What is the mode of action of Furazolidone?

Mode of Action of Furazolidone

Furazolidone is a nitrofuran derivative antimicrobial agent that acts through inhibition of bacterial monoamine oxidase and diamine oxidase activities, interfering with bacterial metabolism and energy production. 1

Mechanism of Action

• Furazolidone functions as an antimicrobial with both antibacterial and antiprotozoal properties 2
• It inhibits mono- and diamine oxidase activities in bacteria, which appears to depend on the presence of gut flora in some species 1
• The drug interferes with thiamin utilization, which may contribute to some of its effects and side effects 1
• As a nitrofuran derivative, it disrupts bacterial metabolism and energy production pathways 2

Antimicrobial Spectrum

• Effective against both bacterial and protozoal pathogens that cause diarrheal diseases 3
• Has been used successfully in treating:
  • Bacterial diarrhea and enteritis caused by susceptible organisms 3
  • Cholera (Vibrio cholerae infections) 2, 4
  • Helicobacter pylori infections (as an alternative agent) 2
  • Certain protozoal infections 2

Pharmacokinetic Properties

• Traditionally considered a non-absorbable antimicrobial agent for gastrointestinal infections 5
• However, studies show it does achieve measurable systemic absorption:
  • Peak serum concentrations ≤0.84 mg/L after a single oral dose (5 mg/kg) in adults 5
  • Approximately 4.78% of the ingested dose is excreted in urine 5
  • Can penetrate the blood-brain barrier in cases of meningitis, with cerebrospinal fluid/serum ratios ranging from 1.02 to 5.95 5

Clinical Applications

• Used for specific and symptomatic treatment of bacterial or protozoal diarrhea for over 30 years 3
• Effective in cholera treatment, including as a single dose in children 4
• Alternative agent for Helicobacter pylori infections when other antibiotics cannot be used 2
• Has been used successfully for typhoid fever treatment in some countries 5
• Novel research suggests potential anti-leukemic activity in acute myeloid leukemia through different mechanisms 6

Advantages and Limitations

Advantages:

• Relatively specific antimicrobial action 3
• Effectiveness comparable or superior to other drugs for certain infections 3
• Relatively low toxicity profile for short-term use 3
• Minimizes development of resistant organisms compared to some other antimicrobials 3

Limitations:

• Can cause inhibition of monoamine oxidase, leading to potential drug interactions 1
• Associated with side effects including skin reactions and photosensitivity 2
• No longer widely recommended for many indications due to limited recent data on efficacy and bacterial resistance patterns 2
• Has been shown to possess carcinogenic activity in some animal studies, raising concerns about residues in treated animals 1

Conclusion

Furazolidone acts primarily through inhibition of bacterial monoamine and diamine oxidase activities, disrupting bacterial metabolism. While it has historically been an effective antimicrobial for various gastrointestinal infections, its use has declined in favor of newer agents with better safety profiles and more robust clinical data.