Ciprofloxacin in Brief
- Generic name : Ciprofloxacin hydrochloride
- Brand names: Cipro, Ciprobay, Ciproxin, Ciproxine,
- Therapeutic class: Antibiotic
- Pharmacologic class: Fluoroquinolone, 2ng generation
- FDA Approved: October 22, 1987
- Pregnancy Category: C
- Originally discovered: 1981, Bayer, Germany
The discovery and development of ciprofloxacin is that rare case of
an actual groundbreaking new drug development, opening up an entire
new class of antibiotics for further research, development, and marketing.
Ciprofloxacin was the first fluoroquinolone to be on the market.
It was discovered in 1981 by Bayer, the German-based drug and chemical
company. In 1987 Cipro was approved by the FDA in the United States
as the first oral broad-spectrum antibiotic of this class. An intravenous
formulation followed in 1991. Cipro has been extensively studied and
its safety profile is well documented in more than 32,000 publications.
FDA approved uses
- Urinary tract infections: urethritis (infection of the urethra),
cystitis (infection of the bladder ), pyelonephritis (infection of
- Acute uncomplicated cystitis in women.
- Chronic bacterial prostatitis. Ciprofloxacin 500 mg twice daily for 28 days provides one of the most cost effective treatment for chronic bacterial prostatitis 33.
- Lower respiratory infections (pneumonia, bronchitis, tracheobronchitis).
Ciprofloxacin is not a drug of first choice in the treatment of pneumonia
secondary to Streptococcus pneumoniae. Ciprofloxacin has poor activity against S. pneumoniae, and its use has been associated with the rapid emergence of resistance in pneumococci 12.
- Acute sinusitis (inflammation of the paranasal sinuses). However, ciprofloxacin is not recommended by IDSA Guideline due to limited activity against Streptococcus pneumoniae.
- Skin and skin structure infections: cellulitis (infection of the
dermis and subcutaneous tissue), erysipelas (superficial form of cellulitis),
folliculitis (inflammation of the hair follicles, if the infection
of the follicle is deeper and involves more follicles, it moves into
the furuncle and carbuncle), furuncles, carbuncles, abscesses, impetigo, infected ulcers and infected
burns and other.
- Bone and joint infections: septic (infectious) arthritis (infection
in the fluid and tissues of a joint), osteomyelitis (bone infection).
- Complicated intra-abdominal infections: those in which an operation would not remove all of
the infected tissue. Intra-abdominal infections include: intra-abdominal
abscess, peritonitis (infection of the abdominal cavity and its lining),
cholecystitis, cholangitis, diverticulitis and some other.
- Infectious diarrhea: Escherichia coli infection, Campylobacter infection, and Shigellosis.
- Typhoid fever (enteric fever) .
- STDs: uncomplicated cervical and urethral gonorrhea
- Complicated urinary tract infections and pyelonephritis in children (1 to 17 years of age)
- Inhalational anthrax (post-exposure) to reduce the incidence or
progression of disease following exposure to aerosolized Bacillus
anthracis (in adults and children)
Ciprofloxacin is FDA-approved for inhalational anthrax and complicated UTI and pyelonephritis in children.
Ciprofloxacin is NOT effective in the treatment of syphilis.
Off-label & Investigational uses
- Chlamydia infections 2, 3.
In general, ciprofloxacin is not the best option for Chlamydia infections.
Although it has good activity against Chlamydia in laboratory environment,
ciprofloxacin even in high dosages of 2 g daily is insufficient for
treatment and often results in relapsing infection
3. Doxycycline and azithromycin
are more effective options for Chlamydia.
- Mycoplasma infections 15.
Ciprofloxacin is not the optimal antibiotic for pneumonia caused by
Mycoplasma pneumoniae 16,
however it may be effective for genital Micoplasma infections.
- Gonorrhea in adolescents 23.
Single 500-mg dose of ciprofloxacin is among the
recommended treatments by Centers for Disease Control and Prevention (CDC) for uncomplicated gonorrhea infection in adolescents.
- Pelvic inflammatory disease (PID) 11-13.
PID is the infection of the upper female reproductive organs. PID
can affect the cervix (cervicitis), uterus (endometritis), fallopain
tubes (salpingitis) and ovaries (oophoritis). Ciprofloxacin is not
an optimal treatment for pelvic inflammatory disease if
used alone 14.
- Inflammatory bowel diseases (IBD) 9-10.
The research suggests that ciprofloxacin produces anti-inflammatory
effect on intestinal inflammation.
- Chronic ear disease 30-31.
