Indotril

Indotril has anti-inflammatory as well as antirheumatic activity.

Indications Indotrila

It is used for such violations:

• arthritis in acute form, having a diverse etiology (this also includes acute gouty attacks), except for infectious;
• arthritis of a chronic nature, especially for rheumatic diseases, ankylosing spondylitis and others;
• arthrosis, spondylitis or spondylarthrosis;
• extraarticular pathology affecting soft tissues of rheumatic nature (myositis or bursitis);
• inflammation or painful swelling after surgery and trauma;
• neuralgia or myalgia;
• diffuse inflammatory diseases affecting connective tissue;
• thrombophlebitis

[1], [2]

Release form

The release of the substance is made in tablet form, in the amount of 10 pieces inside the package. 1, 3 or 6 packs - in a box.

Pharmacodynamics

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 manifestations.

The drug effect of thiotriazolin 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 centrolobular hepatic necrosis; together with this, it helps to produce reparative restoration of hepatocytes and stabilizes their metabolism of carbohydrates, proteins with lipids and pigments. Increases the speed of binding and secretion of bile, and besides it stabilizes its chemical structure.

The drug leads to the development of a pronounced retarding effect on the activity of COX-1 and 2, thereby reducing the biosynthesis of PG (prostaglandins with thromboxane). By significantly reducing inflammatory exudation, the drug improves microcirculation, and at the same time stimulates the activity of the antioxidant system and slows down lipid peroxidation in the areas of inflammation.

Increases the limit of sensitivity to painful stimuli, suppressing the binding of PGs, which provoke nociceptors hypersensitivity to mechanical and chemical stimuli (the development of hyperalgesia). Reduces joint pain (when moving and at rest), relieves swelling and stiffness in the morning and helps increase motor volume.

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

Membrane stabilizing, antioxidant, as well as anti-ischemic activity are provided by chondroprotective effects. Indotril can limit chondrocytic destruction, as well as the replacement of chondrocytes by connective tissues.

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

[3], [4], [5], [6],

Pharmacokinetics

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

Intlasma protein synthesis is 90-98%. Metabolic processes develop inside the liver.

The excretion of most of the medication is carried out with the urine (60-75%), and the remainder is excreted in the feces. Half-life varies in the range of 2.6-11.2 hours (average 5.8 hours). Most of the drug is synthesized with protein inside the plasma.

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

The drug does not affect the values of gastric pH, and the excretion mainly flows through the kidneys. Indomethacin has no effect on secretion.

[7], [8], [9], [10], [11]

Dosing and administration

Adolescents from 14 years of age and adults should use a 1-pill drug after a meal, 3 times a day (corresponding to 30-45 mg of indomethacin). If the desired result is not achieved with this portion, it is increased to 2 tablets 2-3 times per day (for several days, until the acute manifestations of the disease are eliminated).

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

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

[15]

Use Indotrila during pregnancy

Do not use the drug during breastfeeding, as well as pregnancy.

Contraindications

Main contraindications:

• strong idiosyncrasy with respect to indomethacin, aspirin or other NSAIDs (history includes urticaria, bronchospasm or rhinitis caused by 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 type gastritis;
• severe failure of the liver, heart or kidneys, and in addition pancreatitis;
• AND;
• elevated blood pressure of malignant nature.

[12], [13], [14],

Side effects Indotrila

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

• lesions associated with the gastrointestinal tract: nausea, diarrhea, pain in the epigastric zone, loss of appetite and vomiting; sometimes there is obstipation. Occasionally, ulcerogenic effects may develop and bleeding inside the gastrointestinal tract may occur;
• disorders of the central nervous system: prolonged use of the drug can lead to dizziness, weakening of visual acuity, headaches, a feeling of indisposition or drowsiness, problems with concentration. In addition, depression, diplopia, mental disorders, parkinsonism, muscle weakness and paresthesia sometimes develop;
• signs of allergy: rash, itching, and besides this, dermatitis and urticaria;
• other: there are single disorders in the kidneys (hematuria or glomerulonephritis of proliferative nature) and liver (jaundice or hepatitis and an increase in the blood values of bilirubin and transaminases of the liver), leuko- or neutropenia (it can go as far as suppressing the bone marrow). Disorders of carbohydrate metabolism, cardiac arrhythmia, and swelling associated with water and electrolyte retention are also noted.

Overdose

If Indotril is poisoned, such manifestations occur: vomiting, feeling of disorientation, severe headaches, nausea, memory loss and dizziness. With severe disorders, seizures or paresthesias appear and numbness of the limbs 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 in this case will be ineffective.

[16], [17], [18]

Interactions with other drugs

With different drug combinations, different manifestations may occur:

• Phenytoin, digoxin, or lithium drugs — an increase in the plasma parameters of these drugs is possible;
• antihypertensive drugs, diuretics and β-blockers - perhaps a weakening of the activity of these medicines;
• potassium-sparing diuretics - the development of hyperkalemia;
• GCS, other NSAIDs, as well as colchicine - an increase in the likelihood of the development of negative signs in the gastrointestinal tract;
• cyclosporine and gold medications - an increase in toxic activity relative to the kidneys;
• aspirin or other salicylates - an increase in the likelihood of side symptoms;
• hypoglycemic drugs - may cause hyper-or hypoglycemia. With such drug combinations, blood glucose values are monitored;
• methotrexate - during the 24-hour period before and after drug use, the level of methotrexate may increase and its toxicity may potentiate;
• anticoagulants - it is required to constantly monitor the blood coagulability function, because in this case the potentiation of the exposure occurs and the probability of hemophilia increases.

[19], [20]

Storage conditions

Indotril is required to keep in a dark, closed from the penetration of children, dry place. Temperature range - within the limits of 15-25 ° С.

[21], [22], [23], [24]

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 (younger than 14 years of age).

Analogs

Analogues of drugs are medicines Indometacin, Ketorol, Aertal with Ketorolac, and in addition Blokum B12 and Ketanov.