Biosynthesis instructions for use. Ointment "Indomethacin-Biosynthesis": instructions for use, description and reviews. Interaction with other medicinal products

10 pieces. - contour cell packaging (2) - cardboard packs.
10 pieces. - contour cell packaging (3) - cardboard packs.
30 pcs. - polymer cans (1) - cardboard packs.
30 pcs. - plastic containers (1) - cardboard packs.

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 surgery 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 dysfunctions, 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, 60 mg is administered i / m 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, dyspnoea , 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, 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 in case of liver, kidney, gastrointestinal tract diseases in history, with dyspeptic symptoms at the time of use, arterial hypertension, heart failure, immediately after serious surgical interventions, with parkinsonism, epilepsy.

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

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

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 use 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.

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.

Registration number: LS-001918-300911
Tradename: Isoniazid
International non-proprietary name: isoniazid
Chemical name: isonicotinic acid hydrazide
Dosage form: pills

Composition for one tablet.
Active substance:
Isoniazid - 100mg - 200mg - 300mg
Excipients:
calcium stearate monohydrate - 1.1 mg - 2.2 mg - 3.3 mg
polysorbate-80 (tween-80) - 0.15 mg - 0.3 mg - 0.5 mg
crospovidone (Kollidon CL-M) - 1.1 mg - 2.2 mg - 3.3 mg
potato starch - a sufficient amount to obtain a tablet weighing
- 110 mg - 220 mg - 330 mg

Description: tablets of white or white color with a creamy shade, flat-cylindrical shape with a bevel. Tablets with a dosage of 200 mg and 300 mg, scored.

Pharmacotherapeutic group: anti-tuberculosis drug

ATX code:

Pharmacological properties

Anti-tuberculosis drug; acts bacteriostatically. It is a prodrug - mycobacterial catalase-peroxidase metabolizes isoniazid to an active metabolite, which, by binding to the enoyl (acyl-transferring protein) reductase of fatty acid synthase II, disrupts the conversion of delta 2-unsaturated fatty acids into mycolic acid. The latter is a branched chain fatty acid, which, when combined with arabinogalactan (polysaccharide), participates in the formation of components of the cell wall of Mycobacterium tuberculosis. Isoniazid is also an inhibitor of mycobacterial catalase-peroxidase, which reduces the protection of the microorganism against reactive oxygen species and hydrogen peroxide. Isoniazid is also active against a small number of strains of Mycobacterium kansasii (for infections caused by this pathogen, it is necessary to determine the sensitivity to isoniazid before starting treatment).

Pharmacokinetics

Isoniazid is rapidly and completely absorbed when taken orally, food reduces absorption and bioavailability. The bioavailability index is greatly influenced by the "first pass" effect through the liver. The period of maximum concentration is 1-2 hours, the maximum concentration after taking a single dose of 300 mg is 3-7 μg / ml. The connection with proteins is insignificant - up to 10%. The volume of distribution is 0.57-0.76 l / kg. It is well distributed throughout the body, penetrating into all tissues and fluids, including cerebrospinal, pleural, ascites; high concentrations are created in lung tissue, kidneys, liver, muscles, saliva and sputum. Penetrates through the placental barrier and into breast milk.
It is metabolized in the liver by acetylation to form inactive products. In the liver, it is acetylated by N-acetyltransferase with the formation of N-acetylisoniazide, which is then converted into isonicotinic acid and monoacetylhydrazine, which has a hepatotoxic effect by the formation of an active intermediate metabolite by the cytochrome P450 system during N-hydroxylation. The rate of acetylation is genetically determined; people with "slow" acetylation have little N-acetyltransferase. It is an inducer of the isoenzyme CYP2E1, the half-life for "fast acetylators" is 0.5-1.6 hours; for "slow" ones - 2-5 hours. In renal failure, the half-life can increase to 6.7 hours. The half-life for children aged 1.5 to 15 years is 2.3-4.9 hours, and in newborns - 7.8-19.8 hours (due to imperfect acetylation processes in newborns). Despite the fact that the half-life indicator varies significantly depending on the individual intensity of acetylation processes, the average half-life is 3 hours (600 mg ingestion) and 5.1 hours (900 mg). With repeated appointments, the half-life is shortened to 2-3 hours.
It is excreted mainly by the kidneys: within 24 hours, 75-95% of the drug is excreted, mainly in the form of inactive metabolites - N-acetylisoniazide and isonicotinic acid. At the same time, in "fast acetylators" the content of N-acetylisoniazid is 93%, and in "slow" ones - no more than 63%. Small amounts are excreted in faeces. The drug is removed from the blood during hemodialysis; 5-hour hemodialysis removes up to 73% of the drug from the blood.

