Grepafloxacin

What is Grepafloxacin

NOTE: This drug is discontinued in the US.

Grepafloxacin is an oral, once-a-day fluoroquinolone antibiotic.

It is indicated for the treatment of respiratory tract infections due to susceptible organisms (e.g., mild to moderate cases of chronic bronchitis, and for community-acquired pneumonia) and for uncomplicated gonorrhea and non-gonococcal urethritis and cervicitis due to Chlamydia trachomatis.

The gram-negative activity of grepafloxacin is comparable to that of fleroxacin, lomefloxacin, and ofloxacin. Gram-positive and anaerobic activity is slightly greater than that of other fluoroquinolones.

Grepafloxacin does not require dosage adjustment in patients with renal dysfunction, however adjustments are necessary in patients with hepatic dysfunction; the drug is contraindicated in patients with hepatic failure.

Grepafloxacin is metabolized by CYP1A2 and CYP3A4 and has a significant interaction with theophylline.

Grepafloxacin was approved by the FDA on November 6, 1997. Grepafloxacin was voluntarily withdrawn from marketing on October 27, 1999 due to severe cardiovascular adverse reactions, including 3 cases of torsades de pointes.

In Germany, the drug has the trade name Vaxar.

Indications

  1. bronchitis
  2. Chlamydia trachomatis
  3. community-acquired pneumonia
  4. Haemophilus influenzae (beta-lactamase negative)
  5. Haemophilus influenzae (beta-lactamase positive)
  6. Moraxella catarrhalis
  7. Mycoplasma pneumoniae
  8. Neisseria gonorrhoeae
  9. Streptococcus pneumoniae

Side Effects

  1. abdominal pain
  2. acute respiratory distress syndrome (ARDS)
  3. agranulocytosis
  4. anemia
  5. angioedema
  6. anorexia
  7. anxiety
  8. aplastic anemia
  9. arthralgia
  10. asthenia
  11. bronchospasm
  12. confusion
  13. constipation
  14. depression
  15. diarrhea
  16. dizziness
  17. drowsiness
  18. dysgeusia
  19. dyspepsia
  20. dyspnea
  21. fever
  22. hallucinations
  23. headache
  24. hemolytic anemia
  25. hepatic failure
  26. hepatic necrosis
  27. hepatitis
  28. hypotension
  29. increased intracranial pressure
  30. insomnia
  31. interstitial nephritis
  32. jaundice
  33. laryngeal edema
  34. leukopenia
  35. leukorrhea
  36. myalgia
  37. nausea
  38. nightmares
  39. orthostatic hypotension
  40. pancytopenia
  41. paranoia
  42. paresthesias
  43. photosensitivity
  44. pneumonitis
  45. pruritus
  46. pseudomembranous colitis
  47. psychosis
  48. QT prolongation
  49. rash
  50. renal failure (unspecified)
  51. restlessness
  52. seizures
  53. serum sickness
  54. sinus tachycardia
  55. Stevens-Johnson syndrome
  56. syncope
  57. tendon rupture
  58. thrombocytopenia
  59. thrombotic thrombocytopenic purpura (TTP)
  60. torsade de pointes
  61. toxic epidermal necrolysis
  62. tremor
  63. urticaria
  64. vaginitis
  65. vasculitis
  66. visual impairment
  67. vomiting
  68. xerostomia

Monitoring Parameters

  • LFTs
  • serum creatinine/BUN

Contraindications

  • atrial fibrillation
  • bradycardia
  • breast-feeding
  • cerebrovascular disease
  • children
  • corticosteroid therapy
  • diabetes mellitus
  • diarrhea
  • GI disease
  • heart failure
  • hepatic disease
  • hypokalemia
  • infants
  • inflammatory bowel disease
  • myasthenia gravis
  • neonates
  • organ transplant
  • pregnancy
  • pseudomembranous colitis
  • QT prolongation
  • quinolone hypersensitivity
  • seizure disorder
  • sunlight (UV) exposure
  • tendinitis
  • tendinopathy
  • tendon pain
  • tendon rupture
  • torsade de pointes
  • ulcerative colitis
  • viral infection

Interactions

No information is available regarding drug interactions associated with Grepafloxacin