Ofloxacin; Uses, Dosage, Side effects, Interactions, Pregnancy

Ofloxacin is a quinolone/fluoroquinolone antibiotic. Ofloxacin 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. Notably the drug has 100 times higher affinity for bacterial DNA gyrase than for mammalian. Ofloxacin is a broad-spectrum antibiotic that is active against both Gram-positive and Gram-negative bacteria.

Mechanism of Action of Ofloxacin

Ofloxacin is a quinolone antimicrobial agent. The mechanism of action of ofloxacin and other fluoroquinolone antimicrobials involves inhibition of bacterial topoisomerase IV and DNA gyrase (both of which are type II topoisomerases), enzymes required for DNA replication, transcription, repair and recombination. Ofloxacin has in vitro activity against a wide range of gram-negative and gram-positive microorganisms. Ofloxacin is often bactericidal at concentrations equal to or slightly greater than inhibitory concentrations. Fluoroquinolones, including ofloxacin, differ in chemical structure and mode of action from aminoglycosides, macrolides and beta-lactam antibiotics, including penicillins. Fluoroquinolones may, therefore, be active against bacteria resistant to these antimicrobials. Resistance to ofloxacin due to spontaneous mutation in vitro is a rare occurrence . Although cross-resistance has been observed between ofloxacin and some other fluoroquinolones, some microorganisms resistant to other fluoroquinolones may be susceptible to ofloxacin.

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Quinolones are widely used in infection therapy due to their good antimicrobial characteristics. However, there potential joint chondrotoxicity on immature animals has stood in the way of the therapeutic application of these agents, the exact mechanism of which is still unclear. This study was undertaken to investigate the role of oxidative damage in ofloxacin (one typical quinolones)-induced arthropathy. Chondrocytes from juvenile rabbit joints were incubated with ofloxacin at concentrations of 0, 5, 10, 20, 40 and 80 ug/mL, respectively. The extent of oxidative damage was assessed by measuring the reactive oxygen species level, activities of antioxidant enzymes, and oxidative damage to some macromolecules. It was observed that ofloxacin induced a concentration-dependent increase in intracellular reactive oxygen species production, which may be an early mediator of ofloxacin cytotoxicity. Similarly, ofloxacin resulted in a significant lipid peroxidation, revealed by a concentration-dependent increase in the level of thiobarbituric acid reactive substances. At the same time, ofloxacin induced DNA damage in a concentration-dependent manner for 24 hr measured by comet assay, which may be a cause for overproduction of reactive oxygen species. Furthermore, antioxidant enzyme activities, such as glutathione peroxidase (GPx), catalase and superoxide dismutase (SOD), were rapidly decreased after treatment with ofloxacin. In addition, SOD decline and reactive oxygen species production were strongly inhibited, and the loss in cell viability was partly abated by additional glutathione (GSH), N-acetylcysteine (NAC) and dithiothreitol (DTT). In conclusion, these results clearly demonstrated that ofloxacin could induce oxidative stress, lipid peroxidation and DNA oxidative damage to chondrocytes.

Indications of Ofloxacin

• For the treatment of infections (respiratory tract, kidney, skin, soft tissue, UTI), urethral and cervical gonorrhoea.
• Bladder Infection
• Anthrax
• Anthrax Prophylaxis
• Bone infection
• Conjunctivitis
• Epididymitis
• Hansen’s Disease
• Nongonococcal urethritis
• Otitis Externa
• Prostatitis
• Skin and Subcutaneous Tissue Bacterial Infections
• Spontaneous Bacterial Peritonitis (SBP)
• Travelers’ Diarrhea
• Ulcerative keratitis
• Acute Pelvic inflammatory disease
• Acute, uncomplicated Gonorrhea
• Chronic suppurative Otitis media
• Uncomplicated Cystitis
• Bronchitis
• Campylobacter Gastroenteritis
• Cervicitis
• Chancroid
• Chlamydia Infection
• Epididymitis, Non-Specific
• Epididymitis, Sexually Transmitted
• Gonococcal Infection, Disseminated
• Gonococcal Infection, Uncomplicated
• Joint Infection
• Kidney Infections
• Methicillin-Resistant Staphylococcus Aureus Infection
• Mycobacterium avium-intracellulare, Treatment
• Nongonococcal Urethritis
• Pelvic Inflammatory Disease
• Cervicitis
• Community Acquired Pneumonia (CAP)
• Plague
• Pneumonia
• Prostatitis
• Salmonella Enteric Fever
• Salmonella Gastroenteritis
• Shigellosis
• Skin or Soft Tissue Infection
• Traveler’s Diarrhea
• Tuberculosis, Active
• Urinary Tract Infection

