Levomycetinum

General characteristics. Structure:

International and chemical names: chloramphenicol; D-(-)-трео-1-пара-нитрофенил-2-дихлорацетиламино-пропандиол-1,3;основные physical and chemical properties: tablets of a round form, color, white or white with a yellowish shade, with a flat surface, risky and a facet. Existence of scarcely noticeable impregnations of yellow color is allowed; structure: 1 tablet contains chloramphenicol (levomycetinum) 500 mg in terms of 100% dry matter;
excipients: potato starch, calcium stearate.

Pharmacological properties:

Pharmacodynamics. Levomycetinum, an antibiotic of a broad spectrum of activity, possesses bacteriostatic action. In high concentration or in relation to highly sensitive microorganisms he can show bactericidal effect. Being fat-soluble, levomycetinum gets through a cellular membrane of bacteria and reversibly contacts subunit 50S of bacterial ribosomes in which movement of amino acids to the growing peptide chains is late (perhaps as result of oppression of activity of a peptidiltransferaza) therefore formation of peptide bonds and the subsequent synthesis of protein is broken.
It is active in relation to Escherichia coli, Shigella dysenteria spp., Shigella flexneri spp., Shigella boydii spp., Shigella sonnei spp., Salmonella spp., (including Salmonella typhi), affects Streptococcus spp. (including on Streptococcus pneumoniae), Neisseria gonorrhoeae, Neisseria meningitidis, a number of strains of Proteus spp., on some strains of Pseudomonas aeruginosa; active in relation to Ricketsia spp., Treponema spp., Chlamydia spp. (including Chlamydia trachomatis).
Does not affect Mycobacterium tuberculosis, pathogenic protozoa and mushrooms.
It is active in relation to strains of the bacteria resistant to penicillin, tetracyclines, streptocides. Stability of microorganisms develops slowly.
Due to the high toxicity Levomycetinum is used for treatment of heavy infections at which less toxic antibacterial agents are inefficient or contraindicated.

Pharmacokinetics. Quickly and almost it is completely soaked up from a digestive tract. Bioavailability at intake makes 80%. Time of achievement of the maximum concentration – 1 – 3 hour. Therapeutic concentration keeps 4 – 5 hours after administration of drug.
45 – 50% contact proteins. Well gets into liquids and body tissues, gets through a placenta, gets into breast milk. The greatest concentration of Levomycetinum are observed in a liver and kidneys. In bile about 30% of the entered dose are observed. Well gets through GEB: the maximum concentration in liquor is observed in 4 – 5 hours after single introduction inside. It Biotransformirutsya in a liver, 90% contact an inactive glucuronide. Chloramphenicol palmitate is hydrolyzed to a stand-at-ease in a digestive tract prior to absorption. Sodium chloramphenicol succinate is hydrolyzed to a stand-at-ease in a blood plasma, a liver, lungs and kidneys. At a fruit and premature children the liver is insufficiently developed to connect Levomycetinum that causes accumulation of toxic concentration of an active form of drug, and can lead to development of "a gray syndrome". Drug mainly with urine (preferential in the form of inactive metabolites), partially through intestines (1 – 3%) is removed.
The elimination half-life at adults with normal function of kidneys and a liver makes 1,5 – 3,5 hours, at an impaired renal function – 3 – 4 hours, at a heavy abnormal liver function – 4,6 – 11 hours.

Indications to use:

The infectious and inflammatory diseases caused by the microorganisms sensitive to Levomitsetin: typhoid, paratyphoid, shigellosis, brucellosis, salmonellosis, иерсиниоз, tularemia, pneumonia, sepsis, purulent peritonitis, meningitis, rickettsioses, clamidioses, chronic diseases of biliary tract. Drug is shown in cases of inefficiency of other antimicrobic means in connection with strong side effects.

Route of administration and doses:

Drug is accepted inside in 30 minutes prior to food, in case of nausea, by vomitings – in 1 hour after food. The mode of a dosage is set individually depending on disease severity, by conditions of the patient.
The adult appoint 250 – 500 mg 3 – 4 times a day. The daily dose makes 2 g. At severe forms of infections in the conditions of a hospital increase in a dose to 3 g a day is possible.
To children from 3 to 8 years appoint 150 – 200 mg in a single dose, 8 years – 200 – 300 mg are more senior. Frequency rate of reception 3 – 4 times a day.
The course of treatment usually makes 7 – 10 days. In need of and on condition of good tolerance, in the absence of changes in composition of peripheral blood, extension of a course of treatment up to 2 weeks is possible.

