Tibinyl E400

Tibinil E400 is an anti-tuberculosis drug with a bacteriostatic type of activity. It inhibits the reproduction of tuberculosis mycobacteria that are resistant to isoniazid, ethionamide, PAS with streptomycin and kanamycin.

At the initial stage of therapy, an increase in the volume of sputum and an increase in cough may be observed. The drug can only be used in combination with other anti-tuberculosis drugs. During long-term treatment, it is necessary to constantly monitor the parameters of peripheral blood and the functioning of the kidneys and liver. [ 1 ]

Indications Tibinyl E400

It is used for different types of tuberculosis (both pulmonary and affecting other organs).

Release form

The drug is released in the form of tablets.

Pharmacokinetics

After oral administration, it is absorbed in the gastrointestinal tract (approximately 75-80% of ethambutol).

The drug is distributed throughout many fluids and tissues. High levels of the drug are found in the lungs with urine, saliva and kidneys. [ 2 ]

Metabolic processes occur mostly inside the liver: about 15% of the drug is transformed during metabolism into inactive metabolic components. [ 3 ]

The half-life is 3-4 hours. Excretion occurs through the kidneys; about 80% of the drug is excreted over a period of 24 hours. At the same time, 20% of the substance is excreted with feces in the form of metabolic elements that have no activity.

Dosing and administration

In case of primary therapy for persons over 15 years of age and adults, doses of 15 mg/kg are used, 1 time per day.

When undergoing a repeated treatment cycle, the medication is used in a dosage of 25 mg/kg, once a day for a period of 2 months. After that, a transition to a dose of 15 mg/kg, once a day, is made.

• Application for children

Tibinil E400 should not be prescribed to persons under 15 years of age.

Use Tibinyl E400 during pregnancy

It is prohibited to use the medication during pregnancy and breastfeeding.

Contraindications

Main contraindications:

• strong personal sensitivity to the drug;
• cataract or neuritis affecting the optic nerve;
• inflammation in the eye area and diabetic retinopathy.

Side effects Tibinyl E400

Side effects include:

• neuritis affecting the optic nerve (1- or 2-sided; it is characterized by a disorder of perception of certain colors (green and red), narrowing of the visual fields and weakening of visual acuity almost to complete blindness) or hemorrhages in the retinal area;
• headaches, disorientation, confusion and dizziness, as well as hallucinations, polyneuropathy, paresthesia and malaise;
• symptoms of intolerance are occasionally observed (fever, itching, epidermal rashes, tachycardia, leukopenia, vasculitis and arthralgia; anaphylaxis, SJS or TEN are observed occasionally);
• heartburn, abdominal pain, diarrhea, anorexia, metallic taste and vomiting, as well as jaundice and increased transaminase activity;
• thrombocytopenia or tubulointerstitial nephritis may occur, as well as the development of an acute gout attack and a decrease in uric acid clearance rates.

Negative manifestations are mainly observed in diabetics, the elderly, people with liver failure or chronic alcoholism.

Overdose

In case of poisoning, neurological disorders are likely to occur (especially damage to the optic nerve (resulting in blindness)). Diarrhea, loss of appetite, fever, vomiting, confusion, headaches, hallucinations, dizziness, asystole and respiratory depression may also occur.

The drug has no antidote; symptomatic procedures are performed. Due to rapid absorption of the drug, vomiting should be induced immediately or gastric lavage should be performed. The use of activated carbon is advisable only immediately after the administration of Tibinil E400.

It is necessary to monitor and support the functioning of vital organs and systems; if necessary, resuscitation procedures are performed. Peritoneal dialysis, forced diuresis or hemodialysis can be performed. If the patient's condition is life-threatening, exchange blood transfusion is performed (due to the fact that this allows the removal of red blood cells, inside which ethambutol accumulates in large volumes).

Interactions with other drugs

Al hydroxide and similar antacids interfere with the absorption of ethambutol from the gastrointestinal tract, which is why they cannot be used together with the drug.

Pyrazinamide and ethambutol have a synergistic effect on uric acid excretion.

Exposure to ethambutol may reduce the activity of digitoxin.

The combination of Tibinil E400 and isoniazid using cyclosporine A causes potentiation of the latter's breakdown with an increased risk of transplant rejection.

Combination with disulfiram may increase serum levels of ethambutol and potentiate its toxicity.

Ethanol potentiates the toxic activity of ethambutol in relation to the visual organ, which is why it is necessary to stop drinking alcohol during the period of therapy.

Storage conditions

Tibinil E400 should be stored in a place protected from sunlight and children. The temperature is standard for medicines.

Shelf life

Tibinil E400 can be used within a 36-month period from the date of manufacture of the pharmaceutical product.

Analogues

The analogs of the drug are the substances Teriz and Paizina with Inbutol, as well as Phenazid and Pyra.