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

Excipients: lactose monohydrate 45.00 mg, wheat starch 35.00 mg, microcrystalline cellulose (type 101) 6.50 mg, povidone-K25 5.00 mg, silicon dioxide colloidal anhydrous 1.25 mg, talc 1.00 mg, magnesium stearate 1.25 mg;

shell composition: a solution of methacrylic acid and methyl methacrylate copolymer (1: 1) - eudragit L-12,5 (dry) 0.90 mg, a solution of methacrylic acid and methyl methacrylate copolymer (1: 2) - eudragit S-12,5 (dry) 1.83 mg, dibutyl phthalate 0.27 mg, diethyl phthalate 0.41 mg, macrogol-400 0.22 mg, macrogol-6000 0.41 mg, castor oil ordinary seed oil 0.15 mg, talc 3.29 mg, titanium dioxide 2.34 mg, dye brown Euroblend [dye sunset yellow (E 110) + dye brown chocolate HT (E 155)] 0.18 mg.

Description:

Round, biconvex tablets of orange-brown color. The view on the fracture is from white to light yellow.

Pharmacotherapeutic group:NSAIDs

ATX: & nbsp

C.01.E.B.03 Indomethacin

S.01.B.C.01 Indomethacin

M.02.A.A.23 Indomethacin

Pharmacodynamics:

The derivative of indoleacetic acid, has anti-inflammatory, analgesic, antipyretic and anti-aggregation effect. Suppresses the activity of proinflammatory factors, reduces platelet aggregation. Depressing cyclooxygenase I and II, disrupts 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. Eliminates or reduces pain syndrome of rheumatic and non-rheumatic nature (including pain in joints at rest and during movement, decrease in morning stiffness and swelling of joints, contributes to an increase in the volume of movements, in inflammatory processes that occur after operations and trauma, quickly facilitates both spontaneous pain, and pain during movement, reduces inflammatory swelling at the wound site).

Pharmacokinetics:

Bioavailability for oral administration is 80-90%. The maximum plasma concentration is achieved within 1-2 hours. It is absorbed through the mucosa of the small intestine, and to a much lesser extent through the gastric mucosa. It is distributed in all organs of tissues and tissues.Penetrates through the placental and blood-brain barrier. It penetrates through the synovial membrane into the joints, and the concentration of indomethacin in the synovial fluid rises. The connection with plasma proteins is 90-98%, the half-life is 2.6 and 11.2 hours. It is metabolized mainly in the liver, 10-20% of the drug is eliminated in an unchanged form, 70% is excreted by the kidneys, 30% through the gastrointestinal tract (GIT). It is not removed during dialysis. Excreted in breast milk.

Indications:

- Acute and chronic pain in inflammatory diseases of the musculoskeletal system: rheumatoid arthritis, juvenile chronic arthritis, ankylosing chronic spondylitis (Bechterew's disease), gouty arthritis, psoriatic arthritis, Reiter's disease;

- diseases of the periarticular tissues: tendinitis, bursitis, tendo bursitis, tendovaginitis;

- injury to athletes;

- discopathy, neuritis, plexitis, radiculoneuritis;

- dysmenorrhea.

Contraindications:

- Hypersensitivity to indomethacin or any of the excipients of the drug;

- hypersensitivity to acetylsalicylic acid or other non-steroidal anti-inflammatory drugs with a clinical manifestation of an asthmatic attack, hives or rhinitis;

- gastric ulcer and 12 duodenal ulcer, inflammatory bowel disease (ulcerative colitis, Crohn's disease), bleeding (including intracranial, from the gastrointestinal tract (GIT);

- Congenital heart defects (severe coarctation of the aorta, pulmonary atresia, heavy tetralogy of Fallot), period after coronary artery bypass grafting;

- severe heart failure;

- renal failure (creatinine clearance (CK) less than 30 ml / min);

- hepatic insufficiency, active liver disease;

- bleeding disorders (including hemophilia, prolonged bleeding, bleeding tendency);

- violation of hematopoiesis (leukopenia and anemia);

- confirmed hyperkalemia;

- pregnancy and breastfeeding;

- children's age (up to 14 years).

Carefully:

Ischemic heart disease, cerebrovascular disease, chronic heart failure, dyslipidaemia, hyperlipidemia, diabetes, thrombocytopenia, peripheral artery disease, hypertension, smoking, CC less than 60 ml / min, cirrhosis with portal hypertension, hyperbilirubinemia, ulcerative gastrointestinal lesion history, infection Helicobacter pylori, long-term use of NSAIDs, frequent alcohol consumption, severe somatic diseases, concomitant therapy with the following drugs: anticoagulants (incl. warfarin), antiaggregants (incl. acetylsalicylic acid, clopidogrel), oral glucocorticosteroids (incl. prednisolone), selective inhibitors of serotonin reuptake (including citalopa, fluoxetine, paroxetine, sertraline); mental disorders, epilepsy, parkinsonism, depression, elderly age.

Pregnancy and lactation:

Pregnancy

Indomethacin is not used during pregnancy.

Breast-feeding

Indomethacin excreted in breast milk. If it is necessary to treat the drug, breastfeeding should be discontinued.

Dosing and Administration:

Inside, after eating, squeezed with enough water.

