Tetracycline, 100 mg 20 pcs.

Pharmacotherapeutic group

Antibiotic, tetracycline

ATCode

J01AA07

Pharmacodynamics:

Bacteriostatic antibiotic from the tetracycline group. It disrupts formation of the complex between transporter 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 fusifonnis;

– 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 prawazekii-Rickettsia reckettsn Rickettsia akari Borrelia Vinceni Borrelia “recurrentis Borrelia burgdorferi Brucella spp. (in combination with streptomycin); Calymmatobacterium granulomatis’ Francisella tularensis Treponema pallidum Treponema pertenue;

– when contraindicated for the administration of penicillins – Clostridiumspp. Neisseria gonorrhoeae Actinomyces spp.;

– active against Chlamydia trachomatis; Chlamydia psittaci Entamoeba histolytica;

– microorganisms resistant to tetracycline: Pseudomonas aeruginosa Proteus spp.

– Serratia spp. most strains of Bacteroides. spp. and beta-haemolytic viruses fungi; Streptococcus groupA (including 44% of Streptococcus pyogenes strains and 74% of Streptococcus faecalis strains). Pharmacokinetics:

Absorption – 75-77% when ingested decreases binding to plasma proteins – 55-65%.

The time to reach maximum concentration when taken orally is 2-3 h (it may take 2-3 days to reach therapeutic concentration). Over the next 8 hours the concentration gradually decreases. Maximum concentration is 15 g. 35 mg/l (a concentration of 1mg/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. In large amounts it accumulates in bone tissue tumor tissues in dentin and enamel of milk 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 with inflammatory processes in the brain membranes, the concentration in the cerebrospinal fluid is 8-36% of the plasma concentration. It penetrates through the placental barrier and into the breast milk. The volume of distribution is 13-16 l/kg.

It is slightly metabolized in the liver. Elimination half-life is 6-11 hours with anuria 57-108 hours. It is found in high concentration in urine within 2 hours after intake and is maintained for 6-12 hours; during the first 12 hours up to 10-20% of dose is excreted by kidneys. Smaller amount (5-10% of total dose) is excreted with bile in intestine where partial reverse absorption occurs, which promotes prolonged circulation of active substance in organism (intestine-hepatic circulation).

The intestinal excretion is 20-50%. With hemodialysis it is removed slowly.

Indications

Active ingredient

Composition

1 tablet contains:

The active substance: Tetracycline hydrochloride in terms of the active substance -100 mg.

Excipients: sucrose (refined sugar) – 7.1 mg, calcium stearate monohydrate – 1.26 mg, magnesium disilicate (talc) – 1.26 mg, gelatin – 0.54 mg, potato starch – 15.84 mg.

The film coating: hypromellose (oxypropyl methylcellulose) – g 1.332 mg, paraffin, liquid (vaseline oil) – 0.25 mg, polysorbate-80 (tween-80) – 0.388 mg, dye azoru bin(acid red 2 C)-0.03 mg.

How to take, the dosage

Ingestion with plenty of fluid.

Adults – 03-05 g every 6 hours (4 times a day) or 05-1 g every 12 hours (2 times a day).’Maximum daily dose – 4 g. The course of treatment is 5-10 days.

Children over 8 years of age – 625-125 mg/kg every 6 hours or 125-25 mg/kg every 12 hours.

In acne: 05-2 g/day in divided doses. If the condition improves (usually after 3 weeks), the dose is gradually reduced to a maintenance dose of 01-1 g. Adequate remission of acne can be achieved by using the drug every other day or by intermittent therapy.

Brucellosis: 05 g every 6 hours for 3 weeks concomitantly 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 15 g then 05 g every 6 hours for 4 days (total dose of 9 g).

Syphilis: 05 g every 6 hours for 5 days (early syphilis) or 30 days (late syphilis).

Uncomplicated urethral endocervical and rectal infections caused by Chlamydia trachomatis: 05 g every 6 hours for at least 7 days.

Lyme disease (early stage only) – 10-15 g per day for 10-14 days.

Listeriosis – 02-03 g every 6 hours for 7-10 days.

Actinomycosis – 3 g a day for the first 10 days then 05 g every 6 hours for the last 18 days.

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

In inguinal granuloma venereal lymphogranuloma – 05 g every 6 hours for 3-4 weeks.

Psittacosis: 05 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 to prevent relapse.

Vesicular rickettsiosis – 08-12 g per day for 8-10 days.

Tularemia – 15-2 g per day. After normalization of temperature the treatment is continued for 5-7 days more.

Frambiesia – 05 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 0Zg every 6 hours.

Interaction

Reduces 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 preparations of iron and colestyramine.

Chymotrypsin increases concentration and duration of circulation.

Special Instructions

Possible development of photosensitization requires limitation of insolation.

Per prolonged use requires periodic monitoring of renal function of the liver and hematopoietic organs.

Possible masking of syphilis manifestations; 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 in any bone-forming tissue. Because of this, taking it while teeth are developing can cause long-term yellow-gray-brown staining of the teeth, as well as enamel hypoplasia.

B and K vitamins Beer Yeast should be prescribed to prevent hypovitaminosis.

Contraindications

Side effects

Digestive system: decreased appetite vomiting diarrhea nausea glossitis esophagitis gastritis ulceration of the stomach and duodenum hypertrophy of papillae of the tongue dysphagia hepatotoxic effect pancreatitis intestinal dysbacteriosis enterocolitis increased activity of “liver” transaminases antibiotic-‘associated diarrhea.

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

Hematopoietic organs: hemolytic anemia thrombocytopenia neutropenia eosinophilia.

Urinary system disorders’ azotemia hypercreatininemia nephrotoxic effect.

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

Overdose

Pregnancy use

It is contraindicated in pregnancy (tetracyclines pass through the placenta and accumulate in the bones and dental buds of the fetus disrupting their mineralization and can cause severe disorders of bone development).

The FDA fetal category is D.

Breast-feeding must be stopped during treatment (tetracyclines penetrate into breast milk and may affect the development of baby’s bones and teeth and cause photosensitization reactions from oral and vaginal candidiasis in babies).

Similarities