Ciprofloxacin chemical structure
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Cipro

Ciprofloxacin is the generic international name for the synthetic antibiotic manufactured and sold by Bayer Pharmaceutical under the brand names Cipro® and Ciproxin® (and other brand names in other markets, e.g. veterinary drugs), belonging to a group called fluoroquinolones. Ciprofloxacin is bactericidal and its mode of action depends on blocking of bacterial DNA replication by binding itself to an enzyme called DNA gyrase, which allows the untwisting required to replicate one DNA double helix into two. more...

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Notably the drug has 100 times higher affinity for bacterial DNA gyrase than for mammalian.

Activity

Ciprofloxacin is a broad-spectrum antibiotic that is active against both Gram-positive and Gram-negative bacteria.

  • Enterobacteriaceae
  • Vibrio
  • Haemophilus influenzae
  • Neisseria gonorrhoeae
  • Neisseria menigitidis
  • Moraxella catarrhalis
  • Brucella
  • Campylobacter
  • Mycobacterium intracellulare
  • Legionella sp.
  • Pseudomonas aeruginosa
  • Bacillus anthracis - that causes anthrax

Weak activity against:

  • Streptococcus pneumoniae
  • Chlamydia trachomatis
  • Chlamydia pneumoniae

No activity against:

  • Bacteroides
  • Burkholderia cepacia
  • Enterococcus faecium
  • Ureaplasma urealyticum
  • and others

The major adverse effect seen with use of is gastrointestinal irritation, common with many antibiotics. Because of its general safety, potency and broad spectrum activity, ciprofloxacin was initially reserved as a "last-resort" drug for use on difficult and drug-resistant infections. As with any antibiotic, however, increasing time and usage has led to an increase in ciprofloxacin-resistant infections, mainly in the hospital setting. Also implicated in the rise of resistant bacteria is the use of lower-cost, less potent fluoroquinolones, and the widespread addition of ciprofloxacin and other antibiotics to the feed of farm animals, which leads to greater and more rapid weight gain, for reasons which are not clear.

Label information

The drug is available for oral and parenteral use. It is used in lower respiratory infections (pneumonias), urinary tract infections, STDs, septicemias, Legionellosis and atypical Mycobacterioses. Dosage in respiratory infections is 500-1500 mg a day in 2 doses.

It is contraindicated in children, pregnancy, and in patients with epilepsy. Dose adjustment or avoidance may be necessary with liver or renal failure.

Ciprofloxacin can cause photosensitivity reactions and can elevate plasma theophylline levels to toxic values. It can also cause constipation and sensitivity to caffeine.

Interactions

Quercetin, a flavonoid occasionally used as a dietary supplement may interact with fluroquinolones, as quercetin competitively binds to bacterial DNA gyrase. Some foods such as garlic and apples contain high levels of quercetin. Whether this inhibits or enhances the effect of Fluoroquinolones is not immediately clear.

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Cipro beats amoxicillin-clavulanate in cystitis study: young women, uncomplicated cystitis - News
From OB/GYN News, 11/1/03 by Bruce Jancin

CHICAGO -- Amoxicillin-clavulanate is clearly inferior to ciprofloxacin for treatment of uncomplicated cystitis in young women--even in those infected with a uropathogen strain susceptible to amoxicillin-clavulanate, Dr. Thomas M. Hooten reported.

In an era when concern over the high rate of resistance to trimethoprim / sulfamethoxazole among the Escherichia coli responsible for most uncomplicated cystitis has led to increased use of alternative agents, amoxicillin-clavulanate is not the way to go, according to Dr. Hooten of the University of Washington, Seattle.

He presented a randomized trial in which 321 young women with uncomplicated cystitis received 3 days of ciprofloxacin at 250 mg b.i.d, or amoxicillin-clavulanate at 500 mg b.i.d, and were then followed for 4 months. The mean age of participants was 24 years; nearly three-quarters had a history of prior urinary tract infection. Compliance with all six doses of medication was 98% in both study arms, Dr. Hooten said at the annual Interscience Conference on Antimicrobial Agents and Chemotherapy.

Clinical cure rates were significantly better in the ciprofloxacin group at every time point during follow-up. (See chart.)

Laboratory studies demonstrated that while 98.2% of strains of the causative uropathogen were sensitive to ciprofloxacin and 0.3% were resistant to the fluoroquinolone, only 75.2% of isolates were sensitive to amoxicillin-clavulanate and 9.4% were resistant to the drug.

Even among amoxicillin-clavulanate-susceptible strains, however, the clinical cure rate after a course of amoxicillin-clavulanate ranged from a mere 76% at 2 weeks' follow-up to 57% at 8 weeks and 52% at 12 weeks. These rates of freedom from urinary tract infection were significantly lower than in the ciprofloxacin group at each time point.

"This is in keeping with the poor performance of other [beta]-lactams in the treatment of urinary tract infections," the physician said at the conference, which was sponsored by the American Society for Microbiology.

Amoxicillin-clavulanate was also much more likely to cause GI and vaginal side effects. Seventeen percent of women on the drug reported vaginal discomfort, compared with 7% in the ciprofloxacin group. Sixteen percent of amoxicillin-clavulanate--treated patients complained of loose stools, compared with 3% on ciprofloxacin.

COPYRIGHT 2003 International Medical News Group
COPYRIGHT 2003 Gale Group

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