Instruction for use: Nimesil

Active substance Nimesulide

ATX code M01AX17 Nimesulide

Pharmacological group

Other non-narcotic analgesics, including non-steroidal and other anti-inflammatory drugs

Nosological classification (ICD-10)

K08.8.0 * Painful toothache

Dentinal pain, Dentinal pains, Pain pulpitis, Anesthesia in dentistry, Pain syndromes in dental practice, Pain after removal of tartar, Pain when extracting a tooth, Toothache, Pain after dental interventions

M19.9 Arthrosis, unspecified

Change in brush with osteoarthritis, Osteoarthritis, Osteoarthrosis, Arthrosis of large joints, Pain syndrome in osteoarthritis, Pain syndrome in acute inflammatory diseases of the musculoskeletal system, Pain syndrome in chronic inflammatory diseases of the musculoskeletal system, Deforming arthrosis, Deforming osteoarthritis, Deforming osteoarthritis of joints, Osteoarthritis in the acute stage, Osteoarthritis of large joints, Acute pain syndrome with osteoarthritis, Post-traumatic osteoarthritis, Rheumatic osteoarthritis, Spondylarthrosis, Chronic osteoarthritis

M25.5 Pain in the joint

Arthralgia, Pain syndrome in musculo-articular diseases, Pain syndrome in osteoarthritis, Pain syndrome in osteoarthritis, Pain syndrome in acute inflammatory diseases of the musculoskeletal system, Pain syndrome in chronic inflammatory diseases of the musculoskeletal system, Pain in the joints, Soreness of the joints, Soreness of joints in severe physical exertion, Painful inflammatory joint damage, Painful conditions of the musculoskeletal system, Painful joint conditions, Painful traumatic affection of joints, Pain in the musculoskeletal system, Pain in Shoulder Joints, Pain in the joints, Joint pain, Joint pain with injuries, Musculoskeletal pain, Pain with osteoarthritis, Pain in the pathology of the joints, Pain in rheumatoid arthritis, Pain in chronic degenerative bone diseases, Pain in chronic degenerative joint

diseases, Bone-joint pain, Joint pain, Arthritic pain of rheumatic origin, Articular pain syndrome, Joint pain, Rheumatic pain, Rheumatic pains

M54 Dorsalgia

Pain in the back area, Pain in the spine, Back pain, Pain in different parts of the spine, Backache, Painful pain syndrome in the spine, Pain in the musculoskeletal system

M54.5 Pain below the back

Pain in the lower back, Lumbar pain, Lumbalia, Painful conditions of the spinal column, Back pain, Lower Back Pain Syndrome

M71 Other bursopathies

Bursitis, Bursopathy, Diseases of soft tissues, Osteoarthritis in musculo-articular diseases, Inflammatory

disease of soft tissues, Subacute bursitis

M77.9 Other unspecified

Capsule, Periarthritis, Tendonitis, Tendopathy, Periarthropathy

M79.1 Myalgia

Myofascial pain syndromes ,Pain syndrome in musculo-articular diseases, Pain syndrome in chronic inflammatory diseases of the musculoskeletal system, Pain in the muscles, Tenderness of muscles, Muscular soreness in severe physical exertion, Painful conditions of the musculoskeletal system, Pain in the musculoskeletal system, Pain in the muscles, Pain at rest, Muscle aches, Muscle pain, Musculoskeletal pain, Myalgia, Muscle pain, Muscle pain at rest, Muscle pain, Muscular pain of non-rheumatic origin, Muscle pain of rheumatic origin, Acute muscle pain, Rheumatic pain, Rheumatic pains, Myofascial syndrome, Fibromyalgia

N94.6 Dysmenorrhea Unspecified

Pain during menstruation, Functional disorders of the menstrual cycle, Menstrual cramps, Emmeniopathy, Pain during menstruation, Painful menstrual irregularities, algomenorrhea, algomenoreya, Pain smooth muscle spasm, Pain spasm of smooth muscles (renal and biliary colic, intestinal spasms, dysmenorrhea), Pain spasm of smooth muscles of internal organs (kidney and biliary colic, intestinal spasms, dysmenorrhea), Disalgomenoreya, dysmenorrhea, Dysmenorrhea (essential) (Exfoliative), menstrual disorder, menstruation painful, metrorrhagia, Violation of the menstrual cycle, Menstrual irregularities, Prolaktinzavisimoe menstrual disorders, Prolaktinzavisimoe menstrual dysfunction, Pain spasm of smooth muscles of internal organs, Spasmodic dysmenorrhea, Primary disalgomenoreya

