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Tablets Indomethacin: instructions for use. Indomethacin instructions for use, contraindications, side effects, reviews Indomethacin tablets dosage

Pain management is an important part of treatment. various diseases. In many cases, it is a consequence of inflammatory processes that develop in any system of the body. Therefore, not just a symptomatic correction is required, but an impact on pathological mechanisms. This is served by the well-known non-steroidal anti-inflammatory drugs (NSAIDs), which include indomethacin. Detailed information about the drug is in the instructions, and every doctor knows the main points related to its use.

Properties

Indomethacin has been used in clinical practice for more than half a century, but to the present it has not lost its relevance, remaining one of the most powerful NSAIDs. Being a derivative of indoleacetic acid, the drug has all the properties characteristic of the group of anti-inflammatory drugs.

Action

The main effects of indomethacin are due to its influence on the synthesis of metabolites of arachidonic acid - prostaglandins. It is these substances that are responsible for the development of inflammation in various organs and tissues. By inhibiting the activity of the enzyme cyclooxygenase (COX), the drug has a pronounced analgesic effect. In the focus of inflammation, tissue permeability decreases, and, consequently, swelling. Indomethacin acts on the blood coagulation system, reducing platelet aggregation. Thus, the main therapeutic effects of the drug are as follows:

Anti-inflammatory.
Anesthetic.
Antiplatelet.

The most active inflammatory processes are suppressed in the musculoskeletal system, soft tissues And vascular system, which significantly expands the scope of the drug.

Distribution in the body

After oral administration, indomethacin is rapidly absorbed into digestive tract and has a high bioavailability (at least 90%). Already after 2 hours, its plasma concentration reaches its maximum level. The drug circulates in unchanged form and in the form of various metabolic products. Penetrates through biological barriers: blood-brain, placental, enters breast milk. It is metabolized in the liver and excreted by the kidneys (70%) and through the gastrointestinal tract (30%).

Application

The active anti-inflammatory effect allows indomethacin to be included in the treatment regimens for many diseases, but it can only be used as directed by a doctor. Recently, when new representatives appear in the NSAID group, the drug in question may fade into the background. This is largely determined by conflicting information regarding the safety of indomethacin. But it remains the standard for pain relief and anti-inflammatory effects against which all other drugs are compared.

Indications

The pronounced therapeutic effect allows us to recommend indomethacin as a drug for the treatment of inflammatory diseases accompanied by intense pain. It allows you to get a quick clinical improvement in rheumatic processes and acute gouty arthritis, being the benchmark for the treatment of such a pathology. The drug relieves pain well, reduces stiffness in the joints and reduces the biochemical indicators of inflammation in the blood. Indomethacin is considered a highly effective tool in the fight against. The range of application of the drug is quite wide and includes the following conditions:

Diseases of the musculoskeletal system (arthritis, osteoarthritis, myositis, tendinitis,).
Pain of various origins (traumatic, neurogenic, headache, dental, menstrual).
Vascular diseases (thrombophlebitis).
Open ductus arteriosus.
Diseases of the pelvic organs (adnexitis, cystitis, prostatitis).
ENT pathology (tonsillitis, pharyngitis, otitis).

Indomethacin is highly effective in many inflammatory diseases, as well as severe pain syndrome.

How to use

It is necessary to use the drug in accordance with medical recommendations and official instructions. The medicine is produced in various forms: injection solution, tablets, capsules, dragees, suppositories, and eye drops. Accordingly, a general and local effect on the focus of inflammation is expected.

Most often, indomethacin is used in tablets. At first, the doctor will prescribe a small dose, gradually increasing it as part of individual tolerance. Take the drug should be 2-3 times a day after eating, drinking plenty of water. The maximum daily dose corresponds to 8 tablets. The course of application depends on the disease: chronic processes require long-term treatment(up to 4 weeks or more).

An injection solution is used to eliminate acute inflammation and pain. It is administered intramuscularly in 1 ampoule 1-2 times a day. The maximum dose of the drug should not exceed 3 ampoules per day. And after 1-2 weeks of treatment, you should switch to taking pills or using suppositories.

Using indomethacin, the dosages indicated in the prescription should not be exceeded, since this is associated with an increased likelihood of side effects of the drug.

Side effects

Like any drug from the NSAID group, indomethacin is not without side effects. They are class-specific and dose-dependent, do not develop in all patients and not always. Despite its pronounced therapeutic effect, indomethacin has a rather mediocre level of safety. Its toxicity can sometimes exceed other drugs from this group. But mostly this is due to a violation of the dosage or course of administration.

Side effects of the drug leads to the following manifestations:

Gastroenterological: abdominal pain, nausea, vomiting, heartburn, diarrhea, liver disorders.
Neurological: headaches, dizziness, mood lability, depression, insomnia.
Cardiovascular: accelerated heartbeat, increased pressure, arrhythmia, edema.
Hematopoietic: anemia, thrombo- and leukopenia, increased eosinophils, agranulocytosis.
Renal: the appearance of protein in the urine (proteinuria) and blood (hematuria), nephrotic syndrome, insufficiency.
Metabolic: increase in blood glucose and potassium.
Allergic reactions.
Hearing, vision and taste disorders.
Individual hypersensitivity.

