Indomethacin tablets: instructions for use. Ointment and tablets Indomethacin - instructions for use Indomethacin tablets for how long can you take

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

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

Release form

The medicine Indomethacin is produced in the form:

• oral tablets No. 10 to No. 300;
• candles No. 6-No. 50;
• gel 40 grams;
• ointment 10-40 grams.

pharmachologic effect

Antiaggregatory, analgesic, anti-inflammatory, antipyretic.

Pharmacodynamics and pharmacokinetics

Medicinal agent Indomethacin ( Sopharma; Berlin Chemie, Balkanfarma etc.) is a derivative indoleacetic acid and refers to drugs of the NSAID group, which are characterized by their antipyretic , anti-inflammatory , antiaggregatory and pain relievers action.

The effectiveness of this therapeutic agent is associated with its inhibitory (depressing) 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 administration of Indomethacin reduces the severity pain syndrome especially with regard to joint pain , both in a state of motion and at rest, reduces the manifestations of morning swelling of the joints and their stiffness, and also increases the range of motion. The anti-inflammatory effect develops after 5-7 days of treatment.

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

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

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

Indications for use

Indomethacin tablet and suppository indications include:

• articular syndrome (including painful manifestations, ankylosing spondylitis , );
• various ;
• pain 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 painful manifestations gout , rheumatoid arthritis , ankylosing spondylitis , osteoarthritis );
• back pain;
• neuralgia .

Contraindications

Indomethacin tablets (Sopharma, Balkanfarma, etc.), as well as Indomethacin suppositories (Berlin Chemi, Sopharma, etc.) are contraindicated for use when:

• Crohn's disease ;
• liver failure or active;
• hypersensitivity;
• pregnancy;
• breastfeeding;
• acute or, in the past, caused by the use of NSAIDs;
• confirmed hyperkalemia;
• Chronic renal failure (with CC less than 30 ml / min) or progressive;
• recently held coronary artery bypass grafting ;
• blood clotting disorders;
• congenital heart defects ;
• disorders of hematopoiesis (including anemia and leukopenia );
• under the age of 14.

Additionally, Indomethacin 50/100 suppositories (Berlin Chemi, Sopharma, etc.) are prohibited for use with:

• manifestations;
• rectal bleeding ;
• symptoms proctitis .

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

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

Topical gel and ointment are contraindicated for:

• damage to the skin in the area of ​​application;
• III trimester of pregnancy (in the case of applying 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 gastrointestinal ulcer ;
• breastfeeding;
• blood clotting disorders ;
• up to 6 years old.

Side effects

Side effects when using tablets or suppositories

Digestive system:

• nausea, vomiting;
• bleeding of the gastrointestinal tract;
• 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;

Suppositories Indomethacin, instructions for use

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

Gel and ointment Indomethacin, instructions for use

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

5% external agents are shown to be applied at intervals of 3-4 times every 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. For adult patients, one-time use of 4-5 cm of the squeezed out drug can be used, and the maximum per day is 15-20 cm. Children are shown the use of half the dosages.

Overdose

The negative symptoms of an overdose of Indomethacin, most often observed with the use of oral or rectal dosage forms, is manifested by: nausea / vomiting, severe, memory impairment ,. In especially serious cases, it was noted numbness of the limbs , convulsions .

The prescribed treatment must correspond to the negative manifestations being monitored.

Interaction

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

Parallel received ethanol-containing drugs, glucocorticoids , and corticotropin increase the likelihood of occurrence bleeding of the gastrointestinal tract .

Co-administration with medicinal products, 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 development bleeding .

Co-administered drugs gold and increase nephrotoxicity (most likely due to inhibition in the kidney synthesis

Anti-inflammatory drugs are used to relieve inflammation itself, have an analgesic effect, lower fever, and remove fever. Preparations of the NSAID group (non-steroidal) have their own advantage over others - the absence of undesirable properties of steroids. Indomethacin is a drug of this group, the appointment of which, in some situations, is inevitable.

This medicine can be produced in various forms (tablets, suppositories, ointments), there are conflicting opinions about its positive effects, as it gives strange kind of consequences.

The first thing worth noting is that this remedy cannot be used in any way without the recommendation and prescription of a doctor. The drug belongs to the group of NSAIDs, in addition, it is a manufacturer of indoleic acid. Its actions are aimed at coping with the inflammatory process, reducing pain at the site of the lesion. Indomethacin tablets block the work of inflammatory pathogens, and also reduce platelet aggregation. The active ingredient is indomethacin. In various forms of the drug, other excipients can be used.

