Indometacin coated enteric tablets 25 mg. №30

Description

Indometacin Composition

active substance: 1 tablet contains 25 mg of indomethacin
excipients: lactose, wheat starch, povidone K 25, microcrystalline cellulose, magnesium stearate, talc, colloidal silicon dioxide
enteric shell: copolymer methacrylic acid ethyl acrylate (1: 1) 30% dispersion (eudragit L 30 D-55), copolymer methyl acrylate: methyl methacrylate: methacrylic acid 30% dispersion (eudragit FS 30 D), sodium hydroxide, triethyl citrate, polysorbate 80, suspension pigments – brown WAS FS (talc, triethyl citrate, titanium dioxide (E 171), iron oxide yellow (E172), iron oxide red (E172), propane-1,2 diolalginate, potassium sorbate).

Indometacin Dosage form

Film-coated tablets.

Basic physical and chemical properties:

round biconvex enteric-coated tablets, 7 mm in diameter, orange-brown in color.

Pharmacological group

Non-steroidal anti-inflammatory drugs. ATX code M01A B01.

Indometacin Pharmacological properties

Pharmacodynamics.

Indomethacin – a derivative of indolocytic acid, belongs to the group of non-steroidal anti-inflammatory drugs (NSAIDs). Has a pronounced anti-inflammatory effect, significantly exceeds the effect of phenylbutazone and acetylsalicylic acid. Its analgesic activity is comparable to that of metamizole. Has antipyretic effect. Indomethacin has a strong inhibitory effect on prostaglandin synthesis by inhibiting cyclooxygenase. In addition, it reduces platelet aggregation and lipoxygenase activity in the area of ​​inflammation, respectively, and leukotrienes also reduces the release of endogenous pyrogens, inactivates lysosomal enzymes, and inhibits the activity of neutral proteases. Its other effects may also be important, such as decoupelling of oxidative phosphorylation and inhibition of the reuptake of catecholamines, an increase in norepinephrine metabolism, and a ganglion blocking effect is known.

Pharmacokinetics.

Resorption: after oral administration, 80-90% of the dose is absorbed through the mucous membrane in the small intestine. Reaches the maximum concentration in blood plasma within 1-2 hours.

Distribution is distributed over all tissues and organs. Penetrates the placental and blood-brain barrier. Penetrates through the synovial membrane into the joints, while its concentration in the synovial fluid is higher than in the blood plasma. Plasma protein binding in 90-98% and therefore is able to displace other drugs, and enhance their therapeutic effect with simultaneous use.

Metabolism is metabolized in the liver through oxidation and conjugation.

Conclusion: the half-life of indomethacin varies between 2.6 and 11.2 hours, or an average of 5.8 hours. Up to 60-75% is excreted through the kidneys, 10-20% of which are unchanged, and the rest is excreted in bile and feces. Penetrates into breast milk.

Indications

The effectiveness of short-term symptomatic treatment with indomethacin has been established in relation to the following conditions:

acute and chronic pain in inflammatory and degenerative diseases of the musculoskeletal system: acute and acute rheumatoid arthritis, chronic ankylosing spondylitis (ankylosing spondylitis), gout attack and gouty arthritis, moderate to severe osteoarthritis
diseases of the periarticular tissues tendonitis, bursitis (acute painful shoulder), tendobursitis, tendovaginitis, pain syndrome and inflammation after injuries (including in athletes) and surgical interventions
discopathy, plexitis, radiculoneuritis
dysmenorrhea.

Contraindications

Hypersensitivity to drug components
hypersensitivity to acetylsalicylic acid or other NSAIDs with clinical manifestations of an asthmatic attack, angioedema, urticaria, or rhinitis
active gastric and duodenal ulcers or relapses (two or more cases of proven ulcers and bleeding), ulcerative colitis and / or enterocolitis
a history of gastrointestinal bleeding and perforation associated with a history of NSAIDs
concomitant use of other non-steroidal anti-inflammatory drugs, including specific inhibitors of cyclooxygenase-2 for an increased risk of undesirable effects
severe heart failure
severe hepatic and renal impairment
pre- and postoperative pain during coronary artery bypass grafting.