tetracycline

Brand: Sumycin

Prototype Drug
Drug Class: tetracycline antibiotic
Drug Family: antibiotic
Subclass: prototypical tetracycline
Organ Systems: infectious-disease

Mechanism of Action

Reversibly binds 30S ribosomal subunit, blocking aminoacyl-tRNA binding; bacteriostatic. Prototype tetracycline with broad spectrum including atypical bacteria, chlamydiae, rickettsiae, and some protozoa.

30S ribosomal subunit

Indications

  • Rocky Mountain spotted fever (Rickettsia)
  • chlamydial infections
  • Lyme disease (alternative to doxycycline)
  • H. pylori eradication (quadruple therapy)
  • acne vulgaris (oral)
  • cholera
  • brucellosis

Contraindications

  • tetracycline hypersensitivity
  • pregnancy
  • children <8 years
  • renal impairment (relative — avoid)

Adverse Effects

Common

  • GI upset (most common with this class)
  • photosensitivity
  • esophageal irritation

Serious

  • hepatotoxicity (high doses)
  • pseudotumor cerebri
  • permanent tooth discoloration (children)
  • renal azotemia (anti-anabolic effect)

Pharmacokinetics (ADME)

Absorption 75–80%; significantly reduced by food, dairy, antacids, and divalent cations
Distribution widely distributed; bone and dental deposition
Metabolism not significantly metabolized
Excretion renal (40–50%) and biliary (significant enterohepatic recirculation)
Half-life 6–11 hours
Onset 1–3 hours
Peak 2–4 hours
Duration 6–12 hours
Protein Binding 65%
Vd moderate-large

Drug Interactions

Drug / Agent Mechanism Severity
dairy products/antacids/iron/calcium/magnesium chelation by divalent/trivalent cations dramatically reduces oral absorption major
warfarin gut flora suppression may potentiate anticoagulation moderate
penicillins bacteriostatic effect antagonizes the bactericidal activity of penicillins moderate

Nursing Considerations

  1. Administer on an empty stomach (1 hour before or 2 hours after meals); absolutely avoid concurrent dairy, antacids, calcium supplements, and iron — chelation can reduce absorption by >90%.
  2. Patient should take each dose with a full glass of water and avoid lying down for 30 minutes to prevent esophageal ulceration.
  3. Renal dose adjustment required; avoid use in patients with significant renal impairment as tetracycline has an anti-anabolic effect that worsens azotemia.
  4. Do not administer to pregnant women or children under 8 years; document this contraindication in the patient's chart.

Clinical Pearls

  • Tetracycline is the prototype of the class but has been largely superseded by doxycycline due to its more favorable PK (twice-daily vs four-times-daily dosing, less affected by food).
  • Tetracyclines chelate calcium during tooth development and bone growth, depositing yellow-brown pigment and causing enamel hypoplasia in children and fetuses — an irreversible and preventable complication.

Safety Profile

Pregnancy contraindicated
Lactation avoid
Renal Adjustment Required
Hepatic Adjustment Required
TDM Not required