Li-butol - instructions for use, doses, side effects, contraindications

Excipients: dicalcium phosphate 16.66 mg, silicon dioxide colloid 3.34 mg, corn starch 13.33 mg, gelatin 8.34 mg, talc purified 6.66 mg, magnesium stearate 6.66 mg, purified enough water.

Description:Round flat tablets of white or almost white color with a risk and a mark LB/4 on the one hand and smooth on the other. On the break the tablets are white or almost white in color.

Pharmacotherapeutic group:anti-tuberculosis drug

ATX: & nbsp

J.04.A.K.02 Ethambutol

Pharmacodynamics:

Etambutol is a chemotherapeutic agent with a bacteriostatic effect on Mycobacterium tuberculosis. Ethambutol, inhibiting the synthesis of ribonucleic acids in bacterial cells, disrupts the cellular metabolism, causes the cessation of reproduction and the death of bacteria. The minimum inhibitory concentration is 1 mg / ml. It is active only for intensively dividing cells. Affects intracellular and extracellular bacterial species. Suppresses growth and reproduction Mycobacterium tuberculosis, resistant to streptomycin, isoniazid, aminosalicylic acid, ethionamide, kanamycin.

About 1% of patients have primary resistance to ethambutol.

Pharmacokinetics:

Absorption is high; bioavailability is 75-80%. After oral administration at a dose of 25 mg / kg, the maximum concentration in the plasma is achieved in 2-4 hours and is 1-5 μg / ml, after 24 hours - the concentration is less than 1 μg / ml.

It binds to plasma proteins by 20-30%.

It penetrates well into tissues and organs, as well as into biological fluids, with the exception of ascitic and pleural (in cerebrospinal fluid - only with meningitis). The greatest concentrations are created in the kidneys, lungs, saliva, urine. Penetrates into breast milk. Do not pass through the intact blood-brain barrier. Ethambutol penetrates the placenta. In fetal blood, the concentration of ethambutol is approximately 30% of the concentration in the mother's blood.

Etambutol is partially metabolized in the liver to dicarboxylic acid derivatives (inactive metabolites). The half-life period is 3-4 hours, and with renal insufficiency it lengthens to 8 hours. It is excreted by the kidneys - 80-90% (50% - unchanged, 15% - in the form of inactive metabolites) and the intestines - 10-20% (unchanged). It is excreted in hemodialysis and peritoneal dialysis.

Indications:

Tuberculosis (all forms) in combination therapy.

Contraindications:

- Hypersensitivity to ethambutol, components of the drug;

- optic neuritis;

- cataract;

- diabetic retinopathy;

- inflammatory diseases of the eyes;

- gout;

- children's age (up to 13 years);

- pregnancy, the period of breastfeeding.

Carefully:

Chronic renal failure.

Pregnancy and lactation:

The use of the drug is contraindicated in pregnancy and lactation.

Dosing and Administration:

Inside.

Adults (initial treatment period): 15-20 mg / kg body weight / day - single dose.When conducting a second course of treatment: 25 mg / kg of body weight / day in one session during 2 months, then switch to taking the drug at a dose of 15 mg / kg of body weight / day at one time.

The dose can be increased to 30 mg / kg of body weight per day (but not more than 2.0 g) in the initial period of treatment, with relapse of the disease, with resistance Mycobacterium tuberculosis to other anti-tuberculosis drugs.

You can use the drug 2-3 times a week (during the continuation of treatment): 3 times a week - 30 (25-35) mg / kg of body weight per day in one session; 2 times a week - 45 (40-50) mg / kg of body weight per day in a single dose. The maximum daily dose is 2.5 g.

Children from the age of 13 (with the possibility of conducting ophthalmic control), the drug is prescribed at a rate of 15-25 mg / kg body weight once a day after breakfast. The maximum daily dose of 1 g. The full course of treatment lasts 9 months.

In case of impaired renal function Correction of the dosing regimen is performed depending on the creatinine clearance.

Creatinine clearance (ml / min)	Daily dose
More than 100	20 mg / kg bw / day
70-100	15 mg / kg bw / day
less than 70	10 mg / kg bw / day
With hemodialysis	5 mg / kg bw / day
On the day of dialysis	7 mg / kg bw / day

Side effects:

Allergic reactions: dermatitis, skin rash, itching, joint pain, fever, anaphylactic reactions.

From the digestive system: loss of appetite, nausea, vomiting, gastralgia, "metallic" taste in the mouth, impaired liver function (up to a lethal outcome) - increased activity of "liver" transaminases, jaundice.

From the nervous system and sensory organs: weakness, headache, dizziness, confusion, disorientation, hallucinations, depression, convulsions, peripheral neuritis (paresthesia in the limbs, numbness, paresis, pruritus), optic neuritis (decreased visual acuity, visual field limitation, color loss (mostly green and red), color blindness, central or peripheral scotoma), bleeding in the retina.

Other: an increase in the concentration of uric acid in the blood serum, exacerbation of gout, leukopenia, thrombocytopenia, neutropenia.

Overdose:

Symptoms: nausea, vomiting, hallucinations.

Treatment: symptomatic.

Interaction:

Strengthens the effects of antituberculous drugs: the neurotoxicity of ciprofloxacin, aminoglycosides, asparaginase, carbamazepine, lithium salts, imipenem, methotrexate, quinine.

Simultaneous intake of aluminum hydroxide reduces the absorption of ethambutol from the digestive tract. The intake of aluminum hydroxide is recommended 4 hours after taking ethambutol. Ethambutol changes the metabolism of certain trace elements, mainly zinc.

Special instructions:

Etambutol is used only in complex therapy with other anti-tuberculosis drugs: isoniazid, aminosalicylic acid, streptomycin, cycloserine, pyrazinamide, ethionamide and rifampicin.

At the beginning of treatment, it is possible to increase cough, increase the amount of sputum.

In patients with impaired renal function, the dose of ethambutol should be reduced because of the possibility of cumulation of the drug in the body.

Before starting treatment with ethambutol, ophthalmic control should be carried out: examination of the fundus, visual fields, visual acuity and color perception. In the process of treatment, ophthalmic studies should be performed periodically, taking into account the possibility of developing optic neuritis. The occurrence of visual impairments depends on the duration of treatment and the existing diseases of the eyeball.If they occur, ethambutol treatment should be discontinued. The vision changes are usually reversible, after the cessation of treatment disappear after a few weeks, in some cases in a few months. In exceptional cases, changes in the eyeball are irreversible due to atrophy of the optic nerve.

It is recommended to perform periodic monitoring of liver, kidney and general blood test.

Effect on the ability to drive transp. cf. and fur:

During the treatment period, one should refrain from managing vehicles and other potentially hazardous activities requiring increased attention and speed of psychomotor reactions.

Form release / dosage:Tablets, 400 mg.

Packaging:

For 10 tablets per blister (PVC / AL) or strip (AL / AL).

For 2 or 10 blisters or strips are placed in a cardboard bundle along with instructions for use.

For 100 or 1000 tablets in a polyethylene bag is placed in a bottle of high-density polyethylene. A sachet of silica gel (1 or 2, respectively) is placed in the vial and instructions for use (for hospitals).

Storage conditions:

In a dry, the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

4 years.

Do not use the drug after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:П N016310 / 01

Date of registration:27.05.2005

The owner of the registration certificate:FARMGID CJSCFARMGID CJSC Russia

Manufacturer: & nbsp

Laika Labs Limited India

Information update date: & nbsp05.10.2015

Illustrated instructions

Instructions

Li-Butol (Ly-butol)