Ибуклин®

General characteristics. Structure:

Active agent: ibuprofen of 400 mg and paracetamol of 325 mg.
Excipients: cellulose of microcrystallic 120 mg, starch of corn 76 mg, глицерол 3 mg, sodium carboxymethylstarch (type A) of 7 mg, silicon dioxide of colloid 5 mg, talc of 8 mg, magnesium stearate of 6 mg.
Cover: gipromelloza of 6 cps of 11,32 mg, dye sunset yellow (E110) varnish of aluminum 1,78 mg, macrogoal-6000 of 2,2 mg, talc of 4,06 mg, titanium dioxide of 0,16 mg, polysorbate-80 of 0,16 mg, sorbic acid of 0,16 mg, диметикон 0,16 mg.

Description
Tablets of a kapsulovidny form, coated orange color, with risky on one party; for separate tablets the coloring mramornost is allowed.

Pharmacological properties:

Pharmacodynamics. The combined drug which effect is caused by the components which are its part.
The ibuprofen - non-steroidal anti-inflammatory drug (NPVP), has analgetic, antiinflammatory, febrifugal effect. Oppressing a tsikloksigenaza (TsOG) 1 and 2, breaks metabolism of arachidonic acid, reduces amount of prostaglandins (mediators of pain, an inflammation and hyper thermal reaction), both in the inflammation center, and in healthy fabrics, suppresses exudative and proliferative phases of an inflammation.
Paracetamol - not selectively blocks TsOG, is preferential in the central nervous system, poorly influences a water salt metabolism and a mucous membrane of the digestive tract (DT). Has anesthetic and febrifugal effect. In the inflamed fabrics of peroxidase neutralize influence of paracetamol on TsOG 1 and 2 that explains low antiinflammatory effect.
Efficiency of a combination is higher, than separate components. Weakens an arthralgia at rest and at the movement, reduces morning constraint and a swelling of joints, promotes increase in volume of movements.

Pharmacokinetics. Ibuprofen.
Absorption - high, is quickly and almost completely soaked up from the digestive tract (DT). Time of achievement of the maximum concentration (TCmax) after intake - about 1-2 hours. Communication with proteins of a blood plasma - more than 90%. An elimination half-life (T1/2) - about 2 h. Slowly gets into a cavity of joints, collects in synovial fluid, creating in it higher concentration, than in a blood plasma. After absorption about 60% pharmacological of an inactive R-form are slowly transformed to an active S-form. Is exposed to metabolism. More than 90% are removed by kidneys (in an invariable look no more than 1%) and, to a lesser extent, with bile in the form of metabolites and their conjugates.
Paracetamol.
Absorption - high, communication with proteins of plasma - less than 10% and slightly increases at overdose. Sulphatic and glyukuronidny metabolites do not contact proteins of plasma even in rather high kontsetration. The size Cmax - 5-20 mkg/ml, TCmax - 0,5-2 hours. It is rather evenly distributed in fluid mediums of an organism. Gets through a blood-brain barrier.
About 90-95% of paracetamol are metabolized in a liver with formation of inactive conjugates with glucuronic acid (60%), taurine (35%) and cysteine (3%), and also a small amount of hydroxylated and deacetylated metabolites. A small part of drug is hydroxylated by microsomal enzymes with education highly active N-acetyl-n-benzokhinonimina which contacts sulphhydryl groups of glutathione. At exhaustion of reserves of glutathione in a liver (at overdose) fermental systems of hepatocytes can be blocked, leading to development of their necrosis.
T1/2 is 2-3 h. At patients with cirrhosis of T1/2 increases a little. At elderly patients the clearance of drug decreases and T1/2 increases. It is removed by kidneys, preferential, in the form of glyukuronidny and sulphatic conjugates (less than 5% - in not changed look). Less than 1% of the accepted paracetamol dose get into breast milk. At children ability to formation of conjugates with glucuronic acid is lower, than at adults.

Indications to use:

Decrease in the increased body temperature (a feverish syndrome) at catarrhal and other infectious and inflammatory diseases.
Pain syndrome of weak or moderate intensity of various etiology: at inflammatory diseases of a musculoskeletal system (a pseudorheumatism, the psoriasis, juvenile and chronic arthritis ankylosing a spondylitis; gouty arthritis);
at degenerative diseases of a musculoskeletal system (the deforming osteoarthrosis, osteochondrosis);
at diseases of circumarticular fabrics (a tendovaginitis, a bursitis);
lumbago, sciatica, neuralgia, mialgiya;
posttraumatic pain syndromes (bruises, stretchings, dislocations, fractures, bruises of soft tissues);
dentagra;
headache.
Drug is intended for symptomatic therapy, reduction of pain and an inflammation at the time of use, does not influence progressing of a disease.

Route of administration and doses:

Inside (to or in 2-3 h after food), without chewing, washing down with enough water. To adults and children 12 years – on 1 tablet 2-3 times a day are more senior. The minimum interval between administration of drug – 4 hours. The maximum dose for adults: one-time – 2 tablets, daily – 6 tablets.
At renal failures or a liver, for patients of advanced age the break between administrations of drug has to be not less than 8 hours.
It is not necessary to accept drug more than 5 days as anesthetic and more than 3 days as febrifugal without observation of the doctor.