R52.0 Acute pain

Acute pain syndrome, Acute pain syndrome with osteoarthritis, Acute pain syndrome of traumatic origin, Severe pain of a neurogenic nature, Severe pain, Pain syndrome at delivery

R68.8.0 * Inflammatory syndrome

Painful syndrome of inflammatory genesis, Pain syndrome with inflammation of non-rheumatic nature, Pain syndrome with inflammatory lesions of the peripheral nervous system, Painful inflammation of the shoulder joint, Painful inflammation after trauma or surgery, Painful inflammation after surgery, Painful hemorrhoidal nodes, Inflammation of the tympanic membrane, Inflammation of the larynx, Inflammation of the gums, Inflammation of cellulose, Inflammation of lymph nodes, Tonsillitis, Inflammation of muscles, Inflammation of soft tissues, Inflammation of the mouth, Inflammation after surgery and trauma, Inflammation after orthopedic surgery, Inflammation after trauma, Inflammation in rheumatoid arthritis, Inflammation of the middle ear, Inflammatory gum disease, Inflammatory diseases of the eyelids, Inflammation of the eye, Inflammatory swelling of soft tissues, Inflammatory processes, Inflammatory processes after surgical interventions, Inflammatory process, Inflammatory Syndrome, Inflammatory syndrome of non-rheumatic origin, Inflammatory syndrome after surgery, Purulent infections, Infringements of function of a liver of an inflammatory etiology, Acute inflammation of the musculoskeletal tissue, Pre-inflammatory soft tissue inflammation

T14.3 Dislocation, sprain and damage to the capsular-ligamentous apparatus of the joint of the unspecified area of the body

Painful stretching of muscles, Pain and inflammation in tension, Dislocation of dislocation, Degenerative changes in the ligamentous apparatus, Edema due to sprains and bruises, Edema after interventions for sprains, Damage and rupture of ligaments, The musculoskeletal system is damaged, Damage to ligaments, Damage to the joints, Ligament ruptures, Tendon tendons,Ruptures of the tendons of muscles,Stretching, Crick, Stretching of the muscle, Sprain, Tension of the tendons, Extensions,Stretch muscles, Sprains, Tension of the tendons, Injury of the musculoskeletal system, Injuries to the joints, Injuries of capsule-articular tissues, Injuries of the osteoarticular system, Injuries to ligamentsInjuries to the joints, Joint wounds, Stretching of the ligamentous apparatus, Habitual stretching and tearing

T14.9 Injury unspecified

Pain syndrome after trauma, Pain syndrome with injuries, Pain syndrome with trauma and after surgery, Pain in case of injury, Pain of a traumatic nature, Joint pain with injuries, Postoperative and post-traumatic pain, Pain in case of injury, Pain of a traumatic origin, Severe pain syndrome of traumatic origin, Deep tissue damage, Deep scratches on the trunk, Closed injury, Minor Household Injuries, Minor skin damage, Violations of the integrity of soft tissues, Uncomplicated trauma, Extensive traumatic injury, Acute pain syndrome of traumatic origin, Edema with trauma, Postponed sports injuries, Post-traumatic pain, Soft tissue injuries, Joint wounds, Sports injuries, Injury, Traumatic pain, Traumatic pains, Traumatic infiltrate,Injuries to sports

Composition

Granules for the preparation of a suspension for oral administration 1 pack.

active substance:

nimesulide 100 mg

auxiliary substances: ketomacrogol 1000; sucrose; maltodextrin; citric acid is anhydrous; orange flavor

Description of dosage form

Light yellow granular powder with orange smell.

pharmachologic effect

Pharmacological action - anti-inflammatory, antipyretic, analgesic.

Pharmacodynamics

Nimesulide is an NSAID from the class of sulfonamides. Has anti-inflammatory, analgesic and antipyretic effect. Nimesulide acts as an inhibitor of the COX enzyme responsible for the synthesis of PG and inhibits mainly COX-2.

Pharmacokinetics

After ingestion, the drug is well absorbed from the digestive tract, reaching Cmax in the blood plasma after 2-3 hours; communication with plasma proteins - 97.5%; T1 / 2 is 3.2 to 6 hours. Easily penetrates through the histogematic barriers.

Metabolised in the liver with the help of cytochrome P450CYP2C9 isoenzyme. The main metabolite is the pharmacologically active parahydroxy derivative of nimesulide - hydroxynimidesulide. Hydroxynimesulide is excreted in the metabolized form with bile (found only in the form of glucuronate - about 29%).

