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What-is-terramycin

Can you use terramycin on humans?

Posted on  April 21, 2021, Edited by Jason, Category  

What is terramycin?

1. Definition

Terramycin is a light yellow tablet or sugar-coated tablet, belonging to tetracyclines, easily soluble in water and acidic. It is a broad-spectrum semi-synthetic antibiotic that is antibacterial rather than bactericidal.

Terramycin is a broad-spectrum bacteriostatic agent, and many rickettsia, mycoplasma, chlamydia, spirochetes, amoeba and some plasmodium are sensitive to oxytetracycline. Enterococcus is resistant to it. Others such as Actinomyces, Bacillus anthracis, Listeria monocytogenes, Clostridium, Nocardia, Vibrio, Brucella, Campylobacter, Yersinia, etc. are sensitive to oxytetracycline.

Terramycin has certain antibacterial activity against Neisseria gonorrhoeae and meningococcus, but penicillin-resistant Neisseria gonorrhoeae is also resistant to oxytetracycline. Over the years, due to the wide application of tetracyclines, common clinical pathogens are highly resistant to oxytetracycline, including gram-positive bacteria such as staphylococci and most gram-negative bacilli. There is cross-resistance between different varieties of tetracycline antibiotics.

The mechanism of action of oxytetracycline is that the drug can specifically bind to the A position of the 30S subunit of the bacterial ribosome to inhibit the growth of peptide chains and affect the synthesis of bacterial proteins.

It is used for dysentery, trachoma, conjunctivitis, pneumonia, otitis media, skin purulent infection, etc. It is also used to treat amoebic enteritis and intestinal infections.

2. Physical and chemical properties

The hydrochloride salt of terramycin is light yellow crystalline or amorphous powder, odorless and darkening in sunlight, and is easily damaged in alkaline solutions. It is slightly soluble in ethanol and water, soluble in sodium hydroxide solution and dilute hydrochloric acid.

3. Purpose

It can be used to treat respiratory, urethral, ​​skin and soft tissue infections in dogs and cats, including brucellosis, rickettsial disease and chlamydia in dogs, colibacillosis in dogs and cats, and cats caused by rickettsiae The infectious anemia is also used to prevent leptospirosis in dogs.

4. Pharmacological effects

Oxytetracycline has a broad-spectrum anti-pathogenic microorganism effect, is a fast antibacterial agent, and has a bactericidal effect on certain bacteria at high concentrations. The mechanism of action is that the drug can specifically bind to the A position of the 30S subunit of the ribosome to prevent the connection of aminoacyl-tRNA at this position, thereby inhibiting the growth of peptide chains and affecting the protein synthesis of bacteria or other pathogenic microorganisms.

Oxytetracycline has strong antibacterial activity against Staphylococcus aureus, pneumococcus, Streptococcus pyogenes, Neisseria gonorrhoeae, meningococcus, Escherichia coli, Aerobacter, Shigella, Yersinia, Listeria monocytogenes, etc.; in addition, oxytetracycline also has a strong effect on rickettsia, mycoplasma, chlamydia, actinomycetes, etc.

5. Pharmacokinetics

The oral absorption of oxytetracycline hydrochloride is not complete (about 30%-58% can be absorbed), and the volume of distribution is about 0.9-1.9L/kg. The peak blood concentration after a single oral dose of 1 g is about 3.9 mg/L. The drug is widely distributed after absorption, and can penetrate into pleural effusion and abdominal effusion, and can also enter the fetal blood circulation through the placental barrier, but it is not easy to penetrate the blood-cerebrospinal fluid barrier, so the concentration of the drug in the cerebrospinal fluid is low.

Oxytetracycline can also be distributed in the liver, spleen, bone marrow, bones, dentin and tooth enamel. The drug can also reach high concentrations in milk. The binding rate of oxytetracycline protein is about 20%-35%. The half-life of patients with normal renal function is 6-10h, and prolonged half-life with renal insufficiency.

It can reach 47-66h for anuria patients. The drug is mainly excreted through glomerular filtration, and 70% of the dose can be excreted within 24 hours of administration, and a small amount of the drug is excreted through feces via bile. Hemodialysis can remove 10%-15% of the drug.

