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Norfloxacin is a synthetic, broad-spectrum fluoroquinolone with antibacterial activity. Norfloxacin inhibits the activity of DNA gyrase, thereby blocking bacterial DNA replication. Norfloxacin concentrates in the renal tubules and bladder and is bactericidal against a wide range of aerobic gram-positive and gram-negative organisms.
Norfloxacin is a synthetic fluoroquinolone (FLUOROQUINOLONES) with broad-spectrum antibacterial activity against most gram-negative and gram-positive bacteria. Norfloxacin inhibits bacterial DNA GYRASE.
Norfloxacin is a Quinolone Antimicrobial. The chemical classification of norfloxacin is Quinolones.
Mechanism of Action of Norfloxacin
The bactericidal action of Norfloxacin results from inhibition of the enzymes topoisomerase II (DNA gyrase) and topoisomerase IV, which are required for bacterial DNA replication, transcription, repair, and recombination. Norfloxacinis a broad-spectrum antibiotic that is active against both gram-positive and gram-negative bacterias. The fluorine atom at the 6 position increases potency against gram-negative organisms, and the piperazine moiety at the 7 position is responsible for anti-pseudomonal activity
or
Fluoroquinolones prolong the QT interval by blocking voltage-gated potassium channels, especially the rapid component of the delayed rectifier potassium current I(Kr), expressed by HERG (the human ether-a-go-go-related gene). According to the available case reports and clinical studies, moxifloxacin carries the greatest risk of QT prolongation from all available quinolones in clinical practice and it should be used with caution in patients with predisposing factors for Torsades de pointes (TdP).
Indications of Norfloxacin
- For the treatment of urinary tract infection
- Treatment of acute or chronic complicated pyelonephritis due to susceptible organisms
- Uncomplicated urinary tract infections (including cystitis)
- Complicated urinary tract infections (restricted use) [13]
- Uncomplicated urethral and cervical gonorrhea (however this indication is no longer considered to be effective by some experts due to bacterial resistance) [14][15]
- Prostatitis due to Escherichia coli.[16]
- Syphilis treatment – Norfloxacin has not been shown to be effective in the treatment of syphilis. Antimicrobial agents used in high doses for short periods of time to treat gonorrhea may mask or delay the symptoms of incubating syphilis.[17]
- Though the fluoroquinolones are sometimes used to treat typhoid and paratyphoid fever, it should be noted here that norfloxacin had more clinical failures than the other fluoroquinolones .[18]
- Cystitis
- Gonococcal cervicitis
- Infectious diarrhea
- Pyelitis
- Pyelonephritis
- Spontaneous Bacterial Peritonitis (SBP)
- Travelers’ Diarrhea
- Urethritis gonococcal
Therapeutic Uses of Norfloxacin
- Anti-Bacterial Agents; Enzyme Inhibitors; Nucleic Acid Synthesis InhibitorsOral norfloxacin is used for the treatment of prostatitis caused by E. coli.
- Oral norfloxacin is used in adults for the treatment of complicated UTIs caused by susceptible E. coli, K. pneumoniae, P. mirabilis, Ps. aeruginosa, S. marcescens, or E. faecalis.
- Oral norfloxacin is used in adults for the treatment of uncomplicated urinary tract infections (UTIs) (including cystitis) caused by susceptible Citrobacter freundii, Enterobacter aerogenes, E. cloacae, Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, P. vulgaris, … Pseudomonas aeruginosa. The drug also is used orally in adults for the treatment of uncomplicated UTIs caused by susceptible Staphylococcus aureus, S. epidermidis, S. saprophyticus, Streptococcus agalactiae (group B streptococci), or Enterococcus faecalis.
- Oral norfloxacin has been used in adults for the treatment of uncomplicated 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 N. gonorrhoeae (e.g., pelvic inflammatory disease (PID), epididymitis).