Chronic suppurative otitis media is a common and potentially dangerous
chronic ear disease that is difficult to treat, because the most common
infecting organisms are often resistant to many antibiotics. Ciprofloxacin
is an effective treatment for suppurative chronic otitis media in
adults. The research study demonstrated that ciprofloxacin can also
effectively treat suppurative otitis media in children.
- Salmonellosis 22.
In severe salmonellosis, short treatment with ciprofloxacin is safe
and promotes rapid recovery.
- Legionnaires' disease (Legionella pneumonia) 29.
Legionnaires' disease is a pneumonia caused by bacteria Legionella
pneumophila. Intravenous ciprofloxacin is effective treatment of Legionella
- Cystic fibrosis 26.
Cystic fibrosis (mucoviscidosis) is a hereditary disease that mainly
affects the lungs and digestive system. Antibiotics are often used to help
prevent or fight infections in persons with cystic fibrosis.
Fluoroquinolones are effective against most gram-positive and gram-negative
organisms. They are the only class of oral antibiotics effective against
P. aeruginosa. According to the studies, Ciprofloxacin may be safe
and effective in young persons with bronchopulmonary exacerbation of cystic fibrosis.
- Tuberculosis 27-28.
Ciprofloxacin may be an effective option for tuberculosis in persons
who cannot use conventional anti-tuberculosis medications or for multidrug-resistant
- Cat-scratch disease in adults 17.
Cat scratch fever is a usually benign infectious disease caused by
the intracellular parasite Bartonella. Ciprofloxacin appears to be
an effective treatment for cat-scratch disease.
- Brucellosis 19-20.
Brucellosis (also known as undulant fever or Malta fever) is infectious
disease transmitted from animals to humans and exists worldwide. It
is caused by bacteria Brucella. Despite the high in vitro (in test-tube)
activity of antibiotic against brucella, the treatment of brucellosis
frequently results in therapeutic failures and relapse of infection
18. Combination of ciprofloxacin
with rifampicin may be quite effective for serious cases of this disease
- Cholera 21.
Cholera is an extreme diarrheal disease caused by the bacterium Vibrio
cholerae. Single-dose ciprofloxacin is an effective treatment of severe
cholera in adults and children.
- Tularemia 24.
Tularemia (rabbit fever) is a serious infectious disease caused by
the bacterium Francisella tularensis. Oral ciprofloxacin may be an
effective alternative to injection therapy.
Spectrum of activity
- Campylobacter jejuni
- Citrobacter koseri (diversus)
- Citrobacter freundii
- Enterobacter cloacae
- Escherichia coli
- Haemophilus influenzae
- Haemophilus parainfluenzae
- Klebsiella pneumoniae
- Moraxella catarrhalis
- Morganella morganii
- Neisseria gonorrhoeae
- Proteus mirabilis
- Proteus vulgaris
- Providencia rettgeri
- Providencia stuartii
- Pseudomonas aeruginos -- best activity among Fluoroquinolones
- Salmonella typhi
- Serratia marcescens
- Shigella boydii, Shigella dysenteriae, Shigella flexneri, Shigella sonnei
Note: Ciprofloxacin has the strongest Gram-negative activity of the quinolones.
Ciprofloxacin has only moderate activity against Gram-positive bacteria such as Streptococcus pneumoniae and Enterococcus faecalis.
Most anaerobic bacteria are not susceptible.
Ciprofloxacin is active against Bacillus anthracis.
Moderate activity against atypical bacteria, but good activity against Legionella pneumophila.
Ciprofloxacin "pros" and "cons"
- Ease of use - twice daily regimen.
- Broad spectrum of antibacterial activity.
- Ciprofloxacin is the only fluoroquinolone currently approved for
post-exposure prophylaxis of anthrax.
- Excellent bioavailability both orally and intravenously. Oral
ciprofloxacin is 70-80% bioavailable, meaning that a 500 mg oral
dose gives plasma concentrations in the same range as a 400 mg IV dose.
- Good tissue penetration (especially in kidneys, gallbladder, liver,
lungs, gynecological tissue).
- Unique characteristic of ciprofloxacin is its excellent penetration into prostate
tissue, with concentrations above those reached in most other tissue22.
- Inexpensive and is available in generic version.
- Does not cause a significant prolongation in the QT interval 1.
- Most effective antibiotic against P. aeruginosa (bacteria that
causes infections of the pulmonary tract, external ear, urinary
tract, burns, and wounds and is the most frequent colonizer of medical
devices (e.g. catheters), which is becoming increasingly resistant.
- Experience is favorable and extensive for nosocomial pneumonia,
osteomyelitis, neutropenic fever, travelers diarrhea, chronic prostatitis and UTIs.
- Poor activity against Streptococcus pneumoniae -- major cause of pneumonia and meningitis.
- Several serious drug interactions (e.g. theophylline, propranolol).
