Nimesulid-Teva
Nimesulid-Teva: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Nimesulid-Teva
ATX code: M01AX17
Active ingredient: nimesulide (Nimesulide)
Producer: Blufarma-Industry Pharmaceutika S. A. (Portugal)
Description and photo update: 09.10.2019
Prices in pharmacies: from 70 rubles.
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Nimesulide-Teva is a non-steroidal anti-inflammatory drug (NSAID) that has analgesic, anti-inflammatory, antipyretic and antiplatelet effects.
Release form and composition
The drug is available in the form of tablets: light yellow, round, biconvex, with a dividing line on one side (10 pcs. In blisters, in a cardboard box 1, 2, 3 or 6 blisters and instructions for the use of Nimesulide-Tev).
1 tablet contains:
- active substance: nimesulide - 100 mg;
- auxiliary components: lactose monohydrate, sodium docusate, hyprolose, hydrogenated vegetable oil, sodium carboxymethyl starch, magnesium stearate, microcrystalline cellulose.
Pharmacological properties
Pharmacodynamics
Nimesulide-Teva is a non-steroidal anti-inflammatory drug with anti-inflammatory, antipyretic, analgesic and antiplatelet effects. The active substance of the drug is nimesulide, the mechanism of action of which is due to the suppression of cyclooxygenase (COX), mainly cyclooxygenase-2 (COX-2). Against the background of the use of nimesulide, the synthesis of prostaglandins slows down mainly in the focus of inflammation, therefore, in contrast to indomethacin, side effects are more rarely observed that are associated with inhibition of prostaglandin synthesis in healthy tissues.
Pharmacokinetics
After oral administration, nimesulide is well absorbed in the gastrointestinal tract (GIT). The maximum concentration (C max) in blood plasma is achieved after 2-3 hours, in adults it is up to 3-4 mg / l against the background of a single dose of 100 mg. The area under the concentration-time curve (AUC) varies in the range of 20–35 mg · h / l both after a single dose of 100 mg and with a dosage regimen of 100 mg 2 times a day for 7 days. Simultaneous food intake slows down the rate of absorption, but does not affect its degree.
Binding to blood plasma proteins - 95%, lipoproteins - 1%, erythrocytes - 2%, acid alpha 1- glycoproteins - 1%. The degree of binding does not change with increasing dose.
The volume of distribution is 0.19-0.35 l / kg.
Nimesulide easily overcomes histohematogenous barriers. Its concentration after a single dose in the genital tissues of women can be approximately 40%, in the acidic environment of the focus of inflammation - 40%, synovial fluid - 43% of the level in the blood plasma.
Nimesulide is metabolized in the liver with the participation of monooxygenases (including the cytochrome P 450 CYP2C9 system). Its main active metabolite, water-soluble 4-hydroxynimesulide, undergoes enterohepatic recirculation and has similar pharmacological activity.
About 50% of the dose taken is excreted through the kidneys. The active metabolite is excreted in the urine (65%) and bile (35%). Up to 3% of nimesulide is excreted unchanged.
Half-life (T 1/2): nimesulide - 3-6 hours, 4-hydroxynimesulide - 3-5 hours.
The pharmacokinetic profile of the active substance in elderly patients does not change after a single or repeated administration.
With mild to moderate renal impairment with creatinine clearance (CC) of 30–80 ml / min, the Cmax values of nimesulide and the active metabolite in the blood plasma do not exceed those in healthy individuals, and the use of the drug is not accompanied by cumulation.
Indications for use
- algodismenorrhea, pain in the postoperative and post-traumatic period, arthralgia, myalgia, tendinitis, bursitis, toothache and headache - in order to relieve acute pain syndrome;
- osteoarthritis - for symptomatic treatment in order to reduce pain and inflammation at the time of application (nimesulide does not affect the progression of the disease); only as a second line therapy.
