled carefully after the beginning of application of such combination. Nimesulide temporarily weakens effect of furosemide concerning removal of sodium and to a lesser extent — concerning potassium removal and also reduces diuretic effect. The combined use of furosemide and Nimedar for patients with violation of kidney or warm function demands care.

At healthy volunteers Nimesulide quickly reduces the effect of furosemide directed to removal of sodium and to a lesser extent — to potassium removal and also reduces diuretic action. Simultaneous use of Nimesulide and furosemide leads to reduction (for ≈20%) to AUC and decrease in cumulative excretion of furosemide without changes of kidney clearance of furosemide.

Pharmacokinetic interactions with other medicines. There were messages that NPVP reduce clearance of lithium that leads to increase in level of lithium in blood plasma and toxicity of lithium. When prescribing the medicine Nimedar the patients performing therapy by lithium medicines should carry out regularly control of level of lithium in blood plasma.

does not have

clinically significant interaction with glibenclamide, theophylline, warfarin, digoxin, Cimetidinum and antiacid medicines (combination of aluminum and magnesium of hydroxide) in vivo. Nimesulide suppresses activity of CYP enzyme 2C9. At simultaneous application with Nimedar of the medicines which are substrates of this enzyme, their concentration in blood plasma can increase. The care is required in case Nimesulide is appointed less than for 24 h to or less than for 24 h after reception of a methotrexate as increase in level of the last in blood serum and increase in its toxicity is possible.

Thanks to influence on renal prostaglandins inhibitors sintetaz to which Nimesulide belongs can increase nephrotoxicity of cyclosporines.

Influence of other medicines on Nimesulide. The researches in vitro showed that Nimesulide is forced out from places of binding by tolbutamide, salicylic acid and valproic acid. In spite of the fact that these interactions were defined in blood plasma, the specified effects were not noted in the course of clinical use of medicine.

Overdose

Symptoms of sharp overdose npvp are usually limited to

such as: apathy, drowsiness, nausea, vomiting, pain in epigastric area. these symptoms, as a rule, are reversible at maintenance therapy. developing of gastrointestinal bleeding, ag, opn, respiratory depressions, a coma is possible, however such phenomena note seldom. there were messages about anaphylactoid reactions at application npvp in therapeutic doses and at their overdose. there is no specific antidote. treatment at overdose — symptomatic and supporting. there are no data on removal of Nimesulide by means of a hemodialysis, but if to take into account high extent of linking of Nimesulide with proteins of blood plasma (to 97.5%), then it is improbable that dialysis will be effective.

or after administration of medicament in a high dose during 4 h after its reception to patients can appoint by

in the presence of symptoms of overdose artificial calling of vomiting and/or intake of activated carbon (60–100 g for adults), osmotic depletive. The artificial diuresis, increase in alkalinity of urine, a hemodialysis and hemoperfusion can be inefficient because of high extent of linking of Nimesulide with proteins of blood plasma. It is necessary to control functions of kidneys and a liver.

Storage conditions

In original packing at a temperature not above 25 °C.