Ciprofloxacin can inhibit (prevent the activity) one of the pathways
that is used to eliminate medications from the body. This pathway,
called CYP1A2, works through an enzyme in the liver known as cytochrome
P450 1A2. If CYP1A2 is inhibited, and the dose
is not reduced, the medicine could accumulate in the body to levels
that could cause serious adverse reactions.
- Widespread use of Ciprofloxacin, often inappropriate, resulted
in increasing rates of microbial resistance (development of resistance
in P. aeruginosa, Salmonella, Neisseria gonorrhoeae).
- Tendon damage. Achilles tendon is the most susceptible,
however other tendons also may be affected. Usually, spontaneous
tendon rupture occurs during or shortly after a course of antibiotic,
but symptoms may occur months after taking the medication. Risk
factors for tendon damage include use of corticosteroids, hypercholesterolemia,
gout, rheumatoid arthritis, advanced age, long-term dialysis, and renal transplantation.
- Peripheral neuropathy (peripheral nervous system side effects).
The symptoms of neuropathy include pain, burning, tingling, numbness,
and/or weakness, or is found to have deficits in light touch, pain,
temperature, position sense, vibratory sensation, and/or motor strength.
Ciprofloxacin should be stopped if person experiences these symptoms
in order to prevent the development of an irreversible condition.
- Severe allergic reactions.
- Crystalluria (crystals in the urine). Ciprofloxacin may induce
calculi (kidney stones) via urinary supersaturation. The risk is
higher when urinary pH is greater than 7.3 and antibiotic doses
are greater than 1000 mg.
- Absorption may be significantly reduced by dairy products.
Ciprofloxacin should not be taken with dairy or calcium-fortified
juices alone. However, it may be taken with a meal that contains
these products (e.g. cereal with milk).
- Decrease the metabolism of caffeine (the half-life of caffeine
significantly increases) 7.
- Rare cases of vision disturbance 8.
- Ciprofloxacin may delay the fracture healing 25.
The research data suggest that use of ciprofloxacin during early
fracture repair may compromise the clinical course of fracture-healing.
Mode of action
Ciprofloxacin is a synthetic bactericidal antibiotic that inhibits
bacterial nuclear DNA synthesis, so that bacteria rapidly die. The target
is the enzyme DNA gyrase (topoisomerase II), which is responsible for
the supercoiling and uncoiling of the DNA. Supercoiling of the DNA allows
the long DNA molecule to fit into the cell. Uncoiling of the structure
is the initiative step for replication, transcription, and repair of
the DNA. Thus, prolonged inhibition will lead to the death of the cell.
Time for Ciprofloxacin to clear out the system
Ciprofloxacin half-life is 3-5 hours. So it takes about 15-24 hours to clear out of the system.
Ciprofloxacin during pregnancy and lactation
While there are no controlled studies of ciprofloxacin use in pregnant
women to show safety, an expert review of published data on experiences
with ciprofloxacin use during pregnancy by TERIS - the Teratogen Information
System - concluded that therapeutic doses during pregnancy are unlikely
to produce substantial teratogenic risk, but the data are insufficient
to state that there is no risk 5.
- One publication described 6 pregnant women exposed to longer durations
of ciprofloxacin therapy (3 weeks to 3 months) who delivered normal
- There has also been a case report of a pregnant woman exposed to
three weeks of ciprofloxacin therapy during early third trimester
who delivered a normal baby 5.
Ciprofloxacin is excreted into breast milk but is considered as "usually
compatible with breastfeeding" by the American Academy of Pediatrics.
Ciprofloxacin and Tendon damage
Clinical reports, histopathologic (microscopic examination of tissue)
findings, and an experimental animal model support a relationship between
fluoroquinolone use and tendon ruptures. In some cases changes in tendon
tissue associated with fluoroquinolones may not be completely reversible.
According to reports from France, fluoroquinolones associated with
tendon ruptures include, in decreasing order of risk, pefloxacin, ofloxacin,
norfloxacin, and ciprofloxacin. The risk associated with pefloxacin
has been estimated to be 1 case per 23,130 treatment days, and for ciprofloxacin,
1 case per 779,600 treatment days 6.
Effects on tests
Like other fluoroquinolones, ciprofloxacin may result in false positive opiate screen (JAMA 2001;286:3115-9).
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Published: March 31, 2008
Last updated: July 16, 2014
- Ciprofloxacin is a rare case where the first discovered member
of the class remains the 'gold standard' in terms of efficacy, with
the other drugs developed by other pharmaceutical companies relegated
to 'me-too' status and forced to compete on the basis of lower cost.
- In 2004, ciprofloxacin became the first fluoroquinolone approved for use in children 1-17 years of age.