Etambutol - instructions for use, dose, side effects, contraindications

Excipients: potato starch 76.0 mg, povidone (medium molecular weight polyvinylpyrrolidone, collidon 25) 16.0 mg, microcrystalline cellulose 138.0 mg, talc 4.8 mg, silicon dioxide colloid (aerosil grade A-300) 9.2 mg, magnesium stearate 6.0 mg.

Description:

Round, flat-cylindrical tablets of white or white with a grayish shade of color with a risk and a facet.

Pharmacotherapeutic group:anti-tuberculosis drug

ATX: & nbsp

J.04.A.K.02 Ethambutol

Pharmacodynamics:

Etambutol is a chemotherapeutic agent with a bacteriostatic effect on typical and atypical mycobacteria tuberculosis.

The mechanism of action of the drug is associated with a violation of the synthesis of RNA in bacterial cells. Affects intracellular and extracellular bacterial species.

Pharmacokinetics:

Etambutol is rapidly and 80% absorbed from the digestive tract. The minimum inhibitory concentration is 1 mg / ml.

After oral administration of a single dose of 25 mg / kg body weight in 2-4 hours, the maximum serum concentration is 2-5 μg / ml, after 24 hours the concentration is less than 1 μg / ml.

Well penetrates into many tissues and organs. Ethambutol accumulates in lung tissue and can reach a concentration of 5-9 times higher than in serum.

Intracellular concentration in erythrocytes is twice as high as in serum.

It binds to plasma proteins by 20-30%. Ethambutol is metabolized in the liver to dicarboxylic acid derivatives. The half-life period is 3-4 hours, and with renal insufficiency it lengthens to 8 hours. Within 24 hours more than 50% of the drug dose is excreted unchanged in urine, and 8-15% in the form of inactive metabolites. About 20-22% of the initial dose of the drug is excreted with feces unchanged.

Etambutol penetrates the placenta. In fetal blood, the concentration of ethambutol is approximately 30% of the concentration of the drug in the mother's blood.

Indications:

- Pulmonary tuberculosis;

- extrapulmonary tuberculosis.

Contraindications:

- Hypersensitivity to the drug;

- inflammation of the optic nerve;

- cataract;

- diabetic retinopathy;

- inflammatory diseases of the eyes;

- severe renal insufficiency;

- gout;

- pregnancy;

- lactation,

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

Dosing and Administration:

Adults: initial treatment period: 15 mg / kg body weight / day - single dose; continuous treatment: usually 20 mg / kg body weight / day.

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

Children from the age of 13 prescribe from the calculation of 15-25 mg / kg body weight (but not more than 1.0 g).

The full course of treatment lasts 9 months.

With kidney disease, the dose of the drug depends on the creatinine clearance.

Creatinine clearance (ml / min)	Daily dose
over 100	20 mg / kg bw / day
70-100	15 mg / kg bw / day
below 70	10 mg / kg bw / day
in hemodialysis	5 mg / kg bw / day
on dialysis day	7 mg / kg bw / day

Side effects:

Retrobulbaric inflammation of the optic nerve, one-sided or bilateral (weakening of visual acuity, violation of color perception, the presence of central or peripheral scotoma, limitation of the visual field). 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.

- Allergic reactions: skin rash, itching, joint pain, fever, leukopenia, anaphylaxis;

- gastrointestinal disorders, "metallic" taste in the mouth, nausea and vomiting, abdominal pain, lack of appetite;

- weakness, headache, dizziness, confusion, orientation disorder, hallucinations, convulsions, depression, peripheral neuritis;

- an increase in the level of uric acid in the serum, the phenomenon of urine acid diathesis.

- increased activity of "liver" transaminases.

Overdose:

Symptoms: nausea, vomiting, hallucinations, polyneuritis.

Treatment for overdose: induce vomiting, and wash the stomach.

Interaction:

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

Aluminum hydroxide reduces the absorption of ethambutol from the digestive tract.

Etambutol alters the metabolism of certain trace elements, mainly zinc.

Enhances the neurotoxicity of ciprofloxacin, aminoglycosides, asparaginase, carbamazepine, lithium salts, imipenem, methotrexate, quinine.

Special instructions:

In patients who have previously taken drugs with tuberculostatic action, the resistance of bacteria develops more often. In such cases ethambutol should be taken with at least one or two anti-tuberculosis drugs that the patient had not previously taken and in relation to which no bacterial resistance was noted.

In patients with renal insufficiency, the dose of ethambutol should be reduced because of the accumulation of the drug in the body.

Before starting treatment with ethambutol, ophthalmic control should be carried out periodically: examination of the fundus, visual fields, visual acuity and color perception.

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

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

Because of the possibility of visual impairment (reduced visual acuity, limitation of visual fields, color perception in relation to green and red color) during the treatment with ethambutol, do not drive machines and maintain moving mechanical equipment.

Form release / dosage:

Tablets, 400 mg.

Packaging:

Primary packaging of medicinal product

For 10 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

For 50 or 100 tablets (for hospitals) is placed in a can of polymer with a lid pulled with the control of the first opening. Free space is filled with cotton wool.Labels are applied to cans from paper label or writing or from polymeric materials, self-adhesive.

Secondary packaging of medicinal product

For 5 or 10 contour mesh packages together with the instruction for use are placed in a pack of cardboard.

100 contour-cell packs with an equal number of instructions for medical use are placed in a cardboard box (for hospitals). Banks along with an equal number of instructions for use are placed in a group box-box of corrugated cardboard.

Storage conditions:

In a dry, protected from light place at a temperature of no higher than 25 ° C.

Shelf life:

4 years.

Do not use after the time specified on the package.

Terms of leave from pharmacies:On prescription

Registration number:CP-002624/07

Date of registration:07.09.2007

The owner of the registration certificate:FARMASINTEZ, JSC (Irkutsk) FARMASINTEZ, JSC (Irkutsk) Russia

Manufacturer: & nbsp

FARMASINTEZ, JSC (Irkutsk) Russia

Representation: & nbspPharmasynthesis, JSCPharmasynthesis, JSC

Information update date: & nbsp04.10.2015

Illustrated instructions

Instructions

Ethambutol (Ethambutol)