Amoeolin - instructions for use, dose, side effects, contraindications

Excipients: hypromellose (3.0 mg); cellulose microcrystalline (type 101 and 200) (40.0 mg and 20.0 mg); lactose monohydrate (147.0 mg); starch corn gelatinized (60.0 mg); croscarmellose sodium (20.0 mg); docusate sodium (3.0 mg); magnesium stearate (2.0 mg); Silica colloidal anhydrous dioxide (5.0 mg).

Description:Round, biconvex tablets, from white to light yellow color.

Pharmacotherapeutic group:Non-steroidal anti-inflammatory drugs (NSAIDs)

ATX: & nbsp

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

M.01.A.X.17 Nimesulide

Pharmacodynamics:

Nimesulide is a drug from the group of non-steroidal anti-inflammatory drugs, a class of sulfonanilides. Has anti-inflammatory, analgesic and antipyretic effect. Like most NSAIDs, nimesulide shows its pharmacological action, suppressing the synthesis of prostaglandins. Unlike classic NSAIDs, it acts in the inflammatory zone and suppresses predominantly COX2 and to a weaker degree of COX1, inhibiting the formation of pathogenic pro-inflammatory prostaglandins. Due to the low pH of the preparation (6.5), the gastric mucosa is not significantly damaged. Nimesulide blocks the release of histamine from mast cells; Suppresses the synthesis of elastase, metalloprotease and collagenase, protecting cartilage tissue from damage. Suppressing the release of tumor necrosis factor alpha (TNF-α), nimesulide reduces the hyperallergic effect of kinins.

Pharmacokinetics:

Nimesulide is rapidly and almost completely absorbed from the gastrointestinal tract. After taking 1 tablet, 100 mg the maximum concentration in the blood plasma (about 4 μg / ml) is achieved within 2-3 hours.

The connection with plasma proteins is about 99%.After oral administration, it penetrates the synovial membrane and reaches a concentration in the periarticular fluid exceeding that in the plasma, ranging from 3 to 12 hours. After taking 1 tablet 100 mg, the concentration of nimesulide in female reproductive organs reaches 35-50% of its plasma concentration. The volume of distribution is between 0.18 and 0.39 l / kg. Binding to plasma proteins is reduced in patients with renal and hepatic insufficiency.

Nimesulide is almost completely metabolized to the active metabolite (4-hydroxynimidesulide).

It is excreted by the kidneys in the form of a free or conjugated metabolite (50-71%) and bile (21-29%). The half-life of nimesulide is 2-5 hours, and the active metabolite -3-6 hour.

Indications:

- Pain syndrome of different genesis;

primary dysmenorrhea.

Nimesulide should be prescribed for treatment only as a second-choice drug.

The decision to treat nimesulide is taken by the attending physician after assessing the possible risk for each individual patient (see Contraindications and Special instructions).

Contraindications:

Hypersensitivity, a complete or incomplete combination of bronchial asthma, recurrent polyposis of the nasal mucosa or paranasal sinuses and intolerance to acetylsalicylic acid (ASA) and other NSAIDs (incl.in anamnesis), erosive and ulcerative lesions of the mucous membrane of the stomach and duodenum, active gastrointestinal bleeding, cerebrovascular or other bleeding, inflammatory bowel disease (Crohn's disease, ulcerative colitis) in the phase of exacerbation, hemophilia and other disorders of blood coagulability, decompensated chronic cardiac insufficiency (CHF), hepatic insufficiency or any active liver disease, hepatotoxic reactions with nimesulide in history, alcoholism, drug addict Ia, expressed chronic renal failure (CRF) (CC less than 30 ml / min), progressive renal disease, confirmed hyperkalemia, since the aortocoronary bypass surgery, concurrent treatment with other hepatotoxic drugs, pregnancy, lactation, children under 12 years.

Carefully:

IHD (coronary heart disease), cerebrovascular disease, CHF, dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral arteries, smoking, kidney failure (QC 30-60 ml / min), anamnestic data on the development of gastrointestinal lesions, the presence of infection Helicobacter pylori, old age, long-term use of NSAIDs, severe somatic diseases, simultaneous reception of anticoagulants (incl. warfarin), antiplatelet agents (including ASA, clopidogrel), oral GCS, selective serotonin reuptake inhibitors (incl. citalopram, fluoxetine, paroxetine, sertraline).

