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

auxiliary substances (core): lactose monohydrate (milk sugar) - 41.6 mg, potato starch - 10.0 mg, microcrystalline cellulose - 16.0 mg, povidone (polyvinylpyrrolidone) - 2.50 mg, magnesium stearate - 0.90 mg;

auxiliary substances (shell): cellulose (acetylphthalyl cellulose) 2.20 mg, polysorbate 80 to 0.72 mg, titanium dioxide 1.08 mg.

Description:

The tablets are round biconvex, covered with a film coat of white or almost white color. On the fracture of the tablet, two layers are visible: a white or white core with a yellowish tint of color and a film membrane.

Pharmacotherapeutic group:NSAIDs

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 anti-aggregation effect. Suppresses the activity of proinflammatory factors, reduces platelet aggregation. By depressing cyclooxygenase I and II, it breaks the metabolism of arachidonic acid, reduces the amount of prostaglandins (Pg) both in the focus of inflammation, and in healthy tissues, suppresses the exudative and proliferative phases of inflammation. Eliminates or reduces pain syndrome of rheumatic and non-rheumatic nature (including pain in joints at rest and during movement, decrease in morning stiffness and swelling of joints, contributes to an increase in the volume of movements, in inflammatory processes that occur after surgery and trauma; spontaneous pain, and pain during movement, reduces inflammatory swelling at the wound site).

Pharmacokinetics:

Bioavailability for oral administration is 80-90%. The maximum plasma concentration is achieved within 1-2 hours. It is absorbed through the mucosa of the small intestine, and to a much lesser extent through the gastric mucosa. It is distributed in all organs and tissues. Penetrates through the placental and blood-brain barrier. It penetrates through the synovial membrane into the joints, and the concentration of indomethacin in the synovial fluid rises. The connection with plasma proteins is 90-98%, the half-life is 2.6 and 11.2 hours. It is metabolized mainly in the liver, 10-20% of the drug is eliminated in an unchanged form, 70% is excreted by the kidneys, 30% through the gastrointestinal tract (GIT). It is not removed during dialysis. Excreted in breast milk.

Indications:

- Acute pain and chronic inflammatory diseases of the musculoskeletal system: rheumatoid arthritis, juvenile chronic arthritis, ankylosing spondylitis, chronic (ankylosing spondylitis), gouty arthritis, psoriatic arthritis, Reiter's disease;

- diseases of the periarticular tissues: tendinitis, bursitis, tendobursitis, tendovaginitis;

- injuries in athletes;

- discopathy, neuritis, plexitis, radiculoneuritis.

The drug is intended for symptomatic therapy, reduces pain and inflammation at the time of use, the progression of the disease is not affected

Contraindications:

- Hypersensitivity to indomethacin or any of the excipients of the drug;

- anamnestic data on the attack of bronchial obstruction, rhinitis, urticaria after taking acetylsalicylic acid or other NSAIDs (complete or incomplete acetylsalicylic acid intolerance syndrome - rhinosinusitis, urticaria, polyps of the nasal mucosa, asthma);

- erosive and ulcerative changes in the gastric mucosa or duodenum, active gastrointestinal bleeding;

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

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

- the period after coronary artery bypass grafting;

Decompensated heart failure;

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

- liver failure or active liver disease;

- Violations of blood clotting (including hemophilia, lengthening bleeding time, a tendency to bleeding);

- violation of hematopoiesis (leukopenia and anemia);

- confirmed hyperkalemia;

- hereditary lactose intolerance, lactase deficiency and glucose-galactose malabsorption;

- Pregnancy and breastfeeding;

- Children's age (up to 14 years).

Carefully:

Coronary heart disease, cerebrovascular disease, congestive heart failure, dyslipidemia, hyperlipidemia, diabetes mellitus, thrombocytopenia, peripheral arterial disease, hypertension, smoking, creatinine clearance 30-60 ml / min, liver cirrhosis with portal hypertension, hyperbilirubinemia, gastrointestinal ulcer, of the intestinal tract in the anamnesis, the presence of infection Helicobacter pylori, long-term use of NSAIDs, frequent use of alcohol, severe physical illness. Concomitant therapy with the following drugs: anticoagulants (incl. warfarin), antiaggregants (incl. acetylsalicylic acid, clopidogrel), oral glucocorticosteroids (incl. prednisolone), selective inhibitors of serotonin reuptake (including citalopa, fluoxetine, paroxetine, sertraline); mental disorders, epilepsy, parkinsonism, depression, elderly age.

Pregnancy and lactation:

The drug is contraindicated for use during pregnancy and during breastfeeding.

Indomethacin excreted in breast milk. If necessary use of the drug during lactation at the time of treatment should stop breastfeeding.

Dosing and Administration:

Inside, after eating, squeezed with enough water.

Adults and children over 14 years of age: the initial dose is 25 mg 2-3 times a day. With insufficient therapeutic effect, the dose is increased to 50 mg 3 times a day. The maximum daily dose is 200 mg. With prolonged treatment, the daily dose should not exceed 75 mg.

Gouty Arthritis

For relief of an acute gouty attack, the initial dosage is 100 mg, after which the treatment is continued 50 mg 3 times a day until the pain disappears. Side effects can be reduced by using the minimum effective dose for as short a period of time as possible.

