Indometacin 50/100

General characteristics. Structure:

Active ingredient: indometacin – 50/100 mg; excipients: the fat cured starch corn.

Pharmacological properties:

Indometacin renders antiinflammatory, analgetic, febrifugal and anti-aggregation action. Suppresses activity of pro-inflammatory factors, reduces aggregation of thrombocytes. Oppressing a tsikloksigenaza 1 and 2, breaks metabolism of arachidonic acid, reduces amount of prostaglandins (Pg) both in the inflammation center, and in healthy fabrics, suppresses exudative and proliferative phases of an inflammation. Causes easing or disappearance of a pain syndrome of rheumatic and not rheumatic character (including at joint pains at rest and at the movement, reduction of morning constraint and a swelling of joints, promotes increase in volume of movements; at the inflammatory processes arising after operations and injuries quickly facilitates both spontaneous pain, and an oxycinesia, reduces inflammatory hypostasis on site of a wound).

Pharmacokinetics. Absorption - bystry. Bioavailability at a rectal way of introduction - 80-90%. Communication with proteins of plasma - 90%, an elimination half-life - 4-9 h.

It is metabolized, generally in a liver, in not changed look 30% of drug are removed. 70% are removed by kidneys, 30% - through digestive tract. Is not removed at dialysis. Gets into breast milk.

Indications to use:

Inflammatory and degenerative diseases of a musculoskeletal system: a pseudorheumatism, the psoriasis, juvenile chronic arthritis ankylosing a spondylitis; rheumatic defeats of soft tissues; gouty arthritis.

As supportive application at infectious and inflammatory diseases of ENT organs, an adnexitis, prostatitis, cystitis, neuritis, algodismenory, head and a dentagra (as a part of a combination therapy).

Route of administration and doses:

Rektalno (enter into a rectum). Before use of suppository it is recommended to release intestines.

Suppositories of 50 mg adult 1-3 once a day; during a gout attack to 200 mg a day.

Adults accept suppositories of 100 mg on 1 candle of 1 times a day; during a gout attack to 200 mg a day.

Features of use:

During treatment control of a picture of peripheral blood and a functional condition of a liver and kidneys is necessary. In need of definition of 17 ketosteroids drug should be cancelled for 48 h prior to a research.

During treatment it is necessary to abstain from driving of motor transport and occupations potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

From the alimentary system: NPVP-gastropathy, abdominal pains, nausea, vomiting, heartburn, anorexia, diarrhea: an abnormal liver function (increase in blood of bilirubin, "hepatic" transaminases). At prolonged use in high doses - an ulceration of a mucous membrane of digestive tract.

From a nervous system: headache, dizziness, sleeplessness, excitement, irritability, fatigue, drowsiness, depression, peripheral neuropathy.

From sense bodys: decrease in hearing, sonitus, taste disturbance, diplopia, sight illegibility, opacification of a cornea, conjunctivitis.

From CCC: heart failure, tachyarrhythmia, increase in the ABP.

From an urinary system: renal failure, proteinuria, hamaturia, intersticial nephrite, nephrotic syndrome, necrosis of nipples.

From system of a hemostasis: bleeding (gastrointestinal, gingival, uterine, hemorrhoidal), thrombocytopenia.

Allergic reactions: skin rash, itch, small tortoiseshell, Quincke's edema, bronchospasm; seldom - a Lyell's disease, a knotty erythema, an acute anaphylaxis.

Laboratory indicators: agranulocytosis, leukopenia, hyperglycemia, glucosuria, hyperpotassemia, aplastic anemia, autoimmune hemolitic anemia.

Others: aseptic meningitis (is more often at patients with autoimmune diseases), sweating strengthening, an edematous syndrome.

Local reactions: burning, an itch, weight in anorectal area, an exacerbation of hemorrhoids.

Interaction with other medicines:

Reduces efficiency of uricosuric drugs, hypotensive and diuretics (saluretics); strengthens effect of indirect anticoagulants, antiagregant, fibrinolitik, side effects of mineralokortikosteroid, estrogen, other NPVP; strengthens hypoglycemic effect of derivatives of sulphonylurea.

Sharing with paracetamol increases risk of development of nephrotoxic effects. Ethanol, colchicine, glucocorticosteroids increase risk of development of the gastrointestinal complications accompanied with bleedings.

Increases concentration in blood of drugs of lithium, a methotrexate and digoxin. Cyclosporine, drugs of gold increase nephrotoxicity of indometacin. Tsefamandol, цефоперазон, valproic acid increase risk of development of a prothrombinopenia and danger of bleedings. Reduces elimination of penicillin. Exponentiates toxic action of a zidovudine.

Contraindications:

Hypersensitivity, "aspirinovy" asthma, peptic ulcer of a stomach and duodenum, ulcer colitis, bleeding (intracranial, gastrointestinal), inborn heart diseases (aorta coarctation, an atresia of a pulmonary artery, Fallo's tetrad), disturbance of color sight, cirrhosis with portal hypertensia, diseases of an optic nerve, bronchial asthma, heart failure, hypostases, arterial hypertension, hemophilia, hypocoagulation, a liver failure, a chronic renal failure, decrease in hearing, pathology of a vestibular mechanism, deficit glyukozo-6-fosfatdegidrogenazy; blood diseases; proctitis, hemorrhoids.

Pregnancy, the lactation period, children's and teenage age (up to 18 years).

With care - a hyperbilirubinemia, thrombocytopenia, epilepsy, parkinsonism, a depression, children's and advanced age.

Overdose:

Symptoms: nausea, vomiting, severe headache, dizziness, memory disturbance, disorientation. In hard cases of paresthesia, numbness of extremities, spasms.

Treatment: symptomatic therapy. The hemodialysis is inefficient.

Storage conditions:

List B. At a temperature not above 25 °C. To store in the places unavailable to children. Period of validity 3 years.

Issue conditions:

According to the recipe

Packaging:

Suppositories rectal 50/100 mg on 5 pieces in a blister strip packaging.

Suppositories on 10, 30 or 50 pieces in a blister strip packaging from a film polyvinyl chloride. Planimetric packagings together with the application instruction in a cardboard pack.