Indomethacin (When ATH M01AB01)

When ATH:
M01AB01

Characteristic.

NSAIDs, indole acetic acid derivative.

White or slightly yellowish powder, odorless or almost odorless. Practically insoluble in water. Moderately soluble ethanol, xloroforme, ether. Soluble in alkaline solutions.

Pharmacological action.
Anti-inflammatory, pyretic, analgesic.

Application.

For systemic use (inside, / m, rectally)

Inflammatory and degenerative diseases of the musculoskeletal system: rheumatoid, psoriatic, juvenile chronic arthritis, arthritis, Paget's disease and Reiter, neuralgic amyotrophy (bolyezni Pyersonyeidja Ternera), ankylosing spondylitis (ankylosing spondylitis), podagricheskiy arthritis, rheumatism. Pain syndrome: headache (incl. menstrual syndrome) and toothache, lyumbago, sciatica, neuralgia, myalgia, after injuries and surgeries, accompanied by inflammation, bursitis and tendinitis (It is most effective in the localization of the shoulder and forearm). Algomenorrhea, to maintain pregnancy, Bartter syndrome (secondary hyperaldosteronism), perikardit (symptomatic treatment), delivery (as analgesic and tokoliticheskogo premature labor), inflammatory processes in the pelvis, incl. adnexitis, cleft arterial duct. Infectious-inflammatory diseases of ENT organs with marked pain syndrome (in the complex therapy): pharyngitis, tonsillitis, otitis. Feverish syndrome (incl. with chlamydia, other lymphomas, and hepatic metastases of tumors sólidnyh) — in the case of failure of acetylsalicylic acid and paracetamol.

For topical application, (when applied to the skin)

Due to the traumatic inflammation of tendons, ligaments, muscles and joints (by stretching, dislocation, after exercise and injuries). Localized forms of soft-tissue inflammation, incl. tendinitis, Tendinitis, syndrome "shoulder-hand", ʙursit, myalgia; radiculitis (sciatica, lyumbago). Inflammatory and degenerative diseases of the musculoskeletal system (deforming osteoarthritis, revmaticheskiy arthritis, psoriaticheskiy arthritis, rheumatoid arthritis, frozen shoulder, ankylosing spondylitis, osteochondrosis with radicular syndrome) except degenerative disease of the hip joints.

In ophthalmology (eye drops): inhibition of miosis during cataract surgery; inflammatory process, caused by surgery; prevention and treatment of cystoid macular edema after cataract surgery; treatment and prevention of inflammatory processes of the eyeball; non-infectious conjunctivitis.

In dentistry (systemic and cutaneous application): arthritis and arthrosis of the temporomandibular joint, inflammatory diseases of the oral tissue, myalgia, neuralgia, postoperative period.

Contraindications.

Hypersensitivity.

For systemic use: "Aspirinovaâ" triad (a combination of asthma, recurrent nasal polyposis, and paranasal sinuses, and intolerance of aspirin and drugs pirazolonovogo series), gastric ulcer and duodenal ulcer, yazvennыy colitis, bleeding (incl. intracranial or gastrointestinal), congenital heart disease, where the ductus arteriosus is necessary for the maintenance of pulmonary or systemic blood flow, incl. severe coarctation of the aorta, pulmonary atresia, tetrada Fallo; impaired color vision, diseases of the optic nerve, bronchial asthma, liver cirrhosis with portal hypertension, congestive heart failure, swelling, arterial hypertension, coagulation failure (incl. hemophilia, prolonged bleeding, bleeding tendency), hepatic failure, chronic renal failure, hearing loss, pathology of the vestibular apparatus, deficiency of glucose-6-fosfatdegidrogenazы; violation of hematopoiesis (leukopenia and anemia), pregnancy, lactation, childhood (to 14 years); Rectal (additionally): rectal bleeding, proctitis, hemorrhoids; for cutaneous application: pregnancy (Quarter III-for large surfaces), violation of the integrity of the skin, Children up to age 1 year.

Restrictions apply.

For cutaneous use: pregnancy (I and II trimesters), lactation, Children up to age 6 years.

In ophthalmology (eye drops): epithelial herpetic keratitis (incl. history), pregnancy, lactation, childhood.

Pregnancy and breast-feeding.