The most common will be violations of the gastrointestinal tract. When using indomethacin, there is a serious risk of so-called NSAID-gastropathy. This is due to the inhibition of the activity of not only type 2 COX, located in the focus of inflammation, but also COX-1, which is responsible for the formation of "protective" prostaglandins in the gastric mucosa. With prolonged use, the risk of cardiovascular accidents - heart attack and stroke has been proven.

When using indomethacin, the benefit-risk ratio should be adequately assessed. Along with a pronounced therapeutic effect, you can get serious health consequences.

Restrictions

Given the above features of indomethacin, it should be used with extreme caution. Each patient should undergo a comprehensive examination to ascertain comorbid conditions and other circumstances that may limit the use of the drug.

Contraindications

Any drug must be used within strictly defined limits of safe effects on the body. Knowing about the side effects of indomethacin, it is easy to assume in what situations its use will worsen the patient's condition and become dangerous. Such conditions include:

Aspirin intolerance combined with bronchial asthma and nasal polyps (the "aspirin" triad).
Erosive and ulcerative lesions of the stomach and intestines.
Bleeding.
Heart defects (tetralogy of Fallot, coarctation of the aorta).
Chronic insufficiency of the heart and kidneys.
Liver disease (cirrhosis).
Violations of the hematopoietic and coagulation systems.
Pregnancy and lactation.
Age up to 14 years.

In such cases, the drug should not be used, but it is better to replace it with a safer one or completely abandon the use of NSAIDs.

To protect the patient from undue risk when using indomethacin, all the features of his body must be taken into account.

Precautions

The drug should be taken under the supervision of the attending physician, and the patient should report any changes in his condition. This is especially true for the elderly and people with other diseases who take several drugs at the same time. It is necessary to periodically monitor the composition of blood cells (erythrocytes, leukocytes, platelets), liver and kidney function indicators, coagulogram, electrolytes. The instructions for use indicate that indomethacin reduces the effect of diuretics and antihypertensives (in particular, beta-blockers), increases the concentration of digoxin and methotrexate, enhances the effect of hypoglycemic agents and anticoagulants. The drug cannot be used in conjunction with other NSAIDs, and antitumor agents and cytostatics increase its own toxicity.

Thus, indomethacin is a drug with a powerful anti-inflammatory and analgesic effect, the use of which is not limited to diseases of the musculoskeletal system. But the emergence of more modern drugs with an improved safety profile is gradually pushing it to the reserve.

The composition of all dosage forms of the therapeutic agent includes as an active ingredient indomethacin (Indometacin ) in different mass parts: 25 mg for tablets and 50 mg or 100 mg for suppositories (candles), gel and ointment.

Additional ingredients of drugs may vary slightly depending on the manufacturer, which should also be taken into account by the doctor prescribing this or that drug to the patient.

Release form

The medicine Indomethacin is produced in the form of:

oral tablets No. 10-No. 300;
candles No. 6-No. 50;
gel 40 grams;
ointments of 10-40 grams.

pharmachologic effect

Antiaggregatory, analgesic, anti-inflammatory, antipyretic.

Pharmacodynamics and pharmacokinetics

The drug Indomethacin Sopharma; Berlin Hemi, Balkanpharma etc.) is a derivative indoacetic acid and refers to drugs of the NSAID group, which are characterized by their antipyretic , anti-inflammatory , antiaggregatory And painkillers action.

The effectiveness of this therapeutic agent is associated with its inhibitory (depressant) effect on COX (cyclooxygenase ), which leads to the suppression of metabolic transformations arachidonic acid and decreased synthesis. Also, one of the effects of the drug is inhibition aggregations .

Parenteral and oral use of Indomethacin reduces the severity pain syndrome , especially with regard to joint pain , both in a state of movement and at rest, reduces the manifestations of morning swelling of the joints and their stiffness, and also increases the range of motion. Anti-inflammatory action develops after 5-7 days of treatment.

External use of this drug helps to eliminate pain, reduce swelling and reduce erythema, as well as reduce morning articular stiffness and increase motor activity .

Indomethacin tablets, when taken orally, are rapidly absorbed from the digestive tract. Serum Cmax is noted after 120 minutes. After enterohepatic recirculation, further metabolic transformations take place in the liver. In plasma, the unchanged active ingredient and unbound metabolic products are determined - debenzoyl , demethyl , desmethyl-desbenzoyl metabolites. The average T1 / 2 lasts approximately 4.5 hours. Excretion of 60% of the drug, in the form of unchanged substance and metabolic products, is carried out by the kidneys and 33%, in the form of metabolites, by the intestine.

Rectal suppositories are characterized by rapid absorption in the rectum. Bioavailability with this route of administration of the drug is 80-90%. Approximately 90% of the active ingredient binds to whey proteins. T1 / 2 varies within 4-9 hours. Metabolic transformations take place in the liver. Approximately 70% of the drug is excreted by the kidneys, about 30% by the intestines.

Indications for use

Indications for the use of Indomethacin in the form of tablets and suppositories include:

articular syndrome (including painful manifestations, ankylosing spondylitis , );
various ;
pain syndrome in the spine;
myalgia ;
diffuse painful conditions of the connective tissue;
traumatic inflammatory processes in joints and soft tissues;
infectious and inflammatory processes noted with, and diseases of the upper respiratory tract (auxiliary therapy).

Gel and ointment Indomethacin is indicated for use in:

myalgia ;
traumatic inflammatory processes occurring in the joints and soft tissues;
articular syndrome (including pain symptoms) gout , rheumatoid arthritis , ankylosing spondylitis , osteoarthritis );
pain in the spine;
neuralgia .

