2010/09/21

Aponil

Composition, structure and packing

Tablets are white, with a yellowish tinge, round, flat, with the risk of one hand.

1 tab. Nimesulide 100 mg.

Excipients: lactose monohydrate, microcrystalline cellulose, sodium dokuzat, starch, sodium glycolate, gidroksipropiltsellyuloza, hydrogenated vegetable oil, magnesium stearate.

Clinico-pharmacological group: NSAID. Selective COX-2 inhibitor.

Pharmacological action

NSAIDs (nonsteroidal anti-inflammatory drug). Selective inhibitor of cyclooxygenase-2 (COX-2). The drug has anti-inflammatory, analgesic and antipyretic effect, the mechanism of which is due to selective inhibition of COX-2, which leads to a decrease in the synthesis of prostaglandins in inflammation, as well as in the hypothalamus. Influence of the synthesis of prostaglandins in the gastric mucosa and kidney is much less pronounced, which makes good tolerability of nimesulide.

The drug also inhibits lipid peroxidation and the formation of free oxygen radicals, reduces the formation of platelet activating factor, tumor necrosis factor alpha, release of histamine, proteases and other mediators of inflammation.

Pharmacokinetics

Absorption

Once inside Nimesulide is well absorbed from the gastrointestinal tract, Cmax nimesulide plasma levels achieved after 1-2 h (up to 2.5 h). Eating lowers the rate of absorption without affecting its degree.

Distribution

Plasma protein binding is 99%. Vd of 0.19-0.35 L / kg. Therapeutic concentrations of nimesulide in plasma is maintained for 6-8 hours cumulation during long-term use is not observed.

Metabolism

Nimesulide biotransformiruetsya in the liver with the formation of active (gidroksinimesulid - up to 25% of the dose) and several inactive metabolites.

Withdrawal

T1 / 2 of 2-3 hours is excreted in the urine (65-98% of the dose during the day) and faeces (up to 35% of the dose).

Statement
Pain syndrome of different genesis (including headache, toothache, tuberculosis,, posttraumatic and postoperative pain);
fever different genesis (including acute respiratory viral infections and other infectious and inflammatory diseases);
inflammatory diseases of the musculoskeletal (arthritis, osteoarthritis, tendovaginitah, bursitis, myositis).

Dosage regimen

The dose for adults is from 50 to 200 mg, average dose - 100 mg maximum daily dose - 400 mg. Children over 12 years of drug administered in a single dose rate of 1.5 mg / kg body weight (but not more than 100 mg) and the maximum daily dose - 5 mg / kg.

The drug take 2 times per day after meals; pills naturally pure water.

Side effect
On the part of the digestive system: pain in the epigastric region, gastrointestinal ulcerations, diarrhea, heartburn, nausea, increase in liver transaminases; rarely - vomiting.
On the part of the central nervous system: headache, dizziness, drowsiness.
From the urinary system: rarely - hematuria, oliguria, fluid retention in the body, swelling.
On the part of the hemopoietic system: thrombocytopenia, leukopenia, anemia, agranulocytosis, prolongation of bleeding time.

Allergic reactions: skin rash, urticaria, anaphylactic shock.

Contraindications
erosive-ulcerative lesions GIT (exacerbation);
gastrointestinal bleeding;
Aspirin asthma;
severe liver problems;
severe renal dysfunction (CC less than 30 ml / min);
III trimester of pregnancy;
lactation (breastfeeding);
Children under 12 years
hypersensitivity to nimesulide and other NSAIDs.

Application of pregnancy and breastfeeding

The drug can be used during pregnancy only in cases where the expected benefit to the mother outweighs the potential risk to the fetus.

Do not appoint a drug during lactation. If necessary, use during lactation should decide on the termination of breastfeeding.

In experimental studies, does not have embryotoxic and teratogenic action of the drug.

Application for violations of liver function

Contraindicated in severe liver problems.

Application for violations of renal function

Contraindicated in severe renal dysfunction (CC less than 30 ml / min).

Cautions

Precautions should be appointed Aponi in arterial hypertension, heart failure and diabetes mellitus type 2.

With caution and in low doses prescribed Aponi with renal failure, with abnormal liver function, gastric ulcer and duodenal ulcer history, systemic lupus erythematosus, while the use of diuretics, and anticoagulants in the elderly. In appointing Aponi patients with hypersensitivity to other NSAIDs may develop allergic reactions.

Overdose

Symptoms: possible nausea, vomiting.

Treatment: gastric lavage, the appointment of adsorbents, if necessary - infusion therapy, the appointment of osmotic diuretics, holding symptomatic therapy.

Drug Interactions

With simultaneous application of nimesulide competes for binding to plasma proteins and increases the risk of side effects of sulfonylurea derivatives (including oral hypoglycemic funds), hydantoin, digitalis drugs, cyclosporine and methotrexate.

When combined with the use of acetylsalicylic acid, nimesulide is displaced from its association with plasma proteins, with the concentration of free nimesulide in plasma increased by 2-3 times.

With simultaneous application of nimesulide increases the effects of indirect anticoagulants.

When applied simultaneously with the preparations of lithium Nimesulide increases the concentration of lithium in blood plasma.

Terms and Conditions of storage

The product should be stored in dry, dark place at temperatures not above 25 ° C. Shelf life - 3 years.