Absorption is fast enough, the process of disintegration of the drug, its metabolism, is carried out in the liver.

This medicine is used to improve the condition of a patient who suffers from rheumatic pain syndromes. But it should be understood that without a doctor's prescription, it is not recommended to buy drugs of this group, since side effects are possible that contribute to the deterioration of health. There are reception options, both inside and outside. Depending on the diagnosis and personal tolerance, the doctor prescribes the best option, there are cases when the drug is used in several forms at once. The use of indomethacin can be prescribed for such ailments:

• Neuralgia;
• Pain in the spine and other joints;
• All sorts of traumatic inflammations.

These ailments cause serious pain, in such cases, a specialist may offer indomethacin ointment for quick external use. If the patient has had surgical interventions, then in order to relieve inflammation, such a drug can be used (topical application).

There are also a number of reasons why you will be prescribed a drug of the NSAID group:

• Inflammation associated with deformation of the joints, various kinds of arthritis about which we advise you to read in more detail;
• In cases of soft tissue damage, but only if it is rheumatic in nature;
• Prescribed in cases and complex therapy, but again, in order to relieve pain and inflammation itself.

Forms releasing, how to use the drug correctly

This medicine, as mentioned above, can be released in different forms, this is necessary so that the doctor can choose a high-quality course of treatment for the patient, directions for eliminating pain and inflammation in places of immediate localization. Prices for such a drug may vary, depending on whether you buy ointment or tablets. But it should be understood that if you have been prescribed pills, you do not need to replace them with something else.

Today, the following forms of drug release can be distinguished:

• Eye drops. They are rarely prescribed, but they do occur. The price for them is about 200-220 rubles;
• Indomethacin suppositories. They can be prescribed in cases of severe pain in the spine, with severe inflammation of soft tissues (under conditions of a traumatic nature), with pain in the joints;
• Tablets / dragees. The most common treatment option. It is in this form that the doctor prescribes this drug. But there is another opinion that it is better to use suppositories, or ointments, for a quick effect of eliminating pain and inflammation. It is better to use tablets in a complex method of treatment, then the effect will be 100%. Issue price -30-45 rubles;
• Capsules. Similar to tablets. They are prescribed, but it is better to do it in combination. They have an advantage over tablets - they dissolve quickly;
• Ointment. It is used in cases of severe pain in the joints and back. The ointment is applied to the very site of the lesion. The effect occurs after a minimum amount of time. It is worth using as directed by a doctor.

Speech about self-medication cannot even be such a drug. Therefore, the specialist himself will prescribe you a course of treatment, decide on the dosage. Instructions for the use of Indomethacin are attached to any form of release, but it is better to take the drug based on the prescribed instructions by the doctor:

1. Pills. Their number and duration of use depends on the severity of the disease. In general, an adult should take about 25 mg of such a substance, and then breaking it down into 2-3 doses. It is possible to increase the dosage up to 50 mg. After 4 weeks of treatment, with a positive outcome, the dosage begins to be reduced. In no case should you exceed 75 mg of the drug per day. Since the drug is quite serious, you should not drink it on an empty stomach, use it after meals;
2. The use of Indomethacin suppositories is prescribed for severe back pain. It should be understood that the drug enters the body through the rectum, so it is worth emptying the intestines before using the drug directly. Most often, an adult is prescribed only 100 mg of the drug, 1 candle. Possible options are two times 50 mg. If they are more acute, they can raise the dosage, up to 200 mg;
3. Injections. They will be used in the most serious forms of the disease. Assign 60 mg, injected intramuscularly. This course of treatment is about 2 weeks, while the injection itself is done 1 time in 1-2 days.

Rectal suppositories

Indomethacin rectal suppositories have been used in medicine for a long time, they have a number of properties necessary in the treatment of diseases of the spine and other joints:

1. Pain relieve;
2. Their action is aimed at reducing the inflammatory process;
3. They tend to relieve fever.

Positive reviews, candles received during their use in such diseases:

• All kinds of arthritis, osteoarthritis.
• Diseases of the joints;
• Neuralgia, various pains in the spine;
• During the treatment of soft tissues that have suffered as a result of various kinds of injuries.

The instructions for the candles can tell you how much this drug should be used, but without the recommendation of a doctor, this is not recommended. As practice shows, with severe acute manifestations of pain and inflammation, the patient can be prescribed 2 suppositories per day. The dosage of the substance is from 50 mg to 100 mg. It should be understood that it is not recommended to use more than 200 mg per day.

