Naisulid - Instructions For Use, Tablets, Price, Reviews, Analogues

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Naisulid

Naisulid: instructions for use and reviews

1. 1. Release form and composition
2. 2. Pharmacological properties
3. 3. Indications for use
4. 4. Contraindications
5. 5. Method of application and dosage
6. 6. Side effects
7. 7. Overdose
8. 8. Special instructions
9. 9. Application during pregnancy and lactation
10. 10. Use in childhood
11. 11. In case of impaired renal function
12. 12. For violations of liver function
13. 13. Use in the elderly
14. 14. Drug interactions
15. 15. Analogs
16. 16. Terms and conditions of storage
17. 17. Terms of dispensing from pharmacies
18. 18. Reviews
19. 19. Prices in pharmacies

Latin name: Neusulid

ATX code: M01AX17

Active ingredient: nimesulide (Nimesulide)

Manufacturer: JSC "Pharmaceutical Enterprise" Obolenskoe "(Russia)

Description and photo update: 09.10.2019

Prices in pharmacies: from 136 rubles.

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Naisulide is a non-steroidal anti-inflammatory drug (NSAID) with antipyretic, analgesic and anti-inflammatory effects.

Release form and composition

Dosage forms of Naisulide:

• tablets: oblong, biconvex, with rounded ends, scored; color - light yellow with a slight greenish tint [10, 15, 20 or 30 pcs. in blister contour packages made of polyvinyl chloride (PVC) film and lacquered printed aluminum foil, in a cardboard box along with instructions for use of the drug 1, 2, 3, 4, 5 or 6 packages];
• tablets, dispersible in the oral cavity: round, flat-cylindrical, scored and chamfered; color - from light yellow to yellow; tablets with a dosage of 50 mg - with a banana odor, a dosage of 100 mg - with pineapple (10 pcs. in blister contour packs made of PVC film and varnished printed aluminum foil, in a cardboard box together with instructions for use of the drug 1, 2, 3, 4 or 5 packs);
• granules for the preparation of a suspension for oral administration: a mixture of granules and powder having an orange smell and color from white with a light yellowish tint to light yellow; when water is added, a suspension with an orange smell is formed, the color of the finished suspension is from white to light yellow [2 g each in heat-sealable sachets, made of a multilayer combined packaging type "laminated foil" (buflen), in a cardboard box 9, 15 or 30 sachets and instructions for use Naisulid].

Composition of 1 tablet:

• active ingredient: nimesulide - 100 mg;
• additional ingredients: microcrystalline cellulose (MCC), potato starch, sodium starch glycolate (sodium carboxymethyl starch), magnesium stearate, lactose monohydrate, povidone K-30, talc.

Composition of 1 orodispersible tablet:

• active ingredient: nimesulide - 50 or 100 mg;
• additional ingredients: MCC, pregelatinized corn starch, corn starch, citric acid monohydrate, aspartame, magnesium stearate, aerosil (colloidal silicon dioxide), sodium carboxymethyl starch (type A), talc; additionally for tablets with a dosage of 50 mg - banana flavor, with a dosage of 100 mg - pineapple flavor.

Composition of 1 sachet with granules for preparation of oral suspension:

• active ingredient: nimesulide - 100 mg;
• additional ingredients: sucrose (sugar), macrogol cetostearyl ether (cetomacrogol 1000), maltodextrin, anhydrous citric acid, orange flavor.

Pharmacological properties

Pharmacodynamics

Nimesulide is a non-steroidal anti-inflammatory drug from the sulfonamide class. It has a pronounced anti-inflammatory, in addition analgesic and, to a lesser extent, antipyretic effect.

Nimesulide, in contrast to non-selective NSAIDs, predominantly inhibits cyclooxygenase-2 (COX-2). Due to this, the inhibition of the synthesis of prostaglandins in the focus of inflammation is more significant than that in the gastric mucosa or kidneys. Also, the drug has an inhibitory effect on cyclooxygenase-1 (COX-1), but to a less pronounced degree. Nimesulide, affecting a number of other factors, blocks the synthesis of proteinases and histamine, inhibits tumor necrosis factor alpha, a platelet activating factor.