Contraindications

Indomethacin tablets (Sopharma, Balkanpharma, etc.), as well as Indomethacin suppositories (Berlin Chemie, Sopharma, etc.), are contraindicated for use with:

Crohn's disease ;
liver failure or active;
hypersensitivity;
pregnancy;
breastfeeding;
acute or, in the past caused by taking NSAIDs;
confirmed hyperkalemia;
CRF (with CC less than 30 ml / min) or progressive;
recent coronary artery bypass grafting ;
blood clotting disorders;
congenital heart defects ;
hematopoietic disorders (including anemia And leukopenia );
under the age of 14 years.

Additionally, suppositories Indomethacin 50/100 (Berlin Chemie, Sopharma, etc.) are not allowed to be used for:

manifestations;
rectal bleeding ;
symptoms proctitis .

With caution, both dosage forms of the drug should be prescribed for:

ischemic heart disease ;
somatic diseases of a severe nature;
cerebrovascular disorders;
dyslipidemia;
hyperlipidemia;
mental disorders;
thrombocytopenia;
pathologies of peripheral arteries;
ulcerative lesions of the gastrointestinal tract in history;
long-term use of other NSAIDs;
CRF (with CC 30-60 ml / min);
hyperbilirubinemia ;
availability Helicobacter pylori ;
with accompanying portal hypertension ;
parallel use of anticoagulants (), oral glucocorticoids (), antiplatelet agents (,), SSRIs (,);
in old age.

Gel and ointment for topical use are contraindicated in:

skin damage in the area of application;
III trimester of pregnancy (in case of application of the drug to large areas of the body);
hypersensitivity ;
under the age of 1 year.

External dosage forms are prescribed with caution when:

any combination with nasal/paranasal sinuses and intolerance to NSAIDs ;
I and II trimester of pregnancy;
exacerbation peptic ulcer of the gastrointestinal tract ;
breastfeeding;
blood clotting disorders ;
up to 6 years old.

Side effects

Side effects when using tablets or suppositories

Digestive system:

nausea, vomiting;
gastrointestinal bleeding;
jaundice ;
discomfort or pain in the abdomen;
perforation of the gastrointestinal tract;
erosive and ulcerative lesions of the gastrointestinal tract ;
stomatitis ;
intestinal strictures;
bleeding from a diverticulum or sigmoid colon;

Candles Indomethacin, instructions for use

Candles Indomethacin ( Altfarm, Sopharma etc.) are intended for rectal (into the rectum) application. The procedure for the introduction of suppositories should be performed at bedtime after preliminary cleaning of the intestines. Candles Indomethacin ( Berlin Hemi, Biosynthesis etc.), it is necessary to try to enter into the rectum as deeply as possible, in order to better absorb the drug. Usually, in 24 hours, a 3-time administration of 50 mg suppositories or a single administration of 100 mg suppositories is prescribed. In case of severe pain syndrome (for example, an attack of gout), rectal daily use of 200 mg of the drug in suppositories is allowed (in addition to oral administration).

Gel and ointment Indomethacin, instructions for use

Gel and ointment Indomethacin ( Sopharma, Balkanpharma etc.) are intended for application and rubbing into skin located directly above the site of the painful area of the body, for which the gel or ointment Indomethacin ( Sopharma, Akrikhin etc.) apply a thin layer on intact and previously cleansed skin.

5% external agents are indicated to be applied at intervals of 3-4 times in 24 hours. Applications of 10% drugs should be carried out 2-3 times a day. Single and maximum dosages of the external forms of the drug are calculated based on the amount (in centimeters) of the squeezed out gel or ointment from the tube. Adult patients can use 4-5 cm of the extruded drug at a time, and a maximum of 15-20 cm per day. Children are shown to use half the dosage.

Overdose

Negative symptoms of an overdose of Indomethacin, most often observed with the use of oral or rectal dosage forms, are manifested by: nausea / vomiting, severe, memory impairment , . In particularly serious cases, limb numbness , convulsions .

The prescribed treatment should be consistent with the monitored adverse events.

Interaction

Combined use, drugs lithium and increases their serum concentrations, which can cause an increase in their toxicity .

Concurrently received ethanol-containing drugs, glucocorticoids , And corticotropin increase the possibility of gastrointestinal bleeding .

Co-administration with therapeutic agents, including, increases the risk nephrotoxicity .

Combinatorial treatment with and others hypoglycemic drugs enhances their effect.

Simultaneous use with indirect antiplatelet agents , anticoagulants And thrombolytics enhances their effects, which increases the possibility of developing bleeding .

Co-administered drugs gold and raise nephrotoxicity (most likely due to inhibition of synthesis in the kidneys

Indomethacin is an anti-inflammatory drug. Available in the form of a solution for injection, coated tablets and rectal suppositories.

Pharmacological action of Indomethacin

In accordance with the instructions for Indomethacin, the active ingredient in the drug of all forms of release is indomethacin.

Auxiliary substances in the composition of Indomethacin tablets are potato starch, cellactose, copovidone, calcium stearate, titanium dioxide, Eudragit L 100-55 or L 100, talc, dye, macrogol 6000.

The auxiliary components that make up the suppositories of Indomethacin are semi-synthetic glycerides and cetyl alcohol.

