Thiotriazoline
Thiotriazoline: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. Use in the elderly
- 13. Drug interactions
- 14. Analogs
- 15. Terms and conditions of storage
- 16. Terms of dispensing from pharmacies
- 17. Reviews
- 18. Price in pharmacies
Latin name: Thiotriasoline
ATX code: A05BA
Active ingredient: Morpholinium-methyl-triazolyl-thioacetate (Thiotriazolin) (Thiotriasoline)
Producer: Galichpharm (Ukraine), Kievmedpreparat (Ukraine)
Description and photo update: 2018-23-10
Prices in pharmacies: from 388 rubles.
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Thiotriazoline is a drug with anti-ischemic, antioxidant, membrane stabilizing and immunomodulatory effects.
Release form and composition
Dosage forms of Thiotriazoline release:
- tablets: flat, almost white or white, round, beveled; 200 mg - with a risk (10 pcs. in blisters, in a cardboard box of 3, 5 or 9 blisters);
- solution for intramuscular and intravenous administration: transparent, colorless or with a slightly yellowish tinge (in blisters 5 or 10 ampoules of 2 or 4 ml, in a cardboard box 1-2 packs or 10 ampoules).
Composition of 1 tablet:
- active substance: morpholinium-methyl-triazolyl-thioacetate (thiotriazoline) - 100 or 200 mg;
- auxiliary components: microcrystalline cellulose, sucrose, potato starch, calcium stearate, low molecular weight povidone.
Composition of 1 ml solution:
- active substance: morpholinium-methyl-triazolyl-thioacetate (thiotriazoline, in terms of 100% substance) - 25 mg;
- additional component: water for injection - up to 1 ml.
Pharmacological properties
Pharmacodynamics
The pharmacological effect of morpholinium-methyl-triazolyl-thioacetate is due to membrane stabilizing, anti-ischemic, immunomodulatory and antihypoxant effects.
The effect of the drug is due to an increase in the compensatory activation of anaerobic glycolysis and the activation of oxidative processes in the Krebs cycle while maintaining the intracellular fund of adenosine triphosphate. The presence in the structure of the thiotriazoline molecule of sulfur thiol, which is characterized by redox properties, and tertiary nitrogen, which binds excess hydrogen ions, causes the activation of the antioxidant properties of the drug.
The reducing properties of the thiol group cause a reaction with lipid radicals and reactive oxygen species. The initiation of reactive oxygen species is prevented by the reactivation of antiradical enzymes, including superoxide dismutase, catalase and glutathione peroxidase.
Thiotriazoline, given its hepatoprotective properties, is used in the treatment of liver diseases. The drug prevents the destruction of hepatocytes, helps to reduce the degree of fatty infiltration and the prevalence of centrilobular necrosis of the liver, as well as to activate the processes of reparative regeneration of hepatocytes, normalizing carbohydrate, protein, pigment and lipid metabolism in them. Thanks to the use of the drug, the chemical composition of bile is stabilized, the rate of its excretion and synthesis increases.
The effect of morpholinium-methyl-triazolyl-thioacetate in the ischemic areas of the myocardium helps to inhibit lipid oxidation, prevent progressive suppression of the contractile function of the heart, decrease myocardial sensitivity to catecholamines, and decrease and stabilize the size of myocardial necrosis and ischemia zones. Improves metabolic processes in the myocardium, as well as the rheological properties of blood (due to the activation of the fibrinolytic system).
According to the results of a clinical study, the use of the drug can reduce the number of angina attacks and the number of nitroglycerin tablets required to relieve angina attacks.
Pharmacokinetics
After oral administration, morpholinium-methyl-triazolyl-thioacetate is rapidly absorbed in the gastrointestinal tract, its absolute bioavailability is 53%. After a single oral administration of 200 mg, the maximum plasma concentration in the blood is reached after 1.6 hours. The half-life is about 8 hours. The substance is excreted mainly by the kidneys.
The maximum plasma concentration in the blood after intramuscular administration is 399 μg / ml. The time to reach the maximum plasma concentration is 0.84 / 0.1 hours (intramuscular / intravenous). The degree of absolute bioavailability is 34.6%, the volume of distribution is 318 ml.
Indications for use
- toxic liver damage, including viral, alcoholic and drug etiology (tricyclic antidepressants, antibacterial, antituberculosis, antitumor, antiviral drugs, oral contraceptives, etc.);
- fatty degeneration of the liver, chronic viral hepatitis, liver cirrhosis;
- chronic alcoholic hepatitis of moderate / minimal activity;
- ischemic heart disease - simultaneously with other drugs to prevent attacks of stable angina pectoris (tablets).
Contraindications
- renal failure;
- intolerance to fructose, isomaltase / sucrase deficiency, glucose-galactose malabsorption (tablets);
- age up to 18 years;
- pregnancy and the period of breastfeeding;
- individual intolerance to the components of the drug.
