Indomethacin suppositories 50mg, No. 10

• Articular syndrome (including rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, gout), back pain, neuralgia, myalgia, traumatic inflammation of soft tissues and joints, rheumatism, diffuse connective tissue diseases, dysmenorrhea.

• As an adjuvant in infectious and inflammatory diseases of the upper respiratory tract, adnexitis, prostatitis, cystitis.

• It is intended for symptomatic therapy, reducing pain and inflammation at the time of application, does not affect the progression of the disease.

For supportive treatment used rectally 50-100 mg 1 time / day at night.

Rectal suppositories from white to light yellow, torpedo-shaped, with a smooth surface, odorless; the cut surface must be smooth and uniform.

1 supp. indomethacin 50 mg

Excipients: solid fat (Witepsol N 15) - 1.3 g, solid fat (Witepsol W 35) - 0.65 g.

• Hypersensitivity to indomethacin,

• erosive and ulcerative lesions of the gastrointestinal tract in the acute phase,

• 'aspirin triad',

• hematopoietic disorders, blood clotting disorders,

• severe impairment of liver and / or kidney function,

• confirmed hyperkalemia,

• severe forms of chronic heart failure,

• congenital heart defects

• period after coronary artery bypass grafting,

• severe arterial hypertension,

• pancreatitis,

• pregnancy,

• breast-feeding;

• children up to age 14;

• for rectal use - proctitis, recent bleeding from the rectum.

• With caution IHD, cerebrovascular diseases, congestive heart failure, dyslipidemia, hyperlipidemia, diabetes mellitus, thrombocytopenia, peripheral arterial disease, arterial hypertension, smoking, CC 30-60 ml / min, cirrhosis of the liver with portal hypertension, hyperbilirubinemia, gastrointestinal ulceration , the presence of Helicobacter pylori 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 corticosteroids (including prednisolone), selective serotonin reuptake inhibitors (incl. citalopam, fluoxetine, paroxetine, sertraline); mental disorders, epilepsy, parkinsonism, depression, old age.

pharmachologic effect

NSAID, a derivative of indoleacetic acid. It has anti-inflammatory, analgesic and antipyretic effects. The mechanism of action is associated with inhibition of the COX enzyme, which leads to inhibition of the synthesis of prostaglandins from arachidonic acid.

Suppresses platelet aggregation.

When administered orally and parenterally, it helps to alleviate pain, especially joint pain at rest and during movement, to reduce morning stiffness and swelling of the joints, and to increase the range of motion. The anti-inflammatory effect develops by the end of the first week of treatment.

Pharmacokinetics

After oral administration, indomethacin is rapidly absorbed from the gastrointestinal tract. Cmax in plasma is reached after 2 hours. It is metabolized in the liver. Undergoes enterohepatic recirculation. Indomethacin is determined in blood plasma in the form of an unchanged substance and unbound metabolites - desmethyl, desbenzoyl, desmethyl-desbenzoyl.

When administered rectally, absorption is fast, bioavailability is 80-90%.

T1 / 2 is about 4.5 hours. It is excreted in the urine - 60% in the form of unchanged substances and metabolites, and with feces - 33%, mainly in the form of metabolites.

Side effect

From the digestive system: nausea, anorexia, vomiting, pain and discomfort in the abdomen, constipation or diarrhea, erosive and ulcerative lesions, bleeding and perforation of the gastrointestinal tract; rarely - intestinal strictures, stomatitis, gastritis, flatulence, bleeding from the sigmoid colon or from the diverticulum, jaundice, hepatitis.

From the nervous system: dizziness, headache, depression, tiredness; rarely - anxiety, fainting, drowsiness, seizures, peripheral neuropathy, muscle weakness, involuntary muscle movements, sleep disturbances, mental disorders (depersonalization, psychotic episodes), paresthesia, dysarthria, parkinsonism.

From the side of the cardiovascular system: edema, increased blood pressure, tachycardia, chest pain, arrhythmia, palpitation, arterial hypotension, congestive heart failure, hematuria.

