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NSAIDs
. The active substance is
Indomethacin
. The main component is an indoleacetic acid derivative. Indomethacin has analgesic, anti-inflammatory action.
Antipyretic effect
associated with the process of suppressing the activity of a non-selective COX-1, 2, who are actively involved in synthesizing prostaglandins. The drug has
antiplatelet effects
. The drug is in the form of a gel and ointment eliminates pain, joint swelling, morning stiffness, erythema, swelling around the joints, makes it possible to expand the range of motion. Indomethacin released in a tablet dosage form, in the form of pills, capsules, gel, ointment, solution, suppository.
Indications:
Instructions on the drug indomethacin recommends that prescribers in the pathology of the musculoskeletal system degenerative and inflammatory: Personeydzha disease-Turner (neuralgic amyotrophy) Reiter's disease arthritis Paget's disease, juvenile chronic arthritis, psoriatic arthritis, rheumatoid arthritis, ankylosing spondylitis (ankylosing spondylitis), rheumatic, gouty arthritis (except acute attacks of gout).
The drug relieves pain: backache, toothache, after traumatic injuries and surgical interventions, headache, pain in the tendinitis and bursitis, neuralgia , Sciatica, myalgia. The drug is indicated for the symptomatic treatment of pericarditis , Secondary hyperaldosteronism ( Bartter syndrome ) At algodismenoree, with cleft batallova duct, adnexitis, inflammation in the pelvis. During delivery the medication prescribed as a tocolytic and anesthetic. Indomethacin indicated in otitis, pharyngitis, tonsillitis and other infectious and inflammatory diseases of the upper respiratory tract, accompanied by pain. Indomethacin prescribed for feverish syndrome (liver metastases of solid tumors, lymphomas, megakaryoblastoma ) In the absence of the therapeutic effect of paracetamol and acetylsalicylic acid .
Indomethacin gel and ointment prescribed for traumatic injuries of the joints, ligaments, muscles, tendons (sprains, strains, contusions, load). The drug is indicated for localized inflammation of the soft tissues as tendinitis, tenosynovitis, bursitis, syndrome of "shoulder-hand." Ointment and gel is prescribed for myalgia, lumbago , Sciatica, radiculitis , Rheumatoid arthritis, deforming osteoarthritis, osteochondrosis with radicular syndrome, ankylosing spondylitis, frozen shoulder , Psoriatic arthritis. The exception is a degenerative pathology of the small intervertebral and hip joints.
Contraindications:
Indomethacin is not appointed at birth heart defects (severe tetralogy of Fallot, pulmonary atresia, severe coarctation of the aorta), and peptic ulcer disease of the digestive tract, bleeding (from the gastrointestinal tract, intracranial), and "Aspirin" triad (Intolerance to medication pyrazoline series, and acetylsalicylic acid, recurrent polyposis of the paranasal sinuses and nasal, bronchial asthma), and ulcerative colitis , Liver cirrhosis with portal hypertension, disorders of the visual and color perception, in arterial hypertension, edema, congestive heart failure, asthma, diseases of the optic nerve, liver failure, bleeding disorders (tendency to frequent bleeding, increased bleeding time, hemophilia ), When carrying a pregnancy, disorders of hematopoiesis (anemia, leukopenia), the pathology of the vestibular apparatus, reduced auditory perception, chronic renal pathology system, breastfeeding. Rectal forms of drugs are contraindicated with hemorrhoids, proctitis and rectal bleeding. Elderly patients and children, depression, Parkinsonism, epilepsy, thrombocytopenia, hyperbilirubinemia Indomethacin administered with caution. Ointment and gel is not indicated for children under 1 year, in violation of the integrity of the skin.
Side effect:
The digestive tract: irregularities in the system of liver, diarrhea, epigastric pain, NSAID-gastropathy . heartburn , Vomiting, increased liver enzymes, hyperbilirubinemia, decreased appetite, nausea. Prolonged therapy can lead to ulceration of the mucous membranes in the digestive system. Senses: corneal opacity, disorders of visual perception, diplopia , Auditory perception disorders, tinnitus, changes in taste perception, conjunctivitis. Nervous system: peripheral neuropathy , Depression, increased sleepiness, fatigue, agitation, dizziness, irritability, headaches, insomnia . Cardiovascular system: swelling, tachyarrhythmia , Exacerbation of chronic heart failure, increased blood pressure. Urinary system: papillary necrosis, nephrotic syndrome , Interstitial nephritis, renal disorders in the system, hematuria, proteinuria .
