Pefloxacin is an antimicrobial agent. It is a synthetic fluoroquinolone, belonging to the 3rd generation of quinolones.
Additional recommended knowledge
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.
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
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
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,
Pancreatic tissue 4.6mcg/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
Indicated for the following conditions:
Ear, nose and throat infections
Renal and urinary infections
Abdominal and hepato-biliary infections
Bone and joint infections
Skin and soft tissue infection
Septicaemia and endocarditis
Children or adolescents
History of hypersensitivity to quinolones
Patients with a history of tendon lesion tendinitis or tendon rupture
Precaution & side effects
Avoid exposure to sunlight during treatment
Photo sensitivity reaction
Pefloxacin vs. Ciprofloxacin
Pefloxacin 400mg oral Ciprofloxacin 500mg oral
Bioavailability 100% 50-70%
Peak plasma conc.(mcg/ml) 8-10 2.3-2.7
Trough 4-5 0.3-0.4
Plasma half life (hours) 11-12 4-5
Pefloxacin vs. Norfloxacin
Pefloxacin 400mg oral Norfloxacin 400mg oral
Absorption 100% 30-40%
Peak plasma conc.(mcg/ml) 4-5 1.4-1.6
Plasma protein binding 30% 15%
Plasma half life (hours) 11-12 3-4
Urinary Excretion 60% 30-50%
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)