Indomethacin - instructions for use, dose, side effects, contraindications

Excipients: silicon dioxide colloid (aerosil), fat solid, castor oil, urea (carbamide), propyl parahydroxybenzoate (nipazole), polysorbate (Tween-80).

Description:

Suppositories white with a yellowish or creamy hue of color with a weak specific odor, torpedo-shaped.

Pharmacotherapeutic group:NSAIDs

ATX: & nbsp

C.01.E.B.03 Indomethacin

S.01.B.C.01 Indomethacin

M.02.A.A.23 Indomethacin

Pharmacodynamics:

Indomethacin has anti-inflammatory, analgesic, antipyretic and antiplatelet effect. Suppresses the activity of proinflammatory factors, reduces platelet aggregation. By depressing cyclooxygenase 1 and 2, it breaks the metabolism of arachidonic acid, reduces the amount of prostaglandins (Pg) both in the focus of inflammation, and in healthy tissues, suppresses the exudative and proliferative phases of inflammation. It causes a weakening or disappearance of the pain syndrome of a rheumatic and non-rheumatic nature (incl.with pain in the joints at rest and during movement, a decrease in morning stiffness and swelling of the joints, contributes to an increase in the volume of movements; in inflammatory processes that occur after surgery and trauma, quickly alleviates both spontaneous pain and pain during movement, reduces inflammatory edema at the wound site).

Pharmacokinetics:

Absorption is fast. Bioavailability in the rectal route of administration is 80-90%. The connection with plasma proteins is 90%, the half-life is 4-9 hours. Metabolized, mainly in the liver, 30% of the drug is unchanged. It is excreted by the kidneys at 70%, with 30% unchanged, and through the gastrointestinal tract - 30%. It is not removed during dialysis. Penetrates into breast milk.

Indications:

NSAIDs are intended for symptomatic therapy, reducing pain and inflammation at the time of use, the progression of the disease is not affected.

Inflammatory and degenerative diseases of the musculoskeletal system: rheumatoid arthritis, psoriatic, juvenile chronic arthritis, ankylosing spondylitis, rheumatic soft tissue damage; gouty arthritis.

As an auxiliary for infectious-inflammatory diseases ENT organs, adnexitis, prostatitis, cystitis, neuritis, algodismenorrhea, headache and toothache (as part of combination therapy).

Contraindications:

NSAIDs are contraindicated:

- in the period after aortocoronary shunting;

- bleeding (including intracranial, from the digestive tract), blood clotting disorders (including hemophilia, prolonged bleeding time, a tendency to bleeding), hematopoiesis (leukopenia and anemia); for rectal administration - rectal bleeding;

- Congenital heart defects (coarctation of the aorta, pulmonary atresia, tetralogy of Fallot), heart failure;

- III trimester of pregnancy, lactation period;

- children's age till 14 years;

- hypersensitivity to the active substance or ancillary components;

- anamnestic data on an attack of bronchial obstruction, rhinitis, urticaria after taking acetylsalicylic acid or other NSAIDs (complete or incomplete acetylsalicylic acid intolerance syndrome - rhinosinusitis, urticaria, polyps of the nasal mucosa, asthma);

- ulcerative colitis, erosive and ulcerative changes in the mucous membrane of the stomach or duodenum, active gastrointestinal bleeding;

- inflammatory bowel disease;

- cirrhosis of the liver with portal hypertension, severe hepatic insufficiency or active liver disease;

- severe renal failure (creatinine clearance less than 30 ml / min), progressive kidney disease;

- confirmed hyperkalemia;

- diseases of the optic nerve, impaired color vision, hearing loss;

- bronchial asthma, edema;

- pathology of the vestibular apparatus;

- deficiency of glucose-6-phosphate dehydrogenase;

- blood diseases;

- proctitis, hemorrhoids;

- arterial hypertension, hemophilia, hypocoagulation.

Carefully:

Ischemic heart disease, cerebrovascular disease, congestive heart failure, dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral arterial disease, smoking, creatinine clearance less than 60 ml / min, hyperbilirubinemia, thrombocytopenia, epilepsy, parkinsonism, depression, hypertension, cirrhosis with portal hypertension , severe somatic diseases, mental disorders.

