Ibuprofen (coated tablets 0.2 g)
Tabulettae Ibuprofeni obductae 0.2
International not patented name
Ibuprofen
Pharmacotherapeutic group
Not narcotic analgesics (non-steroid anti-inflammatory drug)
Composition
1 coated tablet contains 200 mg of ibuprofen.
Pharmacologic action
Pharmacodynamics
The preparation exerts analgesic, anti-inflammatory, antipyretic actions. It inhibits cyclooxygenase and blocks the prostaglandins biosynthesis. The analgesic action is caused by the inflammation intensity reduction, by the bradikinin production and algogeneity reduction; the anti-inflammatory action is caused by interference into various units of the inflammation pathgenesis (the increased vessels permeability normalizes, the microcirculation improves, the histamine, bradikinin, and inflammation mediators liberation reduces, the ACE formation is hindered thus causing the inflammatory process energy supply decrease); the antipyretic action is caused by the diencephalon thermoregulating centers excitability reduction. The antipyretic effect pronouncement depends on the body initial temperature and the preparation dose. It inhibits the platelets aggregation the inhibition being reversible.
In case of rheumatoid arthritis it effects mainly the exccudation and partially the proliferation components of the inflammatory reaction, has a quick and pronounced analgesic effect, reduces the edema, morning constrain and joints movements restriction.
In case of a primary dysmenorrhea it reduces the intrauterine pressure and the uterine contractions rate.
Pharmacokinetics
About 80% of the preparation dose taken is absorbed (quickly). The maximal blood plasma concentration is achieved in 60 minutes. The plasma proteins fixation is 99%. It penetrates the joint cavity slowly delaying in the synovial tissue forming concentrations in it larger than in the plasma. It is biotransformed forming three basic metabolites. The metabolic degradation products are eliminated from the body quickly and completely with urine. The period of half elimination is 2 – 2.5 hours.
Indications
Rheumatoid arthritis, deforming osteoarthrosis, ankylosing spondilitis, articular syndrome in case of the gout exacerbation, psoriatic arthritis; neuralgia, myalgia, tendovaginitis, bursitis, radiculitis, soft tissues and locomotor system traumatic inflammations. As an additional drug it used for managing infectious and inflammatory diseases of ROL organs, adnexitis, primary dysmenorrhea, headache and toothache.
Mode of appliance and dosing regime
Adults and children over 12 are prescribed 0.2 g 3 – 4 times a day as an initial dose. For achieving a quicker therapeutic effect the dose may be increased to 0.4 g 3 times a day. The therapeutic effect achieved the 24-hour dose is reduced to 0.6 – 0.8 g.
The first day dose is taken before meal being followed by a large quantity of water so that the preparation could be absorbed quickly. The remaining doses are taken during the day after meals (gradual absorption).
The maximal single dose is 0.4 g, the maximal day dose is 1.2 g.
Special warning
Alcohol intake is not recommended during the therapy.
Side effects
Heartburn, nausea, vomiting, meteorism, dizziness, headache, anxiety, insomnia, dermal allergic reactions, toxic amblyopia, renal function disturbances sodium and water retained. The gastro-intestinal tract erosive and ulcerous changes are observed rarely. When the side effects are pronounced the preparation intake should stopped and a physician addressed.
Contraindications
Hypersensitivity (including that to acetylsalicylic acid and other NSAIDs); bronchial asthma provoked by the acetylsalicylic acid intake; diseases of the optic nerve; peptic ulcer of the stomach and/or of the intestine at the exacerbation stage, thrombocytopenia, hemorrhagic diathesis, non-specific ulcerous colitis, portal hypertension, scotoma, amblyopia, the pregnancy last trimester, lactation (the breast feeding should be stopped for the period of therapy).
Interaction with other medicines
It reduces the ACE inhibitors antihypertensive activity, the furocemide and hypotiaside natriuretic activities. It may enhance the methotrexate and lithium preparations toxicity. When applied together with anti-coagulants of the kumarin type and alcohol the risk for hemorrhagic complications increases, a combined appliance with glucocorticoids in tablets increases the gastro-intestinal bleedings danger.
Overdosing
Symptoms: abdominal pains, nausea, vomiting, mental slowing down, sleepiness, depression, headache, murmur in the ears, metabolic acidosis, coma, acute renal failure, hypotension, bradycardia, tachycardia, auricles fibrillation, breathing arrest.
Treatment: washing of the stomach (within 1 hour after the preparation intake), activated charcoal (for the absorption reduction), alkaline drink, forced diuresis and symptomatic therapy (AAR, AP, gastro-intestinal bleedings correction).
Dosage form
200 mg tablets. 10 tablets in contour cellular packs, 50 tablets in a pot. 5 contour cellular packs in a cartoon.
