Indotril

Indotril has anti-inflammatory and antirheumatic activity.

Indications Indotril

It is used for the following disorders:

• acute arthritis of various etiologies (this also includes acute gout attacks), except for infectious ones;
• chronic arthritis, especially in rheumatic diseases, Bechterew's disease and others;
• arthrosis, spondyloarthritis or spondyloarthrosis;
• extra-articular rheumatic pathologies affecting soft tissues (myositis or bursitis);
• inflammation or painful swelling after surgeries and injuries;
• neuralgia or myalgia;
• diffuse inflammatory diseases affecting connective tissues;
• thrombophlebitis.

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Release form

The substance is released in tablet form, in the amount of 10 pieces per package. 1, 3 or 6 packages per box.

Pharmacodynamics

A complex medicine whose activity is provided by the action of its components - thiotriazoline and indomethacin. The first enhances the analgesic and anti-inflammatory effect of indomethacin, and also eliminates its negative effects.

The medicinal effect of thiotriazoline leads to the development of membrane-stabilizing, anti-ischemic, immunomodulatory and antioxidant activity. The substance prevents the destruction of hepatocytes, reduces the severity of fat infiltration, as well as the spread of centrilobular liver necrosis; at the same time, it helps to produce reparative restoration of hepatocytes and stabilizes their metabolism of carbohydrates, proteins with lipids and pigments. Increases the rate of binding and secretion of bile, and in addition, stabilizes its chemical structure.

The drug causes the development of a pronounced slowing effect on the activity of COX-1 and 2, due to which the biosynthesis of PG (prostaglandins with thromboxane) decreases. By significantly reducing inflammatory exudation, the drug helps improve the state of microcirculation, and at the same time stimulates the activity of the antioxidant system and slows down lipid peroxidation in inflammation zones.

Increases the sensitivity limit to pain stimuli, suppressing the binding of PG, which provokes hypersensitivity of nociceptors to mechanical and chemical stimuli (development of hyperalgesia). Reduces joint pain (during movement and at rest), reduces swelling and stiffness in the morning and helps increase the range of motion.

The drug has antipyretic properties, which also occurs due to the disorder of PG binding (mainly PG E1) and the weakening of their pyrogenic effect relative to the thermoregulatory center.

Membrane-stabilizing, antioxidant, and anti-ischemic activity are provided by the chondroprotective effect. Indotrile can limit chondrocyte destruction, as well as the replacement of chondrocytes with connective tissues.

The drug has a fibrinolytic effect, can slow down platelet aggregation and leads to the development of a moderate anticoagulant effect.

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Pharmacokinetics

The drug is complex, so its pharmacokinetic characteristics correspond to the parameters of its elements. After taking the substance orally, blood indicators Cmax are noted after 1-2 hours.

Intraplasmic protein synthesis accounts for 90-98%. Metabolic processes develop inside the liver.

Most of the drug is excreted in urine (60-75%), and the remainder is excreted in feces. The half-life ranges from 2.6 to 11.2 hours (average 5.8 hours). Most of the drug is synthesized with protein within the plasma.

The relative bioavailability values of the thiotriazoline component are 64.5%, the half-absorption period is 0.28 hours, and the half-life is 1.3 hours; plasma Cmax values are achieved after 1.18 hours; protein synthesis is 10%.

The drug does not affect gastric pH values, and excretion occurs mainly through the kidneys. It does not affect the secretion of indomethacin.

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Dosing and administration

Teenagers from 14 years of age and adults should take 1 tablet of LS after meals, 3 times a day (equivalent to 30-45 mg of indomethacin). If the desired result cannot be achieved with this dose, it is increased to 2 tablets 2-3 times a day (for several days, until the acute manifestations of the disease are eliminated).

To eliminate acute gout attacks, the medicine is used in a dose of 2 tablets 3-4 times a day. After receiving a clinical result, the therapy continues for another 1 month (taking 2 tablets 3 times a day after eating). A repeated treatment cycle can be carried out after 3-4 months.

With prolonged use of the drug, its dosage can be a maximum of 75 mg of the substance.

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Use Indotril during pregnancy

The medication should not be used during breastfeeding or pregnancy.

Contraindications

Main contraindications:

• severe individual intolerance to indomethacin, aspirin or other NSAIDs (history includes mentions of urticaria, bronchospasms or runny nose caused by the use of aspirin or other NSAIDs);
• mental pathologies in the acute phase (schizophrenia, as well as epilepsy);
• aggravated ulcers in the gastrointestinal tract, enterocolitis or ulcerative colitis, as well as recurrent gastritis;
• severe liver, heart or kidney failure, as well as pancreatitis;
• BA;
• elevated blood pressure of a malignant nature.

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Side effects Indotril

After prolonged use of the drug, although the effective dose of indomethacin inside it is reduced, and its toxic effect is blocked by the action of thiotriazoline, patients may experience negative symptoms depending on personal sensitivity, duration of the therapy cycle and dosage size:

• Gastrointestinal tract lesions: nausea, diarrhea, epigastric pain, loss of appetite and vomiting; sometimes constipation occurs. Ulcerogenic effects and bleeding inside the gastrointestinal tract may occasionally develop;
• CNS disorders: long-term use of the drug may lead to dizziness, decreased visual acuity, headaches, a feeling of malaise or drowsiness, problems with concentration. In addition, depression, diplopia, mental disorders, Parkinsonism, muscle weakness and paresthesia sometimes develop;
• signs of allergy: rashes, itching, and also dermatitis and urticaria;
• Other: isolated disorders of the kidneys (hematuria or proliferative glomerulonephritis) and liver (jaundice or hepatitis and increased blood levels of bilirubin and liver transaminases), leuko- or neutropenia (may reach bone marrow suppression) occur. Disorders of carbohydrate metabolism, cardiac arrhythmia and edema associated with water and electrolyte retention are also noted.

Overdose

In case of poisoning with Indotril, the following symptoms occur: vomiting, feeling of disorientation, severe headaches, nausea, memory disorder and dizziness. In severe cases, convulsions or paresthesias appear and numbness of the extremities occurs.

When eliminating disorders, it is necessary to quickly remove the drug from the body by gastric lavage, and then perform the required symptomatic procedures. Hemodialysis will be ineffective in this case.

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Interactions with other drugs

Different drug combinations may cause different manifestations:

• phenytoin, digoxin or lithium agents - an increase in plasma levels of these drugs is possible;
• antihypertensive drugs, diuretics and β-blockers - the activity of these drugs may be reduced;
• potassium-sparing diuretics – development of hyperkalemia;
• GCS, other NSAIDs, and colchicine – increase the likelihood of developing negative symptoms in the gastrointestinal tract;
• cyclosporine and gold drugs - increased toxic activity in relation to the kidneys;
• aspirin or other salicylates - increased likelihood of side effects;
• hypoglycemic drugs - hyper- or hypoglycemia may occur. With such drug combinations, it is necessary to monitor blood glucose levels;
• methotrexate - during the 24-hour period before and after taking the drug, the level of methotrexate may increase and its toxicity may be potentiated;
• anticoagulants – it is necessary to constantly monitor the blood clotting function, because in this case there is a potentiation of the effect and an increase in the likelihood of hemophilia.

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Storage conditions

Indotril should be stored in a dark, dry place, out of the reach of children. Temperature range – within 15-25°C.

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Shelf life

Indotril can be used within a 2-year period from the date of manufacture of the therapeutic drug.

Application for children

Indotril is not used in pediatrics (under 14 years of age).

Analogues

The analogs of the drug are the medications Indomethacin, Ketorol, Aertal with Ketorolac, as well as Blokium B12 and Ketanov.