Indications for use

Tuberculosis (any localization, in adults and children, treatment and prevention, as part of combination therapy).

Contraindications

Hypersensitivity, drug hepatitis and liver failure (against the background of previous treatment with isoniazid), liver disease in the acute stage, children under 3 years of age (for this dosage form).

Carefully

Alcoholism, liver failure, renal failure, seizures, age over 35 years, long-term use of other drugs, withdrawal of isoniazid therapy in history, peripheral neuropathy, HIV infection, decompensated diseases of the cardiovascular system (chronic heart failure, angina pectoris, arterial hypertension ), hypothyroidism, pregnancy (do not prescribe in a dose higher than 10 mg / kg).

Method of administration and dosage

Inside, after meals, 600-900 mg / day in 1-3 doses, the maximum single dose is 600 mg, the daily dose is 900 mg.
Children - 5-15 mg / kg / day, the frequency of administration is 1-2 times a day, the maximum dose is 500 mg / day.
For the purpose of prophylaxis - 5-10 mg / kg / day in 2 doses for 2 months.
During pregnancy and in severe pulmonary heart failure, severe atherosclerosis, coronary heart disease and arterial hypertension, doses of more than 10 mg / kg should not be prescribed.

Side effects

From the nervous system: headache, dizziness, paresthesia, numbness of the extremities, peripheral neuropathy; rarely - excessive fatigue or weakness, irritability, euphoria, insomnia, optic neuritis, polyneuritis, toxic psychosis, emotional lability, depression, convulsions, toxic neuropathy, memory impairment.
On the part of the cardiovascular system: palpitations, angina pectoris, increased blood pressure.
From the digestive system: nausea, vomiting, gastralgia; increased activity of alanine aminotransferase, asparagine aminotransferase, hyperbilirubinemia, bilirubinuria, jaundice; rarely - toxic hepatitis, including fatal ones.
From the side of the hematopoietic organs: agranulocytosis, hemolytic, sideroblastic or aplastic anemia, thrombocytopenia, eosinophilia.
Allergic reactions: skin rash (crustaceous, maculopapular, exfoliative, purpura), itching, fever, arthralgia, lymphadenopathy, vasculitis.
From the side of metabolism: hypovitaminosis B6, pellagra, hyperglycemia, metabolic acidosis, gynecomastia.
Others: very rarely - menorrhagia, a tendency to bleeding and hemorrhage.
If any of the side effects indicated in the instructions are aggravated, or any other side effects not indicated in the instructions are noted, you should immediately inform your doctor about it.

Overdose

Symptoms appear within 0.5-3 hours after ingestion: nausea, vomiting; dizziness, blurry speech, visual impairment, visual hallucinations. In case of severe overdose: respiratory distress syndrome, depression of the central nervous system quickly passing from stupor to coma, severe intractable convulsions, severe metabolic acidosis, acetonuria, hyperglycemia.
Treatment: in case of severe overdose (80-150 mg / kg), insufficient therapy leads to neurotoxicity with a fatal outcome. With adequate therapy, the prognosis is favorable.
In case of asymptomatic overdose: activated charcoal, gastric lavage. When taken in a dose of more than 80 mg / kg in the same dose, pyridoxine is injected intravenously, if the dose of isoniazid taken is unknown, then 5 g of pyridoxine is injected intravenously for adults, 80 mg / kg for children for 30-60 minutes.
With clinical manifestations: adequate ventilation, maintenance of the cardiovascular system, prevention of aspiration of gastric contents. If the dose of isoniazid taken is known, the same amount of pyridoxine is injected intravenously for 3-5 minutes. If the dose of isoniazid taken is unknown, then 5 g of pyridoxine is administered intravenously to adults, 80 mg / kg to children. If the seizures persist, the dose can be repeated. Rarely, it is necessary to prescribe a dose of more than 10 g. The maximum safe dose of pyridoxine in case of isoniazid overdose is unknown. If pyridoxine is ineffective, diazepam is prescribed.
It is necessary to control the content of electrolytes, urea, glucose and the partial pressure of gases in the blood. With the development of metabolic acidosis, sodium bicarbonate can increase hypercapnia (constant monitoring is required).
Dialysis is prescribed if convulsions and acidosis have not been stopped by pyridoxine, diazepam, and sodium bicarbonate.

