Expiration date: 01/2025
Formdata:
Bacteriostatic antibiotic of the tetracycline group. Disrupts the formation of the complex between transfer RNA and the ribosome, leading to inhibition of protein synthesis.
Active against gram-positive bacteria: Staphylococcus spp. (including Staphylococcus aureus, including penicillinase-producing strains), Streptococcus spp. (including Streptococcus pneumoniae), Listeria spp., Bacillus anthracis, Clostridium spp., Actinomyces israelii;
gram-negative microorganisms: Haemophilus influenzae, Haemophilus ducreyi, Bordetella pertussis, the majority of Enterobacteriaceae: Escherichia coli, Enterobacter spp., including Enterobacter aerogenes, Klebsiella spp., Salmonella spp., Shigella spp. Yersinia pestis, Bartonella bacilliformis, Vibrio cholerae, Vibrio fetus, Rickettsia spp. Borrelia burgdorferi, Brucella spp. (in combination with streptomycin);
if contraindications for prescription of penicillins - Clostridium spp. Neisseria gonorrhoeae, Actinomyces spp.; it is also active against causative agents of venereal and inguinal lymphogranuloma, Treponema spp.
Tetracycline resistant organisms: Pseudomonas aeruginosa, Proteus spp., Serratia spp. most strains of Bacteroides spp. and fungi, viruses, beta-hemolytic Streptococcus group A (including 44% of strains of Streptococcus pyogenes and 74 percent of strains of Streptococcus faecalis).
Pharmacokinetics:
Absorbance is 75-77%, while food intake decreases, the relationship blood plasma is 55-65%. TCmax after oral administration is 2-3 hours (to achieve a therapeutic concentration may require 2-3 days). Over the next 8 h, the concentration gradually decreases. Cmax = 1.5-3.5 mg/l (to achieve a therapeutic effect enough concentration of 1 mg/l).
In the body is distributed unevenly: Cmax determined in liver, kidney, lungs and organs with a well-developed RES - spleen, lymph nodes. Concentration of bile 5-10 times higher than in serum.
In the tissues of the thyroid, the prostate, the concentration of tetracycline meets detectable in plasma; pleural, ascitic fluid, saliva, and milk of nursing women is 60-100% of plasma concentration.
In large amounts it accumulates in bone tissue, the tissues of the tumors in the enamel and dentine of deciduous teeth.
Poor permeates through GEB. When intact meninges in the CSF is not detected or detected in small amounts (5-10% of plasma concentrations). In patients with CNS diseases, especially in inflammatory processes in the meninges, concentrations in CSF is 8-36% of the concentration in plasma.
Penetrates through the placental barrier and in breast milk. The volume of distribution is 1.3-1.6 l/kg.
Slight metabolised in the liver. T1/2 - 6-11 h, when anurii - 57-108 h In the urine is found in high concentrations after 2 h after administration and lasts for 6-12 h; for the first 12 hours the news is up to 10-20% of the dose. In smaller amounts (5-10% of the total dose) is excreted in the bile into the intestine, where there is a partial reverse suction that facilitates long circulation of the active substance in the body (enterohepatic circulation).
Excretion through the intestine is 20-50%. During hemodialysis is removed slowly.
Indications:
Infectious diseases caused by sensitive pathogens:
pneumonia and respiratory tract infections caused by Mycoplasma pneumoniae,
respiratory tract infections caused by Haemophilus influenzae and Klebsiella spp.
bacterial infection of the urinary organs,
infections of skin and soft tissue, ulcerative and necrotic gingivostomatitis, conjunctivitis, acne, actinomycosis,
intestinal amebiasis, anthrax, brucellosis, bartonellosis, chancroid, cholera, chlamydia,
uncomplicated gonorrhea, inguinal granuloma, lymphogranuloma venereum, listeriosis, plague, fever, vesicular rickettsiosis, Rocky mountain spotted fever, typhus, relapsing fever, syphilis, trachoma, tularemia, yaws.
Contraindications:
Hypersensitivity, pregnancy (II-III trimester), lactation, children's age (till 8 years), leukopenia.
With caution. Renal failure.
Dosing:
Inside, squeezed liquid, adults - 0.25-0.5 g 4 times a day or 0.5-1 g every 12 hours Maximum daily dose - 4 g
For acne: 0.5-2 g/day in divided doses. In the case of improvement (usually 3 weeks) the dose was gradually reduced to a maintenance - 0.125-1 g. Adequate remission of acne can be achieved using the drug in a day or intermittent therapy.
Brucellosis - 0.5 g every 6 h for 3 weeks, simultaneously with the/m introduction of streptomycin in doses of 1 g every 12 h for 1 week and 1 times a day for 2 weeks.
Uncomplicated gonorrhea: an initial single dose of 1.5 g, followed by 0.5 g every 6 h for 4 days (total dose 9 g).
Syphilis - 0.5 g every 6 h for 15 days (early syphilis) or 30 days (late syphilis).
Uncomplicated urethral, endocervical or rectal infection caused by Chlamydia trachomatis - 0.5 g 4 times a day for at least 7 days.
Children over 8 years - 6.25-12.5 mg/kg every 6 h or 12.5-25 mg/kg every 12 h