Allergic reactions: rarely - itching, urticaria, angiitis, erythema nodosum, skin rash, exfoliative dermatitis, Stevens-Johnson syndrome, erythema multiforme, toxic epidermal necrolysis, hair loss, acute respiratory distress, a sharp drop in blood pressure, anaphylactic reactions, angioedema , bronchial asthma, pulmonary edema.

From the hematopoietic system: rarely - leukopenia, petechiae or ecchymosis, purpura, aplastic and hemolytic anemia, thrombocytopenia, DIC syndrome.

From the senses: rarely - impaired clarity of visual perception, diplopia, orbital and periorbital pain, tinnitus, hearing impairment, deafness.

From the urinary system: rarely - proteinuria, nephrotic syndrome, interstitial nephritis, renal impairment, renal failure.

From the side of metabolism: rarely - hyperglycemia, glucosuria, hyperkalemia.

Others: rarely - vaginal bleeding, hot flashes, increased sweating, nosebleeds, enlargement and tension of the mammary glands, gynecomastia.

Local reactions: at the place of intramuscular injection in some cases - the formation of infiltration, abscess; with rectal administration, irritation of the rectal mucosa, tenesmus, exacerbation of chronic colitis are possible.

For external use: itching, redness, rash at the site of application.

Application during pregnancy and lactation

Use during pregnancy and breastfeeding is contraindicated.

Indomethacin in small amounts is excreted in breast milk.

Application for violations of liver function

Contraindicated in severe liver dysfunction. Use with caution in liver diseases.

Application for impaired renal function

Contraindicated in severe renal impairment. Use with caution in kidney disease.

Application in children

Contraindicated in children under 14 years of age.

Use in elderly patients

Use with caution in elderly patients.

special instructions

It is used with caution in elderly patients, as well as with a history of liver, kidney, gastrointestinal tract diseases, with dyspeptic symptoms at the time of use, arterial hypertension, heart failure, immediately after serious surgical interventions, with parkinsonism, epilepsy.

If there is a history of allergic reactions to NSAIDs, they are used only in urgent cases.

During the period of treatment, systematic monitoring of the function of the liver and kidneys, and the picture of peripheral blood is necessary.

Influence on the ability to drive vehicles and mechanisms

During the period of treatment, one should refrain from potentially hazardous activities associated with the need for concentration and increased speed of psychomotor reactions.

Drug interactions

The simultaneous use of indomethacin with other drugs from the NSAID group, acetylsalicylic acid, GCS, alcohol, colchicine and corticotropin increases the risk of bleeding from the gastrointestinal tract.

Indomethacin reduces the effectiveness of diuretics, with the use of potassium-sparing diuretics, the risk of hyperkalemia increases; reduces the effectiveness of uricosuric and antihypertensive drugs; enhances the action of indirect anticoagulants, antiplatelet agents, thrombolytics (alteplase, streptokinase and urokinase); enhances the side effects of GCS, NSAIDs, estrogens, acetylsalicylic acid; enhances the hypoglycemic effect of sulfonylurea derivatives.

Concomitant use with paracetamol increases the risk of developing nephrotoxic effects.

Cyclosporine and gold preparations increase nephrotoxicity (apparently by suppressing the synthesis of prostaglandins in the kidneys).

Increases the plasma concentration of methotrexate, which can lead to increased toxicity.

With the simultaneous use of indomethacin with digoxin, an increase in the concentration of digoxin in the blood plasma and an increase in T1 / 2 of digoxin are possible.

Indomethacin in a dose of 50 mg 3 times / day increases the concentration of lithium in the blood plasma and reduces the clearance of lithium from the body in patients with mental illness. With the simultaneous use of indomethacin with lithium preparations, one should bear in mind the possibility of the appearance of symptoms of the toxic effect of lithium.

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

Potentiates the toxic effect of zidovudine.

Antacids and cholestyramine reduce the absorption of indomethacin.

Myelotoxic drugs increase the manifestation of the drug's hematotoxicity.

Concomitant use with quinolones may increase the risk of seizures in patients with or without a history of epilepsy or seizures.

Enhances the hypoglycemic effect of insulin and oral hypoglycemic drugs.