The instructions for the use of suppositories say that this drug has side effects and a number of contraindications. Side effects include:

• Vomiting, nausea (from the gastrointestinal tract);
• Constant drowsiness, dizziness, irritability, depression (from the nervous system);
• Shortness of breath is manifested, pain in the heart is possible (from the cardiovascular system);
• Back pain (from the genitourinary system);
• Allergies are possible.

Despite the fact that these candles have a good effect, and easily cope with their functions, there are a number of contraindications that should be taken into account so as not to provoke other diseases:

1. Immediate personal intolerance to the drug, hypersensitivity to the main substance;
2. All degrees of ulcer;
3. Liver and kidney problems;
4. Inflammation of the rectum, no matter what stage;
5. Hemorrhoids as well as inflammation of the colon.

The use of indomethacin in gynecology also takes place. This is due to the fact that almost all diseases of the female genital organs cause severe back pain, so doctors safely prescribe this drug.

Its direct function in this matter is to relieve pain. Due to the fact that the suppository of the drug is quickly absorbed, relief comes almost instantly. In addition, the drug relieves inflammation, which is also necessary for a number of ailments.

The use of indomethacin suppositories in gynecology is logical and possible with such diseases:

1. In gynecology, it is used for cystitis. In this situation, it is prescribed with a number of other tablets (antibiotics);
2. Suppositories with indomethacin in gynecology are relevant in the postoperative period in order to prevent the formation of adhesions;
3. Myoma of the uterus.

Instructions for the use of suppositories in gynecology should be written out by the doctor himself, since in such a situation self-medication is strictly prohibited. Most often, during treatment, the patient is not prescribed more than 1-2 suppositories per day. This amount of the drug allows you to maintain the correct therapeutic concentrate in the blood.

Ointment Indomethacin

What indomethacin ointment helps from has long been known. It is prescribed for joint problems, pain in the spine, and muscle pain. The composition of such a drug includes not only the main substance, but also auxiliary (dimexide, trolamine).

The biosynthesis ointment is applied directly to the sore spot. It not only has an analgesic effect, but also relieves inflammation. But it should be understood that its use should be carried out 2-3 times a day, no more. The ointment is absorbed through the pores of the skin and takes effect.

The main substance has a quick analgesic effect. But it should be understood that there are certain contraindications that should be taken into account before using the ointment:

• Immediate sensitivity to the drug.

It is important to understand that before you start using the ointment, make sure you are not taking other NSAIDs. The very same ointment should be applied exclusively to the site of damage. In case of contact with eyes, rinse immediately.

The use of indomethacin ointment is carried out according to a certain scheme: the daily rate of the ointment should not be more than 15 cm squeezed out of the tube. Apply only to sore areas, in a thin layer, 2-3 times a day.

The instruction for the ointment describes that during the application of such an ointment, side effects can be noticed:

• Inflammation at the sites of application of the ointment;
• Dryness and flaking;

Tablets how to replace indomethacin

Indomethacin tablets, instructions for use say that it should be used at 25 mg, 2-3 times a day, but only after a doctor's prescription. The dose may be increased, but this is done only after visiting a doctor. Up to 50 mg per day 3 times. The daily rate of such a drug should not be 200 mg.

Indomethacin tablets are used only as directed by a doctor. Tablets can also have side effects associated with disruption of various systems of the human body. Also, it should be noted that indomethacin biosynthesis is not always combined with other drugs. For example, it should not be used in conjunction with drugs of the NSAID group.

If you are not satisfied with the price, for this drug, or it is not in the pharmacy, you can be offered analogs to indomethacin: Metindol Retard, Indocollir and others.

It should be understood that absolutely all treatment with drugs of the NSAID group should be carried out only with the filing of the attending physician.

Excipients: lactose monohydrate 41.6 mg, potato starch 10 mg, microcrystalline cellulose 16 mg, 2.5 mg, magnesium stearate 0.9 mg.

The composition of the film shell: cellacephate 2.2 mg, polysorbate-80 0.72 mg, titanium dioxide 1.08 mg.

10 pieces. - contour cell packages (aluminum / PVC) (1) - cardboard packs.
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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, to increase the range of motion. The anti-inflammatory effect develops by the end of the first week of treatment.

When applied topically, it relieves pain, reduces edema and erythema.

When applied externally, in addition, it helps to reduce morning stiffness, increase the range of motion.

Pharmacokinetics

After oral administration, indomethacin is rapidly absorbed from the gastrointestinal tract. C max 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.

T 1/2 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.

Indications

For systemic use: 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.

For topical use: prevention of the inflammatory process during surgical interventions for cataracts and on the anterior segment of the eye, inhibition of miosis during surgery.