According to the instructions, Indomethacin belongs to the group of non-steroidal anti-inflammatory drugs. Indomethacin is widely used in gynecology and general practice.

The active substance of the drug contributes to the inhibition of the cyclooxygenase enzyme, due to which the synthesis of prostaglandins from arachidonic acid is inhibited.

The drug also has properties such as cupellation of oxidative phosphorylation, increased norepinephrine metabolism, and inhibition of catecholamine reuptake. When used, Indomethacin has a ganglioblocking effect.

The drug helps to slow down the biosynthesis of proteoglycan in cartilage in accordance with the concentrations observed in the patient, inhibits platelet aggregation.

When using tablets, solution and suppositories, Indomethacin eliminates pain, reduces erythema and edema.

In the treatment of rheumatic diseases, due to the analgesic and anti-inflammatory properties of Indomethacin, symptoms such as pain at rest and on movement, morning stiffness and joint swelling are alleviated.

When used, Indomethacin has an antipyretic effect that exceeds the effect of acetylsalicylic acid and phenylbutazone.

In gynecology, Indomethacin is used for diseases of the uterus and appendages.

As a rule, the anti-inflammatory effect is manifested by the end of the first week of treatment. With prolonged therapy, the drug has a desensitizing effect on the body.

When taken internally, Indomethacin is rapidly absorbed from the gastrointestinal tract. The maximum concentration of the drug in the blood occurs after 2 hours. Metabolized in the liver, excreted by the kidneys. The period of complete elimination of the drug from the body is 8-10 hours.

Indications for the use of Indomethacin

The drug is prescribed for the treatment of such diseases and conditions:

Degenerative and inflammatory diseases of the musculoskeletal system: psoriatic, juvenile, chronic rheumatoid arthritis, Personage-Turner disease (neuralgic amyotrophy), arthritis in Reiter's and Paget's disease, Bechterew's disease (ankylosing spondylitis), gouty arthritis, rheumatism;
Pain syndromes: dental and headache, pain during menstrual syndrome and inflammatory processes, sciatica, lumbago, neuralgia, pain after surgery and injuries, myalgia, tendinitis and bursitis;
Infectious inflammatory diseases of the ENT organs, accompanied by pain syndrome (as part of complex therapy): tonsillitis, pharyngitis, otitis media.

Indomethacin is also prescribed for the treatment of algomenorrhea, secondary hyperaldosteronism (Barter's syndrome), pericarditis (as symptomatic therapy) and inflammatory processes in the pelvis.

In gynecology, Indomethacin is used as a tocolytic and analgesic drug during childbirth, as well as in the complex treatment of painful menstruation, cystitis and adnexitis.

The drug is prescribed for febrile syndrome, including liver metastases of tumors, lymphogranulomatosis in case of therapeutic inefficiency of paracetamol and acetylsalicylic acid.

Method of application and dosage

Indomethacin tablets should be taken orally during or after a meal with a small amount of milk. For adults, the drug is prescribed in an initial dose of 25 mg 2-3 times a day. With insufficient severity of the therapeutic effect, the dose is recommended to be increased to 50 mg 3 times a day. After the onset of the effect, treatment with the drug is continued for 4 weeks. With long-term therapy with Indomethacin tablets, the maximum daily dose should not exceed 75 mg.

For the relief of exacerbations of chronic diseases and for the treatment of acute conditions, an intramuscular injection of a solution of Indomethacin 60 mg 1-2 times a day is prescribed. The duration of the injection is 1-2 weeks, followed by a transition to oral administration or rectal administration of Indomethacin suppositories (1 suppository 2 times a day, for maintenance treatment - once at bedtime).

Rectally, the suppository is administered after a natural bowel movement deep into the rectum ½ suppository 1-3 times a day or 1 suppository at bedtime. At the onset of a gouty attack - 2 suppositories per day as an addition to the internal reception. The maximum daily dose of rectal suppositories should not exceed 2 pcs.

Contraindications to the use of indomethacin

Indomethacin is not prescribed to patients who have:

Hypersensitivity to components;
Peptic ulcer of the stomach and duodenum, colitis;
"Aspirin" triad;
Bleeding of various genesis;
Congenital heart disease;
Cirrhosis of the liver;
Bronchial asthma;
Diseases of the optic nerve;
swelling;
Chronic heart failure;
Arterial hypertension;
Liver failure, including chronic;
Blood clotting disorders.

Contraindications for rectal use of suppositories Indomethacin are rectal bleeding, hemorrhoids, proctitis, childhood up to 14 years old.

With caution, you should take the drug for thrombocytopenia, hyperbilirubinemia, epilepsy, depression, parkinsonism, in old age.

In gynecology, Indomethacin is not prescribed during pregnancy and lactation.

Side effects of indomethacin

When using suppositories and tablets, Indomethacin does not exclude such side effects like headaches, dizziness, nausea, vomiting, drowsiness, loss of appetite, spasms in the epigastric region.

Indomethacin can cause ulceration in the stomach and bleeding in the gastrointestinal tract.

Allergic reactions are also possible in the form of a rash, itching, urticaria, redness.

Overdose

When using the drug in quantities significantly exceeding those prescribed, vomiting, migraine, disorientation, dizziness may occur.

Terms and conditions of storage

According to the instructions for Indomethacin, the medicine should be stored in a cool and dark place. Shelf life - 2 years.