Contraindications
Absolute:
- cerebrovascular bleeding;
- bleeding disorders, which may be accompanied by bleeding;
- hemophilia;
- an indication of a history of gastrointestinal bleeding or perforation of the intestinal walls, which are caused by the use of NSAIDs;
- two or more confirmed episodes of erosive and ulcerative lesions and / or bleeding of the mucous membrane of the stomach and duodenum;
- period of exacerbation of inflammatory bowel diseases (including ulcerative colitis, Crohn's disease);
- decompensated heart failure;
- period of exacerbation of any liver disease;
- liver failure;
- an indication in the history of hepatotoxic reactions against the background of the use of nimesulide;
- simultaneous use with other potentially hepatotoxic agents;
- progressive kidney disease;
- severe renal failure (CC less than 30 ml / min);
- confirmed hyperkalemia;
- period after coronary artery bypass grafting;
- the presence of a concomitant cold disease, accompanied by a high fever;
- impaired absorption of glucose or galactose, congenital lactose intolerance, lactase deficiency;
- III trimester of pregnancy;
- breast-feeding;
- age up to 12 years;
- established individual intolerance to NSAIDs, including acetylsalicylic acid;
- an indication in the history of the development of hypersensitivity reactions (including bronchospasm, rhinitis, urticaria, complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose and paranasal sinuses) in response to NSAIDs;
- hypersensitivity to drug components.
With caution, Nimesulide-Teva should be prescribed for such severe somatic diseases as cerebrovascular diseases, ischemic heart disease, dyslipidemia or hyperlipidemia, obliterating pathologies of peripheral arteries, diabetes mellitus, renal failure (CC 30-80 ml / min), Helicobacter pylori infection, hemorrhagic diathesis, a history of the development of ulcerative lesions of the gastrointestinal tract, smoking, alcoholism, in old age.
In addition, caution is required in the case of prolonged use of NSAIDs, concomitant therapy with anticoagulants (including warfarin), antiplatelet agents (including acetylsalicylic acid, clopidogrel), selective serotonin reuptake inhibitors (including citalopram, sertraline, fluoxetine, paroxetide glucocorticosteroids), peroxetine.
Care should be taken when prescribing Nimesulide-Teva during the planning of conception, in the I and II trimesters of pregnancy.
Nimesulide-Teva, instructions for use: method and dosage
Nimesulide-Teva tablets are taken orally after meals.
When prescribing the drug, the minimum effective dose should be used for the shortest possible course of treatment.
Recommended dosage for patients over the age of 12 years: 100 mg (1 pc.) 2 times a day. The doctor determines the duration of the course of therapy individually, but it should not exceed 15 days.
Elderly patients do not need dose adjustment.
In case of impaired renal function (CC 30-80 ml / min), the general dosage regimen of Nimesulide-Teva is usually used. In renal failure, the maximum daily dose should be 100 mg.
Side effects
Adverse reactions from systems and organs when taking the drug Nimesulide-Teva (criteria for assessing the occurrence: very often - ≥ 10%; often - from ≥ 1% to <10%; infrequently - from ≥ 0.1% to <1%; rarely - from ≥ 0.01% to <0.1%; very rarely - <0.01%):
- from the immune system: rarely - hypersensitivity reactions; very rarely - anaphylaxis;
- from the digestive system: often - nausea, vomiting, increased activity of liver enzymes; infrequently - flatulence, constipation, gastritis; very rarely - stomatitis, dyspepsia, abdominal pain, gastrointestinal bleeding, melena, ulcer and perforation of the stomach and / or duodenum, hepatitis (including fulminant course, jaundice, cholestasis);
- from the nervous system and sensory organs: infrequently - dizziness; rarely - blurred vision; very rarely - visual impairment;
- mental disorders: rarely - fear, nervousness, anxiety, nightmares;
- on the part of the cardiovascular system: infrequently - arterial hypertension; rarely - tachycardia, lability of blood pressure (BP), flushing of the face;
- from the urinary system: rarely - urinary retention, dysuria, hematuria; very rarely - interstitial nephritis, renal failure, oliguria;
- on the part of the respiratory system: infrequently - dyspnea; very rarely - bronchospasm;
- dermatological reactions: infrequently - increased sweating, itching, rash; rarely - dermatitis, erythema; very rarely - facial edema, urticaria, erythema multiforme, angioedema, toxic epidermal necrolysis, Stevens-Johnson syndrome;
- on the part of the blood and lymphatic system: rarely - eosinophilia, anemia; very rarely - purpura, thrombocytopenia, pancytopenia;
- violations of water and electrolyte balance: rarely - hyperkalemia;
- systemic disorders: infrequently - edematous syndrome; rarely - malaise, asthenia; very rarely - hypothermia.