Therapeutic Indications

• Ofloxacin is used in the treatment of acute pelvic inflammatory disease (PID) caused by susceptible C. trachomatis or N. gonorrhoeae, but should not be used if QRNG may be involved or if in vitro susceptibility cannot be tested.
• Ofloxacin is used in adults for the treatment of nongonococcal urethritis and cervicitis caused by Chlamydia trachomatis.
• Ofloxacin is used in adults for the treatment of uncomplicated urinary tract infections (UTIs) (cystitis) caused by susceptible gram-negative bacteria, including Citrobacter diversus,  Enterobacter aerogenes,  Escherichia coli, Klebsiella pneumoniae, … Proteus mirabilis, or Pseudomonas aeruginosa.
• The drug also has been effective in a limited number of adults when used orally for the treatment of uncomplicated urinary tract infections caused by susceptible gram-positive bacteria, including Staphylococcus aureus, S. epidermidis, S. saprophyticus, Enterococcus faecalis (formerly Streptococcus faecalis), viridans streptococci, or Streptococcus agalactiae (group B streptococci). However, because of concerns about emergence of resistant strains of certain gram-positive bacteria (e.g., staphylococci) secondary to widespread use of quinolones, such use should be selective.
• Ofloxacin is used in adults for the treatment of pyelonephritis and other complicated urinary tract infections caused by susceptible gram-negative bacteria, including … C. freundii, Enterobacter, M. morganii,rettgeri. As with other anti-infectives, ofloxacin is more effective in the treatment of uncomplicated UTIs than in complicated infections.
• Ofloxacin is used in adults for the treatment of pyelonephritis and other complicated urinary tract infections caused by susceptible gram-negative bacteria, including C. diversus, E. coli, K. pneumoniae P. mirabilis,Ps. aeruginosa. As with other anti-infectives, ofloxacin is more effective in the treatment of uncomplicated UTIs than in complicated infections. /Included in US product label/
• Ofloxacin is used in adults for the treatment of uncomplicated urinary tract infections (UTIs) (cystitis) caused by susceptible gram-negative bacteria, including … C. freundii,E. cloacae Morganella morganii,
• Ofloxacin is used in adults for the treatment of lower respiratory tract infections, including community-acquired pneumonia (CAP) and acute exacerbations of chronic bronchitis caused by susceptible Haemophilus influenzae or Streptococcus pneumoniae.
• Ofloxacin has been used alone with some success for the treatment of acute exacerbations of bronchopulmonary Ps. aeruginosa infections in adults with cystic fibrosis.
• Ofloxacin also has been effective when used for the treatment of lower respiratory tract infections caused by susceptible Moraxella catarrhalis, S. aureus, viridans streptococci, Enterobacteriaceae, or Ps. aeruginosa.
• Oral ofloxacin has been used in the treatment of Helicobacter pylori infection and duodenal ulcer disease.
• Oral ofloxacin is used for the short-term treatment of travelers’ diarrhea or for the prevention of travelers’ diarrhea in adults traveling for relatively short periods of time to high-risk areas.
• Oral ofloxacin is used for the treatment of shigellosis caused by susceptible Shigella.
• Oral ofloxacin has been effective when used in adults for the treatment of infectious diarrhea caused by susceptible strains of enterotoxigenic E. coli or Shigella.
• Although efficacy of ofloxacin in the treatment of bone and joint infections has not been definitely established, oral ofloxacin has been effective when used in adults for the treatment of mild to moderate bone and joint infections, including osteomyelitis, caused by susceptible Escherichia coli, Enterobacter, Klebsiella oxytoca, K. pneumoniae, Proteus mirabilis, Pseudomonas aeruginosa, Serratia, Staphylococcus aureus, or S. epidermidis.
• Oral ofloxacin has been effective when used alone or in conjunction with amikacin for the treatment of postoperative sternotomy wound or soft tissue infections caused by M. fortuitum. The drug also has been used effectively in a few patients for the treatment of M. fortuitum pulmonary or urinary tract infections.
• Ofloxacin is used as an alternative agent in multiple-drug regimens used for the treatment of multibacillary lepros and also is used in a single-dose rifampin-based multiple-drug regimen for the treatment of single-lesion paucibacillary leprosy
• Fluoroquinolones, including ofloxacin, have been used in multiple-drug regimens for the treatment of active tuberculosis, usually in patients with infections caused by Mycobacterium tuberculosis resistant to first-line agents and in patients intolerant of some first-line agents. Although the potential role of fluoroquinolones and the optimal length of therapy have not been fully defined, the CDC, ATS, and IDSA state that use of fluoroquinolones as alternative agents for the treatment of active tuberculosis can be considered in patients with relapse, treatment failure, or M. tuberculosis resistant to isoniazid and or rifampin or when first-line drugs cannot be tolerated. These experts state that fluoroquinolones should not be considered first-line agents for the treatment of tuberculosis caused by M. tuberculosis susceptible to first-line agents.
