Indomethacin - instructions for use, dose, side effects, contraindications

tablet core excipients: lactose monohydrate 30.00 mg, microcrystalline cellulose 15.00 mg, wheat starch 43.20 mg, gelatin 2.00 mg, magnesium stearate 1.20 mg, talc 3.00 mg, silicon dioxide colloid 0.60 mg;

shell auxiliary substances: Eudrajit L-12.5% (Methacrylic acid-methyl methacrylate copolymer 1: 1) (as a dry matter) 2.25 mg, Eudrajit S-12.5% (Methacrylic acid-methyl methacrylate copolymer 1: 2) (as a dry matter) 3.00 mg, talc 2.00 mg, titanium dioxide 4.30 mg, macrogol 6000 0.51 mg, macrogol 400 0.18 mg, diethyl phthalate 0.51 mg, iron oxide dye yellow Sicovit yellow 10 E 172 1.05 mg, iron oxide dye red Sicovit red 30 E 172 0.225 mg.

Description:

Tablets are round, biconvex, covered with a shell, light brown in color.

Pharmacotherapeutic group:Non-steroidal anti-inflammatory drug

ATX: & nbsp

C.01.E.B.03 Indomethacin

S.01.B.C.01 Indomethacin

M.02.A.A.23 Indomethacin

Pharmacodynamics:

Indomethacin has anti-inflammatory, analgesic, antipyretic and antiplatelet effect.Suppresses inflammatory factors, reduces platelet aggregation. Inhibiting cyclooxygenase 1 and 2, gives the metabolism of arachidonic acid, prostaglandins decreases the amount (Pg) both in inflammation and in healthy tissue, inhibits the exudative and the proliferative phases of inflammation. It causes weakening or disappearance of the pain syndrome of rheumatic and non-rheumatic nature (including pain in joints at rest and during movement, decrease in morning stiffness and swelling of the joints, contributes to an increase in the volume of movements, in inflammatory processes that occur after operations and trauma, quickly facilitates both spontaneous pain and pain during movement, reduces inflammatory edema at the wound site).

Pharmacokinetics:

Absorption is fast. Bioavailability is 90-98%. After oral administration, the time to reach the maximum concentration in the blood plasma (TC_mOh) -2 hours, the maximum concentration in the blood plasma (C_mOh) - 0.69 μg / ml.

The connection with plasma proteins is 90%. Metabolized mainly in the liver.

The half-life (T_1/2) - 4-9 h (the indicator can vary depending on the severity of systemic metabolism, intestinal-hepatic circulation and reabsorption). It is excreted by the kidneys at 70%, with 30% unchanged, and through the intestines - 30%.Penetrates into breast milk. When a mother receives 200 mg of the drug per day in breast milk, 0.5 to 2 mg of indomethacin is determined. Indomethacin not removed during dialysis.

Indications:

Inflammatory and degenerative diseases of the musculoskeletal system: rheumatoid, psoriatic, juvenile chronic arthritis, ankylosing spondylitis (Bekhterev's disease); rheumatic affections of soft tissues; gouty arthritis (with an acute attack of gout, quick-acting dosage forms are preferred).

Contraindications:- Hypersensitivity to indomethacin and other components of the drug;

- period after coronary artery bypass grafting;

- complete or incomplete combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses and intolerance to acetylsalicylic acid or other non-steroidal anti-inflammatory drugs (NSAIDs) (including in history);

- Stomach ulcer and duodenal ulcer;

- bleeding (including intracranial and from the organs of the gastrointestinal tract (GIT));

- inflammatory bowel disease (ulcerative colitis, Crohn's disease);

- hepatic insufficiency or active liver disease;

- chronic renal failure (creatinine clearance less than 30 ml / min), progressive kidney disease;

- confirmed hyperkalemia;

- Congenital heart defects (severe coarctation of the aorta, pulmonary atresia, heavy tetralogy of Fallot),

- disorders of blood clotting (including hemophilia, lengthening bleeding time, propensity to bleed),

- disorders of hematopoiesis (leukopenia and anemia);

- pregnancy, lactation, children under 14 years;

- deficiency of lactase, lactose intolerance, glucose-galactose malabsorption.

Carefully:

Coronary heart disease, cerebrovascular diseases, chronic heart failure, dyslipidemia / hyperlipidemia, diabetes mellitus, thrombocytopenia, peripheral arterial disease, hypertension, smoking, chronic renal failure (creatinine clearance 30-60 ml / min), liver cirrhosis with portal hypertension, hyperbilirubinemia , immediately after surgery; ulcerative gastrointestinal lesion in history, if there is an infection Helicobacter pylori, elderly age, with prolonged use of NSAIDs, frequent use of alcohol,severe somatic diseases, with concomitant therapy with the following drugs: anticoagulants (for example, warfarin), antiplatelet agents (e.g., acetylsalicylic acid, clopidogrel), oral glucocorticosteroids (for example, prednisolone), selective serotonin reuptake inhibitors (for example, citalopram, fluoxetine, paroxetine, sertraline), mental disorders, epilepsy, parkinsonism, depression.