Overdose
Symptoms: drowsiness, apathy, nausea, vomiting, increased blood pressure, respiratory depression, gastrointestinal bleeding, acute renal failure.
Treatment: during the first 4 hours after an overdose of Nimesulide-Teva, it is necessary to induce vomiting, and then take activated charcoal in a dose of 1 g per 1 kg of body weight. The patient should be provided with careful observation, supportive and symptomatic therapy. There is no specific antidote.
The use of forced diuresis or hemodialysis is ineffective.
special instructions
To reduce the risk of undesirable effects, the drug should be prescribed in the lowest effective dose, using the shortest possible course of therapy. Long-term use of Nimesulide-Teva, especially when using high doses, is associated with the risk of arterial thrombosis, a potential manifestation of which may be myocardial infarction or ischemic stroke.
Treatment with Nimesulide-Teva should be accompanied by regular (1 time in 14 days) monitoring of the functional state of the liver. Symptoms such as fatigue, itching, abdominal pain, nausea, vomiting, pain in the right hypochondrium, darkening of urine, jaundice, and increased activity of hepatic transaminases may indicate liver damage. When each of them appears, it is recommended to immediately stop taking the pills and consult a doctor. Reappointment of nimesulide in this category of patients is contraindicated.
In case of visual impairment during the treatment of NSAIDs, immediate withdrawal is required.
Nimesulide-Teva can cause fluid retention in the body, therefore, the drug should be used with extreme caution in patients with high blood pressure or signs of congestive heart failure.
If it is necessary to combine nimesulide with drugs that have an ulcerogenic effect on the gastrointestinal tract, patients should be under close medical supervision.
The simultaneous administration of Nimesulide-Teva with selective COX-2 inhibitors and other NSAIDs or non-narcotic analgesics is contraindicated.
Nimesulide-Teva is not capable of replacing the prophylactic use of antiplatelet agents (clopidogrel, ticlopidine, acetylsalicylic acid) in patients with cardiovascular diseases, although it has a reducing effect on platelet aggregation.
The appearance of an elevated body temperature and other signs of a cold is the basis for canceling Nimesulide-Teva.
If it is necessary to prescribe high doses of NSAIDs, including in patients with a history of gastric and duodenal ulcers or in the elderly, concomitant use of proton pump inhibitors or misoprostol is indicated. This will reduce the risk of bleeding, ulceration, or perforation of the stomach or intestines.
In patients with impaired renal function, taking the drug may worsen the condition. If there is a further decrease in creatinine clearance, treatment should be discontinued.
When prescribing Nimesulide-Teva, the doctor should warn the patient about the need to immediately contact a medical facility if any unusual abdominal symptoms appear, especially if they occur in the early stages of therapy.
When the first signs of hypersensitivity (rash, mucosal damage) appear, treatment with nimesulide should be canceled immediately.
Influence on the ability to drive vehicles and complex mechanisms
During the period of taking Nimesulide-Tev when engaging in potentially hazardous activities that require increased attention and speed of psychomotor reactions, including driving, caution is recommended in cases where the patient feels dizzy or drowsy during therapy.
Application during pregnancy and lactation
The use of Nimesulide-Teva in the third trimester of pregnancy is contraindicated. This is due to the fact that nimesulide, like other inhibitors of prostaglandin synthesis, can have a negative effect both on the fetus (impaired renal function up to the development of renal failure, cardiopulmonary toxicity with the development of pulmonary hypertension as a result of premature closure of Botallov's arterial duct), so and on the mother and newborn (delay and lengthening of labor as a result of a decrease in uterine contractions, lengthening of bleeding time even after taking low doses of Nimesulide-Teva).
