Ethambutol instructions for use, contraindications, side effects, reviews. Dosage and Administration Treatment of tuberculosis ethambutol

capsules 250 mg; can (jar) 250;

Structure
1 capsule contains ethambutol 250 mg; in cans of 250 pcs.

Pharmacodynamics of the drug Ethambutol

A chemotherapeutic agent with a bacteriostatic effect on typical and atypical mycobacterium tuberculosis.
The mechanism of action of the drug is associated with rapid penetration into the cell, where lipid metabolism, RNA synthesis are disturbed, magnesium and copper ions bind, the structure of ribosomes and protein synthesis in bacterial cells.
Acts on intracellular and extracellular types of bacteria. About 1% of patients have primary drug resistance. Ethambutol is well absorbed in lung tissue and can reach a concentration 5-9 times higher than in serum, it penetrates well into many tissues and organs.
The intracellular concentration in erythrocytes is twice as high as in the blood serum.

Pharmacokinetics of the drug Ethambutol

Ethambutol is rapidly and 80% absorbed from digestive tract... The minimum inhibitory concentration is 1 mg / ml.
After oral administration of a single dose of 25 mg / kg of body weight, in 2-4 hours Cmax in serum is reached 2-5 μg / ml, after 24 hours the concentration is less than 1 μg / ml.
It binds to plasma proteins by 20-30%.
Ethambutol is metabolized in the liver by dicarboxylic acid derivatives.
T1 / 2 is 3-4 hours, and in renal failure it lengthens to 8 hours. Within 24 hours, more than 50% of the drug dose is excreted in the urine unchanged, and 8-15% in the form of inactive metabolites. About 20-22% of the initial dose of the drug is excreted in the feces unchanged.
Ethambutol crosses the placenta. In fetal blood, the concentration of ethambutol is approximately 30% of the concentration of the drug in the mother's blood.

Use of the drug Ethambutol for impaired renal function

Contraindication: severe renal failure... In kidney disease, the dose of the drug depends on the degree of renal failure, an indicator of which is CC.

Contraindications to the use of the drug Ethambutol

Inflammation optic nerve;
- cataract;
- diabetic retinopathy;
- inflammatory diseases eye;
- severe renal failure;
- gout:
- pregnancy;
- lactation,
- childhood up to 13 years old;
- hypersensitivity to the drug.

Side effects of the drug Ethambutol

Retrobulbar inflammation of the optic nerve, unilateral or bilateral (weakening of visual acuity, impaired color perception, the presence of central or peripheral scotoma, limitation of the field of vision).
The occurrence of visual impairment depends on the duration of treatment and existing diseases eyeball. If they appear, treatment with ethambutol should be discontinued. Changes in vision are usually reversible; after stopping treatment, they disappear after a few weeks, in some cases after a few months. In exceptional cases, changes in eyeball irreversible due to optic nerve atrophy.
Allergic reactions: skin rash, itchy skin, joint pain, fever, leukopenia.
Gastrointestinal Disorders: metallic taste mouth, nausea and vomiting, abdominal pain, lack of appetite.
From the side of the central nervous system: headaches and dizziness, confusion, disorientation, hallucinations, convulsions.
From the urinary system: an increase in the level of uric acid in the blood serum, the phenomenon of uric acid diathesis.

Method of application and dose of the drug Ethambutol

Inside, once, 20-25 mg / kg / day or (for adults only) - 50 mg / kg 1-2 times a week. Children - the highest single dose is 25 mg / kg / day.

Overdose with Ethambutol

Cases of overdose with ethambutol are not described.
Measures in case possible overdose: induce vomiting, gastric lavage.

Interactions of the drug Ethambutol with other drugs

Aluminum hydroxide reduces the absorption of ethambutol from the digestive tract.
Ethambutol alters the metabolism of several trace elements, mainly zinc.

