Levomycetinum

General characteristics. Structure:

Active agent: levomycetinum - 0,25 or 0,5 g.

Excipients: potato starch, polyvinylpirrolidone low-molecular medical (povidone), stearic acid.

Description: tablets of color, white or white with a weak yellowish shade, ploskotsilindrichesky with a facet and risky.

Pharmacological properties:

Pharmacodynamics. The bacteriostatic antibiotic of a broad spectrum of activity, breaks process of synthesis of protein in a microbic cell. It is effective concerning strains of the bacteria steady against penicillin, tetracyclines, streptocides. It is active in the relation of many gram-positive and gram-negative bacteria, causative agents of purulent infections, a typhoid, dysentery, meningococcal infection: Escherichia coli,  Shigella dysenteria, Shigella flexneri spp.,  Shigella boydii spp., Shigella sonnei spp., Salmonella spp., (including Salmonella typhi, Salmonella paratyphi), Staphylococcus spp., Streptococcus spp., (including Streptococcus pneumoniae), Neisseria meningitidis,  Neisseria gonorrhoeae, number of strains of Proteus spp., Burkholderia pseudomallei; Rickettsia spp., Treponema spp., Leptospira spp., Chlamydia spp., (including Chlamydia trachomatis), Coxiella burnetii, Ehrlichia canis, Bacteroides fragilis, Klebsiella pneumoniae, Haemophilus influenzae. Does not affect acid resisting bacteria (including Mycobacterium tuberculosis), a pyocyanic stick, clostridiums, strains of stafilokokk, Acinetobacter, Enterobacter, Serratia marcescens, indolpositive strains of Proteus spp, steady against Methicillinum., Pseudomonas aeruginosa spp., protozoa and mushrooms. Stability of microorganisms develops  slowly.

Pharmacokinetics. Absorption – 90% (bystry and almost full). Bioavailability – 80%. Communication with proteins of plasma – 50-60% Time of achievement of the maximum concentration after oral administration - 1-3 h. Distribution volume - 0,6-1,0 l/kg. Therapeutic concentration in blood remains within 4-5 hours after reception. Well gets into  liquids  and body tissues. The greatest concentration  are created in a liver and kidneys. In bile about 30% of the entered dose are found. The maximum concentration  in cerebrospinal fluid is defined by 4-5 h after single introduction inside  and can reach  at an uninflammed meninx 21-50%  of the maximum concentration in plasma and 45-89% - at the inflamed meninx. Passes through a placental barrier, concentration in blood serum of a fruit can make 30-80% of concentration in mother's blood. Gets into breast milk. The main quantity (90%) is metabolized in a liver. In intestines  under the influence of colibacilli it is hydrolyzed with formation  of inactive metabolites. It is removed during  24 h by kidneys – 90% (by glomerular filtering  - 5 – 10% in an invariable look, by calcic secretion in the form of inactive metabolites – 80%), through intestines - 1 – 3%. An elimination half-life at adults – 1,5-3,5 h, at a renal failure – 3-11 h. An elimination half-life at children – from 1 month to 16 years – 3-6,5 h. Poorly is exposed to a hemodialysis. 

Indications to use:

The diseases caused by sensitive microorganisms including brain abscess, typhoid, paratyphoid, salmonellosis (mainly, generalized forms) dysentery, a brucellosis, a tularemia, Ku's fever,  a meningococcal infection, rickettsioses (including a sapropyra, trachoma, spotty fever of the Rocky Mountains), an inguinal lymphogranuloma, clamidioses, iyersinioza, эрлихиоз, infections of urinary tract, a purulent  wound fever, pneumonia, purulent peritonitis, infections of biliary tract, purulent otitis.

Route of administration and doses:

Inside in 30 min. prior to food.

The adult - on 0,25-0,5 g 3-4 times a day. A daily dose – 2 g. At severe forms of an infection in the conditions of a hospital increase in a dose to 3-4 g/days is possible (the maximum daily dose for adults, under strict control of a condition of blood and function of a liver and kidneys).

The single dose of drug for children from 3 to 8 years – 0,15-0,2 g, is more senior than 8 years on 0,2-0,3 g.

Frequency rate of reception – 3-4 times a day.

The course of treatment makes 7-10 days.

Features of use:

Owing to high toxicity it is not recommended without need to apply to treatment and prevention of banal infections, catarrhal diseases, flu, pharyngitis, a bacteriocarrier. Heavy complications from the hemopoietic system are, as a rule, connected using high doses (more than 4 g/days) a long time.

At a concomitant use of alcohol development of disulfiramovy reaction is possible (a hyperemia of integuments, tachycardia, nausea, vomiting, reflex cough, spasms).

In the course of treatment systematic control of a picture of peripheral blood is necessary.

Side effects:

From the alimentary system: irritation of a mucous membrane of an oral cavity and pharynx, dyspepsia, nausea, vomiting (the probability of development decreases at reception in 1 h after food), diarrhea, dermatitis, dysbacteriosis (suppression of normal microflora).

From bodies of a hemopoiesis: reticulocytopenia, leukopenia, granulocytopenia, thrombocytopenia, erythrocytopenia; seldom – aplastic anemia, an agranulocytosis.

From a nervous system: psychomotor frustration, depression, confusion of consciousness, peripheral neuritis, optic neuritis  , visual and auditory hallucinations, decrease in visual acuity and hearing, headache.

Allergic reactions: skin rash, Quincke's disease.

Others: consecutive fungal infection.

Interaction with other medicines:

At simultaneous use with phenobarbital, Phenytoinum, indirect anticoagulants weakening of metabolism  of these HP, delay  of removal and increase in their concentration in plasma is noted (suppresses fermental system of P450 cytochrome).

At simultaneous use with the drugs oppressing a marrowy hemopoiesis with radiation therapy, the risk of development of side effect increases.

At simultaneous use with erythromycin, clindamycin, lincomycin mutual weakening of action is noted because levomycetinum can force out these drugs from the connected state or interfere with their linkng with subunit 50S of bacterial ribosomes.

At a concomitant use of ethanol development of disulfiramovy reaction is possible.
Reduces antibacterial effect of penicillin and cephalosporins. Myelotoxic HP strengthen manifestations of a gematotoksichnost of drug.

At appointment with peroral hypoglycemic drugs strengthening of their action due to suppression of metabolism of these drugs in a liver and increases in their concentration in a blood plasma is noted.

Contraindications:

Oppression of a marrowy hemopoiesis, individual hypersensitivity to drug components, an acute intermittent porphyria, skin diseases (psoriasis, eczema, fungal infections), pregnancy and  the period of a lactation, children's age up to 3 years, the expressed abnormal liver functions and/or kidneys, deficit of enzyme glyukozo-6-fosfatdegidrogenazy.

With care appoint chloramphenicol to the patients receiving earlier treatment by cytostatic drugs or radiation therapy.

Overdose:

Adults have no data on overdose.

Storage conditions:

List B. In the place protected from light. In places unavailable to children. Period of validity of 5 years. Not to use after the term specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Tablets on 0,25 g and 0,5 g.

On 10 tablets in planimetric bezjyacheykovy packaging  or a strip packaging.

2 blister strip packagings with the application instruction place in a pack from a cardboard.

600 planimetric bezjyacheykovy or 1000 blister strip packagings with application instructions place in a box from a cardboard (for hospitals).