Nimesulide is excreted from the body, mostly by the kidneys (about 50% of the dose taken).

The pharmacokinetic profile of nimesulide in elderly patients does not change with the administration of single and multiple / repeated doses.

According to an experimental study conducted with patients with mild to moderate renal failure (Cl creatinine 30-80 ml / min) and healthy volunteers, Cmax nimesulide and its metabolite in patients with plasma did not exceed the concentration of nimesulide in healthy volunteers. AUC and T1 / 2 in patients with renal insufficiency were 50% higher, but within the pharmacokinetic parameters. When you re-take the drug cumulation is not observed.

Indications

treatment of acute pain (pain in the back, lower back, pain syndrome in the pathology of the musculoskeletal system, including trauma, sprains and joints, tendonitis, bursitis);

toothache;

symptomatic treatment of osteoarthritis with pain syndrome;

disalgomenorrhea.

The drug is intended for symptomatic therapy, reducing pain and inflammation at the time of use.

Contraindications

increased sensitivity to nimesulide or to one of the components of the drug;

Hyperergic reactions (in the anamnesis), for example bronchospasm, rhinitis, urticaria, associated with the use of acetylsalicylic acid or other NSAIDs, incl. nimesulide;

hepatotoxic reactions to nimesulide (in anamnesis);

concurrent (simultaneous) drug use with potential hepatotoxicity, for example, paracetamol or other analgesic agents or NSAIDs;

inflammatory bowel disease (Crohn's disease, ulcerative colitis) in the phase of exacerbation;

period after aortocoronary shunting;

febrile syndrome for colds and acute respiratory viral infections;

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

peptic ulcer of the stomach or duodenum in the phase of exacerbation, the presence in the anamnesis of an ulcer, perforation or bleeding in the gastrointestinal tract;

presence in the anamnesis of cerebrovascular hemorrhages or other bleeding, as well as diseases accompanied by bleeding;

severe blood clotting disorders;

severe heart failure;

severe renal failure (Cl creatinine <30 ml / min), confirmed hyperkalemia;

hepatic insufficiency or any active liver disease;

pregnancy and lactation;

alcoholism, drug addiction;

children under the age of 12 years.

With caution: severe forms of hypertension, type 2 diabetes, heart failure, ischemic heart disease, cerebrovascular disease, dyslipidemia / hyperlipidemia, peripheral arterial disease, smoking, Cl creatinine less than 60 mL / min.

Anamnestic data on the presence of ulcerative lesions of the gastrointestinal tract, infection caused by Helicobacter pylori; elderly age; prolonged previous use of NSAIDs; severe physical illness.

Concomitant therapy with the following drugs: anticoagulants (eg warfarin), antiaggregants (eg acetylsalicylic acid, clopidogrel), oral GCS (eg prednisolone), SSRIs (eg citalopram, fluoxetine, paroxetine, sertraline).

The decision to prescribe Nimesil® should be based on an individual assessment of the risk and benefit of taking the drug.

pregnancy and lactation

Like other NSAID drugs that inhibit the synthesis of PG, nimesulide may adversely affect pregnancy and / or embryo development and lead to premature closure of the arterial duct, hypertension in the pulmonary artery system, impaired renal function that can translate into renal insufficiency with oligohydramnion, an increased risk of bleeding, a decrease in contractility of the uterus, the emergence of peripheral edema.

In this regard, nimesulide is contraindicated during pregnancy and lactation.

The use of Nimesil® can negatively affect female fertility and is not recommended for women planning a pregnancy. When planning pregnancy, consultation with the doctor is necessary.

Side effects

The frequency is classified according to the headings, depending on the occurrence of the case: very often (> 10), often (> 100 - <10); infrequently (> 1000- <100), rarely (> 10000- <1000), very rarely (<10000).

Disorders from the blood and lymphatic systems: rarely - anemia, eosinophilia, hemorrhages; very rarely - thrombocytopenia, pancytopenia, purpura thrombocytopenic.

Allergic reactions: infrequently - itching, rash, excessive sweating; rarely - hypersensitivity reactions, erythema, dermatitis; very rarely - anaphylactoid reactions, urticaria, angioedema, erythema polyforma, Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome).

Disorders 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).

Impaired sensory organs: rarely - blurred vision.

Disorders from the CCC: infrequently - arterial hypertension, tachycardia, lability of blood pressure, hot flashes.