Pregnancy and lactation:

Pregnancy

Nimesulide is contraindicated during pregnancy (risk of atony of the uterus and premature closure ductus arteriosus in the fetus).

Breast-feeding

Nimesulide excreted in breast milk. If it is necessary to treat the drug, breastfeeding should be discontinued.

Dosing and Administration:

Adults and children from the age of 12: Inside, 100 mg (1 tablet) after meals, 2 times a day (daily dose of 200 mg).

The course of treatment depends on the clinical situation, should be as short as possible and set by the attending physician. The maximum duration of treatment should not be more than 15 days. With prolonged use of nimesulide, it is necessary to monitor the parameters of the functional state of the liver at a frequency of once every 2 weeks. In the case of critical indicators of ALT, ACT, The drug should be discontinued.

Patients of advanced age (over 65 years): there is no need to adjust the dose.

Side effects:

The following side effects are based on controlled clinical trials * (approximately 7,800 patients) and post-marketing studies.

Side effects are classified by organs and systems and by frequency: very frequent (> 1/10), frequent (≥1 / 100 and <1/10), infrequent (≥1 / 1,000 and <1/100), rare (≥ 1/10 000 and <1/1 000), very rare (<10 000) and with unknown frequency (on the basis of existing data it is impossible to make an estimate).

On the part of the hematopoiesis and lymphatic system

Rare: anemia*, eosinophilia *; Very rare: thrombocytopenia, pancytopenia, purpura;

Co hand immune systems

Rare: hypersensitivity *; Very rare: anaphylaxis;

From the side of metabolism / metabolism, nutrition:

Rare: hyperkalemia*;

From the side CNC and peripheral nervous system

Infrequent: dizziness*; Rare, anxiety *, nervousness *, nightmares *; Very rare: headache, drowsiness, encephalopathy (Reye's syndrome);

From the sense organs

Rare: blurred vision *; Very rare: impaired vision, dizziness;

From the side of the cardiovascular system

Infrequent: hypertension *; Rare: tachycardia *, hemorrhage *, unstable blood pressure *, hot flashes *;

From the respiratory system

Infrequent: dyspnoe *; Very rare: asthma, bronchospasm;

From the digestive system

Frequent: diarrhea *, nausea *, vomiting *, increased levels of hepatic enzymes *; Infrequent: constipation *, flatulence *, gastritis *, gastrointestinal bleeding, ulcers of the duodenum and stomach, perforation; Very rare: abdominal pain, dyspepsia, stomatitis, milena, hepatitis, fulminant hepatitis (including fatal outcome), jaundice, cholestasis;

From the urinary system

Rare: dysuria *, hematuria *, urinary retention *; Very rare: renal failure, oliguria, interstitial nephritis;

From the skin and subcutaneous tissue

Infrequent: itching *, rash *, increased sweating *; Rare: erythema *, dermatitis *; Very rare: urticaria, angioedema, facial edema, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis;

Common violations

Infrequent: edema*; Rare: malaise *, asthenia *; Very rare: hypothermia.

* Frequency is based on clinical trials

Overdose:

Symptoms: a feeling of fatigue, a headache, dizziness, nausea, vomiting, epigastric pain.

Treatment. There is no specific antidote. In case of an overdose, treatment with nimesulide is stopped. General measures are taken to remove the non-resorbed amount of the drug. Symptomatic treatment is performed.

Interaction:

Salicylates or other NSAIDs: It is not recommended simultaneous use with nimesulide because of the increased risk of ulceration of the gastrointestinal tract. Nimesulide displaces salicylic acid when it binds to plasma proteins.

Oral anticoagulants: There is a higher risk of hemorrhage with simultaneous treatment with nimesulide and acenocoumarol. In the first days of treatment, prothrombin time control is necessary.

Methotrexate: with simultaneous application nimesulide may increase the possibility of side effects.

Heparin (parenteral): increased risk of hemorrhage.

Lithium: with simultaneous application nimesulide increases the concentration of lithium in blood plasma. The risk of side effects due to lithium toxicity is increasing.

