Тетрациклин
Тетрациклин Uses, Dosage, Side Effects, Food Interaction and all others data.
Тетрациклин has its main mechanism of action on protein synthesis, and an energy-dependent active transport system pumps the drug through the inner cytoplasmic membrane of bacteria. Once inside the bacterial cell, Тетрациклин binds specifically to the 30s ribosomes and inhibit bacterial protein synthesis.
Many Gram positive aerobic Cocci are susceptible, but many strains of staphylococci, streptococci and even some pneumococci are resistant to Тетрациклин. Thus, tetracycline is not the drug of choice in infections due to gram positive aerobes.
Pseudomonas and many Enterobacteriaceae are resistant. Urinary concentrations are adequate for some community - acquired E. coli and consequently, Тетрациклин is still used in uncomplicated initial UTIs. Тетрациклин is also active against and is the drug of choice for Brucella species, Calymmatobacterium granulomatis, Vibrio cholerae and V. vulnificus.
Тетрациклин is also active against anaerobic species of bacteria and since concentrations of the drug are quite high in the gastrointestinal contents, the enteric flora are usually altered by the drug.
Тетрациклин is incompletely absorbed from the gastro-intestinal tract, about 60 to 80% of a dose of tetracycline usually being available. It is widely distributed through the body tissues and fluids.
Тетрациклин has a half-life of about 12 hours. It is excreted in the urine and in the faeces.
Тетрациклин exhibits its bacteriostatic action by reversibly binding to the 30S subunits of the ribosome, thus preventing protein synthesis and arresting cell growth. It has a broad spectrum of antimicrobial activity including Chlamydiaceae, Mycoplasma spp., Rickettsia spp., spirochaetes, many aerobic and anaerobic gm+ve and gm-ve pathogenic bacteria and some protozoa.
Тетрациклин is a short-acting antibiotic that inhibits bacterial growth by inhibiting translation. It binds to the 30S ribosomal subunit and prevents the amino-acyl tRNA from binding to the A site of the ribosome. It also binds to some extent to the 50S ribosomal subunit. This binding is reversible in nature. Additionally tetracycline may alter the cytoplasmic membrane of bacteria causing leakage of intracellular contents, such as nucleotides, from the cell.
Trade Name | Тетрациклин |
Availability | Prescription only |
Generic | Tetracycline |
Tetracycline Other Names | Abramycin, Anhydrotetracycline, Deschlorobiomycin, Tetracyclin, Tétracycline, Tetracycline, Tetracyclinum, Tetrazyklin, Tsiklomitsin |
Related Drugs | amoxicillin, prednisone, omeprazole, pantoprazole, doxycycline, ciprofloxacin, cephalexin, metronidazole, azithromycin, clindamycin topical |
Type | |
Formula | C22H24N2O8 |
Weight | Average: 444.4346 Monoisotopic: 444.153265754 |
Protein binding | 20 - 67% protein bound |
Groups | Approved, Vet approved |
Therapeutic Class | Tetracycline Group of drugs |
Manufacturer | |
Available Country | Russia, Ukraine |
Last Updated: | September 19, 2023 at 7:00 am |
![Тетрациклин Тетрациклин](https://www.medicinesfaq.com/media/png/ru-tetracycline.png)
Uses
Тетрациклин ointment is used for followings-
- Treatment of bacterial conjunctivitis
- Treatment of trachoma (by preference use oral azithromycin for this indication)
- Prevention of chlamydial and gonococcal neonatal conjunctivitis
Тетрациклин is the drug of choice in the following infections :
- Ricketsial infection (Rocky Mountain spotted fever, endemic and scrub typhus fever and human ehrlichiosis).
- Mycoplasma pneumoniae infections in adults. Outbreaks of pneumonia caused by this organism are common in barracks and institutions. Most cases occur in children and young adults. Maculopapular rashes, haemolytic anaemia and meningo-encephalitis occur rarely.
- Chlamydial Infections: Chlamydia psittaci: This organism is the cause of psittacosis (ornithosis), a systemic illness contracted from infected birds. The pneumonia associated with it may be extensive, and severe systemic upset and death are common.Headache is a prominent early symptom.
- Non-gonococcal or non specific urethritis: Inflammation of the urethra not resulting from gonococcal, chlamydial, or other specific infectious agents.
- Lyme disease
- Brucellosis
- Miscellaneous infections, including granuloma inguinale, cholera, glanders, relapsing fever and V. vulnifians.
Other common uses of tetracycline include the following:
- Urinary Tract Infections with susceptible organisms (including the acute urethral syndrome in women).
