Levomycetin-UBF - instructions for use, dose, side effects, contraindications

A bacteriostatic broad-spectrum antibiotic disrupts the process of protein synthesis in a microbial cell (having fat-solubility, penetrates through the bacterial cell membrane and reversibly binds to the 50S subunit of bacterial ribosomes, in which the movement of amino acids to growing peptide chains is delayed, which leads to a violation of protein synthesis). It is effective against strains of bacteria that are resistant to penicillin, tetracycline, sulfonamides. It is active against Escherichia coli, Haemophilus influenzae, Klebsiella pneumoniae, certain Enterobacter species (Aerobacter), Neisseria species, Staphylococcus aureus, Streptococcus spp. (including Streptococcus pneumoniae, Streptococcus hemolyticus), Moraxella lacunata, rickettsia and mycoplasmas.

It is effective against Pseudomonas aeruginosa, Serratia marcescens, does not act on acid-fast bacteria (t.ch.mycobacterium tuberculosis), anaerobes, methicillin-resistant strains of staphylococci, Acinetobacter, Enterobacter, indole-positive strains of Proteus spp., protozoa and fungi.

Stability of microorganisms develops slowly.

Pharmacokinetics:

Absorption - 90% (fast and almost complete). Bioavailability is 80% after ingestion. The connection with plasma proteins is 50-60%. Time to reach the maximum concentration (T_Сmах) after oral administration - 1-3 hours. The volume of distribution is 0.6-1.0 l / kg. The therapeutic concentration in the blood persists for 4-5 hours after ingestion, with the use of tablets with prolonged action - for 12 hours. It penetrates well into the body fluids and tissues. The greatest concentrations of it are created in the liver and kidneys. In bile, up to 30% of the administered dose is detected. The maximum concentration in the cerebrospinal fluid is determined 4-5 hours after a single injection inwards and can reach 21-50% of uninflammated meninges C_max in plasma and 45-89% - with inflamed meninges. Passes through the placental barrier, concentrations in the fetal blood serum can be 30-80% of the concentration in the mother's blood. Penetrates into breast milk. The majority (90%) is metabolized in the liver.In the intestines, under the action of intestinal bacteria, it hydrolyses with the formation of inactive metabolites. It is excreted for 24 hours by kidneys - 90% (by glomerular filtration - 5-10% unchanged, by tubular secretion in the form of inactive metabolites - 80%), through the intestine - 1-3%. Half-life (T_1/2) in adults - 1.5-3.5 h, with a violation of the kidneys - 3-11 hours Weakly undergoing hemodialysis.

Indications:Diseases caused by sensitive microorganisms: typhoid fever, paratyphoid, salmonellosis, dysentery, brucellosis, tularemia, fever, meningococcal infection, rickettsiosis (including typhus, trachoma, spotted fever of the Rocky Mountains), inguinal lymphogranuloma, chlamydia, iersiniosis, erlichiosis, urinary tract infections, purulent wound infection, pneumonia, purulent peritonitis, bile duct infections, purulent otitis media.

Contraindications:Hypersensitivity, oppression of bone marrow hematopoiesis, acute intermittent porphyria, deficiency of glucose-6-phosphate dehydrogenase, hepatic and / or renal failure, skin diseases (psoriasis, eczema, fungal lesions), pregnancy, lactation.

Carefully:Early childhood.

Dosing and Administration:

Inside 30 minutes before meals, and with the development of nausea and vomiting - 1 hour after meals, 3-4 times a day. Single dose for adults - 0,25-0,5 g, daily - 2 g / day. In severe forms of infection (including typhoid fever, peritonitis), in hospital conditions, an increase in the dose to 3-4 g / day is possible. The average duration of the course of treatment is 8-10 days.

Children are prescribed control of the concentration of the drug in the blood serum, depending on the age: premature and full-term newborns under 2 weeks of age - by mouth at 6.25 mg / kg every 6 hours; thoracic children 2 weeks. and older - inside, at 12.5 mg / kg every 6 hours or 25 mg / kg every 12 hours, with severe infections (bacteremia, meningitis) - up to 75-100 mg / kg per day.

Side effects:

From the digestive system: dyspepsia, nausea, vomiting (the probability of development decreases with admission after 1 hour after eating), diarrhea, irritation of the mucous membrane of the mouth and throat, dysbiosis (suppression of normal microflora).

On the part of the organs of hematopoiesis: reticulocytopenia, leukopenia, granulocytopenia, thrombocytopenia, erythrocytopenia; rarely - aplastic anemia, agranulocytosis.

From the nervous system: psychomotor disorders, depression, confusion, peripheral neuritis, optic neuritis, visual and auditory hallucinations, decreased visual acuity and hearing, headache.

Allergic reactions: skin rash, angioedema. Other: secondary fungal infection, collapse (children under 1 year).

Overdose:

In case of an overdose, dyspepsia, nausea, vomiting, diarrhea, irritation of the mucous membrane of the mouth and throat are possible.

Symptoms: "gray syndrome" (cardiovascular syndrome) in unresolved and newborns with high doses (the cause of the development is the accumulation of chloramphenicol, due to the immaturity of liver enzymes, and its direct toxic effect on the myocardium) -deep-gray skin color, low body temperature, non-rhythmic breathing, lack of reactions, cardiovascular failure. Mortality - within 2-3 days 1 40% -60% of children. Treatment: hemosorption, symptomatic therapy.

Interaction:Simultaneous prescription with drugs that depress hemopoiesis (sulfonamides, cytostatics) that affect liver metabolism with radiation therapy increases the risk of side effects.When administered with oral hypoglycemic drugs, their effect is noted (by suppressing metabolism in the liver and increasing their concentration in the plasma). With simultaneous use with erythromycin, clindamycin, lincomycin, there is a mutual weakening of action due to the fact that levomycetin can displace these drugs from the bound state or prevent their binding to the subunit of 50S bacterial ribosomes. Reduces the antibacterial effect of penicillins and cephalosporins. Levomycetin inhibits the enzymatic system of cytochrome P450, so when used with phenobarbital, phenytoin, indirect anticoagulants, there is a weakening of the metabolism of these drugs, a slowdown in the excretion and an increase in their concentration in the plasma.

Special instructions:

Due to the high toxicity, it is not recommended without resorting to banal infections, colds, flu, pharyngitis, bacteriocarriers for treatment and prevention. Severe complications from the hematopoietic system, as a rule, are associated with the use of large doses (more than 4 g / day) for a long time.During the treatment, systematic monitoring of the peripheral blood pattern is necessary. Be wary appoint patients who received previous treatment with cytostatic drugs or radiation therapy. With the simultaneous administration of ethanol, the development of a disulfiram reaction (hyperemia of the skin, tachycardia, nausea, vomiting, reflex cough, convulsions) is possible.

Children are prescribed control of the concentration of the drug in the blood serum.

Form release / dosage:Tablets 500 mg.

Packaging:For 10 tablets in a contiguous cell-free or contiguous cell package. For 10, 20, 30, 40, 50, 60 tablets in a polymer can. 1, 2, 3, 5 contour packs are placed in a cardboard pack.

Storage conditions:List B. In a place protected from light, inaccessible to children, at room temperature.

Shelf life:5 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:P N002578 / 01

Date of registration:31.10.2008

Expiration Date:Unlimited

The owner of the registration certificate:URALBIOFARM, OJSC URALBIOFARM, OJSC Russia

Manufacturer: & nbsp

URALBIOFARM, OJSC Russia

Information update date: & nbsp07.03.2018

Illustrated instructions

Instructions

Levomycetin-UBF (Levomycetin-UBF)