Composition, form of production and packaging
The tablets covered with a film membrane of white or almost white color, round, biconcave, with risk from one side.
1 tab.
ethambutol hydrochloride 400 mg
Auxiliary substances: corn starch, microcrystalline cellulose, povidone (PVPK-30), stearic acid, sodium carboxymethyl starch, silicon dioxide colloid, talc purified, magnesium stearate.
Sheath composition: hypromellose, ethylcellulose, macrogol 6000, talc purified, titanium dioxide.
10 pieces. - blisters (10) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2011.
PHARMACHOLOGIC EFFECT
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 of body weight after 2-4 hours, C max in the serum is 2-5 Ојg / ml, after 24 hours the concentration is less than 1 Ојg / ml.
Well penetrates into many tissues and organs. Etambutol accumulates in the 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%. Etambutol is metabolized in the liver to dicarboxylic acid derivatives. T 1/2 is 3-4 hours, and with renal failure is extended 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.
DOSING MODE
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 13 years are appointed at the rate 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
more than 100 20 mg / kg bw / day
70-100 15 mg / kg bw / day
below 70 10 mg / kg bw / day
with hemodialysis 5 mg / kg bw / day
on the day of dialysis 7 mg / kg bw / day
SIDE EFFECT
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 impairment 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;
- Increase of uric acid level in blood serum, the phenomenon of urine acid diathesis;
- increased activity of hepatic transaminases.
CONTRAINDICATIONS
- Inflammation of the optic nerve;
- cataract;
- diabetic retinopathy;
- Inflammatory eye diseases;
- severe renal insufficiency;
- gout;
- Pregnancy;
- lactation;
- Children's age (up to 13 years);
- Hypersensitivity to the drug.
PREGNANCY AND LACTATION
Contraindicated in pregnancy and lactation.
APPLICATION FOR FUNCTIONS OF THE LIVER
Contraindicated in severe renal failure.
Use with caution in case of impaired renal function.
APPLICATION FOR CHILDREN
Contraindicated in children under 13 years.
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 antituberculosis drugs that the patient had not previously taken and against 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.
Impact on the ability to drive vehicles and manage mechanisms
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.
OVERDOSE
Symptoms: nausea, vomiting, hallucinations, polyneuritis.
Treatment: induce vomiting, rinse stomach.
DRUG INTERACTION
Etambutol is used in complex therapy with other anti-tuberculosis drugs: isoniazid, paraaminosalicylic acid, streptomycin, cycloserine, pyrazinamide, ethionamide and rifampicin.
Enhances the neurotoxicity of ciprofloxacin, aminoglycosides, asparaginase, carbamazepine, lithium salts, imipenem, methotrexate, quinine.
Aluminum hydroxide reduces the absorption of ethambutol from the digestive tract. Etambutol alters the metabolism of certain trace elements, mainly zinc.
TERMS OF RELEASE FROM PHARMACY
On prescription.
TERMS AND CONDITIONS OF STORAGE
List B. In a dry, the dark place at a temperature of no higher than 25 В° C. Keep out of the reach of children. Shelf life - 3 years.