- Bronchitis in patients with known underlying chronic lung diseases.
- Pelvic inflammatory disease and other sexually transmitted diseases (STDs) regimen.
- Travelers diarrhoea.
- Acne vulgaris
- Prostatitis.
- As an alternative agent in the penicillin allergic patient with syphilis.
- Anaerobic infections with susceptible organisms.
Тетрациклин is also used to associated treatment for these conditions: Acinetobacter infection, Acne Rosacea, Actinomycosis, Anthrax, Bacterial Infections, Bartonellosis, Brucellosis, Campylobacter Infection, Chancroid, Chlamydial Infections, Cholera, Conjunctivitis, Inclusion, Cystitis, Endometritis, Entamoebic histolytica infection, Escherichia infections, Gonorrhoea, Granuloma Inguinale, Helicobacter Pylori Infection, Infection, Infection, Bacteroides, Klebsiella Infections, Listeria infection, Lower respiratory tract infection bacterial, Lymphogranuloma Venereum, Necrotizing ulcerative gingivostomatitis, Neisseria Gonorrhoeae Infection, Nephritis, Ornithosis, Plague, Prostatitis, Psittacosis, Q Fever, Relapsing Fever, Rickettsialpox, Rocky Mountain Spotted Fever, Severe Acne, Shigella Infection, Skin and Subcutaneous Tissue Bacterial Infections, Skin infection caused by Staphylococcus aureus, Syphilis, Trachoma, Tularemia, Typhus, Urinary Tract Infection, Yaws, Bacterial upper respiratory tract infections, Clostridia infections, Grade 1, grade 2, grade 3, grade 4 Urinary Tract Infection
How Тетрациклин works
Тетрациклин passively diffuses through porin channels in the bacterial membrane and reversibly binds to the 30S ribosomal subunit, preventing binding of tRNA to the mRNA-ribosome complex, and thus interfering with protein synthesis.
Dosage
Тетрациклин dosage
The usual adult oral dosage of Тетрациклин is 1-2 g daily given in 2-4 divided doses. The usual oral dosage of Тетрациклин for children older than 8 years of age in 25-50 mg/kg daily given in 2-4 divided doses. Alternatively some clinicians recommended that children should receive 0.6-1.2 g/m2 daily.
Тетрациклин should be taken preferably one hour before or 2 hours after meals.
Some specific indications along with some information on dosage is given below:
Acne vulgaris: 250 mg four times daily or 500 mg 12 hourly for 1 week; 125-250 mg for several weeks or months.Duration of therapy is determined by individual progress
Acutestaphylococcal infections: 1-2 g daily in divideddoses for 10-14 days
Acute streptococcal infections:1-2 g daily in divided doses for 10 days.Prolonged therapy is needed to avoid risk of rheumatic fever or glomerulonephritis
Amoebiasis:1 g daily in four divided doses or 500 mg 12 hourly for 7 days.Given in association with amoebicidal agents
Brucellosis: 500 mg four times daily plus 1 g streptomycin twice daily for 1 week ; then 500 mg four times daily (no streptomycin) for 1 week.Prolonged therapy is necessary to avoid relapse
Subacute bacterial endocarditis:1-2 g daily in divided doses for 6 weeks.Usually given in combination with a bactericidal agent
Syphilis:Total 30-40 g given in divided doses over 10-15 days.Serology and spinal fluid examination should follow the administration of tetracycline
Wash the eyes with boiled and cooled water before each application. Use sterile sodium chloride 0.9% for newborns. Apply tetracycline 1% into the conjunctival sac of both eyes:
- Conjunctivitis: one application 2 times daily for 7 days
- Trachoma: one application 2 times dailyfor 6 weeks
- Prevention of neonatal conjunctivitis: one single application immediately after birth
Side Effects
Teeth and bone: Тетрациклин can cause depression of bone growth, permanent graybrown discoloration of the teeth and enamel hypoplasia when given during tooth development (i.e. during the later half of pregnancy, during infancy and in childhood).
Hypersensitivity reactions such as anaphylaxis, urticaria and rashes are uncommon. Photosensitivity reactions consisting of a red rash on areas exposed to intense sunlight can occur with Тетрациклин.
Gastrointestinal effects: Epigastric distress and nausea are commonly seen after oral administration, and these symptoms are somewhat dose related. Vomiting can occur.
Accentuated prerenal azotemia: Тетрациклин appears to aggravate pre-existing renal failure by inhibiting protein synthesis, which increases the azotemia from amino acid metabolism.