Special instructions when taking the drug Ethambutol

In patients with renal insufficiency, the dose of ethambutol should be reduced due to the accumulation of the drug in the body.
Before starting treatment with ethambutol, ophthalmological control should be periodically performed: examination of the fundus, visual fields, visual acuity and color perception.
It is recommended to periodically monitor the functions of the liver, kidneys and general analysis blood.
Influence on the ability to drive vehicles and use mechanisms
Due to the possibility of visual impairment (decreased visual acuity, limitation of the field of vision, disorder of color perception in relation to green and red colors) during the treatment with ethambutol, you should not drive cars and service moving mechanical equipment.

Photo of the drug

Latin name: Ethambutol

ATX code: J04AK02

Active substance:

Producer: Pharmasintez JSC (Russia), Shreya Life Sciences (India), Makiz-Pharma (Russia), KhFK Akrikhin (Russia), Darnitsa (Ukraine)

Description up to date on: 21.12.17

Ethambutol

International non-proprietary name

Ethambutol

Dosage form

Tablets 400 mg

Structure

One tablet contains

active substance - ethambutol hydrochloride 400 mg;

excipients: calcium hydrogen phosphate anhydrous, potato starch, gelatin, calcium stearate, talc, sodium lauryl sulfate.

Description

Tablets are round in shape, with a flat-cylindrical surface, white or white with cream, or white with a gray tint, with a double-sided bevel and a score on one side.

Pharmacotherapeutic group

Anti-tuberculosis drugs. Ethambutol.

ATX code J04AK02

Pharmacological properties

Pharmacokinetics

Ethambutol is rapidly, almost 80% absorbed from the digestive tract. Absorption is slowed down when taken with food. Therefore, it should be taken 1 hour before meals or after meals. The minimum inhibitory concentration is 0.5 - 8.0 μg / ml. After oral administration of a single dose of 25 mg / kg of body weight, a maximum serum concentration of 5 μg / ml is reached after 2 to 4 hours, and after 24 hours the concentration is less than 1 μg / ml. It binds to plasma proteins by 20-30%. Ethambutol is metabolized in the liver to dicarboxylic acid derivatives. The half-life is 3-4 hours, and in renal failure it is extended to 8 hours. Within 24 hours, more than 50% of the dose of the drug is excreted in the urine unchanged, and 8-15% in the form of inactive metabolites. About 20 - 22% of the initial dose of the drug is excreted unchanged in the feces. Ethambutol crosses the placenta. In fetal blood, the concentration of ethambutol is approximately 30% of that in the mother's blood.

Pharmacodynamics

Ethambutol has a bacteriostatic effect on tuberculosis microbacteria. The mechanism of action of the drug is associated with rapid penetration into the cell, where lipid metabolism, RNA synthesis are disturbed, magnesium and copper ions bind; the structure of ribosomes and protein synthesis in bacterial cells are disrupted. Ethambutol is used in combination with other anti-tuberculosis drugs, since drug resistance develops rapidly.

Indications for use

tuberculosis of the lungs and other organs (as part of combination therapy)

Method of administration and dosage

Ethambutol is administered orally once daily.

Ethambutol is used in the intensive phase (IF) treatment for patients

Children 400 mg per day with a weight of 21 to 30 kg. Permissible dose fluctuations for children are 15-25 mg / kg.

In renal disease, the dosage depends on the degree of renal failure, as measured by creatinine clearance.

IN complex therapy with ethambutol, isoniazid, pyrazinamide and rifampicin are used. Use strictly as directed by your doctor.

