Norfloxacin (Norflox) is an orally available antibiotic that belongs to the class of medicines called fluoroquinolones. It is used to treat urinary tract infections and diarrhea.

Norfloxacin (Norflox) Uses:

• Susceptible gram-negative and gram-positive bacteria cause uncomplicated and complicated urinary tract infections.
• Sexually transmitted disease (eg, uncomplicated urethral & cervical gonorrhea) caused by N. gonorrhoeae.
• Prostatitis due to E. coli

Note:

• As of April 2007, for the treatment of gonococcal disease, the CDC no longer recommends the use of fluoroquinolones.

• Limitations of use:

  • Reserve norfloxacin for use in patients who have no alternative treatment options for acute uncomplicated urinary tract infections, because fluoroquinolones have been associated with disabling and potentially irreversible serious adverse reactions (eg, tendinitis and tendon rupture, peripheral neuropathy, CNS effects).

• Off Label Use of Norfloxacin in Adults:

  • Infectious Diarrhea
  • Prevention of spontaneous bacterial peritonitis

Norfloxacin (Norflox) Dose in Adults

Note:

• In US, Noroxin is no longer available.

Norfloxacin (Norflox) Dose in the treatment of Prostatitis:

• P/O:
• 400 mg every 12 hours for 4-6 weeks

Norfloxacin (Norflox) Dose in the treatment of Uncomplicated gonorrhea:

• P/O:
• 800 mg as a single dose.

Note:

• The CDC no longer recommends the use of fluoroquinolones for the treatment of uncomplicated gonococcal disease as of April 2007.

Norfloxacin (Norflox) Dose in the treatment of Urinary tract infections: Oral:

• Uncomplicated due to E. coli, K. pneumoniae, P. mirabilis:

  • 400 mg twice daily for 3 days

• Uncomplicated UTI due to other organisms:

  • 400 mg twice daily for 7-10 days,

• Complicated UTI:

  • 400 mg twice daily for 10-21 days,

Norfloxacin (Norflox) Dose in the treatment of Dysenteric enterocolitis (Shigella) (off-label):

• 400 mg twice daily for three days

Norfloxacin (Norflox) Dose in the prevention of spontaneous bacterial peritonitis (SBP) (off-label):

• Prior SBP or low protein ascites:

  • Long-term prophylaxis:
  • 400 mg once daily.

Norfloxacin (Norflox) Dose in the treatment of Variceal hemorrhage:

• Short-term prophylaxis:

  • 400 mg every 12 hours for 7 days.
  • During active GI bleed, may also administer norfloxacin 400 mg every 12 hours for 7 days after a course of IV ceftriaxone.

Norfloxacin (Norflox) Dose in the treatment of Traveler's diarrhea (off-label):

• 400 mg twice daily for three days, a single dose may also be effective.

Use in Children:

Not indicated

Pregnancy Risk Factor C

• Some adverse events were observed in animal reproduction studies.
• Norfloxacin is used to distribute amniotic fluid and cord blood.
• According to available data, norfloxacin has not been shown to increase the risk of teratogenic side effects in pregnancy.

Norfloxacin use during breastfeeding:

• Norfloxacin wasn't detected in the milk of nursing mothers who were given an oral 200mg dose.
• It is unknown if concentrations will be detectable at higher doses or after multiple doses.
• A manufacturer recommends that the mother decide whether to stop nursing her infant or discontinue using the drug. This is in consideration of the possibility of serious adverse reactions.

Dose in Kidney Disease:

• CrCl ≤30 mL/min/1.73 m²:
  • 400 mg once daily

Dose in Liver Disease:

• In the manufacturer’s labeling, no dosage adjustment provided.

Common Side Effects of Norfloxacin (Norflox):

• Central Nervous System:

  • Dizziness
  • Headache

• Gastrointestinal:

  • Nausea
  • Abdominal Cramping

• Hematologic & Oncologic:

  • Eosinophilia

• Hepatic:

  • Liver Enzymes Increased

Less Common Side Effects Of Norfloxacin (Norflox):

• Central Nervous System:

  • Drowsiness

• Dermatologic:

  • Hyperhidrosis
  • Pruritus
  • Rash

• Endocrine & Metabolic:

  • Decreased WBC Count
  • Increased Serum Alkaline Phosphatase

• Gastrointestinal:

  • Abdominal Pain
  • Anorectal Pain
  • Anorexia
  • Constipation
  • Diarrhea
  • Dyspepsia
  • Flatulence
  • Loose Stools
  • Vomiting
  • Xerostomia

• Genitourinary:

  • Proteinuria

• Hematologic And Oncologic:

  • Decreased Platelet Count
  • Leukopenia
  • Thrombocytopenia
  • Decreased Hematocrit
  • Decreased Hemoglobin

• Neuromuscular & Skeletal:

  • Weakness
  • Back Pain

• Miscellaneous:

  • Fever

Contraindications to Norfloxacin (Norflox):

• Hypersensitivity to norfloxacin or quinolones or any other component of the formulation
• Associated with quinolone usage, tendinitis history or tendon rupture.

Warnings and precautions

• Modified cardiac conduction

  • Fluoroquinolones can extend the QTc interval.
  • Avoid use in patients with a history of QTc prolongation, uncorrected hypokalemia, hypomagnesemia, or concurrent administration of other medications known to extend the QT interval (including Class Ia and Class III antiarrhythmics, cisapride, erythromycin, antipsychotics, and tricyclic antidepressants).

• Aneurysm of the aorta and dissection

  • Fluoroquinolones are associated with ruptures of the aorta or dissections within 2 months, especially in elderly patients.
  • Patients with a history of aneurysm should not use fluoroquinolones, or those at higher risk.
  • This includes patients with hypertension, peripheral atherosclerotic diseases, hypertension, and genetic disorders involving blood vessel change (eg, Marfan, Ehlers Danlos syndrome), as well as elderly patients.
  • Risk may be increased by prolonged treatment (e.g., >14 days).

• Regulation of Glucose

  • Fluoroquinolones are often associated with the development of severe, sometimes fatal hypoglycemia.
  • These events are most common in diabetics, but they have also been reported in those without diabetes.
  • It is important to promptly identify and treat hypoglycemia.
  • This effect may be caused by a variety of quinolones.
  • This was evident most with gatifloxacin, which is no longer being marketed as a systemic formulation.
  • The use of fluoroquinolones has been linked to hyperglycemia.
  • Disordered glucose regulation should be checked out by a physician.

• Hypersensitivity reactions

  • Severe hypersensitivity reactions have been reported with quinolone therapy.
  • These reactions can have a wide spectrum.
  • You may experience typical allergic reactions (eg itching, urticaria and rash), or severe idiosyncratic dermatologic symptoms (eg Stevens-Johnson or toxic epidermal Necrolysis), usually following multiple doses.
  • You should immediately stop taking any drugs if you experience a skin rash, or any other symptoms.

• Phototoxicity:

  • Avoid too much sun and take precautions to reduce exposure (e.g., loose-fitting clothes, sunscreen).
  • Phototoxicity reactions may be moderate to severe.
  • If you develop photosensitivity, discontinue using the product.

• Warning: Serious adverse reactions

  • Fluoroquinolones can cause severe and potentially irreversible adverse reactions, such as tendinitis, tendon rupture, peripheral neuropathy, CNS effects, and CNS effects.
  • If you experience any of these severe adverse reactions, stop taking norfloxacin immediately and discontinue using fluoroquinolones.
  • These reactions have been reported by patients of all ages and without any pre-existing risk factors.
  • Initiation can occur in as little as a few hours or even weeks.

• CNS effects

  • Fluoroquinolones are associated with increased CNS risk, including seizures, elevated intracranial pressure (including pseudotumor cebri), and toxic psychosis.
  • It can also lead to anxiety, nervousness, panic, anxiety, nightmares and paranoia.
  • It may occur after the first dose.
  • Fluoroquinolones should be stopped immediately and avoided by patients with these reactions.
  • Patients with a CNS disorder or other risk factors, such as a known or suspected CNS disorder or a seizure threshold lower or predisposing factors, should be cautious.

• Peripheral neuropathy:

  • Fluoroquinolones have been linked to an increased risk for peripheral neuropathy.
  • It may happen soon after the therapy has been initiated.
  • If you experience symptoms of sensorimotor or sensory neuropathy, discontinue use.
  • Patients who have had peripheral neuropathy in the past should not be used.

