DrugFriday: Ciprofloxacin

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DFCiprofloxacin

Ciprofloxacin is an antibacterial drug belonging to the Fluoroquinolone class of antibiotics.

Mechanism of action:

It causes DNA breakdown in bacteria by inhibiting enzyme DNA gyrase

Pharmacology:

Oral bioavailability of Ciprofloxacin is 50-85%

Peak plasma time: 0.5-2.5 hours depending on immediate or extended release

Distribution:

Ciprofloxacin is distributed widely throughout body and tissue concentrations often exceed serum concentrations, especially in kidneys, gallbladder, liver, lungs, gynecologic tissue, and prostatic tissue; cerebrospinal fluid (CSF) concentration is 10% in noninflamed meninges and 14-37% in inflamed meninges; crosses placenta; enters breast milk.

Metabolism:

Ciprofloxacin is metabolized mainly in the liver.

Elimination:

40-50% excretion of Ciprofloxacin is via urine and ~30% is via stools

Indications and dosage:

  1. Bone and joint infections:
    • Mild/moderate: 500 mg orally 12hrly or 400 mg IV 12hrly for ≥4-6 weeks
    • Severe/complicated: 750 mg orally 12hrly or 400 mg IV 8hrly for ≥4-6 weeks
  2. Chronic prostatitis
    • Indicated for chronic bacterial prostatitis caused by Escherichia coli or Proteus mirabilis
    • Mild/moderate: 500 mg orally 12hrly or 400 mg IV 12hrly for 28 days
  3. Infectious diarrhea:
      Mild/moderate/severe: 500 mg PO 12hrly for 5-7 days
  4. Intra abdominal infections:
      Complicated: 500 mg PO 12hrly or 400 mg IV 12hrly for 7-14 days
  5. Lower respiratory infections:
    • Mild/moderate: 500 mg PO 12hrly or 400 mg IV 12hrly for 7-14 days
    • Severe/complicated: 750 mg PO 12hrly or 400 mg IV 8hrly for 7-14 days
  6. Skin infections
    • Mild/moderate: 500 mg PO 12hrly or 400 mg IV 12hrly for 7-14 days
    • Severe/complicated: 750 mg PO 12hrly or 400 mg IV 8hrly for 7-14 days
  7. Urinary tract infections:
    • Acute uncomplicated:, 250 mg PO 12hrly for 3 days
    • Mild/moderate: 250 mg PO 12hrly or 200 mg IV 12hrly for 7-14 days
    • Severe/complicated: 500 mg PO 12hrly or 400 mg IV q12hr for 7-14 days
  8. Urethral and cervical gonococcal infections:
      Uncomplicated: 250-500 mg PO once
  9. Bronchiectasis

Adverse effects:

  • Gastrointestinal: nausea, vomiting, abdominal pain, increased liver enzymes
  • Allergic reactions
  • Restlessness, insomnia, headache
  • Hallucinations
  • Anorexia
  • Nephritis, polyuria

Use in pregnancy:

Category C: Used if benefits outweigh risks.

Warnings:

  • Fluoroquinolones are associated with increased risk of tendinitis and tendon rupture; this risk is further increased in older patients (usually >60 years); in kidney, heart, and lung transplant recipients; and with use of concomitant steroid therapy
  • May exacerbate muscle weakness in patients with myasthenia gravis; avoid fluoroquinolones with known history of myasthenia gravis

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