Tetracycline
Producer: RUP of Belmedpreparata Republic of Belarus
Code of automatic telephone exchange: J01AA07
Release form: Firm dosage forms. Tablets.
General characteristics. Structure:
Active ingredient: 1 tablet, coated, contains 100 mg of tetracycline.
Excipients: sucrose, starch corn, talc, magnesium carbonate the main, dextrin, calcium stearate, gelatin, acid red 2C, tropeolin O.
Tetracycline is an antibiotic of a broad spectrum of activity.
Pharmacological properties:
Pharmacodynamics. A bacteriostatic antibiotic from group of tetracyclines. Breaks formation of a complex between acceptor RNA and a ribosome that leads to disturbance of synthesis of protein. It is active concerning gram-positive microorganisms - Staphylococcus spp. (including Staphylococcus aureus, including the strains producing a penicillinase), Streptococcus spp. (some strains, including Streptococcus pneumoniae), at contraindications to purpose of penicillin - Listeria spp. Bacillus anthracis;
Microorganisms are steady against tetracycline: Pseudomoivas aeruginosa, Proteus spp., Serratia spp., majority of strains of Bacteroides spp. and mushrooms, small viruses, beta and hemolitic streptococci of group A (including 44% of strains of Streptococcus pyogenes and 74% of strains of Streptococcus faecalis).
Pharmacokinetics. Absorption - 75-77%, at meal decreases, communication with proteins of plasma - 55-65%. Time of achievement of the maximum concentration 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 - 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: in the maximum concentration contains in a liver, kidneys, lungs and in bodies with the endothelial system which is well developed retikulo-a spleen, lymph nodes. Concentration in bile is 5-10 times higher, than in blood serum. In fabrics thyroid and a prostate the content of tetracycline same, as 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. Badly gets through a blood-brain barrier. At an intact meninx in cerebrospinal fluid it is not defined or found in insignificant quantity (510% 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 - 6-11 h, at an anury of-57-108 h. In urine it is found in high concentration in 2 h after introduction and remains during 6-12 h; for the first 12 h kidneys remove about 10-20% of a dose. In smaller quantities (510% 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:
Drug is appointed sick bronchitis, pneumonia, pleurisy, a subacute septic endocarditis, applied at an actinomycosis, an ulitis, stomatitis, average otitis, pharyngitis, sinusitis, purulent meningitis, cholecystitis, quinsy, scarlet fever, whooping cough, bacterial and amoebic dysentery, a brucellosis, a tularemia, sypny and a typhinia, a psittacosis, gonorrhea, syphilis, at infectious diseases of urinogenital ways, infections of skin and soft tissues, and also at other infectious diseases caused by the microorganisms sensitive to this antibiotic. Tetracycline can also be applied to the prevention of infectious complications at surgical patients.
Route of administration and doses:
Inside, washing down with a large amount of liquid, the adult - 0.25-0.5 g 4 times a day, or on 0.5-1 g each 12 h. The maximum daily dose - 4 g. 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. 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 - 0.125-1 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 during 3 weeks, along with intramuscular administration of streptomycin in a dose of 1 g each 12 h within the first week and 1 times a day within the second week.
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.
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 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.
Side effects:
From the alimentary system: anorexia, vomiting, diarrhea, nausea, glossitis, esophagitis, gastritis, ulceration of a stomach and duodenum, hypertrophy of nipples of language, dysphagy, hepatotoxic action, pancreatitis, intestinal dysbacteriosis, increase in activity of "hepatic" transaminases.
From a nervous system: increase in intracranial pressure, toxic action on TsNS (dizziness or instability).
From bodies of a hemopoiesis: hemolitic anemia, thrombocytopenia, neutropenia.
From an urinary system: azotemia, giperkreatininemiya.
Allergic and immunopatologochesky reactions: makulo-papular rash, dermahemia, Quincke's disease, anaphylactoid reactions, medicinal lupus erythematosus, photosensitization.
Others: superinfection, candidiasis, a group B vitamin deficiency, a hyperbilirubinemia, discoloration of an adamantine substance of tooth at children.
Interaction with other medicines:
Absorption is reduced by the antacids containing aluminum, magnesium and calcium, iron preparations and Colestyraminum. 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).
Chymotrypsin increases concentration and duration of circulation.
Reduces efficiency of estrogensoderzhashchy oral contraceptives and increases risk of development of bleedings of "break"; Retinolum - risk of development of increase in intracranial pressure.
Contraindications:
Use of tetracycline at hypersensitivity to it and related is contraindicated to it to antibiotics, at fungus diseases, at the expressed abnormal liver functions and kidneys, during pregnancy, to a lactation (for treatment it is necessary to refuse breastfeeding), children up to 8 years.
Storage conditions:
List B. In the dry, protected from light place, at a temperature not above 25 °C. To store in the place, unavailable to children. Period of validity 3 years. Not to use after expiry date.
Issue conditions:
According to the recipe
Packaging:
Tablets, coated, on 0,1g. On 10 tablets in a blister strip packaging; on two blister strip packagings together with the application instruction place in a pack from a cardboard.
