Levomycetinum Aktitab

General characteristics. Structure:

Active ingredient: 250 mg or 500 mg of chloramphenicol in 1 tablet.

Excipients: silicon dioxide colloid (aerosil), cellulose microcrystallic, povidone, кросповидон, calcium stearate, for a dosage of 250 mg - опадрай II (series 85) [polyvinyl alcohol, a macrogoal, talc, titanium dioxide, ferrous oxide yellow, ferrous oxide red, ferrous oxide black], for a dosage of 500 mg – опадрай II (series 85) [polyvinyl alcohol, a macrogoal, talc, titanium dioxide, an aluminum varnish on the basis of quinolinic yellow, an aluminum varnish on the basis of indigo carmine].

Antibiotic of a broad spectrum of activity.

Pharmacological properties:

Pharmacodynamics. The bacteriostatic antibiotic of a broad spectrum of activity, breaks process of synthesis of protein in a microbic cell at a stage of transfer of amino acids t-RNK on ribosomes.

It is effective concerning strains of the bacteria steady against penicillin, tetracyclines, streptocides.

It is active concerning the following microorganisms: Escherichia coli, Shigella dysenteria, Shigella flexneri spp., Shigella boydiispp., Shigellasonnei, Salmonellaspp. (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), anaerobe bacterias, strains of stafilokokk, Acinetobacter spp, steady against Methicillinum., Enterobacter spp., Serratia marcescens, indolpositive strains of Proteus spp., Pseudomonas aeruginosa spp., protozoa and mushrooms. Stability of microorganisms develops slowly.

Pharmacokinetics. After reception communication with proteins of plasma makes – 50-60%. Time of achievement of the maximum concentration (TCmax) after reception – 1-3 h. Distribution volume – 0,6-1,0 l/kg. Therapeutic concentration in blood remains during 4-5 h after reception. Well gets into liquids and body tissues. Its greatest concentration are created in a liver and kidneys. In bile about 30% of the entered dose are found. The maximum concentration (Cmax) in cerebrospinal fluid is defined by 4-5 h after a single dose and can reach in the absence of an inflammation of a meninx 21-50% of Cmax in plasma and 45-89% – in the presence of an inflammation of a meninx. Passes through a placental barrier, concentration in blood serum of a fruit can make 30-80% of that mother in 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 not changed look, by canalicular secretion in the form of inactive metabolites – 80%), through intestines – 1-3%. Adults – 1,5-3,5 h, at a renal failure - 3-11 p. T1/2 have an elimination half-life (T1/2) at children – 3,0-6,5 h. It is poorly removed during a hemodialysis.

Indications to use:

The infections of urinary and biliary tract caused by sensitive microorganisms.

Apply to treatment of the infectious and inflammatory diseases caused by microorganisms, sensitive to chloramphenicol, including: typhoid, paratyphoid, dysentery, tularemia, whooping cough, sapropyra and other rickettsioses; pneumonia, meningitis, sepsis, osteomyelitis. It is used for topical administration in ophthalmology: inflammatory diseases of eyes.

Route of administration and doses:

Inside (in 30 min. prior to food, and at development of nausea and vomiting – in 1 h after food), 3-4 times a day. A single dose for adults – 0,25-0,5 g, daily – 2 g. At severe forms of infections (in the conditions of a hospital) increase in a dose to 3-4 g/days is possible (under control of a condition of blood, function of kidneys and a liver).

To children is more senior than 3 years and/or with a body weight more than 20 kg each 6 h or on 25 mg each 12 h appoint 12,5 mg/kg, at the heavy course of infections – to 75-100 mg/kg/days (under control of concentration of drug in blood serum).

The average duration of treatment – 8-10 days.

Features of use:

Heavy complications from the hemopoietic system are, as a rule, connected using high doses a long time.

At a concomitant use of ethanol development of disulfiramopodobny reaction is possible (a hyperemia of the person, a spasm in a stomach and in a stomach, nausea, vomiting, a headache, a lowering of arterial pressure, tachycardia, short wind).

Side effects:

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

Suppresses fermental system of P450 cytochrome therefore at simultaneous use with phenobarbital, Phenytoinum, indirect anticoagulants note weakening of metabolism of these medicines, delay of removal and increase in their concentration in plasma.

Reduces antibacterial effect of penicillin and cephalosporins. At simultaneous use with erythromycin, clindamycin, lincomycin mutual weakening of action is noted because chloramphenicol can force out these medicines from the connected state or interfere with their linkng with subunit 50S of bacterial ribosomes.

Co-administration with the medicines oppressing a hemopoiesis (streptocides, cytostatics), influencing a metabolism in a liver with radiation therapy increases risk of development of side effect.

At appointment with peroral hypoglycemic HP strengthening of their action is noted (due to suppression of metabolism in a liver and increases in their concentration in plasma).

Myelotoxic medicines strengthen manifestations of a gematotoksichnost of drug.

Contraindications:

Hypersensitivity, oppression of a marrowy hemopoiesis, acute intermittent porphyria, deficit glyukozo-6-fosfatdegidrogenazy, liver and/or renal failure, skin diseases (psoriasis, eczema, fungal infections), pregnancy, the lactation period, children's age up to 3 years and/or body weight is less than 20 kg.

With care: To the patients receiving earlier treatment by cytostatic drugs or radiation therapy.

Overdose:

Symptoms: nausea, vomiting.

Treatment: gastric lavage, symptomatic therapy, hemosorption.

Storage conditions:

List B. To store in the dry, protected from light place, at a temperature not above 25 °C. To store in the place, unavailable to children! Term a godnostiya - 2 years. Not to use after the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Tablets, film coated, 250 mg and 500 mg. On 10, 12 or 15 tablets in a blister strip packaging from a film of the polyvinyl chloride or import and printing aluminum foil varnished or import. On 1, 2, 3, 4, 5 or 6 blister strip packagings together with the application instruction place in a pack from a cardboard.