In addition, in the mechanism of suppressing the inflammatory process of nimesulide, an important role is played by its ability to inhibit the release of the enzyme from lysosomes of white blood cells of neutrophils - myeloperoxidase, as well as the property to inhibit the synthesis of free oxygen radicals (does not affect hemostasis and phagocytosis).

Pharmacokinetics

The main pharmacokinetic parameters of nimesulide:

• absorption: after oral administration, nimesulide is well absorbed from the gastrointestinal tract (GIT). Oral ingestion of 100 mg of the substance provides the maximum plasma concentration (C _max) in the blood on average after 2-3 hours, it is 3-4 mg / l. The area under the concentration-time curve (AUC) ranges from 20 to 35 mg × h / L;
• distribution: binding to blood plasma proteins - 95–97.5%, with erythrocytes - 2%, with acid alpha ₁ -glycoproteins - 1%, with lipoproteins - 1%. Nimesulide penetrates into the tissues of the female genital organs, where its concentration (after a single dose) is approximately 40% of the plasma concentration. It penetrates well into the synovial fluid (43%) and the acidic environment of the inflammation focus (40%). Easily overcomes histohematogenous barriers;
• metabolism: metabolized in the liver by the cytochrome P ₄₅₀ isoenzyme CYP2C9. The main metabolite is hydroxynimesulide (pharmacologically active parahydroxy derivative of nimesulide), which is found exclusively in the form of glucuronate;
• excretion: nimesulide is excreted mainly through the kidneys (about 50% of the dose taken). The main metabolite is excreted in the urine (65%) and bile (29–35%), and undergoes enterohepatic recirculation. The half-life of nimesulide (T _1/2) when taking tablets ranges from 1.56 to 4.95 hours, hydroxynimesulide - from 2.89 to 4.78 hours. When taking the drug in the form of a suspension or dispersible tablets, T _1/2 is 3, 2-6 hours

In elderly patients and patients with renal insufficiency of mild and moderate severity, single and repeated / repeated administration of Naisulide has no effect on the pharmacokinetic profile.

In a study involving patients with renal insufficiency of mild and moderate severity [creatinine clearance (CC) from 30 to 80 ml / min], it was found that the C _max values of nimesulide and its main metabolite were similar to those in healthy volunteers. T _1/2 and AUC were 50% higher, but remained within the range of T _1/2 and AUC values that were observed during the use of the drug in healthy volunteers. Repeated use of nimesulide did not lead to cumulation.

Indications for use

Naisulide is used for symptomatic treatment, reduction of inflammation and relief of pain at the time of use, for the following diseases / conditions:

• pain syndrome of various origins, including acute pain [lumboischialgia, headache, algomenorrhea (including primary), toothache, arthralgia, pain in the postoperative period and in trauma, inflammation of the tendons, ligaments (including post-traumatic inflammation of the soft tissues), pain in the lower back, back, musculoskeletal system (sprains, bruises, joint dislocations), bursitis, tendinitis];
• osteochondrosis with radicular syndrome;
• osteoarthritis (osteoarthritis) with pain syndrome;
• rheumatoid arthritis, as well as articular syndrome as a result of exacerbation of gout;
• psoriatic arthritis;
• myalgia of rheumatic / non-rheumatic genesis;
• ankylosing spondylitis.

It is recommended to prescribe Naisulide as a second-line drug.

Contraindications

Absolute:

• severe heart failure;
• the period after CABG (coronary artery bypass grafting);
• anamnestic data on cerebrovascular bleeding or other diseases accompanied by increased bleeding;
• severe bleeding disorders;
• a history of gastrointestinal perforation or gastrointestinal bleeding;
• chronic benign inflammatory bowel disease (ulcerative colitis and Crohn's disease) in the acute phase;
• gastric ulcer or 12 duodenal ulcer in the acute phase, erosive and ulcerative lesions of the digestive tract;
• drug addiction, alcoholism;
• active liver disease, liver failure;
• confirmed hyperkalemia, severe renal failure (CC less than 30 ml / min);
• suspicion of acute surgical pathology;
• febrile syndrome, as a complication of colds and acute respiratory viral infections;
• children under 12 years old;
• breast-feeding;
• pregnancy;
• a history of hyperergic reactions (rhinitis, bronchospasm, urticaria), arising from the use of acetylsalicylic acid or other NSAIDs (including nimesulide);
• aspirin triad - a complete / incomplete combination of bronchial asthma, recurrent nasal polyposis (paranasal sinuses) with intolerance to acetylsalicylic acid, as well as other NSAIDs, including a history of data;
• concomitant use with other drugs with potential hepatotoxicity (for example, other NSAIDs);
• a history of hepatotoxicity to nimesulide;
• increased individual sensitivity to nimesulide or auxiliary components included in the drug.