Features of use:

In the course of treatment it is necessary to control composition of peripheral blood, to watch a condition of a liver and kidneys.
At emergence of a leukopenia, thrombocytopenia, anemia or other pathological changes of blood Levomycetinum needs to be cancelled.
For forecasting of aplastic anemia clinical blood test does not make sense as it is usually shown after the end of treatment. Therefore such symptoms as pale skin, a pharyngalgia and the increased temperature, unusual bleedings, weakness (if they appear in several weeks or months after drug withdrawal), demand acute management.
At patients who were treated by cytostatic drugs earlier or applied radiation therapy, it is necessary to compare risk and advantage of treatment as Levomycetinum exponentiates risk of development of side effect.
The concomitant use of ethanol leads to development of disulfiramovy reaction (a dermahemia, tachycardia, nausea, vomiting, reflex cough, spasms).
Treatment should not be more long than the term necessary for obtaining effect, however it has to be rather long to exclude or minimize a possibility of a recurrence.
Unacceptably uncontrolled purpose of Levomycetinum and its use at easy forms of infectious processes, especially in pediatric practice.
There are no data that drug can negatively influence the drivers and people working with the equipment.
With care apply at cardiovascular diseases and tendency to allergic reactions.

Side effects:

At use of Levomycetinum can be observed:
- dispeptic phenomena (nausea, vomiting, diarrhea), irritation of mucous membranes of an oral cavity, pharynx;
- allergic reactions in the form of skin rashes, a dermatosis, a Quincke's disease;
- toxic impact on system of a hemopoiesis (a reticulocytopenia, an agranulotsitopeniya, anemia), in hard cases is possible development of aplastic anemia, thrombocytopenia, a leukopenia;
- intestinal microflora oppression, dysbacteriosis, consecutive fungal infections.
High doses of Levomycetinum can cause psychomotor frustration, confusion of consciousness, visual and auditory hallucinations, decrease in auditory acuity and sight, paralysis of eyeglobes.

Interaction with other medicines:

Long use of Levomycetinum which is inhibitor of enzymes of a liver during the preoperative period or during operation can reduce plazmovy clearance and prolong time of action of an alfetanil.
Simultaneous use of chloramphenicol with the drugs oppressing a hemopoiesis (cytostatics, streptocides, etc.), or with radiation therapy can strengthen their oppressing action on marrow.
At simultaneous use of Levomycetinum with Tolbutamidum (Butamidum) and Chlorproramidum their hypoglycemic effect can amplify (in connection with oppression of metabolism of these drugs in a liver and increase in their concentration) that demands correction of doses.
Long simultaneous use of Levomycetinum and estrogensoderzhashchy oral contraceptives can lead to decrease in reliability of contraception and increase in frequency of breakthrough bleedings.
At simultaneous use of Levomycetinum with penicillin, erythromycin, clindamycin, lincomycin mutual weakening of antimicrobic action therefore it is necessary to avoid their simultaneous use is observed.
Oppression by Levomycetinum of fermental system of R-450 cytochrome can weaken hepatic metabolism of phenobarbital, a fentoin, warfarin and other drugs, метаболизующихся oksidazny system of the mixed function that causes a delay of removal and increase in their concentration in blood.
At simultaneous use with B12 vitamin Levomycetinum can counteract stimulation of a hemogenesis B12 vitamin.

Contraindications:

The increased individual sensitivity (allergy) to Levomycetinum, a tiamfenikol, an azidamfenikol and other components of drug.
Blood diseases, the expressed abnormal liver functions, kidneys, deficit of enzyme glyukozo-6-fosfatdegidrogenazy, a skin disease (psoriasis, eczema, fungus diseases), pregnancy, a lactation, children under 3 years inclusive, an acute porphyria.
It is not necessary to appoint levomycetinum at acute respiratory diseases, quinsy, and also for the purpose of prevention.

Overdose:

Heavy complications from system of a hemopoiesis which are, as a rule, connected with use a long time of high doses (more than 3 g a day) – pale skin, a pharyngalgia and the increased temperature, unusual bleedings and hemorrhages, unusual fatigue or weakness.
The gray collapse which is observed preferential at newborns is especially dangerous, but at overdose it is possible also at children of advanced age or at especially sensitive people (abdominal distention, vomiting, a respiratory distress with a heavy metabolic acidosis, gray skin color, a cardiovascular collapse).
Treatment: drug withdrawal and purpose of symptomatic therapy, gastric lavage, purpose of enterosorbents.

Storage conditions:

To store in the unavailable to children, protected from light place at a temperature not above 25 °C.

Period of validity - 3 years.

Issue conditions:

According to the recipe

Packaging:

On 10 tablets in planimetric bezjyacheykovy packaging.