Indomethacin is a non-steroidal anti-inflammatory drug with analgesic and antipyretic effects, available in the form of tablets, rectal suppositories (candles), ointments, eye drops and injections.

The anti-inflammatory effect is observed by the end of the first week of indomethacin use. With prolonged therapy, it has a desensitizing effect on the body. When applied topically, it eliminates pain, reduces swelling and erythema.

Indomethacin is one of the most active drugs from the group of non-steroidal anti-inflammatory drugs. Due to the action of its main component in the human body, the biosynthesis of prostaglandins from arachidonic acid is inhibited, the inflammatory process decreases and the swelling of the affected tissues is removed.

Additionally, Indomethacin delays the production of active biological substances responsible for the development of pain and swelling in the area of the inflammatory process. The drug inhibits the aggregation of blood clots, increases the range of motion and reduces morning stiffness.

Indomethacin in the form of suppositories provides a reduction or cessation of pain in rheumatism (articular pain without movement or in movement, relieving numbness and immobility of the joints in the morning, reducing swelling of the joints, increasing the range of motion. With postoperative and post-traumatic inflammation, it helps relieve pain, reduce swelling).

Indications for the use of Indomethacin

For topical use:

inhibition of miosis during surgery;
prevention of the inflammatory process during operations on the anterior segment of the eye and for cataracts.

For outdoor use:

articular syndrome (including rheumatoid arthritis, arthrosis or osteoarthritis, ankylosing spondylitis, gout);
pain in the spine;
neuralgia;
myalgia;
traumatic inflammation of soft tissues and joints.

For systemic use:

diffuse connective tissue diseases;
dysmenorrhea;
neuralgia;
articular syndrome;
myalgia;
traumatic inflammation of the joints and soft tissues;
pain in the spine;
as an additional remedy for adnexitis, cystitis, prostatitis, as well as infectious and inflammatory diseases of the upper respiratory tract.

Instructions for use Indomethacin, dosage

The initial dosage of the drug usually begins with 0.025 g (25 mg) 2-3 times a day (adults), then, depending on tolerance, increase the daily dose to 100-150 mg per day (in 3-4 doses).

- Attacks in acute form - 0.05 g of the drug three times a day;
- Prevention of exacerbations - 0.025 g twice a day.

The maximum daily dose of Indomethacin is 200 mg.

When the desired therapeutic effect is achieved, treatment with Indomethacin is continued for 4 weeks at the same or reduced dose. With prolonged use, the daily dose should not exceed 75 mg.

Indomethacin injections

For the treatment of acute conditions or relief (removal) of exacerbation of a chronic process, 60 mg of indomethacin is administered intramuscularly 1-2 times a day.
The duration of intramuscular administration of the drug is 7-14 days. Further therapy is carried out with the use of tablets or suppositories.

Candles Indomethacin

Rectal suppositories are used for exacerbations of chronic processes or acute conditions. In this case, the standard dosage is 1 suppository (0.05 or 0.1 g) 2 times a day. It is necessary to ensure that the maximum daily dose does not exceed 0.2 g.

For maintenance treatment, suppositories are used at a dosage of 0.05-0.1 g once a night. Rectally, the suppository is inserted after a natural bowel movement deep into the rectum.

Ointment

Indomethacin ointment, according to the instructions for use, is applied to the affected area with a thin layer. For a day, you can not exceed the maximum dosage - up to 15 centimeters of the product squeezed out of the tube. For children, the maximum dose cannot exceed 7 centimeters.

Indomethacin is usually prescribed for a long time. Premature discontinuation may lead to the resumption of manifestations of the disease. The duration of the course of treatment depends on the severity of the disease and is determined individually by the attending physician.

Contraindications

hypersensitivity to active substance drug;
gastrointestinal ulcer in the acute phase;
"aspirin triad";
hematopoietic disorders;
severe violations of the liver and / or kidneys;
severe forms of CHF, arterial hypertension, pancreatitis;
3rd trimester of pregnancy;
children's age up to 14 years;
for rectal use: proctitis, recent bleeding from the rectum.

Side effects:

nausea, vomiting, gastropathy, heartburn, loss of appetite, liver dysfunction, abdominal pain. When used in large doses, long-term use - ulceration of the gastrointestinal mucosa.
dizziness, headache, agitation, insomnia, fatigue, irritability, depression, drowsiness, peripheral neuropathy.
tachyarrhythmia, arterial hypertension, heart failure.
tinnitus, hearing loss, diplopia, taste disturbance, corneal clouding, blurred vision, conjunctivitis.
nephrotic syndrome, impaired renal function, hematuria, proteinuria, necrosis of the renal papillae, interstitial nephritis, renal failure.
hematuria, bleeding, thrombocytopenia.
skin rash, urticaria, itching, angioedema, bronchospasm, rarely - Lyell's syndrome, anaphylactic shock, erythema nodosum.
autoimmune hemolytic anemia, aplastic anemia, aseptic meningitis (more often in patients with autoimmune diseases), edematous syndrome, increased sweating. Possible water and electrolyte retention, swelling.
itching, burning, dermatitis, feeling of heaviness and bleeding in the anorectal region, exacerbation of hemorrhoids.

Overdose

When using Indomethacin in amounts significantly exceeding those prescribed, vomiting, migraine, disorientation, dizziness may occur.

Use in children

Contraindicated in children and adolescents under the age of 14 years.