Disturbances from the respiratory system: infrequent - dyspnea; very rarely - exacerbation of bronchial asthma, bronchospasm.

Disorders from the digestive tract: often - diarrhea, nausea, vomiting; infrequently - constipation, flatulence, gastritis; very rarely - abdominal pain, dyspepsia, stomatitis, tarry stool, gastrointestinal bleeding, ulcer and / or perforation of the stomach or duodenum.

Disturbances from the liver and bile excretory system: very rarely - hepatitis, fulminant hepatitis, jaundice, cholestasis, increased activity of hepatic enzymes.

Disorders from the kidneys and urinary system: rarely - dysuria, hematuria, urinary retention; very rarely - renal failure, oliguria, interstitial nephritis.

Common disorders: rarely - malaise, asthenia; very rarely - hypothermia.

Other: rarely - hyperkalemia.

Interaction

Pharmacodynamic interactions

GCS. Increase the risk of gastrointestinal ulcers or bleeding.

Antiplatelet agents and SSRIs, for example fluoxetine. Increase the risk of gastrointestinal bleeding.

Anticoagulants. NSAIDs can enhance the action of anticoagulants, such as warfarin. Because of the increased risk of bleeding, this combination is not recommended and is contraindicated in patients with severe coagulation disorders. If combined therapy can still be avoided, careful monitoring of blood coagulation should be carried out.

Diuretics. NSAIDs may reduce the effect of diuretics.

In healthy volunteers, nimesulide temporarily reduces the excretion of sodium by furosemide, to a lesser extent - the excretion of potassium and reduces the actual diuretic effect.

The simultaneous administration of nimesulide and furosemide results in a decrease (approximately 20%) in AUC and a decrease in cumulative furosemide excretion without altering the renal clearance of furosemide.

Co-administration of furosemide and nimesulide requires caution in patients with impaired renal or cardiac function.

ACE inhibitors and angiotensin II receptor antagonists. NSAIDs may reduce the effect of antihypertensive drugs. In patients with mild and moderate renal failure (Cl creatinine 30-80 ml / min), concomitant administration of ACE inhibitors, angiotensin II receptor antagonists, or substances suppressing the COX system (NSAIDs, antiaggregants) may further impair kidney function and the occurrence of acute renal disease insufficiency, which, as a rule, happens to be reversible. These interactions should be considered in patients taking Nimesil® in combination with ACE inhibitors or angiotensin II receptor antagonists. Therefore, joint intake of these drugs should be administered with caution, especially for elderly patients. Patients should receive a sufficient amount of fluid, and renal function should be carefully monitored after the initiation of co-therapy.

Pharmacokinetic interactions with other drugs

Lithium preparations. There is evidence that NSAIDs decrease lithium clearance, which leads to an increase in the concentration of lithium in the blood plasma and its toxicity. When nimesulide is prescribed, patients receiving lithium therapy should be monitored regularly for plasma lithium concentrations.

Clinically significant interactions with glibenclamide, theophylline, digoxin, cimetidine and antacid preparations (for example, a combination of aluminum and magnesium hydroxides) were not observed.

Nimesulide inhibits the activity of the isoenzyme CYP2C9. With the simultaneous administration of nimesulide drugs, which are substrates of this enzyme, the concentration of these drugs in the plasma may increase.

Caution is required when administering nimesulide less than 24 hours before or after taking methotrexate. in such cases, the level of methotrexate in the plasma and, accordingly, the toxic effects of this drug may increase.

In connection with the effect on renal PG, COX inhibitors, such as nimesulide, may increase the nephrotoxicity of cyclosporins.

Interaction of other drugs with nimesulide

In vitro studies have shown that nimesulide is displaced from the binding sites by tolbutamide, salicylic acid and valproic acid, but these effects have not been observed during clinical use of the drug.

Dosing and Administration

Inside, after eating. 1 pack. (100 mg of nimesulide) 2 times a day. The contents of the sachet are poured into a beaker and dissolved in about 100 ml of water. The prepared solution is not subject to storage.

Nimesil® is only used to treat patients older than 12 years.

Teenagers (from 12 to 18 years). Based on the pharmacokinetic profile and pharmacodynamic characteristics of nimesulide, adolescents do not need to adjust the dose.

Patients with impaired renal function. Based on pharmacokinetic data, the need for dose adjustment in patients with mild and moderate forms of renal failure (Cl creatinine 30-80 ml / min) is not present.

