Indomethacin

Dosage form

Rectal suppositories

Composition per suppository:

Active substance

: indomethacin – 50 mg (100 mg).

Excipients

: solid fat (Vitepsol N 15) – 1.30 g (1.30 g), solid fat (Vitepsol W 35) – 0.65 g (0.60 g).

Description

Suppositories are torpedo-shaped with a smooth surface, white to light yellow, odorless. The cut surface should be smooth and uniform.

Pharmacotherapeutic group

Non-steroidal anti-inflammatory drug (NSAID).

ATX code

: M01AB01.

pharmachologic effect

Pharmacodynamics

Indomethacin has anti-inflammatory, analgesic, antipyretic and antiplatelet effects. Suppresses the activity of anti-inflammatory factors, reduces platelet aggregation. By inhibiting type II cyclooxygenase, it disrupts the metabolism of arachidonic acid, reduces the amount of prostaglandins both in the site of inflammation and in healthy tissues, and suppresses the exudative and proliferative phases of inflammation. Eliminates or reduces pain of a rheumatic and non-rheumatic nature (including pain in the joints at rest and during movement, reduces morning stiffness and swelling of the joints, helps to increase range of motion; in inflammatory processes that occur after operations and injuries, 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%. Bonding with plasma proteins is 90%, half-life is 4.5 hours. Metabolized mainly in the liver, 70% is excreted by the kidneys (30% unchanged), 30% through the gastrointestinal tract (GIT). Not removed by dialysis. Passes into breast milk.

Indications for use

Acute and chronic pain in inflammatory and degenerative diseases of the musculoskeletal system: rheumatoid arthritis; juvenile chronic arthritis; ankylosing spondylitis (ankylosing spondylitis); gouty arthritis; psoriatic arthritis; Reiter's disease;
Rheumatic lesions of soft tissues: tendinitis, bursitis, tendobursitis, tendovaginitis;
Discopathies, neuritis, plexitis, radiculoneuritis;
Dysmenorrhea.

The drug is intended for symptomatic therapy, reducing pain and inflammation at the time of use, and does not affect the progression of the disease.

Contraindications

Hypersensitivity to indomethacin or any of the excipients of the drug;
Complete or incomplete combination of bronchial asthma, recurrent loliposis of the nose and paranasal sinuses and intolerance to acetylsalicylic acid or other non-steroidal anti-inflammatory drugs (including a history), urticaria or rhinitis;
Peptic ulcer of the stomach and duodenum, inflammatory bowel diseases (ulcerative colitis, Crohn's disease), bleeding (including intracranial, from the gastrointestinal tract (GIT);
Congenital heart defects (severe coarctation of the aorta, pulmonary atresia, severe tetralogy of Fallot), period after coronary artery bypass grafting;
Severe heart failure;
Renal failure (creatinine clearance less than 30 ml/min), active liver disease;
Liver failure
Blood clotting disorders (including hemophilia, prolongation of bleeding time, bleeding tendency);
Hematopoietic disorders (leukopenia, anemia);
Confirmed hyperkalemia;
Pregnancy and breastfeeding;
Children's age (up to 15 years).

Carefully

Coronary heart disease, cerebrovascular diseases, chronic heart failure, dyslipidemia, hyperlipidemia, diabetes mellitus, thrombocytopenia, peripheral arterial disease, arterial hypertension, smoking, chronic renal failure (creatinine clearance 36-60 ml/min), liver cirrhosis with portal hypertension, hyperbilirubinemia, a history of ulcerative lesions of the gastrointestinal tract, the presence of Helicobacter ruby infection, long-term use of NSAIDs, frequent alcohol consumption, severe somatic diseases, concomitant therapy with the following drugs: anticoagulants (including warfarin), antiplatelet agents (including acetylsalicylic acid, clopidogrel) , oral glucocorticosteroids (including prednisolone), selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline); mental disorders, epilepsy, parkinsonism, depression, old age.

Use during pregnancy and breastfeeding

Pregnancy

Indomethacin is not used during pregnancy.

Breast-feeding

Indomethacin is excreted in breast milk. If treatment with the drug is necessary, breastfeeding should be stopped.

Directions for use and doses

Rectally. Adults and children over 15 years of age: suppositories 50 mg twice a day or 100 mg once a day. The maximum daily dose is 200 mg. Doses above 150-200 mg increase the risk of side effects. Duration of treatment: no more than 7 days.

Side effects can be reduced by using the lowest effective dose for the shortest possible period of time.

Side effect

From the digestive system

– NSAID gastropathy, nausea, heartburn, loss of appetite, abdominal pain, hemorrhages and ulcers, vomiting (including blood), diarrhea, constipation, melena, ulcerative stomatitis, increased activity of “liver transaminases” (ALAT, ASAT) ), transient increase in bilirubin; rarely toxic hepatitis with or without jaundice; very rarely - fulminant hepatitis. With long-term use in large doses, ulceration of the mucous membrane of the gastrointestinal tract occurs.

