Products
Tetracyclines are commercially available in many countries in the form of tablets, capsules, and injection and infusion solutions, among others. This article refers primarily to peroral therapy. The first tetracycline, chlortetracycline (aureomycin, Lederle), was discovered in the 1940s during screening of soil samples under the direction of Benjamin Minge Duggar and became commercially available at the end of the decade.
Structure and properties
Tetracyclines are natural substances from -species. The name tetracycline is derived from the four rings that are fused together. Chlortetracycline (aureomycin, Lederle) was isolated from in the 1940s. Oxytetracycline (Terramycin, Pfizer) was obtained from in the 1950s. Tetracycline could be prepared by removing the chlorine atom from chlortetracycline. It also occurs naturally. In the 1950s, demeclocycline was also discovered, which, like chlortetracycline, is formed from. Doxycylcin (1960s) and minocycline (1970s) are produced semisynthetically. Minocycline is an example of a lipophilic tetracycline.
Effects
Tetracyclines (ATC J01AA) have bacteriostatic properties against Gram-positive and Gram-negative pathogens. The effects are based on inhibition of bacterial protein synthesis by binding to the 30S subunit of ribosomes. Tetracyclines additionally exert anti-inflammatory, antioxidant, and antiparasitic effects, among others. They have strong chelating effects and bind divalent cations. Tetracyclines therefore inhibit matrix metalloproteases and are susceptible to drug-drug interactions.
Indications
Indications for use include:
- Bacterial infectious diseases with susceptible pathogens.
- Acne (Acne vulgaris)
- Rosacea
- Malaria prevention and treatment
Dosage
According to the professional information. Intake depends on the active ingredient and the drug. For some drugs, fasting administration is recommended. Others should be administered with a meal to avoid gastrointestinal upset. Tetracyclines should be taken with adequate water while sitting or standing to prevent irritation and ulceration of the esophagus. Do not take just before bedtime (keep at least one hour apart). Tetracyclines should not usually be given with milk. Avoid exposure to strong sunlight or UV radiation during treatment, as the drugs can make the skin more sensitive to the sun. The use of a sunscreen should be considered. Combination with a probiotic may be recommended.
Active Ingredients
The active ingredients contain the suffix -cycline:
- Chlortetracycline (aureomycin, CH out of commerce).
- Demeclocycline (leather mix)
- Doxycycline (vibramycin, vibravenous, generic).
- Doxycycline for rosacea treatment (Oracea).
- Lymecycline (Tetralysal)
- Minocycline (Minocin)
- Oxytetracycline (Terramycin, out of commerce).
- Sarecycline (Seysara)
- Tetracycline (Pylera, combination)
- Tigecycline (Tygacil)
Contraindications
Contraindications include:
- Hypersensitivity
- Severe liver or kidney dysfunction (depending on the active ingredient).
- Pregnancy, lactation
- Children under 12 years
- Treatment with retinoids
Use during tooth development (children under 12 years, pregnancy) may cause permanent discoloration of teeth and is therefore contraindicated. Full precautions can be found in the drug information leaflet.
Interactions
Other drugs and foods may reduce the absorption of tetracyclines. These include, for example, antacids, multivitamins, calcium, magnesium, iron, and colestyramine. They should not be administered concomitantly. Other drug interactions occur (see the SmPC).
Adverse effects
The most common possible adverse effects of tetracyclines include:
- Hypersensitivity reactions
- Central disorders such as headache, fatigue, dizziness.
- Gastrointestinal disorders such as nausea, vomiting, abdominal pain, diarrhea, oral mucositis.
- Photosensitivity
As with other antibiotics, resistance is a problem.
