Indomethacin, rectal 50 mg, 6 pcs.

Pharmgroup:

NSAIDs.

Pharmic Action:

NSAID, indoleacetic acid derivative; has anti-inflammatory, analgesic and antipyretic effects associated with indiscriminate inhibition of COX1 and COX2 that regulate Pg synthesis. It has antiaggregant effect.

Pharmacokinetics:

Absorption is fast. Bioavailability during oral administration of usual tablets, capsules is 90-98%, during administration of sustained-action tablets within 12 hours 90% of the administered dose is absorbed, for rectal suppositories – 80-90%. After oral administration the TCmax is 2 hours, Cmax is 0.69 mcg/ml.

Binding with plasma proteins is 90%. It is metabolized mainly in liver.

T1/2 – 4-9 h (this figure may vary depending on the severity of systemic metabolism, enterohepatic circulation and reabsorption). Excreted by the kidneys is 70%, with 30% unchanged, and by the gastrointestinal tract 30%. It penetrates into the breast milk, when the mother uses 200 mg of the drug per day, 0.5 to 2 mg is determined in the milk. The drug is not eliminated by dialysis.

Indications

Inflammatory and degenerative diseases of the musculoskeletal system: rheumatoid, psoriatic, juvenile chronic arthritis, arthritis in Paget’s disease and Reiter’s disease, neuralgic amyotrophy (Personej-Turner disease), ankylosing spondylitis (Behterev disease), gouty arthritis (in acute gout attack, fast acting pharmaceutical forms are preferable), rheumatism.

Pain syndrome: headache (including menstrual syndrome) and toothache, lumbago, sciatica, neuralgia, myalgia, after injuries and surgery accompanied by inflammation, bursitis and tendinitis (most effective for localization in the shoulder and forearm).

Algodysmenorrhea; Bartter’s syndrome (secondary hyperaldosteronism); pericarditis (symptomatic treatment); childbirth (as analgesic and tocolytic agent); pelvic inflammatory processes, including Adnexitis.

Infection of the Botallic duct.

Infectious inflammatory diseases of the ENT with a pronounced pain syndrome (in the treatment): pharyngitis, tonsillitis, otitis.

Fever syndrome (including lymphogranulematosis, other lymphomas and liver metastases of solid tumors) – in case of ineffectiveness of ASA and paracetamol. The drug is intended for symptomatic therapy, to reduce pain and inflammation at the time of use, it has no effect on the progression of the disease.

Active ingredient

Indomethacin

Composition

Active substance:

Indomethacin 50 mg

How to take, the dosage

Rectally (inserted into the rectum). Before administering the suppository, it is recommended to empty the intestines. Wash your hands, remove the suppository from the lozenge by cutting it with scissors or by hand, pulling the edges of the lozenge at different ends, and insert the suppository into the anus with the pointed end, as deeply as possible. For more convenient application of the suppository it is recommended to bend or sit down; it is possible to insert it lying on the side.
Suppositories 50 mg adults 1-3 times a day; children (older than 14 years) once a day;
Suppositories 100 mg – once a day;
During a gout attack to 200 mg a day.
Recommended for nighttime use.

Interaction

Concomitant use of indomethacin may reduce the effects of saluretics, beta-adrenoblockers; increase the effects of indirect anticoagulants.

In concomitant use of indomethacin and diflunisal there is a risk of severe bleeding from the gastrointestinal tract.

Concomitant use with probenecid may increase the plasma concentration of indomethacin.

Indomethacin may decrease the tubular secretion of methotrexate, which leads to increased toxicity.

The toxicity of cyclosporine is increased when used concomitantly with NSAIDs.

Indomethacin in dose of 50 mg 3 times daily increases plasma lithium concentration and decreases clearance of lithium from the body in patients with psychiatric disorders.

Concomitant use of indomethacin with digoxin may increase the plasma concentration of digoxin and increase the elimination half-life of digoxin.

Special Instructions

With caution, use in elderly patients, as well as in patients with a history of liver, renal, GI diseases, dyspeptic symptoms at the time of use, arterial hypertension, heart failure, immediately after major surgical interventions, with parkinsonism, epilepsy.

