Nimesan pills 100mg 20pcs

Composition

Per tablet: Active ingredient:

Nimesulide 100,00 mg

Auxiliary substances:

Lactose monohydrate 50.00 mg,

corn starch 216.39 mg,

methyl parahydroxybenzoate 0.60 mg,

propyl parahydroxybenzoate 0.010 mg,

crospovidone (collidone C 1) 13.00 mg,

talc 4.00 mg,

magnesium stearate 1.00 mg

Pharmacological action

Pharmacotherapy group: Nonsteroidal anti-inflammatory drug (NSAID) ATX code: M 01 AH 17 Pharmacological action

Nonsteroidal anti-inflammatory drug (NSAID) from the class of sulfonanilides. It is a selective competitive inhibitor of cyclooxygenase-2 – COX-2), an enzyme involved in the synthesis of prostaglandins – mediators of edema, inflammation, and pain. It has anti-inflammatory, analgesic and antipyretic effects.

Reversibly inhibits the formation of prostaglandin E2, both in the focus of inflammation and in the ascending pathways of the nociceptive system, including the pathways of spinal cord pain impulses.

Reduces the concentration of short-lived prostaglandin H 2, from which prostaglandin E 2 is formed under the action of prostaglandin isomerase. A decrease in the concentration of prostaglandin E 2 leads to a decrease in the degree of activation of EP-type prostanoid receptors, which is expressed in analgesic and anti-inflammatory effects.

To a small extent, it acts on COX-1, practically without interfering with the formation of prostaglandin E 2 from arachidonic acid under physiological conditions, which reduces the number of side effects of the drug.

The drug also suppresses platelet aggregation by inhibiting the synthesis of endoperoxides and thromboxane A2, inhibits the synthesis of platelet aggregation factor, and inhibits plasminogen activation by increasing the concentration of inhibitor-1. Inhibits the release of histamine, and also reduces the degree of bronchospasm caused by exposure to histamine and acetaldehyde. Inhibits the release of tumor necrosis factor a, which causes the formation of cytokinins.

Nimesulide has been shown to inhibit the synthesis of interleukin-6 and urokinase, thereby preventing the destruction of cartilage tissue. Inhibits the synthesis of metalloproteases (elastase, collagenase), preventing the destruction of proteoglycans and collagen of cartilage tissue.

It has antioxidant properties, inhibits the formation of toxic oxygen degradation products by reducing the activity of myeloperoxidase. It interacts with glucocorticoid receptors, activating them by phosphorylation, which also enhances the anti-inflammatory effect of the drug.

Pharmacokinetics

Absorption by mouth is high. Food intake reduces the rate of absorption, without affecting its degree. The time to reach the maximum concentration of the Active ingredient in blood plasma is 1.5 – 2.5 hours. The connection with plasma proteins is 95%, with red blood cells-2%, with lipoproteins-1%, with acidic alpha-1-glycoproteins-1%.

The dose of the drug does not affect the degree of its binding to blood proteins.

The maximum concentration of nimesulide in blood plasma reaches 3.5-6.5 mg/l. The volume of distribution is 0.19-0.35 l / kg. Penetrates into the tissues of the female genital organs, where after a single dose, its concentration is about 40% of the plasma concentration. It penetrates well into the acidic environment of the inflammatory focus (40%), synovial fluid (43%).

Easily penetrates through histo-hematic barriers.

It is metabolized in the liver by tissue monooxygenases. The main metabolite,4-hydroxynimesulide (25%), has similar pharmacological activity.

The half-life of nimesulide is 1.56-4.95 hours,4-hydroxynimesulide-2.89-4.78 hours. 4-hydroxynimesulide is excreted by the kidneys (65%) and bile (35%).

In patients with renal insufficiency (creatinine clearance 1.8-4.8 l/h or 30-80 ml/min), as well as in children and the elderly, the pharmacokinetic profile of nimesulide does not change significantly.

Indications

Rheumatoid arthritis, osteoarthritis, arthritis of various etiologies, arthralgia, myalgia, postoperative and post-traumatic pain, bursitis, tendonitis, algodismenorrhea, tooth and headache.

Contraindications

• hypersensitivity to the components of the drug,
• complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose or paranasal sinuses and intolerance of acetylsalicylic acid and other NSAIDs (including in history),
• erosive and ulcerative lesions of the gastric mucosa and duodenal ulcers,
• active gastrointestinal bleeding,
• cerebrovascular or other bleeding,
• inflammatory bowel disease (Crohn’s disease, ulcerative colitis) in the acute phase,
• hemophilia and other blood clotting,
• decompensated congestive heart failure,
• liver failure, or any active liver disease
• hepatotoxic reactions when using nimesulide, a history of
• alcoholism,
• drug abuse,
• severe chronic renal failure (creatinine clearance less than 30 ml/min),
• progressive kidney diseases,
• confirmed hyperkalemia,
• period after coronary artery bypass grafting conduct,
• concomitant use of other hepatotoxic drugs,
• pregnancy,
• lactation,
• children’s age up to 12 years.

