Levomycetin tablets 0.5 №10

Description

Levomycetin tablets
active substance: chloramphenicol (chloramphenicol);

1 tablet contains chloramphenicol (chloramphenicol) 500 mg (0.5 g);

excipients: potato starch; calcium stearate.

Tablets.

Main physical and chemical properties: white or white tablets with a slightly yellowish tinge, with a flat surface, beveled edges and a dash.

Pharmacotherapeutic group
Antibacterial agents for systemic use. Amphenicols. Chloramphenicol.

ATX code J01B A01.

Pharmacological properties
Pharmacodynamics.

Chloramphenicol is a broad-spectrum bacteriostatic antibiotic. The action is associated with a violation of the process of protein synthesis in the microbial cell at the stage of transfer of t-rNA amino acids to ribosomes. Effective against many gram-positive and gram-negative bacteria: Escherichia coli, Shigella flexneri spp., Shigella boydii spp., Shigella sonnei spp., Salmonella spp., (Including Salmonella typhi), acts on Streptococcus spp. (including Streptococcus pneumoniae), Neisseria gonorrhoeae, Neisseria meningitidis, a number of strains of Proteus spp., some strains of Pseudomonas aeruginosa; active against Ricketsia spp., Treponema spp., Chlamydia spp. (including Chlamydia trachomatis), pathogens of purulent infections, typhoid fever, dysentery, meningococcal infection, brucellosis, rickettsiae, chlamydia, spirochetes. Does not affect Mycobacterium tuberculosis, pathogenic protozoa and fungi. Active against strains of bacteria resistant to penicillin, tetracyclines, sulfonamides. Resistance of microorganisms develops slowly. The drug is inactive against acid-fast bacteria, Pseudomonas aeruginosa, clostridia and protozoa.

The mechanism of action is due to inhibition of protein synthesis in the cells of microorganisms. In therapeutic concentrations it has a bacteriostatic effect. Resistance of microorganisms to the drug develops slowly and, as a rule, there is no cross-resistance to other chemotherapeutic agents. Due to its high toxicity, chloramphenicol can be used to treat severe infections in which less toxic antibacterial agents are ineffective or contraindicated.

Pharmacokinetics.

It is quickly and almost completely absorbed from the digestive tract. The maximum concentration in blood plasma is reached in 2-3 hours. Therapeutic concentration in the blood is maintained for 4-5 hours. Bioavailability after oral administration is 80%. It penetrates well into organs, tissues and body fluids, penetrates the blood-brain barrier (BPH), placenta, and breast milk. 50-60% of chloramphenicol is bound to plasma proteins. The highest concentrations of chloramphenicol are observed in the liver and kidneys. In bile up to 30% of the entered dose are observed. The maximum concentration in cerebrospinal fluid is observed in 4-5 hours after a single oral administration. Biotransformed in the liver, 90% binds to inactive glucuronide. Chloramphenicol palmitate is hydrolyzed to the free state in the digestive tract before absorption. Chloramphenicol sodium succinate is hydrolyzed to the free state in blood plasma, liver, lungs and kidneys. In the fetus and premature infants, the liver is underdeveloped to bind chloramphenicol, which leads to the accumulation of toxic concentrations of the active form of the drug and can lead to the development of “gray syndrome”. In the intestine under the action of intestinal bacteria is the hydrolysis of chloramphenicol with the formation of inactive metabolites.

It is excreted mainly in the urine (mainly in the form of inactive metabolites), partly in the bile (up to 30% of the dose) and feces.

The half-life in adults with normal renal and hepatic function is 1.5-3.5 hours, with impaired renal function – 3-4 hours, with severe hepatic impairment – 4.6-11 hours.

Indication
Infectious and inflammatory diseases caused by microorganisms sensitive to the drug: typhoid fever, paratyphoid fever, yersiniosis, brucellosis, shigellosis, salmonellosis, tularemia, rickettsiosis, chlamydia, purulent peritonitis, bacterial meningitis, biliary tract infections.

The drug is indicated in cases of ineffectiveness of other antimicrobials due to the possibility of severe side effects.

Contraindication
Hypersensitivity (allergy) to chloramphenicol (chloramphenicol), thiamphenicol, azidamphenicol and other components of the drug;
blood diseases, including inhibition of hematopoiesis;
severe liver and / or kidney dysfunction;
deficiency of the enzyme glucose-6-phosphate dehydrogenase;
skin diseases (psoriasis, eczema, fungal diseases);
porphyria.
Chloramphenicol should not be prescribed for acute respiratory diseases, sore throat, as well as to prevent bacterial infection.