Tetracycline, 100 mg 20 pcs.

Pharmacotropic group: antibiotic, tetracycline.

TATX code: [J01AA07].

Pharmacokinetics

Absorption – 75-77%, decreases with food, binding to plasma proteins – 55-65%.

The time to reach maximum concentration when taken orally is 2-3 hours (it may take 2-3 days to reach therapeutic concentration). Over the next 8 hours the concentration gradually decreases. Maximum concentration is 1.5-3.5 mg/l (a concentration of 1 mg/l is sufficient to achieve therapeutic effect).

In the body it is distributed unevenly: the maximum concentration is contained in the liver, kidneys, lungs and in organs with a well developed reticuloendothelial system – spleen, lymph nodes. The concentration in bile is 5-10 times higher than in blood serum. In thyroid and prostate tissues tetracycline content is the same as in plasma; in pleural, ascitic fluid, saliva, milk of lactating women – 60-100% concentration in plasma. It accumulates in large quantities in bone tissue, tumor tissues, dentin and enamel of deciduous teeth. It penetrates poorly through the blood-brain barrier. In intact cerebral membranes in the cerebrospinal fluid is not determined or detected in insignificant amounts (5-10% of the concentration in plasma). In patients with diseases of the central nervous system, especially in inflammatory processes in the brain membranes, the concentration in cerebrospinal fluid is 8-36% of the plasma concentration. It penetrates through the placental barrier and into breast milk. Volume of distribution is 1.3-1.6 l/kg.

It is slightly metabolized in the liver. The elimination half-life is 6-11 hours; in anuria it is 57-108 hours. It is detected in high concentration in urine within 2 hours after intake and retained for 6-12 hours; during the first 12 hours up to 10-20% of dose is excreted by kidneys. Smaller amounts (5-10% of the total dose) are excreted with bile in the intestine, where it is partially reabsorbed, which allows for prolonged circulation of the active substance in the body (intestine-hepatic circulation). Excretion through the intestine is 20-50%. With hemodialysis it is removed slowly.

Pharmacodynamics

Bacteriostatic antibiotic of tetracycline group. It 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 spp. (some strains, including Streptococcus pneumoniae), Listeria monocytogenes, Bacillus anthracis, Clostridium spp, Actinomyces spp., Propionibacterium acnes, Bacillus fusiformis;

Gram-negative microorganisms – Haemophilus influenzae, Haemophilus ducreyi, Bordetella pertussis, Escherichia coli, Enterobacter spp. (including Enterobacter aerogenes), Klebsiella spp, Neisseria gonorrhoeae, Shigella spp, Yersinia pestis, Bartonella bacilliformis, Vibrio cholerae, Vibrio fetus, Rickettsia prowazekii, Rickettsia rickettsii, Rickettsia akari, Borrelia Vinceni, Borrelia recurrentis, Borrelia burgdorferi, Brucella spp. (in combination with streptomycin); Calymmatobacterium granulomatis, Francisella tularensis, Treponema pallidum, Treponema pertenue;

In case of contraindications to the administration of penicillins – Clostridium spp, Neisseria gonorrhoeae, Actinomyces spp;

Active against Chlamydia trachomatis; Chlamydia psittaci, Entamoeba histolytica;

Tetracycline-resistant microorganisms: Pseudomonas aeruginosa, Proteus spp; Serratia spp, most strains of Bacteroides spp. and fungi, viruses, group A beta-haemolytic streptococci (including 44% of Streptococcus pyogenes strains and 74% of Streptococcus faecalis strains).

Indications

Active ingredient

Composition

One tablet contains:

The active ingredient:

Tetracycline hydrochloride (in terms of the active ingredient) – 100.00 mg.

Excipients:

Saccharose (white sugar), calcium stearate, talc, gelatin, potato starch.

The film coating:

Hypromellose (oxypropyl methylcellulose), lactose monohydrate (milk sugar), polysorbate 80 (tween-80), dye azorubin (acid red 2C, carmoisin).

How to take, the dosage

Overly with plenty of fluid.

Adults – 0.3-0.5 g every 6 hours (4 times a day) or 0.5-1 g every 12 hours (2 times a day). The maximum daily dose is 4 g. The course of treatment is 5-10 days.

In children over 8 years of age – 6.25-12.5 mg/kg every 6 hours or 12.5-25 mg/kg every 12 hours.

In acne: 0.5-2 g/day in divided doses. If the 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 intermittent therapy.