Teratogenic effects. Research teratogenicity, conducted in rats and mice at doses 0,5; 1,0; 2,0 and 4,0 mg / kg / day, shown, at a dosage 4 mg / kg / day there was no increase in the frequency of malformations in comparison with the control group, except for delayed ossification in fetuses (It is seen as secondary to reduce the average weight of the fruits). In other studies in mice with higher doses (5-15 Mg / kg / day) It was discovered toxicity and mortality for females, increase in resorption and fetal malformations. Comparative study in rodents using high doses of aspirin showed similar effects in females and their fetuses. However, reproductive studies in animals do not always predict effects in humans. There are no adequate and well-controlled studies in pregnant women have not held.

Nonteratogenic effects. As it is well known adverse effects of NSAIDs on the cardiovascular system of the fetus (premature closure of the ductus arteriosus), should be avoided in pregnancy (especially in the later stages).

Effects of indomethacin and other drugs of this class in the human fetus in the III trimester of pregnancy include: intrauterine closure of the ductus arteriosus, tricuspid valve and pulmonary hypertension; unclosed ductus arteriosus in the postnatal period, Resistance to medical correction; degenerative changes in the myocardium, platelet disorders, leading to bleeding, intracranial hemorrhage, renal dysfunction or failure, failure / kidney malformation, which can lead to renal failure, oligogidramnion, gastrointestinal bleeding or perforation, increased risk of necrotising enterocolitis.

In studies in rats and mice, treated with indomethacin at doses 4 mg / kg / day in the last 3 day of pregnancy, there was a reduction in body weight of females and a small number of deaths and female fetuses. It was observed increase in the incidence of neuronal necrosis in the diencephalon in fetuses born alive. At a dose of 2,0 mg / kg / day to increase the frequency of neuronal necrosis as compared to the control group was not. Introduction 0,5 or 4,0 mg / kg / day in the first 3 day life does not cause an increase in the frequency of neuronal necrosis.

Labor and delivery. In studies in rats show, NSAIDs, as well as other means, ingibiruyushtie synthesis NG, increase the number of cases of obstructed labor, causing delay in the onset of labor and delivery, decrease in the number of surviving cubs.

Category actions on the fetus by the FDA — with. (The study of reproduction in animals has revealed adverse effects on the fetus, and adequate and well-controlled studies in pregnant women have not held, However, the potential benefits, associated with drugs in pregnant, may justify its use, in spite of the possible risk.)

Indomethacin passes into breast milk, so you should stop breast-feeding during treatment or avoid the use of indomethacin during breastfeeding.

Side effects.

Systemic side effects

From the nervous system and sensory organs: headache, dizziness, vertigo, excitation, irritability, excessive fatigue, drowsiness, depression, perifericheskaya neuropathy, taste disturbance, hearing loss, noise in ears, diplopia, blurred vision, aglia, conjunctivitis.

Cardio-vascular system and blood (hematopoiesis, hemostasis): development (aggravation) chronic heart failure, integuments, edematous syndrome, increased blood pressure, bleeding (from the gastrointestinal tract, gingival, Royal, hemorrhoidal), anemia (incl. autoimmune hemolytic and aplastic), leukopenia, thrombocytopenia, eozinofilija, agranulocytosis, trombotsitopenicheskaya purpura.

From the digestive tract: NSAID-gastropathy, nausea, vomiting, abdominal pain, heartburn, decreased appetite, diarrhea, abnormal liver function (increase in liver transaminases, giperʙiliruʙinemija); long-term use at high doses - erosive and ulcerative lesions of the gastrointestinal tract.

With the genitourinary system: impairment of renal function, proteinuria, hematuria, interstitial nephritis, nephrotic syndrome, papillary necrosis.

Allergic reactions: itching, rash, hives, exfoliative dermatitis, uzlovataya эritema, anaphylactic shock, bronchospasm, angioedema, toxic epidermal necrolysis (Lyell's syndrome).

Other: giperglikemiâ, glycosuria, hyperkalemia, photosensitivity; aseptic meningitis (more frequently in patients with autoimmune diseases), increased sweating; local reactions at the rectal: burning, itchy skin, heaviness in the anorectal area, aggravation of hemorrhoids.

When applied to the skin: allergic reactions; itchiness and redness of the skin, rash at the site of application, xerosis, burning; in a few cases, aggravation of psoriasis; in the long-term use-systemic manifestations.

When instilled in the eye: allergic reactions; in the long-term use-clouding of the cornea, conjunctivitis, systemic side effects.

Cooperation.