Interaction with other medicinal products

When combined with paracetamol, hepato- and nephrotoxicity increases; isoniazid induces the cytochrome P450 system, resulting in an increase in the metabolism of paracetamol to toxic products.
Ethanol increases the hepatotoxicity of isoniazid and speeds up its metabolism.
Reduces the metabolism of theophylline, which can lead to an increase in its concentration in the blood.
Reduces metabolic transformations and increases blood concentration of alfentanil. Cycloserine and disulfiram increase the adverse central effects of isoniazid. Increases the hepatotoxicity of rifampicin.
The combination with pyridoxine reduces the risk of developing peripheral neuritis.
With caution, it should be combined with potentially neuro-, hepato- and nephrotoxic drugs because of the danger of increased side effects.
It enhances the effect of coumarin and indandione derivatives, benzodiazepines, carbamazepine, theophylline, since it reduces their metabolism due to the activation of cytochrome P450 isoenzymes. Glucocorticosteroids accelerate metabolism in the liver and reduce active concentrations in the blood.
Suppresses the metabolism of phenytoin, which leads to an increase in its concentration in the blood and an increase in the toxic effect (correction of the phenytoin dosage regimen may be required, especially in patients with slow acetylation of isoniazid); should be considered when prescribing as an anticonvulsant for isoniazid overdose.
Antacid drugs (especially aluminum-containing ones) slow down absorption and reduce the concentration of isoniazid in the blood (antacids should be taken no earlier than 1 hour after taking isoniazid).
When used simultaneously with enflurane, isoniazid can increase the formation of an inorganic fluoride metabolite, which has a nephrotoxic effect.
When taken together with rifampicin, it reduces the concentration of ketoconazole in the blood.
Increases the concentration of valproic acid in the blood (control of the concentration of valproic acid is necessary; correction of the dosage regimen may be required).

special instructions

In some cases, fatal drug-induced hepatitis develops during treatment, which may occur even after several months of use. The risk increases with age (the highest incidence in the 35-64 age group), especially with daily ethanol consumption. Therefore, it is necessary to monitor liver function monthly, for persons over 35 years of age, liver function is additionally examined before starting treatment. In addition to ethanol use, additional risk factors are chronic liver disease, parenteral drug use, and the postpartum period; under these circumstances, monitoring of liver function (laboratory and clinical) should be carried out more often. Patients should be informed about the need to report any manifestations of liver damage (unexplained anorexia, nausea, vomiting, dark urine, jaundice, rash, paresthesia of the hands and feet, weakness, fatigue or fever lasting more than 3 days, abdominal pain, especially in the right hypochondrium ). In these cases, isoniazid is discontinued immediately. Patients who have previously had isoniazid hepatitis are prescribed alternative anti-tuberculosis drugs. If it is necessary to resume therapy, it begins after the complete resolution of the clinical and laboratory signs of hepatitis, followed by constant monitoring of liver function. If there is any sign of relapse, isoniazid should be stopped immediately. In patients with acute liver disease, isoniazid prophylaxis should be postponed.
To slow the development of microbial resistance, they are prescribed in conjunction with other anti-tuberculosis drugs.
Due to the different metabolic rate before using isoniazid, it is advisable to determine the rate of its inactivation (by the dynamics of the content in the blood and urine). In "fast acetylators" isoniazid is used in higher doses.
At risk of developing peripheral neuritis (patients over 65 years of age, concomitant diabetes mellitus, pregnancy, chronic renal failure, alcoholism, vitamin B6 deficiency due to malnutrition, concomitant anticonvulsant therapy), it is recommended to prescribe 10-25 mg / day of pyridoxine.
During treatment, you should avoid eating cheese (especially Swiss or Cheshire), fish (especially tuna, sardinella, skipjack), since when they are used simultaneously with isoniazid, reactions may occur (skin flushing, itching, feeling hot or cold, palpitations, increased sweating, chills, headache, dizziness) associated with suppression of the activity of monoamine oxidase and diamine oxidase and leading to disruption of the metabolism of tyramine and histamine contained in fish and cheese.
It should be borne in mind that isoniazid can cause hyperglycemia with secondary glucosuria; copper reduction tests may be false positive; the drug does not affect enzyme tests for glucose.
Taking into account the possible side effects, during the period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions.