Use during pregnancy and lactation

Indomethacin is contraindicated in the 3rd trimester of pregnancy. In the 1st and 2nd trimesters of pregnancy, as well as during lactation (breastfeeding), the use is not recommended.

Analogues of the drug Indomethacin, list

Structural analogues for the active substance:

Indobene;
Indovis EU;
Indocollier;
Indotard;
Indocide;
Metindol.

It is important to understand that the instructions for use of Indomethacin, price and reviews do not apply to analogues and cannot be used for prescribing, replacing or other actions with medicinal preparations. The replacement of Indomethacin with analogues should be carried out by a specialist, after studying the medical history and tolerability of side effects.

Dosage form

Enteric coated tablet 25 mg

Composition

One tablet contains

active substance: indomethacin 25 mg,

Excipients:

composition of the tablet core: lactose monohydrate, wheat starch, microcrystalline cellulose (type 101), povidone K25, magnesium stearate, anhydrous colloidal silicon dioxide, talc.

shell composition: 30% dispersion of methacrylic acid copolymer: ethyl acrylate (1:1); 30% dispersion of methyl acrylate: methyl methacrylate: methacrylic acid copolymer; sodium hydroxide; polysorbate 80; pigment suspension - brown (talc, triethyl citrate, titanium dioxide (E171), iron oxide yellow (E172), iron oxide red (E172), propane-1,2 diol-alginate, potassium sorbate); triethyl citrate.

Description

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

Pharmacotherapeutic group

Anti-inflammatory and antirheumatic drugs. Non-steroidal anti-inflammatory drugs. Acetic acid derivatives. Indomethacin.

ATX code M01AB01

Pharmacological properties

Pharmacokinetics

Suction

After oral administration, up to 80-90% of the dose taken is absorbed in the small intestine, and to a lesser extent in the stomach. The maximum plasma level is determined after 1-2 hours.

Distribution

Distributed in all tissues and organs. Penetrates through the placental and blood-brain barrier. Penetrates through the synovial membrane into the joints, and its concentration in the synovial fluid is higher than in plasma. It binds to plasma proteins in 90-98% and has the ability to displace other drugs from protein binding and enhance their therapeutic effect when used simultaneously.

Metabolism

Metabolized in the liver by oxidation and conjugation.

breeding

The half-life of indomethacin varies from 2.6 to 11.2 hours, or on average it is 5.8 hours. It is excreted through the kidneys in 60-75%, 10-20% of which is unchanged, and the rest is excreted with bile and feces. It is allocated with breast milk.

Pharmacodynamics

Indomethacin Sopharma is a derivative of indoleacetic acid and belongs to the group of non-steroidal anti-inflammatory drugs. It has a pronounced anti-inflammatory effect, which significantly exceeds the effect of phenylbutazone and acetylsalicylic acid. Its analgesic activity is commensurate with the activity of metamizole. Has antipyretic action. Indomethacin has a powerful inhibitory effect on prostaglandin synthesis by inhibiting cyclooxygenase. In addition, it reduces both platelet aggregation and lipoxygenase activity in the inflamed area, respectively, and leukotrienes; also reduces the release of endogenous pyrogens, inactivates lysosomal enzymes, inhibits the activity of neutral proteases. Other effects may also be important, such as decupellation of oxidative phosphorylation and suppression of catecholamine reuptake, increased norepinephrine metabolism, and a known ganglioblocking effect.

Indications for use

Short-term symptomatic treatment:

Acute and chronic pain in inflammatory and degenerative diseases of the musculoskeletal system: rheumatoid arthritis; acute and in the acute stage chronic ankylosing spondylitis (Bekhterev's disease); gout attack and gouty arthritis; psoriatic arthritis; Reiter's disease;

Diseases of the periarticular tissues: tendinitis, bursitis, tendobursitis, tendovaginitis, injuries in athletes;

Dosage and administration

Tablets are taken orally after meals. The tablets are swallowed whole with a sufficient amount of water.

The frequency of side effects can be reduced by using the lowest possible effective dose for the shortest possible time to control symptoms.

Adults and teenagers over 18 years of age

The initial dose is 25-50 mg (1-2 tablets) 2-4 times a day.

With insufficient therapeutic effect, the dose is increased to 150 mg per day, divided into three doses. The maximum daily dose is 200 mg. With prolonged treatment, the daily dose should not exceed 75 mg.

To stop an acute gouty attack, an initial dose of 100 mg is prescribed, after which treatment is continued at a dose of 50 mg 3 times a day until the pain decreases.

There is an increased risk of side effects. The lowest effective dose is recommended for the shortest possible time. Patients should be monitored for possible bleeding from the gastrointestinal tract.

Children under 18 years of age

Side effects

Side effects are classified below by frequency. The frequency is defined as follows: very frequent (≥1/10), frequent (≥1/100 to<1/10), нечастые (≥1/1 000 до <1/100), редкие (≥1/10 000 до < 1/1 000), очень редкие (<1/10 000), с неизвестной частотой (на основании существующих сведений невозможно сделать оценку).