Relative (Naisulid should be used with precautions):

• compensated heart failure;
• Ischemic heart disease (coronary heart disease);
• peripheral arterial disease;
• arterial hypertension;
• cerebrovascular diseases;
• dyslipidemia, hyperlipidemia;
• hemorrhagic diathesis;
• diabetes;
• smoking;
• severe psychosomatic illnesses;
• history of ulcerative lesions of the gastrointestinal tract;
• a history of bacterial infection caused by Helicobacter pylori (Helicobacter pylori);
• renal failure with CC indications 30-60 ml / min;
• long-term previous use of NSAIDs;
• simultaneous use with antiplatelet agents (for example, clopidogrel, acetylsalicylic acid), anticoagulants (for example, warfarin), selective serotonin reuptake inhibitors (for example, fluoxetine, citalopram, sertraline, paroxetine), oral glucocorticosteroids (for example, predisposition);
• elderly age.

Naisulid, instructions for use: method and dosage

Naisulide granules and tablets are intended for oral administration.

To minimize the risk of developing negative side reactions, the drug should be taken in the minimum effective dose for the shortest possible course.

The preferred time of admission is after meals. Patients with gastrointestinal diseases are advised to take Naisulid immediately after a meal or immediately at the end of a meal.

Nysulid tablets should be taken with a sufficient amount of liquid.

The tablet to be dispersed in the oral cavity must be put on the tongue, it will quickly dissolve. If necessary, you can drink it with water (but this is usually not required).

To prepare the suspension, the contents of the sachet should be dissolved in about 100 ml of water at room temperature. The finished solution is white or light yellow. The suspension must be taken immediately, since it cannot be stored.

The recommended dosage regimen of Naisulide for adults and children over 12 years old weighing more than 40 kg:

• tablets: 100 mg twice a day;
• orodispersible tablets: 100 mg twice daily;
• granules for preparation of oral solution: 1 sachet twice a day.

The maximum daily dose of Naisulide is no more than 200 mg.

The duration of therapy for adults and children over 12 years old should not exceed 15 days.

Side effects

Unwanted disorders that occur when taking Naisulid [frequency is classified according to the occurrence: very often - ≥ 1/10; often - (≥ 1/100 and <1/10); infrequently - (≥ 1/1000 and <1/100); rarely - (≥ 1/10 000 and <1/1000); very rare - <(1/10 000, including isolated cases)]:

• cardiovascular system: infrequently - increased blood pressure (BP); rarely - flushes of blood to the skin of the face, tachycardia, palpitations, lability of blood pressure;
• blood and lymphatic system: rarely - eosinophilia, anemia, hemorrhages; very rarely - pancytopenia, thrombocytopenia, thrombocytopenic purpura;
• skin and subcutaneous tissue: infrequently - skin rash, itching, increased sweating; rarely - dermatitis, erythema; very rarely - erythema polyform, toxic epidermal necrolysis (Lyell's syndrome), angioedema, urticaria, facial edema, Stevens-Johnson syndrome;
• immune system: rarely - hypersensitivity reactions; very rarely - anaphylactoid reactions;
• psyche: rarely - nervousness, nightmares, fear;
• nervous system: infrequently - dizziness; very rarely - encephalopathy (Reye's syndrome), headache, drowsiness;
• respiratory system: infrequently - shortness of breath; very rarely - bronchospasm, exacerbation of bronchial asthma;
• kidneys and urinary tract: rarely - urinary retention, hematuria, dysuria; very rarely - oliguria, renal failure, interstitial nephritis;
• liver and biliary tract: often - increased activity of liver enzymes; very rarely - cholestasis, jaundice, hepatitis, fulminant (fulminant) hepatitis, sometimes fatal;
• digestive system: often - nausea, vomiting, diarrhea; infrequently - bleeding in the gastrointestinal tract, ulcer and / or perforation of the stomach or duodenum, flatulence, gastritis, constipation; very rarely - stomatitis, dyspepsia, abdominal pain, tarry stools;
• water and electrolyte metabolism: rarely - hyperkalemia;
• hearing organ and labyrinthine disorders: very rarely - vertigo;
• organ of vision: rarely - blurred vision; very rarely - visual impairment;
• others: infrequently - peripheral edema; rarely - asthenia, malaise; very rarely - hypothermia.

