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

A selective cyclooxygenase inhibitor, an enzyme that catalyzes the reaction of the conversion of arachidonic acid to prostaglandin H₂, which is a precursor of the remaining prostaglandins, thromboxane A₂ and prostacyclin. Has anti-inflammatory and analgesic, as well as antipyretic effect.

It acts primarily on cyclooxygenase-2, therefore it suppresses the synthesis of prostaglandins in the inflammatory foci to a greater extent,than in the mucous membrane of the stomach and in the kidneys.

Without affecting phagocytosis and hemostasis nimesulide suppresses the formation of free oxygen radicals. Inhibits the release of myeloperoxidase.

Pharmacokinetics:

After oral administration, an empty stomach is absorbed up to 80% in the gastrointestinal tract. The maximum concentration in the blood plasma is reached after 1-2 hours. The connection with plasma proteins is 99%.

Therapeutic effect develops after the reception. Metabolism in the liver. One of the metabolites (25%) - hydroxynimidesulide also has pharmacological activity.

Half-life is 2-3 hours. Elimination by the kidneys is 65% and with feces - 35%. Do not cumulate.

Indications:

It is used for the treatment of osteoarthritis, rheumatoid arthritis, ostearthrosis, bursitis, tendinitis, pain syndromes of various etiology, including postoperative period and gynecological diseases. Used for injuries and fever caused by infectious and inflammatory diseases.

ICD-10

XIII.M05-M14.M05.8 Other seropositive rheumatoid arthritis

XIII.M15-M19.M15 Polyarthrosis

XIV.N80-N98.N94.6 Dysmenorrhea, unspecified

XIV.N80-N98.N94.5 Secondary dysmenorrhea

XIV.N80-N98.N94.4 Primary dysmenorrhea

XVIII.R50-R69.R50 Fever of unknown origin

XVIII.R50-R69.R52.9 Pain, unspecified

XVIII.R50-R69.R52.2 Another constant pain

XVIII.R50-R69.R52.1 Constant unrestrained pain

XVIII.R50-R69.R52.0 Acute pain

XVIII.R50-R69.R51 Headache

XVIII.R00-R09.R07 Sore throat and chest

XIII.M50-M54.M54.6 Pain in the thoracic spine

XIII.M50-M54.M54.5 Lower back pain

XIII.M20-M25.M25.5 Pain in the joint

Contraindications:

Peptic ulcer of stomach and duodenum, ulcerative colitis, gastritis.

Individual intolerance.

Carefully:

Severe renal and hepatic insufficiency.

Pregnancy and lactation:

Recommendations for FDA - in the first and second trimesters - B, in the third - D. Contraindicated during lactation.

Dosing and Administration:

Inside after eating 100 mg 2 times / day; subcutaneously 75 mg (2 ml) once a day.

Outdoor application: 1% 3 cm gel is applied to the affected area and rubbed into intact skin.

The highest daily dose: 200 mg.

The highest single dose: 100 mg.

Side effects:

Central and peripheral nervous system: dizziness, drowsiness.

The system of hematopoiesis: rarely - thrombocytopenia.

Digestive system: nausea, heartburn, diarrhea.

Urinary system: rarely - oliguria.

With topical application in the place of application: erythema, itching, flaking, transient skin discoloration.

Allergic reactions.

Overdose:

Pain in epigastrium, nausea, vomiting, drowsiness. Rarely - gastrointestinal bleeding, muscle twitching, respiratory depression, coma.

Symptomatic therapy.

Interaction:

Increases the effectiveness of oral hemocoagulants.

With simultaneous use with barbiturates, narcotic analgesics, caffeine, phenothiazine derivatives, diphenhydramine, phenacetin, analgesic effects are enhanced.

Anti-inflammatory effect increases salicylates and metamizol sodium.

Special instructions:

Coagulogram monitoring with prolonged use of the drug. During treatment with the drug should refrain from driving the car and works requiring increased concentration of attention.

Instructions

Nimesulide (Nimesulidum)