Brustan tablets, No. 10

For adults:

pain syndrome of moderate intensity with trams (bruises, sprains, dislocations, fractures);

postoperative period;

algodismenorrhea;

toothache;

neuralgia;

myalgia;

lumbago;

fibrositis;

tenosynovitis;

rheumatoid arthritis;

osteoarthritis;

ankylosing spondylitis;

sinusitis;

tonsillitis;

headache;

fever.

For children (as an aid):

tonsillitis;

acute infectious and inflammatory diseases of the upper respiratory tract.

Inside.

Adults - 1 table. 3-4 times a day. Children - in a daily dose of 20 mg / kg in several doses.

Film-coated tablets

1 tab.

ibuprofen 400 mg

paracetamol 325 mg

Hypersensitivity;

peptic ulcer of the stomach and duodenum (in the acute phase);

hepatic and / or renal failure;

diseases of the hematopoietic organs;

deficiency of glucoose-6-phosphate dehydrogenase;

Aspirin asthma;

pregnancy;

lactation period.

With care: bronchial asthma, bronchospasm, heart failure.

pharmachologic effect

Combined drug containing ibuprofen (NSAIDs) and paracetamol (analgesic-antipyretic).

Ibuprofen has an analgesic, anti-inflammatory, antipyretic effect. Oppressing COX-1 and COX-2, disrupts the metabolism of arachidonic acid, reduces the amount of prostaglandins (mediators of pain, inflammation and hyperthermic reaction), both in the focus of inflammation and in healthy tissues, suppresses the exudative and proliferative phases of inflammation.

Paracetamol indiscriminately blocks COX, mainly in the central nervous system, has little effect on water-salt metabolism and the gastrointestinal mucosa. It has an analgesic and antipyretic effect. In inflamed tissues, peroxidases neutralize the effect of paracetamol on COX-1 and COX-2, which explains the low anti-inflammatory effect.

Pharmacokinetics

Ibuprofen. Absorption is high. Cmax in plasma is achieved within 1-2 hours after administration. Plasma protein binding - 90%. T1 / 2 - 2 hours. Slowly penetrates into the joint cavity, lingers in the synovial tissue, creating higher concentrations in it than in plasma. After absorption, about 60% of the pharmacologically inactive R-form is slowly transformed into the active S-form. Metabolized. It is excreted by the kidneys (not more than 1% unchanged) and, to a lesser extent, with bile.

Paracetamol. Absorption is high. Cmax in plasma is achieved within 0.5-2 hours after administration. Plasma protein binding - 15%. Penetrates the BBB. It is metabolized in the 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 are conjugated with glutathione to form already inactive metabolites. With a lack of glutathione, these metabolites can block the enzyme systems of hepatocytes and cause their necrosis. The isoenzyme CYP2E1 is also involved in the metabolism of the drug. T1 / 2 - 1-4 hours. It is excreted by the kidneys in the form of metabolites, mainly conjugates. Less than 5% is excreted unchanged. T1 / 2 is 4-5 hours.

Side effect

From the digestive system: NSAIDs-gastropathy - nausea, vomiting, heartburn, anorexia, epigastric discomfort or pain, diarrhea, flatulence; rarely - erosive and ulcerative lesions, bleeding; liver dysfunction, hepatitis, pancreatitis; irritation or dryness in the mouth, pain in the mouth, ulceration of the gum mucosa, aphthous stomatitis; constipation.

From the nervous system: headache, dizziness, insomnia, anxiety, nervousness, irritability, agitation, drowsiness, depression, confusion, hallucinations; rarely - aseptic meningitis (more often in patients with autoimmune diseases).

From the senses: hearing loss, tinnitus, visual impairment, toxic damage to the optic nerve, blurred vision or double vision, scotoma, amblyopia.

From the side of the cardiovascular system: heart failure, increased blood pressure, tachycardia.

From the side of hematopoiesis: anemia (including hemolytic and aplastic), thrombocytopenia, thrombocytopenic purpura, agranulocytosis, leukopenia.

From the respiratory system: shortness of breath, bronchospasm.

From the urinary system: allergic nephritis, acute renal failure, nephrotic syndrome, edema, polyuria, cystitis.