Overdose

Symptoms of an overdose of nimesulide: epigastric pain, nausea, vomiting, drowsiness, apathy (symptomatic and supportive therapy can eliminate these adverse events). In some cases, excessive intake of Naisulide is accompanied by an increase in blood pressure, bleeding in the gastrointestinal tract, acute renal failure, anaphylactoid reactions, respiratory depression, coma.

To stop the above pathologies, symptomatic and supportive therapy is performed. If no more than 4 hours have passed since the overdose, you need to induce vomiting and / or take activated charcoal (the dose of an adult is 60-100 g), and / or an osmotic laxative. Since nimesulide has a high degree of binding to blood plasma proteins (up to 97.5%), hemodialysis, hemoperfusion, forced diuresis and urine alkalization are ineffective. It is necessary to monitor the state of the kidneys and liver. There is no specific antidote.

special instructions

Undesirable side effects can be minimized if Naisulide is used in the minimum effective dose for the shortest possible course necessary to eliminate pain.

There have been reports of extremely rare cases of the development of serious reactions from the liver, sometimes fatal, associated with the use of drugs containing nimesulide. The appearance of symptoms similar to signs of liver damage, such as dark urine, itching, yellowing of the skin, abdominal pain, nausea, vomiting, anorexia, increased activity of hepatic transaminases, is the basis for immediate discontinuation of Naisulide and seeking medical attention. It is forbidden to re-use the drug in such patients.

Short-term use of nimesulide caused reactions from the liver, in most cases reversible.

During therapy with nimesulide, it is necessary to refrain from taking other analgesics, including NSAIDs (including selective COX-2 inhibitors).

In patients with a history of gastrointestinal diseases, such as Crohn's disease, ulcerative colitis, Naisulid should be used with caution, since their exacerbation is possible.

With an increase in the dose of NSAIDs, the risk of bleeding from the gastrointestinal tract, perforation of the stomach or duodenum, peptic ulcers in elderly patients and with a history of ulcerative lesions of the gastrointestinal tract (Crohn's disease, ulcerative colitis) in history increases. For such patients, Naisulid therapy should be started with the lowest possible dose. In addition, they, as well as patients who need the combined use of acetylsalicylic acid in low doses or drugs that can increase the risk of complications from the gastrointestinal tract, need to additionally use gastroprotective agents (proton pump blockers or misoprostol).

Patients with a history of gastrointestinal diseases, especially elderly patients, should inform the doctor about new symptoms from the gastrointestinal tract (especially those that may indicate the development of gastrointestinal bleeding).

Due to the increased risk of ulceration or bleeding, Naisulide is used with caution in patients taking oral corticosteroids, anticoagulants (for example, warfarin), selective serotonin reuptake inhibitors or antiplatelet agents (for example, acetylsalicylic acid).

If the use of Naisulide has led to the development of gastrointestinal bleeding or ulcerative lesions of the gastrointestinal tract, the treatment must be stopped urgently.

There are reports of visual impairments in patients taking other NSAIDs, therefore, if any visual impairment occurs, taking Naisulid should be stopped immediately and an ophthalmological examination should be performed.

Taking nimesulide can lead to fluid retention in the body, and therefore patients with heart and / or renal failure, or arterial hypertension should be especially careful when using Naisulide. And in case of further deterioration of the condition, immediately stop therapy.