- Norfloxacin has been used for 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. The most common cause of travelers’ diarrhea worldwide is noninvasive enterotoxigenic strains of E. coli (ETEC), but travelers’ diarrhea also can be caused by various other bacteria including enteroaggregative E. coli (EAEC), Campylobacter jejuni, Shigella, Salmonella, A. hydrophila, P. shigelloides, Yersinia enterocolitica, V. parahaemolyticus, or non-O-group V. cholerae.In some cases, travelers’ diarrhea is caused by parasitic enteric pathogens (e.g., Giardia duodenalis (also known as G. lamblia or G. intestinalis), Cryptosporidium parvum, Cyclospora cayetanensis, Entamoeba histolytica, Dientamoeba fragilis) or viral enteric pathogens (e.g., rotavirus, norovirus).
- Oral norfloxacin is used for the treatment of shigellosis caused by susceptible Shigella. product
- Norfloxacin has been effective when used in the treatment of cholera, including infections caused by Vibrio cholerae serotypes 01 or 0139.
- Norfloxacin has been effective when used in adults for the treatment of gastroenteritis caused by susceptible enterotoxigenic E. coli, Aeromonas hydrophila, Plesiomonas shigelloides, Salmonella, Shigella (including Sh. boydii, Sh. dysenteriae, Sh. flexneri, Sh. sonnei), Vibrio cholerae, or V. parahaemolyticus.
- Oral norfloxacin is used in adults for the treatment of uncomplicated urinary tract infections (UTIs) (including cystitis) caused by susceptible Morganella morganii, Providencia rettgeri or Serratia marcescens.
Contra Indications of Norfloxacin
- Clostridium difficile infection
- Glucose-6-Phosphate Dehydrogenase (G6PD) Deficiency
- Low amount of potassium in the blood
- Acquired decrease of all cells in the blood
- Anemia
- Decreased Blood Platelets
- Deficiency of Granulocytes a Type of White Blood Cell
- Decreased white blood cells
- Psychotic disorder
- Lower Seizure Threshold
- Pseudotumor cerebri
- Peripheral pain, numbness, tingling, or weakness. সহজ বাংলা: স্নায়ুর ক্ষতি/সমস্যা।" data-rx-term="neuropathy" data-rx-definition="Neuropathy means nerve damage or irritation causing pain, numbness, tingling, or weakness. সহজ বাংলা: স্নায়ুর ক্ষতি/সমস্যা।">neuropathy
- Myasthenia Gravis
- Disease of Inadequate Blood Flow to the Heart Muscle
- Very Rapid Heartbeat – Torsades de Pointes
- prolonged QT interval on EKG
- Abnormal EKG with QT changes from Birth
- Severe Hardening of the Arteries in the Brain
- Severe renal impairment
- infection, or irritation, often causing pain, swelling, heat, or redness. সহজ বাংলা: শরীরের প্রদাহ; ব্যথা, ফোলা বা লালভাব হতে পারে।" data-rx-term="inflammation" data-rx-definition="Inflammation is the body’s response to injury, infection, or irritation, often causing pain, swelling, heat, or redness. সহজ বাংলা: শরীরের প্রদাহ; ব্যথা, ফোলা বা লালভাব হতে পারে।">Inflammation of the Tendon
- Rupture of a Tendon
- Hallucination
- Seizures
- Involuntary Quivering
- abnormal liver function tests
- High Pressure Within the Skull
- Anemia from Pyruvate Kinase and G6PD Deficiencies
- Lung Transplant
- Heart Transplant
- Allergies to Quinolones
Dosage of Norfloxacin
- Strengths: 400 mg
Cystitis
- 400 mg orally every 12 hours
Duration of Therapy
- Complicated urinary tract infections (UTIs):10 to 21 days
- Uncomplicated UTIs (cystitis) due to Escherichia coli, Klebsiella pneumoniae, or Proteus mirabilis: 3 days
- Uncomplicated UTIs due to other listed organisms: 7 to 10 days
Urinary Tract Infection
- 400 mg orally every 12 hours
Duration of Therapy
- Complicated urinary tract infections (UTIs):10 to 21 days
- Uncomplicated UTIs (cystitis) due to Escherichia coli, Klebsiella pneumoniae, or Proteus mirabilis: 3 days
