Tetracyclines

On this page

Tetracyclines - The Ribosome Wreckers

  • Broad-spectrum, bacteriostatic antibiotics.
  • MoA: Reversibly bind 30S ribosomal subunit, blocking aminoacyl-tRNA access to A-site. 📌 Buy AT 30.
  • Key Drugs: Doxycycline, Minocycline (long-acting); Tetracycline (short-acting).
  • Uses: Atypical pneumonias (Mycoplasma, Chlamydia), Rickettsia, Brucellosis, Cholera, Acne.
  • AEs: GI distress, photosensitivity, teeth/bone issues (<8 yrs), Fanconi syndrome (expired).
  • Contraindications: Pregnancy, breastfeeding, children <8 yrs.

⭐ Tetracyclines are bacteriostatic, binding reversibly to the 30S ribosomal subunit and thereby preventing the attachment of aminoacyl-tRNA. Tetracycline mechanism of action on bacterial ribosomeoka

Tetracyclines - Journey Through Body

  • Oral Absorption:
    • Variable; food ↓ (not Doxy, Mino).
    • Chelation with Ca²⁺, Mg²⁺, Fe²⁺, Al³⁺ impairs absorption.

    ⭐ Avoid with dairy, antacids, iron supplements due to this chelation.

  • Distribution:
    • Wide; CSF (Mino > Doxy).
    • Accumulates: liver, kidney, spleen, skin.
    • Binds calcified tissues (bone, teeth).
    • Crosses placenta, breast milk.
  • Metabolism:
    • Most: minimal. Doxy/Mino some hepatic met.
  • Excretion:
    • Tetracycline: Renal.
    • Doxycycline: GI/fecal (safe in renal failure).
    • Minocycline: Hepatic met., renal/fecal excretion.
    • Tigecycline: Biliary/fecal.

Tetracyclines - Bug Busters' Hit List

  • Broad-spectrum: G+, G-, many anaerobes.
  • Effective against:
    • Atypical bacteria: Mycoplasma pneumoniae, Chlamydia spp. (trachomatis, psittaci), Rickettsia spp.

      ⭐ Drug of choice for Rickettsial infections (e.g., Rocky Mountain Spotted Fever, Q fever), Chlamydial infections (e.g., LGV, psittacosis), and Mycoplasma pneumoniae.

    • Spirochetes: Borrelia burgdorferi (Lyme disease), Leptospira interrogans, Treponema pallidum (if penicillin-allergic).
    • Zoonotic diseases: Brucellosis (with aminoglycoside), Plague (Yersinia pestis), Tularemia (Francisella tularensis).
    • Vibrio cholerae.
    • Acne vulgaris (low-dose, anti-inflammatory).
    • Malaria: Prophylaxis & treatment (Doxycycline).
    • Part of H. pylori eradication regimens.
  • 📌 Mnemonic for spectrum: VACUUM THe BedRoom.

Tetracyclines - The Nasty Side Effects

  • Gastrointestinal: Nausea, vomiting, diarrhea, epigastric pain, esophageal ulceration.
  • Bones & Teeth:
    • Permanent yellow-brown tooth discoloration, enamel hypoplasia.
    • Reversible bone growth inhibition in premature infants.

    ⭐ Contraindicated in pregnancy, breastfeeding, and children <8 years due to deposition in developing bones and teeth, causing permanent discoloration and enamel hypoplasia.

  • Phototoxicity: Exaggerated sunburn reaction (esp. demeclocycline, doxycycline).
  • Hepatotoxicity: ↑ risk in pregnancy (IV), pre-existing liver disease.
  • Renal Toxicity: Fanconi-like syndrome (outdated); worsens azotemia (except doxycycline, minocycline).
  • Vestibular Toxicity: Dizziness, vertigo, ataxia (minocycline).
  • Other: Superinfections (Candida, C. difficile), benign intracranial hypertension (pseudotumor cerebri). oka

Tetracyclines - Resistance & Risky Mixes

  • Resistance Mechanisms:
    • ↑ Efflux (e.g., TetA, TetK) - common
    • Ribosomal protection (e.g., TetM, TetO) - alters 30S
    • Enzymatic inactivation - less common
  • Risky Drug Interactions: ⚠️
    • Cations ($Ca^{2+}$, $Mg^{2+}$, $Fe^{2+}$), Dairy: ↓ absorption (chelation)
    • Penicillins: Antagonistic effect
    • Oral Contraceptives: ↓ efficacy
    • Warfarin: ↑ anticoagulant effect
    • Retinoids (e.g., Isotretinoin): ↑ risk of pseudotumor cerebri

⭐ Tigecycline, a glycylcycline, overcomes major resistance mechanisms like efflux pumps and ribosomal protection proteins.

High‑Yield Points - ⚡ Biggest Takeaways

  • Bacteriostatic; inhibit protein synthesis by binding 30S ribosomal subunit.
  • Broad spectrum: atypicals (Mycoplasma, Chlamydia, Rickettsia), spirochetes.
  • Oral absorption impaired by divalent/trivalent cations (milk, antacids, iron).
  • AEs: Photosensitivity, GI distress, teeth discoloration & bone issues in children <8 yrs, Fanconi syndrome (outdated).
  • Doxycycline: long-acting, fecal excretion (safer in renal impairment), DOC for Lyme disease, RMSF.
  • Tigecycline: IV glycylcycline, active against MRSA, VRE.
  • Contraindicated in pregnancy, breastfeeding, and children <8 years.

Practice Questions: Tetracyclines

Test your understanding with these related questions

Which of the following is NOT a mechanism of antibiotic resistance?

1 of 5

Flashcards: Tetracyclines

1/10

_____ is associated with vestibular toxicity

TAP TO REVEAL ANSWER

_____ is associated with vestibular toxicity

Minocycline (Tetracycline)

browseSpaceflip

Enjoying this lesson?

Get full access to all lessons, practice questions, and more.

Start Your Free Trial