Levomycetin sodium succinate - instructions for use, dose, side effects, contraindications

A bacteriostatic broad-spectrum antibiotic disrupts the process of protein synthesis in a microbial cell at the stage of transfer of t-RNA amino acids to ribosomes.

It is effective against strains of bacteria that are resistant to penicillin, tetracycline, sulfonamides.

It is active against gram-positive and gram-negative bacteria: Escherichia coli. Shigella dysenteria, Shigella flexneri spp., Shigella boydii spp. Shigella sonnei, Salmonella spp. (at t.ch. Salmonella typhi, Salmonella paratyphi). Staphylococcus spp., Streptococcus spp. (incl. Streptococcus pneumoniae). Neisseria meningitidis, Neisseria gonorrhoeae, a number of strains Proteus spp., Burkholderia pseudomallei, Rickettsia spp., Treponema spp., Leptospira spp., Chlamydia spp. (incl. Chlamydia trachomatis), Coxiella burnetii, Ehrlichia canis, Bacteroides fragilis, Klebsiella pneumoniae, Haemophilus influenzae.

He acts on acid-fast bacteria (incl. Mycobacterium tuberculosis), anaerobes, methicillin-resistant strains of staphylococci, Acinetobacter spp., Enterobacter spp., Serratia marcescens, indol-positive strains Proteus spp., Pseudomonas aeruginosa spp., protozoa and fungi.

Stability of microorganisms develops slowly.

Pharmacokinetics:

Absorption - 90% (fast and almost complete). Bioavailability - 70% after intramuscular injection (in / m). The connection with plasma proteins is 50-60%, in preterm infants - 32%. Time to reach the maximum concentration (TCmax) after intravenous administration (in / in) -1-1.5 hours. The volume of distribution is 0.6-1 l / kg.

It penetrates well into body fluids and tissues. Its greatest concentrations are created in the liver and kidneys. In bile, up to 30% of the administered dose is detected. The maximum concentration (Cma) in the cerebrospinal fluid (CSF) is determined 4-5 hours after a single injection and can reach 21-50% of C max in plasma and 45-89% in the presence of inflammation of the meninges in the absence of inflammation of the meninges. Passes through the placental barrier, the concentration in the fetal blood serum can be 30-80% of that in the mother's blood. Penetrates into breast milk. The majority (90%) is metabolized in the liver. In the intestines, under the influence 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%. The half-life of the drug from the blood plasma (T_1/2) in adults - 1.5-3.5 h, with a violation of the kidneys - 3-11 h. T_1/2 in children from 1 month to 16 years of age - 3-6.5 hours, in newborns from 1 to 2 days - 24 hours or more (especially varies in children with low birth weight), 10-16 days-10 hours. during hemodialysis.

Indications:

Infectious-inflammatory diseases caused by sensitive microorganisms, incl. abscess of the brain, typhoid fever, paratyphoid, salmonellosis (mostly generalized forms), dysentery, brucellosis, tularemia, Ku fever, meningococcal infection, rickettsiosis (including typhus, trachoma, spotted fever of the Rockies), inguinal lymphogranuloma, iersiniosis , erlichiosis, urinary tract infections, purulent wound infection, purulent peritonitis, bile duct infections.

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

Carefully:

Early childhood, patients who received previous treatment with cytostatic drugs or radiation therapy.

Dosing and Administration:

Intravenous (intravenously) slowly or intramuscularly (in / m).

Adults in / in or / m in a dose of 0.5-1.0 g per injection 2-3 times a day. In severe forms of infections (including typhoid fever, peritonitis) in hospital conditions, an increase in the dose to 3-4 g / day is possible.

The maximum daily dose is 4 g.

Children are prescribed control of the concentration of the drug in the serum depending on the age: infants and older - 12.5 mg / kg (base) every 6 hours or 25 mg / kg (base) every 12 hours, with severe infections (bacteremia, meningitis) - up to 75-100 mg / kg (base) / day.

The solutions are prepared immediately before the injection.

For intravenous administration, the contents of the 0.5 g bottle are dissolved in 2.5 ml, the contents of the vial of 1 g in 5 ml of 5% and 40 % solutions of glucose or water for injection. Patients suffering from diabetes, the drug is administered in a solution of sodium chloride 0.9%.

When administered intramuscularly, the volume of the solvent is usually 2-3 ml per gram of antibiotic. As a diluent of the drug used intramuscularly, 0.25-0.5% solutions of novocaine can be used.

The average duration of treatment is 8-10 days.

Side effects:

From the gastrointestinal tract: dyspepsia (nausea, vomiting, diarrhea), dysbacteriosis (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 (in children under 1 year).

Overdose:

Overdose may increase the side effects.

Treatment: hemosorption, symptomatic therapy.

Interaction:

Suppresses the enzymatic system of cytochrome P450, so when used simultaneously with phenobarbital, phenytoin,indirect anticoagulants marked by a weakening of the metabolism of these drugs, slowing the excretion and increasing their concentration in the plasma.

Reduces the antibacterial effect of penicillins and cephalosporins.

With simultaneous use with erythromycin, clindamycin, lincomycin, there is a mutual weakening of the effect due to the fact that chloramphenicol can displace these drugs from the bound state or interfere with their binding to the subunit 50S bacterial ribosomes.

Simultaneous prescribing with drugs that oppress 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).

Myelotoxic drugs increase manifestations of hematotoxicity preparation.

Special instructions:

Inadmissible uncontrolled administration of chloramphenicol and its use in mild forms of infectious processes, especially in children's practice!

With the simultaneous administration of ethanol, the development of a disulfiram reaction (hyperemia of the skin, tachycardia, nausea, vomiting, reflex cough, convulsions) is possible.

During the treatment, systematic monitoring of the peripheral blood pattern is necessary. Severe complications from the hematopoietic system are usually associated with the use of large doses (more than 4 g / day) for a long time.

Form release / dosage:Powder for the preparation of solution for intravenous and intramuscular injection 0.5 g, 1 g.

Packaging:

In bottles with a capacity of 10 ml.

1, 5, 10 bottles with instructions for use in a pack of cardboard.

Storage conditions:

List B. In a dry, the dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:

3 years. Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:P N001174 / 01

Date of registration:19.11.2007

Expiration Date:Unlimited

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

Manufacturer: & nbsp

SYNTHESIS, OJSC Russia

Information update date: & nbsp07.03.2018

Illustrated instructions

Instructions

Levomycetin sodium succinate (Levomycetin sodium succinate)