Furosemide and thiazide diuretics: NSAIDs lower natriuretic effect. With simultaneous treatment with nimesulide and furosemide, it is necessary to monitor the water-salt balance and the diuretic action of furosemide.

ACE Inhibitors: NSAIDs reduce the antihypertensive effect. If necessary, combined treatment, this interaction should be taken into account.

Ticlopidine: increased risk of hemorrhages due to synergistic antiplatelet effect.

Beta-blockers: when used simultaneously with nimesulide, their antihypertensive effect decreases.

Cyclosporin: there is a high risk of intensifying nephrotoxic action with simultaneous application with nimesulide, especially in elderly patients.

Special instructions:

- Nimesulide appoint after a thorough assessment of the risk / benefit ratio.

- In case of fever and the appearance of influenza-like symptoms, the use of nimesulide should be discontinued.

- Patients suffering from bronchial asthma, chronic rhinitis, chronic sinusitis and / or polyposis of the nose, belong to the group with an increased risk of allergic reactions when taking NSAIDs.The use of nimesulide in such patients can cause an asthmatic attack.

- A relatively high risk exists in elderly patients, while using drugs that reduce blood clotting or affect platelet aggregation in people who abuse alcohol and smokers. In such patients, treatment with NSAIDs should begin with the lowest possible dose, with the possible addition of protective agents (eg misoprostol or proton pump inhibitors). This is also recommended in cases of simultaneous use in low doses of acetylsalicylic acid or other drugs that increase the risk of gastrointestinal complications (corticosteroids, selective serotonin reuptake inhibitors).

- Particular caution is required in patients with gastrointestinal diseases such as ulcerative colitis and Crohn's disease, whose aggravation may occur when using NSAIDs.

- Special attention should be paid to patients with an anamnesis of hypertension and / or mild to moderate congestive heart failure, as there are reports of edema and fluid retention associated with the treatment of NSAIDs.

- Clinical studies and epidemiological data show that the use of certain NSAIDs (especially in high doses and for a long time) can be associated with a slight increase in the risk of arterial thrombotic events (eg myocardial infarction or stroke). There is not enough data to exclude such a risk for nimesulide.

- Treatment with nimesulide is not recommended for rapidly progressing rheumatic or post-traumatic conditions.

- When symptoms such as anorexia, nausea, vomiting, abdominal pain, rapid fatigue, dark urine, jaundice, it is necessary to follow the liver laboratory indicators (transaminase, bilirubin, alkaline phosphatase, gamma-GPT). When the hepatic parameters change, treatment with nimesulide should be discontinued. In such patients, repeated use of nimesulide is contraindicated.

- Serious skin reactions, including fatalities, which are very rare in the use of NSAIDs, relate to cases of exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis. The highest risk is noted at the beginning of treatment.The drug should be discontinued at the first cutaneous or other signs of hypersensitivity.

During treatment with nimesulide, renal function should be monitored in patients with chronic heart failure, with diuretic treatment, after surgery, with concomitant hypovolemia, and especially in elderly patients.

At women in reproductive age there is an opportunity of suppression of fertility at application of a preparation.

- Treatment with nimesulide should be stopped immediately if visual impairment occurs.

Amoeolin contains a lactose excipient, which can pose a threat to persons with glucose / galactose malabsorption syndrome.

Effect on the ability to drive transp. cf. and fur:During treatment with nimesulide, it is necessary to refrain from engaging in potentially dangerous activities that require increased attention and speed of psychomotor reactions (motor vehicle management).

Form release / dosage:

Tablets of 100 mg.

Packaging:

For 10 tablets in a blister of PVC film and aluminum foil.

1 (10 tablets) or 2 (20 tablets) blister along with instructions for use in a cardboard pack.

Storage conditions:

In 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 after the expiry date printed on the package!

Terms of leave from pharmacies:On prescription

Registration number:PL-000837

Date of registration:10.10.2011

Expiration Date:10.10.2016

The owner of the registration certificate:Sopharma, AOSopharma, AO Bulgaria

Manufacturer: & nbsp

SOPHARMA, AD Bulgaria

Representation: & nbspSOFARMA SA SOFARMA SA Bulgaria

Information update date: & nbsp03.08.2017

Illustrated instructions

Instructions

Amoeolin (Ameolin)