For external use: articular syndrome (including rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, gout), back pain, neuralgia, myalgia, traumatic inflammation of soft tissues and joints.

Contraindications

Hypersensitivity to indomethacin, erosive and ulcerative lesions of the gastrointestinal tract in the acute phase, "aspirin triad", hematopoiesis disorders, severe liver and / or kidney dysfunction, severe forms of chronic heart failure, arterial hypertension, pancreatitis, III trimester of pregnancy, children under 14 years; for rectal use: proctitis, recent bleeding from the rectum.

Dosage

Set individually, taking into account the severity of the course of the disease. For adults, when taken orally, the initial dose is 25 mg 2-3 times / day. If the clinical effect is insufficient, the dose is increased to 50 mg 3 times / day. Sustained-release dosage forms are used 1-2 times / day. Maximum daily dose: 200 mg.

When the effect is achieved, treatment is continued for 4 weeks at the same or reduced dose. With prolonged use, the daily dose should not exceed 75 mg. It is taken after meals.

For the treatment of acute conditions or relief of an exacerbation of a chronic process, intramuscular injection of 60 mg is administered 1-2 times / day. Duration of intramuscular injection is 7-14 days. Then indomethacin is administered orally or rectally at 50-100 mg 2 times / day, while maximum daily dose should not exceed 200 mg. For supportive treatment used rectally 50-100 mg 1 time / day at night.

For topical use in ophthalmology, the dose, frequency and duration of use are determined individually.

Topically applied 2 times / day.

Side effects

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

On the part of the cardiovascular system: edema, increased blood pressure, tachycardia, chest pain, arrhythmia, palpitation, arterial hypotension, congestive insufficiency, 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 edema, dyspnoema , 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: in 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.

Drug interactions

With the simultaneous use of indomethacin can reduce the effects of saluretics; enhance the effects of indirect anticoagulants.

With the simultaneous use of indomethacin and diflunisal, there is a risk of severe bleeding from the gastrointestinal tract.

With simultaneous use with probenecid, an increase in the concentration of indomethacin in the blood plasma is possible.

Indomethacin can reduce tubular secretion, which leads to increased toxicity.

With simultaneous use with NSAIDs, the toxicity of cyclosporine increases.

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 digoxin, an increase in the concentration of digoxin in the blood plasma and an increase in T 1/2 of digoxin are possible.

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

Indomethacin should not be used concomitantly with diflunisal.

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.

When applied topically, do not apply to the wound surface of the skin, and avoid contact with eyes or mucous membranes.

Influence on the ability to drive vehicles and control 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.

Pregnancy and lactation

Indomethacin is contraindicated in the third trimester of pregnancy. In the I and II trimesters of pregnancy, as well as during lactation (breastfeeding), use is not recommended.

Indomethacin in small amounts is excreted in breast milk.

Childhood use

Contraindicated in children under 14 years of age.

With impaired renal function

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

For violations of liver function

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

Use in the elderly

Use with caution in elderly patients.

Gross formula

Pharmacological group of the substance Indomethacin

Nosological classification (ICD-10)

CAS code

Characteristics of the substance Indomethacin

NSAID, a derivative of indoleacetic acid.

A white or slightly yellowish powder, odorless or almost odorless. Practically insoluble in water. Let's moderately dissolve in ethanol, chloroform, ether. Let's dissolve in solutions of alkalis.

Pharmacology

It inhibits cyclooxygenase (COX-1 and COX-2), reduces the synthesis of GHGs, which cause pain development in the inflammation focus, an increase in temperature and an increase in tissue permeability. It has an antiplatelet effect.

It causes a weakening or disappearance of pain syndrome 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 motion; in inflammatory processes that occur after operations and injuries, quickly relieves both spontaneous pain and pain on movement, reduces inflammatory edema at the site of the wound).

After oral administration of a single dose of 25 or 50 mg is rapidly absorbed, T max - about 2 hours; with rectal use, the absorption rate is higher. When taken orally, the bioavailability is 90-98%, with rectal administration, it is slightly less - 80-90%, which is probably due to the insufficient retention time of the suppository (less than 1 hour) to ensure complete absorption. Plasma protein binding - 90-98%. T 1/2 - 4-9 hours. With a daily intake of 25 or 50 mg of indomethacin three times a day, the equilibrium concentration is on average 1.4 times higher than the concentration after a single dose. Biotransformed mainly in the liver. In blood plasma is in the form of an unchanged substance and desmethyl-, desbenzoyl- and desmethyl-desbenzoylmetabolites, present in unconjugated form. It is excreted mainly by the kidneys - 70% (30% - unchanged) and the gastrointestinal tract - 30%. Passes through the BBB, placenta, enters breast milk. It is not removed by hemodialysis.