Patients of advanced age. In the treatment of elderly patients, the need to adjust the daily dose is determined by the doctor based on the possibility of interaction with other drugs.

The maximum duration of treatment with nimesulide is 15 days.

To reduce the risk of undesirable side effects, use the lowest effective dose with a minimally short course.

Overdose

Symptoms: apathy, drowsiness, nausea, vomiting, pain in the epigastric region. With maintenance therapy of gastropathy, these symptoms are usually reversible. There may be a gastrointestinal bleeding. In rare cases, it is possible to raise blood pressure, acute renal failure, respiratory depression and coma, anaphylactoid reactions.

Treatment: symptomatic. There is no specific antidote. In case an overdose has occurred within the last 4 hours, induction of vomiting and / or the administration of activated charcoal (from 60 to 100 g per adult) and / or osmotic laxative. Forced diuresis, hemodialysis - ineffective because of the high connection of the drug with proteins (up to 97.5%). The control of kidney and liver function is shown.

special instructions

Unwanted side effects can be minimized by using the lowest effective dose of the drug as little as possible a short course.

Nimesil® should be used with caution in patients with gastrointestinal ailments in history (ulcerative colitis, Crohn's disease), as possible exacerbation of these diseases.

The risk of gastrointestinal bleeding, ulcers or perforation of the ulcer increases with an increase in the dose of NSAIDs in patients with a history of an ulcer, especially complicated by bleeding or perforation, and in elderly patients, so treatment should be started with the lowest possible dose. In patients receiving drugs, reducing blood clotting or suppressing platelet aggregation also increases the risk of gastrointestinal bleeding. In case of gastrointestinal bleeding or ulcers in patients taking Nimesil®, treatment with the drug should be discontinued.

Since Nimesil® is partially excreted by the kidneys, its dosage should be reduced for patients with impaired renal function, depending on the level of urination.

There are data on the occurrence of rare cases of reactions from the liver. If signs of liver damage (itchy skin, yellowing of the skin, nausea, vomiting, abdominal pain, darkening of the urine, increased activity of liver transaminases), stop taking the drug and consult a doctor.

Despite the rarity of visual impairment in patients taking nimesulide concomitantly with other NSAIDs, treatment should be stopped immediately. If any visual impairment occurs, the patient should be examined by an oculist.

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

In patients with renal or heart failure, Nimesil® should be used with caution, since renal impairment may be impaired. In case of worsening, treatment with Nimesil® should be stopped.

Clinical studies and epidemiological data suggest that NSAIDs, especially in high doses and with prolonged use, can lead to an insignificant risk of myocardial infarction or stroke. To exclude the risk of such events occurring when nimesulide is used, data is insufficient.

The composition of the drug includes sucrose, this should be taken into account for patients suffering from diabetes (0.15-0.18 XE per 100 mg of the drug) and those who observe a low-calorie diet. Nimesil® is not recommended for patients with intolerance to fructose, malabsorption of glucose-galactose, or insufficiency of sucrose-isomaltose.

If there are signs of a cold or an acute respiratory viral infection during treatment with Nimesil®, the drug should be discontinued.

Do not use Nimesil® concomitantly with other NSAIDs.

Nimesulide can change the properties of platelets, so care must be taken when using the drug in people with hemorrhagic diathesis, but the drug does not replace the preventive effect of acetylsalicylic acid in cardiovascular diseases.

Elderly patients are particularly susceptible to adverse reactions to NSAIDs, incl. risk of gastrointestinal bleeding and perforations, threatening the life of the patient, worsening kidney, liver and heart function. When taking Nimesil® for this category of patients, proper clinical control is necessary.

There are reports of the occurrence in rare cases of skin reactions (such as exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis) on nimesulide as well as other NSAIDs. At the first signs of skin rashes, lesions of mucous membranes or other signs of an allergic reaction, the drug Nimesil® should be stopped.

Effect of the drug on the ability to drive vehicles and manage mechanisms. The influence of Nimesil® on the ability to drive vehicles and control mechanisms has not been studied, therefore, during the period of treatment with Nimesil®, caution should be exercised when driving vehicles and engaging in potentially hazardous activities requiring increased attention and speed of psychomotor reactions.

Form of issue

Granules for the preparation of a suspension for oral administration, 100 mg. 2 g of granulate in three-layer bags (paper / aluminum / PE). For 30 pax. placed in a cardboard box.

Conditions of leave from pharmacies

On prescription.

storage conditions

In a dry, the dark 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.