Side effects:

From the digestive system: NSAIDs-gastropathy, abdominal pain, nausea, vomiting, heartburn, anorexia, diarrhea, bleeding, impaired liver function (increase in the blood of bilirubin, "hepatic" transaminases (ALT, ASAT)). With prolonged use in large doses - ulceration of the mucous membrane of the gastrointestinal tract, ulcerative stomatitis. Toxic hepatitis with jaundice or without jaundice, fulminant hepatitis.

From the central nervous system: headache, dizziness, agitation, drowsiness, fatigue, peripheral neuropathy. Sensitivity disorders, including paresthesia; feeling of disorientation, insomnia, irritability, depression, anxiety, memory disorder, psychotic reactions.

From the cardiovascular system: development (aggravation) of the phenomena of chronic heart failure, tachyarrhythmia, there are reports of edematous syndrome, increased blood pressure.

From the sense organs: hearing loss, tinnitus, taste disorder, diplopia, blurred vision, corneal opacity, conjunctivitis.

From the urinary system: edema, proteinuria, hematuria, interstitial nephritis, nephrotic syndrome, papillary necrosis.

From the hemopoietic system and hemostasis system: bleeding (gastrointestinal, of gums, uterine, hemorrhoidal), thrombocytopenia, eosinophilia, agranulocytosis, thrombocytopenic purpura.

Allergic reactions: skin rash, itching; urticaria, angioedema, bronchospasm; photosensitivity, Lyell's syndrome, erythema nodosum, Stevens-Johnson syndrome, anaphylactic shock.

Laboratory indicators: agranulocytosis, leukopenia, thrombocytopenia, Hyperglycemia, glucosuria, hyperkalemia.

Overdose:

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

Treatment: symptomatic therapy.Hemodialysis is ineffective.

Interaction:

Simultaneous use of indomethacin with other drugs from the group of NSAIDs, acetylsalicylic acid, glucocorticosteroids, alcohol, colchicine and corticotropin increases the risk of bleeding in the gastrointestinal tract.

Indomethacin reduces the effectiveness of diuretics, against the background of the use of potassium-sparing diuretics, the risk of hyperkalemia increases; reduces the effectiveness of uricosuric and hypotensive drugs; strengthens the effect of indirect anticoagulants, antiplatelet agents, thrombolytic agents (alteplase, streptokinase and urokinase); increases the side effects of glucocorticosteroids, NSAIDs, estrogens, acetylsalicylic acid; enhances the hypoglycemic effect of sulfonylurea derivatives.

Sharing with paracetamol increases the risk of developing nephrotoxic effects.

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

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

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

Potentiates the toxic effect of zidovudine.

Antacids and colestramine reduce the absorption of indomethacin.

Myelotoxic drugs increase the manifestation of hematotoxicity of the drug.

Co-administration with quinolones may increase the threat of seizures in patients with or without anamnesis data on epilepsy or seizures.

Strengthens the hypoglycemic effect of insulin and oral hypoglycemic drugs.

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 17-ketosteroids, the drug should be discontinued 48 hours before the test.

To reduce the risk of adverse events on the part of the gastrointestinal tract, a minimally effective dose should be used with the minimum possible short course.

Serious skin reactions, including those with a fatal outcome, very rarely observed with the use of NSAIDs, concern cases of exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis.The highest risk is at the beginning of treatment. The drug should be discontinued at the appearance of the first cutaneous or other signs of hypersensitivity.

The drug can mask the symptoms of acute inflammation, which requires the exclusion of bacterial infection when it is prescribed.

When taking drugs from the NSAID group, there is a risk of developing hyperkalemia, especially in patients over 65 years of age, patients with kidney failure, patients who take β-blockers, ACE inhibitors and potassium-sparing diuretics. In such patients, serum potassium levels should be monitored.

In women of reproductive age, there is a risk of reversible suppression of fertility.

The drug contains lactose monohydrate as an auxiliary substance, which must be taken into account when appointing patients with lactase deficiency, galactosemia, glucose / galactose malabsorption syndrome.

Patients with glutein enteropathy should take into account the presence of the drug starch potato

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

In the period of treatment with indomethacin it is necessary to refrain from driving and practicing potentially dangerous activities,requiring increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Tablets coated with enteric coating, 25.0 mg.

Packaging:

For 10, 30 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

By 10, 20, 30, 40, 50, 60 or 100 tablets in cans of polymeric for medicines.

One jar or 1, 2, 3, 4, 5, 6, 8 or 10 contour squares, together with the instructions for use, are placed in a cardboard package (pack) of cardboard.

Storage conditions:

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

Keep out of the reach of children.

Shelf life:

3 years.

Do not use the drug after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-002131

Date of registration:05.07.2013

Expiration Date:05.07.2018

The owner of the registration certificate:ATOLL, LLC ATOLL, LLC Russia

Manufacturer: & nbsp

OZONE, LLC Russia

Representation: & nbspOZONE LLC OZONE LLC Russia

Information update date: & nbsp31.10.2017

Illustrated instructions

Instructions

Indomethacin (Indometacin)