Pefloxacin

Pefloxacin is an antimicrobial agent. It is a synthetic fluoroquinolone, belonging to the 3rd generation of quinolones.

Additional recommended knowledge

Essential Laboratory Skills Guide

Recognize and detect the effects of electrostatic charges on your balance

Safe Weighing Range Ensures Accurate Results

Mode of Action

• Chromosomal DNA in bacterial cells occurs mainly in the form of a double stand ring.
• One of a group of bacterial enzymes- DNA gyrase is responsible for the supercoiling process.
• Pefloxacin bactericidal affect is due to its ability to inhibit the activity of this vital enzyme.
• The result of this inhibitions is the prevention of bacterial DNA replication.
• Although inhibition of DNA replication is undoubtedly the chief means by which Abaktal exerts its antibacterial effect, two other actions are also observed:
  • Pefloxacin reduces the ability of E-coli and staphylococcus to adhere to the walls of uroephithelial cells.
  • Pefloxacin has effects on the immune system, stimulating the phagocytic activity of white blood.

Spectrum of antibacterial activity

• Extensive in vitro & in vivo testing has established that Abaktal has a broad antibacterial spectrum.
• The MICs of Pefloxacin even against bacteria resistant to beta-lactams and aminoglycosides are very low
• Initial plasma level of 4.0 mcg/ml, well above M.I.C. for sensitive pathogens, are ready and rapidly attained after a single 400mg dose (oral or i.v.)
• Excellent tissue penetration level is achieved with Pefloxacin in human and animals studies
• Species usually sensitive (MIC < 1pg/ml)are Escherichia coli, Klebsiella, Enterobacter, Serratia, Proteus mirabilis, Proteus vulgaris, Citrobacter, Salmonella, Shigella, Haemophilus influenzae, Staphylococcus aureus, and Neisseria gonorrhoeae.
• Species variably sensitive include Streptococcus and Pneumococcus, Pseudomonas aeruginosa, Acinetobacter, Clostridium perfringens, Mycoplasma, and Chlamydia.

Pharmacokinetics

• After oral administration, Abaktal is well absorbed; the bio availability is 100%.
• Peak plasma levels is reached in 1-1.5 hours
• Peak serum levels of 3.8-6.6mcg/ml is attained after single dose of 400mg
• Peak serum levels after multiple dose of 400mg, 12 hourly is 8-10 mcg/ml
• Steady state concentration is achieved
• Dose depended increase in plasma level over the dose of 200- 800mg
• Food slows the absorption but does not effects bio availability
• Oral & injectable forms are bio-equivalent
• Elimination half life is 11-12 hours mainly through metabolites
• Pefloxacin is metabolized in liver (85%-90%)
• Plasma protein binding is 20-30%
• Major route of elimination is renal – 9-16% of the drugs is eliminated unchanged
• Major metabolites constitute up to 84% of drugs recovered in urine
• Limited excretion via bile
• N-dismethyl pefloxacin (norfloxacin) activity unknown
• Pefloxacin N-oxide active
• Oxodimethyl activity unknown
• Oxo pefloxacin activity unknown
• Pefloxacin achieves high tissue concentration

Tissue Concentration Bronchial tissues 5 mcg/ml Oropharyngeal concentration 6 mcg/ml Tonsils 9 mcg/ml Maxillary sinus cavity sinus 2.82 mcg/ml, 4.1 mcg/ml, 2-8mcg/ml aspirate sinus cystic fluid nasal secretions Muscles 5.6 mcg /ml Gall bladder 80 mcg /ml Bile 78 mcg /ml Kidney 90 mcg /ml Prostate 10 mcg /ml Gynecological tissue 38 mcg/ml 4-6 higher than serum conc., Myometrium- 38.6 mcg /ml, Fallopian tube 31.9 mcg /ml, Ovaries 44.8mcg/ml Pancreatic tissue 4.6mcg/ml Peritonium 3.5mcg/ml

• There are no major change in plasma pharmacokinetics as a function of renal impairment
• Elimination half life increase slightly to approx.15 hours
• There is a fall in urinary excretion of Abaktal & its metabolites
• There is no major change in Abaktal plasma levels whatever the degrees of renal impairment
• Pefloxacin is not readily dialyzed
• There are marked changes in pharmacokinetics in patients with hepatic impairment
• Marked increase in :
  • Elimination half life 3-5 times
  • Area under curve 3-6 times
  • Urinary excretion of unchanged Abaktal 3-4 times
• Careful monitoring of plasma levels together with appropriate dosage adjustment will be necessary

Indications

Indicated for the following conditions:

• Respiratory infections
• Ear, nose and throat infections
• Renal and urinary infections
• Gynaecological infection
• Abdominal and hepato-biliary infections
• Bone and joint infections
• Skin and soft tissue infection
• Septicaemia and endocarditis

Contraindications

• Children or adolescents
• Pregnant women
• Nursing mothers
• History of hypersensitivity to quinolones
• Patients with a history of tendon lesion tendinitis or tendon rupture

Precaution & side effects

Precautions

• Hepatic dysfunction
• Avoid exposure to sunlight during treatment

Side effects

• Nausea
• Skin rash
• Photo sensitivity reaction
• Insomnia
• Headache
• Myalgia
• Thrombo-cytopenia

Drug comparisons

Pefloxacin vs. Ciprofloxacin

Pefloxacin vs. Norfloxacin

Dosage & Presentation

Oral Tablets: 400mg Twice daily

Injection: Administer by slow I.V. at a dosage of 400mg diluted in 100 or 250 ml of 5% isotonic solution (Over a period of 1 hr) Twice daily