Precautionary measures at use
Coronary heart disease, chronic heart failure, cerebrovascular diseases, dislipidemiya / lipidemia, diabetes mellitus, diseases of peripheral arteries, smoking, KK less than 60 ml/min., digestive tract cankers in the anamnesis, existence of an infection of Helicobacter pylori, advanced age, long use of NPVP, an alkolizm, heavy somatopathies, a concomitant use of peroral glucocorticosteroids (including, Prednisolonum), anticoagulants (including, warfarin), antiagregant (including, acetylsalicylic acid, klopidogret), selective serotonin reuptake inhibitors (including, a tsitaloprama, fluoxetine, a paroksetin, sertraline).

Features of use:

Expediency of use of drug as antipyretic is solved in each case depending on expressiveness, character and portability of a feverish syndrome. For decrease in risk of development of the undesirable phenomena from a GIT it is necessary to use a minimal effective dose minimum possible short course.
At simultaneous use of anticoagulants of indirect action it is necessary to control indicators of coagulant system of blood.
It is necessary to avoid joint administration of drug of Ibuklin® with other NPVP.
In order to avoid the possible damaging action on a liver during administration of drug it is not necessary to take alcohol.
At long (more than 5 days) administration of drug control of peripheral blood and a functional condition of a liver is necessary.
Drug can distort results of laboratory researches at quantitative definition of glucose, uric acid in blood serum, 17 ketosteroids (drug withdrawal for 48 h prior to a research is necessary).

Influence on ability to manage vehicles, mechanisms
During treatment the patient has to abstain from occupations potentially dangerous types of activity requiring special attention and speed of psychomotor reactions.

Side effects:

From the alimentary system: seldom – the dispeptic phenomena, at prolonged use in high doses – a hepatotoxic action.
From system of a hemopoiesis: seldom – thrombocytopenia, a leukopenia, a pancytopenia, a neutropenia, an agranulocytosis.
Allergic reactions: seldom – skin rash, an itch, a small tortoiseshell.

Interaction with other medicines:

At simultaneous use of the drug Ibuklin® with medicines development of various effects of interaction is possible.
The long combined use with paracetamol increases risk of development of nefrotoksichny effects.
The combination to ethanol, glucocorticosteroids, corticotropin increases risk of an erosive canker of a GIT.
The ibuprofen strengthens action of straight lines (heparin) and indirect (derivatives of coumarin and an indandion) anticoagulants, thrombolytic agents (an alteplaza, an anistreplaza, Streptokinasa, an urokinase), antiagregant,  colchicine the risk of development of hemorrhagic complications increases.
Strengthens hypoglycemic effect of insulin and peroral hypoglycemic medicines.
Weakens effects of hypotensive medicines and diuretics (at the expense of inhibition of synthesis of renal prostaglandins).
Increases concentration in blood of digoxin, drugs of lithium and a methotrexate.
Caffeine strengthens analgeziruyushchy action of an ibuprofen.
Cyclosporine and drugs of gold increase nephrotoxicity.
Tsefamandol, цефаперазон, цефотетан, valproic acid, пликамицин increase the frequency of development of a prothrombinopenia.
Antacids and Colestyraminum reduce drug absorption.
Myelotoxic medicines promote manifestation of a gematotoksichnost of drug.

Contraindications:

The increased individual sensitivity to drug components (including, to other NPVP), a peptic ulcer of a stomach and duodenum in an aggravation phase, gastrointestinal bleedings, a heavy renal failure (KK less than 30 ml/min.), a full or incomplete combination of bronchial asthma, the nose recuring a polypose and okolonosovy bosoms and intolerance of acetylsalicylic acid or other NPVP (including, in the anamnesis), damages of an optic nerve, genetic absence glyukozo-6-fosfatdegidrogenazy, diseases of system of blood, the period after performing aortocoronary shunting; the progressing diseases of kidneys, a heavy liver failure or an active disease of a liver, the confirmed hyperpotassemia, active gastrointestinal bleeding, inflammatory diseases of intestines, children's age up to 12 years.

Use at pregnancy and in the period of a lactation
In need of use of the drug Ibuklin® at pregnancy and in the period of a lactation (breastfeeding), it is necessary to weigh carefully expected advantage of therapy for mother and potential risk for a fruit or the child.
In need of use in the I trimester of pregnancy it is necessary to exclude long administration of drug of Ibuklin®.
In need of short-term use of the drug Ibuklin® in the period of a breastfeeding termination lactation usually it is not required.
In pilot studies embriotoksichesky, teratogenic and mutagen action of components of the drug Ibuklin® is not established.

Overdose:

Symptoms of overdose, measure for assistance at overdose
Symptoms: gastrointestinal frustration (diarrhea, nausea, vomiting, anorexia, pain in epigastric area), increase in a prothrombin time, bleeding in 12-48 h, block, drowsiness, a depression, a headache, a sonitus, disturbance of consciousness, disturbance of a cordial rhythm, a lowering of arterial pressure, manifestations gepato-and nephrotoxicity, a spasm, is possible development of a gepatonekroz.
Treatment: a gastric lavage within the first 4 hours; alkaline drink, artificial diuresis; absorbent carbon inside, introduction of donators of SH-group and predecessors of synthesis of glutathione - methionine in 8-9 h after overdose and N-Acetylcysteinum inside or intravenously  in 12 h, antiacid drugs; hemodialysis; symptomatic therapy. Need for holding additional therapeutic actions (further administration of methionine, intravenous administration of N-Acetylcysteinum) is defined depending on concentration of paracetamol in blood, and also from time which passed after reception.

Storage conditions:

In dry, protected from light and the place, unavailable to children, at a temperature not above 25 °C. Period of validity of 5 years. Not to use after the expiry date specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Tablets, film coated 400 mg + 325 mg. On 10 tablets in PVC/Al the blister. On 1, 2 or 20 blisters are packed into a pack cardboard with the application instruction.