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Post by Velsundar » Tue Oct 24, 2017 10:31 am


An antibiotic which belongs to the group called Fluoroquinolones
Exhibit concentration dependent bactericidal activity
It inhibits the activity of DNA grrase and topoisomerase and enzyme essential for bacterial DNA replication

Ciproflxacin - oral or parenteral
Gemifloxacin - oral
Fluoroquinolones are divided into 2 groups based on antimicrobial spectrum and pharmacology
Older group : ciprofloxacin, norfloxacin and ofloxacin
Newer group : Gemifloxacin, levofloxacin and moxifloxacin
Many newer fluoroquinolones like trovfloxacin, gatifloxacin, grepafloxacin, temafloxacin and lomefloxacin, sparfloxacin and enxacin have been withdrawn due to severe toxicity

Oral absorption is diminished by coadministration of aluminium, Mg, Ca, Zinc and Iron prepatations
Fluoroquinolones get widely distributed in most extracellular and intracellular fluids
Get concentrated in prostate, lungs and bile
Get metabolized in liver
Excreted in urine reaching high levels in urine
(Moxifloxacin is eliminated primarily in bile)

Infections by
Haemophilus influenzae
Moraxella catarrhalis
Mycoplasma sp
Chlamydia sp
Legionella sp
Pseudomonas aeriginosa (paricularly cipro)
Mycobacterium tuberculosis
Some atypical mycobacteria
Methicillin-sensitve staphylococci
Nosocomial methicillin resistant staphylococci are usually resistant
Older fluoroquinolones less active against streptococci and anaerobes
Newer fluoroquinolones more active against streptococci and anaerobes

Clinical Uses
Fluoroquinolones (except moxifloxacin) used for E.coli resistant to trimethoprim/sulfamethoxazole
Bacterial prostatitis
Salmonella bacterimia
Typhoid fever
Infectious diarrheas (bacterial diarrhoeas by Campylobacter sp., Salmonellae, Shigellae, vibrios, Yersinia enterocolitica; but not effective against Clostridium difficile)

Ofloxacin - Chlamydia trachomatis
Newer fluoroquinolones - Community-adquired pneumonia
Ciprofloxacin - Hospital - acquired pneumonia, Long-term oral treatment of gram-negative bacillary or staphylococcus aureus osteomyelitis
Meningococcal prophylaxis
Anthrax prophylaxis

Pregnancy & Lactation
Fluoroquinolones are in pregnancy category C - clinical benefit sometimes exceeds risk
Fluoroquinolones enter breast milk. Use during breastfeeding is not recommended.

Adverse Effects
Serious adverse effects are uncommon;
Upper GI adverse effects occur in about 5% of patients because of direct GI irritation and CNS effects.
CNS - mild headache, drowsiness, insomnia, dizziness, mood alteration
NSAIDs may enhance the CNS stimulatory effects of fluoroquinolones.
Fuoroquinolones should not be used in patients with CNS disorders.
Peripheral neuropathy may occur soon after taking the drug and may be permanent.
If symptoms occur (eg, pain, burning, tingling, numbness, weakness, change in sensation), use of the fluoroquinolone should be stopped to prevent irreversible damage.
Tendinopathy, including rupture of the Achilles tendon, may occur even after short-term use of fluoroquinolones.
QT-interval prolongation can occur, potentially leading to ventricular arrhythmias and sudden cardiac death.
Pseudomembranous colitis, especially that due to the hypervirulent C. difficile ribotype 027.
Diarrhea, leukopenia, anemia, and photosensitivity are uncommon.
Rash is uncommon unless gemifloxacin is used for > 1 wk and is more likely to develop in women < 40.

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