Side effects

metallic taste in the mouth, lack of appetite, nausea, vomiting, abdominal pain, diarrhea, pseudomembranous colitis (when used together with rifampicin and isoniazid)

increased body temperature, chills

leukopenia, thrombocytopenia, eosinophilia, lymphadenopathy

headaches, dizziness, confusion, hallucinations, seizures, depression, disorientation

peripheral neuritis (paresthesia in the limbs, numbness, paresis, itching), retrobulbar neuritis

deterioration of visual acuity, impaired color perception (mainly green and red), narrowing of the central and peripheral fields of vision, hemorrhages in the retina, the occurrence of cattle, in rare cases, irreversible visual impairment up to blindness is possible

an increase in the level of uric acid in the blood serum, the phenomenon of uric acid diathesis, interstitial nephritis

at long-term use in large doses, damage to the heart muscle and the development of heart failure (pericarditis, myocarditis, arterial hypotension, tachycardia) are possible

• increased cough, increased phlegm

  infiltrates in the lungs with or without eosinophilia, pneumonitis

  peripheral polyneuropathy

  increased activity of "hepatic" transaminases, hepatitis, jaundice

  dermatitis, skin rash, pruritus, arthralgia, fever, anaphylaxis, erythema, exanthema, Stevens-Johnson syndrome, Lyell's syndrome, bronchospasm, vasculitis

  exacerbation of gout

Contraindications

hypersensitivity to the drug

inflammation of the optic nerve, inflammatory eye diseases

cataract

diabetic retinopathy

chronic renal failure (end stage)

• mental disorders (exacerbation stage)

  pregnancy, lactation

  children under 12 years old

Drug interactions

Aluminum hydroxide reduces the absorption of ethambutol from the digestive tract. Ethambutol alters the metabolism of some trace minerals, mainly zinc. With isoniazid, ftivazid, metazid, a slowdown in the development of mycobacterium tuberculosis resistance is observed. With isoniazid, while the use of cyclosporin A - increased breakdown of cyclosporin A with the risk of graft rejection. With anti-tuberculosis drugs - to enhance the effects of anti-tuberculosis drugs. Isoniazid, paraaminosalicylic acid (PASK), streptomycin, cycloserine, pyrazinamide can be used to treat tuberculosis in combination therapy with ethambutol. When interacting with digitoxin, the effectiveness of the latter decreases.

With ciprofloxacin, aminoglycosides, asparaginase, carbamazepine, lithium preparations, imipenem, methotrexate, quinine - the effects are enhanced and the neurotoxicity of the above drugs is increased. With disulfiram, there is an increase in the concentration of ethambutol and its toxicity. With ethionamide, the simultaneous use of ethambutol with ethionamide is not recommended due to pharmacological antagonism (it is better to alternate drugs every other day). With pyrazinamide, there is a synergistic effect on the excretion of uric acid. FROM ethyl alcohol the negative effect of ethambutol on the organs of vision increases, therefore, during treatment, you should stop drinking alcohol.

Ethambutol can increase the concentration of uric acid in the serum, it is necessary to prescribe an increased dosage of uricosuric agents. The effectiveness of ethambutol is reduced with the simultaneous use of spermine, spermidine and magnesium. False positive results are possible in the diagnosis of adrenal tumors when ethambutol interacts with serum phentolamine.

special instructions

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

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

If visual impairment occurs, ethambutol should be discontinued immediately to prevent optic nerve atrophy. Changes in vision are usually reversible; after stopping treatment, they disappear after a few weeks, in some cases - after a few months. In exceptional cases, changes in vision are irreversible due to atrophy of the optic nerve. In case of visual impairment, use hydroxycobalamin or cyanocobalamin.

Despite the absence of visual impairment in children, treatment of children with ethambutol is not recommended, since it is almost impossible to determine visual impairment in them. Only in children over 12 years of age, treatment with ethambutol is possible, subject to control precautions.

Treatment with ethambutol can increase the concentration of urate in the blood, which is associated with a decrease in the excretion of uric acid by the kidneys.

In patients who have previously taken drugs with tuberculostatic action, bacterial resistance to ethambutol develops more often.

Long-term or repeated use of ethambutol can lead to the development of secondary infections. If you suspect an infection, you should see a doctor.

If the symptoms of tuberculosis do not disappear within 2-3 weeks, or if the condition worsens, it is recommended to see a doctor.

Complete treatment is necessary, whether or not symptomatic, is present to prevent recurrence or the development of resistance.

Ethyl alcohol enhances the toxic effect of ethambutol on the organs of vision, therefore, during treatment, you should stop drinking alcohol.