When instilling eye drops, it penetrates into the anterior chamber of the eye. After a single instillation, it is determined in the moisture of the anterior chamber for several hours.

Carcinogenicity, mutagenicity, effects on fertility

In an 81-week chronic toxicity study in rats, when administered orally at doses up to 1 mg / kg / day, no carcinogenic effect was found. In carcinogenicity studies in rats (study period - 73-110 weeks) and in mice (study period - 62-88 weeks) at doses up to 1.5 mg / kg / day, indomethacin caused neoplastic or hyperplastic changes.

Indomethacin mutagenicity was not detected in a number of bacterial tests in vitro(Ames test, test with E.Coli with / without metabolic activation) and in a series of tests in vivo including test for sex-linked recessive flying Drosophyla, micronucleus test in mice.

In reproduction studies, incl. in two generations, at a dose level of up to 0.5 mg / kg / day, indomethacin did not affect fertility in mice and rats.

Application of the substance Indomethacin

For systemic use (inside, intramuscularly, rectally)

Inflammatory and degenerative diseases of the musculoskeletal system: rheumatoid, psoriatic, juvenile chronic arthritis, arthritis in Paget's and Reiter's disease, neuralgic amyotrophy (Parsonage-Turner disease), ankylosing spondylitis (Bechterew's disease), gouty arthritis, rheumatism. Pain syndrome: headache (including with menstrual syndrome) and toothache, lumbago, sciatica, neuralgia, myalgia, after injuries and surgical interventions accompanied by inflammation, bursitis and tendonitis (most effective when localized in the shoulder and forearm). Algodismenorrhea, to preserve pregnancy, Barter's syndrome (secondary hyperaldosteronism), pericarditis (symptomatic treatment), childbirth (as an analgesic and tocolytic agent in preterm labor), inflammatory processes in the small pelvis, incl. adnexitis, non-closure of the botallov's duct. Infectious and inflammatory diseases of ENT organs with severe pain syndrome (as part of complex therapy): pharyngitis, tonsillitis, otitis media. Feverish syndrome (including with lymphogranulomatosis, other lymphomas and hepatic metastases of solid tumors) - in case of ineffectiveness of acetylsalicylic acid and paracetamol.

For topical use (when applied to the skin)

Traumatic inflammation of tendons, ligaments, muscles and joints (as a result of sprains, dislocations, after stress and bruises). Localized forms of soft tissue inflammation, incl. tendovaginitis, tendinitis, shoulder-arm syndrome, bursitis, myalgia; sciatica (sciatica, lumbago). Inflammatory and degenerative diseases of the musculoskeletal system (deforming osteoarthritis, rheumatoid arthritis, psoriatic arthritis, rheumatoid arthritis, periarthritis of the shoulder scapula, ankylosing spondylitis, osteochondrosis with radicular syndrome), with the exception of degenerative diseases of the hip joints.

In ophthalmology (eye drops): inhibition of miosis during cataract surgery; inflammatory process caused by surgery; prevention and treatment of cystic edema of the macular retina after surgical removal of cataracts; treatment and prevention of inflammatory processes of the eyeball; non-infectious conjunctivitis.

In dentistry(systemic and cutaneous application): arthritis and arthrosis of the temporomandibular joint, inflammatory diseases of the tissues of the oral cavity, myalgia, neuralgia, postoperative period.

Contraindications

Hypersensitivity.

For systemic use:"Aspirin" triad (a combination of bronchial asthma, recurrent polyposis of the nose and paranasal sinuses, as well as intolerance to acetylsalicylic acid and pyrazolone drugs), gastric ulcer and duodenal ulcer, ulcerative colitis, bleeding (including intracranial or from the gastrointestinal tract) congenital heart defects, in which a patent ductus arteriosus is necessary to maintain pulmonary or systemic circulation, incl. severe coarctation of the aorta, pulmonary atresia, tetrad of Fallot; violation of color vision, diseases of the optic nerve, bronchial asthma, cirrhosis of the liver with portal hypertension, chronic heart failure, edema, arterial hypertension, bleeding disorders (including hemophilia, prolonged bleeding time, tendency to bleeding), liver failure, chronic renal failure, hearing loss, pathology of the vestibular apparatus, deficiency of glucose-6-phosphate dehydrogenase; disorders of hematopoiesis (leukopenia and anemia), pregnancy, lactation, children (up to 14 years); for rectal use(optional): rectal bleeding, proctitis, hemorrhoids; for cutaneous use: pregnancy (III trimester - for application to large surfaces), violation of the integrity of the skin, children under 1 year of age.

