Description
Tetracycline Pharmacodynamics
Bacteriostatic antibiotic of tetracycline group. Disrupts formation of the complex between transport RNA and ribosome, which leads to suppression of protein synthesis.
Active against Gram-positive microorganisms: Staphylococcus spp. (including Staphylococcus aureus, including penicillinase-producing strains), Streptococcus pneumoniae, Listeria spp., Bacillus anthracis, Clostridium spp., Actinomyces israelii.
Gram-negative microorganisms: Haemophilus influezae, Haemophilus ducreyi, Bordetella pertussis, Escherichia coli, Enterobacter spp. (including Enterobacter aerogenes), Acinetobacter spp., Klebsiella spp, Yersinia pestis, Francisella tularensis, Bartonella bacilliformis, Vibrio cholerae, Vibrio fetus, Rickettsia spp., Brucella spp. (in combination with streptomycin); in case of contraindications to use of drugs of penicillin group – Neisseria gonorrhoeae, Actinomyces spp. It is also active against Calymmatobacterium granulomatis, Chlamydia trachomatis, Chlamydia psittaci, Mycoplasma pneumoniae, Treponema spp.
Pseudomonas aeruginosa, Proteus spp., Serratia spp., most strains of Bacteroides spp. and fungi, viruses, Streptococcus pyogenes, Streptococcus faecal is resistant to tetracycline.
Indications
Infectious and inflammatory diseases caused by microorganisms sensitive to tetracycline: pneumonia and respiratory tract infections caused by Mycoplasma pneumoniae, respiratory tract infections caused by Haemophilus influenzae and Klebsiella spp, Bacterial infections of urogenital organs, skin and soft tissue infections, ulcerative necrotizing gingivostomatitis, conjunctivitis, acne, actinomycosis, intestinal amebiasis, anthrax, brucellosis, bartonellosis, chancroid, cholera, chlamydia, uncomplicated gonorrhea, inguinal granuloma, venereal lymphogranuloma, listeriosis, plague, psittacosis, vesicular rickettsiosis, Rocky Mountain spotted fever, typhus, syphilis, trachoma, tularemia, yaws.
Contraindications
Hypersensitivity to tetracycline, other components of the drug, pregnancy, lactation, children (under 8 years), leukopenia, renal insufficiency (creatinine clearance less than 50 ml/min), liver function abnormality, acute porphyria, systemic lupus erythematosus, simultaneous use with vitamin A and retinoids.
Caution
Renal insufficiency (creatinine clearance more than 50 ml/min), patients with a history of allergic reactions, concomitant use with hepatotoxic drugs.
Administration during pregnancy and breast-feeding
Contraindicated in pregnancy (tetracyclines pass through the placenta, accumulate in the bones and teeth embryos, disrupting their mineralization, and can cause severe disorders of bone development). Contraindicated during breastfeeding (tetracyclines penetrate into breast milk and can adversely affect the development of bones and teeth of the child, as well as cause photosensitization reactions, oral cavity and vaginal candidiasis in infants.
Dosage and administration
- Orally, with plenty of fluid, for adults – 0.3 – 0.5 g 4 times a day, or 0.5 – 1.0 g every 12 hours. The maximum daily dose is 2 g. The course of treatment is 5-10 days.
- For acne: 0.5-2 g/day in divided doses. If condition improves (usually after 3 weeks), the dose is gradually reduced to a maintenance dose of 0.1-1 g. Adequate remission of acne can be achieved by using the drug every other day or by intermittent therapy.
- Brucellosis – 0.5 g every 6 h for 3 weeks, concomitantly with intravenous streptomycin administration at a dose of 1 g every 12 h for 1 week and once daily for 2 weeks.
- Uncomplicated gonorrhea: initial single dose – 1.5 g, then 0.5 g every 6 h for 4 days (total dose of 9 g).
- Syphilis: 0.5 g every 6 hours for 15 days (early syphilis) or 30 days (late syphilis).
- Uncomplicated urethral, endocervical and rectal infections caused by Chlamydia trachomatis – 0.5 g 4 times a day for at least 7 days.
- In children over 8 years old the dose is prescribed at the rate of 20-25 mg/kg of body weight every 6 hours.
- In renal failure: a single dose of 0.3-0.5 g, depending on renal function, in creatinine clearance (CK) 80-50 ml/min, the dosing interval is 6 hours; in CK less than
- 50 ml/min is contraindicated.