• Oral ofloxacin has been recommended as one of several treatment options for the treatment of Legionnaires’ disease.
• Ofloxacin is used for the treatment of epididymitis most likely caused by sexually transmitted enteric bacteria (e.g., E. coli) or when culture or nucleic acid amplification tests are negative for N. gonorrhoeae.
• Oral ofloxacin has been used as follow-up therapy in the treatment of disseminated gonococcal infections caused by susceptible N. gonorrhoeae.
• Oral ofloxacin has been used in men and women for the treatment of acute, uncomplicated urethral and endocervical gonorrhea caused by susceptible Neisseria gonorrhoeae. Although fluoroquinolones (ciprofloxacin, levofloxacin, ofloxacin) were previously considered drugs of choice for the treatment of uncomplicated gonorrhea, the CDC currently states that fluoroquinolones should not be used for the treatment of gonorrhea or any associated infections that may involve Neisseria gonorrhoeae (e.g., pelvic inflammatory disease (PID), epididymitis). Neisseria gonorrhoeae with decreased susceptibility to fluoroquinolones (quinolone-resistant N. gonorrhoeae; QRNG) has been reported with increasing frequency worldwide and is widespread in the US.
• The CDC and others state that ofloxacin can be considered an alternative agent for the treatment of urogenital chlamydial infections caused by C. trachomatis.
• Oral ofloxacin has been used effectively for selective decontamination of the GI tract in granulocytopenic patients. It has been suggested that the drug may be particularly useful for prophylaxis of infection in these patients since it reduces or eradicates gram-negative bacteria from fecal flora but generally does not affect normal anaerobic fecal flora. Oral ofloxacin has been used with some success alone or in conjunction with other anti-infectives for prophylaxis of infection in neutropenic patients with leukemia or other malignancies and for empiric anti-infective therapy in febrile granulocytopenic patients.
• Oral ofloxacin has been effective when used in adults for the treatment of typhoid fever (enteric fever) caused by susceptible strains of Salmonella typhi, including chloramphenicol-resistant strains. However, the precise role of fluoroquinolones compared with other anti-infectives in the treatment of typhoid fever remains to be established.
• Ofloxacin has been used successfully in a limited number of patients for the treatment of various rickettsial infections.
• Fluoroquinolones (e.g., ciprofloxacin, levofloxacin, ofloxacin) have been suggested as alternative agents for the treatment of plague caused by Yersinia pestis and also have been recommended for postexposure prophylaxis following a high risk exposure to Yersinia pestis, including exposure in the context of biologic warfare or bioterrorism. The recommendation for use of fluoroquinolones for treatment or prophylaxis of plague is based on results of in vitro and animal testing. Although human studies are not available, results of in vitro studies indicate that ofloxacin is active against Yersinia pestis and the drug has been effective for the treatment of murine plague infections.
• Ofloxacin otic solution is instilled into the ear canal in patients with tympanostomy tubes for the treatment of acute otitis media caused by susceptible S. aureus, S. pneumoniae, H. influenzae, Moraxella catarrhalis, or P. aeruginosa.
• Ofloxacin otic solution is instilled into the ear canal in patients with perforated tympanic membranes for the treatment of chronic suppurative otitis media (CSOM) caused by susceptible Staphylococcus aureus, Proteus mirabilis, or Pseudomonas aeruginosa. Because commercially available ofloxacin oticsolution is sterile, unlike ciprofloxacin and hydrocortisone otic suspension (which is nonsterile), the ofloxacin otic solution can be used in the treatment of otic infections even when the tympanic membrane is perforated.
• Ofloxacin otic solution is instilled into the ear canal for the treatment of otitis externa caused by susceptible Escherichia coli, Staphylococcus aureus or Pseudomonas aeruginosa.
• Ofloxacin ophthalmic solution is used for the treatment of conjunctivitis caused by susceptible Enterobacter cloacae, Haemophilus influenzae, Proteus mirabilis, Pseudomonas aeruginosa, Staphylococcus aureus, Staphylococcus epidermidis, or Streptococcus pneumoniae. /Included in US product label/
• Ofloxacin ophthalmic solution is used in the treatment of keratitis (corneal ulcers) caused by susceptible Pseudomonas aeruginosa, Propionibacterium acnes, Serratia marcescens, Staphylococcus aureus, S. epidermidis, or Streptococcus pneumoniae; the drug is designated an orphan drug by the US Food and Drug Administration (FDA) for this use. /Included in US product label/