Restrictions on use

For cutaneous use: pregnancy (I and II trimesters), lactation, children under 6 years of age.

In ophthalmology (eye drops): epithelial herpetic keratitis (including history), pregnancy, lactation, childhood.

Application during pregnancy and lactation

Teratogenic effects. Teratogenicity studies conducted in rats and mice using doses of 0.5; 1.0; 2.0 and 4.0 mg / kg / day showed that at a dose of 4 mg / kg / day there was no increase in the incidence of malformations compared with the control group, with the exception of delayed ossification in fetuses (considered as secondary to a decrease in average fruit weight). In other studies in mice, using higher doses (5-15 mg / kg / day), toxicity and mortality in females, increased resorption and fetal malformations were found. A comparative study in rodents using high doses of acetylsalicylic acid showed similar effects in females and their fetuses. However, reproductive studies in animals do not always predict effects in humans. There are no adequate and strictly controlled studies in pregnant women.

Non-teratogenic effects. Since the adverse effect of NSAIDs on the cardiovascular system of the fetus (premature closure of the ductus arteriosus) is known, use should be avoided during pregnancy (especially in later stages).

The effects of indomethacin and other drugs of this class on the human fetus in the third trimester of pregnancy include: intrauterine closure of the ductus arteriosus, tricuspid valve insufficiency and pulmonary hypertension; non-closure of the ductus arteriosus in the postnatal period, resistant to drug correction; degenerative changes in the myocardium, platelet disorders leading to bleeding, intracranial bleeding, renal dysfunction or failure, kidney damage / malformation that can lead to renal failure, oligohydramnios, gastrointestinal bleeding or perforation, increased risk of necrotizing enterocolitis.

In studies in rats and mice treated with indomethacin at doses of 4 mg / kg / day in the last 3 days of pregnancy, there was a decrease in body weight in females and a small number of deaths in females and fetuses. An increase in the incidence of neuronal necrosis in the diencephalon in live fetuses has been noted. At a dose of 2.0 mg / kg / day, there was no increase in the frequency of neuronal necrosis compared with the control group. Administration of 0.5 or 4.0 mg / kg / day in the first 3 days of life did not increase the frequency of neuronal necrosis.

Childbirth and delivery. Studies in rats have shown that NSAIDs, like other drugs that inhibit the synthesis of PG, increase the number of cases of obstructed labor, cause a delay in the onset of labor and delivery, and a decrease in the number of surviving pups.

Indomethacin passes into breast milk, so you should stop breastfeeding during treatment or avoid using indomethacin during breastfeeding.

Side effects of the substance Indomethacin

Systemic side effects

From the nervous system and sensory organs: headache, dizziness, vertigo, agitation, irritability, excessive fatigue, drowsiness, depression, peripheral neuropathy, taste disturbances, hearing loss, tinnitus, diplopia, blurred vision, corneal opacity, conjunctivitis.

On the part of the cardiovascular system and blood (hematopoiesis, hemostasis): development (worsening) of chronic heart failure, tachyarrhythmia, edema syndrome, increased blood pressure, bleeding (from the gastrointestinal tract, gingival, uterine, hemorrhoidal), anemia (including autoimmune hemolytic and aplastic), leukopenia, thrombocytopenia, eosinophilia, agranulocytosis, purpura.

From the digestive tract: NSAIDs-gastropathy, nausea, vomiting, abdominal pain, heartburn, loss of appetite, diarrhea, liver dysfunction (increased activity of hepatic transaminases, hyperbilirubinemia); with prolonged use in high doses - erosive and ulcerative lesions of the gastrointestinal tract.

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

Allergic reactions: pruritus, rash, urticaria, exfoliative dermatitis, erythema nodosum, anaphylactic shock, bronchospasm, angioedema, toxic epidermal necrolysis (Lyell's syndrome).

Others: hyperglycemia, glucosuria, hyperkalemia, photosensitivity; aseptic meningitis (more often in patients with autoimmune diseases), increased sweating; local reactions with rectal application: burning, itching of the skin, heaviness in the anorectal region, exacerbation of hemorrhoids.

When applied to the skin: allergic reactions; itching and flushing of the skin, rash at the site of application, dry skin, burning; in isolated cases - exacerbation of psoriasis; with prolonged use - systemic manifestations.

When instilled in the eye: allergic reactions; with prolonged use - corneal opacity, conjunctivitis, systemic side effects.

