Prolide - instructions for use, doses, side effects, contraindications

1 the tablet contains nimesulide as an active ingredient 100 mg and auxiliary substances: microcrystalline cellulose, corn starch, magnesium stearate, purified talc, sodium saccharinate, sodium carboxymethyl starch, silicon dioxide colloid, aspartame, mango flavor, citric acid.

Description:pills of light yellow color, round, flat with embossing "N" on one side.

Pharmacotherapeutic group:nonsteroidal anti-inflammatory drug.

ATX: & nbsp

M.01.A.X Other non-steroidal anti-inflammatory drugs

M.01.A.X.17 Nimesulide

Pharmacodynamics:

Nimesulide is a non-steroidal anti-inflammatory drug (NSAID) from the sulfonanilide class. Selective inhibitor of cyclooxygenase-2 (COX-2) - an enzyme involved in the synthesis of prostaglandins - mediators of edema, inflammation and pain. Has anti-inflammatory, analgesic and antipyretic effect.

Reversibly inhibits the formation of prostaglandin Eg, both in the focus of inflammation, and in the ascending pathways of the nociceptive system, including ways of carrying painful spinal cord impulses.

Reduces the concentration of short-lived prostaglandin Hg, from which prostaglandin E2 is formed by prostaglandin isomerase. Reducing the concentration of prostaglandin E2 leads to a decrease in the degree of activation of prostanoid EP receptors, which is expressed in analgesic and anti-inflammatory effects.

The effect on the stomach and kidney mucosa is negligible, because nimesulide weakly inhibits COX-1, responsible for the synthesis of prostaglandins regulating the physiological activity of cells. The drug also suppresses platelet aggregation by inhibiting the synthesis of endoperoxides and thromboxane A2, inhibits the synthesis of platelet aggregation factor, inhibits the activation of plasminogen by increasing the concentration of inhibitor-1.Suppresses the release of histamine, and also reduces the degree of bronchospasm caused by the action of histamine and acetaldehyde. Inhibits the release of tumor necrosis factor a, which causes the formation of cytokinins. Has antioxidant properties, inhibits formation toxic products of oxygen decay due to a decrease in activity myeloperoxidase. Interacts with glucocorticoid receptors, activating them by phosphorylation, which also enhances the anti-inflammatory effect of the drug.

Not only systemic, but also local action of nimesulide was detected (50% of the concentration in the plasma penetrates into the joint).

Pharmacokinetics:

Suction

Nimesulide is well absorbed from the gastrointestinal tract. Eating lowers the absorption rate without affecting its degree. After ingestion of 100 mg of the drug, the time to reach the maximum concentration of the active substance in the blood plasma is 1.5-2.5 hours. The maximum concentration in the blood plasma (C_max) is 3.5 - 6.5 mg / l. Increase in the concentration of the drug in blood plasma is dose-dependent.

Distribution

It circulates in the blood in a connected form. The connection with plasma proteins is 95 %, with erythrocytes - 2%, with lipoproteins -1%, with acid alpha 1-glycoproteids - 1%. The volume of distribution is 0.19-0.35 l / kg. It penetrates into the acidic environment of the inflammatory focus (40%), synovial fluid (43%). Easily penetrates through the histohematological barriers. The drug penetrates into the tissues of the female genital organs, where after a single intake its concentration is about 40 % of the concentration in the plasma. The therapeutic concentration of nimesulide is maintained in blood plasma for up to 6 hours.

Metabolism and excretion

The drug is almost completely metabolized in the liver by tissue monooxygenases, undergoing biotransformation with the formation of several metabolites: the main pharmacologically active 4-hydroxynimidesulide (25%) and several inactive metabolites. The half-life (T1/2) nimesulide is 1.56 - 4.95 hours, 4-hydroxynimidesulide - 2.89-4.78 hours. 4-hydroxynimidesulide is excreted by the kidneys (65%) and bile (35%), is subjected to enterohepatic recirculation. From 1% to 3% of the drug is excreted unchanged in the urine. With prolonged use, the drug does not accumulate.

In children and the elderly, as well as in patients with moderate renal impairment (creatinine clearance 30 to 80 ml / min), the pharmacokinetic profile of nimesulide varies only slightly.

