Tetracycline

General characteristics. Structure:

Active ingredient: 100 mg of tetracycline of a hydrochloride.

Tablet kernel excipients: starch potato grade "Extra", cellulose microcrystallic, sodium carboxymethylstarch, gelatin of 20 meshes, talc, calcium stearate, sugar (sucrose), twin-80 (polysorbate 80).

Excipients of a film cover: hypro rod, methyl cellulose-16, twin-80 (polysorbate 80), titanium dioxide, dye azoruby, dye tropeolin Oh, silicone emulsion of KE 10-16.

Pharmacological properties:

Pharmacodynamics. It is active concerning gram-positive microorganisms: Staphylococcus spp. (including Staphylococcus aureus, including the strains producing a penicillinase), Streptococcus pneumoniae, Listeria spp., Bacillus anthracis, Clostridium spp., Actinomyces israelii; gram-negative microorganisms: Haemophilus influenzae, Haemophilus ducreyi, Bordetella pertussis, Escherichia coli, Enterobacter spp. (including Enterobacter aerogenes), Acinetobacter spp., Klebsiella spp., Salmonella spp., Shigella spp., Yersinia pestis, Francisella tularensis, Bartonella bacilliformis, Vibrio cholerae, Vibrio fetus, Rickettsia spp., Borrelia burgdorferi, Brucella spp. (in a combination with streptomycin); at contraindications to use of penicillin - Clostridium spp., Neisseria gonorrhoeae, Actinomyces spp.; Chlamydia trachomatis, Chlamydia psittaci, Mycoplasma pneumoniae, Treponema spp is active also concerning Calymmatobacterium granulomatis.

Are steady against tetracycline: Pseudomonas aeruginosa, Proteus spp., Serratia spp., majority of strains of Bacteroides spp. and mushrooms, viruses, Streptococcus pyogenes, Streptococcus faecalis.

Pharmacokinetics. Absorption - 75-77%, at meal decreases, communication with proteins of plasma - 55-65%. Time of achievement of the maximum concentration of drug in plasma (TCmax) at oral administration - 2-3 h (for achievement of therapeutic concentration 2-3 days can be required). During the subsequent 8 h concentration gradually decreases. The maximum concentration of drug in plasma - 1.5-3.5 mg/l (for achievement of medical effect there is enough concentration of 1 mg/l).

In an organism it is distributed unevenly: the maximum concentration of drug decides in a liver, kidneys, lungs and in bodies on well developed reticuloendothelial system - a spleen, lymph nodes. Concentration in bile is 5-10 times higher, than in blood serum. In fabrics thyroid and a prostate concentration of tetracycline corresponds found in plasma; in pleural, ascitic liquid, saliva, milk of the feeding women - 60-100% of concentration in plasma. In large numbers collects in a bone tissue, fabrics of tumors, in dentine and enamel of milk teeth. Badly gets through a blood-brain barrier. At an intact meninx in cerebrospinal fluid it is not defined or found in insignificant quantity (5-10% of concentration in plasma). At patients with diseases of the central nervous system, especially at inflammatory processes in brain covers, concentration in cerebrospinal fluid makes 8-36% of concentration in plasma. Gets through a placental barrier and into breast milk. Distribution volume - 1.3-1.6 l/kg.

It is slightly metabolized in a liver. An elimination half-life of drug (T1/2) - 6-11 h, at an anury - 57-108 h. In urine it is found in high concentration in 2 h after reception and remains during 6-12 h; for the first 12 h kidneys remove about 10-20% of a dose. In smaller quantities (5-10% of the general dose) it is removed with bile in intestines where there is a partial return absorption that promotes long circulation of active agent in an organism (enterohepatic circulation). Removal through intestines - 20-50%. At a hemodialysis is removed slowly.

Indications to use:

The infectious diseases caused by microorganisms, sensitive to tetracycline: the pneumonia and respiratory infections caused by Mycoplasma pneumoniae, respiratory infections caused by Haemophilus influenzae and Klebsiella spp., bacterial infections of urinogenital bodies, infections of skin and soft tissues, ulcer and necrotic gingivostomatitis, conjunctivitis, acne rash, actinomycosis, intestinal amebiasis, malignant anthrax, brucellosis, bartonellosis, шанкроид, cholera, clamidiosis, uncomplicated gonorrhea, inguinal granuloma, venereal lymphogranuloma, listeriosis, plague, psittacosis, vesicular rickettsiosis, spotty fever of the Rocky Mountains, sapropyra, typhinia, syphilis, trachoma, tularemia, frambeziya.