Contra Indications of Ofloxacin

• History of severe hypersensitivity (e.g. anaphylactic reaction) to any other type of betalactam antibacterial agent (penicillins, monobactams and carbapenems).
• Hemolytic anemia
• Liver problems
• Interstitial nephritis
• Subacute cutaneous lupus erythematosus
• Systemic lupus erythematosus
• use should be avoided in pregnant or lactating women, and in children with developing teeth because they may result in permanent staining (dark yellow-gray teeth with a darker horizontal band that goes across the top and bottom rows of teeth), and possibly affect the growth of teeth and bones.
• Allergy
• Avoid taking this medicine if you have a known allergy to it or any other fluoroquinolones.
• Avoid if you have a past history of tendinitis or tendon rupture after using this medicine.
• Myasthenia Gravis

Strengths:  200 mg ,400 mg

Uncomplicated Cystitis

• Due to E. coli or K. pneumoniae: 200 mg PO q12hr for 3 days
• Due to other approved pathogens: 200 mg PO q12hr for 7 days

Side Effects of Ofloxacin

The most common 

• Abdominal or stomach cramps and pain (severe)
• diarrhea (watery and severe), which may also be bloody
• pain, inflammation, or swelling in calves, shoulders, or hands
• allergic reactions like skin rash, itching or hives, swelling of the face, lips, or tongue
• pain, swelling, irritation where injected
• sweating
• skin color change, mild diarrhea
• mild nausea
• loss of appetite
• swelling of feet or legs
• chest pain
• constipation
• cough
• difficulty with breathing
• dizziness
• heartburn

More common

• Abdominal or stomach pain, discomfort, or tenderness
• chills or fever
• headache, severe and throbbing
• joint or back pain
• muscle aching or cramping
• muscle pains or stiffness
• chest pressure or squeezing pain in chest
• excessive sweating
• feeling of heaviness, pain, warmth and/or swelling in a leg or in the pelvis
• sudden tingling or coldness in an arm or leg
• sudden slow or difficult speech
• sudden drowsiness or need to sleep
• fast breathing
• sharp pain when taking a deep breath
• fast or slow heartbeat
• coughing up blood
• decreased amount of urine

Rare

• Anxiety
• change in vision
• seizures
• tremors
• weight loss
• chest pain or tightness
• confusion
• cough
• Agitation
• blurred vision
• chest pain or discomfort
• convulsions
• extra heartbeats
• hallucinations
• headache
• irritability
• lightheadedness
• mood or mental changes
• muscle pain or cramps

Drug Interactions of Ofloxacin

Ofloxacin may interact with following drugs, supplyments, & may change the efficacy of drugs

• antacids that contain aluminum, calcium, or magnesium
• birth control medications
• bismuth subsalicylate
• calcium supplements
• digoxin
• Rosuvastatin
• Duloxetine
• Albuterol
• Topiramate
• Carbamazepin
• Vitamin D3 (cholecalciferol)
• Alprazolam
• Cetirizine
• insulin
• iron supplements
• penicillin
• vitamin A derivatives (e.g. isotretinoin)
• warfarin
• zinc sulfate or gluconate

Pregnancy and Lactation of Ofloxacin

FDA pregnancy category C

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