Allergic reactions: skin rash, pruritus, urticaria, Quincke's edema, bronchospasm, dyspnoea, allergic rhinitis, dryness and irritation of the eyes, edema of the conjunctiva and eyelids, eosinophilia, fever, anaphylactic shock, erythema multiforme (non-Stevens Johns syndrome) (Lyell's syndrome).

Laboratory indicators: a decrease in serum glucose concentration, a decrease in hematocrit and hemoglobin, an increase in bleeding time, an increase in serum creatinine concentration, an increase in the activity of hepatic transaminases.

Others: increased sweating.

With long-term use in high doses: ulceration of the gastrointestinal tract mucosa, bleeding (gastrointestinal, gingival, uterine, hemorrhoidal), visual impairment (impaired color vision, scotoma, amblyopia).

Application during pregnancy and lactation

In the I and II trimesters of pregnancy, use is possible only as directed by a doctor in cases where the potential benefit outweighs the possible risk to the mother and the potential risk to the fetus. The use of this combination in the third trimester of pregnancy is contraindicated.

If necessary, use during lactation should stop breastfeeding.

Application for violations of liver function

Contraindicated in liver failure.

Application for impaired renal function

Contraindicated in renal failure.

special instructions

With care: coronary artery disease, chronic heart failure, cerebrovascular disease, dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral arterial disease, smoking, CC less than 60 ml / min, history of gastrointestinal ulcers, Helicobacter pylori infection, advanced age, prolonged use of NSAIDs, alcoholism, severe somatic diseases, concomitant use of oral corticosteroids (including prednisolone), anticoagulants (including warfarin), antiplatelet agents (including acetylsalicylic acid, clopidogrel), selective serotonin reuptake inhibitors (including including citalopram, fluoxetine, paroxetine, sertraline), viral hepatitis, hepatic and / or renal failure of mild or moderate severity, benign hyperbilirubinemia (Gilbert's syndrome, Dubin-Johnson syndrome, Rotor syndrome),cirrhosis of the liver with portal hypertension, nephrotic syndrome.

Simultaneous use with other medicinal products containing paracetamol and / or NSAIDs should be avoided. When using the drug for more than 5-7 days as directed by a doctor, the peripheral blood parameters and the functional state of the liver should be monitored.

With the simultaneous use of indirect anticoagulants, it is necessary to monitor the indicators of the blood coagulation system.

You should avoid taking this combination together with other NSAIDs.

To avoid possible damaging effects on the liver, you should not drink alcohol while taking the drug.

The drug can distort the results of laboratory tests in the quantitative determination of glucose, uric acid in the blood serum, 17-ketosteroids (the drug must be discontinued 48 hours before the study).

Influence on the ability to drive vehicles and mechanisms

During the period of treatment, the patient should refrain from engaging in potentially hazardous activities that require increased attention and speed of psychomotor reactions.

Drug interactions

With simultaneous use with acetylsalicylic acid, ibuprofen reduces its anti-inflammatory and antiplatelet effect (it is possible to increase the incidence of acute coronary insufficiency in patients receiving small doses of acetylsalicylic acid as an antiplatelet agent after the start of administration).

The combination with ethanol, GCS increases the risk of erosive and ulcerative lesions of the gastrointestinal tract.

Ibuprofen enhances the action of direct (heparin) and indirect (coumarin and indandion derivatives) anticoagulants, thrombolytic agents (alteplase, anistreplase, streptokinase, urokinase), antiplatelet agents, colchicine - the risk of hemorrhagic complications increases.

This combination enhances the hypoglycemic effect of insulin and oral hypoglycemic drugs.

Weakens the effects of antihypertensive drugs and diuretics (by inhibiting the synthesis of renal prostaglandins).

Increases the concentration in the blood of digoxin, lithium preparations and methotrexate.

Caffeine enhances the analgesic effect of ibuprofen.

With the simultaneous use of this combination with cyclosporine, gold preparations, nephrotoxicity increases.

With the simultaneous use of this combination with cefamandol, cefoperazone, cefotetan, valproic acid, plikamycin, the incidence of hypoprothrombinemia increases.

Antacids and cholestyramine reduce the absorption of the ibuprofen + paracetamol combination.

Myelotoxic drugs contribute to the manifestation of hematotoxicity of the ibuprofen + paracetamol combination.