Superinfections with oral and anogenital candidiasis are relatively common in patients taking Тетрациклин.
Esophageal ulcerations: In most cases, the patients were taking the capsules with little or no fluid before going to bed. To help minimize this, oral doses should be given with adequate amounts of fluid.
Eye/Ear: Burning, irritation, visual disturbances, superinfections, photosensitivity, hypersensitivity
Toxicity
LD50=808mg/kg (orally in mice)
Precaution
Care should be taken if Тетрациклин Hydrochloride is given to patients with impaired liver function and high doses should be avoided. Potentiality hepatotoxic drugs (including erythromycin, chloramphenicol, isoniazide and sulphonamides) should not be given concomitantly.
Hepatic impairment. Avoid exposure to sunlight. Periodic evaluation of renal, hepatic and haematological system during prolonged therapy.
Interaction
Impaired absorption with antacids containing divalent and trivalent cations (e.g. Al, Ca, Mg), Fe, Zn and Na bicarbonate preparations, kaolin-pectin, bismuth subsalicylate, sucralfate, strontium ranelate, colestipol and colestyramine. May interfere with the bactericidal action of penicillin. May potentiate the effect of anticoagulants. May decrease efficacy of oral contraceptives. Nephrotoxic effects may be exacerbated by diuretics or other nephrotoxic drugs. May increase the hypoglycaemic effect of insulin and sulfonylureas in patients with DM. May increase toxic effects of ergot alkaloids and methotrexate.
Food Interaction
- Avoid milk and dairy products.
- Take on an empty stomach. Take at least 1 hour before or 2 hours after meals.
- Take with a full glass of water.
[Moderate] ADJUST DOSING INTERVAL: Administration with food, particularly dairy products, significantly reduces tetracycline absorption.
The calcium content of these foods forms nonabsorbable chelates with tetracycline.
MANAGEMENT: Тетрациклин should be administered one hour before or two hours after meals.
Тетрациклин multivitamins interaction
[Moderate] GENERALLY AVOID: The bioavailability of oral tetracyclines and iron salts may be significantly decreased during concurrent administration.
Therapeutic failure may result.
The proposed mechanism is chelation of tetracyclines by the iron cation, forming an insoluble complex that is poorly absorbed from the gastrointestinal tract.
In ten healthy volunteers, simultaneous oral administration of ferrous sulfate 200 mg and single doses of various tetracyclines (200 mg to 500 mg) resulted in reductions in the serum levels of methacycline and doxycycline by 80% to 90%, oxytetracycline by 50% to 60%, and tetracycline by 40% to 50%.
In another study, 300 mg of ferrous sulfate reduced the absorption of tetracycline by 81% and that of minocycline by 77%.
Conversely, the absorption of iron has been shown to be decreased by up to 78% in healthy subjects and up to 65% in patients with iron depletion when ferrous sulfate 250 mg was administered with tetracycline 500 mg.
Available data suggest that administration of iron 3 hours before or 2 hours after a tetracycline largely prevents the interaction with most tetracyclines except doxycycline.
Due to extensive enterohepatic cycling, iron binding may occur with doxycycline even when it is given parenterally.
It has also been shown that when iron is administered up to 11 hours after doxycycline, serum concentrations of doxycycline may still be reduced by 20% to 45%.
Coadministration of a tetracycline with any iron-containing product should be avoided if possible.
Otherwise, patients should be advised to stagger the times of administration by at least three to four hours, although separating the doses may not prevent the interaction with doxycycline.
Тетрациклин Drug Interaction
Unknown: aripiprazole, zolpidem, aspirin, lorazepam, duloxetine, omega-3 polyunsaturated fatty acids, escitalopram, atorvastatin, pregabalin, esomeprazole, acetaminophen, fluoxetine, montelukast, levothyroxine, acetaminophen, cyanocobalamin, ascorbic acid, cholecalciferol, alprazolam, cetirizine
Тетрациклин Disease Interaction
Major: colitisModerate: hepatotoxicity, renal dysfunction, esophageal irritation
Elimination Route
Bioavailability is less than 40% when administered via intramuscular injection, 100% intravenously, and 60-80% orally (fasting adults). Food and/or milk reduce GI absorption of oral preparations of tetracycline by 50% or more.
Half Life
6-12 hours
Elimination Route
They are concentrated by the liver in the bile and excreted in the urine and feces at high concentrations in a biologically active form.
Pregnancy & Breastfeeding use
Тетрациклин should not be used during pregnancy because of the risk of hypertoxicity in the mother as well as the effects on the developing foetus. Use in pregnancy potentially during breast-feeding and in children up to the age of 8, or some authorise say 12 years, may result in impaired bone growth and permanent discoloration of the child's teeth.