Dosing and Administration:

Inside, during or after a meal, washed down with milk, adults - in an initial dose of 25 mg 2-3 times a day. If the clinical effect is inadequate, the dose is increased to 50 mg 3 times a day. The maximum daily dose is 200 mg. When the effect is achieved, treatment is continued for 4 weeks at the same or reduced dose. With prolonged use, the maximum daily dose is 75 mg. To reduce the risk of developing adverse events, the minimum effective dose should be used during the minimum possible course of treatment.

Children over 14 years of age on 1,5-2,5 mg / kg / day.

Side effects:

From the digestive system: NSAIDs - gastropathy, abdominal pain, nausea, vomiting,heartburn, anorexia, diarrhea, impaired liver function (increased activity of "liver" transaminases, hyperbilirubinemia). With prolonged use in large doses - ulceration of the mucosa of the gastrointestinal tract.

From the central nervous system: headache, dizziness, insomnia, agitation, irritability, fatigue, drowsiness, depression, peripheral neuropathy.

From the sense organs: hearing loss, tinnitus, impaired taste, diplopia, blurred vision, corneal opacity, indomethacin deposition in the cornea, retinal damage, conjunctivitis.

From the cardiovascular system: development (aggravation) of the phenomena of chronic heart failure, tachyarrhythmia, increase of arterial pressure.

From the urinary system: impaired renal function, proteinuria, hematuria, interstitial nephritis, nephrotic syndrome, necrosis of renal papillae.

On the part of the system of hematopoiesis and hemostasis system: bleeding (gastrointestinal, gingival, uterine, hemorrhoidal), anemia (including hemolytic and aplastic), leukopenia, thrombocytopenia, eosinophilia, agranulocytosis, thrombocytopenic purpura.

Allergic reactions: skin rash, itchy skin, urticaria, angioedema, bronchospasm; in isolated cases - photosensitivity, toxic epidermal necrolysis (Lyell's syndrome), erythema nodosum, anaphylactic shock.

Laboratory indicators: agranulocytosis, hyperglycemia, glucosuria, hyperkalemia.

Other: aseptic meningitis (more often in patients with autoimmune diseases), edematous syndrome, increased sweating.

Overdose:

Symptoms: nausea, vomiting, severe headache, dizziness, memory impairment, disorientation. In severe cases - paresthesia, numbness of limbs, convulsions.

Treatment is the rapid removal of indomethacin from the body and the use of symptomatic therapy. Hemodialysis is ineffective.

Interaction:

Reduces the effectiveness of uricosuric drugs, antihypertensive medications (including beta-blockers) and diuretics, against the background of the use of potassium-sparing diuretics, the risk of hyperkalemia increases; strengthens the effect of indirect anticoagulants, antiaggregants, thrombolytics (alteplase, streptokinase and urokinase) - there is a risk of bleeding.

Increases the side effects of mineralocorticosteroids, glucocorticosteroids, estrogens, other NSAIDs.

Strengthens hypoglycemic action of insulin and oral hypoglycemic drugs (sulfonylurea derivatives).

Sharing with paracetamol increases the risk of developing nephrotoxic effects.

Ethanol, colchicine, glucocorticosteroids and corticotropin increase the risk of developing gastrointestinal complications, accompanied by bleeding.

Antacids and colestramine reduce the absorption of indomethacin.

Increases the concentration in the blood of lithium, methotrexate and digoxin, which can lead to an increase in their toxicity.

Cyclosporine, gold preparations increase nephrotoxicity (apparently due to suppression of prostaglandin synthesis in the kidneys).

Cefamandol, cefaperazone, cefotetan, valproic acid, plikamycin increase the risk of hypoprothrombinemia and bleeding.

Potentiates the toxic effect of zidovudine (by inhibiting metabolism).

Myelotoxic drugs increase the manifestation of hematotoxicity of the drug.

Special instructions:

During treatment, it is necessary to monitor the picture of peripheral blood and the functional state of the liver and kidneys.

If it is necessary to determine the concentration of 17-ketosteroids, the drug should be discontinued 48 hours before the study.

To prevent and reduce dyspepsia, antacids should be used.

In the event of visual impairment, the drug is immediately withdrawn.

Effect on the ability to drive transp. cf. and fur:

During the treatment period it is necessary to refrain from driving motor vehicles and practicing potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:Tablets coated with enteric coating, 25 mg.

Packaging:

30 tablets in a blister made of polyvinyl chloride film and aluminum foil.

For 1 blister with instructions for use in a cardboard bundle.

Storage conditions:

In a dry, the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

5 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:П N012784 / 01

Date of registration:28.04.2011

Expiration Date:Unlimited

The owner of the registration certificate:Balkanfarma - Dupnitsa ADBalkanfarma - Dupnitsa AD Bulgaria

Manufacturer: & nbsp

BALKANPHARMA-DUPNITSA, AD Bulgaria

Representation: & nbspAktavis, Open Company Aktavis, Open Company

Information update date: & nbsp31.10.2017

Illustrated instructions

Instructions

Indomethacin (Indometacin)