Clinical studies and epidemiological data indicate that NSAIDs, especially in high doses or in the case of long-term use, may cause a small risk of stroke or myocardial infarction. There is too little data to exclude the likelihood of such events occurring when taking nimesulide.

If, against the background of Naisulid therapy, signs of the development of an acute respiratory viral infection (ARVI) appear, the drug should be discontinued.

Naisulide is capable of influencing the properties of platelets, and therefore persons with hemorrhagic diathesis should take precautions when taking the drug. Nevertheless, drug therapy does not replace the prophylactic action of acetylsalicylic acid in cardiovascular diseases.

Elderly patients have a particularly high risk of adverse reactions when taking NSAIDs, including bleeding in the gastrointestinal tract and perforations that threaten the patient's life, and a decrease in renal, hepatic and cardiac functions. Patients in this category when taking Naisulid should ensure proper clinical control.

In rare cases, during therapy with NSAIDs, including nimesulide, skin reactions such as exfoliative dermatitis, toxic epidermal necrolysis, and Stevens-Johnson syndrome have occurred. At the first manifestations of a skin rash, damage to the mucous membranes, or other signs of an allergic reaction, you should immediately stop taking Naisulide.

Influence on the ability to drive vehicles and complex mechanisms

There are no data on the effect of Naisulid on the ability to drive vehicles and work with complex mechanisms. In this regard, during the period of drug therapy, care must be taken when engaging in potentially hazardous activities, which require a high concentration of attention and speed of psychomotor reactions.

Application during pregnancy and lactation

Nimesulide, like other NSAIDs that inhibit the synthesis of prostaglandins, can have a negative effect on the course of pregnancy and / or on the development of the embryo. Its use during gestation can lead to hypertension in the fetal pulmonary artery system, premature closure of the ductus arteriosus, impaired renal function, which can develop into renal failure with oliguria in the fetus, and also increase the risk of bleeding, a decrease in the contractile ability of smooth muscle cells of the myometrium, the occurrence of peripheral edema in the mother.

When conducting epidemiological studies, data were obtained confirming an increase in the risk of spontaneous abortion, the development of heart disease and gastroschisis in the case of the use of drugs that block the synthesis of prostaglandins in early pregnancy. The absolute risk of developing cardiovascular abnormalities increases from approximately 1% to 1.5%. It is generally accepted that it increases with increasing dose and duration of use.

Due to the high risk of developing adverse reactions, Naisulide is contraindicated in pregnant women.

When preparing for pregnancy, it should be borne in mind that nimesulide has a negative effect on female fertility. Patients planning to conceive should consult their doctor.

Since there is no data on the penetration of nimesulide into breast milk, it is contraindicated to use Naisulide for breastfeeding women.

Pediatric use

Naisulide is contraindicated in pediatric patients under the age of 12.

With impaired renal function

In the presence of chronic renal failure of mild / moderate severity (CC 30-60 ml / min), dose adjustment is not required.

For patients with severe renal failure (CC less than 30 ml / min), Naisulid is contraindicated.

For violations of liver function

Naisulide is contraindicated in patients with hepatic impairment or active liver disease.

Use in the elderly

When treating elderly patients, it is necessary to take into account possible interactions of Naisulide with other drugs. Drug therapy in patients of this category should be carried out with caution.

Correction of daily doses is not required.

