Ibuklin tablets 400 + 325mg, No. 10

• Feverish conditions (including with flu and colds);

• myalgia;

• neuralgia;

• back pain;

• joint pain, pain syndrome in inflammatory and degenerative diseases of the musculoskeletal system;

• pain with bruises, sprains, dislocations, fractures;

• post-traumatic and postoperative pain syndrome;

• toothache;

• algodismenorrhea (painful menstruation).

The drug is intended for symptomatic therapy, reducing pain and inflammation at the time of use; does not affect the progression of the disease.

Inside, before or 2-3 hours after meals, without chewing, drinking plenty of water.

Adults. 1 table. 3 times a day. The maximum daily dose is 3 tablets.

Children over 12 years old (body weight over 40 kg). 1 table. 2 times a day.

The duration of treatment is no more than 3 days as an antipyretic agent and no more than 5 days as a pain reliever. Continuation of treatment with the drug is possible only after consulting a doctor.

Film-coated tablets

1 tab.

active substances:

ibuprofen 400 mg

paracetamol 325 mg

excipients: MCC - 120 mg; corn starch - 76 mg; glycerol - 3 mg; sodium carboxymethyl starch (type A) - 7 mg; colloidal silicon dioxide - 5 mg; talc - 8 mg; magnesium stearate - 6 mg film shell: hypromellose 6 cps - 11.32 mg; dye 'Sunset Sun' yellow (E110), aluminum varnish - 1.78 mg; macrogol 6000 - 2.2 mg; talc - 4.06 mg; titanium dioxide - 0.16 mg; polysorbate 80 - 0.16 mg; sorbic acid - 0.16 mg; dimethicone - 0.16 mg

• Hypersensitivity to the components of the drug (including other NSAIDs);

• peptic ulcer of the stomach and duodenum in the acute phase;

• gastrointestinal bleeding;

• severe renal failure (Cl creatinine less than 30 ml / min);

• complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose and paranasal sinuses and intolerance to acetylsalicylic acid or other NSAIDs (including history);

• damage to the optic nerve;

• hereditary insufficiency of glucose-6-phosphate dehydrogenase;

• diseases of the blood system;

• period after coronary artery bypass grafting;

• progressive kidney disease;

• severe liver failure or active liver disease;

• confirmed hyperkalemia;

• active gastrointestinal bleeding;

• inflammatory bowel disease;

• pregnancy (III trimester);

• children under 12 years of age.

With care: coronary heart disease; chronic heart failure; cerebrovascular diseases; dyslipidemia / hyperlipidemia; diabetes; peripheral arterial disease; smoking; Cl creatinine less than 60 ml / min; history of ulcerative lesions of the gastrointestinal tract; presence of Helicobacter pylori infection; elderly age; long-term use of NSAIDs; alcoholism; severe somatic diseases; simultaneous administration of oral corticosteroids (including prednisone), anticoagulants (including warfarin), antiplatelet agents (including acetylsalicylic acid, clopidogrel), SSRIs (including citalopram, fluoxetine, paroxetine, sertraline ); viral hepatitis; hepatic and / or renal failure of moderate and mild severity; benign hyperbilirubinemia (Gilbert, Dubin-Johnson and Rotor syndrome); cirrhosis of the liver with portal hypertension;nephrotic syndrome.

pharmachologic effect

Combined drug, the action of which is due to its constituent components.

Ibuprofen - NSAIDs, 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.

The effectiveness of the combination is higher than that of the individual components. Weakens arthralgia at rest and during movement, reduces morning stiffness and swelling of the joints, helps to increase the range of motion.

Pharmacokinetics

Ibuprofen

Absorption and distribution

Absorption - high, quickly and almost completely absorbed from the gastrointestinal tract. Tmax after oral administration - about 1-2 hours. Plasma protein binding is more than 90%. It slowly penetrates into the joint cavity, accumulates in the synovial fluid, creating higher concentrations in it than in the blood plasma.

Metabolism and excretion

After absorption, about 60% of the pharmacologically inactive R-form is slowly transformed into the active S-form. Metabolized.

T1 / 2 - about 2 hours. More than 90% is excreted by the kidneys (unchanged, no more than 1%) and, to a lesser extent, with bile in the form of metabolites and their conjugates.

