What is/are Ciprofloxacin?
Ciprofloxacin (INN) is a second-generation fluoroquinolone antibiotic. Its spectrum of activity includes most strains of bacterial pathogens responsible for respiratory, urinary tract, gastrointestinal, and abdominal infections, including Gram-(-) (Escherichia coli, Haemophilus influenzae, Klebsiella pneumoniae, Legionella pneumophila, Moraxella catarrhalis, Proteus mirabilis, and Pseudomonas aeruginosa), and Gram-(+) (methicillin-sensitive but not methicillin-resistant Staphylococcus aureus, Streptococcus pneumoniae, Staphylococcus epidermidis, Enterococcus faecalis, and Streptococcus pyogenes) bacterial pathogens. Ciprofloxacin and other fluoroquinolones are valued for this broad spectrum of activity, excellent tissue penetration, and for their availability in both oral and intravenous formulations.
Ciprofloxacin is used alone or in combination with other antibacterial drugs in the empiric treatment of infections for which the bacterial pathogen has not been identified, including urinary tract infections and abdominal infections among others. It is also used for the treatment of infections caused by specific pathogens known to be sensitive. In 2010 over 20 million outpatient prescriptions were written for ciprofloxacin, making it the 35th most commonly prescribed drug, and the 5th most commonly prescribed antibacterial, in the US.
It is a second-generation fluoroquinolone antibacterial. It kills bacteria by interfering with the enzymes that cause DNA to rewind after being copied, which stops synthesis of DNA and of protein.
Ciprofloxacin was first patented in 1983 by Bayer A.G. and subsequently approved by the US Food and Drug Administration (FDA) in 1987. Ciprofloxacin has 12 FDA-approved human uses and other veterinary uses, but it is often used for unapproved uses (off-label).
Generic Cipro (CIPROFLOXACIN) is a fluoroquinolone antibiotic used to treat bacterial infections.
Ciprofloxacin is used to treat a number of infections, including infections of bones and joints, endocarditis, gastroenteritis, malignant otitis externa, respiratory tract infections, cellulitis, urinary tract infections, prostatitis, anthrax, and chancroid, as well as:
- Urinary tract infections (recommended as a first-line antibiotic)
- Acute uncomplicated cystitis in females
- Chronic bacterial prostatitis (recommended as a first-line antibiotic choice)
- Lower respiratory tract infections (not recommended as a first-line antibiotic choice)
- Acute sinusitis (not recommended as a first-line antibiotic choice)
- Skin and skin structure infections
- Bone and joint infections
- Infectious diarrhea
- Typhoid fever (enteric fever) caused by Salmonella typhi
- Uncomplicated cervical and urethral gonorrhea (due to N. gonorrhoeae) – however, this indication is no longer effective in some areas (for example, Asian countries, United States (including Hawaii), Canada, and Scotland) due to bacterial resistance. Fluoroquinolones are no longer recommended in the USA for this indication.
Ciprofloxacin is not recommended for the treatment of tuberculosis.
It is also used in combination with other specific drugs:
- Complicated intra-abdominal infections (in combination with metronidazole);
- Empirical therapy for febrile neutropenic patients (in combination with piperacillin)
Oral and intravenous fluoroquinolones are approved by the FDA for use in children for only two indications due to the risk of permanent injury to the musculoskeletal system.
- Complicated urinary tract infections and pyelonephritis due to Escherichia coli
- Inhalational anthrax (postexposure)
Ciprofloxacin is not recommended to treat community-acquired pneumonia (CAP) as a stand-alone first-line agent due to its modest activity against Streptococcus pneumoniae, a common causative pathogen. "Respiratory quiniolones" such as levofloxacin, having greater activity against this pathogen, are recommended as first line agents for the treatment of CAP in patients with important co-morbidities and in patients requiring hospitalization (Infectious Diseases Society of America 2007). The guidelines include a warning that "Data exist suggesting that resistance to macrolides and older fluoroquinolones (ciprofloxacin and levofloxacin) results in clinical failure. Other studies have shown that repeated use of fluoroquinolones predicts an increased risk of infection with fluoroquinolone-resistant pneumococci...."
Ciprofloxacin may be approved for other uses, or restricted, by the various regulatory agencies worldwide.
Ciprofloxacin is available as tablets, syrups, intravenous solutions, and eye and ear drops.
The status of the patient's renal and hepatic functions must also be taken into consideration to avoid an accumulation that may lead to an overdose and the development of toxicity. Ciprofloxacin is eliminated primarily by renal excretion. However, the drug is also metabolized and partially cleared through the liver and the intestines. Modification of the dosage is 'recommended' using the table found within the package insert for those with impaired liver or kidney function. However, since the drug is known to be substantially excreted by the kidneys, the risk of toxic reactions to this drug may be greater in patients with impaired renal function. The duration of treatment depends upon the severity of infection, and is usually seven to 14 days.
The safety of fluoroquinolones is similar to that of other antibiotics. In most, adverse reactions are mild to moderate; but serious adverse effects occur on occasion.
49,038 patients received courses of ciprofloxacin in pre-approval clinical trials. Most of the adverse events reported were described as only mild or moderate in severity, abated soon after the drug was discontinued, and required no treatment. Ciprofloxacin was discontinued because of an adverse event in 1% of orally treated patients.
The most frequently reported drug-related events, from clinical trials of all formulations, all dosages, all drug-therapy durations, and for all indications of ciprofloxacin therapy, were nausea (2.5%), diarrhea (1.6%), abnormal liver function tests (1.3%), vomiting (1%), and rash (1%). Other adverse events occurred at rates of <1%.
A number of regulatory actions have been taken as a result of such adverse reactions, which included published warnings, additional warnings and safety information added to the package inserts together with the issuance of "Dear Doctor Letters" concerning the recent addition of black box warnings.
Overdose of ciprofloxacin may result in reversible renal toxicity. Treatment of overdose includes emptying of the stomach by induced vomiting or gastric lavage. Careful monitoring and supportive treatment, monitoring of renal function, and maintaining adequate hydration is recommended by the manufacturer. Administration of magnesium-, aluminium-, or calcium-containing antacids can reduce the absorption of ciprofloxacin. Hemodialysis or peritoneal dialysis removes only less than 10% of ciprofloxacin. Ciprofloxacin may be quantified in plasma or serum to monitor for drug accumulation in patients with hepatic dysfunction or to confirm a diagnosis of poisoning in acute overdose victims.
Mechanism of action
Ciprofloxacin is a broad-spectrum antibiotic active against both Gram-positive and Gram-negative bacteria. It functions by inhibiting DNA gyrase, a type II topoisomerase, and topoisomerase IV, enzymes necessary to separate bacterial DNA, thereby inhibiting cell division.
The effects of 200–400 mg of ciprofloxacin given intravenously are linear; drug accumulation does not occur when administered at 12-hour intervals. Bioavailability is approximately 70-80%, with no significant first pass effect. IV administration produces a similar serum levels as those achieved with administration of 500 mg administered orally. IV administration over 60 min given every 8 h produces similar serum levels of the drug as 750 mg administered orally every 12 h. Biotransformation is hepatic. The elimination half life is 4 h.
This article uses material from the Wikipedia article Ciprofloxacin, which is released under the Creative Commons Attribution-Share-Alike License 3.0.