Nimesan, tablets 100 mg 20 pcs

Pharmacotherapeutic group: Non-steroidal anti-inflammatory drug (NSAID)

ATX code: M01AX17

Pharmacological action

Non-steroidal 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.

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

Decreases the concentration of short-lived prostaglandin H2, from which prostaglandin E2 is formed under the action of prostaglandin isomerase. Decrease of prostaglandin E2 concentration leads to decrease of activation of prostanoid receptors EP type, which is reflected in analgesic and anti-inflammatory effects.

The drug acts on COX-1 to a small extent, practically not preventing formation of prostaglandin E2 from arachidonic acid in physiological conditions, due to which the number of side effects of the drug is reduced.

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

It was shown that nimesulide can inhibit the synthesis of interleukin-6 and urokinase, thus preventing the destruction of cartilage tissue. It 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 products of oxygen decay by reducing the activity of myeloperoxidase. It interacts with glucocorticoid receptors, activating them through phosphorylation, which also increases the anti-inflammatory effect of the drug.

Pharmacokinetics

Absorption when taken orally is high. Food intake reduces the rate of absorption without affecting its degree. Time of reaching maximum concentration of active substance in blood plasma – 1.5-2.5 hours. Binding with plasma proteins is 95%, with red blood cells – 2%, with lipoproteins – 1%, with acidic alpha1-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. It penetrates into the tissues of the female genitalia, where after a single administration its concentration is about 40% of the plasma concentration. It penetrates well into the acidic environment of the inflammation focus (40%) and synovial fluid (43%).

It easily penetrates through the histo-hematic barriers.

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 is 2.89-4.78 hours. 4-hydroxynimesulide is excreted by the kidneys (65%) and in the 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 elderly persons the pharmacokinetic profile of nimesulide does not change significantly.

Indications

Rheumatoid arthritis, Headache, Painful menstruation (algodysmenorrhea)Rheumatoid arthritis, osteoarthritis, arthritis of various etiologies, arthralgia, myalgia, postoperative and posttraumatic pain, bursitis, tendonitis, algodysmenorrhea, toothache and headache.

Active ingredient

Nimesulide

How to take, the dosage

Overly, after meals, 50-100 mg twice a day.

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

The lowest effective dose should be used for the shortest possible course.

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

Interaction

The effect of drugs that reduce blood clotting is increased 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 concomitant use of methotrexate.

The level of lithium in plasma is increased when concomitant use of lithium and nimesulide. Because of the high degree of binding of nimesulide to plasma proteins, patients treated concomitantly with hydantoin and sulfonamides should be monitored by a physician with monitoring at short intervals.

Nimesulide may increase the effect of cyclosporine on the kidneys.

The use with glucocorticosteroids, serotonin reuptake inhibitors increases the risk of GI bleeding.

Special Instructions

When prescribing the drug to elderly patients dosage regimen adjustment is not required.

Long-term use requires systematic monitoring of liver and renal function. Laboratory parameters of liver transaminase activity should be monitored at least once a week.

Contraindications

• high sensitivity to the drug components,
• complete or incomplete combination of bronchial asthma, recurrent nasal or paranasal sinus polyposis and intolerance to acetylsalicylic acid and other NSAIDs (including anamnesis),
• erosive-ulcerative lesions of the mucous membrane of the stomach and duodenum,
• active gastrointestinal bleeding,
• cerebrovascular or other bleeding,
• inflammatory bowel diseaseInflammatory bowel disease (Crohn’s disease, ulcerative colitis) in the acute phase,
• hemophilia and other blood clotting disorders,
• decompensated chronic heart failure,
• hepatic insufficiency or any active liver disease,
• history of hepatotoxic reactions when using nimesulide,
• alcoholism,
• drug abuse,
• explicit chronic renal failure (creatinine clearance less than 30 ml/min),progressive renal disease,
• confirmed hyperkalemia,
• period after aortocoronary bypass,
concurrent use of other hepatotoxic medications,
• pregnancy,
• lactation period,
• children under 12 years of age.

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

Side effects

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

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

Central nervous system: infrequent – dizziness; rare – feeling of fear, nervousness, nightmares; very rare – headache, somnolence, encephalopathy (Reye syndrome).

Respiratory organs: infrequent – shortness of breath; very rare – bronchial asthma, bronchospasm.

Cardiovascular system: infrequent – arterial hypertension; rare – tachycardia, hemorrhages, “hot flashes”.

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

The skin and mucous membranes: infrequent – itching, rash, increased sweating, rare – erythema, dermatitis, very rare – hives, angioedema, swollen face, erythema multiforme, including Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell’s syndrome).

Liver and biliary system: often – increase of “liver” transaminases; very rarely – hepatitis, hepatitis fulminant, jaundice, cholestasis.

Kidney and urinary system: infrequent – edema; rare – dysuria, hematuria, urinary retention, hyperkalemia; very rare – renal failure, oliguria, interstitial nephritis.

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

Allergic reactions: rare – hypersensitivity reactions; very rare – anaphylactoid reactions.

General reactions: rare – general weakness; very rare – hypothermia.

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

Overdose

Symptoms: apathy, drowsiness, nausea, vomiting. These are usually reversible with supportive care. Gastrointestinal bleeding, arterial hypertension, acute renal failure, respiratory depression may occur.

Treatment: symptomatic treatment of the patient and supportive care is required. There is no specific antidote. If overdose occurred within the last 4 hours it is necessary to induce vomiting, provide intake of activated charcoal (60-100 g per adult), osmotic laxatives. Forced diuresis and hemodialysis are ineffective due to high protein binding of the drug.

Similarities

Naiz, Nimesil, Nimesulide, Nemulex, Nimesulide-TEVA, Nimulide, Nimesan tablets 100 mg 20 pcs, Naisulide, Mialais