Ibuprofen

General characteristics. Structure:

International and chemical names: Іbuprofen; (2RS)-2-[4-(2-methylpropyl) phenyl] propanoic acid; main physical and chemical properties: tablets of a round form, coated, pink color with a biconvex surface. On a cross break the kernel surrounded with a cover layer is visible; structure: 1 tablet contains 200 mg of an ibuprofen in terms of 100% dry matter; excipients: potato starch, magnesium stearate, sugar, wheat flour, povidone, magnesium carbonate the main, aerosil, titanium dioxide, talc, acid red, beeswax, liquid paraffin.

Pharmacological properties:

Pharmacodynamics. Derivative fenilpropionovy acid, the having antiinflammatory, analgeziruyushchy and febrifugal effect. The mechanism of action is connected with non-selective oppression of activity of cyclooxygenase (TsOG-1 and TsOG-2) – the main enzyme of metabolism of arachidonic acid, being the predecessor of prostaglandins playing a major role in a pathogeny of an inflammation, pain and fever. Analgeziruyushchy action is caused as peripheral  (indirectly,  through  suppression of synthesis  of prostaglandins),    and  the central mechanism which is implemented due to oppression of synthesis of prostaglandins in the central nervous system. The ibuprofen reduces aggregation of thrombocytes.

Pharmacokinetics. At intake the ibuprofen is almost completely soaked up from a digestive tract. The maximum concentration in blood is reached in 1–2 hours. The concomitant use of food slows down absorption speed in a digestive tract. Well contacts blood proteins – 90-95%. Drug slowly gets into a joint cavity, but is late in synovial fabric, creating in it big concentration, than in a blood plasma. Metabolism of an ibuprofen is carried out in a liver. The elimination half-life makes 2-3 h 80% of the accepted dose is removed with urine preferential in the form of metabolites (10% – in not changed look); other 20% are removed through intestines also in the form of metabolites.

Indications to use:

Inflammatory and degenerative diseases of joints and backbone (including rheumatic and the pseudorheumatism ankylosing a spondylitis, an osteoarthrosis), a joint syndrome at an exacerbation of gout, the psoriasis arthritis   ankylosing a spondylitis, a tendinitis, a bursitis, radiculitis, a traumatic inflammation of soft tissues and a musculoskeletal system. Neuralgia, mialgiya, a pain syndrome at infectious and inflammatory diseases of ENT organs, an adnexitis, альгодисменорея, head and a dentagra. Fever at infectious and inflammatory diseases.

Route of administration and doses:

The dose is established individually, depending on a nosological form of a disease, expressiveness of clinical manifestations. At intake for adults the single dose makes 200-800 mg, reception frequency – 3-4 times a day; to children 12 years – 20 mg/kg in stages are more senior. The maximum  daily dose for adults at intake – 2,4 g. The course of treatment makes from several days to two weeks and is defined by achievement of therapeutic effect and sensitivity to drug.

Features of use:

Take drug at chronic heart failure with caution. In the course of treatment systematic control of function of a liver and a hemopoiesis, a picture of peripheral blood is necessary. Drug does not possess teratogenic action that gives the chance to apply it at pregnancy, behind an exception ІІІ a trimester (in urgent cases). The patients having bronchial asthma, hay cold, chronic bronchitis can react especially sharply to drug (asthma attacks, a rhinedema, etc.). The ibuprofen can have an adverse effect on ability of control of vehicles, especially at the use against the background of therapy by an alcohol ibuprofen.

Side effects:

From system of digestion: often nausea, anorexia, vomiting, a sensation of discomfort in epigastriums, diarrhea; development of erosive cankers of digestive tract is possible; seldom – bleedings from a digestive tract; at prolonged use abnormal liver functions are possible.
From the central nervous system: dizziness, sleep disorders, drowsiness, disturbances of visual and acoustical perception.
From system of a hemopoiesis: at prolonged use anemia, thrombocytopenia, an agranulocytosis are possible.
From an urinary system: at prolonged use renal failures, a hyperpotassemia, a hyperuricemia, an azotemia are possible.
Allergic reactions: often – skin rash, a Quincke's edema; seldom – aseptic meningitis (is more often at patients with autoimmune diseases); bronchospasms.

Interaction with other medicines:

At simultaneous use with digoxin, dipheninum, lithium drugs the ibuprofen can change concentration of the above-stated drugs. Drug reduces action of diuretic and anti-hypertensive means. At simultaneous use with kaliysberegayushchy diuretics development of a hyperpotassemia is possible. At an ibuprofen combination to glucocorticoids or other non-steroidal anti-inflammatory drugs the risk of emergence of side effects from digestive tract increases. The ibuprofen can increase concentration and toxic impact on a methotrexate organism. The concomitant use of acetylsalicylic acid reduces ibuprofen level in a blood plasma. With care use drug in a combination with indirect anticoagulants, thiazide diuretics.

Contraindications:

Digestive tract erosive cankers in an aggravation phase, the bronchospasms connected with reception of non-steroidal anti-inflammatory drugs in the anamnesis, "triad" (the eosinophilic rhinitis recuring nose polyposes, hyperplastic sinusitis), diseases of an optic nerve, hemopoiesis disturbance, hemorrhagic diathesis, the third trimester of pregnancy, a lactation, children's age up to 12 years, the expressed renal failures and/or a liver, hypersensitivity to an ibuprofen and other non-steroidal anti-inflammatory drugs.

Overdose:

At overdose by the drug Ibuprofen the headache, dizziness, block, a loss of consciousness, and also abdominal pains, nausea, vomiting are possible. Besides, hypotension, respiratory depression, cyanosis is possible. There is no specific antidote. Treatment: gastric lavage; if necessary – correction of electrolytic balance. The hemodialysis is inefficient.

Storage conditions:

To store in dry, protected from light, the place, unavailable to children, at a temperature not above 25 °C.

Period of validity - 3 years.

Issue conditions:

According to the recipe

Packaging:

On 50 tablets in a blister strip packaging.