Route of administration and doses:

Inside, washing down with a large amount of liquid, the adult - 0.5 g 4 times a day or on 0.5-1 g each 12 h. The maximum daily dose - 4 g. At acne rash: 0.5-2 g/days in the divided doses. In case of improvement of a state (usually in 3 weeks) the dose is gradually reduced to supporting - 0.5-1 g. Adequate remission of acne rash can be reached when using drug every other day or discontinuous therapy.

Brucellosis - 0.5 g each 6 h within 3 weeks, along with intramuscular administration of streptomycin in a dose of 1 g each 12 h within 1 week and 1 times a day within 2 weeks.

Uncomplicated gonorrhea: an initial single dose - 1.5 g, then on 0.5 g each 6 h within 4 days (a total dose of 9 g).

Syphilis - 0.5 g each 6 h within 15 days (early syphilis) or 30 days (late syphilis).

The uncomplicated urethral, endocervical and rectal infections caused by Chlamydia trachomatis - 0.5 g 4 times a day within not less than 7 days. To children 8 years - on 6.25-12.5 mg/kg each 6 h or on 12.5-25 mg/kg each 12 h are more senior.

Features of use:

Due to the possible development of a photosensitization insolation restriction is necessary. At long use periodic control of function of kidneys, a liver, bodies of a hemopoiesis is necessary. Can mask displays of syphilis in this connection, at a possibility of multi-infection, monthly carrying out serologic assay for 4 months is necessary.

All tetracyclines form resistant complexes with calcium ions in any kostnoobrazuyushchy fabric. In this regard inclusion in the period of development of teeth can become the reason of long-term coloring of teeth in yellow-gray-brown color, and also enamel hypoplasias.

For prevention of a hypovitaminosis it is necessary to appoint vitamins of group B and K, beer yeast.

Use at pregnancy and during breastfeeding. Contraindicated at pregnancy (tetracyclines pass through a placenta, collect in bones and dental germs of a fruit, breaking their mineralization, can cause heavy disturbances of development of a bone tissue). Category of action on a fruit on FDA — D.

For the period of treatment it is necessary to stop breastfeeding (tetracyclines get into breast milk and can negatively influence development of bones and child's teeth, and also to cause reactions of a photosensitization, candidiasis of an oral cavity and vagina in babies).

Influence on ability to control of vehicles or potentially dangerous mechanisms. There are no data on influence on speed of response at control of vehicles or work with mechanisms.

Side effects:

From the alimentary system: loss of appetite, vomiting, diarrhea, nausea, glossitis, esophagitis, gastritis, ulceration of a stomach and 12-perstny gut, hypertrophy of nipples of language, dysphagy, hepatotoxic action, increase in activity of "hepatic" transaminases, pancreatitis, intestinal dysbacteriosis, coloenteritis.

From a nervous system: increase in intracranial pressure, dizziness or instability, headache.

From bodies of a hemopoiesis: hemolitic anemia, thrombocytopenia, neutropenia, eosinophilia.

From an urinary system: azotemia, giperkreatininemiya.

Allergic and immunopathological reactions: makulopapulezny rash, dermahemia, Quincke's disease, anaphylactoid reactions, medicinal system lupus erythematosus, photosensitization.

Others: superinfection, candidiasis, hypovitaminosis In, a hyperbilirubinemia, discoloration of an adamantine substance of tooth at children, stomatitis.

Interaction with other medicines:

Due to the suppression of intestinal microflora reduces a prothrombin ratio (demands a dose decline of indirect antikoagulyatn).

Reduces efficiency of the bactericidal antibiotics breaking synthesis of a cell wall (penicillin, cephalosporins).

Reduces efficiency of estrogensoderzhashchy oral contraceptives and increases risk of development of bleedings of "break"; Retinolum - risk of development of increase in intracranial pressure.

Absorption is reduced by the antacids containing aluminum ions, ions of magnesium and calcium, iron preparations and Colestyraminum.

Chymotrypsin increases concentration and duration of circulation.

Contraindications:

Hypersensitivity to tetracycline, drug components, deficit of invertase/isomaltase, intolerance of fructose, glyukozo-galaktozny malabsorption, a renal failure, a leukopenia, pregnancy, the lactation period, children's age up to 8 years (up to 8 years tetracycline can cause long-term discoloration of teeth, an enamel hypoplasia, delay of longitudinal growth of bones of a skeleton in children).

With care. It is necessary to appoint drug with care the patient with the instruction to allergic reactions in the anamnesis.

Overdose:

Symptoms. Strengthening of dozozavisimy side effects is possible.

Treatment: symptomatic therapy.

Storage conditions:

In the dry place at a temperature not above 25 °C. In the place, unavailable to children. A period of validity - 3 years. Not to use after the expiry date specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Tablets, film coated 100 mg. On 10 tablets in a blister strip packaging. 2 blister strip packagings with the application instruction place in a pack from a cardboard.