Reduces the diuretic effect of potassium-sparing, thiazide and loop diuretics. Increases (mutually) the risk of side effects (primarily gastrointestinal lesions) other NSAIDs. Increases in plasma concentration of digoxin, methotrexate and drugs Li⁺, which may lead to increased toxicity. Sharing with paracetamol increases the risk of nephrotoxicity manifestations. Ethanol, Colchicine, corticotropin and glucocorticoids increases the risk of bleeding in the gastrointestinal tract. Enhances hypoglycemic effect of insulin and oral hypoglycemic drugs; It increases the effect of indirect anticoagulants, antiagregantov, fibrinolitikov (alteplaza, streptokinase and urokinase) and increases the risk of bleeding. Against the background of the use of potassium-sparing diuretics increase the risk of hyperkalemia; reduces the effectiveness of antihypertensive drugs and urikozuricheskih (incl. beta-blockers); It intensifies the side effects of mineralogy- and glucocorticoids, estrogen. Cyclosporine and drugs increase the nephrotoxicity of gold (due to the suppression of PG synthesis in the kidneys). Цefamandol, cefoperazone, cefotetan, valproic acid increases the frequency of and the risk gipoprotrombinemii bleeding. Antacids and cholestyramine reduce the absorption of indomethacin. Increases toxicity of zidovudine (by inhibiting the metabolism), in infants increases the risk of toxic effects of aminoglycosides (tk. reduced renal clearance and increases the concentration in the blood). Myelotoxic drugs increase the expression gematotoksichnosti.

Overdose.

Symptoms: nausea, vomiting, Strong headache, dizziness, memory impairment, disorientation; in severe cases, paresthesia, numbness and cramps.

Treatment: simptomaticheskaya therapy. Hemodialysis nyeeffyektivyen.

Dosing and Administration.

Inside, / m, rectally, fur gloves, konъyunktyvalno. The mode set individually depending on the evidence, severity of the disease and other factors.

Inside: adults appointed dose on 25 mg 2-3 times a day, with the lack of expressiveness of effect is on 50 mg 3 once a day, retard tablets (75 mg) -1-2 times a day, The maximum daily dose - 200 mg. With long-term use, the maximum daily dose should not exceed 75 mg. Upon reaching the effect of treatment was continued for 4 weeks in the same or a reduced dose.

For the treatment of acute conditions or edema exacerbation of chronic process is introduced into / m 60 mg 1-2 times a day for 7-14 days, and then transferred to ingestion or rectal administration. Rectal: after the liberation of the intestine, by 50 mg 1-3 times a day or 100 mg at bedtime; The maximum daily dose - 200 mg. Children over 14 years are 1.5-2.5 mg/kg/day.

Fur gloves: rub a thin layer of the skin over the painful parts of the body (Apply only to undamaged areas) 3-4 Times daily.

Konъyunktyvalno: for the inhibition of intraoperative miosis instill 1 a drop in the conjunctival sac for 2 h intervals 30 m (4 times) before the operation. In other testimony is on 1 drop 3-4 times per day.

In dentistry: inside, adults — on 25-50 mg 3-4 times a day; locally — 10% ointment rubbed into the skin (Apply only to undamaged areas) 3-4 Times daily.

Precautions.

Particularly close medical supervision is required when specifying a history of allergic reactions to the drug "aspirin" series, "Aspirin" triad, gastric ulcer and duodenal ulcer, as well as blood coagulation disorders, giperʙiliruʙinemii, thrombocytopenia, epilepsy, parkinsonizme, depression, in childhood and old age.

The risk of cardiovascular events. NSAIDs, incl. indomethacin, can cause increased risk of serious cardiovascular complications, incl. myocardial infarction and stroke, that can lead to death, especially with prolonged use. Patients with cardiovascular disease or risk factors for cardiovascular disease risk is particularly high.

The risk of gastrointestinal complications. NSAIDs, incl. indomethacin, cause increased risk of serious side effects from the gastrointestinal tract, including bleeding, ulceration and perforation of the stomach or intestines, which can be fatal, especially with prolonged use. These complications can occur at any time without the use of the symptoms heralding. Elderly patients are at greater risk of serious complications from the gastrointestinal tract.

When referring to a history of allergic reactions to NSAIDs used only in emergency cases.

During treatment requires monitoring of peripheral blood and functional state of the liver and kidneys. If you want to determine the 17-ketosteroids drug should be discontinued for 48 h before the test.

Eyedrop: after removal of contact lenses produced by landfill 5 m. In the presence of infection or threat of development at the same time appoint a local antibacterial treatment.

Avoid contact with eyes, on mucous membranes and open wounds forms for dermal application.

During the period of treatment must be careful when driving and occupation of other potentially hazardous activities, require high concentration and speed of psychomotor reactions.

Cautions.

During an acute attack of gout preferred fast dosage forms.

Cooperation