Hemostatic system, organs of hematopoiesis: leukopenia, anemia (aplastic and haemolytic forms), bleeding (gingival, gastrointestinal, hemorrhoids, uterine), eosinophilia, thrombocytopenia , Thrombocytopenic purpura, agranulocytosis. Allergic reactions: bronchospasm , Angioedema, hives . itching , Skin rash, anaphylactic shock, erythema nodosum , Photosensitivity, Lyell's syndrome (epidermal necrolysis toxic). Changes in laboratory parameters: increase in potassium agranulocytes, sugar, glycosuria, leukopenia, thrombocytopenia. Local reactions: aggravation of hemorrhoids, heaviness and discomfort in the anorectal area, itching, burning sensation. Among the other possible reactions autoimmune hemolytic anemia, aplastic anemia , Sweating, aseptic meningitis (in patients with autoimmune disorders). The gel and ointment may cause exacerbation of psoriasis, rash, flushing, and applications in place, long-term treatment may be systemic manifestations.
Overdose:
Manifested severe headaches, severe dizziness, vomiting, memory impairment, nausea, disorientation in time and space. In severe cases, seizures occur, paresthesia , Numb limbs. Requires emergency removal of the drug from the human body, further tactics is based on symptomatic therapy. Hemodialysis is not proven effective. The specific antidote is not developed.
Mode of application:
Indomethacin administered rectally, topically and inside. Initially adults appoint indomethacin 25 mg 2-3 times a day (after a meal, drink milk). When failure amount of medicament increased to 150 mg daily (three times, 50 mg). Indomethacin retard taken 1-2 times a day (one tablet contains 75 mg of active substance). The day not more than 200 mg. After achieving the desired effect amount of the drug is gradually reduced over 4 weeks.
The maximum daily dosage for long-term treatment is 75 mg. Indomethacin administered intramuscularly 1-2 times a day to 60 mg for the relief of chronic process, acute conditions. Intramuscular injections were for 7-14 days and then transferred for oral or rectal forms of administration. Rectal suppositories are administered 1-3 times a day for 50 mg much as possible deep after the complete liberation of the intestine before bedtime. In attacks of gout prescribed 200 mg per day in suppositories (in addition to receiving inside). The gel and ointment applied only topically applying to the area affected joints 3-4 times a day, may be imposed occlusive dressings (but not recommended). For adults the total amount of the ointment should be more than 15 cm per day, for children - 7 5 cm ointment extruded from the tube.
Special instructions:
Indomethacin cancel 48 hours prior to determining the level of 17-ketosteroids. During treatment requires control of the functional state of the liver and kidney systems, indicators Peripheral Blood . Use of antacid medicaments can reduce and prevent dyspepsia caused by the intake of indomethacin. Indomethacin is able to influence the management of complex machinery, motor vehicles. Avoid getting gel ointments and indomethacin on the mucous membranes, the eyes, the damaged tissue.
Drug Interactions:
Severity nephrotoxic effects increases when combined with acetaminophen. The drug increases levels Methotrexate , Drugs with lithium ions, digoxin, which leads to increased severity of their toxic effects. Glucocorticoids, colchicine, corticotrophin, ethanol increases the risk gastrointestinal bleeding . The medicament enhances hypoglycemic effect of oral hypoglycemic agents, insulin; improves antiplatelet agents , Anticoagulants, thrombolytics (urokinase, alteplase, streptokinase); possible bleeding.
Indomethacin increases the side effects of the ISS, estrogen, glucocorticosteroids , Aspirin, NSAIDs. The drug reduces the effect of diuretics. The risk of hyperkalemia is significantly increased in patients receiving potassium-sparing diuretics . Indomethacin is able to decrease the effectiveness of antihypertensive agents and urikozuricheskih. Due to suppression of the synthesis of prostaglandins in the kidney increased nephrotoxicity when taking drugs Au, cyclosporine . The absorption of the basic substance is reduced when receiving kolestiramina and antacids.
Plicamycin, tsefotetan, cefamandole, valproic acid, tsefaperazon increase the risk of bleeding and increase the incidence of gipoprotrombinemii . Gematotoksichnosti increases with concurrent therapy myelotoxic drugs. Due to the inhibition of metabolism of indomethacin increases the toxicity of zidovudine. The drug increases the risk of toxic effects from the use of aminoglycosides in newborn infants (by increasing the concentration of active substance in the blood and reduce renal clearance ).