Adults and children over 14 let: the initial dose is 25 mg 2-3 times a day. With insufficient therapeutic effect, the dose is increased to 50 mg 3 times a day. The maximum daily dose is 200 mg. With prolonged treatment, the daily dose should not exceed 75 mg.

Gout

For relief of an acute gouty attack, the initial dosage is 100 mg, after which the treatment is continued 50 mg 3 times a day until the pain disappears.

Side effects can be reduced by using the minimum effective dose for as short a period of time as possible.

Side effects:

From the digestive system: NSAID-gastropathy, abdominal pain, nausea, vomiting, heartburn, anorexia, diarrhea, bleeding, impaired liver function (increase in the blood of bilirubin, "liver" transaminases (ALT, ASAT)). With prolonged use in large doses - ulceration of the mucous membrane of the gastrointestinal tract, ulcerative stomatitis. Rarely toxic hepatitis with jaundice or without jaundice. Very rarely - fulminant hepatitis.

From the central nervous system: headache, dizziness, agitation, rarely - drowsiness, fatigue, peripheral neuropathy. Very rarely - sensitivity disorders, including paresthesia, a sense of disorientation, insomnia, irritability, depression, anxiety, memory disorder, psychotic reactions.

From the side of the cardiovascular system: rarely - development (aggravation) of CHF phenomena, tachyarrhythmia, there are reports of edematous syndrome, increased blood pressure.

From the sense organs: hearing loss, tinnitus, taste disorder, diplopia, blurred vision, corneal opacity, conjunctivitis.

From the urinary system: rarely - edema, very rarely - proteinuria, hematuria, interstitial nephritis, nephrotic syndrome, papillary necrosis.

From the hemopoietic system and the hemostasis system: bleeding (gastrointestinal, gingival, uterine, hemorrhoidal), thrombocytopenia, eosinophilia, agranulocytosis, thrombocytopenic purpura.

Allergic reactions: skin rash, itching, rarely - hives, angioedema, bronchospasm; in isolated cases - photosensitivity, Lyell's syndrome, erythema nodosum, Stevens-Johnson syndrome, anaphylactic shock.

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

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

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:

Simultaneous use of indomethacin with other drugs from the group of NSAIDs, acetylsalicylic acid, glucocorticosteroids, alcohol, colchicine and corticotropin increases the risk of bleeding in the gastrointestinal tract.

Indomethacin reduces the effectiveness of diuretics, against the background of the use of potassium-sparing diuretics, the risk of hyperkalemia increases; reduces the effectiveness of uricosuric and antihypertensive drugs (incl. β-blockers); strengthens the effect of indirect anticoagulants, antiplatelet agents, thrombolytic agents (alteplase, streptokinase and urokinase); increases the side effects of glucocorticosteroids, NSAIDs, estrogens, acetylsalicylic acid; enhances the hypoglycemic effect of sulfonylurea derivatives.

Sharing with paracetamol increases the risk of developing nephrotoxic effects.

Cyclosporine and gold preparations increase nephrotoxicity (apparently due to suppression of synthesis Pg in the kidneys).

Increases the concentration in the plasma of lithium, methotrexate and digoxin, which can lead to an increase in their toxicity.

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

Potentiates the toxic effect of zidovudine.

Antacids and colestramine reduce the absorption of indomethacin.

Myelotoxic drugs increase the manifestation of hematotoxicity of the drug.

Co-administration with quinolones may increase the threat of seizures in patients with or without anamnesis data on epilepsy or seizures.

Strengthens the hypoglycemic effect of insulin and oral hypoglycemic drugs.

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

Serious skin reactions, including those with a lethal outcome, very rarely observed with NSAIDs, relate to cases of exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis. The highest risk is at the beginning of treatment. The drug should be discontinued at the appearance of the first cutaneous or other signs of hypersensitivity.

The drug can mask the symptoms of acute inflammation, which requires the exclusion of bacterial infection when it is prescribed.

When taking drugs from the NSAID group, there is a risk of developing hyperkalemia, especially in patients over 65 years of age, patients with renal insufficiency, patients who take beta-blockers, ACE inhibitors and potassium-sparing diuretics. In such patients, serum potassium levels should be monitored.

In women of reproductive age, there is a risk of reversible suppression of fertility.

The drug contains lactose monohydrate as an auxiliary substance, which must be taken into account when appointing patients with lactase deficiency, galactosemia. syndrome of glucose / galactose malabsorption.Patients with glutenic enteropathy should take into account the presence of wheat starch in the formulation.

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

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

Form release / dosage:

Tablets coated with enteric coating, 25 mg.

Packaging:

For 30 tablets in a blister of colorless transparent PVC film / aluminum foil.

1 blister together with instructions for use are placed in a cardboard box.

45 blisters together with instructions for use are placed in a cardboard box (for hospitals).

Storage conditions:

In dry, the dark place at a temperature of no higher than 25 C.

XWound in a place inaccessible to children.

Shelf life:

5 years.

Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N011963 / 01

Date of registration:15.02.2011 / 25.11.2015

Expiration Date:Unlimited

The owner of the registration certificate:Sopharma, AOSopharma, AO Bulgaria

Manufacturer: & nbsp

SOPHARMA, AD Bulgaria

Representation: & nbspSOFARMA SA SOFARMA SA Bulgaria

Information update date: & nbsp31.10.2017

Illustrated instructions

Instructions

Indomethacin Sopharma (Indometacin Sopharma)