• Tendinitis/tendon rupture:

  • Fluoroquinolones have been linked to tendinitis and tendon rupture at all ages.
  • Patients over 60 years old, recipients of solid organ transplants, and patients who are concurrently taking corticosteroids may be at greater risk.
  • However, this has also been observed in patients with no risk factors.
  • Most often, ruptures of the Achilles tendon have been reported.
  • However, there have been reports of tendon injuries at other sites, such as the rotator cuff and biceps.
  • Both bilateral inflammation and rupture can occur.
  • Patients have reported cases within hours or days of therapy being initiated, and for several months afterwards.
  • Strenuous physical activity, kidney failure, and previous tendon disorders could all be risk factors for tendon rupture.
  • Do not continue if you feel any tendon pain, swelling or inflammation.
  • Patients with tendon disorders, tendinitis, or tendon rupture should not use this product.

• Superinfection

  • Extended use can lead to fungal and bacterial superinfections, such as C. Difficile -associated diarrhea (CDAD), and pseudomembranous collitis.
  • CDAD was observed for >2 months after antibiotic treatment.

• Myasthenia gravis: [US Boxed Warning]:

  • Might exacerbate muscle weakness due to myasthenia Gravis.
  • Patients with a history of myasthenia gravis should not be given this medication.
  • There have been cases of severe exacerbations, including deaths and ventilatory support.

• Renal impairment

  • Careful when you have a renal impairment
  • Adjustment is required.
  • Increased risk of tendon rupture.

• Rheumatoid arthritis:

  • Patients with rheumatoid arthritis should be cautious.
  • Increased risk of tendon rupture.

• Syphilis:

  • Norfloxacin is not effective in treating syphilis and may mask symptoms. All patients should be tested for it at the time they are diagnosed with gonorrhea.

Norfloxacin (United States: not available): Drug Interaction

Monitoring Parameters:

• If therapy is prolonged, monitor CBC, renal, and hepatic function periodically.

How to administer Norfloxacin (Norflox)?

P/O:

• Hold antacids, sucralfate, or multivitamins/supplements containing iron, zinc, magnesium, or aluminum for at least 2 hours before or after giving norfloxacin.
• Do not administer together.
• On an empty stomach, administer with water (at least 1 hour before or 2 hours after meals, milk, or other dairy products).

Mechanism of action of Norfloxacin (Norflox):

• Norfloxacin acts as a DNA gyrase inhibitor.
• DNA gyrase, an essential bacterial enzyme, is responsible for maintaining the DNA's superhelical structure.
• DNA gyrase is essential for DNA repair and replication, transcription, transposition, and recombination.
• Bactericidal

Absorption:

• P/O:
• Rapid, up to 40%

Protein binding:

• 10%-15%

Metabolism:

• Hepatic

Half-life elimination:

• 3-4 hours.
• Renal impairment (CrCl ≤30 mL/min):
  • 6.5 hours.
• Elderly:
  • 4 hours
• Time to peak serum concentration:
  • 1-2 hours

Excretion:

• Urine (26% to 32% as unchanged drug; 5% to 8% as metabolites).
• Feces (30%)

International Brands of Norfloxacin:

• ALTI-Norfloxacin
• APO-Norfloxacin
• CO Norfloxacin
• PMS-Norfloxacin
• TEVANorfloxacin
• Ambigram
• Anquin
• Ansor
• Apiflox
• Baccidal
• Barazan
• Bexinor
• Biofloxin
• Chibroxin
• Chibroxine
• Chibroxol
• Ectalin
• Epinor
• Euroflox
• Flox
• Floxacin
• Fluseminal
• Fulgram
• Gonorcin
• Gyrablock
• Janacin
• Laxifloxin
• Lexinor
• M-Flox
• Manoflox
• Microxin
• Mitatonin
• Myfloxin
• Naflox
• Negaflox
• Nolicin
• Noracin
• Norax
• Norbactin
• Norbactin Eye Drops
• Norf
• Norflohexal
• Norflox
• Norflox Eye
• Norflox-N
• Norfloxacine
• Norfloxin
• Norfloxin-400
• Norlox
• Normac
• Normax
• Normax Eye Ear Drops
• Noroxin
• Noroxin Oftalmico
• Noroxine
• Norsol
• Nufloxib
• Oprelex
• Oranor
• Orsanac
• Quinox
• Roxin
• Sefnor
• Sofasin
• Uridon
• Uriflox
• Urigen
• Urobacid
• Uroctal
• Uroflox
• Uronor
• Uroxacin
• Uroxin
• UT-in
• Winaflox
• Xacin
• Xasmun
• Zoroxin

Norfloxacin Brand Names in Pakistan: