pefloxacin

Action and Spectrum

Actions and Spectrum: 

Actions: 

Like other fluoroquinolones, pefloxacin exerts its antibacterial effects by inhibiting bacterial DNA gyrase and topoisomerase IV enzymes. These enzymes play crucial roles in bacterial DNA replication, transcription, and repair. By interfering with these processes, pefloxacin disrupts the bacterial DNA structure and ultimately leads to the death of the bacterial cell. 

Spectrum: 

pefloxacin has a broad spectrum of activity, making it effective against a variety of bacterial pathogens like: 

Gram-positive bacteria. Here are some examples of bacteria that pefloxacin can target: 

Gram-negative bacteria: 

• Escherichia coli 
• Klebsiella pneumoniae 
• Pseudomonas aeruginosa 
• Enterobacter species 
• Proteus species 
• Salmonella species 
• Shigella species 

Gram-positive bacteria: 

• Staphylococcus aureus  
• Streptococcus pneumoniae 
• Enterococcus species

Drug Interaction

Adverse Reaction

Frequency not defined 

Difficult breathing 

Hives 

Face swelling 

Nausea 

Gastric Pain 

Vomiting 

Photosensitivity 

Black Box Warning

Black Box Warning: 

None 

Contraindication / Caution

Contraindication/Caution: 

Contraindications: 

• Hypersensitivity 
• Tendinitis 
• Tendon rupture 
• Children and adolescents 

Cautions: 

• Renal impairment 
• Elderly patients 
• Seizure disorders 
• Gastrointestinal disorders 
• Cardiovascular disorders 
• Myasthenia gravis 

Pregnancy / Lactation

Pregnancy consideration:  

The drug is contraindicated during pregnancy. 

Breastfeeding warnings:  

The drug is not indicated during lactation.  

Pregnancy category: 

Category A: Well-controlled and satisfactory studies show no risk to the fetus in the initial or later trimester. 

<b>Category B: There was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 

Category C: There was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    

Category X: Drugs listed in this category outweigh the risks over benefits. Hence, these categories of drugs need to be avoided by pregnant women.    

Category N: No data is available for the drug under this category. 

Pharmacology

Pharmacology:  

pefloxacin disrupts the bacterial DNA synthesis process, inhibiting bacterial growth and ultimately causing cell death. pefloxacin’s action is bactericidal, killing bacteria rather than just inhibiting their growth. 

Pharmacodynamics: 

pefloxacin is a fluoroquinolone antibiotic with bactericidal activity. It works by inhibiting two bacterial enzymes: DNA gyrase and topoisomerase IV. These enzymes are involved in DNA replication, transcription, and repair in bacteria. By interfering with these processes, pefloxacin disrupts bacterial DNA synthesis, leading to cell death. 

Pharmacokinetics: 

Absorption: 

pefloxacin is well absorbed after oral administration, and its bioavailability is generally high. Food intake can slightly delay its absorption but does not affect overall absorption. 

Distribution:  

pefloxacin has a relatively large volume of distribution, indicating that it distributes well throughout the body tissues and fluids. It can penetrate various tissues, including the lungs, urinary tract, prostate, and bone. 

Metabolism: 

pefloxacin undergoes minimal metabolism in the liver. The primary metabolic pathway is through de-ethylation to form its main metabolite, norfloxacin. However, the metabolism of pefloxacin is relatively minor compared to some other drugs. 

Elimination and Excretion: 

pefloxacin is primarily excreted unchanged in the urine. Renal clearance is an essential route of elimination. 

Adminstartion

Administration: 

pefloxacin tablets are usually taken by mouth with a full glass of water. They can be taken with or without food. However, taking them on an empty stomach might result in faster absorption. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: pefloxacin 

Pronounced as: pe-flox-a-sin 

Why do we use pefloxacin? 

• Urinary Tract Infections (UTIs): pefloxacin was effective against many bacteria that commonly cause UTIs, such as Escherichia coli, Klebsiella pneumoniae, and Enterobacter species. 
• Respiratory Tract Infections: It could be used to treat lower respiratory tract infections like bronchitis and pneumonia caused by certain bacteria like Streptococcus pneumoniae and Haemophilus influenzae. 
• Gastrointestinal Infections: pefloxacin could be prescribed for treating infections of the gastrointestinal tract, including some cases of diarrhea caused by bacteria like Salmonella and Shigella. 
• Skin and Soft Tissue Infections: pefloxacin might have been used to treat skin infections, especially those caused by Gram-negative bacteria. 
• Sexually Transmitted Infections: pefloxacin could have been used for treating certain sexually transmitted infections, such as gonorrhea, caused by susceptible strains of Neisseria gonorrhoeae. 
• Bone and Joint Infections: In some cases, pefloxacin might have been used for treating bone and joint infections.