Tetracycline (Tablets, Ointment) Instructions for Use

ATC Code

J01AA07 (Tetracycline)

Active Substance

Tetracycline (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Antibiotic of the tetracycline group

Pharmacotherapeutic Group

Systemic antibacterial agents; tetracyclines

Pharmacological Action

A broad-spectrum antibiotic. It exerts a bacteriostatic effect by suppressing the protein synthesis of pathogens due to disruption of the complex formation between transfer RNA and the ribosome.

It is 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 influenzae, Haemophilus ducreyi, Bordetella pertussis, Escherichia coli, Enterobacter spp. (including Enterobacter aerogenes), Acinetobacter spp., Klebsiella spp., Salmonella spp., Shigella spp., Yersinia pestis, Francisella tularensis, Bartonella bacilliformis, Vibrio cholerae, Vibrio fetus, Rickettsia spp, Brucella spp. (in combination with streptomycin); in case of contraindications to the use of penicillin group drugs – Clostridium spp., Neisseria gonorrhoeae, Actinomyces spp; also active against Calymmatobacterium granulomatis, Chlamydia trachomatis, Chlamydia psittaci, Mycoplasma pneumoniae, Treponema spp., Entamoeba spp.

Pseudomonas aeruginosa, Proteus spp., Serratia spp., most strains of Bacteroides fragilis, most fungi, viruses, Streptococcus pyogenes, Streptococcus faecalis are resistant to tetracycline.

Pharmacokinetics

After oral administration, absorption is 75-77%, it decreases when taken with food, plasma protein binding is 55-65%.

The time to reach C_max after oral administration is 2-3 hours (it may take 2-3 days to reach therapeutic concentration). Over the next 8 hours, the concentration gradually decreases. C_max is 1.5-3.5 mg/L (a concentration of 1 mg/L is sufficient for a therapeutic effect). It is distributed unevenly in the body: C_max is determined in the liver, kidneys, lungs, and in organs with a well-developed reticuloendothelial system – the spleen, lymph nodes. The concentration in bile is 5-10 times higher than in blood serum. The concentration of tetracycline in the tissues of the thyroid and prostate glands corresponds to that found in plasma; in pleural, ascitic fluid, saliva, and breast milk of women – 60-100% of the plasma concentration. It accumulates in large quantities in bone tissue, tumor tissues, and in the dentin and enamel of milk teeth. It penetrates poorly through the blood-brain barrier. With intact meninges, it is not detected in the cerebrospinal fluid or is found in insignificant amounts (5-10% of the plasma concentration). In patients with CNS diseases, especially with inflammatory processes in the meninges, the concentration in the cerebrospinal fluid is 8-36% of the plasma concentration. It penetrates the placental barrier and is excreted in breast milk. V_d is 1.3-1.6 L/kg. It is minimally metabolized in the liver. T_1/2 is 6-11 hours, with anuria – 57-108 hours. It is detected in urine in high concentration 2 hours after administration and persists for 6-12 hours; within the first 12 hours, 10-20% of the dose is excreted by the kidneys. In smaller amounts (5-10% of the total dose), it is excreted with bile into the intestine, where partial reabsorption occurs, which contributes to the long-term circulation of the active substance in the body (enterohepatic circulation). Excretion through the intestine is 20-50%. It is removed slowly during hemodialysis.

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 the urinary and reproductive system organs, skin and soft tissue infections, ulcerative necrotizing gingivostomatitis, conjunctivitis, acne, actinomycosis, intestinal amebiasis, anthrax, brucellosis, bartonellosis, chancroid, cholera, chlamydia, uncomplicated gonorrhea, granuloma inguinale, venereal lymphogranuloma, listeriosis, plague, psittacosis, vesicular rickettsiosis, Rocky Mountain spotted fever, typhus, syphilis, trachoma, tularemia, yaws.

ICD codes

Dosage Regimen

For adults, administer a single oral dose of 250-500 mg every 6 hours.

Alternatively, for certain indications, use a total daily dose of 1-2 grams, divided into 2 or 4 equal doses.

For severe infections, an initial loading dose may be required, not exceeding 2 grams on the first day.

For children over 8 years, calculate the dose at 25-50 mg/kg of body weight per day, divided into 4 equal doses administered every 6 hours.