Anamnestic data on the development of gastrointestinal lesions, the presence of infection Helicobacter pylori, children's and elderly age, long-term use of NSAIDs,frequent use of alcohol, severe physical illness, concomitant therapy with the following drugs:

- anticoagulants (for example, warfarin);

- antiaggregants (eg, acetylsalicylic acid, clopidogrel);

- oral glucocorticosteroids (for example, prednisolone);

- selective serotonin reuptake inhibitors (eg, citalopram, fluoxetine, paroxetine, sertraline).

To reduce the risk of developing adverse events on the part of the gastrointestinal tract, a minimum effective dose should be used with the minimum possible short course.

Dosing and Administration:

Rectal: after the release of the intestine, if possible deep into the rectum - 50 mg 1-3 times a day or 100 mg at bedtime, during a gout attack to 200 mg per day. The maximum daily dose is 200 mg.

Side effects:

From the digestive system: NSAIDs-gastropathy, abdominal pain, nausea, vomiting, heartburn, anorexia, diarrhea, impaired liver function (increase in the blood of bilirubin, "liver" transaminases). With prolonged 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 sense organs: hearing loss, tinnitus, taste disorder, diplopia, blurred vision, corneal opacity, conjunctivitis, photosensitivity.

From the CAS side: heart failure, tachyarrhythmia, increased blood pressure.

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

From the side of the hemostasis system: bleeding (gastrointestinal, gingival, uterine, hemorrhoidal), thrombocytopenia.

Allergic reactions: skin rash, itching, urticaria, angioedema, bronchospasm; rarely - Lyell's syndrome, erythema nodosum, anaphylactic shock.

Laboratory indicators: agranulocytosis, leukopenia, hyperglycemia, glucosuria, hyperkalemia.

Other: aplastic anemia, autoimmune hemolytic anemia, aseptic meningitis (more often in patients with autoimmune diseases), increased sweating, edematous syndrome, eosinophilia, thrombocytopenic purpura.

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

Overdose:

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

Treatment: symptomatic therapy, hemodialysis is ineffective.

Interaction:

Reduces the effectiveness of uricosuric drugs, hypotensive and diuretics (saluretics); strengthens the effect of indirect anticoagulants, antiaggregants, fibrinolytics, side effects of mineralocorticosteroids, estrogens, other NSAIDs; enhances the hypoglycemic effect of derivatives of sulfonylureas, enhances the hypoglycemic action of insulin and oral hypoglycemic drugs.

Against the background of the use of potassium-sparing diuretics, the risk of hyperkalemia increases. Sharing with paracetamol increases the risk of developing 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, gold preparations increase the nephrotoxicity of indomethacin.

Cefamandol, cefoperazone, cefotetan, valproic acid, plikamycin - increase the risk of hypoprothrombinemia and the risk of bleeding.

Increases the toxic effect of zidovudine.

Myelotoxic drugs increase the manifestation of hematotoxicity of the drug.

In newborns, the risk of toxic effects of aminoglycosides increases.

Special instructions:

During treatment, it is necessary to monitor the picture of peripheral blood and the functional state of the liver and kidneys.

If it is necessary to determine 17-ketosteroids, the drug should be discontinued 48 hours before the test.

Effect on the ability to drive transp. cf. and fur:

During the treatment period it is necessary to refrain from driving motor vehicles and practicing potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Suppositories rectal, 50 mg and 100 mg.

Packaging:

5 pieces are placed in a contour mesh package made of a polyvinyl chloride film.

Two contour mesh packages together with the instruction for use are placed in a pack of cardboard.

Storage conditions:

In a dry place, protected from light, out of reach of children, at a temperature not exceeding 25 ° C.

Shelf life:

2 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:P N001072 / 03

Date of registration:08.12.2008 / 07.09.2009

Expiration Date:Unlimited

The owner of the registration certificate:BIOSINTEZ, PAO BIOSINTEZ, PAO Russia

Manufacturer: & nbsp

BIOSINTEZ, PAO Russia

Representation: & nbspBIOSINTEZ JSC BIOSINTEZ JSC Russia

Information update date: & nbsp31.10.2017

Illustrated instructions

Instructions

Indomethacin (Indometacin )