With caution:  coronary heart disease, cerebrovascular diseases, chronic heart failure, dyslipidemia/hyperlipidemia, diabetes mellitus, peripheral arterial diseases, smoking, renal failure (creatinine clearance 30-60 ml/min), anamnestic data on the development of ulcerative lesions of the gastrointestinal tract, the presence of Helicobacter pylori infection, the elderly, long-term use of nonsteroidal anti-inflammatory drugs, alcoholism, severe somatic diseases, concomitant use anticoagulants (including warfarin), antiplatelet agents (including acetylsalicylic acid, clopidogrel), oral glucocorticosteroids, selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline).

Side effects

Frequency is classified by category, depending on the occurrence of the case: very often (>10), often (><10 – <100), infrequently (<100-<1000), rarely (<1000-< 10000), very rarely (

Gastrointestinal tract:  often – diarrhea, nausea, vomiting; infrequently-constipation, flatulence, gastritis; very rarely-abdominal pain, stomatitis, tarry stools, gastrointestinal bleeding, ulceration and / or perforation of the stomach or duodenum.

Central nervous system:  infrequently – dizziness; rarely-feeling of fear, nervousness, nightmares; very rarely-headache, drowsiness, encephalopathy (Reye’s syndrome).

Respiratory organs:  infrequently-shortness of breath; very rarely-bronchial asthma, bronchospasm.

Cardiovascular system:  infrequently-arterial hypertension; rarely-tachycardia, hemorrhages, hot flashes.

Sensory organs:  rarely-blurred vision, very rarely-dizziness.

Skin and mucous membranes:  infrequently-pruritus, rash, increased sweating; rarely: erythema, dermatitis; very rarely: urticaria, angioedema, facial edema, erythema multiforme, including Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell’s syndrome).

Liver and biliary system:  often-an increase in “hepatic” transaminases; very rarely-hepatitis, lightning hepatitis, jaundice, cholestasis.

Kidneys and urinary system:  infrequently-edema; rarely-dysuria, hematuria, urinary retention, hyperkalemia; very rarely-renal failure, oliguria, interstitial nephritis.

Hematopoietic organs:  rarely-anemia, eosinophilia; very rarely-thrombocytopenia, pancytopenia, purpura, prolongation of bleeding time.

Allergic reactions:  rarely-hypersensitivity reactions; very rarely-anaphylactoid reactions.

General reactions:  rarely-general weakness; very rarely – hypothermia.

If you experience any other side effects that are not mentioned above, or if you feel unwell, please contact your doctor immediately.

Interaction

The effect of medications that reduce blood clotting is enhanced when they are used simultaneously with nimesulide.

Nimesulide may reduce the effect of furosemide. Reduces the therapeutic effect of antihypertensive drugs. Nimesulide may increase the possibility of side effects when taking methotrexate at the same time.

The level of lithium in plasma increases with simultaneous administration of lithium and nimesulide preparations. Due to the high degree of binding of nimesulide to plasma proteins, patients treated simultaneously with hydantoin and sulfonamides should be monitored by a doctor, undergoing examinations at short intervals.

Nimesulide may increase the effect of cyclosporine on the kidneys.

Use with glucocorticosteroids, serotonin reuptake inhibitors increases the risk of gastrointestinal bleeding.

How to take it, course of administration and dosage

Inside, after meals,50-100 mg 2 times a day.

In patients with chronic hepatic insufficiency, the daily dose is 100 mg.

The minimum effective dose should be used in the shortest possible course.

Children over 12 years of age are prescribed at the rate of a single dose of 1.5 mg/kg of the child’s body weight, the maximum daily dose of the drug is 5 mg / kg per day (no more than 200 mg / day).

Overdose

Symptoms:  apathy, drowsiness, nausea, vomiting. They are usually reversible when providing supportive care for patients.Gastrointestinal bleeding, hypertension, acute renal failure, and respiratory depression may occur. Treatment: the patient needs symptomatic treatment and supportive care. There is no specific antidote. If an overdose has occurred within the last 4 hours, it is necessary to induce vomiting, provide activated charcoal (60-100 g per adult), osmotic laxatives. Forced diuresis and hemodialysis are ineffective due to the high binding of the drug to proteins.

Special instructions

When prescribing the drug to elderly patients, no dosage adjustment is required. With prolonged use, systematic monitoring of liver and kidney function is necessary. It is necessary to monitor laboratory parameters of hepatic transaminase activity at least once a week.

Storage conditions

At a temperature not exceeding 25°C. Keep out of reach of children.

Shelf

life is 3 years. Do not use after the expiration date indicated on the package.

Active ingredient

Nimesulide

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

Children as directed by a doctor, Children over 12 years of age, Adults as directed by a doctor

Indications

Dislocations and Sprains, Osteoarthritis, Arthritis, Rheumatoid Arthritis, Myositis, Migraines, Sciatica, Tendon Inflammation, Osteochondrosis, Bursitis, Lumbago, Gout, Sciatica, Osteoarthritis