Paracetamol

Absorption and distribution

Absorption is high, binding to plasma proteins is less than 10% and slightly increases in case of overdose. Sulfate and glucuronide metabolites do not bind to plasma proteins even at relatively high concentrations. Cmax - 5-20 ?g / ml, Tmax is 0.5-2 hours. It is evenly distributed in body fluids. Penetrates the BBB. Less than 1% of the taken dose of paracetamol penetrates into breast milk.

Metabolism

About 90-95% of paracetamol is metabolized in the liver to form inactive conjugates with glucuronic acid (60%), taurine (35%) and cysteine ??(3%), as well as a small amount of hydroxylated and deacetylated metabolites. A small part of the drug is hydroxylated by microsomal enzymes to form highly active N-acetyl-n-benzoquinone imine, which binds to sulfhydryl groups of glutathione. When glutathione reserves in the liver are depleted (in case of overdose), the enzyme systems of hepatocytes can be blocked, leading to the development of their necrosis.

Withdrawal

T1 / 2 - 2-3 hours. It is excreted by the kidneys, mainly in the form of glucuronide and sulfate conjugates (less than 5% - unchanged).

Pharmacokinetics in special clinical situations

In patients with liver cirrhosis, T1 / 2 increases slightly.

In elderly patients, the clearance of the drug decreases and T1 / 2 increases.

In children, the ability to form conjugates with glucuronic acid is lower than in adults.

Side effect

From the digestive system: NSAID-gastropathy - nausea, vomiting, heartburn, anorexia, discomfort or pain in the epigastrium, 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 and sensory organs: headache, dizziness, insomnia, anxiety, nervousness, irritability, agitation, drowsiness, depression, confusion, hallucinations; rarely - aseptic meningitis (more often in patients with autoimmune diseases); 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 the drug in the third trimester of pregnancy is contraindicated.

If necessary, the use of the drug during lactation (breastfeeding) should stop breastfeeding.

In experimental studies, the embryotoxic, teratogenic and mutagenic effects of the components of the IbuklinЃ drug have not been established.

Application for violations of liver function

Contraindicated in severe liver failure or active liver disease.

The drug should be used with caution in viral hepatitis, mild to moderate hepatic failure, benign hyperbilirubinemia (Gilbert's syndrome, Dubin-Johnson syndrome, Rotor syndrome), liver cirrhosis with portal hypertension.

Application for impaired renal function

Contraindicated in severe renal failure (CC less than 30 ml / min), progressive kidney disease.

The drug should be used with caution in case of mild or moderate renal failure, nephrotic syndrome.

Application in children

Contraindicated in children under 12 years of age.

Use in elderly patients

The drug should be taken with caution in old age.

special instructions

Avoid the simultaneous use of the drug with other drugs containing paracetamol and / or NSAIDs. 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 IbuclinЃ 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 of 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.

Overdose

Symptoms: gastrointestinal disorders (diarrhea, nausea, vomiting, anorexia, epigastric pain), increased prothrombin time, bleeding after 12-48 hours, lethargy, drowsiness, depression, headache, tinnitus, impaired consciousness, heart disorders rhythm, decrease in blood pressure, manifestations of hepato- and nephrotoxicity, convulsions, possibly the development of hepatonecrosis.

Treatment: in case of overdose delay, the patient should immediately seek medical help. Gastric lavage is recommended for the first 4 hours; alkaline drinking, forced diuresis; activated charcoal inside, the introduction of SH-group donors and precursors of the synthesis of glutathione - methionine 8-9 hours after an overdose and N-acetylcysteine ??inside or intravenously - after 12 hours, antacids; hemodialysis; symptomatic therapy. The need for additional therapeutic measures (further administration of methionine, intravenous administration of N-acetylcysteine) is determined depending on the concentration of paracetamol in the blood, as well as on the time elapsed after its administration.

Drug interactions

With the simultaneous use of the drug IbuklinЃ with drugs, the development of various interaction effects is possible.

When taken simultaneously 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 admission).

The combination with ethanol, corticotropin corticosteroids 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.

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.

Cyclosporine and gold preparations increase nephrotoxicity.

Cefamandol, cefoperazone, cefotetan, valproic acid, plikamycin increase the incidence of hypoprothrombinemia.

Antacids and cholestyramine reduce the absorption of the drug.

Myelotoxic drugs contribute to the manifestation of hematotoxicity of the drug.