Ciprofloxacin
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, eg. veterinary drugs), belonging to a group called fluoroquinolones. Ciprofloxacin is bactericidal. Its mode of action depends upon blocking bacterial DNA replication by binding itself to an enzyme called DNA gyrase, thereby preventing the enzyme's ability to untwist the DNA double helix, which is required for DNA replication.
Activity
Ciprofloxacin is a broad-spectrum antibiotic that is active against both Gram-positive and Gram-negative bacteria.
Weak activity against:
No activity against:
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.
In cell culture it is used to treat infection with mycoplasma.
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. Ciprofloxacin is also known to cause swelling of certain joints and cartilage.
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 entirely clear.
Contraindications
Metal cations such as aluminium, magnesium, calcium, ferrous sulfate, and zinc are thought to form chelation complexes with fluoroquinolone antibiotics and prevent the drugs from being absorbed. Because of this, avoid taking antacids which contain aluminium, magnesium or calcium with ciprofloxacin. Sucralfate, which has a high aluminium content, also reduces the bioavailability of ciprofloxacin to approximately 4%. Ciprofloxacin may be taken with meals or on an empty stomach. Ciprofloxacin should not be taken with dairy products or calcium-fortified juices alone, but may be taken with a meal that contains these products.
Heavy exercise is discouraged, as achilles tendon rupture has been reported in patients taking ciprofloxacin. Achilles tendon rupture due to ciprofloxacin use is typically associated with renal failure.
The toxicity of drugs that are metabolised by the cytochrome P450 system is enhanced by concomitant use of some quinolones. They may also interact with the GABA A receptor and cause neurological symptoms; this is further augmented by certain non-steroidal anti-inflammatory drugs.
Fluoroquinolones are increasingly contraindicated for patients who have been to S.E. Asia due to the growing prevalance of antibiotic resistance to the class of antibiotics in that region.
Dosing
Ciprofloxacin is available in oral tablets (250, 500, 650, and 1000 mg), as well as ready-made infusion bottles (200 and 400 mg). A combination preparation of ciprofloxacin 500 mg and tinidazole 600 mg is marketed under the name Ciplox-TZ® for infections where anaerobes or protozoa together with ciprofloxacin-sensitive aerobes are likely.
Due to its elimination half-life, ciprofloxacin is administered twice daily. No dose adjustments are generally required for mild to moderate renal impairment.
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