If side effects appear, the dose must be adjusted in the direction of decreasing it; if such a step is impossible, the transition to intermittent drug intake (every other day or 2 times a week).

Features of influence drug for the ability to drive vehicles and /or potentially dangerous mechanisms.

Due to the possibility of visual impairment (decreased visual acuity, limitation of visual fields, disturbance of color perception in relation to green and red colors) during the treatment with ethambutol, you should not operate machines and maintain moving mechanical equipment

Overdose

Symptoms Development neurological disorders, damage to the optic nerve (possibly blindness), deterioration in visual acuity or increased manifestations of other adverse reactionsloss of appetite, nausea, vomiting, diarrhea, fever, headache, dizziness, confusion, hallucinations, polyneuritis, respiratory depression, asystole.

Treatment. There is no specific antidote, the treatment is symptomatic. Due to the rapid absorption of the drug, vomiting or gastric lavage should be induced immediately after administration, and enterosorbents should be prescribed. Exercise control and measures to support the vital functions of the body, if necessary, carry out resuscitation measures. Shows forced diuresis, peritoneal dialysis or hemodialysis. When allergic reactions the use of desensitizing agents is shown. In threatening conditions, it is necessary to carry out a blood transfusion to remove red blood cells, where ethambutol accumulates.

Release form

10 tablets are placed in a blister strip made of polyvinyl chloride film or similar imported and printed aluminum foil varnished or similar imported.

| Ethambutolum

Analogs (generics, synonyms)

Diambutol, Miambutoya, Afimocil, Ambutol, Anvital, Batakox, Tsidanbutol, Clobutol, Dadibutol, Dexambutol, Ebutol, Etambin, Farmabutol, Li-Butol, Mycobutol, Tembutol, Tibistal, Tubetelol,

Recipe (international)

Rp .: Tab. Ethambutoli 0.4 No. 100
D.S. 3 tablets per day after meals.

pharmachologic effect

A chemotherapeutic agent with a bacteriostatic effect on typical and atypical mycobacterium tuberculosis. The mechanism of action of the drug is associated with rapid penetration into the cell, where lipid metabolism, RNA synthesis are disrupted, magnesium and copper ions bind, the structure of ribosomes and protein synthesis in bacterial cells are disrupted.

Acts on intracellular and extracellular types of bacteria. About 1% of patients have primary drug resistance. Ethambutol is well absorbed in lung tissue and can reach a concentration 5-9 times higher than in blood serum, it penetrates well into many tissues and organs. The intracellular concentration in erythrocytes is twice as high as in blood serum.

Mode of application

For adults: Inside, 1 time a day (after breakfast), for primary patients who have not previously taken anti-tuberculosis drugs, 15 mg / kg; patients who previously took anti-tuberculosis drugs - 25 mg / kg. The course of treatment is 2 months. Then the drug is prescribed in maintenance doses - 15 mg / kg once a day.

Indications

- pulmonary tuberculosis;
- extrapulmonary tuberculosis.

Contraindications

- inflammation of the optic nerve;
- cataract;
- diabetic retinopathy;
- inflammatory eye diseases;
- severe renal failure;
- gout:
- pregnancy;
- lactation,
- children up to age 13;
- hypersensitivity to the drug.

Side effects

Possible deterioration of vision, allergic reactions.

Release form

tablets of 0.1 and 0.4 g in a package of 100 pieces; pills of 0.25 g in a package of 50 pieces.

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Ethambutol - a new description of the drug, you can see pharmachologic effect, side effects, prices in pharmacies for Ethambutol. Helpful Reviews for Ethambutol -

Anti-tuberculosis drug of the II row.
Drug: ETAMBUTOL
The active substance of the drug: ethambutol
ATX encoding: J04AK02
KFG: Anti-tuberculosis drug
Registration number: P No. 014625 / 01-2002
Date of registration: 15.12.02
Owner reg. ID: SHREYA LIFE SCIENCES Pvt. Ltd. (India)

Release form Ethambutol, drug packaging and composition.