Interaction

Reduces the diuretic effect of potassium-sparing, thiazide and loop diuretics. Increases (mutually) the risk of side effects (primarily gastrointestinal lesions) of other NSAIDs. Increases the plasma concentration of digoxin, methotrexate and Li + preparations, which can lead to an increase in their toxicity. Concomitant use with paracetamol increases the risk of nephrotoxicity. Ethanol, colchicine, glucocorticoids, 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, fibrinolytics (alteplase, streptokinase and urokinase) and increases the risk of bleeding. Against the background of 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 mineral and glucocorticoids, estrogens. Cyclosporine and gold preparations increase nephrotoxicity (by suppressing the synthesis of PG in the kidneys). Cefamandol, cefoperazone, cefotetan, valproic acid - increase the incidence of hypoprothrombinemia and the risk of bleeding. Antacids and cholestyramine reduce the absorption of indomethacin. Increases the toxicity of zidovudine (by inhibiting metabolism), in newborns it increases the risk of developing the toxic effects of aminoglycosides (because it reduces renal clearance and increases blood concentration). Myelotoxic drugs increase the manifestations of hematotoxicity.

Overdose

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

Treatment: symptomatic therapy. Hemodialysis is ineffective.

Route of administration

Inside, in / m, rectally, cutaneous, conjunctivally.

Precautions for the substance Indomethacin

Particularly careful medical supervision is required when a history of allergic reactions to drugs of the "aspirin" series, "aspirin" triad, gastric ulcer and duodenal ulcer, as well as in violation of blood coagulation, hyperbilirubinemia, thrombocytopenia, epilepsy, parkinsonism, childhood and depression old age.

Against the background of degenerative and dystrophic lesions of the vertebrae, joints, with severe bruises, injuries, sprains, inflammation develops, tissue edema appears, and pains of varying intensity disturb. Indomethacin is an indiscriminate NSAID with high efficacy.

Tablets of a non-selective cyclooxygenase blocker are prescribed to relieve acute discomfort if negative symptoms need to be quickly eliminated. Indomethacin is active, but often causes negative reactions. The drug is prescribed in a short course with a powerful pain syndrome against the background of damage to cartilage, bone and muscle tissue.

Composition and form of release

The drug Indomethacin contains an active ingredient with the same name. One drug tablet contains 25 mg of active substance. Biconvex tablets with a diameter of 7 mm are enteric coated, light brown in color.

A cardboard box contains 1 or 3 blisters, the total number of units in a package is 30. Indomethacin can be purchased with a prescription.

Action on the body

The indoleacetic acid derivative blocks not only the synthesis of prostaglandins that cause pain, fever, inflammation, but also the protective enzyme cyclooxygenase - 1. Against the background of the active substance, tissue permeability decreases, the inflammatory process decreases, the pain of non-rheumatic and rheumatic origin in the lesion focus disappears, the temperature decreases.

Suppression of pathological changes has a positive effect on the mobility of the spine and joints. Patients note: the stiffness of the problem area disappears, swelling against the background of injury or inflammation, the joints less actively respond to changes in weather and loads of various kinds.

Indications for use

The drug for systemic use is prescribed for the defeat of various parts of the musculoskeletal system. It is important to remember about the indiscriminate effect of the active substance: uncontrolled intake increases the likelihood of unwanted reactions.

Indomethacin tablets help in the treatment of the following pathologies:

• arthritis: juvenile, rheumatic, psoriatic, gouty;
• inflammation of the elements of the musculoskeletal system in Reiter's and Paget's disease;
• rheumatism;
• neuralgic amyotrophy;
• pain syndrome in muscles and joints;
• the postoperative period in the surgical treatment of the spine, muscles, joints;
• tendinitis, bursitis;

On a note! Indomethacin is also prescribed for fever, pain, swelling against the background of infectious and inflammatory processes in the small pelvis, during childbirth, algodismenorrhea, fever, pericarditis. The drug quickly eliminates inflammation and negative sensations if paracetamol and acetylsalicylic acid do not show a noticeable effect. Indomethacin actively relieves toothache.

Contraindications

A non-selective non-steroidal anti-inflammatory agent is not prescribed:

• patients with peptic ulcer disease;
• with the aspirin triad;
• with bleeding in various parts of the body;
• against the background of congenital heart defects with impaired patency of the arterial duct;
• with damage to the optic nerve;
• when bronchial asthma is detected;
• under the age of 14;
• patients with glucose-6-phosphate dehydrogenase deficiency;
• with swelling and severe arterial hypertension;
• hearing impaired patients;
• with problems with the vestibular apparatus;
• patients with chronic renal failure;
• during pregnancy and breastfeeding;
• with hypersensitivity to indomethacin or other types of NSAIDs;
• revealed hepatitis, severe liver failure.