From the nervous system

– headache, dizziness, insomnia, psychomotor agitation, irritability, excessive fatigue, drowsiness, depression, peripheral neuropathy.

From the senses

– diplopia, blurred vision, hearing loss, tinnitus, taste disturbance, corneal clouding, conjunctivitis.

From the cardiovascular system

– tachyarrhythmia, edema syndrome, increased blood pressure, development (worsening) of chronic heart failure.

From the urinary system

– renal dysfunction, nephrotoxic syndrome, proteinuria, hematuria, interstitial nephritis, papillary necrosis.

From the hematopoietic organs and hemostasis system

– bleeding (gastrointestinal, gingival, uterine, hemorrhoidal), leukopenia, thrombocytopenia, agranulocytosis, anemia (including hemolytic and aplastic), eosinophilia, thrombocytopenic purpura.

Allergic reactions

– usually itchy skin, skin rash; rarely - urticaria, bronchospasm, asthmatic attacks, angioedema; very rarely - bullous rashes, redness of the skin, eczema, exfoliative dermatitis, allergic purpura, Stevens-Johnson syndrome, in isolated cases - photosensitivity, toxic epidermal necrolysis (Lyell's syndrome), erythema nodosum, anaphylactic shock.

Laboratory indicators

– agranulocytosis, leukopenia, thrombocytopenia, hyperglycemia, glucosuria, hyperkalemia.

Local reactions

– irritation, heaviness in the anorectal area, exacerbation of hemorrhoids.

Others

– aseptic meningitis (more often in patients with autoimmune diseases), increased sweating, aplastic anemia, autoimmune hemolytic anemia.

Overdose

Symptoms

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

Treatment

: rapid elimination of the drug from the body, symptomatic therapy.

Hemodialysis is ineffective.

Interaction with other drugs

Increases plasma concentrations of digoxin, methotrexate and Li+ drugs, which can lead to increased toxicity. Combined use with paracetamol increases the risk of developing nephrotoxic effects. Ethanol, colchicine, glucocorticosteroids and corticotropin increase the risk of gastrointestinal bleeding. Enhances the hypoglycemic effect of insulin and oral hypoglycemic drugs; enhances the effect of indirect anticoagulants, antiplatelet agents, thrombolytics (alteplase, streptokinase and urokinase) - there is a risk of bleeding. Reduces the effect of diuretics; with the use of potassium-sparing diuretics, the risk of hyperkalemia increases; reduces the effectiveness of uricosuric and antihypertensive drugs (including beta-blockers); enhances the side effects of methotrexate, glucocorticosteroids, and other NSAIDs. Cyclosporine and gold preparations increase nephrotoxicity (apparently by suppressing the synthesis of prostaglandins in the kidneys). Cefamandole, cefoperazone, cefotetan, valproic acid, plicamycin increase the incidence of hypoprothrombinemia and the risk of bleeding. Antacids and cholestyramine reduce the absorption of indomethacin. Increases the toxicity of zidovudine (due to inhibition of metabolism); in newborns, it increases the risk of developing toxic effects of aminoglycosides (since it reduces renal clearance and increases blood concentrations). Myelotoxic drugs increase the manifestations of hemotoxicity of the drug.

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.

To prevent and reduce dyspeptic symptoms, antacid medications should be used.

The drug should not be used simultaneously with other NSAIDs.

The drug can change the properties of platelets, but does not replace the preventive effect of acetylsalicylic acid in cardiovascular diseases. The use of the drug may adversely affect female fertility and is not recommended for women planning pregnancy.

Impact on the ability to drive vehicles and operate machinery

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

Release form

Rectal suppositories 50 mg, 100 mg.

1, 2, 3, 4, 5, 6, 7, 8, 9, 10 suppositories in a blister pack made of a two-layer film or a film made of PVC/PE polymer materials or a white combined PVC/PE film or a polyvinyl chloride film.

1, 2, 3, 4, 5, 6, 7, 8, 9, 10 blister packs together with instructions for medical use of the drug are placed in a cardboard pack.

Storage conditions

In a place protected from light at a temperature not exceeding 25 ° C.

Keep out of the reach of children.

Best before date

3 years.

Do not use after the expiration date stated on the packaging.

Vacation conditions

On prescription.

Indomethacin enteric-coated tablets 25 mg 30 pcs. in Moscow

Inhibits cyclooxygenase (COX-1 and COX-2), reduces the synthesis of PGs, which cause the development of pain at the site of inflammation, an increase in temperature and an increase in tissue permeability. Has an antiplatelet effect.

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