Terramycin Uses

Terramycin-Uses
Terramycin-Uses

1. Indications

A. Oxytetracycline may be used as an alternative treatment for the following diseases:

  • Rickettsiosis, including epidemic typhus, endemic typhus, and tsutsugamushi;
  • Infection caused by Mycoplasma pneumoniae;
  • Chlamydia infections, including psittacosis, inguinal granuloma (lymphgranuloma venereal disease), nonspecific urethritis, salpingitis and trachoma;
  • Relapsing fever;
  • Brucellosis (in combination with aminoglycoside drugs);
  • Cholera;
  • Plague (in combination with aminoglycoside drugs);
  • Tularemia.

B. Oxytetracycline can be used to treat tetanus, gas gangrene, yaws, syphilis, gonorrhea and leptospirosis allergic to penicillin antibiotics.

C. Oxytetracycline can also be used to treat respiratory tract, biliary tract, urinary tract and skin and soft tissue infections caused by sensitive bacteria.

D. Oxytetracycline can also be used for acne treatment.

2. Uses

Why was terramycin discontinued? Terramycin, also known as oxytetracycline, is also a derivative with a common polycyclic tetracenecarboxamide core. It belongs to one of the tetracyclines. Because of its low price, many people have used it in the treatment of fish diseases. Now its use in aquaculture is banned.

Although it is a banned drug, it does not mean that it has good effect. Although it is a broad-spectrum antibiotic, it is usually a bacteriostatic antibiotic. It can only kill bacteria when the concentration is high. It has a weaker effect on gram-positive bacteria Staphylococcus, Streptococcus hemolyticus, and Clostridium than penicillins and cephalosporins; it is more sensitive to E. coli, Salmonella, and Pasteurella in Gram-negative bacteria, but it is not as effective as aminoglycosides and chloramphenicol.

Although the antibacterial and bactericidal effect of terramycin is not as good as other antibiotics, its metabolism is slow in the body, and it can also carry out hepato-intestinal circulation like doxycycline. Oxytetracycline is slightly soluble in water and easy to fail in alkaline solutions.

Its hydrochloride salt is commonly used. It has stable properties and is yellow crystalline powder, but it is unstable after being dissolved in water. The absorption of terramycin is irregular and incomplete. It is mainly absorbed in the upper part of the small intestine. When there are polyvalent metal ions such as aluminum, magnesium, calcium, iron, and manganese in the gastrointestinal tract, they can form insoluble chelates with them, thereby reducing the efficacy.

After absorption, it is widely distributed and easily penetrates into the thoracic cavity and abdominal cavity. It is stored in the bile, spleen, teeth and bones in the body. It can be concentrated in the liver and secreted by bile. The drug concentration in bile can reach more than 10 times the drug concentration in the blood. This part of the medicinal effect will be excreted into the intestines along with the bile, be absorbed and utilized again, and enter the hepato-intestinal circulation.

When using terramycin, it should be noted that the dosage range is very large, and the dosage is 5-100 mg per kilogram of body weight. If the dosage is too large, or the oral administration time is too long, it will cause intestinal flora disorder, enteritis and double infection. Especially for renal dysfunction of the body, oxytetracycline is mainly excreted by the kidneys, which will slow down the excretion, prolong the half-life, and increase the toxicity to the liver. Like doxycycline, it is not suitable to be used under alkaline conditions. The effect of taking medicine on an empty stomach is better.

3. Dosage

  • Adults: 0.25~0.5g each time, once every 6 hours.
  • Children: Children over 8 years old, 6.25~12.5 mg/kg each time, once every 6 hours.

4. Veterinary Uses

Oxytetracycline has a broad-spectrum antibacterial effect. It also has a certain inhibitory effect on sensitive bacteria including pneumococcus, streptococcus, some staphylococci, Bacillus anthracis, tetanus, Mycoplasma hyopneumoniae, Chlamydia, and spirochetes.

Functions and indications:

  • It has significant curative effect on pigs' paratyphoid fever, eperythrocytes, anthracnose, asthma, dysentery, and swine pneumonia.
  • Poultry dysentery and chlamydia can also be used to relieve stress, increase egg production, and promote weight gain of young birds.
  • Aquatic products are used in the treatment of fish Vibrio disease, dephosphorization disease, gill rot disease, eel disease, trout sore disease, eel red fin disease, etc.

