Brustan, 1000 mg 10 pcs

Pharmacotherapeutic group

Non-steroidal anti-inflammatory drug (NSAID) and analgesic non-narcotic.

The ATC code: M01AE51.

Pharmacological properties

A combination drug. It has analgesic, anti-inflammatory and antipyretic effects. The mechanism of anti-inflammatory action of ibuprofen is due to inhibition of cyclogenase (COX) activity with subsequent inhibition of prostaglandin synthesis.

Paracetamol is a non-narcotic analgesic which blocks COX mainly in CNS, affecting centers of pain and thermoregulation, has analgesic and antipyretic effect.

Pharmacokinetics

Ibuprofen is well absorbed from the stomach. Tmax is about 1 hour. Absorption is slightly reduced when the drug is taken after a meal. About 99% is bound to plasma proteins. Ibuprofen is slowly distributed in synovial fluid and is eliminated from it more slowly than from plasma. It is metabolized in the liver, mainly through hydroxylation and carboxylation of isobutyl group. CYP2C9 isoenzyme is involved in metabolism of the drug. After absorption about 60% of pharmacologically inactive R-form of ibuprofen is slowly transformed into active S-form. It has biphasic elimination kinetics. The plasma elimination half-life (T ? ) is 2-3 hours. Up to 90% of the dose can be detected in the urine as metabolites and their conjugates. Less than 1% is excreted unchanged in the urine and, to a lesser extent, in the bile. Ibuprofen is completely eliminated within 24 hours.

Paracetamol is quickly absorbed from the gastrointestinal tract. Time to reach C max in 0.5-2 hours. It is evenly distributed in body fluids. Binding to plasma proteins is variable within 15%. It penetrates through the BBB. It is metabolized in liver (90-95%): 80% enters into conjugation reactions with glucuronic acid and sulfates to form inactive metabolites; 17% undergoes hydroxylation to form 8 active metabolites, which when conjugated with glutathione form inactive metabolites. In case of glutathione deficiency these metabolites can block enzyme systems of hepatocytes and cause their necrosis. The CYP2E1 isoenzyme is involved in the metabolism of paracetamol. T 1/2 1-4 hours. It is excreted by the kidneys as conjugates and only 3% unchanged. In elderly patients, paracetamol clearance is decreased and T1/2 is increased.

Indications

For adults:

In children (as an adjunct): tonsillitis; acute inflammatory and infectious diseases of the upper respiratory tract.

Active ingredient

How to take, the dosage

Interaction

Special Instructions

The drug should be administered in the lowest effective dose, for the shortest possible course.

The peripheral blood count and the functional state of the liver and kidneys should be monitored during treatment.

In case of gastropathy symptoms a thorough control is indicated, including esophagogastroduodenoscopy, blood tests with determination of hemoglobin and hematocrit, stool examination for occult blood.

In order to prevent the development of NSAID gastropathy it is recommended to combine it with prostaglandin E preparations (misoprostol).Patients should refrain from all activities requiring increased attention, rapid mental and motor reactions. During treatment the intake of alcohol (ethanol) is not recommended.

When concomitant use with indirect anticoagulants, the clotting system should be monitored.

Contraindications

Side effects

Overdose

Similarities