Very common (in more than 1 in 10 patients):

Gastrointestinal disorders. Possible peptic ulcer, perforation or bleeding from the gastrointestinal tract (sometimes fatal) mainly in elderly patients

Common: (with a probability of occurring in 1 to 10 patients in 100) include:

Dizziness, headache, drowsiness, depression, fatigue

Nausea, vomiting, diarrhea, dyspepsia, constipation, abdominal pain

Uncommon: (with a probability of occurrence in 1 to 10 patients per 1,000) include:

Leukopenia, thrombocytopenia, agranulocytosis, hemolytic anemia, aplastic anemia, disseminated intravascular coagulation (DIC)

Fluid retention, hyperglycemia, glucosuria, hyperkalemia

Malaise, anxiety, weakness, impaired concentration, including paresthesia, disorientation, insomnia, irritability, peripheral neuropathy, memory disorders, psychotic reactions, syncope, convulsions, muscle weakness, sensory disturbances, dysarthria, nervousness

Involuntary movements, confusion

Depersonalization, hallucinations, drowsiness, seizures, epilepsy

parkinsonism

Diplopia, blurred vision

Tachycardia, angina pectoris, palpitation, arrhythmia, edema

Arterial hypertension, hypotension

Flatulence, melena, hematemesis, ulcerative stomatitis, exacerbation of an existing ulcer, exacerbation of ulcerative colitis, Crohn's disease

Itching with or without rash, urticaria, petechiae, ecchymosis

Proteinuria, hematuria, interstitial nephritis

Acute renal failure, nephrotic syndrome

papillary necrosis

Rare: (with an incidence of 1 to 10 patients in 10,000) include:

Toxic hepatitis with or without jaundice

Very rare: (likely to occur in less than 1 in 10,000 patients) include:

Bronchospasm, asthma attacks, anaphylactic or anaphylactoid reactions

Hearing impairment, tinnitus

Worsening of heart failure associated with the use of NSAIDs

Clinical studies and epidemiological data show that the use of some NSAIDs (especially at high doses and with long-term use) can be associated with a slightly increased risk of arterial thrombotic events (eg, myocardial infarction or stroke)

Fulminant hepatitis

Exfoliative dermatitis, purpura, erythema nodosum, erythema multiforme, bullous eruptions, including Stevens-Johnson syndrome and toxic epidermal necrolysis.

Influence on the results of laboratory and instrumental studies: Increased levels of serum aminotransferases (ALT, AST), transient increase in bilirubin.

Contraindications

Hypersensitivity to the active 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, urticaria or rhinitis, polyps of the nasal mucosa

Past medical history of gastrointestinal bleeding or perforation due to NSAID use

Active or recurrent peptic ulcer/bleeding from the stomach and duodenum (two or more cases of proven ulcers or hemorrhage), ulcerative colitis and/or enterocolitis, Crohn's disease

Severe heart failure, congenital heart disease

Severe liver and kidney failure

Indomethacin is contraindicated for the treatment of perioperative pain during coronary artery bypass grafting (CABG)

Pregnancy and lactation

Children under 18 years of age

Hemophilia, hypocoagulation and other blood diseases.

Drug Interactions

Simultaneous use of indomethacin with:

Other NSAIDs, alcohol: The simultaneous use of indomethacin with other NSAIDs and alcohol increases the risk of side effects from the gastrointestinal tract.

Diflunisal: Increases plasma levels and decreases renal clearance of indomethacin. Fatal gastrointestinal hemorrhages may occur. This combination is not recommended.

Digoxin: Indomethacin can increase the plasma concentration of digoxin (reduces its excretion through the kidneys), which requires dose adjustment and monitoring of digoxin levels.

Lithium salts: Indomethacin prolongs and potentiates the action of lithium salts and increases lithium toxicity, which requires monitoring of lithium levels.

Immunosuppressants: The concomitant use of indomethacin and immunosuppressants such as methotrexate and cyclosporine leads to an increase in their toxicity.

Diuretics (diuretics): NSAIDs reduce the therapeutic efficacy of diuretics (due to a decrease in their tubular secretion). There may be an increased risk of hyperkalemia when combined with potassium-sparing diuretics and a decrease in renal function with an increased risk of acute renal failure when combined with thiazide diuretics (triamterene) Diuretics may increase the nephrotoxicity of indomethacin.

Antihypertensive agents: Indomethacin may weaken the antihypertensive effect of ACE inhibitors and beta-blockers when used simultaneously.

Corticosteroids: Increased risk of gastrointestinal ulceration and hemorrhage.

Anticoagulants: Increased risk of ulceration and hemorrhage due to suppression of platelet function and aggressive action on the mucosa of the gastrointestinal tract.

It is necessary to control bleeding time and prothrombin time. Indomethacin competes with coumarin anticoagulants at plasma protein binding sites, resulting in increased plasma concentrations. In cases of their simultaneous use, indomethacin is prescribed at the lowest possible dose and the possibility of prescribing protective agents is discussed.

Antiplatelet agents and selective serotonin reuptake inhibitors (SSRIs): Increased risk of gastrointestinal bleeding.

Quinolones: The combined use of quinolones and indomethacin may increase the risk of seizures in patients with or without a history of epilepsy or seizures.

Probenecid: Slows down the excretion and increases the toxicity of indomethacin.

Antidiabetic agents: Indomethacin does not change the therapeutic efficacy of oral antidiabetic agents and insulin, despite the fact that there are observations of hypo- or hyperglycemic action when they are used simultaneously.

special instructions

Side effects can be reduced by using the lowest possible effective dose of the drug for the shortest possible period of time and the following gastrointestinal and cardiovascular risk factors to control symptoms).

The simultaneous use of indomethacin with another drug from the NSAID group, including selective COX-2 inhibitors, should be avoided.