Release form
Tablets 100 mg, 200 mg, 300 mg.
50 or 100 tablets in orange glass jars or polymer jars.
10 tablets each in a blister strip made of polyvinyl chloride film and lacquered aluminum foil or in a blister-free contour packaging made of polyethylene-coated paper.
Each jar, 2, 5 or 10 contour cell or contour non-cell packs, together with instructions for use, are placed in a carton box.
100 contour cell or contour non-cell packs with an equal number of instructions for use are placed in cardboard boxes (for hospitals).

Storage conditions
In a dry, dark place at a temperature not exceeding 25 ° C.
Keep out of the reach of children.

Shelf life
5 years. Do not use after the expiration date printed on the package.

Indometacin-Biosynthes

Active substance

Indomethacin * (Indomethacinum)

ATX:

Pharmacological group

• NSAIDs - Acetic acid derivatives and related compounds

Indications of the drug

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. Febrile 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 (osteoarthritis deformans, 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.

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 GHG synthesis, increase the number 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

Systemic side effects

From the nervous system and sensory organs: headache, dizziness, vertigo, agitation, irritability, excessive fatigue, drowsiness, depression, peripheral neuropathy, taste disturbance, 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, edematous 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.

Precautionary measures

Particularly careful medical supervision is required when indicating 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.

The risk of cardiovascular complications. NSAIDs, incl. and indomethacin, may increase the risk of serious cardiovascular complications, incl. myocardial infarction and stroke, which can be fatal, especially with prolonged use. Patients with cardiovascular disease or cardiovascular risk factors are particularly at risk.

Risk of gastrointestinal complications. NSAIDs, incl. and indomethacin, increase the risk of serious gastrointestinal side effects, including bleeding, ulceration, and perforation of the stomach or intestines, which can be fatal, especially with prolonged use. These complications can occur at any time of application without predictive symptoms. Elderly patients are at a higher risk of serious gastrointestinal complications.

When indicating a history of allergic reactions to NSAIDs, they are used only in urgent cases.

During treatment, it is necessary to control the picture of peripheral blood and the functional state of the liver and kidneys. If it is necessary to determine 17-ketosteroids, the drug should be discontinued 48 hours before the study.

For eye drops: After removing the contact lenses, instillation is performed after 5 minutes. In the presence of infection or the threat of its development, local antibacterial treatment is simultaneously prescribed.

Avoid contact with eyes, mucous membranes and open wounds of cutaneous application forms.

During the period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions.

special instructions

For an acute attack of gout, fast-acting dosage forms are preferred.

Storage conditions of the drug

In a dry, dark place.

Keep out of the reach of children.

The last updated description by the manufacturer 02.08.2004

Filtered list

Active substance:

ATX

Pharmacological group

Composition and form of release

in a contour acheikova or non-celled packaging 10 pcs .; in a pack of cardboard 2 or 3 packages or in dark glass cans or polymer cans or plastic containers 30 pcs.; in a pack of cardboard 1 can or container.

in a contour acheikova package 5 pcs .; in a pack of cardboard 2 packages.

in aluminum tubes or cans of 30 and 40 g; in a pack of cardboard 1 tube or bank.

pharmachologic effect

Method of administration and dosage

Inside, rectally, externally.

