Terizidone
Terizidone: 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: Terizidone
ATX code: J04AK03
Active ingredient: terizidone (Terizidone)
Manufacturer: Simpex Pharma Pvt Ltd. (Simpex Pharma, Pvt. Ltd.) (India); Rozlex Pharm, LLC (Russia); Riemser Arzneimittel, AG (Germany); Technologist, PrJSC (Ukraine); Scan Biotech Ltd. (Scan Biotech, Ltd.) (India); Redkinskiy Experimental Plant, CJSC (Russia)
Description and photo update: 2019-09-07
Terizidone is an antibacterial drug used in the complex therapy of drug-resistant forms of tuberculosis.
Release form and composition
Dosage form - capsules: hard gelatinous, inside the capsules contains powder from light yellow to white; 150 mg each - size No. 1, brown cap and body; 250 mg each - size No. 0, yellow cap and body; 300 mg each - size No. 0, blue cap, yellow body [in a cardboard box 1–5 or 10 blisters / blisters / blisters made of PVC film and Al printed varnished foil, 10 capsules each together with instructions for use of Terizidone; in a polymer can with a polypropylene / high-pressure polyethylene lid with a first opening control (a polyethylene terephthalate can with a screw cap or with a first opening control) a polyethylene bag with 30 or 100 capsules; in a cardboard box 1 polypropylene container with a low density polyethylene lid and a ring of the first opening, 50 capsules each].
Composition of 1 capsule:
- active substance: terizidone - 150, 250 or 300 mg;
- auxiliary components (150/250/300 mg): lactose monohydrate - 150/30/35 mg; purified talc - 20/20/15 mg;
- capsule cap (150/250/300 mg): gelatin - 83.095 8 / 83.226 7 / 83.226 7%; sodium lauryl sulfate - 0.15 / 0.15 / 0.15%; povidone - 0.1 / 0.1 / 0.1%; bronopol - 0.1 / 0.1 / 0.1%; titanium dioxide - 1.75 / 1.667 / 1.667%; red dye iron oxide (III) - 0.2 / 0/0%; yellow dye iron oxide (III) - 0.004 2/0/0%; dye blue brilliant - 0/0 / 0.156 3%; quinoline yellow dye - 0 / 0.156 3/0%; propyl parahydroxybenzoate 0.025 / 0.025 / 0.025%; methyl parahydroxybenzoate - 0.075 / 0.075 / 0.075%; purified water - 14.5 / 14.5 / 14.5%;
- capsule body (150/250/300 mg): gelatin - 83.095 8 / 83.226 7 / 83.226 7%; bronopol - 0.1 / 0.1 / 0.1%; povidone - 0.1 / 0.1 / 0.1%; titanium dioxide - 1.75 / 1.667 / 1.667%; red dye iron oxide (III) - 0.2 / 0/0%; yellow dye iron oxide (III) - 0.004 2/0/0%; quinoline yellow dye - 0 / 0.156 3 / 0.156 3%; sodium lauryl sulfate - 0.15 / 0.15 / 0.15%; propyl parahydroxybenzoate - 0.025 / 0.025 / 0.025%; methyl parahydroxybenzoate - 0.075 / 0.075 / 0.075%; purified water - 14.5 / 14.5 / 14.5%.
The appearance, as well as the qualitative and quantitative composition of the auxiliary components, including the composition of the capsule, may vary depending on the manufacturer.
Pharmacological properties
Pharmacodynamics
The action of the active substance Terizidone is aimed at complete blockade of the enzyme that converts the aliphatic amino acid alanine into alanyl-alanine dipeptide, which is the main component of the microbial wall of mycobacteria. Cross-resistance with other anti-TB drugs does not develop.
Terizidone has pronounced and broad antimicrobial properties, due to which it has a significant effect not only on strains that cause tuberculosis or urinary tract infections, but also on strains that show resistance to other known antibiotics.
MIC (minimum inhibitory concentration) of a substance for susceptible strains is in the range from 4 to 130 mg / ml.
Strains susceptible to the action of terizidone: Shigella, Bacillus subtilis, Mycobacterium tuberculosis, Candida albicans, various strains of Streptococcus (including S. Pyogenes), Escherichia coli, Klebsiella pneumonie, Pasteurella multocida, Staphylococcus aerlococcus, epidermapidis, a pseudomonas entericia causing paratyphoid fever, typhus, endemic typhus.
Pharmacokinetics
One of the most important properties of terizidone is the ability to provide high urinary and plasma concentrations after oral administration of the drug, which makes it especially convenient in the treatment of infectious processes of the urinary tract, including chronic forms.
Terizidone after oral administration on an empty stomach is absorbed quickly and almost completely (from 70 to 90% of the dose), the peak plasma concentration develops in 2-4 hours.
The substance is widely distributed in body fluids and tissues - in the lungs, bile, lymph, semen, cerebrospinal, ascitic, pleural, synovial fluid. There is a very good penetration of terizidone into the cerebrospinal fluid (from 80 to 100% of the plasma concentration) with the highest level in the inflammatory process of the meningeal membranes.
The excretion of the substance is carried out slowly and in stages through the urinary tract, so the level remains at the middle of the peak plasma concentration even 24 hours after ingestion. Thanks to long-term excretion, effective urinary concentrations are maintained for 12 hours. From 60 to 70% of the dose is excreted as unchanged substance by glomerular filtration, excreted in the feces and a small volume of terizidone is metabolized.
In case of impaired liver function (liver failure), terizidone is used without precautions, except in patients with a high risk of seizures and patients with alcoholic hepatitis.
The drug is easily tolerated by most patients with a low degree of renal failure, therefore, in the treatment of tuberculosis in this group of patients, it can be used for a long time. In case of impaired renal function with creatinine clearance less than 30 ml / min and patients on hemodialysis, the dosage regimen must be adjusted.
Indications for use
Terizidone is prescribed for the treatment of tuberculosis of various forms and localization (as part of the complex therapy of drug-resistant forms of the disease).
Contraindications
Absolute:
- severe chronic renal failure (in patients with a creatinine concentration of more than 2 mg / dL);
- organic diseases of the central nervous system (including atherosclerosis of the vessels of the brain);
- mental disorders;
- epilepsy;
- alcoholism;
- lactase deficiency, glucose-galactose malabsorption, galactose intolerance;
- age up to 14 years;
- pregnancy and lactation;
- individual intolerance to the components of the drug, as well as cycloserine.
Relative (Terizidone capsules are used under medical supervision):
- chronic renal failure;
- chronic heart failure;
- elderly age.
Terizidone, instructions for use: method and dosage
Terizidone capsules are taken orally during meals, whole with a small amount of liquid. Single doses during the day must be taken at regular intervals.
Terizidone is excreted during hemodialysis, so it must be taken at the end of the procedure.
The duration of the course is 3-4 months.
Capsules 150 and 300 mg
The recommended dosage regimen, depending on the weight:
- up to 60 kg: 2 times a day, 300 mg;
- 60–80 kg: 300 mg 3 times a day;
- from 80 kg: 2 times a day, 600 mg.
For patients with creatinine clearance below 30 ml / min, it is recommended to reduce a single dose of the drug to 150 mg, and also to reduce the frequency of taking Terizidone.
Patients from 60 years old and weighing up to 50 kg in the presence of renal failure Terizidone is prescribed 2 times a day, 150 mg.
250 mg capsules
The recommended dosage regimen, depending on the weight:
- up to 60 kg: 3 times a day, 250 mg;
- from 60 kg: 4 times a day, 250 mg.
In patients with creatinine clearance less than 30 ml / min, Terizidone should be taken daily at 250 mg or 3 times a week at 500 mg.
Side effects
- digestive system: flatulence, abdominal pain, diarrhea;
- nervous system: feeling of intoxication, tremors, dizziness, headache, irritability, insomnia, convulsions, psychosis, depression;
- others: allergic reactions, skin rash.
Overdose
The main symptoms: acute poisoning (when using more than 1000 mg of Terizidone), Chronic toxicity is determined by the dosage and can occur with a daily intake of more than 500 mg of the drug.
Toxic effects are usually detected from the central nervous system and are manifested in the form of headache, dizziness, confusion, increased irritability, paresthesias, dysarthria, psychosis. When high doses are taken, peripheral paresis, convulsions and coma can occur. Ethanol increases the risk of developing epileptic seizures.
Therapy: symptomatic and supportive. To reduce the absorption of terizidone, activated charcoal is more effective than gastric lavage. With the development of neurotoxic effects, the use of 200-300 mg of pyridoxine per day is indicated. Terizidone is eliminated from the blood using hemodialysis, but this does not exclude the development of a toxic effect, which can pose a threat to life.
special instructions
In case of development of symptoms of damage to the nervous system or allergic reactions, it is necessary to reduce the dose or stop taking Terizidone.
If the level of terizidone in the blood is more than 30 mg / l, poisoning may occur, this is most likely in case of an overdose or violation of the clearance of the drug.
During the period of therapy, it is necessary to monitor hematological parameters, renal excretory function, liver function and the level of the drug in the blood.
Therapeutic index of Terizidone is low.
Before starting treatment, it is necessary to isolate the culture of microorganisms and determine the sensitivity of the strain to the action of terizidone. In case of tuberculosis infection, the sensitivity of the strain to other anti-tuberculosis drugs should be determined.
In patients with impaired renal function, taking terizidone in a daily dose of 500 mg and who have symptoms of overdose, the concentration of terizidone in the blood should be monitored at least once a week. The dose should be adjusted so that the concentration of the drug in the blood remains at a level not exceeding 30 mg / l.
For the prevention of symptoms of damage to the central nervous system (in the form of excitement, seizures, tremors), the use of anticonvulsants and sedatives is effective.
Due to the risk of overdose symptoms, patients taking Terizidone in a daily dose of 500 mg or more should be under medical supervision.
In order to prevent side neurotoxic effects, psychotropic drugs of the benzodiazepine series (diazepam, phenazepam) and nootropics (piracetam, pyridoxine, glutamic acid) are used.
In some patients, the use of Terizidone and other anti-tuberculosis drugs leads to the development of vitamin B 12 (folic acid) deficiency in the body, sideroblastic and megaloblastic anemia, which requires medical advice.
Influence on the ability to drive vehicles and complex mechanisms
During the period of therapy with Terizidone, it is recommended to refuse to perform potentially dangerous types of work, including driving vehicles.
Application during pregnancy and lactation
Terizidone is contraindicated during pregnancy / lactation.
Pediatric use
The safety profile of Terizidone use in patients under 14 years of age has not been studied, therefore, the drug is not prescribed for children.
With impaired renal function
- severe chronic renal failure (in patients with a creatinine concentration of more than 2 mg / dL): therapy is contraindicated;
- chronic renal failure: Terizidone should be used under medical supervision.
Use in the elderly
Elderly patients are prescribed the drug with caution.
Drug interactions
- ethionamide: the neurotoxic effects of terizidone are potentiated;
- isoniazid: the toxic effect of terizidone on the central nervous system increases, which may require dose adjustment; medical supervision is shown;
- alcohol: the combined use is contraindicated, since this increases the risk of developing epileptic seizures;
- indirect anticoagulants: their effectiveness increases; control of prothrombin time is required, if necessary, the dose of anticoagulants is adjusted;
- phenytoin: its excretion is slowed down, which increases the risk of developing intoxication; dose adjustment may be required;
- Suxamethonium chloride (muscle relaxant): its effectiveness, as well as the likelihood of side effects, increases; dose adjustment may be required.
Analogs
The analogues of Terizidone are Resonizat, Loxidon, Tizidone, Terizidone-Mac.
Terms and conditions of storage
Store in a place protected from light and moisture at temperatures up to 25 ° C. Keep out of the reach of children.
Shelf life is 2 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Terizidone
Reviews of Terizidone are few, since the drug is prescribed as part of a complex treatment, and it is difficult to assess its effectiveness and tolerability separately from other drugs used simultaneously.
The price of Terizidone in pharmacies
The approximate price for Terizidone is: 50 capsules of 250 mg - 33,800 rubles, 100 capsules of 150 mg - 22,000 rubles.
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, 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!
