Tetracycline: Uses, Trade Names, Side Effects, Mechanism of Action and Precautions

It is an antibiotic used to treat several infections. This includes acne, cholera, brucellosis, plague, malaria and syphilis.

Tetracyclines have a broad spectrum of antibiotic action. Originally, they possessed some level of bacteriostatic activity against almost all medically relevant aerobic and anaerobic bacterial genera, both Gram-positive and Gram-negative, with some exceptions, such as Pseudomonas aeruginosa and Proteus spp.

Tradenames

It is marketed under the brands Sumycin, Tetracyn and Panmycin, among others. Actisite is a yarn type fiber formulation used in dental applications.

It is also used to produce several semi-synthetic derivatives, which together are known as tetracycline antibiotics. The term “tetracycline” is also used to denote the four-ring system of this compound; “Tetracyclines” are related substances that contain the same four-ring system.

Applications

It is the first line therapy for Rocky Mountain spotted fever (Rickettsia), Lyme disease (B. burgdorferi), Q fever (Coxiella), psittacosis, lymphogranuloma venereum (Chlamydia) and Mycoplasma pneumoniae and to eradicate transport nasal meningococcus

Tetracycline tablets were used in the plague outbreak in India in 1994.

Tetracyclines remain especially useful in the treatment of infections by certain obligate intracellular bacterial pathogens, such as Chlamydia, Mycoplasma and Rickettsia. They are also valuable in spirochetal infections, such as syphilis, leptospirosis and Lyme disease.

Certain exotic or rare infections, such as anthrax, plague and brucellosis, are also susceptible to tetracyclines. These agents also have activity against certain eukaryotic parasites, including those responsible for diseases such as malaria and balantidiasis.

Side effects

Common side effects include:

  • Vomiting
  • Diarrhea.
  • Acne.
  • Loss of appetite

Other side effects include:

  • Poor dental development if children under the age of eight use it.
  • Renal problems.
  • Sunburn easily.

Use during pregnancy can harm the baby. Tetracycline belongs to the family of tetracycline medications. It works by blocking the ability of bacteria to make proteins.

It was patented in 1953 and entered commercial use in 1978. It is on the List of Essential Medicines of the World Health Organization, the most effective and safe medicines needed in a health system. Tetracycline is available as a generic medicine.

Tetracycline was originally made from bacteria of the Streptomyces type.

Precautions

The use of the group of tetracycline antibiotics can be problematic, among its risks are:

  • Permanent teeth of color (yellow-gray-brown), from the prenatal period to childhood and adulthood.
  • Be inactivated by Ca2 + ions, so they should not be taken with milk, yogurt and other dairy products.
  • Being inactivated by aluminum, iron and zinc, should not be taken at the same time as the remedies for indigestion (common antacids and heartburn medications without a prescription).
  • It causes photosensitivity of the skin, so exposure to the sun or intense light is not recommended.
  • It causes lupus induced by medications and hepatitis.
  • It causes microvesicular fatty liver.
  • Causa tinnitus.
  • It interferes with methotrexate by displacing it from the various protein binding sites.
  • It causes respiratory complications, as well as anaphylactic shock , in some people.
  • It can affect the bone growth of the fetus, so it should be avoided during pregnancy.
  • Fanconi syndrome may be the result of ingestion of expired tetracyclines.

Caution should be exercised in long-term use when breastfeeding. Short-term use is safe; the bioavailability in milk is low or zero.

According to the US Food and Drug Administration. UU there have been reports of Stevens-Johnson syndrome, toxic epidermal necrolysis and erythema multiforme associated with the use of doxycycline , but a causal role has not been established.

Mechanism of action

Tetracycline inhibits protein synthesis by blocking the binding of aminoacyl-tRNA charged to site A on the ribosome. This binds to the 30S subunit of the microbial ribosomes. Therefore, it prevents the introduction of new amino acids to the nascent peptide chain.

The action is usually inhibitory and reversible when withdrawing the drug. Mammalian cells are less vulnerable to the effect of tetracyclines, despite the fact that tetracycline binds to the small ribosomal subunit of prokaryotes and eukaryotes (30S and 40S, respectively).

This is because bacteria actively pump tetracycline in their cytoplasm, even against a concentration gradient, while mammalian cells do not. This explains the relatively small effect outside the tetracycline site on human cells.

Mechanisms of resistance:

Bacteria generally acquire resistance to tetracycline from the horizontal transfer of a gene encoding an efflux pump or ribosomal protection protein.

The effluvium pumps actively expel tetracycline from the cell, preventing the accumulation of an inhibitory concentration of tetracycline in the cytoplasm. The ribosomal protection proteins interact with the ribosome and dislodge the tetracycline from the ribosome, allowing translation to continue.

Other uses

Tetracycline hydrochloride is available as a yellow crystalline powder. Since tetracycline is absorbed in bone, it is used as a bone growth marker for human biopsies.

It is also used to determine the amount of bone growth within a certain period of time, usually a period of about 21 days. Tetracycline is incorporated into bone mineralization and can be detected by its fluorescence.

In “double labeling with tetracycline”, a second dose is administered between 11 and 14 days after the first dose, and the amount of bone formed during that interval can be calculated by measuring the distance between the two fluorescent labels.

Tetracycline is also used as a biomarker in wildlife to detect the consumption of baits containing drugs or vaccines.

In genetic engineering, tetracycline is used in transcriptional activation. It is also one of a group of antibiotics that together can be used to treat peptic ulcers caused by bacterial infections.

In cancer research at Harvard Medical School, tetracycline has been used to deactivate leukemia in genetically altered mice, and to do so reliably, when it is added to your drinking water.

The mechanism of action for the antibacterial effect of tetracyclines is based on altering the translation of proteins in bacteria, which damages the ability of microbes to grow and repair. However, the translation of proteins is also altered in eukaryotic mitochondria and produces effects that may confuse the experimental results.

A technique being developed for the control of Aedes aegypti mosquito species uses a strain that is genetically modified to require tetracycline to develop beyond the larval stage.

Modified males raised in a laboratory develop normally since they are supplied with this chemical and can be released in the wild. Their later descendants inherit this trait, but they do not find tetracycline in their environments, so they never become adults.

Tetracycline is used in cell biology as a selective agent in cell culture systems. It is toxic to prokaryotic and eukaryotic cells and selects cells that harbor the bacterial gene tet r, which encodes a membrane-associated protein of 399 amino acids.