- Uncomplicated UTIs due to other listed organisms: 7 to 10 days
Prostatitis
- 400 mg orally every 12 hours for 28 days
Gonococcal Infection
- 800 mg orally once
Pyelonephritis
Some experts recommend
- Mild infections: 400 mg orally every 12 hours for 14 days
Shigellosis
- Infectious Diseases Society of America (IDSA) recommendations: 400 mg orally twice a day
Duration of Therapy
- Immunocompetent patients: 3 days
- Immunocompromised patients: 7 to 10 days
Infectious Diarrhea
- Infectious Diseases Society of America (IDSA) recommendations: 400 mg orally twice a day
Duration of Therapy
- Immunocompetent patients: 3 days
- Immunocompromised patients: 7 to 10 days
Salmonella Enteric Fever
- IDSA recommendations: 400 mg orally twice a day
Duration of Therapy
- Immunocompetent patients: 5 to 7 days
- Immunocompromised patients: Up to 14 days (or longer if relapsing) may be required
Salmonella Gastroenteritis
- IDSA recommendations: 400 mg orally twice a day
Duration of Therapy
- Immunocompetent patients: 5 to 7 days
- Immunocompromised patients: Up to 14 days (or longer if relapsing) may be required
Traveler’s Diarrhea
- IDSA recommendations: 400 mg orally twice a day
- Duration of Therapy: 24 hours to 3 days
Traveler’s Diarrhea Prophylaxis
- IDSA recommendations: 400 mg orally once a day
Side Effects of Norfloxacin
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 Norfloxacin
Norfloxacin may interact with following drugs, supplements, & may change the efficacy of drugs
- antacids containing aluminum hydroxide, calcium, and magnesium hydroxide
- antihistamines (e.g., cetirizine, hydroxyzine, loratadine)
- antipsychotics (e.g. clozapine, haloperidol, olanzapine, quetiapine, risperidone)
- “azole” antifungals (e.g., itraconazole, ketoconazole, voriconazole)
- calcium supplements and multivitamins containing calcium
- inhaled corticosteroids
- oral corticosteroids (e.g., dexamethasone, hydrocortisone, prednisone)
- diabetes medications (e.g., metformin, nateglinide, rosiglitazone)
- formoterol
- iron supplements and multivitamins containing iron (do not take within 2 hours of levofloxacin)
- macrolide antibiotics (e.g., clarithromycin, erythromycin)
- magnesium supplements (e.g., magnesium hydroxide, magnesium oxide, magnesium sulfate)
- multivitamins
- nilotinib
- nonsteroidal anti-inflammatory medications (e.g., diclofenac, ibuprofen, ketoprofen, naproxen)
- other quinolone antibiotics (e.g., ciprofloxacin, , ofloxacin)
- selective serotonin reuptake inhibitors (SSRIs; e.g., citalopram, duloxetine, fluoxetine,paroxetine, sertraline)
- serotonin antagonists (e.g., granisetron, ondansetron)
- sotalol
- theophyllines (e.g., aminophylline, oxtriphylline, theophylline)
- trimethoprim
- tricyclic antidepressants (e.g., amitriptyline, clomipramine, desipramine, trimipramine)
- tyrosine kinase inhibitors (e.g., dasatinib, imatinib, nilotinib, sunitinib)
- vardenafil
- warfarin
Pregnancy and Lactation of Norfloxacin
FDA pregnancy Risk Rategory C
Pregnancy
This medication should not be used during pregnancy unless the benefits outweigh the risks. If you become pregnant while taking this medication, contact your doctor immediately.
Lactation
Norfloxacin may pass into breast milk. If you are a breast-feeding mother and are taking this medication, it may affect your baby. Talk to your doctor about whether you should continue breast-feeding. The safety and effectiveness of using this medication have not been established for children under 16 years of age.
References
- https://www.drugs.com/dosage/norfloxacin.html
- https://www.webmd.com/drugs/2/drug-11054/norfloxacin-oral/details/list-contraindications
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