Tablets - inside, during or after a meal, washed down with milk. Adults - in an initial dose of 25 mg 2-3 times a day, if necessary, the dose is increased to 50 mg 3 times a day, the maximum daily dose is 200 mg. When the effect is achieved, the course is 4 weeks in the same or reduced dose. With prolonged use, the maximum daily dose is 75 mg.

Suppositories - rectally, after emptying the intestines, as deep as possible into the rectum - 50 mg 1-3 times a day or 100 mg before bedtime, during a gout attack - up to 200 mg per day.

Ointment - externally, rub in a thin layer into painful areas of the body 2-3 times a day. For adults, the total amount of ointment squeezed out of the tube per day should not exceed 15 cm, for children over 14 years old - 7.5 cm.

Manufacturer

JSC "Biosintez", Russia.

Storage conditions of the drug Indomethacin-Biosynthesis

Keep out of the reach of children.

Shelf life of the drug Indomethacin-Biosynthesis

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

The main symptom of osteochondrosis in the acute stage is pronounced pain. At the beginning of the treatment of the disease, the symptoms do not disappear immediately; to eliminate it, it is necessary to use complex therapy with the use of drugs in different forms of release. For example, topical products, tablets and injections. It should be noted that a variety of medicated ointments and gels are relatively safe. They have no irreversible side effects. The most common agent used in the treatment of osteochondrosis is Indomethacin-Biosynthesis ointment. Instructions for use will be discussed in this article.

Description of the medicine

So, in more detail. The drug in the form of an ointment "Indomethacin-Biosynthesis" is included in the group of external anti-inflammatory drugs. Non-steroidal.

At the heart of the drug is such an active substance as indomethacin, which is a derivative of the acid subgroup. This also includes substances such as phenylbutazone, piroxicam, ibuprofen, acetylsalicylic acid.

The mechanism of action for all drugs belonging to the group of non-steroidal acid drugs is the same:

• The substance inhibits the formation of prostaglandins - substances similar to hormones that are produced in the body in large quantities in the presence of an inflammatory process.
• They make it possible to inhibit the adhesion of platelets in the blood.
• The drugs have an overwhelming effect on the processes of proliferation and exudation, the stages of the process of inflammation.

According to the instructions for use, the ointment "Indomethacin-Biosynthesis" allows you to weaken and eliminate painful sensations in the place to which it was applied. This is indeed the case.

Composition

The main active ingredient in the drug is indomethacin. In addition to it, the ointment contains some additional components, namely: beeswax, stearyl alcohol, lavender oil, silicon dioxide, anhydrous lanolin, petroleum jelly.

Local application of Indomethacin-Biosynthesis ointment does not result in absorption of active components into the systemic circulation. Thanks to this, the agent can be used for treatment for a long period of time without the occurrence of side effects on the body. This is confirmed by the instructions for use attached to the Indomethacin Biosynthesis ointment and customer reviews.

pharmachologic effect

What else do you need to know? The action of the external ointment with indomethacin:

1. It allows you to significantly reduce pain in the tissues of the joints and muscles, which occur in diseases of a rheumatic and non-rheumatic nature.
2. Eliminates joint stiffness that occurs in the morning.
3. Relieves joint pain during movement and at rest.
4. Promotes an increase in the range of motion along each axis of the joint.
5. Allows to reduce the permeability of the walls of small blood vessels and capillaries.
6. Significantly reduces tissue swelling caused by the inflammatory process.
7. Able to relieve pain on movement, spontaneous pain.

What are the indications for the Indomethacin-Biosynthesis ointment in the instructions for use? We will talk about this further.

Indications for use

Medicinal ointment containing indomethacin is used in the treatment of a number of diseases that affect muscle and articular structures. Let's dwell on this in more detail.

Ointment "Indomethacin-Biosynthesis" is indicated in orthopedics and traumatology, for example, in diseases of the musculoskeletal system with inflammatory or degenerative-dystrophic etymology. These cases include spondylitis, osteoarthritis, arthralgia, arthritis, osteochondrosis.

Judging by the reviews, the "Indomethacin-Biosynthesis" ointment should be used topically if there are inflammatory processes that have developed after traumatic injuries. For example, after bruises, sprains, dislocations.

