Pefloxacin
| File:Pefloxacin.svg | |
| Clinical data | |
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| ATC code | |
| Pharmacokinetic data | |
| Bioavailability | 100% |
| Protein binding | 20–30% |
| Metabolism | Hepatic |
| Elimination half-life | 8.6 hours |
| Excretion | Mostly renal, also biliary |
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| E number | {{#property:P628}} |
| ECHA InfoCard | {{#property:P2566}}Lua error in Module:EditAtWikidata at line 36: attempt to index field 'wikibase' (a nil value). |
| Chemical and physical data | |
| Formula | C17H20FN3O3 |
| Molar mass | 333.358 g/mol |
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Pefloxacin is an antimicrobial agent. It is a synthetic fluoroquinolone, belonging to the 3rd generation of quinolones.
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, Protues vulgaris, Citrobacter, Salmonella, Shigella, Haemophilus influenzae, Staphalococcus aureus, and Neisseria gonorrhoea.
- 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 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) Twice daily
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- Fluoroquinolone antibiotics