Drug interactions

• other NSAIDs: they can enhance the effect of anticoagulants, for example, warfarin, which leads to an increased risk of bleeding; combined use is not recommended and contraindicated for persons with severe coagulation disorders. In case of an urgent need for combination therapy, blood coagulation indicators should be carefully monitored;
• antiplatelet agents and selective serotonin reuptake inhibitors such as fluoxetine: increase the risk of gastrointestinal bleeding;
• glucocorticosteroids: increase the risk of gastrointestinal ulcers / bleeding;
• ACE inhibitors and angiotensin-II receptor antagonists: under the influence of NSAIDs, the effect of antihypertensive drugs is reduced. In patients with mild to moderate severity of renal failure (CC 30-80 ml / min), the combined use of angiotensin II receptor antagonists, ACE inhibitors and agents that suppress the cyclooxygenase system (antiplatelet agents, NSAIDs) can lead to further deterioration of renal function and the development of acute renal failure, in most cases reversible. It is important to consider these interactions in patients taking nimesulide simultaneously with angiotensin II receptor antagonists or ACE inhibitors. Given the above information, the combined use of these drugs must be carried out with caution, especially in elderly patients. Patients should receive adequate fluid intake,also requires careful monitoring of renal function after the start of simultaneous use;
• mifepristone and prostaglandin analogues: their effectiveness decreases due to the antiprostaglandin action of the latter. Limited data show that taking NSAIDs on the same day as a prostaglandin analog does not affect the effect of mifepristone or a prostaglandin analog on uterine contractility, cervical dilatation, and does not reduce the clinical efficacy of medical abortion;
• furosemide: combined administration with nimesulide contributes to a decrease in AUC by about 20% and a decrease in the cumulative excretion of furosemide without changing its renal clearance. Combination therapy with these drugs requires patients with heart or renal failure to take precautions. In clinical trials, when nimesulide was taken by healthy volunteers under the influence of furosemide, sodium excretion temporarily decreased, to a lesser extent - potassium excretion, and the diuretic effect itself decreased;
• lithium: while taking NSAIDs, the clearance of lithium decreases, which leads to an increase in its concentration in the blood plasma and, as a consequence, an increase in toxicity. Patients on therapy with lithium preparations when using nimesulide should regularly monitor the concentration of lithium in the blood plasma;
• theophylline, glibenclamide, cimetidine, digoxin and antacids (for example, a combination of magnesium hydroxide and aluminum hydroxide): no clinically significant interactions with nimesulide have been observed;
• drugs that are substrates of the CYP2C9 isoenzyme: since nimesulide inhibits the activity of this enzyme, when taken together with these drugs, the concentration of the latter in the blood plasma may increase;
• methotrexate: care must be taken when taking Naisulide less than a day before or after taking methotrexate in order to avoid an increase in the concentration of methotrexate in blood plasma and a subsequent increase in toxic effects;
• cyclosporins: nimesulide, being an inhibitor of prostaglandin synthetases, can increase the nephrotoxicity of cyclosporins;
• diuretics: under the influence of NSAIDs, their effect is reduced.

Analogs

Naysulid analogs are Ameolin, Aponil, Nise, Nemulex, Nimesan, Nimesil, Nimesulid, Nimesulide-Inkampharm, Nimesulid-MBF, Nimesulid-LekT, Nimesulid Canon, Nimesulid-SZ, Nimesuliduli-Teva, Nimesulidin and etc.

Terms and conditions of storage

Store out of the reach of children, at a temperature not exceeding 25 ° C.

The shelf life is 3 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Naisulida

Patients leave positive reviews about Naisulide. It is mainly used to relieve headaches, joint pain, and algomenorrhea. In all cases, the rapid analgesic effect of the drug (10 to 30 minutes) is described, which lasts throughout the day. It is also noted to be effective as an anti-inflammatory agent. In addition, among the advantages, users emphasize its affordable price.

As a disadvantage, the frequent absence of Naisulide in the form of tablets and dispersible tablets is mentioned most of all.

Price for Naisulid in pharmacies

The price for Naisulid in pharmacy chains is:

• tablets, 100 mg (pack of 20) - 120-155 rubles;
• tablets dispersed in the oral cavity, 100 mg (in a package of 20 pcs.) - from 180 rubles;
• granules for preparation of a suspension for oral administration, 100 mg in sachets of 2 g (in a package of 30 pcs.) - 559-675 rubles.

Naisulid: prices in online pharmacies

Drug name Price Pharmacy

Naisulid 100 mg tablets 20 pcs. 136 RUB Buy

Naisulid tablets 100mg 20pcs 154 RUB Buy

Nisulide tablets dispersion. oral 100mg 20pcs RUB 160 Buy

Naisulid 100 mg orodispersible tablets 20 pcs. RUB 160 Buy

Naisulide 100 mg granules 2 g 30 pcs. 547 r Buy

Naisulide granules for suspension for internal approx. 100mg pack. 2g 30 pcs. 585 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!