When a history of allergic reactions to NSAIDs is indicated, use only in emergency cases.

During treatment, systematic monitoring of liver and renal function, peripheral blood picture is required.
Simultaneous use with acetylsalicylic acid and other NSAIDs is not recommended.

Indomethacin should not be used concomitantly with diflunisal.

In concomitant use of indomethacin with lithium preparations, be aware of the possibility of symptoms of lithium toxicity.

When used topically, do not apply to the wounded surface of the skin, and avoid contact with the eyes or mucous membranes.

Impact on driving and operating machinery

At any time during treatment, avoid potentially hazardous activities requiring concentration and increased speed of psychomotor reactions.

Contraindications

• Individual hypersensitivity to indomethacin, aspirin or other NSAIDs (history of bronchospasm, urticaria or rhinitis caused by taking acetylsalicylic acid or other NSAIDs);
• gastric and/or intestinal ulcer in the acute phase;
• pregnancy and lactation;
• childhood (under 14 years).
• disorders of hematopoiesis;
• explicit hepatic and/or renal dysfunction;
• severe forms of chronic heart failure, arterial hypertension, pancreatitis;
• for rectal use: proctitis, recent bleeding from the rectum.

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Side effects

Digestive system disorders: nausea, anorexia, vomiting, abdominal pain and discomfort, constipation or diarrhea, erosive ulcerative lesions, bleeding and perforations of the gastrointestinal tract; rarely – intestinal strictures, stomatitis, gastritis, flatulence, bleeding from the sigmoid colon or from diverticulum, jaundice, hepatitis.

CNS and peripheral nervous system disorders:Dizziness, headache, depression, feeling of fatigue; rarely – anxiety, fainting, somnolence, seizures, peripheral neuropathy, muscle weakness, involuntary muscle movements, sleep disorders, mental disorders (depersonalization, psychotic episodes), paresthesias, dysarthria, parkinsonism.

Cardiovascular system disorders: edema, increased BP, tachycardia, chest pain, arrhythmia, palpitation, arterial hypotension, congestive heart failure, hematuria.

Allergic reactions: rare – itching, urticaria, angiitis, erythema nodosum, skin rash, exfoliative dermatitis, Stevens-Johnson syndrome, erythema multiforme, toxic epidermal necrolysis, hair loss, acute respiratory distress, severe BP drop, anaphylactic reactions, angioneurotic edema, dyspnea, bronchial asthma, pulmonary edema.

Hematopoietic system: rarely – leukopenia, petechiae or ecchymoses, purpura, aplastic and hemolytic anemia, thrombocytopenia, DIC syndrome.

Senses: rarely – visual disturbances, diplopia, orbital and periorbital pain, tinnitus, hearing disorders, deafness.

Urinary system disorders: rare – proteinuria, nephrotic syndrome, interstitial nephritis, renal failure.

Metabolism disorders: rare – hyperglycemia, glucosuria, hyperkalemia.

Other: rare – vaginal bleeding, hot flashes, increased sweating, nasal bleeding, enlargement and tightness of the mammary glands, gynecomastia.

Local reactions: in place of injection in some cases – infiltrate and abscess formation; with rectal administration irritation of rectal mucosa, tenesmus, exacerbation of chronic colitis is possible.

In external application: itching, redness, rash in the application area.

Overdose

Symptoms: nausea, vomiting, severe headache, dizziness, memory impairment, disorientation. In severe cases paresthesias, numbness of extremities, convulsions.

Treatment: symptomatic therapy. Hemodialysis is ineffective.

Pregnancy use

Indomethacin is contraindicated in the third trimester of pregnancy. In I and II trimesters of pregnancy as well as during lactation (breastfeeding) use is not recommended.

Indomethacin is excreted in small amounts with breast milk.

Similarities

Indomethacin 100 Berlin-Chemie, Indomethacin 50 Berlin-Chemie, Indomethacin, Indocollir, Metindol Retard