Brucellosis – 0.5 g every 6 hours for 3 weeks, simultaneously with intramuscular administration of streptomycin at a dose of 1 g every 12 hours for 1 week and once daily for 2 weeks.

Uncomplicated gonorrhea – initial single dose of 1.5 g, then 0.5 g every 6 hours 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 every 6 hours for at least 7 days.

Lyme disease (early stage only) – 1.0-1.5 g daily for 10-14 days.

Listeriosis – 0.2-0.3 g every 6 hours for 7-10 days.

Actinomycosis – 3 g per day for the first 10 days, then 0.5 g every 6 hours for the last 18 days.

Chlamydia – 1.5-2 g per day for 10 days (“fresh” forms) and 15-20 days (chronic, complicated forms).

In inguinal granuloma, venereal lymphogranuloma – 0.5 g every 6 hours for 3-4 weeks.

Psittacosis – 0.5 g every 6 hours (relief and disappearance of symptoms occurs after 24-48 hours). Treatment is continued for 7-14 days after normalization of body temperature in order to prevent relapse.

Vesicular rickettsiosis – 0.8-1.2 g per day for 8-10 days.

Tularemia – 1.5-2 g per day. After normalization of temperature the treatment is continued for 5-7 days more.

Frambiesia – 0.5 g every 6 hours for 14 days.

Pestilence – up to 6 g per day. If the condition improves, the dose is reduced to 2 g per day until the temperature normalizes, but for at least 3 days. Contact persons should be given a course of 0.3 g every 6 hours.

Interaction

Due to the suppression of intestinal microflora, reduces the prothrombin index (requires reducing the dose of indirect anticoagulants).

Decreases the effectiveness of bactericidal antibiotics that disrupt cell wall synthesis (penicillins, cephalosporins).

Decreases the effectiveness of estrogen-containing oral contraceptives and increases the risk of breakthrough bleeding; retinol – the risk of developing increased intracranial pressure.

Absorption is reduced by antacids containing aluminum, magnesium and calcium, iron preparations and colestyramine.

Chymotrypsin increases the concentration and duration of circulation.

Special Instructions

Possible development of photosensitization requires limitation of insolation.

Long-term use requires periodic monitoring of kidney, liver and hematopoietic function.

May mask the manifestations of syphilis, therefore, if there is a possibility of mixed infection, serological testing should be performed monthly for 4 months.

All tetracyclines form persistent complexes with calcium ions in any bone-forming tissue. Because of this, taking it during the period of tooth development can cause long-term yellow-gray-brown staining of teeth, as well as enamel hypoplasia.

B and K vitamins and brewer’s yeast should be prescribed to prevent hypovitaminosis.

Impact on the ability to drive vehicles or operate potentially dangerous machinery

There are no data on the effect on reaction rate when driving vehicles or operating machinery.

Contraindications

Side effects

Digestive system disorders: decreased appetite, vomiting, diarrhea, nausea, glossitis, esophagitis, gastritis, gastric and duodenal ulceration, hypertrophy of papillae of the tongue, dysphagia, hepatotoxic effect, pancreatitis, intestinal disbacteriosis, enterocolitis, increased activity of “liver” transaminases, antibiotic-associated diarrhea.

Central nervous system disorders: increased intracranial pressure, headache, toxic effects on the central nervous system (dizziness or unsteadiness).

Hematopoietic disorders: hemolytic anemia, thrombocytopenia, neutropenia, eosinophilia.

More urinary system disorders: azotemia, hypercreatininemia, nephrotoxic effect.

Allergic and immunopathological reactions: maculopapular rash, skin hyperemia, angioedema, anaphylactoid reactions, drug-induced systemic lupus erythematosus, photosensitization.

Other: superinfection, candidiasis, vitamin B hypovitaminosis, hyperbilirubinemia, discoloration of dental enamel in children, stomatitis.

Overdose

The dose-dependent side effects may increase.

Treatment: symptomatic therapy.

Pregnancy use

Contraindicated in pregnancy (tetracyclines pass through the placenta, accumulate in the bones and dental buds of the fetus, disturbing their mineralization, can cause severe disorders of bone development).

The FDA fetal category is D.

Breast-feeding must be stopped for the duration of treatment (tetracyclines penetrate into the breast milk and can have adverse effects on the development of baby’s bones and teeth, and cause photosensitization reactions and oral and vaginal candidiasis in babies).

Similarities