Contraindication
Тетрациклин Hydrochloride is contraindicated in patients hypersensitive to any of the member of tetracycline groups, since cross-sensitivity may occur Тетрациклин Hydrochloride should be avoided in patients with systemic lupus erythematosus. Тетрациклин Hydrochloride is considered to be contraindicated in renal impairment, particularly if severe ; if it must be given, doses should be reduced.
Storage Condition
Store between 20-25° C.
Innovators Monograph
You find simplified version here Тетрациклин
Тетрациклин contains Tetracycline see full prescribing information from innovator Тетрациклин Monograph, Тетрациклин MSDS, Тетрациклин FDA label
FAQ
What is Тетрациклин used for?
Тетрациклин is used to treat infections caused by bacteria including pneumonia and other respiratory tract infections.
How safe is Тетрациклин?
Тетрациклин may cause live bacterial vaccines such as typhoid vaccine to not work as well. Do not have any immunizations/vaccinations while using this medication unless your doctor tells.
What are the common side effects of Тетрациклин?
The common side effects of Тетрациклин may include:Nausea, vomiting, diarrhea, loss of appetite, mouth sores, black hairy tongue, sore throat, dizziness, headache, or rectal discomfort may occur.
Is Тетрациклин safe during pregnancy?
Тетрациклин are avoided during pregnancy because use after 25 weeks might result in staining of teeth in a small percentage of cases and possible effects on bone growth which are reversible.
Is Тетрациклин good for baby?
Do not give Тетрациклин to infants or children 8 years of age and younger unless directed by your doctor.
Is Тетрациклин safe during breastfeeding?
Short-term use of Тетрациклин is acceptable in nursing mothers. As a theoretical precaution, avoid prolonged or repeat courses during nursing.
Can I take Тетрациклин antibiotic while breastfeeding?
Use is not recommended since Тетрациклин pass into breast milk. They may cause the nursing baby's teeth to become discolored and may slow down the growth of the baby's teeth and bones.
Can I take alcohol with Тетрациклин?
It's generally safe to drink alcohol in moderation while taking Тетрациклин.
can I drive after taking Тетрациклин?
Do not drive, use machinery, or do anything that needs alertness until you can do it safely.
Who should not take Тетрациклин?
- diarrhea from an infection with Clostridium difficile bacteria.
- pseudotumor cerebri, a condition with high fluid pressure in the brain.
- liver problems.
- decreased kidney function.
- pregnancy.
What happens if I miss one day of Тетрациклин?
Take the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.
Can I take Тетрациклин long term?
The long-term use of Тетрациклин has been associated with microscopic brown-black discoloration of the thyroid gland.
Does Тетрациклин cause weight gain?
Тетрациклин did not show an antibiotic–weight gain effect.
How many days should I take Тетрациклин?
Should be continued for at least 1 to 2 days after symptoms and fever have subsided. In the treatment of streptococcal infections, a therapeutic dose of Тетрациклин should be given for at least 10 days.
Does Тетрациклин cause anxiety?
Taking antibiotics doesn't cause anxiety. If a person is anxious, being concerned about taking an antibiotic, or being worried about an increase in symptoms because of the antibiotic could be enough to increase apprehensive behavior, including the overly apprehensive behavior that leads to panic attacks.
Is Тетрациклин harmful to humans?
Тетрациклин can cause a dangerous syndrome resulting in damage to the kidneys.
Does Тетрациклин dry out my skin?
Тетрациклин may also cause the skin to become unusually dry, even with normal use.
Can I apply Тетрациклин on my face?
You should apply the medicine to the whole area usually affected by acne, not just to the pimples themselves. This will help keep new pimples from breaking out. Since this medicine contains alcohol, it will sting or burn. Therefore, do not get this medicine in the eyes, nose, mouth, or on other mucous membranes.
Can Тетрациклин cause liver damage?
High doses of intravenous Тетрациклин can induce fatty liver disease and may result in severe hepatic dysfunction, acute liver failure and death.
Can Тетрациклин affect my period?
Тетрациклин don't cause a delay or change to your period.
How should I take Тетрациклин?
Do not take this medicine in larger or smaller amounts or for longer than recommended.
Take Тетрациклин on an empty stomach, at least 1 hour before or 2 hours after a meal.
Do not take this medicine with milk or other dairy products, unless your doctor has told you to. Dairy products can make it harder for your body to absorb the medicine.