When using 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 are treated with beta-blockers, ACE inhibitors and potassium-sparing diuretics. In such patients, it is necessary to control the level of potassium in the blood serum.

It is used with extreme caution in patients with manifestations of hypersensitivity to food and drugs, in patients with allergic diseases - hay rhinitis, bronchial asthma, nasal polyposis.

Elderly patients (over 65 years old)

The use of NSAIDs in patients over 65 years of age is more likely to cause side effects, mainly gastrointestinal hemorrhage or perforation, sometimes fatal

Gastrointestinal hemorrhages, ulcerations and perforations

Gastrointestinal hemorrhages, ulcerations and perforations (sometimes fatal) have been observed with all NSAIDs at any time during treatment, with or without warning symptoms or evidence of prior serious gastrointestinal incidents.

The risk of side effects from the gastrointestinal tract is higher with the use of high doses of NSAIDs, in patients with a history of an ulcer, especially complicated by hemorrhage or perforation, and in elderly patients. In such patients, treatment with NSAIDs should be started at the lowest possible dose, taking into account the need for protective drugs (eg, misoprostol or proton pump inhibitors).

This approach is also recommended in cases of simultaneous use of low doses of acetylsalicylic acid or other drugs that increase the risk of gastrointestinal complications (corticosteroids, anticoagulants, antiplatelet agents, selective serotonin reuptake inhibitors).

Particular care is required in the treatment of patients with other diseases of the gastrointestinal tract (ulcerative colitis, Crohn's disease), which may be exacerbated by the use of NSAIDs.

An increased risk of gastrointestinal complications exists in patients who abuse alcohol or smoke, so they should be treated with extreme caution.

Patients with a history of gastrointestinal problems (especially elderly patients) should be advised to report unusual abdominal symptoms (especially gastrointestinal bleeding), especially at the start of treatment.

Special care is required when treating patients with drugs that may increase the risk of ulceration or bleeding (oral corticosteroids, anticoagulants such as warfarin, selective serotonin reuptake inhibitors, or antiplatelet agents such as acetylsalicylic acid

The use of the drug should be discontinued if gastrointestinal hemorrhages and ulcerations occur.

Disorders of the cardiovascular system and cerebral circulation

Appropriate monitoring and advice should be provided to patients with a history of hypertension and/or mild to moderate congestive heart failure, as there are reports of edema and fluid retention associated with NSAID treatment.

Clinical studies and epidemiological data show that the use of some NSAIDs (especially at high doses and with long-term use) can be associated with a slight increase in the risk of arterial thrombotic events (eg, myocardial infarction or stroke). There is not enough data to exclude such a risk with respect to indomethacin.

Patients with uncontrolled hypertension, congestive heart failure, established coronary artery disease, peripheral arterial disease and/or cerebrovascular disease should only be treated with indomethacin after a careful benefit/risk assessment.

Such a discussion is necessary before initiating long-term treatment in patients with risk factors for cardiovascular events (eg, hypertension, hyperlipidemia, diabetes mellitus, smoking).

Skin reactions

Serious skin reactions, including those with a fatal outcome, are observed very rarely with the use of NSAIDs and relate to cases of exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis. The highest risk of these reactions appears at the beginning of treatment (in the first month). The use of the drug should be discontinued at the first appearance of skin or other symptoms of hypersensitivity.

Renal reactions

Indomethacin is used with caution in patients with renal disease (creatinine clearance< 30 мл) из-за возможного почечного поражения.

Hematological reactions

It is necessary to prescribe with caution to patients with a history of impaired coagulation, since the drug inhibits the biosynthesis of prostaglandins and affects platelet function.

Hepatic reactions

Treatment with indomethacin, as with other drugs from the NSAID group, with prolonged use can cause changes in hepatic function, which requires periodic monitoring of liver enzymes.

Cases of infection

As a result of the existing anti-inflammatory action of the drug, it can mask the symptoms of acute inflammation, which requires that the presence of a bacterial infection be ruled out when prescribing it.

Mental reactions

It is used with caution in patients with mental disorders, depression, epilepsy, parkinsonism, as it can lead to a worsening of the underlying disease.

Excipients

Lactose is included as an excipient in the composition of the tablets. Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicine.

As an auxiliary substance, the composition of the tablets includes wheat starch. Wheat starch can contain only traces of gluten and is considered safe for people with celiac disease.

Fertility, pregnancy and breastfeeding

Pregnancy: The use of NSAIDs, like all other prostaglandin synthesis inhibitors, in the first months of pregnancy is associated with an increased risk of spontaneous abortion and malformations (renal lesions, cardiac malformations). The risk increases with the use of high doses for a long time.

The use of NSAIDs in the last 3 months of pregnancy can lead to prolongation of bleeding time in mother and child (antiplatelet effect, which can appear even at low doses) and suppression of uterine contractions, which leads to a slowdown or lengthening of labor. Indomethacin used in high doses in the last trimester of pregnancy can cause premature closure of the ductus arteriosus in the fetus, followed by persistent pulmonary hypertension. Indomethacin can cause kidney damage, which can progress to renal failure and oligohydramnios.

Breastfeeding: Due to excretion in breast milk, its use during breastfeeding is contraindicated or requires the cessation of breastfeeding during treatment.

Effect on fertility: in women of reproductive age, there is a risk of reversible suppression of fertility when using the drug.