In the field of neurology and vertebrology, this agent is used in the treatment of localized forms of inflammatory processes that occur in soft tissues. For example, myalgia, neuralgia, radiculitis, sciatica, lumbago.

Phlebologists recommend the use of external agents with indomethacin in the treatment of a disease such as superficial thrombophlebitis. Indeed, it helps. This is confirmed by the instructions for use for the "Indomethacin-Biosynthesis" ointment.

Osteochondrosis therapy using the drug

Osteochondrosis, like most diseases, is characterized by interrelated symptoms, manifested in the form of pain, inflammation and edema. The degenerative-dystrophic changes arising against the background of osteochondrosis can lead to the fact that there is an infringement of the nerve endings. An inflammatory process occurs, edema develops in the surrounding tissues, accompanied by severe pain. The result is partial or complete movement in the spine.

Treatment of such symptoms must be carried out with the help of such drugs, which simultaneously have an analgesic and anti-inflammatory effect. Moreover, they should be selected not only for external use, but also for internal use.

The most effective means in the fight against acute inflammation are non-steroidal agents. For local therapy, special gels and ointments are used. For example, Indomethacin-Biosynthesis ointment. Instructions for use, the price are of interest to many. By itself.

Medicinal ointment containing the substance indomethacin is a complex agent. In the fight against osteochondrosis, it eliminates the three main symptoms of the disease: pain, swelling, inflammation. In addition, when using external agents, there is a very low percentage of toxicity, as well as general effects on the body. The external application allows you to achieve a cumulative, prolonged effect.

Contraindications for use

The ointment is contraindicated for use in patients with a history of increased susceptibility to the components of the drug. And also to other non-steroidal drugs of the "aspirin triad".

In addition, it is not recommended to use the remedy for patients who have ulceration of the mucous membranes of the gastrointestinal tract, bleeding disorders, severe forms of liver disease, CVS, kidneys. This is confirmed by reviews and instructions for the "Indomethacin" ointment. The price will be discussed below. It is perfectly acceptable.

Also, do not prescribe a drug for external use "Indomethacin-Biosynthesis" to those patients who have damage to the integrity of the skin, various dermatitis, pustular infections, eczematous rashes. And that's not it. A drug containing indomethacin is contraindicated for diseases of the hip joints that have arisen against the background of degenerative changes.

Pregnant women, women during lactation are not recommended to use the product. Pediatricians allow children to be treated with the drug "Indomethacin-Biosynthesis", but only after six years.

Side effects arising from the use

An external ointment containing indomethacin is capable of provoking an irritation reaction on the skin. It can manifest itself in the form of itching, hyperemia, burning.

The use of the "Indomethacin-Biosynthesis" ointment by people suffering from allergies can provoke a systemic reaction. It manifests itself as extensive rashes, swelling in the area of ​​application, bronchospasm, laryngeal edema.

Price

The ointment is inexpensive. In any pharmacy chain, it can be purchased for 60-70 rubles. This is one of the reasons why the drug has gained such high popularity.

Mode of application

Next moment. It is necessary to apply the topical ointment "Indomethacin" locally. To the area that is damaged. For each procedure, you can apply only an amount of ointment that does not exceed a column of 15 centimeters long. When treating children, you should use a dose that is half that of an adult.

It is necessary to apply an ointment containing indomethacin twice or three times a day. If the treatment is carried out without the supervision of a doctor, on an outpatient basis, then the course of treatment with an external ointment should not last ten days. In the presence of medical indications, the course of treatment can be extended in accordance with the recommendation of a specialist.

However, in such a case, it is necessary to monitor blood parameters in a laboratory. The level of leukocytes and platelets should be kept under control. With prolonged use of a drug for external use - ointment "Indomethacin-Biosynthesis" - instructions for use, reviews indicate that it is also necessary to monitor the state of the liver and kidneys. If any side effects appear, the use of the ointment should be discontinued. So, we examined what the "Indomethacin" ointment helps from.

Drug analogs

There are similar drugs that also contain the main active ingredient indomethacin. The main direct analogue is the tool for external use "Indovazin". The drug is produced by a pharmaceutical company in Iceland. In addition to indomethacin, the analogue contains the substance troxerutin, due to which the drug has an angioprotective and venotonic effect.