Indications:

Acute and chronic pain of various origins (including migraine, toothache, algodismenorea, preoperative and postoperative pain, post traumatic pain, pain with dorsopathy).

Inflammatory diseases of the musculoskeletal system (arthritis of various etiology, arthralgia), exacerbation of chronic joint diseases (rheumatoid arthritis, osteoarthritis, spondyloarthritis, etc.), tendenitis, bursitis, myalgia, myositis.

Designed for symptomatic therapy, reducing pain and inflammation at the time of use, the progression of the disease does not affect /

Contraindications:

- Hypersensitivity to nimesulide or ancillary components;

- Complete or incomplete combination of bronchial asthma, recurrent nasal polyposis or paranasal sinuses and intolerance to acetylsalicylic acid and other non-steroidal anti-inflammatory drugs (including in history);

- Erosive-ulcerative lesions of the gastrointestinal tract in the acute stage, active gastrointestinal bleeding;

- Cerebrovascular or other bleeding;

- Hemophilia and other bleeding disorders;

- Inflammatory bowel disease (Crohn's disease, ulcerative colitis) during the exacerbation phase;

- Severe renal dysfunction (creatinine clearance (CC) - less than 30 ml / min), progressive kidney disease;

- Any active liver disease, hepatotoxic reactions when using nimesulide in an anamnesis;

- Decompensated heart failure, confirmed hyperkalemia, period after aortocoronary bypass surgery;

- Simultaneous reception of other hepatotoxic drugs;

- Patients with fever and / or influenza-like symptoms;

Alcoholism, drug addiction;

- Pregnancy and lactation;

- Children under 12 years.

Carefully:

arterial hypertension, heart failure, including chronic, ischemic heart disease, diabetes mellitus, cerebrovascular disease, dyslipidemia / hyperlipidemia, peripheral arterial disease, smoking, kidney failure (CC less than 60 ml / min), anamnestic data on the development of gastric ulcerative lesions -intestinal tract, infection Helicobacter pylori, elderly age,long-term use of non-steroidal anti-inflammatory drugs, alcoholism, severe somatic diseases, simultaneous administration of anticoagulants (incl. warfarin), antiplatelet agents (incl. acetylsalicylic acid, clopidogrel), oral glucocorticosteroids, selective serotonin reuptake inhibitors (incl. citalopram, fluoxetine, paroxetine, sertraline).

Pregnancy and lactation:The use of nimesulide may adversely affect female fertility and is not recommended for women planning a pregnancy.

Dosing and Administration:

The preparation in the form of dispersible tablets is intended for oral administration. The tablet is dissolved in water or applied sublingually at the end or after eating.

Adults and children over 12 years of age (body weight at least 40 kg) - 100 mg 1-2 times a day. The maximum daily dose is 200 mg.

Side effects:

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

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

Central nervous system: infrequently - dizziness; rarely - a sense of fear, nervousness, nightmarish dreams; very rarely - headache, drowsiness, encephalopathy (Reye syndrome).

Respiratory system: infrequently - shortness of breath; very rarely - bronchial asthma, bronchospasm. The cardiovascular system: infrequently - arterial hypertension; rarely - tachycardia, hemorrhages, "hot flashes".

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

Skin and mucous membranes: infrequently - itching, rash, increased sweating; rarely: erythema, dermatitis; very rarely: urticaria, angioedema, facial swelling, multiform exudative erythema, incl. Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome).

Liver and biliary system: often - increased "liver" transaminases; very rarely - hepatitis, fulminant hepatitis, jaundice, cholestasis.

Kidney and urinary system: infrequently - swelling; rarely - dysuria, hematuria,

urinary retention, hyperkalemia; very rarely interstitial nephritis.

Hematopoiesis: rarely - anemia, eosinophilia; very rarely - thrombocytopenia, leukopenia, agranulocytosis, pancytopenia, purpura, prolongation of bleeding time

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

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

In case of occurrence of other, not mentioned above, side effects or deterioration of state of health it is necessary to immediately consult a doctor.

Overdose:

Symptoms: increased severity of side effects, apathy, drowsiness, nausea, vomiting. They are usually reversible in providing supportive care for patients. There may be gastrointestinal bleeding, arterial hypertension, acute renal failure, respiratory depression.