Dosage:

  • Mixed drinking: add 400 kg of water to 100g per bag for 3-5 days
  • Mixed feeding: each bag of 100g mixed material 200 kg, continuous use for 3-5 days

Terramycin Side Effects

Terramycin-Side-Effects
Terramycin-Side-Effects

1. Adverse Reactions

  • Terramycin can be deposited in teeth and bones, causing different degrees of discoloration and yellowing of teeth, dysplasia of enamel and tooth decay, and dysplasia of bone.
  • Gastrointestinal reactions: Oral terramycin can cause gastrointestinal symptoms such as nausea, vomiting, epigastric discomfort, abdominal distension, and diarrhea.
  • Liver damage: Long-term oral administration of oxytetracycline in large doses can cause liver damage, usually manifested as liver steatosis. Patients with pre-existing liver and kidney dysfunction, and women in late pregnancy are more likely to occur.
  • Allergic reactions: drug fever or skin rashes are common. The latter can be manifested as urticaria, erythema multiforme, eczema-like erythema, etc., and can also induce photo-sensitive dermatitis. Occasionally, symptoms such as anaphylactic shock, asthma, and purpura may occur.
  • Changes in peripheral hemogram: abnormal lymphocytes, granulocyte toxic granules, thrombocytopenia and granulocyte reduction may occur in long-term medication.
  • Central nervous system: occasional benign intracranial pressure increase during medication, manifested as headache, vomiting, optic disc edema, etc.
  • Double infection: Long-term medication can cause double infection. Double infection is mainly manifested as the gastrointestinal, respiratory and urinary tract infections caused by drug-resistant Staphylococcus aureus, Gram-negative bacilli and fungi. In severe cases, it can cause sepsis.
  • Others: Long-term medication can reduce the normal flora in the human body, leading to vitamin deficiency, fungus reproduction, thirsty, sore throat, angular cheilitis, glossitis, dark or discoloration of the tongue coating.

2. Terramycin Interactions

  • Oxytetracycline can enhance its nephrotoxicity when used together with the general anesthetic methoxyflurane.
  • Oxytetracycline and strong diuretics such as furosemide can aggravate renal damage when used together.
  • Oxytetracycline can enhance liver toxicity when used together with other hepatotoxic drugs (such as anti-tumor chemotherapy drugs).
  • When oxytetracycline is used equivalently with antacids such as sodium bicarbonate, the increase in pH in the stomach can reduce the absorption and activity of oxytetracycline.
  • Oxytetracycline can form insoluble complexes with the metal ions in it when it is used together with calcium gluconate, calcium lactate and magnesium laxatives and other drugs containing calcium, magnesium, and iron ions, reducing drug absorption.
  • When the hypolipidemic drugs cholestyramine or colestipo are used together with oxytetracycline, it can affect the absorption of oxytetracycline.
  • Terramycin and oral contraceptives containing estrogen can reduce the efficacy of contraceptives and increase extra-menstrual bleeding.

3. Warnings

  • Cross allergy: People who are allergic to one tetracycline drug may be allergic to other tetracycline drugs.
  • Use with caution: patients with pre-existing liver disease; those with renal impairment.
  • Oxytetracycline in children under 8 years old can cause yellow staining of permanent teeth, enamel dysplasia and bone growth inhibition. Therefore, children under 8 years old should not use oxytetracycline.
  • Oxytetracycline can enter the fetus through the blood-placental barrier and deposit in the calcium area of ​​the teeth and bones, causing tetracycline teeth, poor enamel regeneration and inhibiting the growth of fetal bones. Therefore, pregnant women should not use terramycin.
  • Terramycin can be secreted by breast milk, and the concentration in milk is relatively high. Although terramycin can form insoluble complexes with calcium in milk and has little absorption, it can cause permanent discoloration of teeth, Enamel dysplasia and inhibition of the growth of the baby's bones, so breastfeeding women must weigh the pros and cons before deciding whether to use it.
  • Check or monitor during medication: liver and kidney function should be checked regularly during medication;
  • For those who have been treated with oxytetracycline for a long time, the blood concentration should be measured if necessary.

Conclusion

On the whole, the antibacterial effect of terramycin is not as good as that of chloramphenicol, cephalosporins, penicillin and aminoglycosides, but terramycin is metabolized slowly and can produce enterohepatic circulation. However, oxytetracycline has many side effects and its excessive use in the aquaculture industry has resulted in terramycin being banned from the aquaculture industry.

BALLYA provides a ballya-tetracyclines-test to tell you if there are tetracyclines(including terramycin) residues in honey, chicken and pork.

References

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