Indomethacin 100 Berlin-Chemie, rectal 100 mg 10 pcs

Pharmacodynamics

The drug from the group of NSAIDs, has anti-inflammatory, analgesic, antipyretic and anti-aggregation effects. Inhibits the activity of pro-inflammatory factors and reduces platelet aggregation.

Inhibiting cyclooxygenase 1 and 2 it disrupts arachidonic acid metabolism, decreases quantity of prostaglandins (Pg) both in inflammation focus and healthy tissues, suppresses exudative and proliferative phases of inflammation.

It causes alleviation or disappearance of pain syndrome of rheumatic and non-rheumatic character (including joint pain at rest and on movement, decrease of morning stiffness and joint swelling, promotes increase of movement capacity; in inflammatory processes following operations and injuries it quickly reduces both spontaneous pain and pain on movement, reduces inflammatory swelling of the wound area).

Pharmacokinetics

Absorption is fast. Bioavailability by rectal route of administration is 80-90%. Binding to plasma proteins – 90%, T1/2 – 4-9 hours.

Metabolized mainly in the liver, 30% of the drug is excreted unchanged. 70% is excreted by the kidneys, 30% – through the intestine. It is not eliminated in dialysis. It penetrates into the breast milk.

Indications

Inflammatory and degenerative diseases of the musculoskeletal system: rheumatoid arthritis, psoriatic, juvenile chronic arthritis, ankylosing spondylitis;
rheumatic lesions of soft tissues;
gouty arthritis.
as part of complex therapy for infectious and inflammatory diseases of the ENT organs, adnexitis, prostatitis, cystitis, neuritis, algodismenorrhea, headache and toothache (as part of combination therapy).

Pharmacological effect

Pharmacodynamics

A drug from the NSAID group, it has anti-inflammatory, analgesic, antipyretic and antiaggregation effects. Suppresses the activity of pro-inflammatory factors, reduces platelet aggregation.

By inhibiting cycloxygenase 1 and 2, it disrupts the metabolism of arachidonic acid, reduces the amount of prostaglandins (Pg) both in the site of inflammation and in healthy tissues, and suppresses the exudative and proliferative phases of inflammation.

Causes a weakening or disappearance of pain of a rheumatic and non-rheumatic nature (including pain in the joints at rest and during movement, a decrease in morning stiffness and swelling of the joints, helps to increase the range of movements; in inflammatory processes that occur after operations and injuries, it quickly relieves both spontaneous pain and pain during movement, reduces inflammatory swelling at the wound site).

Pharmacokinetics

Absorption is fast. Bioavailability by rectal route of administration is 80-90%. Connection with plasma proteins – 90%, T1/2 – 4-9 hours

Metabolized mainly in the liver, 30% of the drug is excreted unchanged. 70% is excreted by the kidneys, 30% through the intestines. Not removed by dialysis. Passes into breast milk.

Special instructions

During treatment, monitoring of the peripheral blood picture and the functional state of the liver and kidneys is necessary. If it is necessary to determine 17-ketosteroids, the drug should be discontinued 48 hours before the study.

During the treatment period, it is necessary to refrain from driving vehicles and engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Active ingredient

Indomethacin

Composition

Active ingredients:

indomethacin 100 mg.

Excipients:

solid fat – 1.7 g,

corn starch – 100 mg.

Pregnancy

The drug is contraindicated for use during pregnancy and breastfeeding.

Contraindications

Hypersensitivity to indomethacin and other NSAIDs, incl. “aspirin” asthma;
peptic ulcer of the stomach and duodenum;
ulcerative colitis;
bleeding (intracranial, gastrointestinal);
congenital heart defects (coarctation of the aorta, pulmonary atresia, tetralogy of Fallot);
heart failure;
arterial hypertension;
color vision impairment;
optic nerve disease;
liver cirrhosis with portal hypertension;
liver failure;
bronchial asthma;
hemophilia, hypocoagulation, other blood diseases;
chronic renal failure;
hearing loss;
pathology of the vestibular apparatus;
deficiency of glucose-6-phosphate dehydrogenase;
proctitis, hemorrhoids;
pregnancy and breastfeeding;
children and adolescents up to 18 years of age.

With caution: with hyperbilirubinemia, thrombocytopenia, epilepsy, parkinsonism, depression, as well as in elderly patients.

Side Effects

From the digestive system: NSAID gastropathy, abdominal pain, nausea, vomiting, heartburn, anorexia, diarrhea, liver dysfunction (increased blood bilirubin, “liver” transaminases). With long-term use in large doses – ulceration of the mucous membrane of the gastrointestinal tract.

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

From the senses: hearing loss, tinnitus, taste disturbance, diplopia, blurred vision, corneal clouding, conjunctivitis.

From the cardiovascular system: heart failure, tachyarrhythmia, increased blood pressure.

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

From the hemostatic system: bleeding (gastrointestinal, gingival, uterine, hemorrhoidal), thrombocytopenia.

Allergic reactions: skin rash, itching, urticaria, Quincke’s edema, bronchospasm; rarely – Lyell’s syndrome, erythema nodosum, anaphylactic shock.

From the hematopoietic system: agranulocytosis, leukopenia, aplastic anemia, autoimmune hemolytic anemia.

Metabolism: hyperglycemia, glycosuria.

From the side of water and electrolyte balance: hyperkalemia.

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

Local reactions: burning, itching, heaviness in the anorectal area, exacerbation of hemorrhoids.

Interaction

Reduces the effectiveness of uricosuric drugs, antihypertensive and diuretics (saluretics); enhances the effect of indirect anticoagulants, antiplatelet agents, fibrinolytics, side effects of mineralocorticosteroids, estrogens, and other NSAIDs; enhances the hypoglycemic effect of sulfonylurea derivatives.

Combined use with paracetamol increases the risk of nephrotoxic effects. Ethanol, colchicine, glucocorticosteroids – increase the risk of developing gastrointestinal complications accompanied by bleeding.

Increases the concentration of lithium, methotrexate and digoxin in the blood. Cyclosporine and gold preparations increase the nephrotoxicity of indomethacin. Cefamandole, cefoperazone, valproic acid – increase the risk of developing hypoprothrombinemia and the risk of bleeding. Reduces the elimination of penicillins. Potentiates the toxic effect of zidovudine.

Overdose

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

Treatment: carry out symptomatic therapy. Hemodialysis is ineffective.

Storage conditions

At a temperature not exceeding 25 °C

Shelf life

3 years

Manufacturer

Berlin-Chemie AG, Germany