Pills white or nearly white, round, with a dividing line on one side, with beveled edges; at the break - from almost white to cream color. Tablets 1 tab. ethambutol hydrochloride 200 mg - "- 400 mg -" - 600 mg - "- 800 mg -" - 1 g
Excipients: starch, dibasic calcium phosphate, methylparaben, propylparaben, gelatin, purified talc, magnesium stearate, colloidal silicon dioxide, sodium starch glycolate, purified water.
20 pcs. - strips (1) - cardboard packs.
DESCRIPTION OF THE ACTIVE SUBSTANCE.
All the information given is presented only for familiarization with the drug, you should consult your doctor about the possibility of use.

Pharmacological action Ethambutol

Anti-tuberculosis drug of the II row. It has a bacteriostatic effect only on Mycobacterium tuberculosis, including strains resistant to streptomycin, kanamycin, isoniazid, PASK and ethionamide. The mechanism of action is not precisely established. Apparently, ethambutol, penetrating into mycobacteria, disrupts RNA synthesis. Active only against rapidly dividing bacteria. Mycobacterium tuberculosis is relatively slow to develop resistance to ethambutol.

Pharmacokinetics of the drug.

After oral administration, absorption from the gastrointestinal tract is 80%, the rest of the dose is excreted in the feces unchanged. Food intake does not significantly affect absorption. When single dose 25 mg / kg Cmax of ethambutol in blood plasma is reached after 4 hours and is 5 μg / ml, after 24 hours the concentration is less than 1 μg / ml.
Ethambutol is distributed in most tissues, including the lungs, kidneys, and red blood cells. Penetrates into cerebrospinal fluid with inflamed meninges.
Ethambutol is partially metabolized in the liver to inactive aldehyde and dicarboxylic derivatives, which are excreted in the urine.
T1 / 2 is 3-4 hours. It is excreted mainly in the urine unchanged, 8-15% - in the form of inactive metabolites.

Indications for use:

All forms of pulmonary and extrapulmonary tuberculosis (as part of combination therapy).
MAC infection.

Dosage and method of administration of the drug.

It is taken orally at a dose of 15-25 mg / kg 1 time / day, or 50 mg / kg 2 times a week, or 25-30 mg / kg 3 times a week.
Maximum doses: for adults - 2.5 mg / day.

Side effects of Ethambutol:

From the central nervous system and peripheral nervous system: dizziness, depression, peripheral neuritis, retrobulbar neuritis, disturbances in color perception (mainly green and red), decrease in central and peripheral visual fields, the occurrence of cattle.
From the side digestive system: nausea, vomiting, loss of appetite.
From the musculoskeletal system: arthritis.
Allergic reactions: skin rash.

Contraindications to the drug:

Optic neuritis, cataracts, diabetic retinopathy, inflammatory eye diseases, pregnancy, impaired renal function, children under 13 years of age, hypersensitivity to ethambutol.

Application during pregnancy and lactation.

Use during pregnancy is contraindicated.
Ethambutol crosses the placental barrier and is excreted in breast milk.
In experimental studies, the teratogenic effect of ethambutol has been established.

Special instructions for the use of Ethambutol.

At the beginning of treatment, it is possible to increase the cough, increase the amount of sputum.
Ethambutol is used only in combination with other anti-tuberculosis drugs. In combination with isoniazid and rifampicin, it is highly effective in the treatment of tuberculosis.
When carrying out long-term therapy, it is necessary to regularly monitor the function of vision, the picture of peripheral blood, as well as the functional state of the liver and kidneys.

Interaction of Ethambutol with other drugs.

With simultaneous use with aluminum hydroxide, there is a decrease in the absorption of ethambutol from the gastrointestinal tract.
There is evidence of a possible increase in optic neuropathy caused by the action of ethambutol, when used in combination with isoniazid.
Under the influence of ethambutol, zinc metabolism may change.