Instructions for use and daily dosage

Important points:

• tablets are taken after meals, without chewing;
• initial dosage - 25 mg 2 or 3 times a day;
• gradually increase the rate to 100 or 150 mg (be sure to receive a daily dosage for 3 or 4 doses);
• against the background of a gout attack, the rate is increased to 50 mg for each dose, in total - three times a day. After the negative symptoms subside, for the prevention of exacerbations, the patient takes 1 tablet of Indomethacin in the morning and in the evening;
• course duration - up to 30 days at a standard dosage or longer (as prescribed by a doctor) with a reduced rate (no more than 75 mg per day);
• the maximum rate for 1 day for the relief of acute pain is 200 mg of indomethacin. It is necessary to remember about the consequences for the gastrointestinal tract, liver, heart, central nervous system, to receive the drug in the minimum effective therapeutic dose.

Side effects

Non-selective blocking of the cyclooxygenase enzyme explains a wide range of undesirable reactions from various organs and systems. The severity of negative manifestations depends on compliance with the dosage, the individual characteristics of the patient, the state of the gastrointestinal tract, heart, blood vessels.

During therapy, systemic side effects are possible:

• nausea, heartburn, abdominal discomfort, gastropathy while taking NSAIDs, diarrhea, increased ALT and AST;
• high doses of indomethacin with prolonged use of tablets provoke the risk of bleeding and ulcerative lesions of the gastrointestinal tract;
• allergic reactions of varying severity;
• violation of the composition of the blood;
• impairment of smell, hearing and vision;
• depressive states, nervousness or apathy;
• excessive fatigue or overexcitement;
• conjunctivitis, corneal lesions;
• anemia, thrombocytopenic purpura;
• increased swelling, the development of arrhythmia, tachycardia, increased pressure;
• nephrotic syndrome, the development of interstitial nephritis, hematuria and proteinuria;
• blood loss against the background of severe damage to the mucous membrane of the uterus, gums, rectum.

Overdose

An excess of indomethacin negatively affects the body: signs of drug intoxication appear, the patient complains of disorientation, dizziness, and memory problems. Prolonged intake of high doses of the active substance can provoke paresthesias, numbness of the arms and legs, and convulsive syndrome.

To eliminate signs of an overdose, you need to rinse the stomach as soon as possible, give the patient a sorbent, consult a doctor about symptomatic therapy. It is important to exclude the risk of bleeding in the digestive tract: the patient is under the supervision of a specialist for several days.

Learn about the causes of the development of a deforming and treatment options for the disease.

The page is written about the symptoms of instability of the cervical spine and the treatment of the disease.

Drug interactions

The indiscriminate effect of a powerful non-steroidal drug requires careful use with some groups of drugs. If the patient is undergoing treatment for arterial hypertension, heart and vascular diseases, chronic kidney pathologies, then the doctor must indicate all the names from the list of prescribed drugs.

Interaction of Indomethacin with some names and types of drugs:

• increases the risk of negative reactions from others;
• reduces the diuretic effect of loop, thiazide and potassium-sparing diuretics;
• increases the activity of indirect anticoagulants, fibrinolytics, antiplatelet agents: the risk of bleeding increases many times;
• gold preparations and antibiotics of the cephalosporin group increase the nephrotoxic effect of indomethacin;
• the risk of bleeding in the gastrointestinal tract increases when combined with corticotropin, colchicine, ethanol, GCS;
• a decrease in the prothrombin index, the likelihood of bleeding - a consequence of the combination of indomethacin with Cefoperazone, valproic acid, Cefotetan, Cefamandol;
• the effect of the use of antihypertensive drugs and uricosuric formulations is lower than before the use of indiscriminate NSAIDs;
• absorption of indomethacin is reduced while taking cholestyramine and antacids;
• the combination with myelotoxic drugs adversely affects the composition of the blood.

Price

The price of Indomethacin tablets (pack # 30) is low - 70 rubles. The drug must be stored in its original packaging in a ventilated room, the optimum temperature is up to + 25 C. The non-steroidal drug should not be used uncontrollably by patients of any age: it is important to ensure that children do not accidentally find the tablets.

Indomethacin: analogues

Manufacturers offer several indomethacin-based names:

• Metindol.
• Indocollir.
• Metindol Retard.

With poor tolerance of the components of traditional NSAIDs, doctors recommend safer names of the new generation. Effective non-steroidal formulations of selective action:, Celebrex, Rofecoxib.