NSAIDs can have a negative effect on female fertility, so it is not recommended to use the drug for the treatment of women trying to become pregnant. If necessary, the appointment of Nimesulide-Teva is allowed during the planning period of conception, in the first and second trimesters of pregnancy - only when using the minimum effective doses during a short course of treatment.
It should be borne in mind that the use of NSAIDs in the first trimester of pregnancy is accompanied by an increased risk of spontaneous miscarriage in the early stages, the development of gastroschisis and heart defects in the fetus. With an increase in the dose and duration of the course of treatment, the risk of teratogenicity and embryotoxicity increases.
It is contraindicated to use Nimesulide-Teva during breastfeeding.
Pediatric use
The use of Nimesulide-Teva for the treatment of children under the age of 12 is contraindicated.
No dose adjustment is required for adolescents 12–18 years old.
With impaired renal function
The use of Nimesulide-Teva is contraindicated in patients with severe renal failure (CC less than 30 ml / min), progressive kidney disease and / or confirmed hyperkalemia.
For patients with impaired renal function (CC 30–80 ml / min), the usual doses are indicated. In case of renal failure, the daily dose should not exceed 100 mg.
For violations of liver function
The use of Nimesulide-Teva is contraindicated in case of any exacerbation of liver disease, liver failure, or an indication in history of hepatotoxic reactions against the background of the use of nimesulide.
Use in the elderly
Nimesulide-Teva tablets should be prescribed with caution to elderly patients.
No dose adjustment is required for older patients.
Drug interactions
- other NSAIDs (including acetylsalicylic acid in anti-inflammatory doses - more than 1 g once or 3 g or more per day): combined use with the drug is not recommended;
- anticoagulants (including warfarin), antiplatelet agents (including acetylsalicylic acid, clopidogrel): joint administration leads to an increased risk of bleeding;
- cyclosporine: increased nephrotoxicity of cyclosporine;
- glucocorticosteroids, selective serotonin reuptake inhibitors: the risk of gastrointestinal bleeding increases;
- diuretics and other antihypertensive drugs: may reduce their therapeutic effect;
- angiotensin-converting enzyme (ACE) inhibitors, angiotensin II antagonists: against the background of concomitant therapy with these agents in elderly people with impaired renal function or in dehydrated patients, the manifestations of renal failure may increase, which are usually reversible. Treatment should be accompanied by adequate fluid intake and monitoring of kidney function;
- furosemide: the severity of natriuretic activity and potassium uretic action of furosemide decreases for a short time;
- lithium preparations: lithium clearance decreases, its concentration in blood plasma and toxicity increase;
- methotrexate: combined administration requires caution due to the increased risk of increased toxicity due to an increase in the concentration of methotrexate in blood plasma.
When prescribing Nimesulide-Teva in combination with drugs that are substrates of the CYP2C9 enzyme, it should be borne in mind that as a result of the interaction, their plasma concentrations may increase.
Analogs
Analogs of Nimesulide-Teva are: Nimesulide, Nimesulide-Inkampharm, Nimesulide-LekT, Nimesulide-MBF, Nimesulide-SZ, Ameolin, Aponil, Nise, Naysulid, Nemuleks, Nimesan, Nimesil, Nimesulid, Nimulid.
Terms and conditions of storage
Keep out of the reach of children.
Store at temperatures up to 25 ° C, protected from moisture and light.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Nimesulide-Teva
Reviews about Nimesulide-Teva are positive. Patients note a good analgesic effect of the drug for pain of various etiologies.
Price for Nimesulide-Teva in pharmacies
The price of Nimesulide-Teva for a package containing 20 tablets can be from 122 rubles, 30 tablets - from 157 rubles.
Nimesulid-Teva: prices in online pharmacies
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Drug name Price Pharmacy |
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Nimesulide-Teva 100 mg tablets 30 pcs. RUB 70 Buy |
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Nimesulide-Teva 100 mg tablets 20 pcs. 115 RUB Buy |
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Nimesulide-Teva 100mg tablets 30 pcs. 152 RUB Buy |
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