Thiotriazoline tablets are used under medical supervision in the following cases:
- impaired renal function with creatinine clearance> 60 ml / min;
- diabetes.
Instructions for the use of Thiotriazoline: method and dosage
Pills
Thiotriazoline tablets are taken orally with water. Do not chew the tablets.
Recommended regimen:
- chronic alcoholic hepatitis, toxic liver damage, chronic viral hepatitis, fatty liver disease, liver cirrhosis: 3-4 times a day, 100-200 mg, maximum 800 mg per day; course duration - from 20 to 30 days;
- prevention of attacks of stable angina pectoris: 3 times a day, 200 mg for 8 weeks.
Based on the severity and characteristics of the course of the disease, the doctor may prescribe a second course of therapy.
Injection
In the treatment of chronic hepatitis in the first 5 days, Thiotriazoline is administered 2-3 times a day in one of the following two ways:
- intramuscularly: 2 ml of a 2.5% solution (50 mg);
- intravenously: 4 ml of a 2.5% solution (100 mg) slowly at a rate of 2 ml / min or drip at a rate of 20-30 drops / min (before the introduction of 2 ampoules, a 2.5% solution must be dissolved in physiological solution with a volume of 150-250 ml).
In the future, from the 5th to the 20th days of therapy, Thiotriazoline is taken orally in the form of tablets 3 times a day, 100 mg each.
The total duration of the course varies from 20 to 30 days.
Side effects
In general, Thiotriazoline is well tolerated by patients. In extremely rare cases, the following disorders may develop:
- central nervous system: dizziness, general weakness, tinnitus;
- digestive system: dry mouth, nausea, bloating;
- respiratory system: very rarely - asthma attacks, shortness of breath;
- cardiovascular system: tachycardia, arrhythmias, increased blood pressure, pain in the heart;
- allergic / dermatological reactions: fever, skin flushing, pruritus, urticaria, hypersensitivity reactions; very rarely - Quincke's edema;
- local reactions (at the injection site): rarely - redness and tingling sensation.
Overdose
Overdose cases of Thiotriazoline are unknown.
When taking a large amount of the drug inside, you need to wash the stomach. Symptomatic therapy is indicated.
special instructions
Thiotriazolin tablets contain sucrose: 1 tablet 100 mg - 2.8 mg sucrose, 1 tablet 200 mg - 5.6 mg sucrose. This information should be considered by patients with diabetes mellitus.
Influence on the ability to drive vehicles and complex mechanisms
Studies on the effect of the drug on the ability to drive vehicles and complex mechanisms have not been conducted, but, given the risk of side effects such as dizziness, you should be extremely careful when engaging in activities that require increased concentration of attention and speed of psychomotor reactions.
Application during pregnancy and lactation
Thiotriazoline is not prescribed during pregnancy / breastfeeding.
Pediatric use
Therapy is not prescribed for patients under 18 years of age.
With impaired renal function
According to the instructions, Thiotriazoline is contraindicated in renal failure.
With creatinine clearance> 60 ml / min, oral administration of the drug is possible under medical supervision.
Use in the elderly
When used in elderly patients (over 65 years), dose adjustment is not required. However, due to age-related decline in renal function, periodic monitoring of urea and creatinine should be carried out.
Drug interactions
There is no information on the interaction of Thiotriazoline with other drugs / substances.
Analogs
Thiotriazoline analogs are: VG-5, Larnamin, Laennek, Cryomelt MN, Hepatosan, Dipana, Gepaphor, Methionin, Maksar, Liv.52, Polition, Ornicetil, Ropren and others.
Terms and conditions of storage
Store in a place protected from light at a temperature of 15-25 ° C. Keep out of the reach of children.
Shelf life:
- tablets - 3 years;
- injection solution - 4 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Thiotriazoline
According to reviews, Thiotriazoline is an effective cardioprotector and hepatoprotector. The drug has a wide range of uses. It is prescribed for palpitations, shortness of breath, toxic liver damage. The availability of the drug is noted. Adverse reactions are rarely reported.
The price of Thiotriazoline in pharmacies
The approximate price for Thiotriazoline is:
- tablets of 100 mg (50 pieces per package) - from 780 rubles, 200 mg each (90 pieces per package) - from 921 rubles;
- solution for injection (in a package of 10 ampoules of 4 ml) - from 918 rubles.
Thiotriazoline: prices in online pharmacies
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Drug name Price Pharmacy |
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Thiotriazoline 100 mg tablets 50 pcs. 388 r Buy |
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Thiotriazoline 25 mg / ml solution for intravenous and intramuscular administration 4 ml 10 pcs. 723 RUB Buy |
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Thiotriazoline 200mg tablets 90 pcs. 749 RUB Buy |
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Thiotriazoline 200 mg tablets 90 pcs. 749 RUB Buy |
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