Do not exceed a maximum daily dose of 3 grams for adults or the calculated pediatric maximum.

Take tablets with a full glass of water, at least 1 hour before or 2 hours after meals.

Complete the entire prescribed course of therapy, even if symptoms improve, to prevent the development of resistant bacteria.

For the ointment, apply a thin layer to the affected skin areas 1 to 4 times daily, depending on the severity of the condition.

Apply the ointment to clean, dry skin; an occlusive dressing may be used if directed.

For ophthalmic ointment, apply a small amount (approximately 1 cm ribbon) into the affected eyelid every 2 to 12 hours as directed.

Adjust the dosage regimen based on the specific pathogen, severity of infection, and patient renal function.

Adverse Reactions

From the digestive system: decreased appetite, vomiting, diarrhea, nausea, glossitis, esophagitis, gastritis, gastric and duodenal ulcers, hypertrophy of the tongue papillae, dysphagia, hepatotoxic effect, increased activity of hepatic transaminases, pancreatitis, stomatitis, colitis, intestinal dysbiosis.

From the nervous system: increased intracranial pressure, headache, dizziness or unsteadiness.

From the hematopoietic organs: hemolytic anemia, thrombocytopenia, neutropenia.

From the urinary system: azotemia, hypercreatininemia.

Allergic reactions: maculopapular rash, skin hyperemia, angioedema, anaphylactoid reactions, drug-induced systemic lupus erythematosus (SLE), photosensitivity, eosinophilia, exfoliative dermatitis, fever, urticaria, arthralgia, pericarditis.

Immunological reactions: angioedema, anaphylactoid reactions, drug-induced systemic lupus erythematosus, eosinophilia, fever, urticaria, arthralgia, pericarditis.

From the skin: maculopapular rash, skin hyperemia, photosensitivity, exfoliative dermatitis.

Other: superinfection, candidiasis, vitamin B deficiency, hyperbilirubinemia, discoloration of tooth enamel in children.

Contraindications

Hypersensitivity to tetracycline, leukopenia, renal failure (CrCl<50-10 ml/min), pregnancy, breastfeeding period, children under 8 years of age.

With caution

Renal failure (CrCl>80-50 ml/min).

Use in Pregnancy and Lactation

Contraindicated for use during pregnancy and breastfeeding.

Use in Hepatic Impairment

Use with caution in case of impaired liver function.

Use in Renal Impairment

The drug is contraindicated for use in case of impaired renal function.

Pediatric Use

Contraindicated in children under 8 years of age. The use of tetracycline in children during tooth development can lead to irreversible discoloration of teeth.

Geriatric Use

In elderly patients, use should take into account the state of renal function.

Special Precautions

With long-term use, it is necessary to periodically monitor the functions of the kidneys, liver, and hematopoietic organs.

It may mask the manifestations of syphilis, therefore, in case of possible mixed infection, monthly serological testing for 4 months is necessary.

All tetracyclines form stable complexes with calcium ions in any bone-forming tissue. In this regard, administration during tooth development can cause long-term staining of teeth in yellow-gray-brown color, as well as enamel hypoplasia.

During treatment, to prevent hypovitaminosis, vitamins B, K, and brewer’s yeast should be used.

Tetracycline should not be taken simultaneously with milk and other dairy products, as this impairs the absorption of the antibiotic.

Due to the possible development of photosensitivity, it is necessary to limit sun exposure.

Drug Interactions

Drugs containing metal ions (antacids, drugs containing iron, magnesium, calcium) form inactive chelates with tetracycline, therefore their simultaneous administration should be avoided.

Combination with penicillins and cephalosporins, which have a bactericidal effect and are antagonists of bacteriostatic antibiotics (including tetracycline), should be avoided.

With simultaneous use of tetracycline with retinol, the development of intracranial hypertension is possible.

With simultaneous use with cholestyramine or colestipol, impaired absorption of tetracycline is noted.

Chymotrypsin increases the concentration and duration of circulation of tetracycline in the body.

Due to the suppression of intestinal microflora, it reduces the prothrombin index (requires a reduction in the dose of indirect anticoagulants).

Reduces the effectiveness of estrogen-containing oral contraceptives and increases the risk of breakthrough bleeding.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.