Treatment: It requires symptomatic treatment of the patient and supporting care of the patient. There is no specific antidote. In the event that an overdose has occurred within the last 4 hours, it is necessary to wash the stomach, the purpose of activated charcoal, (60-100 g per adult), osmotic laxatives.Forced diuresis, hemodialysis - ineffective because of the high binding of nimesulide to plasma proteins.

Interaction:

Pharmacokinetic interaction - at the level of binding to plasma proteins (increases the concentration of drugs competing for communication with plasma proteins).

The effect of medications that reduce blood coagulability, increases with their simultaneous use with nimesulide.

Nimesulide may reduce the action of furosemide.

Hepatotoxic drugs - increased risk of hepatotoxic action.

The level of lithium in the plasma increases with the simultaneous use of drugs nimesulide and lithium.

Nimesulide may increase the chance of side effects while taking methotrexate.

Because of the high degree of binding of nimesulide to plasma proteins, patients who are treated with hydantoin and sulfonamides at the same time should be under the supervision of a physician, passing the examination at short intervals.

Nimesulide can enhance the action of cyclosporin on the kidneys.

Care should be taken when using the drug with other non-steroidal anti-inflammatory drugs, digoxin, phenytoin,hypotensive drugs, theophylline, antidiabetics.

Special instructions:

To reduce the risk of developing adverse events from the gastrointestinal tract, a minimum effective dose should be used with the minimum possible short course.

It is not recommended to take the drug for a long time, as well as to use it together with other nonsteroidal anti-inflammatory drugs.

With special caution should be appointed nimesulide with arterial hypertension, heart failure and diabetes mellitus (type II).

With caution and in low doses appoint nimesulide with pronounced violations of the liver and kidney function, with disorders of the gastrointestinal tract (peptic ulcer, bleeding, ulcerative colitis), with the simultaneous use of diuretics, anticoagulants and in the elderly. Because the nimesulide partially excreted by the kidneys, dosage for patients with impaired renal function should be reduced, depending on the level of urination.

With prolonged use, systematic monitoring of kidney function is necessary. Patients should undergo regular medical supervision if they nimesulide take medications, which are characterized by an effect on the gastrointestinal tract.

It should avoid co-administration with hepatotoxic drugs, as well as with alcohol. Given reports of visual impairment in patients taking other non-steroidal anti-inflammatory drugs, treatment should be stopped immediately if any visual impairment occurs and the oculist should examine the patient.

If there are signs of hepatotoxicity (skin itching, yellowing of the skin, nausea, vomiting, abdominal pain, darkening of urine, increased activity of "liver" transaminases), stop taking the drug.

When using the drug for more than 2 weeks, it is necessary to monitor the indicators of liver function (transaminase).

Nimesulide can alter the properties of platelets, but does not replace the preventive effect of acetylsalicylic acid in cardiovascular diseases.

Effect on the ability to drive transp. cf. and fur:In some patients, the drug may cause dizziness or drowsiness. Therefore, patients receiving nimesulide, it is necessary to limit activities related to the need for rapid reaction and high concentration of attention.

Form release / dosage:

Tablets are dispersible 100 mg. For 10 tablets in contour non-cellular package (strip) of aluminum foil or in contour mesh PVC / aluminum package (blister); 1 strip / blister or 10 strips / blisters in a pack of cardboard in place with instructions for use.

Packaging:(10) - packings without glue contour (1) - packs cardboard
(10) - packings without cell contour (10) - packs cardboard
(10) - packings, cellular, outline (1) - packs, cardboard
(10) - packings cellular planimetric (10) - packs cardboard

Storage conditions:

List B.

Store in a dry, dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:3 years. Do not use the product after the expiration date stated on the package!

Terms of leave from pharmacies:On prescription

Registration number:П N013006 / 01

Date of registration:11.01.2009

The owner of the registration certificate:Protek Biosystems Pvt. Ltd.Protek Biosystems Pvt. Ltd. India

Manufacturer: & nbsp

PROTECH BIOSYSTEMS, PVT. Ltd. India

Representation: & nbspProtekh Biosystems Pvt.LtdProtekh Biosystems Pvt.LtdRussia

Information update date: & nbsp15.08.2015

Illustrated instructions

Instructions

Prolide (Prolid)